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Triamcinolone Acetonide; Uses, Dosage, Side Effect, Interactions, Pregnancy

Triamcinolone is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. Upon cell entry, triamcinolone binds to and activates the glucocorticoid receptor, which leads to translocation of the ligand-receptor complex to the nucleus and induces expression of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both mediators of inflammation. In addition, pro-inflammatory cytokine production, including interleukin (IL)-1and IL-6, and the activation of cytotoxic T-lymphocytes is also inhibited. T-cells are prevented from making IL-2 and proliferating. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis through increasing Ikappa-B expression and curtailing activation of nuclear factor (NF)kappa-B.

A glucocorticoid was given, as the free alcohol or in esterified form, orally, intramuscularly, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated.

It is also known under the brand names Kenalog (topical) and Volon A as an injection, to treat allergies, arthritis, eye diseases, intestinal problems, and skin diseases. There are possible risks from an injection. It has been known to cause fat and muscle loss at an injection site, leaving a large divot bone deep.

Mechanism of Action of Triamcinolone

Triamcinolone and its derivatives are synthetic glucocorticoids that are used for their anti-inflammatory or immunosuppressive properties. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition of arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Firstly, however, these glucocorticoids bind to the glucocorticoid receptors which translocate into the nucleus and bind DNA (GRE) and change genetic expression both positively and negatively. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.

or

Glucocorticoids are capable of suppressing the inflammatory process through numerous pathways. They interact with specific intracellular receptor proteins in target tissues to alter the expression of corticosteroid-responsive genes. Glucocorticoid-specific receptors in the cell cytoplasm bind with steroid ligands to form hormone-receptor complexes that eventually translocate to the cell nucleus. There these complexes bind to specific DNA sequences and alter their expression. The complexes may induce the transcription of mRNA leading to the synthesis of new proteins. Such proteins include lipocortin, a protein known to inhibit PLA2a and thereby block the synthesis of prostaglandins, leukotrienes, and PAF. Glucocorticoids also inhibit the production of other mediators including AA metabolites such as COX, cytokines, the interleukins, adhesion molecules, and enzymes such as collagenase.
Corticosteroids diffuse across cell membranes and complex with specific cytoplasmic receptors. These complexes then enter the cell nucleus, bind to DNA (chromatin), and stimulate transcription of messenger RNA (mRNA) and subsequent protein synthesis of various inhibitory enzymes responsible for the anti-inflammatory effects of topical corticosteroids. These anti-inflammatory effects include inhibition of early processes such as edema, fibrin deposition, capillary dilatation, movement of phagocytes into the area, and phagocytic activities. Later processes, such as capillary production, collagen deposition, and keloid formation also are inhibited by corticosteroids. The overall actions of topical corticosteroids are catabolic.

Indications of Triamcinolone acetonide

Therapeutic Uses Triamcinolone

  • Triamcinolone acetonide is effective in the treatment of acute traumatic synovitis and capsulitis in horses with no deleterious side effects.
  • Triamcinolone is indicated as primary maintenance treatment in patients with persistent symptoms of chronic bronchial asthma. Treatment with inhaled corticosteroids is indicated in asthmatic patients whose conditions require anti-inflammatory treatment and in patients dependent on oral corticosteroids who may benefit from a gradual withdrawal from oral corticosteroids to decrease the likelihood of side effects.
  • Regular, continuous use of inhaled corticosteroids controls chronic airway inflammation, decreases airway hyperresponsiveness, prevents asthma symptoms, reduces the frequency of asthma exacerbations, and reduces hospital admissions for asthma. Clinical studies have also reported that regular use with inhaled corticosteroids is associated with decreased mortality. Inhaled corticosteroids are effective in all types of asthma and in patients of all ages.
  • Triamcinolone shares the actions of the other topical corticosteroids and is used for the relief of the inflammatory manifestations of corticosteroid-responsive dermatoses. The drug is also used as a paste for adjunctive treatment to provide temporary relief of symptoms associated with oral inflammatory or ulcerative lesions resulting from trauma.
  • Triamcinolone acetonide nasal inhalation aerosol and aqueous suspension are used for the symptomatic treatment of seasonal or perennial allergic rhinitis. In patients with seasonal or perennial allergic rhinitis, intranasal administration of triamcinolone acetonide generally provides symptomatic relief of rhinorrhea, nasal congestion, sneezing, and itching. In addition to relief of nasal symptoms, improvement of ophthalmic signs and symptoms (e.g., itching, lacrimation) has occurred in some patients, possibly secondary to systemic absorption of the drug. Since intranasal triamcinolone acetonide is thought to exert a local effect on the nasal mucosa, the mechanism of these ophthalmic effects is not fully understood. In patients with seasonal or perennial rhinitis, symptomatic relief usually is evident within several days of continuous intranasal triamcinolone acetonide therapy; however, about 1-2 weeks of continuous therapy may be required for optimum effectiveness in some patients. Onset of response occasionally occurs within 10-16 hours following initiation of intranasal triamcinolone acetonide suspension in patients with seasonal or perennial allergic rhinitis
  • Nasal corticosteroids are indicated in the treatment of seasonal or perennial allergic or (vasomotor nonallergic rhinitis NOT included in US package labeling). in patients who have exhibited significant side effects from, or have exhibited poor response to, other therapies, such as antihistamines and decongestants. Antihistamines and decongestants are generally considered primary therapies for these disorders. However, some clinicians consider nasal corticosteroids primary therapy for perennial or seasonal rhinitis because they are more effective if prophylaxis is started two to four weeks prior to exposure to allergens.
  • Age-related macular degeneration is now considered an important and leading cause of blindness among elderly patients in developed and developing countries. Age-related macular degeneration has two forms, dry and wet; both can lead to visual loss. However, the occurrence of the subfoveal choroidal neovascular membrane in the wet form results in severe visual impairment. Treatment options for choroidal neovascularization are available in order to maintain and in some cases improve vision. Photodynamic therapy has been used to treat both classic and occult membranes. It was known to cause choroidal hypoperfusion and production of vascular endothelial growth factor. Intravitreal steroid can possibly reduce the damage caused due to these undesirable effects. In the recent past, intravitreal injection of triamcinolone acetonide has been used extensively as an adjunct to photodynamic therapy in age-related macular degeneration in order to reduce the number of photodynamic therapy sessions and evaluate possible beneficial effects on vision.
  • Nasal corticosteroids are indicated in the treatment of allergic or inflammatory nasal conditions and nasal polyps.
  • Formulations of triamcinolone acetonide high potency gels and very high potency ointments also are used in the treatment of aphthous stomatitis. These agents also are used to treat other gingival disorders, such as desquamative gingivitis and oral lichen planus when the diagnosis has been confirmed by biopsy testing. Gel formulations of high potency corticosteroids and dental triamcinolone are used in the treatment of lichen planus of the mucous membranes.
  • Triamcinolone acetonide dental paste is indicated for the adjunctive treatment and temporary relief of symptoms associated with nonherpetic oral inflammatory and ulcerative lesions, including recurrent aphthous stomatitis
  • Triamcinolone is used to prevent recurrence of nasal polyps following their surgical removal and sufficient mucosal healing.
  • Indicated as adjunctive therapy during an acute episode or exacerbation /of rheumatic disorders. Local injections are preferred when only a few joints or areas are involved: ankylosing spondylitis, acute gouty arthritis, psoriatic arthritis, rheumatoid arthritis (including juvenile arthritis), post-traumatic osteoarthritis, synovitis of osteoarthritis,
  • Indicated in the treatment (and prophylaxis NOT included in US product labeling/) of respiratory disorders. Prophylactic uses include administration prior to or during extracorporeal circulation in heart surgery if the patient has a pre-existing pulmonary disorder, and administration prior to, during, and following oral, facial, or neck surgery to prevent edema that may threaten the airway: bronchial asthma, berylliosis, Loeffler’s syndrome (eosinophilic pneumonitis or hypereosinophilic syndrome), aspiration pneumonitis, symptomatic sarcoidosis, disseminated or fulminating pulmonary tuberculosis, and (chronic obstructive pulmonary disease (not controlled with theophylline and beta-adrenergic agonists), idiopathic pulmonary (Hamman-Rich syndrome) fibrosis, and status asthmaticus.
  • Triamcinolone is used in the treatment of trichinosis with neurological or myocardial involvement.
  • Triamcinolone is indicated concurrently with other immunosuppressants such as azathioprine or cyclosporine to reduce the risk of rejection of transplanted organs.
  • Indicated for treatment of oral lesions unresponsive to topical therapy. The presence of an oral herpetic lesion must be ruled out prior to initiation of triamcinolone therapy: desquamative gingivitis, recurrent aphthous stomatitis.
  • Indicated in the treatment of severe acute or chronic allergic and inflammatory ophthalmic conditions: chorioretinitis, diffuse posterior choroiditis, allergic conjunctivitis (not controlled topically), herpes zoster ophthalmicus, anterior segment inflammation, iridocyclitis, iritis, keratitis (not associated with herpes simplex or fungal infection), optic neuritis, sympathetic ophthalmia, corneal marginal allergic ulcers, diffuse posterior uveitis and (retrobulbar neuritis /NOT included in US product labeling).
  • Indicated during an acute episode or exacerbation (of nonrheumatic inflammatory disorders). Local injections are preferred when only a few joints or areas are involved: epicondylitis and acute nonspecific tenosynovitis.
  • Indicated for the treatment of hematologic disorders: acquired hemolytic anemia (autoimmune), congenital hypoplastic anemia (erythroid), red blood cell anemia (erythroblastopenia), secondary thrombocytopenia in adults, idiopathic thrombocytopenic purpura in adults and (hemolysis NOT included in US product labeling).
  • Indicated for the treatment of gastrointestinal disorders: ulcerative colitis, Crohn’s disease (Regional enteritis) when systemic therapy is required during a critical period of the disease. Long-term use is not recommended. Indicated for the treatment of dermatologic disorder: alopecia areata, atopic dermatitis, contact dermatitis, exfoliative dermatitis, bullous dermatitis herpetiformis, severe seborrheic dermatitis, severe inflammatory dermatoses, severe erythema multiforme (Stevens-Johnson syndrome), granuloma annulare, keloids, lichen planus, lichen simplex chronicus (neurodermatitis), discoid lupus erythematosus, mycosis fungoides, necrobiosis lipoidica diabeticorum, necrobiosis lipoidica, psoriatic plaques, severe psoriasis, pemphigus, (severe eczema, pemphigoid and localized cutaneous sarcoid
  • Indicated during an acute exacerbation or as maintenance therapy (for collagen disorders): acute rheumatic carditis, systemic lupus erythematosus, (relapsing polychondritis, mixed connective tissue disease, polyarteritis nodosa, relapsing polychondritis, and vasculitis.
  • Indicated for the treatment of severe or incapacitating allergic disorders intractable to adequate trials of conventional treatment: drug-induced allergic reactions, severe perennial or seasonal allergic rhinitis, and serum sickness.
  • Topical corticosteroids of low to medium potency are indicated in the treatment of corticosteroid-responsive dermatologic disorders mild to moderate atopic dermatitis; contact dermatitis; mild nummular dermatitis; seborrheic dermatitis (facial and intertriginous areas); other mild to moderate forms of dermatitis; other mild to moderate inflammatory dermatoses; intertrigo; lichen planus (facial and intertriginous areas); discoid lupus erythematosus (facial and intertriginous areas); polymorphous light eruption; anogenital pruritus; pruritus senilis; psoriasis (facial and intertriginous areas); xerosis (inflammatory phase. Occlusive dressings also may be required for chronic or severe cases of lichen simplex chronicus, psoriasis, eczema, atopic dermatitis, or chronic hand eczema. The more potent topical corticosteroids and or occlusive dressings may be required for conditions such as discoid lupus erythematosus, lichen planus, granuloma annulare, psoriatic plaques, and psoriasis affecting the palms, soles, elbows, or knees. Corticosteroids (topical);
  • Triamcinolone is indicated to relieve fever and inflammation from pericarditis.
  • Indicated for the treatment of endocrine disorders: acute adrenocortical insufficiency and chronic primary adrenocortical insufficiency (Addison’s disease), secondary adrenocortical insufficiency, congenital adrenal hyperplasia, Cushing’s syndrome (diagnosis), hypercalcemia associated with neoplasms, and nonsuppurative thyroiditis.

Contra-Indications of Triamcinolone acetonide

  • Extreme Loss of Body Water
  • The condition resulting from a defective immune system
  • Decreased Function of Bone Marrow
  • Low blood counts due to bone marrow failure
  • Defective Growth of Bone Marrow
  • Severe anemia
  • Severely Decreased Platelets
  • Decreased white blood cells
  • Alcoholism
  • Escape of Fluid into the Lungs
  • Interstitial Pneumonitis
  • Lung Fibrosis
  • Canker Sore
  • Ulcer from Stomach Acid
  • Ulcerated Colon
  • Hardening of the Liver caused by Alcohol
  • Hardening of the Liver
  • Excess Liver Fibrous Tissue
  • Severe liver disease
  • Kidney disease with the reduction in kidney function
  • Diarrhea
  • Ascites
  • Abnormal liver function tests
  • Pregnancy
  • A mother who is producing milk and breastfeeding
  • Allergies to Folic Acid Antagonist & Methotrexate Analogues

Dosage of Triamcinolone

Strengths: 1 mg; 2 mg; 8 mg; 40 mg

40 mg/mL; 10 mg/mL; 3 mg/mL; 75 mcg/inh;acetonide

Osteoarthritis

  • Intra-Articular (IA) Administration; may use 10 mg/mL or 40 mg/mL injectable suspension
  • Smaller joints: 2.5 to 5 mg (up to 10 mg)
  • Larger joints: 5 to 15 mg (up to 40 mg)
  • Maximum dose: For single injections into several joints, up to a total of 20 mg or more (using 10 mg/mL concentration) OR 80 mg (using 40 mg/mL concentration) have been used
  • Maximum frequency: Every 3 to 4 weeks; injection should be as infrequent as possible to avoid possible joint destruction

Extended-release: 32 mg/5 mL

  • For Osteoarthritic Knee Pain only: 32 mg as a single intra-articular injection

Ankylosing Spondylitis

Intra-Articular (IA) Administration

  • Smaller joints: 2.5 to 5 mg (up to 10 mg)
  • Larger joints: 5 to 15 mg (up to 40 mg)
  • Maximum dose: For single injections into several joints, up to a total of 20 mg or more (using 10 mg/mL concentration) OR 80 mg (using 40 mg/mL concentration) have been used
  • Maximum frequency: Every 3 to 4 weeks; injection should be as infrequent as possible to avoid possible joint destruction

Rheumatoid Arthritis

Intra-Articular (IA) Administration

  • Smaller joints: 2.5 to 5 mg (up to 10 mg)
  • Larger joints: 5 to 15 mg (up to 40 mg)
  • Maximum dose: For single injections into several joints, up to a total of 20 mg or more (using 10 mg/mL concentration) OR 80 mg (using 40 mg/mL concentration) have been used
  • Maximum frequency: Every 3 to 4 weeks; injection should be as infrequent as possible to avoid possible joint destruction

Psoriatic Arthritis

Intra-Articular (IA) Administration

  • Smaller joints: 2.5 to 5 mg (up to 10 mg)
  • Larger joints: 5 to 15 mg (up to 40 mg)
  • Maximum dose: For single injections into several joints, up to a total of 20 mg or more (using 10 mg/mL concentration) OR 80 mg (using 40 mg/mL concentration) have been used
  • Maximum frequency: Every 3 to 4 weeks; injection should be as infrequent as possible to avoid possible joint destruction

Gouty Arthritis

Intra-Articular (IA) Administration

  • Smaller joints: 2.5 to 5 mg (up to 10 mg)
  • Larger joints: 5 to 15 mg (up to 40 mg)
  • Maximum dose: For single injections into several joints, up to a total of 20 mg or more (using 10 mg/mL concentration) OR 80 mg (using 40 mg/mL concentration) have been used
  • Maximum frequency: Every 3 to 4 weeks; injection should be as infrequent as possible to avoid possible joint destruction.

Synovitis

Intra-Articular (IA) Administration

  • Smaller joints: 2.5 to 5 mg (up to 10 mg)
  • Larger joints: 5 to 15 mg (up to 40 mg)
  • Maximum dose: For single injections into several joints, up to a total of 20 mg or more (using 10 mg/mL concentration) OR 80 mg (using 40 mg/mL concentration) have been used

Multiple Sclerosis

  • 160 mg IM once a day for 1 week; then 64 mg IM every other day for 1 month

Bursitis

Intra-Articular (IA) Administration

  • Smaller joints: 2.5 to 5 mg (up to 10 mg)
  • Larger joints: 5 to 15 mg (up to 40 mg)
  • Maximum dose: For single injections into several joints, up to a total of 20 mg or more (using 10 mg/mL concentration) OR 80 mg (using 40 mg/mL concentration) have been used
  • Maximum frequency: Every 3 to 4 weeks; injection should be as infrequent as possible to avoid possible joint destruction

Anti-inflammatory

  • Initial dose: 60 mg IM deep into the gluteal muscle
  • Dose adjustments within the range of 40 to 80 mg are generally adequate
  • Dose ranges of 2.5 to 100 mg have been used; in certain overwhelming, acute, life-threatening situations, much higher doses may be used

Psoriasis

  • Use 10 mg/mL concentration only; multiple sites may be injected, separated by 1 cm or more
  • May repeat at weekly or less frequent intervals as necessary

Keloids

  • Use 10 mg/mL concentration only; multiple sites may be injected, separated by 1 cm or more
  • May repeat at weekly or less frequent intervals as necessary

Allergic Rhinitis

  • 40 to 100 mg IM once

Side Effects of Triamcinolone acetonide

The most common

Common

Rare

Drug Interactions of Triamcinolone

Triamcinolone may interact with following drugs, supplyments, & may change the efficacy of drugs

The above list is not the sufficient drugs interactions list, please always consult your doctor or pharmacist before taking this drug.

Pregnancy & Lactation of Triamcinolone

AU TGA pregnancy category: A
AU TGA pregnancy category: C (acetate suspension)
US FDA pregnancy category: C

Pregnancy

This drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. AU TGA pregnancy category: B3 US FDA pregnancy category: C Comments: Topical corticosteroids should not be used extensively on pregnant patients, in large amounts or for extended periods of time.

Lactation

Caution is recommended. Excreted into human milk: Unknown Excreted into animal milk: Data not available Comments: -The effects in the nursing infant are unknown. -Topical steroids should not be applied to the breasts prior to breastfeeding.

References

 

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Methylprednisolone, Uses, Dosage, Side Effect, Interactions, Pregnancy

Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone binds to and activates specific nuclear receptors, resulting in altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cell populations.

Methylprednisolone and its derivatives, methylprednisolone sodium succinate and methylprednisolone acetate, are synthetic glucocorticoids used as anti-inflammatory or immunosuppressive agents. They are synthetic (man-made) corticosteroids. Corticosteroids are naturally-occurring chemicals produced by the adrenal glands located adjacent to the kidneys.

Mechanism of Action of Methylprednisolone

Unbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Or

Glucocorticoids are capable of suppressing the inflammatory process through numerous pathways. They interact with specific intracellular receptor proteins in target tissues to alter the expression of corticosteroid-responsive genes. Glucocorticoid-specific receptors in the cell cytoplasm bind with steroid ligands to form hormone-receptor complexes that eventually translocate to the cell nucleus. There these complexes bind to specific DNA sequences and alter their expression. The complexes may induce the transcription of mRNA leading to synthesis of new proteins. Such proteins include lipocortin, a protein known to inhibit PLA2a and thereby block the synthesis of prostaglandins, leukotrienes, and PAF. Glucocorticoids also inhibit the production of other mediators including AA metabolites such as COX, cytokines, the interleukins, adhesion molecules, and enzymes such as collagenase.

Indications of Methylprednisolone

Therapeutic Indications

Dosage of Methylprednisolone

Allergic Rhinitis

Strengths: 80 to 120 mg IM

Alopecia

Alternatively, Methylprednisolone Dosepak

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Acetate suspension

  • Initial dose: 40 to 120 mg IM once a week for 1 to 4 weeks
  • For relief of acute severe dermatitis due to poison ivy: 80 to 120 mg IM; relief may occur within 8 to 12 hours
  • For relief of chronic contact dermatitis: 80 to 120 mg IM every 5 to 10 days
  • For relief of seborrheic dermatitis: 80 mg IM weekly to control condition
  • Initial dose: 20 to 60 mg injected into lesion; for larger lesions, 1 to 4 injections of 20 to 40 mg should be used to

Dermatologic Lesion

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, Methylprednisolon

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Acetate suspension

  • Initial dose: 40 to 120 mg IM once a week for 1 to 4 weeks
  • For relief of acute severe dermatitis due to poison ivy: 80 to 120 mg IM; relief may occur within 8 to 12 hours
  • For relief of chronic contact dermatitis: 80 to 120 mg IM every 5 to 10 days
  • For relief of seborrheic dermatitis: 80 mg IM weekly to control condition

Psoriasis

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, Methylprednisolone 

  • weight gain,
  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Acetate suspension

  • Initial dose: 40 to 120 mg IM once a week for 1 to 4 weeks

Dermatological Disorders

  • Initial dose: 4 to 48 mg orally once a day or in divided doses.

Alternatively, Methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Acetate suspension

  • Initial dose: 40 to 120 mg IM once a week for 1 to 4 week
  • For relief of acute severe dermatitis due to poison ivy: 80 to 120 mg IM; relief may occur within 8 to 12 hours
  • For relief of chronic contact dermatitis: 80 to 120 mg IM every 5 to 10 days
  • For relief of seborrheic dermatitis: 80 mg IM weekly to control condition
  • Initial dose: 20 to 60 mg injected into lesion; for larger lesions, 1 to 4 injections of 20 to 40 mg should be used to distribute dose.

Keloids

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, Methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Acetate suspension

  • Initial dose: 40 to 120 mg IM once a week for 1 to 4 weeks
  • For relief of acute severe dermatitis due to poison ivy: 80 to 120 mg IM; relief may occur within 8 to 12 hours
  • Initial dose: 20 to 60 mg injected into lesion; for larger lesions, 1 to 4 injections of 20 to 40 mg should be used to distribute dose.

Rheumatoid Arthritis

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

INTRA-ARTICULAR INJECTION Acetate suspension

  • General guidance: Actual doses may vary with severity of condition
  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
  • Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection

Acetate suspension

  • Initial dose: 40 mg IM every 2 weeks

Acute Gout

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Parenteral

  • Sodium succinate (IV or IM); in emergency situations, IV is preferres
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered
  • Alternatively, when oral therapy is not feasible, IM or IV administration may be substituted.
  • Acetate suspension (IM only): For prolonged systemic effect:
  • Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.

INTRA-ARTICULAR Administration

  • General guidance: Actual doses may vary with severity of condition
  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
  • Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
  • Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
  • For conditions of the tendinous or bursal structures: 4 to 30 mg
  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Parenteral

  • Sodium succinate (IV or IM); in emergency situations, IV is preferred
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered.
  • Alternatively, when oral therapy is not feasible, IM or IV administration may be substituted.

Acetate suspension (IM only): For prolonged systemic effect

  • Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.

INTRA-ARTICULAR Administration

  • General guidance: Actual doses may vary with severity of condition
  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
  • Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
  • Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
  • Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.

Bursitis

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Parenteral

  • Sodium succinate (IV or IM); in emergency situations, IV is preferred
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considere

Acetate suspension (IM only): For prolonged systemic effect

  • Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.

INTRA-ARTICULAR Administration

  • General guidance: Actual doses may vary with severity of condition
  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
  • Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection

SOFT TISSUE Administration

  • For conditions of the tendinous or bursal structures: 4 to 30 mg

Nephrotic Syndrome

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Parenteral

  • Sodium succinate (IV or IM); in emergency situations, IV is preferred
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered

Acetate suspension (IM only); For prolonged systemic effect

  • Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.

INTRA-ARTICULAR Administration

  • General guidance: Actual doses may vary with severity of condition
  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
  • Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
  • Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-
  • For conditions of the tendinous or bursal structures: 4 to 30 mg

Osteoarthritis

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Parenteral

  • weight gain,
  • Sodium succinate (IV or IM); in emergency situations, IV is preferred
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered

Acetate suspension (IM only): For prolonged systemic effect

  • Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.

INTRA-ARTICULAR Administration

  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
  • Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
  • Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
  • Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.

SOFT TISSUE Administration

  • For conditions of the tendinous or bursal structures: 4 to 30 mg

Tendonitis

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Parenteral

  • Sodium succinate (IV or IM); in emergency situations, IV is preferred
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered

INTRA-ARTICULAR Administration

  • General guidance: Actual doses may vary with severity of condition
  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
  • Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
  • Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
  • Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.

SOFT TISSUE Administration

  • For conditions of the tendinous or bursal structures: 4 to 30 mg

Neoplastic Diseases

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Parenteral

  • Sodium succinate (IV or IM); in emergency situations, IV is preferred
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered

Acetate suspension (IM only): For prolonged systemic effect

  • Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.

INTRA-ARTICULAR Administration

  • General guidance: Actual doses may vary with severity of condition
  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
  • Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
  • Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection

SOFT TISSUE Administration

  • For conditions of the tendinous or bursal structures: 4 to 30 mg

Epicondylitis

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Parenteral

  • Sodium succinate (IV or IM); in emergency situations, IV is preferred
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered

Acetate suspension (IM only): For prolonged systemic effect

  • Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.

INTRA-ARTICULAR Administration

  • General guidance: Actual doses may vary with severity of condition
  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injectio
  • Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.

SOFT TISSUE Administration

  • For conditions of the tendinous or bursal structures: 4 to 30 mg
  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Alternatively, methylprednisolone 

  • Day 1: 24 mg orally (8 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime
  • Day 2: 20 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 8 mg at bedtime)
  • Day 3: 16 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg after dinner; 4 mg at bedtime)
  • Day 4: 12 mg orally (4 mg before breakfast; 4 mg after lunch; 4 mg at bedtime)
  • Day 5: 8 mg orally (4 mg before breakfast; 4 mg at bedtime)
  • Day 6: 4 mg orally (4 mg before breakfast)

Parenteral

  • weight gain,
  • Sodium succinate (IV or IM); in emergency situations, IV is preferred
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally no more than 48 to 72 hours; after initial emergency period, a longer-acting injectable or oral preparation should be considered
  • Alternatively, when oral therapy is not feasible, IM or IV administration may be substituted.

Acetate suspension (IM only): For prolonged systemic effect

  • Initial dose: 4 to 120 mg IM; may repeat dose depending upon the degree of relief obtained from original injection.

INTRA-ARTICULAR Administration

  • General guidance: Actual doses may vary with severity of condition
  • Large joints (knee, angles, shoulders): 20 to 80 mg via intra-articular injection
  • Medium joints (elbows, wrists): 10 to 40 mg via intra-articular injection
  • Small joints (metacarpophalangeal, interphalangeal, sternoclavicular, acromioclavicular): 4 to 10 mg via intra-articular injection
  • Injections may be repeated every 1 to 5 or more weeks, depending upon the degree of relief obtained from the original injection.

SOFT TISSUE Administration

  • For conditions of the tendinous or bursal structures: 4 to 30 mg

Asthma 

  • Burst therapy: 32 to 64 mg orally once a day or in 2 divided doses until symptoms resolve and PEF (peak expiratory flow) is at least 80 percent of personal best

.Parenteral

  • Sodium succinate: IV administration may be used if rapid hormonal effect of maximum intensity is required.
  • High dose therapy: 30 mg/kg IV over at least 30 minutes every 4 to 6 hours until condition has stabilized, generally 48 to 72 hours; following initial emergency period, a longer-acting injectable or oral preparation should be considered
  • Alternatively, when oral therapy is not feasible, IM or IV administration may be substituted.

Acetate suspension: For prolonged systemic effect

  • 240 mg IM once (guideline dosing); 80 to 120 mg IM (manufacturer dosing)
  • Initial dose: 6 to 48 mg orally once a day or every other day
  • Maintenance dose: Gradually in small decrements at appropriate intervals decrease to the lowest dose that maintains an adequate clinical response.

Multiple Sclerosis

160 mg orally once a day for 1 week; then 64 mg orally every other day for 1 month

Nephrotic Syndrome

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Parenteral

  • Sodium succinate: IV or IM; in emergency situations, IV is preferred
  • Initial dose: 0.11 to 1.6 mg/kg/day (3.2 to 4.8 mg/m2/day) IM or IV divided in 3 or 4 doses (not less than 0.5 mg/kg/24 hours)
  • As a temporary substitute for oral therapy, administer oral daily dose IV or IM divided in 3 or 4 doses

Acetate suspension: For prolonged systemic effect; IM 

  • Initial dose: 0.11 to 1.6 mg/kg/day IM

Inflammatory

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Parenteral

  • Sodium succinate: IV or IM; in emergency situations, IV is preferred
  • Initial dose: 0.11 to 1.6 mg/kg/day (3.2 to 4.8 mg/m2/day) IM or IV divided in 3 or 4 doses (not less than 0.5 mg/kg/24 hours)
  • As a temporary substitute for oral therapy, administer oral daily dose IV or IM divided in 3 or 4 doses
  • Acetate suspension: For prolonged systemic effect; IM only
  • Initial dose: 0.11 to 1.6 mg/kg/day IM.

Pediatric Neoplastic Diseases

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Parenteral

  • Sodium succinate: IV or IM; in emergency situations, IV is preferred
  • Initial dose: 0.11 to 1.6 mg/kg/day (3.2 to 4.8 mg/m2/day) IM or IV divided in 3 or 4 doses (not less than 0.5 mg/kg/24 hours)
  • As a temporary substitute for oral therapy, administer oral daily dose IV or IM divided in 3 or 4 doses
  • Acetate suspension: For prolonged systemic effect; IM only
  • Initial dose: 0.11 to 1.6 mg/kg/day IM

Pediatric Asthma

0 to 11 years of age

Initial dose: 0.8 to 1.6 mg/kg oral or IV (succinate) once a day or in 2 divided doses until symptoms resolve and PEF (peak expiratory flow) is at least 80 percent of personal best

  • Therapy is usually required for 3 to 10 days but in some cases, may be longer
  • Maximum dose: 48 mg

12 years or older

  • Initial dose: 32 to 48 mg orally once a day or in 2 divided doses until symptoms resolve and PEF (peak expiratory

IM (acetate)

  • 0 to 4 years of age: 7.5 mg/kg IM once (guideline dosing) OR 80 to 120 mg IM (manufacturer dosing)
  • 5 years or older: 240 mg IM once (guideline dosing) OR 80 to 120 mg IM (manufacturer dosing)

Pediatric Juvenile Rheumatoid Arthritis

  • Initial dose: 4 to 48 mg orally once a day or in divided doses
  • Adjust or maintain initial dose until a satisfactory response is obtained; then, gradually in small decrements at appropriate intervals decrease to the lowest dose that maintains an adequate clinical response

Parenteral

  • SUCCINATE: May administer IM or IV
  • Initial dose: 0.11 to 1.6 mg/kg/day (3.2 to 4.8 mg/m2/day) IM or IV divided in 3 or 4 doses throughout the day
  • As a temporary substitute for oral therapy, administer oral daily dose IV or IM divided in 3 or 4 doses throughout the day

ACETATE suspension: IM administration only

  • Initial dose: 0.11 to 1.6 mg/kg IM once a day

Allergic Reaction

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Parenteral

  • When oral therapy is not feasible IV (succinate) or IM therapy (acetate or succinate) may be used.

Succinate

  • Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
  • Alternatively, 3.2 to 4.8 mg/m2/day
  • Initial dose: 0.11 to 1.6 mg/kg/day IM once a day

Pediatric Dose for Alopecia

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Parenteral

  • When oral therapy is not feasible IV (succinate) or IM therapy (acetate or succinate) may be used.
  • Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
  • Alternatively, 3.2 to 4.8 mg/m2/day
  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Parenteral

  • When oral therapy is not feasible IV (succinate) or IM therapy (acetate or succinate) may be used.
  • Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
  • Alternatively, 3.2 to 4.8 mg/m2/day

Pediatric Psoriasis

  • Initial dose: 4 to 48 mg orally once a day or in divided doses

Succinate

  • Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
  • Alternatively, 3.2 to 4.8 mg/m2/day
  • Initial dose: 0.11 to 1.6 mg/kg/day IM once a day

Dermatological Disorders

  • Initial dose: 4 to 48 mg orally once a day or in divided doses
  • When oral therapy is not feasible IV (succinate) or IM therapy (acetate or succinate) may be used.

Succinate

  • Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
  • Alternatively, 3.2 to 4.8 mg/m2/day
  • Initial dose: 0.11 to 1.6 mg/kg/day IM once a day

Allergic Urticaria

  • Initial dose: 4 to 48 mg orally once a day or in divided doses.

Succinate

  • Initial dose: 0.11 to 1.6 mg/kg/day IV or IM in 3 or 4 divided doses
  • Alternatively, 3.2 to 4.8 mg/m2/day
  • Initial dose: 0.11 to 1.6 mg/kg/day IM once a day

Side Effects of Methylprednisolone

The most common side effects

Common

Rare

Drug Interactions of Methylprednisolone

Methylprednisolone may interact with following drugs, supplyments, & may change the efficacy of drugs

The avobe list is not the sufficient drugs interactions list, please always consult your doctor or pharmacist before taking this drug.

Pregnancy & Lactation

Pregnancy

There are no adequate or well-controlled studies of the use of methylprednisolone in pregnant women. Complications, including cleft palate, stillbirth, and premature abortion, have been reported when corticosteroids were administered during pregnancy in animals. If these drugs must be used during pregnancy, the potential risks should be discussed with the patient. Babies born to women receiving large doses of corticosteroids during pregnancy should be monitored for signs of adrenal insufficiency, and appropriate therapy should be initiated, if necessary. Corticosteroids have been shown to impair fertility in male rats.

Lactation

A patient who was 6 weeks postpartum and predominantly breastfeeding her infant received 24 mg of depot methylprednisolone plus 15 mg of lidocaine intralesionally for tenosynovitis of the wrist. Thirty hours after the injection, lactation ceased. Her breasts were soft and not engorged at that time. Thirty-six hours later, lactation resumed slowly, reaching normal milk production 24 hours later. The author hypothesized that the suppression might have occurred because the injection was in a highly mobile joint, which might have caused rapid release of the corticosteroid.[9] Large doses of triamcinolone injected into the shoulder and into the wrist have also been reported to cause temporary drop or cessation of lactation.

References

methylprednisolone

By

Prednisolone, Indications, Dosage, Side Effect, Interactions, Pregnancy

Prednisolone is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, prednisolone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cells populations.

Prednisolone is a synthetic glucocorticoid used as the anti-inflammatory or immunosuppressive agent. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.  Prednisolone is indicated in the treatment of various conditions, including congenital adrenal hyperplasia, psoriatic arthritis, systemic lupus erythematosus.

Mechanism of Action of Prednisolone

Glucocorticoids such as Prednisolone can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The anti-inflammatory actions of glucocorticoids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Prednisolone reduces inflammatory reaction by limiting the capillary dilatation and permeability of the vascular structures. These compounds restrict the accumulation of polymorphonuclear leukocytes and macrophages and reduce the release of vasoactive kinins. Recent research suggests that corticosteroids may inhibit the release of arachidonic acid from phospholipids, thereby reducing the formation of prostaglandins. Prednisolone is a glucocorticoid receptor agonist. On binding, the corticoreceptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing an increase or decrease in expression of specific target genes, including suppression of IL2 (interleukin 2) expression.

Indications of Prednisolone

Therapeutic Indications Prednisolone

  • For the treatment of primary or secondary adrenocortical insufficiency, such as congenital adrenal hyperplasia, thyroiditis. Also used to treat psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis, bursitis, acute gouty arthritis and epicondylitis.
  • Also indicated for treatment of systemic lupus erythematosus, pemphigus and acute rhematic carditis. Can be used in the treatment of leukemias, lymphomas, thrombocytopenia purpura and autoimmune hemolytic anemia. Can be used to treat celiac disease, insulin resistance, ulcerative colitis and liver disorders.
  • Alleviation of inflammatory and clinical parameters associated with recurrent airway obstruction (RAO) in horses, in combination with environmental control.

Contra Indications of Prednisolone

  • Serious infections
  • Herpetic eye infections
  • Hypersensitivity to the Prednisolone
  • HBsAg-positive chronic active hepatitis
  • Two months before and fourteen days after prophylactic vaccination
  • Herpes simplex infection
  • Herpes zoster infection
  • Other viral infections
  • Hypersensitivity to prednisolone or any of the excipients
  • Systemic infections unless specific anti-infective therapy is employed.
  • Ocular herpes simplex because of possible perforation.

Prednisolone may be used only with extra precaution and only after the consultations with your doctor in the following situations:

  • Ulcers in the stomach and duodenum
  • Acute and chronic bacterial infections
  • Fungal infections affecting the skin and internal organs
  • Infections caused by parasites
  • Unstable hypertension
  • Osteoporosis
  • Neuropsychiatric disorders
  • Glaucoma
  • Diverticulitis
  • Cushing’s disease

Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Dosage of Prednisolone

Strengths: 5mg/5mL,10mg/5mL, 15mg/5mL, 20mg/5mL ,25mg/5mL suspension

Tablet : 5 mg, 10 mg ,15 mg, 30mg

Rheumatoid Arthritis

  • 5-7.5 mg PO qDay

Multiple Sclerosis

  • 200 mg/day PO for 1 week, then 80 mg PO every other day for 1 month

Acute Exacerbation of COPD 

  • 30-40 mg PO qDay for 10-14 days

Bells Palsy

  • 60 mg PO qDay for 5 days; then taper down by 10 mg daily for 5 days for total duration time of 10 days

Sarcoidosis

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Systemic Lupus Erythematosus

  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Ulcerative Colitis 

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses
  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Iritis

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Optic Neuritis

  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Gouty Arthritis

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Hemolytic Anemia

  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Immunosuppression

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Neoplastic Diseases

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Rheumatic Heart Disease

  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Adrenocortical Insufficiency

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Corneal Ulcers

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Keratitis

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Pemphigus

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Synovitis

  • Dosing should be individualized based on disease and patient response:
  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Thrombocythemia

  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Serum Sickness

  • Initial dose: 5 to 60 mg orally per day; may be give once a day or in divided doses

Nephrotic Syndrome

  • Initial episode: 1 mg/kg (up to 80 mg/day) orally once a day or 2 mg/kg (up to 120 mg) orally once every other day
  • Duration of therapy: 4 to 16 weeks

Pediatric 

Inflammation

  • 0.1-2 mg/kg/day PO in single daily dose or divided q6-12hr; not to exceed 80 mg/day 

Asthma

  • 1-2 mg/kg/day in single daily dose or divided q12hr for 3-5 days 

Nephrotic Syndrome

  • First 4 weeks: 60 mg/m²/day or 2 mg/kg/day PO divided q8hr until urine is protein free for 3 consecutive days; not to exceed 28 days; dose not to exceed 80 mg/day 
  • Subsequent 4 weeks: 40 mg/m² or 1-1.5 mg/kg PO every other day; not to exceed 80 mg/day
  • Maintenance in frequent relapses: 0.5-1 mg/kg/dose PO every other day for 3-6 months

Side Effects of Prednisolone

The most common

Common

Rare

Drug Interactions of Prednisolone

Prednisolone may interact with following drugs, supplements, & may change the efficacy of drugs

The above list is not the sufficient drugs interactions list, please always consult your doctor or pharmacist before taking this drug.

Pregnancy & Lactation of Prednisolone

FDA pregnancy category D

Pregnancy

Very little prednisolone acetate in an eye drop form is absorbed into the body and available to affect an unborn baby. For this reason, prednisolone acetate eye drops are considered safe to use during pregnancy for short periods of time. If you are concerned about using this medication, discuss the benefits and risks of using this medication with your doctor.

Lactation

Corticosteroids pass into breast milk, however in an eye drop form, very little prednisolone acetate is absorbed into the body and available to pass into breast milk. The use of corticosteroid eye drops, including prednisolone acetate, is considered to be safe while breastfeeding.

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By

Prednisone; Indications, Dosage, Side Effect, Interactions, Pregnancy

Prednisone is a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, prednisone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cell populations.

Prednisone is only found in individuals that have used or taken this drug. It is a synthetic anti-inflammatory glucocorticoid derived from cortisone. It is biologically inert and converted to prednisolone in the liver. [PubChem]Prednisone is a glucocorticoid receptor agonist. It is first metabolized in the liver to its active form, prednisolone.
Prednisolone crosses cell membranes and binds with high affinity to specific cytoplasmic receptors. The result includes inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. The anti-inflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Mechanism of Action of Prednisone

Prednisone is a glucocorticoid receptor agonist. It is first metabolized in the liver to its active form, prednisolone. Prednisolone crosses cell membranes and binds with high affinity to specific cytoplasmic receptors. The result includes inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. The anti-inflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Prednisone can stimulate secretion of various components of gastric juice. Suppression of the production of corticotropin may lead to suppression of endogenous corticosteroids. Prednisone has slight mineralocorticoid activity, whereby entry of sodium into cells and loss of intracellular potassium is stimulated. This is particularly evident in the kidney, where rapid ion exchange leads to sodium retention and hypertension.

Or

In physiologic doses, corticosteroids are administered to replace deficient endogenous hormones. In larger (pharmacologic) doses, glucocorticoids decrease inflammation by stabilizing leukocyte lysosomal membranes, preventing release of destructive acid hydrolases from leukocytes; inhibiting macrophage accumulation in inflamed areas; reducing leukocyte adhesion to capillary endothelium; reducing capillary wall permeability and edema formation; decreasing complement components; antagonizing histamine activity and release of kinin from substrates; reducing fibroblast proliferation, collagen deposition, and subsequent scar tissue formation; and possibly by other mechanisms as yet unknown. The drugs suppress the immune response by reducing activity and volume of the lymphatic system, producing lymphocytopenia, decreasing immunoglobulin and complement concentrations, decreasing passage of immune complexes through basement membranes, and possibly by the depressing reactivity of tissue to antigen-antibody interactions. Glucocorticoids stimulate erythroid cells of bone marrow, prolong survival time of erythrocytes and platelets, and produce neutrophilia and eosinopenia. Glucocorticoids promote gluconeogenesis, redistribution of fat from peripheral to central areas of the body, and protein catabolism, which results in negative nitrogen balance. They reduce intestinal absorption and increase renal excretion of calcium.

Indications of Prednisone

Most common or FDA approved uses are listed.

It also is used the treatment of

  • Leukemias
  • Lymphomas
  • Idiopathic thrombocytopenic purpura
  • Autoimmune hemolytic anemia
  • Bronchitis

FDA Approval: Indications of Prednisone

  • Prednisone is approved to be used to reduce inflammation and suppress (lower) the body’s immune response. It is used with other drugs to treat the following types of cancer: Acute lymphoblastic leukemia.
  • Chronic lymphocytic leukemia.
  • Hodgkin lymphoma.
  • Mycosis fungoides.
  • Non-Hodgkin lymphoma.
  • Prednisone is also used alone or with other drugs to prevent or treat the following conditions related to cancer: Anemia.
  • Drug hypersensitivity (allergic reactions).
  • Hypercalcemia (high blood levels of calcium).
  • Thrombocytopenia (low platelet levels).
  • Prednisone is also used alone or with other drugs to treat many other diseases and conditions. The drug continues to be studied in the treatment of many types of cancer and other conditions.

Therapeutic Indications of Prednisone

  • Prednisone is usually considered the oral glucocorticoid of choice for anti-inflammatory or immunosuppressant effects. Because it has only minimal mineralocorticoid properties, the drug is inadequate alone for the management of adrenocortical insufficiency. If prednisone is used in the treatment of this condition, concomitant therapy with a mineralocorticoid is also required.
  • Prednisone tablets and solutions are indicated in the following conditions: Endocrine Disorders: Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the first choice: synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy mineralocorticoid supplementation is of particular importance); congenital adrenal hyperplasia; hypercalcemia associated with cancer; nonsuppurative thyroiditis.
  • Prednisone tablets and solutions are indicated in the following conditions: Rheumatic Disorders: As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in: psoriatic arthritis, rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy), ankylosing spondylitis, acute and subacute bursitis, acute nonspecific tenosynovitis, acute gouty arthritis, post-traumatic osteoarthritis, synovitis of osteoarthritis, epicondylitis.
  • Prednisone tablets and solutions are indicated in the following conditions: Collagen Diseases: During an exacerbation or as maintenance therapy in selected cases of systemic lupus erythematosus, systemic dermatomyositis (polymyositis), acute rheumatic carditis.
  • Prednisone tablets and solutions are indicated in the following conditions: Dermatologic Diseases: Pemphigus; bullous dermatitis herpetiformis; severe erythema multiforme (Stevens-Johnson syndrome); exfoliative dermatitis; mycosis fungoides; severe psoriasis; severe seborrheic dermatitis.
  • Prednisone tablets and solutions are indicated in the following conditions: Allergic States: Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment: seasonal or perennial allergic rhinitis; bronchial asthma; contact dermatitis; atopic dermatitis; serum sickness; drug hypersensitivity reactions.
  • Prednisone tablets and solutions are indicated in the following conditions: Ophthalmic Diseases: Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as: allergic corneal marginal ulcers, herpes zoster ophthalmicus, anterior segment inflammation, diffuse posterior uveitis and choroiditis, sympathetic ophthalmia, allergic conjunctivitis, keratitis, chorioretinitis, optic neuritis, iritis and iridocyclitis.
  • Prednisone tablets and solutions are indicated in the following conditions: Respiratory Diseases: Symptomatic sarcoidosis; Loeffler’s syndrome not manageable by other means; berylliosis; fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy; aspiration pneumonitis.
  • Prednisone tablets and solutions are indicated in the following conditions: Hematologic Disorders: Idiopathic thrombocytopenic purpura in adults; secondary thrombocytopenia in adults; acquired (autoimmune) hemolytic anemia; erythroblastopenia (RBC anemia); congenital (erythroid) hypoplastic anemia.
  • Prednisone tablets and solutions are indicated in the following conditions: Neoplastic Diseases: For palliative management of leukemias and lymphomas in adults, acute leukemia of childhood.
  • Prednisone tablets and solutions are indicated in the following conditions: Edematous States: To induce a diuresis or remission of proteinuria in the nephrotic syndrome, without uremia, of the idiopathic type or that due to lupus erythematosus.
  • Prednisone tablets and solutions are indicated in the following conditions: Gastrointestinal Diseases: To tide the patient over a critical period of the disease in ulcerative colitis.
  • Prednisone tablets and solutions are indicated in the following conditions: Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculous chemotherapy; trichinosis with neurologic or myocardial involvement.
  • Systemic glucocorticoids have been used to reduce the pain, fever, and inflammation of pericarditis, including that associated with myocardial infarction.
  • Systemic conventional glucocorticoids (e.g., prednisone ) have been used in pediatric patients with mild esophageal or gastroduodenal Crohn’s disease. In addition, glucocorticoids (e.g., prednisone or methylprednisolone ) are recommended for the management of moderately to severely active Crohn’s disease, in children.
  • Glucocorticoids (e.g., prednisone) are used in the management of myasthenia gravis, usually in patients who have had an inadequate response to anticholinesterase therapy.
  • Glucocorticoid therapy has been used as an adjunct to anti-infective therapy in the treatment of anthrax in an attempt to ameliorate toxin-mediated effects associated with Bacillus anthracis infections. Some experts suggest that glucocorticoids may be indicated in the treatment of cutaneous anthrax if there are signs of systemic involvement or extensive edema involving the neck and thoracic region. Glucocorticoid therapy also has been used as an adjunct in the treatment of anthrax meningitis.

Contra-Indications of Prednisone

Depending on the indication and the general situation, peptic ulcers, osteoporosis, psychoses, infections, diabetes, and hypertension can represent contraindications.

  • Serious infections
  • Herpetic eye infections
  • Hypersensitivity to the Prednisone
  • HBsAg-positive chronic active hepatitis
  • Two months before and fourteen days after prophylactic vaccination
  • Herpes simplex infection
  • Herpes zoster infection
  • Other viral infections
  • Ulcers in the stomach and duodenum
  • Acute and chronic bacterial infections
  • Fungal infections affecting the skin and internal organs
  • Infections caused by parasites
  • Unstable hypertension
  • Osteoporosis
  • Neuropsychiatric disorders
  • Glaucoma
  • Diverticulitis
  • Cushing’s disease

Dosage of Prednisone

Strengths: 1 mg, 2.5 mg, 5 mg, 10 mg, 20 mg, 50 mg

Rheumatoid Arthritis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.

Gouty Arthritis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.

Psoriatic Arthritis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.

Ankylosing Spondylitis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Osteoarthritis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.

Psoriasis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.

Asthma 

  • Short-course “burst” therapy: 40 to 80 mg orally once a day or in 2 divided doses until peak expiratory flow (PEF) reaches 70% of predicted or personal best
  • For OUTPATIENT “burst” therapy: 40 to 60 mg orally once a day or in 2 divided doses for a total of 5 to 10 days

Aspiration Pneumonia

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained

Hemolytic Anemia

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Rheumatic Heart Disease

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Immunosuppression

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained

Ulcerative Colitis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained

Adrenocortical Insufficiencyency

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained

 Iritis

  • Initial dose: 5 to 60 mg orally per day

Allergic Reaction

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Bursitis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Synovitis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Dermatitis Herpetiformis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained.

Hypercalcemia of Malignancy

  • Initial dose: 5 to 60 mg orally per day

Thrombocytopenic Purpura

  • Initial dose: 5 to 60 mg orally per day

Pediatric 

Ankylosing Spondylitis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Pediatric Aspiration Pneumonia

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Bursitis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain initial dose until a satisfactory response is obtained;

Hypercalcemia of Malignancy

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Osteoarthritis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained

Psoriasis

  • Initial dose: 5 to 60 mg orally per day
  • Maintenance dose: Adjust or maintain the initial dose until a satisfactory response is obtained;

Side Effects of Prednisone

The most common

Common

Rare

Drug Interactions of Prednisone

Prednisone may interact with following drugs, supplements, & may change the efficacy of drugs

The above list is not the sufficient drugs interactions list, please always consult your doctor or pharmacist before taking this drug.

Pregnancy and Lactation of Prednisone

FDA pregnancy category: D 

Prednisone can cause intrauterine growth retardation and cleft palate, and its use during pregnancy is recommended only in situations where the benefits to the mother outweigh the risks to the fetus. Cases of hypoadrenalism (reduced levels of adrenaline in the blood) in newborns have been reported, but symptoms quickly go away without any complications. Cases of cataracts in newborns whose mothers took this drug during pregnancy have been reported.

Lactation and Breastmilk

Published information on the effects of prednisone on serum prolactin or on lactation in nursing mothers was not found as of the revision date. However, medium to large doses of depot corticosteroids injected into joints has been reported to cause temporary reduction of lactation.

  1. https://www.drugs.com/prednisone.html
  2. https://www.webmd.com/drugs/2/drug-6007-9383/prednisone-oral/prednisone-oral/details/list-contraindications
  3. https://pubchem.ncbi.nlm.nih.gov

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Eperisone HCl; Indications, Dosage, Side Effect, Interactions, Pregnancy

Eperisone is an antispasmodic drug which relaxes both skeletal muscles and vascular smooth muscles, and demonstrates a variety of effects such as reduction of myotonia, improvement of circulation, and suppression of the pain reflex. It is not approved for use in the United States, but is available in other countries like India, South Korea, and Bangladesh.

Eperisone is an antispasmodic drug which relaxes both skeletal muscles and vascular smooth muscles, and demonstrates a variety of effects such as reduction of myotonia, improvement of circulation, and suppression of the pain reflex.

Mechanisms of Action of Eperisone

Mechanisms of action of eperisone on isolated dog saphenous arteries and veins. Eperisonerelaxed saphenous arteries and veins previously contracted with norepinephrine, serotonin, acetylcholine, K+, or Ba2+; but in contrast, it produced contractions in the blood vessels contracted with prostaglandin (PG) F2 alpha.of eperisone on isolated dog saphenous arteries and veins.  Eperisonerelaxed saphenous arteries and veins previously contracted with norepinephrine, serotonin, acetylcholine, K+, or Ba2+; but in contrast, it produced contractions in the blood vessels contracted with prostaglandin (PG) F2 alpha.

Indications of Eperisone

Contra Indications of Eperisone

Eperisone is contraindicated in patients with known hypersensitivity to the drug.Side effects: ‘very rare’ excessive relaxation, stomachache, nausea, vertigo, anorexia, drowsiness, skin rashes, diarrhoea, vomiting, indigestion, GI disturbances, insomnia, headache, constipation etc.

Dosage of Eperisone

Strengths : 50 mg, 100 mg

Dosage‎: ‎Adult: PO 50 mg 3 times/day
Dose Single Dose Frequency Route Instructions

Adult Dosage

50 mg 50 (50) 8 hourly PO

Paedriatic Dosage (20kg)

Not recommended in this age group

Neonatal Dosage (3kg)

Not recommended in this age group

Side Effects of Eperisone

The most common

Rare

Weakness, dizziness, insomnia, drowsiness, numbness or trembling in the extremities, hepatic and renal dysfunction, haematological changes, skin rashes, itching, GI disturbances, urinary disorders, Rarely, shock.

Drug Interactions of Eperisone

Whenever you take more than one medicine, or mix it with certain foods or beverages, you’re at risk of a drug interaction.

Interaction with Alcohol

Consumption of alcohol can cause severe and potentially irreversible side effects on the liver when taken along with this medicine.

Instructions

You should avoid consuming alcohol while taking myonal 50 MG Tablet. Symptoms like fever, chills, rashes, joint pain and swelling, excessive weakness, nausea should be immediately reported to the doctor.

Interaction with Medicine

Other adverse reactions

5%>   ≥0.1% <0.1% Incidence unknown
Hepatic Elevation of AST

(GOT), ALT(GPT)

and Al-P, etc.

Renal Proteinuria and

Elevation of BUN etc.

 

Hematologic Anemia
Hypersensitivity Rash Pruritus erythema exudativum

multiforme

Psychoneurologic Sleepiness, insomnia,

headache and numbness

in the extremities

 

Stiffness and tremor

in the extremities

Gastrointestinal Nausea/vomiting,

anorexia, stomach discomfort,

abdominal pain, diarrhea,

constipation and thirst

Stomatitis and tremor

in the extremities

Urinary Urinary retention,

urinary incontinence and

the feeling of residual urine

Pregnancy & Lactation

  • Use During Pregnancy eperisone HCl should only be used in pregnant women or women suspected of being pregnant if the expected therapeutic benefits are evaluated to outweigh the possible risk of treatment. The safety of eperisone HCl in pregnant women has not been established.
  • Use During Lactation It is advisable to avoid the administration of eperisone HCl to nursing mothers. When eperisone HCl must be used, breast feeding should be discontinued during treatment.

 

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Tiemonium Methylsulfate, Indications/Uses, Side Effects, Interactions

Tiemonium Methylsulfate is a synthetic antispasmodic agent. Tiemonium strengthens calcium bonding with phospholipids and proteins thus stabilizing the cell membrane of the GI tract.Tiemonium Methylsulphate is a quarternary ammonium antimuscarinic agent with spasmolytic (antispasmodic) and parasympatholytic (anticholinergic) effects and is used in the relief of visceral spasms.

Indications of Tiemonium Methylsulfate

  • Visceral spasms
  • Tiemonium Methylsulphate may also be used for purposes
  •  It reduces muscle spasms of the intestine, biliary system, bladder and uterus.
  • pain in gastrointestinal and biliary diseases and
  •  urology and gynaecology
  • gastroenteritis,
  • diarrhoea,
  • dysentery,
  • biliary colic,
  • enterocolitis,
  • cholecystitis,
  •  colonopathies,
  • mild cystitis and
  • spasmodic dysmenorrhoea

Contra Indications of Tiemonium Methylsulfate

  • Tiemonium Methylsulphate is a quarternary ammonium antimuscarinic agent with spasmolytic (antispasmodic) and parasympatholytic (anticholinergic) effects and is used in the relief of visceral spasms.
  • angle closure glaucoma
  • urethro prostatic disorder

Dosage of Tiemonium Methylsulfate

Recommended oral dose of Tiemonium Methylsulphate tablet is 2-6 tablets (100-300 mg) daily in divided dosage as required. Xelcom 5 mg/2 ml Injection:

Recommended injectable dose is one or two Tiemonium Methylsulphate Injection three times daily, through Intravenous route slowly or Intramuscular route.

Side Effects of Tiemonium

  • Hypotension
  • Tachycardia
  • Tiemonium Methylsulphate may also cause side-effects

Pregnancy & Lactation

Before using Tiemonium Methylsulfate, inform your doctor about your current list of medications, over the counter products (e.g. vitamins, herbal supplements, etc.), allergies, pre-existing diseases, and current health conditions (e.g. pregnancy, upcoming surgery, etc.). Some health conditions may make you more susceptible to the side-effects of the drug. Take as directed by your doctor or follow the direction printed on the product insert. Dosage is based on your condition. Tell your doctor if your condition persists or worsens. Important counseling points are listed below.

References

Tiemonium Methylsulfate

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Dolasetron, Indications, Dosage, Side Effect, Interactions, Pregnancy

Dolasetron is an indole derivative and a potent serotonin 5-HT3 receptor antagonist with the anti-emetic property. Dolasetron blocks the activity of serotonin released from the enterochromaffin cells of the small intestine by selectively inhibiting and inactivating 5-HT3 receptors located on the nerve terminals of the vagus nerve in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. This results in suppression of signaling to trigger chemo- and radiotherapy-induced nausea and vomiting.

Dolasetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. This drug has not shown to have activity at other known serotonin receptors and has low affinity for dopamine receptors.

Dolasetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. This drug is not shown to have activity at other known serotonin receptors and has low affinity for dopamine receptors.

Mechanism of Action of Dolasetron

Dolasetron is a selective serotonin 5-HT3 receptor antagonist. In vivo, the drug is rapidly converted into its major active metabolite, hydrodolasetron, which seems to be largely responsible for the drug’s pharmacological activity. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. It is suggested that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.

Or

Dolasetron, and its active metabolite hydrodolasetron, are highly specific and selective antagonist of serotonin subtype 3 (5-HT3) receptors. 5-HT3 receptors are present peripherally on vagal nerve terminals and centrally in the area postrema of the brain. Chemotherapeutic medications appear to precipitate release of serotonin from the enterochromaffin cells of the small intestine, which activates 5-HT3 receptors on vagal afferents to initiate the vomiting reflex. Dolasetron has not been shown to have activity at other known serotonin receptors and has low affinity for dopamine receptors.

Indications of Dolasetron

Therapeutic Indications

  • Dolasetron injection is indicated for the prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including high-dose cisplatin. Dolasetrontablets are indicated for the prevention of nausea and vomiting associated with moderate-emetogenic cancer chemotherapy, including initial and repeat courses.
  • Dolasetron injection and tablets are indicated for the prevention of postoperative nausea and/or vomiting. Routine prophylaxis is not recommended when there is little risk of nausea and/or vomiting developing postoperatively, except in patients in whom nausea and/or vomiting must be avoided.
  • Dolasetron injection is indicated for the treatment of postoperative nausea and/or vomiting.
  • Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilation if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary. Monitor for shock and treat if necessary. Anticipate seizures and treat if necessary. For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport. Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool. Cover skin burns with dry sterile dressings after decontamination.
  • Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema. Consider administering a beta agonist such as albuterol for severe bronchospasm. Monitor cardiac rhythm and treat arrhythmias as necessary. Start IV administration of D5W /SRP: “To keep open”, minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer’s if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload. Treat seizures with diazepam or lorazepam. Use proparacaine hydrochloride to assist eye irrigation.
  • Immediate first aid: Ensure that adequate decontamination has been carried out. If the patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention

Contra-Indications of Dolasetron

Dosage of Dolasetron

Strengths: 50 mg; 100 mg, 20 mg/mL;

Postoperative Nausea/Vomiting 

Recommended dose: 12.5 mg IV approximately 15 minutes before the cessation of anesthesia or as soon as nausea and vomiting presents

2 to 16 years

  • Recommended dose: 0.35 mg/kg IV approximately 15 minutes before the cessation of anesthesia or as soon as nausea and vomiting presents
  • Maximum dose: 12.5 mg
  • Alternative dose: 1.2 mg/kg (of the IV injection solution) given orally within 2 hours before surgery, up to a maximum dose of 100 mg

Chemotherapy Induced Nausea/Vomiting 

2 to 16 years

  • Recommended dose: 1.8 mg/kg orally within 1 hour before chemotherapy
  • Maximum dose: 100 mg

Side Effects of Dolasetron

More common

Common

Rare

Drug Interactions of Dolasetron

Dolasetron may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Dolasetron

 FDA Pregnancy Risk Category B
Pregnancy

Dolasetron has been classified as FDA pregnancy risk category B. Animal studies have not revealed any teratogenic effects associated with dolasetron. There are no adequate and well-controlled studies in pregnant women. Because animal studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Other alternatives exist

Lactation

According to the manufacturer, it is not known whether dolasetron is excreted in human milk. However, because of its low molecular weight, transfer into breast milk should be expected. Caution should be exercised when administering dolasetron to a breastfeeding woman. Consider the benefits of breastfeeding

Dolasetron has been used in children age 2 to 16 years and has, overall, has been well tolerated. However, dolasetron should be used cautiously in pediatric patients who have preexisting or are at risk of developing, prolonged cardiac conduction intervals, particularly QTc.

References

  1. Dolasetron

 

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Granisetron; Indications, Dosage, Side Effect, Interactions, Pregnancy

Granisetron is an indazole derivative with antiemetic properties. As a selective serotonin receptor antagonist, granisetron competitively blocks the action of serotonin at 5-hydroxytryptamine3 (5-HT3) receptors, resulting in the suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.
Granisetron is a Serotonin-3 Receptor Antagonist. The mechanism of action of granisetron is as a Serotonin 3 Receptor Antagonist.

Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors

Mechanism of Action of Granisetron

Granisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zoneThe drug is structurally and pharmacologically related to ondansetron, another selective inhibitor of 5-HT3 receptors. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.

or

Granisetron is a potent, selective antagonist of 5-HT3 receptors. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors in turn inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone.

Indications of Granisetron

Contra Indications of Granisetron

Dosage of Granisetron

Strengths: 1 mg , 2 mg,10 mg ,40 mcg/kg, 2 mg/10 mL; 1 mg/mL  IV;

Nausea/Vomiting in Chemotherapy Induced

  • IV: 10 mcg/kg over 5 minutes, beginning 30 minutes before initiation of chemotherapy.
  • Orally: 2 mg, given up to 1 hour before chemotherapy, or 1 mg twice a day (the first dose is given up to 1 hour before chemotherapy, and the second dose is given 12 hours later).

Nausea/Vomiting in Postoperative

  • IV: 1 mg undiluted over 30 seconds, given before induction of anesthesia, or immediately before reversal of anesthesia; or give after surgery.

Nausea/Vomiting in Radiation Induced

  • slow or irregular heartbeat

2 mg orally given within 1 hour of radiotherapy.

Side Effects of Granisetron

The most common

Common

Rare

Drug Interactions of Granisetron

Granisetron may interact with following drugs, supplyments, & may change the efficacy of drugs

Pregnancy & Lactation of Granisetron

FDA Pregnancy Risk Category B
Pregnancy

There are no available data on the use of granisetron in pregnant women; however, animal studies have revealed no teratogenic effects. Granisetron injection, patch, and oral formulations are classified as FDA pregnancy risk category B. It is not known if granisetron crosses the placenta; however, due to its low molecular weight, passage across the placental barrier is expected.

Lactation

It is unknown whether granisetron or its metabolites are excreted in human milk. As a precautionary measure, breastfeeding should not be advised during treatment with Granisetron.


  1. References

    1. https://www.drugs.com/mtm/granisetron.html
    2. https://pubchem.ncbi.nlm.nih.gov

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Palonosetron, Indications, Dosage, Side Effect, Interactions, Pregnancy

Palonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is the most effective of the 5-HT3 antagonists in controlling delayed CINV nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy and is the only drug of its class approved for this use by the U.S. Food and Drug Administration. As of 2008, it is the most recent 5-HT3 antagonist to enter clinical uses

Mechanism of Action of Palonosetron

Palonosetron is a selective serotonin 5-HT3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors, in turn, inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. Alternative mechanisms appear to be primarily responsible for delayed nausea and vomiting induced by emetogenic chemotherapy, since similar temporal relationships between serotonin and emesis beyond the first day after a dose have not been established, and 5-HT3 receptor antagonists generally have not appeared to be effective alone in preventing or ameliorating delayed effects. It has been hypothesized that palonosetron’s potency and long plasma half-life may contribute to its observed efficacy in preventing delayed nausea and vomiting caused by moderately emetogenic cancer chemotherapy.

Indications of Palonosetron

  • Prophylaxis against postoperative nausea and vomiting
  • Delayed chemotherapy-induced nausea and vomiting
  • Prophylaxis of acute chemotherapy-induced nausea and vomiting
  • Highly emetogenic cancer chemotherapy
  • Palonosetron Hospira is indicated in adults for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy, the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron Hospira is indicated in pediatric patients 1 month of age and older for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy and prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron Accord is indicated in adults for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy, the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron Accord is indicated in pediatric patients 1 month of age and older for.
  • The prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy and prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron is indicated in adults for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy, the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.
  • Palonosetron is indicated in pediatric patients 1 month of age and older for the prevention of acute nausea and vomiting associated with highly emetogenic cancer chemotherapy and prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy.

Contra Indications of Palonosetron

Dosage of Palonosetron

Strengths: 0.25 mg/5 mL; 0.075 mg/1.5 mL

Chemotherapy Induce Nausea/Vomiting 

  • Oral: 0.5 mg orally administered approximately 1 hour prior to the start of chemotherapy
  • Parenteral: 0.25 mg IV as a single dose 30 minutes before the start of chemotherapy

 Postoperative Nausea/Vomiting 

  • Parenteral: 0.075 mg IV as a single dose immediately before induction of anesthesia

 Chemotherapy Induce Nausea/Vomiting – Pediatric

  • Parenteral: 20 mcg/kg IV (maximum 1.5 mg x 1) infused over 15 minutes beginning 30 minutes before the start of chemotherapy

Side Effects of Palonosetron

The most common

Common

Rare

Drug Interactions of Palonosetron

Palonosetron may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Palonosetron

 FDA pregnancy risk category B

Pregnancy

Palonosetron is listed in FDA pregnancy risk category B. Animal-based teratology studies have not revealed evidence of impaired fertility or harm to the fetus due to palonosetron. There are, however, no adequate and well-controlled studies in pregnant women. Animal reproduction studies are not always predictive of human response. The effects of palonosetron on labor and delivery are not known.

Lactation

It is not known if palonosetron is excreted in human milk. Many drugs are excreted in human milk and may increase the potential for serious adverse reactions in the breastfeeding infant. The manufacturer warns against the use of palonosetron in breast-feeding women due to the possible risks to the infant.


    1. https://pubchem.ncbi.nlm.nih.gov

    2. https://chealth.canoe.com/drug/getdrug/sporanox-capsules

 

palonosetron

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Ondansetron; Uses, Dosage, Side Effects, Interactions, Pregnancy

Ondansetron is a competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.

Ondansetron is a carbazole derivative with antiemetic activity. As a selective serotonin receptor antagonist, ondansetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.

 

Ondansetron is a well-tolerated drug with few side effects. A headache, constipation, and dizziness are the most commonly reported side effects associated with its use. There have been no significant drug interactions reported with this drug’s use. It is broken down by the hepatic cytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system; Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly to treat nausea and vomiting following chemotherapy. Its effects are thought to be on both peripheral and central nerves. One part is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata, the other is a blockage of serotonin receptors in the chemoreceptor trigger zone. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors; A competitive serotonin types 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties; Ondansetron (INN) is a serotonin 5-HT3 receptor antagonist used mainly to treat nausea and vomiting following chemotherapy. Its effects are thought to be on both peripheral and central nerves. One part is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata, the other is a blockage of serotonin receptors in the chemoreceptor trigger zone. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.

Mechanism of Action of Ondansetron

Ondansetron is a selective serotonin 5-HT3 receptor antagonist. The antiemetic activity of the drug is brought about through the inhibition of 5-HT3 receptors present both centrally (medullary chemoreceptor zone) and peripherally (GI tract). This inhibition of 5-HT3 receptors, in turn, inhibits the visceral afferent stimulation of the vomiting center, likely indirectly at the level of the area postrema, as well as through direct inhibition of serotonin activity within the area postrema and the chemoreceptor trigger zone. Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist, not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serontonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. The temporal relationship between the emetogenic action of emetogenic drugs and the release of serotonin, as well as the efficacy of antiemetic agents, suggest that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.

Indications of Ondansetron

For the prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, postoperation, and radiation. Also used for the treatment of postoperative nausea and vomiting.

Therapeutic Indications of Ondansetron

Contra Indications of Ondansetron

Dosage of Ondansetron

Strengths: 4 mg, 8 mg, 16 mg ,32 mg,  4 mg/5 mL; 32 mg/50 mL-D5%; 2 mg/mL;

Chemotherapy Induced Nausea/Vomiting 

Highly Emetogenic Cancer Chemotherapy (HEC)

  • Recommended dose: 24 mg orally 30 minutes before the start of single-day HEC (including cisplatin doses of 50 mg/m2 or greater)

Moderately Emetogenic Cancer Chemotherapy (MEC)

  • Recommended dose: 8 mg orally twice a day, with the first dose administered 30 minutes before the start of chemotherapy and the subsequent dose 8 hours later; then 8 mg orally 2 times a day (every 12 hours) for 1 to 2 days after the completion of chemotherapy

Parenteral

  • Recommended dose: 0.15 mg/kg IV, with the first dose (infused over 15 minutes) 30 minutes before the start of emetogenic chemotherapy and subsequent doses given 4 and 8 hours after the first dose.
  • Maximum dose: 16 mg per dose

Nausea/Vomiting

Highly Emetogenic Cancer Chemotherapy (HEC)

  • Recommended dose: 24 mg orally 30 minutes before the start of single-day HEC (including cisplatin doses of 50 mg/m2 or greater)

Moderately Emetogenic Cancer Chemotherapy (MEC)

  • Recommended dose: 8 mg orally twice a day, with the first dose administered 30 minutes before the start of chemotherapy and the subsequent dose 8 hours later; then 8 mg orally 2 times a day (every 12 hours) for 1 to 2 days after the completion of chemotherapy

Parenteral

  • Recommended dose: 0.15 mg/kg IV, with the first dose (infused over 15 minutes) 30 minutes before the start of emetogenic chemotherapy and subsequent doses given 4 and 8 hours after the first dose.
  • Maximum dose: 16 mg per dose

Postoperative Nausea/Vomiting 

  • Recommended dose: 16 mg orally 1 hour before the induction of anesthesia

Parenteral

  • Recommended dose: 4 mg IV (undiluted) immediately before induction of anesthesia or postoperatively (nausea and/or vomiting within 2 hours after surgery)
  • Alternative route: 4 mg IM (undiluted)

Radiation Induced Nausea/Vomiting

  • Recommended dose: 8 mg orally 3 times a day
  • Total Body Irradiation: 8 mg orally 1 to 2 hours before each fraction of radiotherapy administered each day
  • Single High-dose Fraction Radiotherapy to the Abdomen: 8 mg orally 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for 1 to 2 days after the completion of radiotherapy
  • Daily Fractionated Radiotherapy to the Abdomen: 8 mg orally 1 to 2 hours before radiotherapy, with subsequent doses every 8 hours after the first dose for each day radiotherapy is given

Pediatric

Chemotherapy Induced Nausea/Vomiting 

4 to 11 years

  • Recommended dose: 4 mg orally 3 times a day, with the first dose administered 30 minutes before the start of chemotherapy, and subsequent doses 4 and 8 hours after the first dose; then 4 mg orally 3 times a day (every 8 hours) for 1 to 2 days after the completion of chemotherapy

12 years and older

  • Recommended dose: 8 mg orally twice a day, with the first dose administered 30 minutes before the start of chemotherapy and the subsequent dose 8 hours later; then 8 mg orally 2 times a day (every 12 hours) for 1 to 2 days after the completion of chemotherapy

Parenteral, 6 months to 18 years

  • Recommended dose: 0.15 mg/kg IV, with the first dose (infused over 15 minutes) 30 minutes before the start of emetogenic chemotherapy, and subsequent doses given 4 and 8 hours after the first dose
  • Maximum dose: 16 mg (per dose)

Chemotherapy Induced Nausea/Vomiting 

4 to 11 years

  • Recommended dose: 4 mg orally 3 times a day, with the first dose administered 30 minutes before the start of chemotherapy, and subsequent doses 4 and 8 hours after the first dose; then 4 mg orally 3 times a day (every 8 hours) for 1 to 2 days after the completion of chemotherapy

12 years and older

  • Recommended dose: 8 mg orally twice a day, with the first dose administered 30 minutes before the start of chemotherapy and the subsequent dose 8 hours later; then 8 mg orally 2 times a day (every 12 hours) for 1 to 2 days after the completion of chemotherapy

Parenteral, 6 months to 18 years

  • Recommended dose: 0.15 mg/kg IV, with the first dose (infused over 15 minutes) 30 minutes before the start of emetogenic chemotherapy, and subsequent doses given 4 and 8 hours after the first dose
  • Maximum dose: 16 mg (per dose)

Or

Children
  • < 4 years: 0.15 mg/kg/dose IV (Max: 16 mg/dose). Safety and efficacy have not been established for PO formulation
  • 4—11 years: 0.15 mg/kg/dose IV (Max: 16 mg/dose). 12 mg/day PO.
  • >= 12 years: 0.15 mg/kg/dose IV (Max: 16 mg/dose). 16 mg/day PO.
Infants
  • 1—5 months: 0.1 mg/kg IV (single dose). Safety and efficacy have not been established for PO formulation.
  • >= 6 months: 0.15 mg/kg/dose IV (Max: 16 mg/dose IV). Safety and efficacy have not been established for PO formulation.

Neonates

  • Safety and efficacy have not been established.

Side Effects of Ondansetron

The most common

Common

Rare

Drug Interactions of Ondansetron

Ondansetron may interact with following drugs, supplyments, & may change the efficacy of drugs

Pregnancy & Lactation Ondansetron

FDA Pregnancy Category B

Pregnancy

The safety of ondansetron for se in human pregnancy has not been established. Evaluation of experimental animal studies does not indicate direct or indirect harmful effects with respect to the development of the embryo, or fetus, the course of gestation and peri- and post-natal development. However, as animal studies are not always predictive of human response the use of ondansetron in pregnancy is not recommended.

Lactation

Tests have shown that ondansetron passes into the milk of lactating animals. It is therefore recommended that mothers receiving Zofran should not breast-feed their babies. There is no information on the effects of ondansetron on human fertility.

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Domperidone; Indications, Dosage, Side Effects, Interactions ,Pregnancy

Domperidone is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.

Domperidone is a peripheral-specific antagonist of the dopamine receptor D2 (D2R), with antiemetic, gastrokinetic and galactagogue activities. Following administration, domperidone binds to D2R expressed by peripheral neurons; this inhibits dopamine binding and D2R-mediated signaling. Inhibition of peripheral D2R signaling prevents or relieves various gastrointestinal (GI) symptoms, such as nausea and vomiting, and may help relief reflux and symptoms of a variety of other upper GI disorders.

Domperidone is only found in individuals that have used or taken this drug. It is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which – among others – regulates nausea and vomiting

Mechanism of Action of Domperidone

Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which – among others – regulates nausea and vomiting

Indications of Domperidone

Therapeutic Indications of Domperidone [FDA Level]

Contra indications of Domperidone

  • Triazole antifungal medications such as ketoconazole, itraconazole, fluconazole.
  • Macrolide antibiotics such as erythromycin and clarithromycin.
  • Grapefruit juice.
  • QT-prolonging drugs like amiodarone.
  • Prolactin secreting pituitary tumor (prolactinoma) or hyperprolactinemia.
  • Mechanical bowel disorders such as bowel obstruction, gastrointestinal haemorrhage or bowel perforation
  • Moderate hepatic impairment (liver disease).
  • Severe renal impairment (kidney disease).
  • Cardiac disease.

Dosage of Domperidone

Strengths: 10 mg ,

 Nausea, and vomiting /gastrointestinal abnormality

  • The usual dose for the treatment is 1 to 2 tablets taken 3 to 4 times a day before meals. Do not take more than 8 tablets (80mg) in 24 hours.

Infants and Children

  • Children weighing less than 35kg (5 stone) should not take these tablets. The usual dose for the treatment is 0.25 0.5mg per kg bodyweight taken 3 to 4 times a day before meals. Your pharmacist may be able to help you if you are not sure.

Side Effects of Domperidone

Most common 

Common

Rare

Drug Interactions of Domperidone

Domperidone may interact with following drugs, supplyments, & may change the efficacy of drugs

Pregnancy & Lactation of Domperidone

FDA  Pregnancy Category C 

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.

Breastfeeding

This medication passes into breast milk. If you are a breastfeeding mother and are taking domperidone, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding. The safety and effectiveness of using this medication have not been established for children.


  1. References

    1. https://pubchem.ncbi.nlm.nih.gov

 

Domperidone

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Loperamide, Indications, Dosage, Side Effects, Interactions, Pregnancy

Loperamide is a synthetic agent chemically related to the opiates with anti-diarrheal properties. Loperamide decreases gastrointestinal motility by effects on the circular and longitudinal muscles of the intestine. Part of its anti-diarrheal effect may be due to a reduction of gastrointestinal secretion produced by opioid receptor binding in the intestinal mucosa.

One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.

Loperamide is a medication used to decrease the frequency of diarrhea. It is often used for this purpose in gastroenteritis, inflammatory bowel disease, and short bowel syndrome. It is not recommended for those with blood in the stool. The medication is taken by mouth

Mechanism of Action of Loperamide 

Loperamide interferes with peristalsis by a direct action on the circular and longitudinal muscles of the intestinal wall to slow motility. Loperamide also may directly inhibit fluid and electrolyte secretion and/or increase water absorption. By increasing the transit time of the intestinal contents, loperamide reduces fecal volume, increases the bulk density and the viscosity of the feces, and decreases the loss of electrolytes and fluids from the body. Although loperamide is chemically related to opioids, it does not exhibit analgesic or opiate-like effects, even at high doses. Tolerance to the antidiarrheal effect of loperamide has not been observed, and it does not appear to produce physical dependence.

Or

The present study investigates the mechanism of the central analgesic effect of loperamide. Adult male Sprague-Dawley rats were subjected to surgery for catheter placement. Following baseline testing, different groups of rats were administered fixed intrathecal doses (1 ug, 3 ugs, 10 ug, and 30 ugs) of loperamide and morphine. Analgesia was compared employing Hargreaves paw withdrawal apparatus at 15 min, 30 min, 60 min, 90 min, and 120 min. Additionally, CTOP, a specific mu-opioid receptor antagonist was co-administered with loperamide to examine the mu-opioid receptor-mediated loperamide analgesia. Furthermore, nefiracetam, a calcium channel opener, was co-administered with loperamide or morphine to evaluate the involvement of Ca(2+) channels in loperamide showed an analgesic effect which was comparable to morphine. However, loperamide produced longer analgesia and the analgesic effect was significantly better at 42 hr and 49 hr compared to morphine. CTOP completely reversed loperamide analgesia. Though nefiracetam significantly reversed loperamide analgesia, it did not have any effect on morphine-induced analgesia. Our findings suggest that loperamide administered intrathecally produces analgesia which is mediated through the mu-opioid receptor and subsequent blockade of downstream calcium channels.

Indications of Loperamide 

Therapeutic Indications of Loperamide 

  • Antidiarrheals
  • Loperamide is used in the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease.
  • The fixed combination containing loperamide and simethicone is used for the control and symptomatic relief of diarrhea when relief of flatulence, bloating, and gas pain also is indicated.
  • Loperamide has also been effective in controlling chronic functional (idiopathic) diarrhea and chronic diarrhea caused by bowel resection or organic lesions.
  • Many physicians are resistant to the idea of prescribing loperamide for acute infectious traveler’s diarrhea and community-acquired diarrhea because of the fear of possible adverse effects.
  • Large randomized trials with loperamide, either alone or as an adjunct to antibiotic treatment, have in fact revealed positive rather than negative effects. International guidelines now often support the use of loperamide for the treatment of infectious diarrhea without dysentery.
  • There seems to be no reason to systematically avoid loperamide in patients with dysentery, but caution is advised.
  •  Loperamide can be used as monotherapy or as an adjunct to antibiotic treatment in immunocompetent adults with acute infectious traveler’s diarrhea or community-acquired diarrhea without severe comorbidities. This can reduce both the frequency of diarrhea and the time until diarrhea stops without the risk of severe complications.

Contra-Indications of Loperamide 

  • Loperamide HCl is contraindicated in patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients.
  • Loperamide HCl is contraindicated in patients with abdominal pain in the absence of diarrhea.
  • Loperamide HCl is not recommended in infants below 24 months of age.
  • Loperamide HCl should not be used as the primary therapy – In patients with acute dysentery, which is characterized by blood in stools and high fever, in patients with acute ulcerative colitis,in patients with bacterial enterocolitis caused by invasive organisms including Salmonella, Shigella, and Campylobacter,in patients with pseudomembranous colitis associated with the use of broad-spectrum antibiotics.

Dosage of Loperamide 

Strengths: 2 mg; 1 mg/5 mL; 1 mg/7.5 mL

Diarrhea

Tablets, capsules, and liquid

  • Initial: 4 mg orally after the first loose stool, then
  • Maintenance: 2 mg after each loose stool, not to exceed 16 mg in any 24-hour period. Clinical improvement is usually observed within 48 hours.

Chewable tablets

  • Initial: 4 mg after the first loose stool, then
  • Maintenance: 2 mg after each subsequent loose stool, but not exceeding 8 mg in 24 hours.

Diarrhea, Chronic

Tablets, capsules, and liquid

  • Initial: 4 mg orally once followed by 2 mg orally after each loose stool, not to exceed 16 mg in any 24-hour period.
  • Maintenance: The average daily maintenance dosage is 4 to 8 mg. Clinical improvement is usually observed within 10 days. If clinical improvement is not observed at a maximum dosage of 16 mg for a duration of 10 days, symptoms are unlikely to be controlled by further administration.

Pediatric Diarrhea, Acute

2 to 6 years (13 to 20 kg)

  • Liquid formulation only to be used in this age group.
  • Initial: 1 mg orally 3 times a day for the first day, then
  • Maintenance: 0.1 mg/kg/dose after each loose stool, but not exceeding the initial dose.

6 to 8 years (20 to 30 kg) Tablets, capsules, and liquid

  • Initial: 2 mg orally twice a day for the first day, then
  • Maintenance: 0.1 mg/kg/dose after each loose stool, but not exceeding the initial dose.

Chewable tablets

  • Initial: 2 mg orally after the first loose stool, then
  • Maintenance: 1 mg orally after each subsequent loose stool, but not exceeding 4 mg in 24 hours.

8 to 12 years (greater than 30 kg) Tablets, capsules, and liquid

  • Initial: 2 mg orally 3 times a day for the first day, then
  • Maintenance: 0.1 mg/kg/dose after each loose stool, but not exceeding initial dose.

Chewable tablets

  • Initial: 2 mg orally after the first loose stool, then
  • Maintenance: 1 mg orally after each subsequent loose stool, but not exceeding 6 mg in 24 hours.

12 to 18 years

  • Tablets, chewable tablets, capsules, and liquid:
  • Initial: 4 mg after the first loose stool, then
  • Maintenance: 2 mg after each subsequent loose stool, but not exceeding 8 mg in 24 hours.

Pediatric Diarrhea, Chronic

less than 2 years

  • The therapeutic dose for the treatment of chronic diarrhea has not been established for this patient population.

Side Effects of Loperamide 

The most common side effects 

Common

Rare

Drug Interactions of Loperamide 

Loperamide may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Loperamide 

FDA Pregnancy Category C

Pregnancy

Teratology studies have been performed in rats using oral doses of 2.5, 10, and 40 mg/kg/day, and in rabbits using oral doses of 5, 20, and 40 mg/kg/day. These studies have revealed no evidence of impaired fertility or harm to the fetus at doses up to 10 mg/kg/day in rats (5 times the human dose based on body surface area comparison) and 40 mg/kg/day in rabbits.

Lactation

While manufacturers do not recommend loperamide use during lactation; the American Academy of Pediatrics generally considers the use of loperamide compatible with breastfeeding as use during lactation is unlikely to adversely affect the infant. Small amounts of loperamide may appear in human breast milk, based on data of the excretion of loperamide in human breast milk at low levels following the use of a prodrug, loperamide oxide. As with all medications, women should consult their healthcare professional prior to self-treatment during lactation.


  1. References

    1. https://www.webmd.com/drugs/2/drug-4789-3025/loperamide-oral/loperamide-liquid-oral/details/list-contraindications
    2. https://pubchem.ncbi.nlm.nih.gov

 

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