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
- Rheumatoid arthritis; including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy)
- Ankylosing spondylitis
- Psoriatic arthritis
- Asthma
- Inflammatory Conditions
- Bronchopulmonary Dysplasia
- Dermatitis
- Immunosuppression
- Multiple Sclerosis
- Nephrotic Syndrome
- Acne Vulgaris
- Acute Exacerbation of Chronic Obstructive Pulmonary Disease
- Acute Gouty Arthritis
- Acute Lymphoblastic Leukaemias
- Aggressive Lymphoma
- Allergic Rhinitis
- Allergic corneal marginal ulcers
- Ankylosing Spondylitis
- Aspergillosis, Allergic Bronchopulmonary
- Aspiration Pneumonitis
- Asthma Bronchial
- Atopic Dermatitis
- Bell’s Palsy
- Congenital Adrenal Hyperplasia
- Congenital Hypoplastic Anemia
- Conjunctivitis, Seasonal Allergic
- Corneal Inflammation
- Crohn’s Disease
- Dermatitis
- Dermatomyositis
- Drug hypersensitivity reaction
- Edema of the cerebrum
- Epicondylitis
- Erythroblastopenia
- Giant Cells Arteritis
- Graves Ophthalmopathy
- Hepatitis, Autoimmune
- Hypercalcemia of Malignancy
- Hypersensitivity Pneumonitis
- Idiopathic Thrombocytopenic Purpura
- Iridocyclitis
- Iritis
- Leukaemia
- Loeffler’s syndrome
- Malignant Lymphomas
- Metastatic Castration Resistant Prostate Cancer
- Multiple sclerosis exacerbation
- Mycosis Fungoides
- Ophthalmia, Sympathetic
- Optic Neuritis
- Pain caused by Herpes zoster
- Pericarditis
- Polymyalgia Rheumatica
- Primary adrenocortical insufficiency
- Proteinuria
- Pulmonary Fibrosis
- Pure Red Cell Aplasia
- Relapsing Polychondritis
- Secondary adrenocortical insufficiency
- Secondary thrombocytopenia
- Serum Sickness
- Severe Seborrheic Dermatitis
- Sjögren’s Syndrome
- Stevens Johnson Syndrome
- Systemic Lupus Erythematosus
- Tuberculosis
- Tuberculous Meningitis
- Ulcerative Colitis
- Uveitis
- Vasculitis
- Acquired immune hemolytic anemia
- Acute Tenosynovitis
- Bronchiolitis obliterans organizing pneumonia
- Diffuse posterior uveitis
- Exfoliative erythroderma
- Idiopathic eosinophilic pneumonias
- Non-suppurative Thyroiditis
- Ocular inflammatory conditions
- Severe Psoriasis
- Subacute Bursitis
- Symptomatic Sarcoidosis
- Synovitis of osteoarthritis
- Systemic Dermatomyositis
- Varicella-zoster virus acute retinal necrosis
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
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
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
- Fluid retention
- Weight gain,
- Mouth sores,
- Drying of the skin
- Change in skin color
- Diarrhea
- Any signs of infection, or a skin rash.
- Stomach pain, especially if it comes along with fever and diarrhea or constipation
- Yellowing of the skin or eyes
- Loss of appetite
- Constipation
- Sleepiness or unusual drowsiness
- Clumsiness or unsteadiness
- Dizziness
- Drowsiness
- Dry mouth
- false sense of well-being
- increased watering of mouth
- lightheadedness
- constipation;
- vision changes;
- breast swelling (in men or women); or
- decreased sex drive, impotence, or difficulty having an orgasm.
- blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
- restless muscle movements in your eyes, tongue, jaw, or neck;
Common
- Drowsiness and lightheadedness the day after taking the medicine.
- Confusion.
- Numbed emotions.
- Visual disturbances such as blurred vision or double vision.
- Shaky movements and unsteady walk (ataxia).
- Loss of memory (amnesia).
- Muscle weakness.
- Dizziness.
- Headache.
- Skin rashes.
- Disturbances of the gut such as diarrhoea, constipation, nausea, vomiting or abdominal pain.
- Difficulty in passing urine (urinary retention).
- Changes in sex drive.
- Low blood pressure (hypotension).
- Blood disorders.
- Jaundice.
- Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
- Nightmares or hallucinations (tell your doctor if you experience this).
Rare
- agitation
- anxiety
- behavioural changes, including aggressiveness, angry outbursts, bizarre behaviour, or decreased inhibitions
- confusion
- increased trouble sleeping
- memory problems
- muscle spasms
- shortness of breath
Drug Interactions of Prednisolone
Prednisolone may interact with following drugs, supplements, & may change the efficacy of drugs
- abatacept
- anakinra
- Amphotericin B
- Antibiotics
- Anticholinesterase agents such as donepezil, rivastigmine, and galantamine
- Anticoagulants such as warfarin
- Antidiabetic agents
- anti-tumour necrosis factor agents (e.g., adalimumab, etanercept, infliximab, )
- azathioprine
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- beta-blockers (e.g., carvedilol, metoprolol, propranolol)
- carbamazepine
- clonidine
- clozapine
- corticosteroids (e.g.dexamethasone, hydrocortisone, prednisone)
- cyclosporine
- diltiazem
- imatinib
- Estrogens, including oral contraceptives
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- methotrexate
- methyldopa
- mycophenolate
- phenobarbital
- phenytoin
- rituximab
- tacrolimus
- verapamil
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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