Desloratadine is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of the gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relief of allergic symptoms.
Loratadine and its metabolic derivative desloratadine are second-generation antihistamines that are used for the treatment of allergic rhinitis, angioedema, and chronic urticaria. Loratadine and desloratadine have been linked to rare, isolated instances of clinically apparent acute liver injury.
Desloratadine is a second generation, a tricyclic antihistamine that which has a selective and peripheral H1-antagonist action. It is the active descarboethoxy metabolite of loratadine (second generation histamine). Desloratadine has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.
Mechanism of action of Desloratadine
Desloratadine is a long-acting second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be “activated,” releasing other chemicals which produce the effects that we associate with allergies. Desloratadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Desloratadine does not enter the brain from the blood and, therefore, does not cause drowsiness. Desloratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine.
Indications of Desloratadine
- Chronic Idiopathic Urticaria
- Perennial Allergic Rhinitis
- Seasonal Allergic Rhinitis
- Asthma
- Allergic intraocular inflammatory diseases
- Atopic eczema
- Inflammatory dermatoses
- Pruritis
- Allergic symptoms like urticaria,
- Rhinorrhea,
- Sneezing and itching
- Skin itching
- Itching of the skin
- Itching skin
Therapeutic Indications
- For the relief of symptoms of seasonal allergic rhinitis, perennial (non-seasonal) allergic rhinitis.
- Desloratadine is also used for the symptomatic treatment of pruritus and urticaria (hives) associated with chronic idiopathic urticaria.
- Aerius is indicated in adults and adolescents aged 12 years and older for the relief of symptoms associated with allergic rhinitis and urticaria
- Symptoms associated with seasonal allergic rhinitis
- Azomyr is indicated in adults and adolescents aged 12 years and older for the relief of symptoms associated with allergic rhinitis and urticaria
- Dasselta is indicated in adults and adolescents aged 12 years and older for the relief of symptoms
- allergic rhinitis, urticaria
- Desloratadine Teva is indicated in adults and adolescents aged 12 years and older for the urticaria
- Desloratadine Actavis is indicated in adults and adolescents aged 12 years and older for the relief of symptoms associated with .allergic rhinitis, urticaria
- Desloratadine Ratiopharm 5 mg film-coated tablets are indicated in adults and adolescents aged 12 years and older for the relief of symptoms associated with
- Neoclarityn is indicated in adults and adolescents aged 12 years and older for the relief of symptoms associated with allergic rhinitis and urticaria
- Desloratadine is indicated in adults and adolescents aged 12 years and older for the relief of symptoms associated with allergic rhinitis and urticaria.
Contra-Indications of Desloratadine
- Liver Problems
- kidney disease with a reduction in kidney function
Allergies
- Antihistamines
- Antihistamines – Piperidine
Dosages of Desloratadine
Strengths: 5 mg; 2.5 mg/5 mL; 2.5 mg
Allergic Rhinitis
- Initial dose: 5 mg orally once a day
- Maintenance dose: 5 mg orally once a day
Urticaria
- Initial dose: 5 mg orally once a day
- Maintenance dose: 5 mg orally once a day
Allergic Rhinitis
-
Initial dose: 5 mg orally once a day.
- Maintenance dose: 5 mg orally once a day.
Urticaria
- Initial dose: 5 mg orally once a day.
- Maintenance dose: 5 mg orally once a day.
Pediatric dosage
Allergic Rhinitis
- >=6m <12m: 1 mg orally once a day
- >=1y <6y: 1.25 mg orally once a day
- >=6y <11y: 2.5 mg orally once a day
- >=12 years of age: 5 mg orally once a day
Urticaria
- >=6m <12m: 1 mg orally once a day
- >=1y <6y: 1.25 mg orally once a day
- >=6y <11y: 2.5 mg orally once a day>=12 years of age: 5 mg orally once a day
Side Effects of Desloratadine
The most common
- dry mouth, sore throat, cough;
- muscle pain;
- drowsiness, tired feeling;
- nausea, diarrhea; or
- headache.
- Weakness
- dry mouth, sore throat, cough;
- muscle pain;
- drowsiness, tired feeling;
- fever, flu symptoms;
- seizure (convulsions); or
- jaundice (yellowing of the skin or eyes).
More common
- headache
- fast, pounding, or uneven heartbeat;
- fever, flu symptoms;
- seizure (convulsions); or
- jaundice (yellowing of the skin or eyes).
- dry mouth, sore throat, cough;
- muscle pain;
- drowsiness, tired feeling;
- nausea,
- fever, flu symptoms;
- seizure (convulsions); or
- jaundice (yellowing of the skin or eyes).
- dry mouth, sore throat, cough;
- muscle pain;
- drowsiness, tired feeling;
- nausea,
Less common
- Dizziness
- dry mouth
- dysmenorrhea, such as, difficult or painful menstruation
- dyspepsia, such as, acid or sour stomach, belching, heartburn, indigestion, stomach discomfort , upset or pain,
- fatigue, such as, unusual tiredness or weakness
- myalgia, such as, joint pain, swollen joints, muscle aching or cramping, muscle pains or stiffness, difficulty in moving
- pharyngitis, such as, body aches or pain, congestion, cough, dryness or soreness ofthroat, fever, hoarseness, runny nose, tender swollen glands in neck, trouble in swallowing, voice changes.
- somnolence, such as, sleepiness or unusual drowsiness
- nausea
Drug Interaction of Desloratadine
Desloratadine may interact with following drugs, supplyments & may increase or decrease the efficacy of drugs
- antihistamines (e.g,. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
- antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- barbiturates (e.g., butalbital, pentobarbital phenobarbital)
- benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
- general anesthetics (medications used to put people to sleep before surgery)
- ipratropium
- ketotifen
- mirabegron
- mirtazapine
- muscle relaxants (e.g., cyclobenzaprine, methocarbamol, orphenadrine)
- narcotic pain relievers (e.g., codeine, fentanyl, morphine, oxycodone)
- seizure medications (e.g., clobazam, ethosuximide, felbamate, levetiracetam, phenobarbital, phenytoin, primidone, topiramate, valproic acid, zonisamide)
- selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
- sleeping medications (e.g., zolpidem, zopiclone)
- tapentadol
- thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, metolazone)
- tiotropium
- tolterodine
- tramadol
- tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
- trazodone
Pregnancy & Lactation of Desloratadine
FDA Pregnancy Category C
Pregnancy
There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, desloratadine should be used during pregnancy only if clearly needed.
Lactation
Desloratadine passes into breast milk; therefore, a decision should be made whether to discontinue nursing or to discontinue desloratadine, taking into account the benefit of the drug to the nursing mother and the possible risk to the child.
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