Aerius

Tablet: Each tablet contains 5 mg of micronized desloratadine.
Syrup: Each mL of desloratadine syrup contains 500 mcg of desloratadine.
Desloratadine tablet and syrup contain desloratadine (SCH 34117), a non-sedating antihistamine with selective peripheral H₁-receptor antagonistic activity. Desloratadine is currently used or under development for the relief of symptoms associated with seasonal and perennial allergic rhinitis, urticaria and other dermatologic disorders.
Desloratadine is a white to off-white powder slightly soluble in water but very soluble in ethanol, propylene glycol, methylene chloride, methanol and octanol. It has an Empirical Formula: C₁₉H₁₉ClN₂ and Molecular Weight of 310.8. The chemical name is 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo-[5,6] cyclohepta [1,2-b]pyridine.
Excipients/Inactive Ingredients: Tablet: Dibasic calcium phosphate dihydrate, microcrystalline cellulose, maize starch, talc, blue color film-coat material, clear film coat material, white wax and carnauba wax.
Syrup: Propylene glycol, sorbitol solution, citric acid anhydrous, sodium citrate dihydrate, sodium benzoate, edetate disodium, sucrose, flavor bubble gum, water purified.

Antihistamine.
Pharmacology: Pharmacodynamics: Desloratadine, the active ingredient in Desloratadine tablets and syrup, is an antihistamine with selective peripheral H₁-receptor antagonist activity.
In addition to antihistamine activity, desloratadine has demonstrated antiallergic activities in in vitro (conducted on human cells) and in vivo studies. These studies have shown that desloratadine can inhibit events in the cascade of allergic inflammation, including: release of inflammatory cytokines including IL-4, IL-6, IL-8, IL-13 from human mast cells/basophils; expression of adhesion molecules such as P-selectin; inhibition of allergic cough in animal models.
Pharmacodynamic Properties: In a clinical program, desloratadine was demonstrated to be safe and efficacious in the treatment of symptoms associated with allergic rhinitis. In addition, the safety and efficacy of desloratadine was demonstrated in the treatment of the symptoms of chronic idiopathic urticaria and other dermatologic disorders.
In a study in which desloratadine was administered at a dose of 45 mg daily (nine times the clinical dose) for ten days, no prolongation of the QTc interval was seen.
Desloratadine does not readily penetrate the central nervous system. At the recommended dose of 5 mg daily for adults and adolescents, there was no excess incidence of somnolence as compared to placebo. Desloratadine given at a single daily dose of 7.5 mg to adults and adolescents did not affect psychomotor performance in clinical studies, nor did a single daily dose of 5 mg to adults affect standard measures of flight performance under simulated flight conditions. Desloratadine has no or negligible influence on the ability to drive and use machines.
No clinically relevant changes in desloratadine plasma concentrations were observed in multiple-dose azithromycin, ketoconazole, erythromycin, fluoxetine or cimetidine interaction trials.
Pharmacokinetics: Desloratadine is well absorbed with maximum concentration achieved after approximately 3 hours; the terminal phase half-life is approximately 27 hours. The degree of accumulation of desloratadine is consistent with its half-life and a once daily dosing frequency. The bioavailability of desloratadine is dose proportional over the range of 5 mg to 20 mg.
Desloratadine is moderately bound (82-88%) to plasma proteins.
Desloratadine is extensively metabolized to 3-hydroxy desloratadine, an active metabolite, which is subsequently glucuronidated. A human mass balance study documented a recovery of approximately 87% of the ¹⁴C-desloratadine dose, which was equally distributed in urine and feces as metabolic products.
The pharmacokinetic profile of desloratadine is comparable in healthy adult volunteers and in healthy geriatric volunteers and no dosage adjustment is required.
In single dose trials of desloratadine tablets (7.5 mg) or syrup (5 mg), there was no effect of food on the disposition of desloratadine. In another study, grapefruit juice had no effect on the disposition of desloratadine.
In single dose, crossover studies of desloratadine, the tablet and syrup formulations were found to be bioequivalent.
Toxicology: Preclinical Studies: Desloratadine is the primary active metabolite of loratadine. Preclinical data with desloratadine reveal no special hazard for humans based on studies of genotoxicity, carcinogenic potential, and toxicity to reproduction.
No significant local irritant effect was noted when desloratadine RediTabs was tested in the hamster cheek pouch buccal irritation assay.

Desloratadine (AERIUS) tablet and syrup are indicated for the rapid relief of symptoms associated with allergic rhinitis, such as sneezing, nasal discharge and itching, congestion/stuffiness, as well as ocular itching, tearing and redness, itching of palate and coughing.
Desloratadine (AERIUS) tablet and syrup are also indicated for the relief of symptoms associated with urticaria such as the relief of itching and the size and number of hives.

Adults (including geriatric patients) and children 12 years of age and older: One Desloratadine (AERIUS) 5 mg tablet or 10 mL (5 mg) of syrup once a day regardless of mealtime for the relief of symptoms associated with allergic rhinitis (including intermittent and persistent allergic rhinitis) and urticaria. For oral use.
Children 6 through 11 years of age: 5 mL (2.5 mg) of Desloratadine (AERIUS) Syrup once a day with or without food.
Children 1 through 5 years of age: 2.5 mL (1.25 mg) Desloratadine (AERIUS) Syrup once a day with or without food.
Children 6 months through 11 months of age: 2 mL (1 mg) Desloratadine (AERIUS) Syrup once a day, with or without food.

In the event of overdose, consider standard measures to remove unabsorbed active substance. Symptomatic and supportive treatment is recommended. Desloratadine is not eliminated by hemodialysis.

Desloratadine is contraindicated in patients who are hypersensitive to this medication or to any of its ingredients, or to loratadine.

No teratogenic effects were observed in animal studies with desloratadine (See Pharmacology: Toxicology: Preclinical Studies under Actions). Since no clinical data on exposure during pregnancy are available with desloratadine, the safe use of desloratadine during pregnancy has not been established. Desloratadine should not be used during pregnancy unless the potential benefit outweighs the risks. Desloratadine passes into breast milk; therefore, breastfeeding is not recommended in lactating women taking desloratadine.
Desloratadine showed no mutagenic effects in in vitro and in vivo mutagenicity studies.
Desloratadine should be administered with caution in patients with a medical or family history of seizures. In particular, young children may be more susceptible to developing new seizures under desloratadine treatment. Healthcare providers may consider discontinuing desloratadine in patients who experience a seizure while on treatment.
Drug Abuse and Dependence: There is no information to indicate that abuse or dependency occurs with desloratadine tablets.
Interference with Laboratory Tests: None identified.
Other Relevant Safety Information: None.

At the recommended 5 mg dose, adverse events reported at a higher incidence than placebo included dry mouth and fatigue and headache.
Very rare cases of hypersensitivity reactions, including anaphylaxis and rash, have been reported during the marketing of desloratadine. In addition, cases of tachycardia, palpitations, seizures, psychomotor hyperactivity, somnolence, elevated liver enzymes and bilirubin, hepatitis, and increased appetite have been reported very rarely.

No clinically relevant interactions with desloratadine were observed in clinical trials in which azithromycin, erythromycin, ketoconazole, fluoxetine or cimetidine was co-administered. There was no effect of food or grapefruit juice on the disposition of desloratadine (See Pharmacology: Pharmacodynamics: Pharmacodynamic Properties under Actions).

Store at temperatures not exceeding 30°C.

Antihistamines & Antiallergics

R06AX27 - desloratadine ; Belongs to the class of other antihistamines for systemic use.

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