Composition:

Each film-coated Delarex tablet contains desloratadine 5 mg.

Each 5 ml Delarex syrup contains 2.5 mg desloratadine.

Pharmacodynamics:

Delarex, desloratadine, is a long-acting tricyclic histamine antagonist with selective H1-receptor histamine antagonist activity.  

It is a metabolite of loratadine.

It does not cross the blood brain barrier.

It inhibited histamine release from human mast cells in vitro.

Pharmacokinetics:

Following oral administration of desloratadine 5 mg, mean peak plasma concentrations are reached within 3 hours.  

A single dose of 10 ml of the syrup containing 5 mg desloratadine is bioequivalent to a single dose of desloratadine tablet.

Neither food nor grapefruit juice had an effect on the bioavailability of desloratadine.

Desloratadine & 3-hydroxydesloratadine are approximately 85% protein bound.

Desloratadine is metabolized to an active metabolite, 3-hydroxydesloratadine.  

This metabolite subsequently undergoes glucuronidation.

Half-life of desloratadine is 27 hours.  

A recovery of approximately 87% of a 14C-desloratadine dose is equally distributed in the urine & feces as metabolic products.

 Therapeutic Indications:

Relief of nasal & non-nasal symptoms of seasonal & perennial allergic rhinitis in patients 6 months of age & older.

Symptomatic relief of pruritus, reduction in the number of hives, & size of hives, in patients with chronic idiopathic urticaria 6 months of age & older.

Symptoms of allergic conjunctivitis.

 Dosage and Administration:

Adults & children 12 years of age & over:

One tablet of Delarex tablet to be taken once daily or two teaspoonfuls of Delarex syrup (5mg in 10 ml) to be taken once daily.

Children 6 to 11 years of age:

One teaspoonful of Delarex syrup (2.5 mg in 5 ml) to be given once daily.

Children 12 months to 5 years of age:

Half a teaspoonful of Delarex syrup (1.25 mg in 2.5 ml) to be given once daily.

Children 6 to 11 months of age:

2 ml (1.0 mg) to be given once daily with a special measuring device.

Patients with hepatic or renal impairment should be given desloratadine 5 mg on alternate days initially.

Precautions:

No adequate & well-controlled studies in pregnant women are documented, therefore, desloratadine should be used during pregnancy only if clearly needed.

As desloratadine passes into breast milk, therefore a decision should be made whether to discontinue nursing or to discontinue desloratadine, taking into account the importance of the drug to the mother.

Dosage adjustment for patients with renal or hepatic impairment is recommended.

Safety of tablets & syrup have not been demonstrated in pediatric patients less than 6 months of age.

 Contraindications:

In patients who are hypersensitive to desloratadine, to any of the product ingredients, or to loratadine.

 Adverse Reactions:

Pharyngitis, dry mouth, myalgia, fatigue, somnolence, dysmenorrhea, incidence of sedation & low antimuscarinic effects.

Other side effects have been reported such as tachycardia, palpitations & rarely arrhythmias & hypersensitivity reactions (such as rash, pruritus, urticaria, edema, dyspnea, & anaphylaxis), extrapyramidal effects, blood disorders & elevated liver enzymes including bilirubin & very rarely hepatitis.

Frequency & magnitude of laboratory & electrocardiographic abnormalities were similar in desloratadine & placebo-treated patients.

Rare side effects of the syrup form may occur such as fever, diarrhea, appetite increase, emotional lability, pharyngitis, somnolence, insomnia.

 N.B:

Overdose of desloratadine: little increase in QT with NO clinically relevant adverse events were reported.

Presentation & Storage:

Delarex tablets are supplied in boxes of 10 tablets each.

Delarex syrup is supplied in bottles of 60 ml each.

Store at a temperature not exceeding 30⁰C, away from heat.