DrugBuyers.Com: Claritin-Loratadine

Claritin-Loratadine

Claritin is called Clarytine in Europe

Loratadine is a white to off-white powder not soluble in water, but very soluble in acetone, alcohol, and chloroform. It has a molecular weight of 382.89, and empirical formula of C22H23ClN2O2; its chemical name is ethyl4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate.

Claritin tablets contain 10 mg micronized loratadine, an antihistamine, to be administered orally. They also contain the following inactive ingredients: Corn starch, lactose, and magnesium stearate.

Claritin syrup contains 1 mg/ml micronized loratadine, an antihistamine, to be administered orally. It also contains the following inactive ingredients: Citric acid, artificial flavor, glycerin, propylene glycol, sodium benzoate, sugar, and water. The pH is between 2.5 and 3.1.

Claritin Reditabs (rapidly-disintegrating tablets) contain 10 mg micronized loratadine, an antihistamine, to be administered orally. It disintegrates in the mouth within seconds after placement on the tongue, allowing its contents to be subsequently swallowed with or without water. Claritin Reditabs also contain the following inactive ingredients: Citric acid, gelatin, mannitol, and mint flavor.

Loratadine is indicated for the relief of nasal and non-nasal symptoms of seasonal allergic rhinitis and for the treatment of chronic idiopathic urticaria in patients 6 years of age or older.

CONTRAINDICATIONS

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

PRECAUTIONS

General

Patients with liver impairment or renal insufficiency (GFR
Carcinogenesis, Mutagenesis, and Impairment of Fertility
In an 18-month carcinogenicity study in mice and a 2-year study in rats, loratadine was administered in the diet at doses up to 40 mg/kg (mice) and 25 mg/kg (rats). In the carcinogenicity studies, pharmacokinetic assessments were carried out to determine animal exposure to the drug. AUC data demonstrated that the exposure of mice given 40 mg/kg of loratadine was 3.6 (loratadine) and 18 (descarboethoxyloratadine) times higher than in humans given the maximum recommended daily oral dose. Exposure of rats given 25 mg/kg of loratadine was 28 (loratadine) and 67 (descarboethoxyloratadine) times higher than in humans given the maximum recommended daily oral dose. Male mice given 40 mg/kg had a significantly higher incidence of hepatocellular tumors (combined adenomas and carcinomas) than concurrent controls. In rats, a significantly higher incidence of hepatocellular tumors (combined adenomas and carcinomas) was observed in males given 10 mg/kg and males and females given 25 mg/kg. The clinical significance of these findings during long-term use of loratadine is not known.

In mutagenicity studies, there was no evidence of mutagenic potential in reverse (Ames) or forward point mutation (CHO-HGPRT) assays, or in the assay for DNA damage (rat primary hepatocyte unscheduled DNA assay) or in two assays for chromosomal aberrations (human peripheral blood lymphocyte clastogenesis assay and the mouse bone marrow erythrocyte micronucleus assay). In the mouse lymphoma assay, a positive finding occurred in the nonactivated but not the activated phase of the study.

Decreased fertility in male rats, shown by lower female conception rates, occurred at an oral dose of 64 mg/kg (approximately 50 times the maximum recommended human daily oral dose on a mg/m2 basis) and was reversible with cessation of dosing. Loratadine had no effect on male or female fertility or reproduction in the rat at an oral dose of approximately 24 mg/kg (approximately 20 times the maximum recommended human daily oral dose on a mg/m2 basis).

Pregnancy Category B

There was no evidence of animal teratogenicity in studies performed in rats and rabbits at oral doses up to 96 mg/kg (approximately 75 times and 150 times, respectively, the maximum recommended human daily oral dose on a mg/m2 basis). There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, loratadine should be used during pregnancy only if clearly needed.

Nursing Mothers

Loratadine and its metabolite, descarboethoxyloratadine, pass easily into breast milk and achieve concentrations that are equivalent to plasma levels with an AUCmilk/AUCplasma ratio of 1.17 and 0.85 for loratadine and descarboethoxyloratadine, respectively. Following a single oral dose of 40 mg, a small amount of loratadine and descarboethoxyloratadine was excreted into the breast milk (approximately 0.03% of 40 mg over 48 hours). A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Caution should be exercised when loratadine is administered to a nursing woman.

Pediatric Use

The safety of loratadine syrup at a daily dose of 10 mg has been demonstrated in 188 pediatric patients 6 to 12 years of age in placebo-controlled 2-week trials. The effectiveness of loratadine for the treatment of seasonal allergic rhinitis and chronic idiopathic urticaria in this pediatric age group is based on an extrapolation of the demonstrated efficacy of loratadine in adults in these conditions and the likelihood that the disease course, pathophysiology, and the drug's effect are substantially similar to that of the adults. The recommended dose for the pediatric population is based on cross-study comparison of the pharmacokinetics of loratadine in adults and pediatric subjects and on the safety profile of loratadine in both adults and pediatric patients at doses equal to or higher than the recommended doses. The safety and effectiveness of loratadine in pediatric patients under 6 years of age have not been established.