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Claritin

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Claritin
IUPAC name4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylic acid ethyl ester
TradenameClaritin, Alavert, others
Drugs.commonograph, loratadine
MedlinePlusa697038
Pregnancy AUB1
Routes of administrationBy mouth
BioavailabilityWell absorbed
Protein bound97–99%
MetabolismLiver (CYP3A4 and CYP2D6)
Elimination half-life8.4 hours (loratadine), 28 hours (desloratadine)
ExcretionUrine (40%) and feces (40%)
CAS number79794-75-5
PubChem3957
DrugBankDB00455
ChemSpiderID3819
UNII7AJO3BO7QN
ChEBI6536
ChEMBL1007
SynonymsSCH 29851
Chemical formulaC22H23ClN2O2
Molecular weight382.88 g·mol−1

Claritin is a widely recognized brand name for the antihistamine drug loratadine, used primarily for the relief of allergy symptoms. It is classified as a second-generation, non-sedating antihistamine, distinguishing it from older agents like diphenhydramine. The medication is available over-the-counter in numerous formulations, including tablets, syrup, and rapidly-dissolving tablets, and is marketed globally by the pharmaceutical company Bayer.

Medical uses

Claritin is indicated for the symptomatic relief of allergic rhinitis, including symptoms such as sneezing, rhinorrhea, pruritus, and ocular redness. It is also effective in managing chronic idiopathic urticaria, reducing wheals and pruritus associated with the condition. Unlike some first-generation antihistamines, it is not typically used for insomnia or motion sickness due to its reduced central nervous system penetration. Clinical studies, such as those published in the Journal of Allergy and Clinical Immunology, have demonstrated its efficacy compared to placebo and other agents like cetirizine.

Adverse effects

The adverse effect profile of Claritin is generally favorable, with most side effects being mild and comparable to placebo. The most commonly reported effects include headache, somnolence, fatigue, and xerostomia. Serious adverse events like cardiac arrhythmia are extremely rare and typically associated with significant overdose or interactions with potent CYP3A4 inhibitors like ketoconazole. Post-marketing surveillance by the U.S. Food and Drug Administration has confirmed its safety profile, with minimal incidence of hepatotoxicity or severe hypersensitivity reactions.

Pharmacology

Loratadine functions as a selective, peripheral histamine H1 receptor antagonist, binding to these receptors on surfaces like vascular endothelial cells and smooth muscle. Its active metabolite, desloratadine, is formed via the cytochrome P450 system, primarily through CYP3A4 and CYP2D6 enzymes. The drug exhibits minimal affinity for muscarinic acetylcholine receptors or serotonin receptors, accounting for its low anticholinergic effects. Pharmacokinetic studies show high protein binding and a biphasic elimination pattern, with the metabolite contributing to the prolonged duration of action.

History

Loratadine was originally developed by the American pharmaceutical company Schering-Plough, with its synthesis first described in the early 1980s. It received approval from the U.S. Food and Drug Administration in 1993, initially as a prescription medication. A significant milestone occurred in 2002 when it became available over-the-counter in the United States, following a review by an FDA advisory committee. This switch was part of a broader trend for antihistamines, similar to the reclassification of fexofenadine. The patent expiration led to widespread production of generic versions by companies like Teva Pharmaceutical Industries.

Society and culture

The marketing of Claritin, particularly its direct-to-consumer advertising campaigns in the United States, played a major role in its commercial success and public recognition. It has been featured prominently in media and was one of the first drugs advertised on American television following changes in FDA regulations. The brand name is owned by Bayer following its acquisition of Merck & Co.'s consumer health division. Its availability without a prescription has made it a staple in pharmacies worldwide, and it is often compared to competitors like Zyrtec and Allegra in consumer guides.

Category:Antihistamines Category:Bayer brands Category:Drugs developed in the United States