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Active ingredient: Loratadine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anti-allergic Agents
  • Antipruritics
  • Antihistamines
  • Histamine H1 Antagonists, Non-Sedating

Dosage Forms

  • Tablet
  • Syrup

Brands / Synonyms

Aerotina; Alarin; Alavert; Alerpriv; Allertidin; Bedix Loratadina; Biloina; Bonalerg; Civeran; Claratyne; Claratyne Cold; Claratyne Decongestant; Clarinase; Clarinase Reperabs; Clarinex; Claritin; Claritin Reditab; Claritin Reditabs; Claritin-D; Claritine; Clarityn; Clarityne; Fristamin; Histaloran; Lergy; Lertamine; Lesidas; Lisino; Loracert; Loradex; Loradif; Loranox; Lorantis; Lorastine; Loratadina [Spanish]; Loratadine [Usan:Ban:Inn]; Loratadinum [Latin]; Loratyne; Loraver; Lorfast; Loritine; Lowadina; Nularef; Optimin; Polaratyne; Pylor; Restamine; Rhinase; Rinomex; Sanelor; Sensibit; Sinhistan Dy; Sohotin; Tadine; Talorat Dy; Velodan; Versal; Zeos

Indications

For the relief of nasal and non-nasal symptoms of seasonal allergic rhinitis and for the treatment of chronic idiopathic urticaria in patients 2 years of age or older

Pharmacology

Loratadine, a non-sedating H1-blocker similar in structure to cyproheptadine and azatadine, is used to treat seasonal allergic rhinitis. Unlike other H1-blockers, loratidine does not penetrate the CNS effectively and has a low affinity for CNS H1-receptors.

Mechanism of Action

Like other H1-blockers, loratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial muscle. Loratadine also has a weak affinity for acetylcholine and alpha-adrenergic receptors.

Absorption

Rapidly absorbed following oral administration (40% bioavailability)

Toxicity

somnolence, tachycardia, and headache LD50=mg/kg (orally in rat)

Biotrnasformation / Drug Metabolism

Hepatic

Contraindications

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

Drug Interactions

Loratadine (10 mg once daily) has been coadministered with therapeutic doses of erythromycin, cimetidine, and ketoconazole in controlled clinical pharmacology studies in adult volunteers. Although increased plasma concentrations (AUC 0-24 hrs) of loratadine and/or descarboethoxyloratadine were observed following coadministration of loratadine with each of these drugs in normal volunteers (n = 24 in each study), there were no clinically relevant changes in the safety profile of loratadine, as assessed by electrocardiographic parameters, clinical laboratory tests, vital signs, and adverse events. There were no significant effects on QTc intervals, and no reports of sedation or syncope. No effects on plasma concentrations of cimetidine or ketoconazole were observed. Plasma concentrations (AUC 0-24 hrs) of erythromycin decreased 15% with coadministration of loratadine relative to that observed with erythromycin alone. The clinical relevance of this difference is unknown. These above findings are summarized in TABLE 1.

TABLE 1 Effects on Plasma Concentrations (AUC 0-24 hrs) of Loratadine and Descarboethoxyloratadine After 10 Days of Coadministration (Loratadine 10 mg) in Normal Volunteers
  Loratadine Descarboethoxyloratadine
 Erythromycin (500 mg q8h) + 40% +46%
 Cimetidine (300 mg qid) +103% + 6%
 Ketoconazole (200 mg q12h) +307% +73%


There does not appear to be an increase in adverse events in subjects who received oral contraceptives and loratadine.

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