It was found to weakly inhibit CYP2B6, CYP2D6, and CYP3A4/ CYP3A5, and not to inhibit CYP1A2, CYP2C8, CYP2C9, or CYP2C19. ĭesloratadine does not have a strong effect on a number of tested enzymes in the cytochrome P450 system. It exhibits only peripheral activity since it does not readily cross the blood–brain barrier hence, it does not normally cause drowsiness because it does not readily enter the central nervous system. 3-Hydroxydesloratadine is the main metabolite. Both desloratadine and 3-hydroxydesloratadine are eliminated via urine and feces with a half-life of 27 hours in normal metabolizers. First, n-glucuronidation of desloratadine by UGT2B10 then, 3-hydroxylation of desloratadine N-glucuronide by CYP2C8 and finally, a non-enzymatic deconjugation of 3-hydroxydesloratadine N-glucuronide. ĭesloratadine is metabolized to 3-hydroxydesloratadine in a three-step sequence in normal metabolizers. In the bloodstream, 83 to 87% of the substance are bound to plasma proteins. Pharmacokinetics ĭesloratadine is well absorbed from the gut and reaches highest blood plasma concentrations after about three hours. This effect is not relevant for the drug's action at therapeutic doses. Īt very high doses, is also an antagonist at various subtypes of the muscarinic acetylcholine receptors. Pharmacology Pharmacodynamics ĭesloratadine is a selective H 1- antihistamine which functions as an inverse agonist at the histamine H 1 receptor. However, no clinically relevant changes were observed. Interactions Ĭo-administration with erythromycin, ketoconazole, azithromycin, fluoxetine or cimetidine resulted in elevated blood plasma concentrations of desloratadine and its metabolite 3-hydroxydesloratadine in studies. The most common side-effects are fatigue (1.2% ), dry mouth (3% ), and headache (0.6% ). Īn emerging indication for desloratadine is in the treatment of acne, as an inexpensive adjuvant to isotretinoin and possibly as maintenance therapy or monotherapy. Desloratadine is available in many dosage forms and under many trade names worldwide. It is the major metabolite of loratadine and the two drugs are similar in safety and effectiveness. Medical uses ĭesloratadine is used to treat allergic rhinitis, nasal congestion and chronic idiopathic urticaria ( hives). It was patented in 1984 and came into medical use in 2001. It is an active metabolite of loratadine. Desloratadine (trade names Clarinex and Aerius) is a tricyclic H 1 inverse agonist that is used to treat allergies.
0 Comments
Leave a Reply. |
AuthorWrite something about yourself. No need to be fancy, just an overview. ArchivesCategories |