Английская Википедия:Desloratadine
Шаблон:Short description Шаблон:Cs1 config Шаблон:Drugbox Desloratadine (trade names Clarinex and Aerius) is a tricyclic H1 inverse agonist that is used to treat allergies. It is an active metabolite of loratadine.[1]
It was patented in 1984 and came into medical use in 2001.[2]
Medical uses
Desloratadine is used to treat allergic rhinitis, nasal congestion and chronic idiopathic urticaria (hives).[3] It is the major metabolite of loratadine and the two drugs are similar in safety and effectiveness.[3] Desloratadine is available in many dosage forms and under many trade names worldwide.[4]
An emerging indication for desloratadine is in the treatment of acne, as an inexpensive adjuvant to isotretinoin and possibly as maintenance therapy or monotherapy.[5][6]
Side effects
The most common side-effects are fatigue (1.2%[7]), dry mouth (3%[7]), and headache (0.6%[7]).[3]
Interactions
Co-administration with erythromycin, ketoconazole, azithromycin, fluoxetine or cimetidine resulted in elevated blood plasma concentrations of desloratadine and its metabolite 3-hydroxydesloratadine in studies. However, no clinically relevant changes were observed.[8][9]
Pharmacology
Pharmacodynamics
Desloratadine is a selective H1-antihistamine which functions as an inverse agonist at the histamine H1 receptor.[10]
At very high doses, is also an antagonist at various subtypes of the muscarinic acetylcholine receptors. This effect is not relevant for the drug's action at therapeutic doses.[11]
Pharmacokinetics
Desloratadine is well absorbed from the gut and reaches highest blood plasma concentrations after about three hours. In the bloodstream, 83 to 87% of the substance are bound to plasma proteins.[9]
Desloratadine is metabolized to 3-hydroxydesloratadine in a three-step sequence 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.[12] Both desloratadine and 3-hydroxydesloratadine are eliminated via urine and feces with a half-life of 27 hours in normal metabolizers.[9][13]
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.[14]
Desloratadine does not have a strong effect on a number of tested enzymes in the cytochrome P450 system. It was found to weakly inhibit CYP2B6, CYP2D6, and CYP3A4/CYP3A5, and not to inhibit CYP1A2, CYP2C8, CYP2C9, or CYP2C19. Desloratadine was found to be a potent and relatively selective inhibitor of UGT2B10, a weak to moderate inhibitor of UGT2B17, UGT1A10, and UGT2B4, and not to inhibit UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A9, UGT2B7, UGT2B15, UGT1A7, and UGT1A8.[12]
Pharmacogenomics
2% of Caucasian people and 18% of people from African descent are desloratadine poor metabolizers. In these people, the drug reaches threefold highest plasma concentrations six to seven hours after intake, and has a half-life of about 89 hours. However, the safety profile for these subjects is not worse than for extensive (normal) metabolizers.[9][13]
See also
References
External links
Шаблон:Schering-Plough Шаблон:Antihistamines Шаблон:Histaminergics Шаблон:Tricyclics Шаблон:Portal bar
- ↑ Шаблон:Cite book
- ↑ Шаблон:Cite book
- ↑ 3,0 3,1 3,2 Шаблон:Cite journal
- ↑ Drugs.com Desloratadine entry at drugs.com international Page accessed May 4, 2015
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ 7,0 7,1 7,2 Шаблон:Cite journal
- ↑ Шаблон:Cite web
- ↑ 9,0 9,1 9,2 9,3 Шаблон:Cite web
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite web
- ↑ 12,0 12,1 Шаблон:Cite journal
- ↑ 13,0 13,1 Drugs.com: Desloratadine Шаблон:Drugs.com.
- ↑ Шаблон:Cite journal
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