|Trade names||Aerius, Allex, Clarinex, others|
|By mouth (tablets, solution)|
|Onset of action||Within 1 hour|
|Duration of action||Up to 24 hours|
|Protein binding||83 to 87%|
|Elimination half-life||27 hours|
|Excretion||40% as conjugated metabolites into urine|
Similar amount into the feces
|Chemical and physical data|
|Molar mass||310.83 g·mol−1|
|3D model (JSmol)|
Desloratadine, sold under the brand name Clarinex among others, is a medication used to treat allergies such as hay fever and hives. Onset occurs within an hour and lasts for up to 24 hours. It is taken by mouth.
Common side effects include nausea, tiredness, dry mouth, and headache. A lower dose is recommended in those with kidney or liver problems. While there is no clear evidence of harm during pregnancy, such use is generally not recommended. It is a second generation antihistamine. It is an active metabolite of loratadine.
Desloratadine was patented in 1984 and came into medical use in 2001. In the United Kingdom it is avaliable as a generic medication and costs the NHS about 1.5 pounds per month. In the United States this amount costs about 17 USD. It is also available with pseudoephedrine.
Desloratadine is used to treat allergic rhinitis, nasal congestion and chronic idiopathic urticaria (hives). It is the major metabolite of loratadine and the two drugs are similar in safety and effectiveness. Desloratadine is available in many dosage forms and under many trade names worldwide.
A number of drugs and other substances that are prone to interactions, such as ketoconazole, erythromycin and grapefruit juice, have shown no influence on desloratadine concentrations in the body. Desloratadine is judged to have a low potential for interactions.
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. Both desloratadine and 3-hydroxydesloratadine are eliminated via urine and feces with a half-life of 27 hours in normal metabolizers.
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.
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.
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.
Society and culture
When initially released in Canada in 2002 it sold for CA$0.82 per dose.
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