Desloratadine

Source: Wikipedia, the free encyclopedia.
Desloratadine
Clinical data
Trade namesClarinex, Aerius, Allex, others[1][2]
AHFS/Drugs.comMonograph
MedlinePlusa602002
License data
Pregnancy
category
  • AU: B1
Routes of
administration		By mouth (tablets, solution)
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityRapidly absorbed
Protein binding83 to 87%
MetabolismUGT2B10, CYP2C8
Metabolites3-Hydroxydesloratadine
Onset of actionwithin 1 hour[3]
Elimination half-life27 hours[3]
Duration of actionup to 24 hours[3]
Excretion40% as conjugated metabolites into urine
Similar amount into the feces
Identifiers
  • 8-chloro-6,11-dihydro-11-(4-piperdinylidene)- 5H-benzo[5,6]cyclohepta[1,2-b]pyridine
JSmol)
  • Clc4cc2c(C(/c1ncccc1CC2)=C3/CCNCC3)cc4
  • InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2 checkY
  • Key:JAUOIFJMECXRGI-UHFFFAOYSA-N checkY
  (verify)

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.[3]

It was patented in 1984 and came into medical use in 2001.[4]

Medical uses

Desloratadine is used to treat

chronic idiopathic urticaria (hives).[5] It is the major metabolite of loratadine and the two drugs are similar in safety and effectiveness.[5] Desloratadine is available in many dosage forms and under many trade names worldwide.[6]

An emerging indication for desloratadine is in the treatment of acne, as an inexpensive adjuvant to isotretinoin and possibly as maintenance therapy or monotherapy.[7][8]

Side effects

The most common side-effects are

dry mouth (3%[9]), and headache (0.6%[9]).[5]

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.[10][11]

Pharmacology

Pharmacodynamics

Desloratadine is a selective H1-

histamine H1 receptor.[12]

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.[13]

Pharmacokinetics

Desloratadine is well absorbed from the gut and reaches highest

plasma proteins.[11]

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.[14] Both desloratadine and 3-hydroxydesloratadine are eliminated via urine and feces with a half-life of 27 hours in normal metabolizers.[11][15]

3-Hydroxydesloratadine is the main metabolite.

It exhibits only peripheral activity since it does not readily cross the

drowsiness because it does not readily enter the central nervous system.[16]

Desloratadine does not have a strong effect on a number of tested enzymes in the

UGT1A7, and UGT1A8.[14]

Pharmacogenomics

2% of

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.[11][15]

See also

References

  1. S2CID 195689362
    .
  2. ^ "Allex EPAR". European Medicines Agency (EMA).
  3. ^
    ISBN 9780323044042
    . Desloratadine is a metabolite of loratadine. The onset of action is within 1 hour. Peak serum concentrations of desloratadine appear 3 hours after dosing. The mean elimination half-life of desloratadine is 27 hours and that of its metabolite is 36 hours. The consumption of food does not interfere with the absorption of desloratadine. Wheal inhibition is detected 1 hour after administration and may last 24 hours.
  4. ISBN 9783527607495
    .
  5. ^
    PMID 14655812. Archived from the original
    on 2005-07-24. Retrieved 2005-08-01.
  6. ^ Drugs.com Desloratadine entry at drugs.com international Page accessed May 4, 2015
  7. S2CID 3406128
    .
  8. PMID 27015774
    .
  9. ^
    S2CID 40472187
    .
  10. U.S. Food and Drug Administration
    . Retrieved 2022-01-21.
  11. ^ a b c d "Aerius: EPAR – Product Information" (PDF). European Medicines Agency. Archived from the original (PDF) on 2019-07-05. Retrieved 2022-01-21.
  12. PMID 23268457
    .
  13. ^ "Aerius: EPAR – Scientific Discussion" (PDF). European Medicines Agency. 2006-04-03. Archived from the original (PDF) on 2018-03-16. Retrieved 2017-10-13.
  14. ^
    PMID 26135009
    .
  15. ^ a b Drugs.com: Desloratadine Monograph.
  16. PMID 10784544
    .

External links

  • "Desloratadine". Drug Information Portal. U.S. National Library of Medicine.
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