Description

Simple

A medication used to treat seasonal allergies and allergic skin reactions.

Clinical

A second generation tricyclic antihistamine used to treat seasonal and non seasonal allergic rhinitis, pruritus, and urticaria.

Overview

Desloratadine is a second generation, tricyclic antihistamine that which has a selective and peripheral H1-antagonist action. It is the active descarboethoxy metabolite of loratidine (a second generation histamine). Desloratidine has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.

Pharmacology

Indication

For the relief of symptoms of seasonal allergic rhinitis, perennial (non-seasonal) allergic rhinitis. Desloratidine is also used for the sympomatic treatment of pruritus and urticaria (hives) associated with chronic idiopathic urticaria.

Pharmacodynamic

Desloratadine is a long-acting second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histami... Read more

Mechanism of action

Like other H1-blockers, Desloratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (... Read more

Absorption

Information currently not available.

Protein binding

82-87%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

50 hours

Route of elimination

Desloratadine (a major metabolite of loratadine) is extensively metabolized to 3-hydroxydesloratadine, an active metabolite, which is subsequently glucuronidated. Approximately 87% of a 14C-desloratadine dose was equally recovered in urine and feces.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Route:
    • Oral
  • Hypersensitivity:
    • loratidine
  • Regions: US

Food Interactions

  • Take without regard to meals.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1,10-Phenanthroline
The therapeutic efficacy of Desloratadine can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Desloratadine.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Desloratadine.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Desloratadine.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Desloratadine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Desloratadine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Desloratadine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Desloratadine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Abemaciclib
The serum concentration of Abemaciclib can be increased when it is combined with Desloratadine.
Abexinostat
The risk or severity of QTc prolongation can be increased when Desloratadine is combined with Abexinostat.
Acebutolol
The risk or severity of QTc prolongation can be increased when Desloratadine is combined with Acebutolol.
Acepromazine
The risk or severity of adverse effects can be increased when Desloratadine is combined with Acepromazine.
Aceprometazine
The risk or severity of adverse effects can be increased when Desloratadine is combined with Aceprometazine.
Acetaminophen
The serum concentration of Acetaminophen can be increased when it is combined with Desloratadine.
Acetazolamide
The risk or severity of adverse effects can be increased when Acetazolamide is combined with Desloratadine.
Acetophenazine
The risk or severity of adverse effects can be increased when Desloratadine is combined with Acetophenazine.
Acetyldigoxin
Desloratadine may decrease the excretion rate of Acetyldigoxin which could result in a higher serum level.
Acetylglycinamide chloral hydrate
The risk or severity of adverse effects can be increased when Desloratadine is combined with Acetylglycinamide chloral hydrate.
Acetylsalicylic acid
The serum concentration of Acetylsalicylic acid can be increased when it is combined with Desloratadine.
Aclidinium
Aclidinium may increase the central nervous system depressant (CNS depressant) activities of Desloratadine.
8 References
  1. 1 . Mann RD, Pearce GL, Dunn N, Shakir S: Sedation with "non-sedating" antihistamines: four prescription-event monitoring studies in general practice. BMJ. 2000 Apr 29;320(7243):1184-6.PubMed: 10784544
  2. 2 . Glass DJ, Harper AS: Assessing satisfaction with desloratadine and fexofenadine in allergy patients who report dissatisfaction with loratadine. BMC Fam Pract. 2003 Aug 13;4:10. Epub 2003 Aug 13.PubMed: 12917016
  3. 3 . See S: Desloratadine for allergic rhinitis. Am Fam Physician. 2003 Nov 15;68(10):2015-6.PubMed: 14655812
  4. 4 . Devillier P, Roche N, Faisy C: Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review. Clin Pharmacokinet. 2008;47(4):217-30.PubMed: 18336052
  5. 5 . Bachert C: A review of the efficacy of desloratadine, fexofenadine, and levocetirizine in the treatment of nasal congestion in patients with allergic rhinitis. Clin Ther. 2009 May;31(5):921-44. doi: 10.1016/j.clinthera.2009.05.017.PubMed: 19539095
  6. 6 . DuBuske L: Desloratadine for chronic idiopathic urticaria: a review of clinical efficacy. Am J Clin Dermatol. 2007;8(5):271-83.PubMed: 17902729
  7. 7 . Bachert C, Maurer M: Safety and efficacy of desloratadine in subjects with seasonal allergic rhinitis or chronic urticaria: results of four postmarketing surveillance studies. Clin Drug Investig. 2010;30(2):109-22. doi: 10.2165/11530930-000000000-00000.PubMed: 20067329
  8. 8 . Simons FE, Prenner BM, Finn A Jr: Efficacy and safety of desloratadine in the treatment of perennial allergic rhinitis. J Allergy Clin Immunol. 2003 Mar;111(3):617-22.PubMed: 12642846