Desloratadine
Desloratadine
Contact Us

We are here to help in anything you need. Please use our online system or send an email to .

Desloratadine

Inquiry
Catalog Number PR100643718
CAS 100643-71-8
Description 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).
Synonyms Clarinex; Descarboethoxyloratadine; Desloratidine; Neoclarityn; Aerius
IUPAC Name 13-chloro-2-piperidin-4-ylidene-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaene
Molecular Weight 310.8
Molecular Formula C19H19ClN2
InChI JAUOIFJMECXRGI-UHFFFAOYSA-N
InChI Key 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
Associated Therapies Antihistamine
Documentation/Certification CEP / USFDA
Drug Categories Anticholinergic Agents; Antihistamines for Systemic Use; Benzocycloheptenes; Central Nervous System Depressants; Cholinergic Agents; Dibenzocycloheptenes; Histamine Agents; Histamine Antagonists; Histamine H1 Antagonists; Histamine H1 Antagonists, Non-Sedating; Loratadine and derivatives; Moderate Risk QTc-Prolonging Agents; Neurotransmitter Agents; P-glycoprotein inhibitors; Piperidines; QTc Prolonging Agents
Drug Interactions 1,2-Benzodiazepine-The risk or severity of CNS depression can be increased when Desloratadine is combined with 1,2-Benzodiazepine.
Acetazolamide-The risk or severity of CNS depression can be increased when Acetazolamide is combined with Desloratadine.
Acetophenazine-The risk or severity of CNS depression can be increased when Desloratadine is combined with Acetophenazine.
Aclidinium-The risk or severity of adverse effects can be increased when Desloratadine is combined with Aclidinium.
Acrivastine-The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Desloratadine.
Half-Life Desloratadine has a mean plasma elimination half-life of approximately 27 hours.
Isomeric SMILES C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4
Type Small Molecule
Therapeutic Category Antihistamines
Pharmacology

Indications

Desloratadine is indicated for the alleviation of symptoms associated with seasonal allergic rhinitis and perennial allergic rhinitis, providing·h as nasal cong·he symptomatic treatment of pruritus and urticaria, particularly those associated with chronic idiopathic urticaria, including·he reduction of itching·he prevention of hives.

Pharmacodynamics

Desloratadine is classified as a long·h1-receptor antagonist with selective and peripheral activity. It functions by blocking·histamine from binding·h1 receptor, thereby inhibiting·he subsequent release of chemicals responsible for allergic symptoms. Unlike many antihistamines, Desloratadine does not penetrate the brain-blood barrier, effectively minimizing·he risk of drowsiness as a side effect.

Absorption

When administered orally, Desloratadine demonstrates efficient absorption characteristics. Upon daily administration of a 5 mg tablet over ten days, Desloratadine reaches a peak plasma concentration (Tmax) of approximately 3 hours, with a mean steady-state Cmax of 4 ng·hr/mL. Comparable pharmacokinetic profiles are observed when delivered as a 10 mL oral solution containing·he active ing·he presence of food does not influence the absorption of Desloratadine.

Metabolism

Desloratadine undergoes hepatic metabolism, converting·hydroxydesloratadine. This metabolite is further processed through glucuronidation, a pathway facilitating·his metabolic transformation plays a crucial role in the drug's efficacy and duration of action.

Mechanism of Action

Desloratadine functions by competing with free histamine for H1-receptor binding sites located in the gastrointestinal tract, uterus, large blood vessels, and bronchial smooth muscle. Through this competitive inhibition, Desloratadine effectively blocks the action of endogenous histamine, providing temporary relief from symptoms such as nasal congestion and watery eyes that are typically induced by histamine.

It should be noted that our service is only used for research, not for clinical use.