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QuickView for cetirizine (compound)


PubChem
Name: Cetirizine
PubChem Compound ID: 150716
Description: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.
Molecular formula: C21H25ClN2O3
Molecular weight: 388.888 g/mol
Synonyms:
NCGC00016949-01; CAS-83881-52-1
DrugBank
Identification
Name: Cetirizine
Name (isomeric): DB00341
Drug Type: small molecule
Description: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.
Synonyms:
Cetirizina [Spanish]; Cetrizine Hcl; Cetirizinum [Latin]
Brand: Zyrtec-D, Formistin, Reactine, Alerlisin, Zirtek, Setir, Zyrtec, Hitrizin Film Tablet, Virlix, Ziptek, Zyrlex, Zyrtec Syrup, Cetryn
Category: Antihistamines, Anti-Allergic Agents, Histamine H1 Antagonists, Non-Sedating
CAS number: 83881-51-0
Pharmacology
Indication: For the relief of symptoms associated with seasonal allergic rhinitis, perennial allergic rhinitis and the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria
Pharmacology: Cetirizine, the active metabolite of the piperazine H1-receptor antagonist hydroxyzine, is used to treat chronic idiopathic urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, allergic asthma, physical urticaria, and atopic dermatitis.
Mechanism of Action:
Cetirizine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The low incidence of sedation can be attributed to reduced penetration of cetirizine into the CNS as a result of the less lipophilic carboxyl group on the ethylamine side cha...
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Absorption: mean peak plasma concentration (Cmax) of 114 ng/mL at a time (Tmax) of 2.2 hours postdose was observed for cetirizine
Protein binding: Very high (93%) plasma protein binding
Half Life: 8.3 hours
Clearance: 53 mL/min [healthy]
Toxicity: Somnolence (sleepiness or unusual drowsiness), restlessness, irritability
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Take without regard to meals.

Targets