DIQTA 1.0: Drug-Induced QT Prolongation Atlas

CETIRIZINE HYDROCHLORIDE

DIR Classification Postmarketing Surveillance Drug Property Information Reference

DIR Classification

Classification:Ambiguous

Severity Score:1.0

Description in Drug Labeling: View Full Labeling: SPL in DailyMed | PDF

CLINICAL PHARMACOLOGY
Pharmacodynamics
In four clinical studies in healthy adult males, no clinically significant mean increases in QTc were observed in cetirizine hydrochloride treated subjects. In the first study, a placebo-controlled crossover trial, cetirizine hydrochloride was given at doses up to 60 mg per day, 6 times the maximum clinical dose, for 1 week, and no significant mean QTc prolongation occurred. In the second study, a crossover trial, cetirizine hydrochloride 20 mg and erythromycin (500 mg every 8 hours) were given alone and in combination. There was no significant effect on QTc with the combination or with cetirizine hydrochloride alone. In the third trial, also a crossover study, cetirizine hydrochloride 20 mg and ketoconazole (400 mg per day) were given alone and in combination. Cetirizine hydrochloride caused a mean increase in QTc of 9.1 msec from baseline after 10 days of therapy. Ketoconazole also increased QTc by 8.3 msec. The combination caused an increase of 17.4 msec, equal to the sum of the individual effects. Thus, there was no significant drug interaction on QTc with the combination of cetirizine hydrochloride and ketoconazole. In the fourth study, a placebo-controlled parallel trial, cetirizine hydrochloride 20 mg was given alone or in combination with azithromycin (500 mg as a single dose on the first day followed by 250 mg once daily). There was no significant increase in QTc with cetirizine hydrochloride 20 mg alone or in combination with azithromycin.
In a four-week clinical trial in pediatric patients aged 6 to 11 years, results of randomly obtained ECG measurements before treatment and after 2 weeks of treatment showed that cetirizine hydrochloride 5 or 10 mg did not increase QTc versus placebo. In a one week clinical trial (N=86) of cetirizine hydrochloride oral solution (0.25 mg/kg bid) compared with placebo in pediatric patients 6 to 11 months of age, ECG measurements taken within 3 hours of the last dose did not show any ECG abnormalities or increases in QTc interval in either group compare

Postmarketing Surveillance

Contingency Table:

Current Drug

Other Drugs

QT Prolongation

24008

Other ADRs

54767

38326820

Odds Ratio = 2.449

Drug Property Information

ATC Code(s):

R06AE07 - cetirizine hydrochloride

R06AE - Piperazine derivatives
R06A - ANTIHISTAMINES FOR SYSTEMIC USE
R06 - ANTIHISTAMINES FOR SYSTEMIC USE
R - RESPIRATORY SYSTEM

Active Ingredient:Cetirizine Hydrochloride

Active Ingredient UNII:64O047KTOA

Drugbank ID:DB00341

PubChem Compound:2678

CTD ID:D017332

PharmGKB:PA448905

CAS Number:83881-51-0

Dosage Form(s):solution

Route(s) Of Administrator:oral

Daily Dose:

10.0 mg/day R06AE07

Chemical Structure:

SMILE Code:
OC(=O)COCCN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=C(Cl)C=C1

Reference

1: Comparative analysis of the cardiotoxicity proclivities of second generation antihistamines in an experimental model predictive of adverse clinical ECG effects.

[Hey J A,del Prado M,Sherwood J,Kreutner W,Egan R W]
Arzneimittelforschung,1996 Feb;46(2):153-8. PMID: 8720304

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