Trade Names:Zyrtec- Tablets 5 mg- Tablets 10 mg- Tablets, chewable 5 mg- Tablets, chewable 10 mg- Syrup 5 mg per 5 mLApo-Cetirizine (Canada)Reactine (Canada)
Competitively antagonizes histamine at the H 1 -receptor site.
Rapidly absorbed. T max is about 1 h. C max is 311 ng/mL.Food
T max is delayed 1.7 h, and C max is decreased 23%.
93% protein bound.
Cetirizine has a low degree of first-pass metabolism. It also is metabolized by oxidative O-dealkylation to an inactive metabolite.
70% is excreted in the urine (50% as unchanged drug) and 10% in the feces. The elimination half-life is 8.3 h. Cl is about 53 mL/min.
20 to 60 min.
At least 24 h.
The half-life is increased 3-fold, and Cl is decreased 70%. Dosage adjustment is recommended in those with moderate or severe impairment.Hepatic Function Impairment
The half-life is increased 50%, and Cl is decreased 40%. Dosage adjustment is recommended.Elderly
The half-life is prolonged 50%, and Cl is 40% lower. Dosage adjustment is recommended.Children
Cl is increased, and half-life is decreased.
Symptomatic relief of symptoms (eg, nasal, nonnasal) associated with seasonal and perennial allergic rhinitis; treatment of uncomplicated skin manifestations of chronic idiopathic urticaria.
Hypersensitivity to any components of the product or to hydroxyzine.
PO 5 or 10 mg/day.Children 2 to 5 yr of age
PO 2.5 mg once daily (max, 5 mg/day as 5 mg once daily or 2.5 mg every 12 h).Children 6 mo to younger than 2 yr of age
PO 2.5 mg once daily. The dose in 12 to 23 mo of age may be increased to a max dosage of 5 mg once daily or 2.5 mg every 12 h.Elderly (77 years of age and older)
PO 5 mg/day.Hepatic Impairment
PO 5 mg/day. Do not administer to children younger than 6 yr of age with hepatic function impairment.Renal ImpairmentCrCl 11 to 31 mL/min or hemodialysis
PO 5 mg/day. Do not administer to children younger than 6 yr of age with renal function impairment.
Store tablets, chewable tablets, and syrup at controlled room temperature (59° to 86°F). Syrup also can be stored in refrigerator (36° to 46°F). Keep container tightly closed.
None well documented.
May prevent or diminish otherwise positive reactions to skin tests.
Cardiac failure, hypertension, palpitation, syncope, tachycardia (less than 2%); severe hypotension (postmarketing).
Headache, somnolence (14%); fatigue (6%); dizziness (2%); aggressive reactions, convulsions, hallucinations, orofacial dyskinesia, suicidal ideation (postmarketing).
Pharyngitis (6%); epistaxis (4%).
Abdominal pain (6%); dry mouth (5%); diarrhea, nausea, vomiting (3%).
Hemolytic anemia, thrombocytopenia (postmarketing).
Cholestasis, hepatitis (postmarketing).
Coughing (4%); bronchospasm (3%).
Stillbirth, suicide (postmarketing).
Assess patient for allergy symptoms (eg, hives, itching, nasal congestion, rhinitis, sneezing, watery eyes) before starting therapy, and periodically throughout therapy.
Category B .
Excreted in breast milk.
Safety and efficacy not established in children younger than 6 mo of age.
No differences in safety were observed in patients 65 yr of age and older compared with younger patients. Studies did not include sufficient numbers of patients aged 65 yr and older to determine whether efficacy is different from younger patients.
Dosage adjustment may be needed.
Dosage adjustment may be needed.
Drowsiness, irritability, restlessness, somnolence.
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