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Cetirizine
Pronunciation
U.S. Brand Names
Generic Available
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Monitoring Parameters
Mental Health: Effects on Mental Status
Mental Health: Effects on Psychiatric Treatment
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Dosage Forms
References

Pronunciation
(se TI ra zeen)

U.S. Brand Names
Zyrtec®

Generic Available

No


Synonyms
Cetirizine Hydrochloride; P-071; UCB-P071

Pharmacological Index

Antihistamine


Use

Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria


Pregnancy Risk Factor

B


Contraindications

Hypersensitivity to cetirizine, hydroxyzine, or any component


Warnings/Precautions

Cetirizine should be used cautiously in patients with hepatic or renal dysfunction and the elderly. Use in breast-feeding women is not recommended. Doses >10 mg/day may cause significant drowsiness


Adverse Reactions

>10%: Central nervous system: Headache has been reported to occur in 10% to 12% of patients, drowsiness has been reported in as much as 26% of patients on high doses

1% to 10%:

Central nervous system: Somnolence, fatigue, dizziness

Gastrointestinal: Xerostomia

<1%: Depression


Overdosage/Toxicology

Symptoms of overdose include seizures, sedation, hypotension. There is no specific treatment for an antihistamine overdose, however, most of its clinical toxicity is due to anticholinergic effects

Anticholinesterase inhibitors may be useful by reducing acetylcholinesterase. For anticholinergic overdose with severe life-threatening symptoms, physostigmine 1-2 mg (0.5 mg or 0.02 mg/kg for children) I.V., slowly may be given to reverse these effects.


Drug Interactions

Increased toxicity: CNS depressants, anticholinergics


Mechanism of Action

Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract


Pharmacodynamics/Kinetics

Onset of effect: Within 15-30 minutes

Absorption: Oral: Rapid

Metabolism: Exact fate is unknown, limited hepatic metabolism

Half-life: 8-11 hours

Time to peak serum concentration: Within 30-60 minutes


Usual Dosage

Children greater than or equal to 6 years and Adults: Oral: 5-10 mg once daily, depending upon symptom severity


Monitoring Parameters

Relief of symptoms, sedation and anticholinergic effects


Mental Health: Effects on Mental Status

Drowsiness is common


Mental Health: Effects on Psychiatric Treatment

Concurrent use with psychotropics may produce additive sedation


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

No effects or complications reported


Patient Information

Take as directed; do not exceed recommended dose. Avoid use of other depressants, alcohol, or sleep-inducing medications unless approved by prescriber. You may experience drowsiness or dizziness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or dry mouth, (frequent small meals, frequent mouth care, chewing gum, or sucking hard candy may help). Report persistent sedation, confusion, or agitation; persistent nausea or vomiting; changes in urinary pattern; blurred vision; chest pain or palpitations; or lack of improvement or worsening or condition. Breast-feeding precautions: Breast-feeding is not recommended.


Dosage Forms

Syrup, as hydrochloride: 5 mg/5 mL (120 mL)

Tablet, as hydrochloride: 5 mg, 10 mg


References

Allegra L, Paupe J, Wieseman HG, et al, "Cetirizine for Seasonal Allergic Rhinitis in Children Aged 2-6 Years. A Double-Blind Comparison With Placebo," Pediatr Allergy Immunol, 1993; 4:157-61.

Barnes CL, McKenzie CA, Webster KD, et al, "Cetirizine: A New, Nonsedating Antihistamine," Ann Pharmacother, 1993; 27:464-70.

Kaiser HB, "Cetirizine in Allergic Rhinitis," Pediatr Allergy Immunol, 1993; 4(Suppl):44-6.

Ramaekers JG, Uiterwijk MM, and O'Hanlon J, "Effects of Loratadine and Cetirizine on Actual Driving and Psychometric Test Performance, and EEG During Driving," Eur J Clin Pharmacol, 1992; 42:363-9.


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