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Pronunciation |
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(se
TI ra
zeen) |
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U.S. Brand
Names |
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Zyrtec® |
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Generic
Available |
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No |
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Synonyms |
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Cetirizine Hydrochloride; P-071; UCB-P071 |
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Pharmacological Index |
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Antihistamine |
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Use |
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Perennial and seasonal allergic rhinitis and other allergic symptoms
including urticaria |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to cetirizine, hydroxyzine, or any
component |
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Warnings/Precautions |
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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 |
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Adverse
Reactions |
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>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 |
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Overdosage/Toxicology |
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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. |
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Drug
Interactions |
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Increased toxicity: CNS depressants, anticholinergics |
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Mechanism of
Action |
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Competes with histamine for H1-receptor sites on effector cells in
the gastrointestinal tract, blood vessels, and respiratory
tract |
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Pharmacodynamics/Kinetics |
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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 |
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Usual Dosage |
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Children greater than or equal to 6 years and Adults: Oral: 5-10 mg once
daily, depending upon symptom severity |
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Monitoring
Parameters |
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Relief of symptoms, sedation and anticholinergic effects |
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Mental Health: Effects
on Mental Status |
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Drowsiness is common |
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Mental Health:
Effects on Psychiatric
Treatment |
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Concurrent use with psychotropics may produce additive
sedation |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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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. |
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Dosage Forms |
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Syrup, as hydrochloride: 5 mg/5 mL (120 mL)
Tablet, as hydrochloride: 5 mg, 10 mg |
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References |
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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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