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Pronunciation
(se TI ra zeen)
Generic Available (U.S.)
Yes: Excludes liquid gel capsule
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Perennial and seasonal allergic rhinitis and other allergic symptoms including urticaria; chronic idiopathic urticaria
Pregnancy Considerations
Maternal use of cetirizine has not been associated with an increased risk of major malformations. The use of antihistamines for the treatment of rhinitis during pregnancy is generally considered to be safe at recommended doses. Although safety data is limited, cetirizine may be a preferred second generation antihistamine for the treatment of rhinitis during pregnancy.
Breast-Feeding Considerations
Cetirizine is excreted into breast milk.
Contraindications
Hypersensitivity to cetirizine, hydroxyzine, or any component of the formulation
Warnings/Precautions
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns:
• Hepatic impairment: Use with caution in patients with hepatic impairment; dosage adjustment recommended.
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment recommended.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Elderly: Use with caution in the elderly; may be more sensitive to adverse effects.
Adverse Reactions
>10%: Central nervous system: Headache (children 11% to 14%, placebo 12%), somnolence (adults 14%, children 2% to 4%)
2% to 10%:
Central nervous system: Insomnia (children 9%, adults <2%), fatigue (adults 6%), malaise (4%), dizziness (adults 2%)
Gastrointestinal: Abdominal pain (children 4% to 6%), dry mouth (adults 5%), diarrhea (children 2% to 3%), nausea (children 2% to 3%, placebo 2%), vomiting (children 2% to 3%)
Respiratory: Epistaxis (children 2% to 4%, placebo 3%), pharyngitis (children 3% to 6%, placebo 3%), bronchospasm (children 2% to 3%, placebo 2%)
<2% (as reported in adults and/or children): Abdomen enlarged, accommodation loss, acne, alopecia, amnesia, anaphylaxis, angioedema, anorexia, anxiety, appetite increased, arthralgia, arthritis, arthrosis, ataxia, back pain, bilirubin increased, blindness, breast pain (female), bronchitis, bullous eruption, cardiac failure, chest pain, cholestasis, concentration impaired, confusion, conjunctivitis, constipation, coordination abnormal, cystitis, deafness, dehydration, depersonalization, depression, dermatitis, diabetes mellitus, dry skin, dysmenorrhea, dyspepsia, dysphonia, dyspnea, dysuria, earache, eczema, edema, emotional lability, eructation, erythematosus rash, euphoria, eye pain, face edema, fever, flatulence, flushing, furunculosis, fussiness, gastritis, glaucoma, glomerulonephritis, hematuria, hemolytic anemia, hemorrhoids, hepatitis, hot flashes, hyperesthesia, hyperkeratosis, hyperkinesia, hypertension, hypertonia, hypertrichosis, hyperventilation, hypoesthesia, hypotension, intermenstrual bleeding, irritability, leg cramps, leg edema, leukorrhea, libido decreased, liver enzymes elevated (transient), liver function abnormal, lymphadenopathy, maculopapular rash, melena, menorrhagia, micturition frequency, migraine, muscle weakness, myalgia, myelitis, nasal polyp, nervousness, ocular hemorrhage, orofacial dyskinesia, ototoxicity, pain, pallor, palpitation, paralysis, paresthesia, paroniria, parosmia, periorbital edema, photosensitivity, pneumonia, polyuria, pruritus, ptosis, purpura, rash, rectal hemorrhage, respiratory disorder, rhinitis, rigors, salivation increased, seborrhea, sinusitis, skin disorder, skin nodule, sleep disorder, sputum increased, stomatitis, sweating, syncope, tachycardia, taste loss, taste perversion, thinking abnormal, thirst, thrombocytopenia, tinnitus, tongue discoloration, tongue edema, tremor, twitching, ulcerative stomatitis, upper respiratory tract infection, urinary incontinence, urinary retention, urinary tract infection, urticaria, vaginitis, vertigo, visual field defect, weakness, weight gain, xerophthalmia
Postmarketing and/or case reports: Aggressive reaction, convulsions, hallucinations, hypotension (severe), suicidal ideation, suicide
Metabolism/Transport Effects
Substrate of CYP3A4 (minor), P-glycoprotein; Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Drug Interactions
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Conivaptan: May increase the serum concentration of CYP3A4 Substrates (Low risk). Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification
P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
Storage
Store at room temperature.
Syrup: Store at room temperature of 15°C to 30°C (59°F to 86°F), or under refrigeration at 2°C to 8°C (36°F to 46°F).
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 action: Suppression of skin wheal and flare: 0.7 hours (Simons, 1999)
Duration of action: Suppression of skin wheal and flare: ≥24 hours (Simons, 1999)
Absorption: Rapid
Distribution: 0.56 L/kg (Simons, 1999)
Protein binding, plasma: Mean: 93%
Metabolism: Limited hepatic
Half-life elimination: 8 hours
Time to peak, serum: 1 hour
Excretion: Urine (70%); feces (10%)
Dosage
Oral:
Children:
6-12 months: Chronic urticaria, perennial allergic rhinitis: 2.5 mg once daily
12 months to <2 years: Chronic urticaria, perennial allergic rhinitis: 2.5 mg once daily; may increase to 2.5 mg every 12 hours if needed
2-5 years: Chronic urticaria, perennial or seasonal allergic rhinitis: Initial: 2.5 mg once daily; may be increased to 2.5 mg every 12 hours or 5 mg once daily
Children ≥6 years and Adults: Chronic urticaria, perennial or seasonal allergic rhinitis: 5-10 mg once daily, depending upon symptom severity
Elderly: Initial: 5 mg once daily; may increase to 10 mg/day. Note: Manufacturer recommends 5 mg/day in patients ≥77 years of age.
Dosage adjustment in renal/hepatic impairment:
Children <6 years: Cetirizine use not recommended
Children 6-11 years: <2.5 mg once daily
Children ≥12 and Adults:
Clcr 11-31 mL/minute, hemodialysis, or hepatic impairment: Administer 5 mg once daily
Clcr <11 mL/minute, not on dialysis: Cetirizine use not recommended
Administration: Oral
May be administered with or without food.
Monitoring Parameters
Relief of symptoms, sedation and anticholinergic effects
Test Interactions
May cause false-positive serum TCA screen. May suppress the wheal and flare reactions to skin test antigens.
Dietary Considerations
May be taken with or without food.
Patient Education
Avoid use of alcohol. You may experience drowsiness, dizziness, or dry mouth. Report persistent sedation, confusion, agitation, persistent nausea or vomiting, blurred vision, or lack of improvement or worsening of condition.
Geriatric Considerations
Adjust dose for renal function. Because of its OTC status, counsel patients on appropriate use.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia and increased salivation (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness is common; may cause abnormal thinking, agitation, amnesia, anxiety, depersonalization, depression, emotional lability, euphoria, impaired concentration, insomnia, nervousness, paroniria, and sleep disturbances. May also cause aggressive reactions.
Mental Health: Effects on Psychiatric Treatment
Concurrent use with psychotropics may produce additive sedation
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, liquid gel, oral, as hydrochloride:
ZyrTEC® Allergy: 10 mg
Solution, oral, as hydrochloride: 5 mg/5 mL (5 mL)
Syrup, oral, as hydrochloride: 5 mg/5 mL (5 mL, 118 mL, 120 mL, 473 mL, 480 mL)
ZyrTEC® Children's Allergy: 5 mg/5 mL (118 mL) [contains propylene glycol; grape flavor]
ZyrTEC® Children's Allergy: 5 mg/5 mL (118 mL) [dye free, sugar free; contains propylene glycol, sodium benzoate; bubblegum flavor]
ZyrTEC® Children's Hives Relief: 5 mg/5 mL (118 mL) [contains propylene glycol; grape flavor]
Tablet, oral, as hydrochloride: 5 mg, 10 mg
All Day Allergy: 10 mg
ZyrTEC® Allergy: 10 mg
Tablet, chewable, oral, as hydrochloride: 5 mg, 10 mg
All Day Allergy: 5 mg [fruit flavor]
ZyrTEC® Children's Allergy: 5 mg, 10 mg [grape flavor]
Pricing: U.S. (www.drugstore.com)
Syrup (Cetirizine HCl Childrens Alrgy)
1 mg/mL (118): $15.99
Tablets (Cetirizine HCl)
5 mg (100): $99.99
10 mg (100): $18.99
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.
Dasgupta A, Wells A, and Datta P, “False-Positive Serum Tricyclic Antidepressant Concentrations Using Fluorescence Polarization Immunoassay due to the Presence of Hydroxyzine and Cetirizine,” Ther Drug Monit, 2007, 29(1):134-9.
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.
International Brand Names
Lexi-Comp.com
Last full review/revision March 2012
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