A-Z Drug Facts > Cetirizine

Cetirizine

Pronouncation: (seh-TEER-ih-zeen)
Class: Piperazine, peripherally selective

Trade Names:
Zyrtec
- Tablets 5 mg
- Tablets 10 mg
- Tablets, chewable 5 mg
- Tablets, chewable 10 mg
- Syrup 5 mg per 5 mL

Apo-Cetirizine (Canada)
Reactine (Canada)

Pharmacology

Competitively antagonizes histamine at the H ₁ -receptor site.

Pharmacokinetics

Absorption

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%.

Distribution

93% protein bound.

Metabolism

Cetirizine has a low degree of first-pass metabolism. It also is metabolized by oxidative O-dealkylation to an inactive metabolite.

Elimination

70% is excreted in the urine (50% as unchanged drug) and 10% in the feces. The t _½ is 8.3 h. Cl is about 53 mL/min.

Onset

20 to 60 minute.

Duration

At least 24 h.

Special Populations

Renal Function Impairment
Moderate impairment (Ccr 11 to 31 mL/min)

The t _½ is increased 3-fold, and Cl is decreased 70%. Dosage adjustment is recommended in those with moderate or severe impairment.

Hepatic Function Impairment

The t _½ is increased 50%, and Cl is decreased 40%. Dosage adjustment is recommended.

Elderly

The t _½ is prolonged 50%, and Cl is 40% lower. Dosage adjustment is recommended.

Children

Cl is increased, and t _½ is decreased.

Indications and Usage

Symptomatic relief of symptoms (eg, nasal, nonnasal) associated with seasonal and perennial allergic rhinitis; treatment of uncomplicated skin manifestations of chronic idiopathic urticaria.

Contraindications

Hypersensitivity to any components of the product or to hydroxyzine.

Dosage and Administration

Adults and children 6 yr of age and older

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 dose 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 Impairment
Ccr (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.)

General Advice

• Administer prescribed dose without regard to meals. Administer with food if GI upset occurs.
• Administer chewable tablets with or without water.
• Measure and administer prescribed dose of syrup using dosing spoon, syringe, or cup.

Storage/Stability

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.

Drug Interactions

None well documented.

Laboratory Test Interactions

May prevent or diminish otherwise positive reactions to skin tests.

Adverse Reactions

Cardiovascular

Palpitations, tachycardia, hypertension, cardiac failure, syncope; severe hypotension (postmarketing).

CNS

Somnolence, headache (14%); fatigue (6%); dizziness (2%); paresthesia, confusion, hyperkinesia, hypertonia, migraine, tremor, vertigo, ataxia, dystonia, abnormal coordination, hyperesthesia, hypoesthesia, myelitis, paralysis, twitching, insomnia, sleep disorder, nervousness, depression, emotional lability, impaired concentration, anxiety, depersonalization, paroniria, abnormal thinking, agitation, amnesia, decreased libido, euphoria, dysphonia, ptosis (less than 2%); convulsions, hallucinations, orofacial dyskinesia, suicidal ideation (postmarketing).

Dermatologic

Pruritus, dry skin, urticaria, acne, dermatitis, erythematous rash, increased sweating, alopecia, angioedema, furunculosis, bullous eruption, eczema, hyperkeratosis, hypertrichosis, photosensitivity reaction, maculopapular rash, seborrhea, purpura, skin disorder, skin nodule, photosensitivity toxic reaction (less than 2%).

EENT

Pharyngitis (6%); epistaxis (4%); visual field defect, earache, blindness, loss of accommodation, eye pain, conjunctivitis, xerophthalmia, glaucoma, ocular hemorrhage, tinnitus, deafness, sinusitis, nasal polyp, parosmia, ototoxicity, periorbital edema (less than 2%).

GI

Abdominal pain (6%); dry mouth (5%); nausea, diarrhea, vomiting (3%); anorexia, salivation, increased appetite, dyspepsia, flatulence, constipation, stomatitis, ulcerative stomatitis, aggravated tooth caries, tongue discoloration, tongue edema, gastritis, rectal hemorrhage, hemorrhoids, melena, eructation, enlarged abdomen, taste perversion, taste loss (less than 2%).

Genitourinary

Urinary retention, polyuria, cystitis, dysuria, UTI, hematuria, micturition frequency, urinary incontinence, dysmenorrhea, female breast pain, intermenstrual bleeding, leukorrhea, menorrhagia, vaginitis (less than 2%); glomerulonephritis (postmarketing).

Hematologic

Hemolytic anemia, thrombocytopenia (postmarketing).

Hepatic

Abnormal hepatic function (less than 2%); cholestasis, hepatitis (postmarketing).

Metabolic

Thirst, dehydration, diabetes mellitus, weight gain (less than 2%).

Musculoskeletal

Myalgia, arthralgia, arthrosis, arthritis, muscle weakness.

Respiratory

Coughing, epistaxis (4%); bronchospasm (3%); bronchitis, rhinitis, dyspnea, upper respiratory tract infection, hyperventilation, increased sputum, pneumonia, respiratory disorder (less than 2%).

Miscellaneous

Flushing, edema (face, leg, peripheral, and generalized), lymphadenopathy, back pain, malaise, fever, asthenia, rigors, pain, chest pain, leg cramps, increased weight, pallor, hot flashes (less than 2%); anaphylaxis, stillbirth, suicide (postmarketing).

Precautions

Monitor Allergy symptoms Assess patient for allergy symptoms (eg, rhinitis, nasal congestion, sneezing, itching, watery eyes, hives) before starting therapy, and periodically throughout therapy. Notify health care provider if symptoms do not improve or worsen.

Pregnancy

Category B .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established in children younger than 6 mo of age.

Renal Function

Dosage adjustment may be needed.

Hepatic Function

Dosage adjustment may be needed.

Overdosage

Symptoms

Somnolence, restlessness, irritability, drowsiness.

Patient Information

• Advise patient to take each dose without regard to meals but to take with food if stomach upset occurs.
• Advise patient or caregiver using syrup to measure and administer each dose using a dosing spoon, syringe, or cup.
• Advise patient using chewable tablet that tablet may be taken with or without water.
• Advise patient that if allergy symptoms are not controlled not to increase the dose of medication or frequency of use but to inform health care provider. Inform patient that larger doses or more frequent dosing does not increase effectiveness and may cause excessive drowsiness or other adverse reactions.
• Caution patient not to take any OTC antihistamines while taking this medication unless advised by health care provider.
• Caution patient to avoid alcohol and other CNS depressants (eg, sedatives) while using this medication.
• Caution patient that drug may cause drowsiness and to use caution driving or performing other tasks requiring mental alertness until tolerance is determined.
• Advise patient that medication may cause sensitivity to sunlight and to avoid unnecessary exposure to UV light (sunlight, tanning booths) and to use sunscreen and wear protective clothing until tolerance is determined.
• Advise patient to take frequent sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
• Advise patient having allergy skin testing not to take cetirizine for at least 4 days before the skin testing.
• Instruct patient to stop taking drug and report persistent dizziness or excessive drowsiness to health care provider.

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