Cetirizine Hydrochloride

Allergic Rhinitis

Self-medication for symptomatic relief of rhinorrhea, sneezing, lacrimation, itching eyes, and/or oronasopharyngeal itching associated with seasonal (e.g., hay fever) allergic rhinitis or other upper respiratory allergies.1 2 3 12 20 25 26 27 42 46 49 62 63 68 69 70 71

Symptomatic relief of perennial (nonseasonal) allergic rhinitis.1

May be used alone or in fixed combination with pseudoephedrine hydrochloride;1 63 69 use fixed-combination preparation only when both antihistamine and nasal decongestant activity are needed concurrently.63

Chronic Idiopathic Urticaria

Self-medication for symptomatic relief of pruritus associated with chronic idiopathic urticaria (e.g., hives);1 2 3 12 20 28 29 46 72 not for prevention of chronic idiopathic urticaria or allergic skin reactions.72

Contraindications

• Known hypersensitivity to cetirizine, hydroxyzine, or any ingredient in the formulation.1 3 63 68 69 70 71 72

Warnings/Precautions

General Precautions

Ensure accuracy of prescription; similarities in spelling, dosage intervals, and tablet strengths of Zyrtec and Zyprexa (olanzapine, an atypical antipsychotic agent) may result in errors.65

Risk of somnolence;1 2 3 5 6 27 28 39 41 42 43 49 caution required when performing hazardous activities requiring mental alertness or physical coordination (e.g., operating machinery, driving a motor vehicle).1 3 (See Specific Drugs under Interactions.)

When used in fixed combination with pseudoephedrine hydrochloride (e.g., Zyrtec-D), consider the cautions, precautions, and contraindications associated with pseudoephedrine.63 69

Specific Populations

Chewable or conventional tablets or oral solution: Category B.1

Fixed-combination cetirizine hydrochloride/pseudoephedrine hydrochloride: Category C.63

Distributed into milk.1 63 Use not recommended.1 3 57 63 68 69 70 71 72

Chewable or conventional tablets or oral solution: Safety and efficacy not established in children <6 months of age; oral solution is the recommended formulation in children <2 years of age.1

Fixed-combination cetirizine hydrochloride/pseudoephedrine hydrochloride: Safety and efficacy not established in children <12 years of age; use not recommended in this age group.63

Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection.66 67 Clinicians should ask caregivers about use of nonprescription cough and cold preparations to avoid overdosage.

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.1 No overall differences in safety relative to younger patients, but increased sensitivity cannot be ruled out.1

Select dosage with caution because of age-related decreases in renal function; periodic monitoring of renal function recommended.1 3 20 39 46 Dosage adjustment recommended in patients ≥65 years of age.1 (See Geriatric Patients under Dosage and Administration.)

Decreased clearance in patients with chronic hepatic impairment.1 3 20 39 Dosage adjustment necessary.1 3 (See Hepatic Impairment under Dosage and Administration.)

Use not recommended in children <6 years of age with hepatic impairment.1

Decreased clearance in patients with moderate renal impairment (Clcr of 11–31 mL/minute) or in those on hemodialysis.1 3 20 46 60 Dosage adjustment necessary.1 (See Renal Impairment under Dosage and Administration.)

Use not recommended in children <6 years of age with renal impairment.1

Common Adverse Effects

Adults and children ≥12 years of age: Somnolence, fatigue, dry mouth.1 Insomnia reported with cetirizine hydrochloride-pseudoephedrine hydrochloride fixed combination.63

Children 2–11 years of age: Headache, pharyngitis, abdominal pain.1

Children 6 months to 2 years of age: Irritability, fussiness, insomnia, fatigue, malaise.1

Metabolized minimally in the liver.2 May have low potential for adverse drug interactions associated with metabolic enzyme systems.2

Drugs Affecting Hepatic Microsomal Enzymes

Concomitant administration with drugs known to inhibit CYP microsomal enzymes has not been associated with clinically important changes in ECG parameters (e.g., QTc intervals).1 3 31 56

Specific Drugs

Storage

Oral

20–25°C (may be exposed to 15–30°C).1 63 68 71 72

20–25°C (may be exposed to 15–30°C).1 Also may be refrigerated at 2–8°C.1

• Exhibits selective antagonism of peripheral histamine H1-receptors.1 2 3 6 14 20 47 48

• Antihistaminic effect is comparable to that of astemizole (no longer commercially available in the US), clemastine, chlorpheniramine, diphenhydramine, hydroxyzine, loratadine, pyrilamine, and terfenadine (no longer commercially available in the US).2 3 20 43 Tolerance to antihistaminic effect usually does not occur.2

• No appreciable anticholinergic or antiserotonergic effects in animal models,56 57 but dry mouth more common with cetirizine than placebo in clinical trials.1 3 20 28 41 49