Levocetirizine Dihydrochloride

Trade Names:
Xyzal
- Tablets 5 mg
- Solution, oral 2.5 mg per 5 mL

Pharmacology

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Inhibition of H ₁ receptors.

Pharmacokinetics

Absorption

Rapidly and extensively absorbed. T _max is 0.9 h. C _max is 270 and 308 ng/mL after single and repeated once-daily dosing, respectively. Steady state achieved after 2 days. Food delayed T _max by about 1.25 h and decreased C _max by 36%.

Distribution

Plasma protein binding is about 92%. Vd is approximately 0.4 L/kg.

Metabolism

Metabolism is less than 14% and by aromatic oxidation, N- and O-dealkylation, and taurine conjugation.

Elimination

The half-life is about 8 to 9 h. Elimination is 85.4% and 12.9% via urine and feces, respectively. Excreted both by glomerular filtration and active tubular secretion.

Special Populations

Dosage should be reduced in patients with renal function impairment.

Has not been studied; however, since levocetirizine is primarily excreted unchanged by the kidneys, it is unlikely that the Cl will be decreased in patients with hepatic function impairment.

Pharmacokinetic data are limited. Total body Cl was approximately 33% lower in 9 elderly subjects, compared with younger adults. Adjust dose in accordance with renal function.

In children 6 to 11 years of age, C _max and AUC values were about 2-fold greater than in adults. Total body clearance was 30% greater and elimination half-life was 24% shorter when compared with adults.

Pharmacokinetics are similar between men and women.

Pharmacokinetics are similar among racial groups.

Indications and Usage

Relief of symptoms associated with allergic rhinitis; treatment of uncomplicated skin manifestations of chronic idiopathic urticaria.

Contraindications

Patients with ESRD (CrCl less than 10 mL/min) and patients undergoing hemodialysis; children 6 to 11 yr of age with renal function impairment; hypersensitivity to any component of the product or to certirizine.

Dosage and Administration

PO 2.5 to 5 mg once daily in the evening (max, 5 mg once daily).

PO 2.5 mg (½ tablet or 1 teaspoon oral solution) once daily in the evening (max, 2.5 mg once daily).

PO Mild renal function impairment (CrCl 50 to 80 mL/min): Recommended dosage is 2.5 mg once daily.

Recommended dosage is 2.5 mg once every other day.

Recommended dosage is 2.5 mg twice weekly, separated by 3 to 4 days.

General Advice

• May be taken without respect to food.

Storage/Stability

Store at 68° to 77°F.

Drug Interactions

Studies performed with racemic cetirizine.

Additive CNS depressant effects; avoid concurrent use.

Cetirizine AUC and half-life may be increased while Cl may be decreased.

May decrease cetirizine Cl.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations (postmarketing).

CNS

Somnolence (6%); fatigue, pyrexia (4%); aggression, agitation, convulsion (postmarketing).

Dermatologic

Fixed drug eruption, pruritus, rash, urticaria (postmarketing).

EENT

Nasopharyngitis (6%); epistaxis, pharyngitis (2%); visual disturbances (postmarketing).

GI

Dry mouth (3%); nausea (postmarketing).

Hepatic

Hepatitis (postmarketing).

Musculoskeletal

Myalgia (postmarketing).

Respiratory

Cough (3%); dyspnea (postmarketing).

Miscellaneous

Anaphylaxis, angioneurotic edema, hypersensitivity (postmarketing).

Precautions

Pregnancy

Category B .

Lactation

Undetermined; however, cetirizine has been been reported to be excreted in breast-milk.

Children

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

Elderly

Use with caution, usually starting at the low end of the dosage range, because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Renal Function

Dosage should be reduced in patients with renal function impairment.

Hazardous Tasks

Patients should avoid engaging in hazardous tasks requiring complete mental alertness and motor coordination, such as operating machinery or driving a motor vehicle.

Overdosage

Symptoms

Drowsiness in adults; agitation and restlessness followed by drowsiness in children.

Patient Information

• Advise patient that drug may cause drowsiness or impaired judgment or thinking skills, and to use caution while driving, riding a bike, or performing other tasks requiring mental alertness.
• Advise patients to avoid alcohol or other CNS depressants because additional reduction in alertness may occur.

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