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Levocetirizine Dihydrochloride

Pronunciation

Pronunciation: LEE-voe-se-TIR-i-zeen dye-HYE-droe-KLOR-ide
Class: Antihistamine

Trade Names

Xyzal
- Tablets 5 mg
- Solution, oral 0.5 mg/mL

Pharmacology

Inhibition of H 1 receptors.

Slideshow: Top Prevention Tips - Seasonal Allergies

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 approximately 1.25 h and decreased C max by approximately 36%.

Distribution

Plasma protein binding is approximately 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

Renal Function Impairment

Dosage should be reduced in patients with renal function impairment.

Hepatic Function Impairment

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

Elderly

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.

Children

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

Gender

Half-life was slightly shorter in women than in men; however, the body weight–adjusted oral Cl in women appears to be comparable with that in men.

Race

Pharmacokinetics are similar among racial groups.

Indications and Usage

Relief of symptoms associated with seasonal and perennial 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 impairment; hypersensitivity to any component of the product or to certirizine.

Dosage and Administration

Seasonal Allergic Rhinitis
Adults and Children 12 yr of age and older

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

Children 6 to 11 yr of age

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

Children 2 to 5 yr of age

1.25 mg (½ teaspoon oral solution) once daily in the evening (max, 1.25 mg once daily).

Perennial Allergic Rhinitis/Chronic Idiopathic Urticaria
Adults and Children 12 yr of age and older

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

Children 6 to 11 yr of age

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

Children 6 mo to 5 yr of age

PO 1.25 mg (½ teaspoon oral solution) once daily in the evening (max, 1.25 mg once daily).

Dose Adjustment for Renal Function Impairment
Adults and Children 12 yr of age and older

PO

Mild renal function impairment (CrCl 50 to 80 mL/min)

2.5 mg once daily.

Moderate renal function impairment (CrCl 30 to 50 mL/min)

2.5 mg once every other day.

Severe renal function impairment (CrCl 10 to 30 mL/min)

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

ESRD (CrCl less than 10 mL/min)

Do not administer.

General Advice

  • May be taken without respect to food.
  • Measure and administer prescribed dose of oral solution using dosing syringe, dosing spoon, or dosing cup.

Storage/Stability

Store at 68° to 77°F; excursions permitted between 59° and 86°F.

Drug Interactions

No formal in vivo drug-drug interaction studies have been performed with levocetirizine. Drug interaction studies have been performed with racemic cetirizine.

Alcohol, CNS depressants

Additive CNS depressant effects; concurrent use should be avoided.

Food

Food had no effect on the extent of levocetirizine exposure; however, the half-life was delayed about 1.25 hours and the C max was decreased about 36% after administration with a high-fat meal. Levocetirizine may be taken without regard to food.

Ritonavir

Cetirizine AUC and half-life may be increased, while Cl may be decreased. The risk of adverse reactions may be increased.

Theophylline

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%); otitis media (3%); epistaxis, pharyngitis (2%); visual disturbances (postmarketing).

GI

Diarrhea, vomiting (4%); 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 reported to be excreted in breast milk.

Children

Safety and efficacy not established in children younger than 2 yr of age for the treatment of seasonal allergic rhinitis or in children younger than 6 mo of age for the treatment of perennial allergic rhinitis and chronic idiopathic urticaria.

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 of 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 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.

Copyright © 2009 Wolters Kluwer Health.

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