Levocetirizine Dihydrochloride
Pronouncation: (LEE-voe-se-TIR-a-zeen dye-HYE-droe-KLOR-ide)Class: Antihistamine
Trade Names:
Xyzal
- Tablets 5 mg
Pharmacology
Inhibition of H 1 receptors.
Pharmacokinetics
Absorption
Rapidly and extensively absorbed. T max is 0.9 h. C max is 270 ng/mL and 308 ng/mL after single and repeated once-daily dosing. Steady state achieved after 2 days.
Distribution
Plasma protein binding about 92%. Vd approximately 0.4 L/kg.
Metabolism
Metabolism less than 14% and by aromatic oxidation, N- and O-dealkylation, and taurine conjugation.
Elimination
The t ½ is about 8 h. Elimination 85.4% and 12.9% via urine and feces, respectively. Excreted both by glomerular filtration and active tubular transport.
Indications and Usage
Relief of symptoms associated with allergic rhinitis; treatment of uncomplicated skin manifestations of chronic idiopathic urticaria.
Contraindications
Patients with end-stage renal disease (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.
Dosage and Administration
Adults and Children 12 yr of age and olderPO 2.5 to 5 mg once daily in the evening (max, 5 mg once daily).
Children 6 to 11 yr of agePO 2.5 mg (½ tablet) once daily in the evening (max, 2.5 mg once daily).
Dose Adjustment for Renal Function ImpairmentAdults and Children 12 yr of age and older
PO Mild renal function impairment (CrCl 50 to 80 mL/min): Recommended dosage is 2.5 mg once daily. Moderate renal function impairment (CrCl 30 to 50 mL/min): Recommended dosage is 2.5 mg once every other day. Severe renal function impairment (CrCl 10 to 30 mL/min): 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.
Alcohol, CNS depressantsAdditive CNS depressant effects; concurrent use should be avoided.
RitonavirCetirizine AUC and t ½ may be increased while Cl may be decreased.
TheophyllineMay decrease cetirizine Cl.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Palpitations (postmarketing).
CNS
Somnolence (6%); fatigue (4%); aggression, agitation, convulsion (postmarketing).
Children 6 to 12 yr of agePyrexia (4%); somnolence (3%).
Dermatologic
Fixed drug eruption, pruritus, rash, urticaria (postmarketing).
EENT
Nasopharyngitis (6%); pharyngitis (2%); visual disturbances (postmarketing).
Children 6 to 12 yr of ageEpistaxis (2%).
GI
Dry mouth (3%); nausea (postmarketing).
Hepatic
Hepatitis (postmarketing).
Musculoskeletal
Myalgia (postmarketing).
Respiratory
Dyspnea (postmarketing).
Children 6 to 12 yr of ageCough (3%).
Miscellaneous
Anaphylaxis; angioneurotic edema, hypersensitivity (postmarketing).
Precautions
Pregnancy
Category B .
Lactation
Undetermined.
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 adjustments may be needed.
Overdosage
Symptoms
Drowsiness in adults, and agitation and restlessness followed by drowsiness in children.
Patient Information
- Advise the 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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