Each film-coated tablet contains Levocetirizine dihydrochloride 5 mg.
Pharmacology: Pharmacodynamics: Mechanism of action: Levocetirizine is the active R-enantiomer of cetirizine, a second generation antihistamine. The drug is selective antagonism of histamine H1-receptors and as a group, is less sedating.
Pharmacokinetics: Levocetirizine is rapidly and extensively absorbed following oral administration, with peak plasma concentration usually attained in 0.9 hour. A high-fat meal reduces peak plasma concentration by about 36% and delays time to peak plasma concentration by about 1.25 hours, but does not affect AUC. The average apparent volume of distribution is 0.4 L/kg. Levocetirizine is approximately 91-92% bound to plasma proteins (mainly albumin). The extent of metabolism of levocetirizine is less than 14% of dose by aromatic oxidation, N-dealkylation, O-dealkylation and taurine conjugation. Levocetirizine is excreted in urine; 85.4% (via glomerular filtration and active tubular secretion) and excreted in the feces 12.9%. The elimination half-life is 8-9 hours in adults.
Levocetirizine is indicated for the treatment of symptoms associated with seasonal allergic rhinitis, perennial allergic rhinitis and chronic urticaria.
Recommended Dose: Adults and children 12 years of age and older:
1 tablet once daily.
Children 6-11 years of age:
½ tablet once daily.
Patients with renal function impairment: The following applies to adults and children 12 years of age and older.
Dosing adjustments for patients with impaired renal function: see table.
Click on icon to see table/diagram/image
Patients with hepatic impairment:
No dosage adjustment is necessary in patients with hepatic impairment.
Mode of Administration:
Levocetirizine dihydrochloride is administered orally once daily without regard to meals.
Symptoms: Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness, followed by drowsiness in children.
Treatment: There is no known specific antidote to levocetirizine. Should overdose occur, symptomatic or supportive treatment is recommended. Gastric lavage should be considered following short-term ingestion. Levocetirizine is not effectively remove by haemodialysis.
Levocetirizine is contraindicated in patients who are hypersensitive to levocetirizine or any ingredient in the formulation or to cetirizine.
Levocetirizine is contraindicated in patients with in end-stage renal disease (creatinine clearance less than 10 mL/min) or undergoing hemodialysis.
Levocetirizine is contraindicated in children 6 months to 11 years of age with renal impairment.
Patients should be advised to avoid performing hazardous activities requiring complete mental alertness or physical coordination (e.g., operating machinery, driving a motor vehicle) following use of levocetirizine.
Concomitant use of levocetirizine with alcohol or other CNS depressants should be avoided.
Use with caution in patients with predisposing factors of urinary retention (eg, spinal cord lesion, prostatic hyperplasia) as levocetirizine may increase the risk of urinary retention. Discontinue if urinary retention occurs.
Pregnancy Category B. Safety for use drug pregnancy has not been established.
Levocetirizine is expected to be distributed into milk (since cetirizine is distributed into milk). The use of levocetirizine in breast-feeding mother is not recommended.
Constipation (infants 6.7%, children 0.9%), diarrhea (infants 13.3%, children 3.5%), painful teething (infants 6.7%, children 1.8%).
Asthenia (2.3%), somnolence (infants 4.4%, children 3%, adults 5%-6%).
Nasopharyngitis (4%-6%), pharyngitis (1% to 2%), xerostomia (2%-3%).
Fatigue (1%-4%), fever (children 4%-4.4%).
No interaction studies have been performed with levocetirizine (including no studies with CYP3A4 inducers); studies with the racemate compound cetirizine demonstrated that there were no clinically relevant adverse interactions (with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam).
Concomitant administration of cetirizine and ritonavir may increase the AUC and half-life and decreased the clearance of cetirizine; the disposition of ritonavir was not altered.
Concomitant use of cetirizine and theophylline resulted in decrease clearance (16%) of cetirizine; the disposition of theophylline was not altered.
Store at a temperature below 30°C.
R06AE09 - levocetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.
FC tab 5 mg (biconvex, oval white. One side has score and has letter "L" and "C" on each side. Another side has figure "5") x 1 x 10's.