Each film-coated tablet contains: Levocetirizine Dihydrochloride 5 mg.
Pharmacology: Pharmacokinetics: Absorption: Levocetirizine is rapidly and extensively absorbed following oral administration. Peak plasma concentrations are achieved 0.9 h after dosing. Steady state is achieved after two days. Peak concentrations are typically 270 ng/mL and 308 ng/mL following a single and a repeated 5 mg o.d. dose, respectively. The extent of absorption is dose-independent and is not altered by food, but the peak concentration is reduced and delayed.
Distribution: No tissue distribution data are available in humans, neither concerning the passage of levocetirizine through the blood-brain-barrier. In rats and dogs, the highest tissue levels are found in liver and kidneys, the lowest in the CNS compartment.
Levocetirizine is 90% bound to plasma proteins. The distribution of levocetirizine is restrictive, as the volume of distribution is 0.4 L/kg.
Metabolism: The extent of metabolism of levocetirizine in humans is less than 14 % of the dose and therefore differences resulting from genetic polymorphism or concomitant intake of enzyme inhibitors are expected to be negligible. Metabolic pathways include aromatic oxidation, N- and O-dealkylation and taurine conjugation. Dealkylation pathways are primarily mediated by CYP 3A4 while aromatic oxidation involved multiple and/or unidentified CYP isoforms. Levocetirizine had no effect on the activities of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 at concentrations well above peak concentrations achieved following a 5 mg oral dose.
Due to its low metabolism and absence of metabolic inhibition potential, the interaction of levocetirizine with other substances, or vice-versa, is unlikely.
Excretion: The plasma half-life in adults is 7.9 ± 1.9 hours. The mean apparent total body clearance is 0.63 mL/min/kg. The major route of excretion of levocetirizine and metabolites is via urine, accounting for a mean of 85.4% of the dose.
Excretion via feces accounts for only 12.9% of the dose. Levocetirizine is excreted both by glomerular filtration and active tubular secretion.
It is used in allergic rhinitis, rhinorrhoea and nasal congestion. It is also used in hay fever (seasonal allergic rhinitis) or perennial allergic rhinitis. Non-allergic rhinitis or non-eosinophilic non-allergic rhinitis.
Adults and children: 5 mg once daily.
For patients with renal impairment: 5 mg every other day or 5 mg every 3 days.
Symptoms: Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness, followed by drowsiness in children.
Treatment of Overdosage: 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 removed by haemodialysis.
Levocetirizine is contraindicated in the patients with the history of hypersensitivity to levocetirizine or any of the other constituents of the formulation.
History of hypersensitivity to levocetirizine or any of the other constituents of the formulation or to any piperazine derivatives.
Patients with severe renal impairment at less than 10 mL/min creatinine clearance.
The use of levocetirizine is not recommended in children aged less than 6 years since the currently available tablets do not yet allow dose adaptation.
Precaution is recommended with intake of alcohol.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase Deficiency or glucose-galactose malabsorption should not take this medicine.
Headache, somnolence, abdominal pain, dry mouth, fatigue, inflammation of the throat (pharyngitis), sleepiness, weakness or loss of strength (asthenia), inflammation of the lining of the nose (rhinitis) causing a blocked or runny nose and migraine.
Store at temperatures not exceeding 30°C. Protect from light.
R06AE09 - levocetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.