Prosp Pharma
Full Prescribing Info
Levocetirizine dihydrochloride.
Each film coated tablet contains Levocetirizine dihydrochloride 5 mg.
Pharmacology: Pharmacodynamics: Levocetirizine is the active R-enantiomer of cetirizine, second generation piperazine derivative, antagonism of histamine H1-receptors. Binding studies, levocetirizine demonstrated a 2-fold higher affinity for H1-receptors than cetirizine. Levocetirizine (at half the dosage of cetirizine) appears to be as potent as cetirizine. Comparing the effect of Levocetirizine, desloratadine, fexofenadine, and loratadine on histamine-induced wheal and flare, Levocetirizine treatment resulted to exhibit greater and more consistent inhibition of histamine-induced wheal and flare compared with other antihistamines. Following administration of a single 2.5 or 5-mg dose of levocetirizine dihydrochloride, the effects of the drug occur within 1 hour and persist for at least 24 hours.
Pharmacokinetics: Absorption: Levocetirizine is Rapidly and extensively absorbed following oral administration. In adult, peak plasma concentration are 0.9 hour after dosing. Food had no effect on the area under the plasma concentration-time curve (AUC) however, time to peak plasma concentration was decrease and delayed.
Distribution: Levocetirizine is 91-92% bound to plasma proteins. The volume of distribution is 0.4 L/kg.
Metabolism: Levocetirizine is metabolized in human less than 14% of dose. Metabolic pathway aromatic oxidation, N-dealkylation, O-dealkylation, and taurine conjugation. Levocetirizine does not inhibit cytochrome P-450 (CYP) isoenzymes 1A2, 2C9, 2C19, 2A1, 2D6, 2E1, or 3A4.
Elimination: The plasma half-life in adult is 8-9 hours. The major route of excretion is urine (85.4%) and in feces (12.9%). Levocetirizine is excreted both by glomerular filtration and active tubular secretion.
Levocetirizine is indicated for the symptoms associated with allergic condition such as: Seasonal allergic rhinitis; Perennial allergic rhinitis; Persistent allergic rhinitis; Chronic urticaria.
Dosage/Direction for Use
Adults and children 12 years and older: The recommended dose is 5 mg (1 film-coated tablet) once daily.
Patients with renal impairment: Dosage of Levocetirizine should be based on the degree of renal impairment.
Patients with hepatic impairment: No adjustment is needed in patients with hepatic impairment.
Mode of Administration: Levocetirizine is administered orally once daily, swallowed whole with liquid and may be taken without regard to meals.
Symptoms: Symptom of overdose may include drowsiness and somnolence in adult. In children resulted in minimal toxicity, agitation, restlessness and drowsiness may occur.
Management of overdose: There is no specific antidote to levocetirizine. Should be Observation and supportive care is recommended. Levocetirizine is not effectively removed by dialysis.
History of hypersensitivity to levocetirizine or any ingredient in the formulation, or to cetirizine.
Patients with end-stage renal disease (creatinine clearance less than 10 mL/minute).
This medicine may cause drowsiness, should not driving or operating machinery or working at risk of falling from a height.
Should not concomitant with alcohol or substance alcoholic ingredients.
Should not use in pregnancy in first trimester, lactation, and children under 2 years of age.
Should be use this medicine with caution with central nervous system medicine such as Benzodiazepines or antidepressant medicine.
Should be use this medicine with caution in hepatic impairment and renal impairment.
This medication may cause blur vision, confused and urinary retention.
Special Precautions
The use of this medicine is not recommended in children aged less than 6 years since the currently available film-coated tablets do not yet allow dose adaptation.
Precaution is recommended with intake of alcohol.
Caution should be taken in patients with predisposing factors of urinary retention (such as spinal cord lesion, prostatic hyperplasia) as levocetirizine may increase the risk of urinary retention.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactose deficiency or glucose-galactose malabsorption should not take this medicine.
Use In Pregnancy & Lactation
Pregnancy: Pregnancy Category B.
Lactation: Levocetirizine is expected to be distributed into milk (since cetirizine is distributed into milk).
Adverse Reactions
Patients 12 years of age and older: Nervous system disorder: Common: headache, somnolence.
Respiratory disorder: Common: Nasopharyngitis.
Gastrointestinal disorder: Common: dry mouth.
Uncommon: abdominal pain.
General disorder and administration site condition: Common: fatigue.
Uncommon: asthenia.
Pediatric patients 6–12 years of age: Nervous system disorder: Common: somnolence.
Respiratory disorder: Common: cough.
Drug Interactions
No formal drug interaction studies have been performed with levocetirizine to date; studies have been performed with racemic cetirizine.
Theophylline: Concomitant administration of cetirizine with theophylline resulted in decreased clearance (16%) of cetirizine; the disposition of theophylline was not altered.
Ritonavir: Concomitant administration of cetirizine and ritonavir, the extent of exposure to cetirizine increased to 42%.
Alcohol: Concomitant administration of cetirizine and alcohol, possible additive adverse CNS effects. Concomitant use should be avoided.
Store below 30°C.
ATC Classification
R06AE09 - levocetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.
FC tab 5 mg (white, oblong, biconvex, plain on both side) x 1 x 10's, 2 x 10's, 3 x 10's, 10 x 10's, 1 x 14's, 2 x 14's, 3 x 14's, 10 x 14's.
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