Levocetirizine dihydrochloride.
Each film coated tablet contains: Levocetirizine Dihydrochloride 5 mg as an antihistaminic and anti-allergic.
Colour: Titanium Dioxide BP.
Excipients/Inactive Ingredients: Microcrystalline Cellulose BP, Maize Starch BP, Calcium Hydrogen Phosphate BP, Purified Talc BP, Colloidal Anhydrous Silica BP, Magnesium Stearate BP, Hypromellose BP (Hydroxy Propyl Methyl Cellulose), Isopropyl Alcohol BP, Dichloromethane BP, Titanium Dioxide BP, Polyethylene Glycol -400 NF and Purified Water BP.
Pharmacology: Pharmacodynamics: Mechanism of Action: The second-generation H1-receptor antagonist cetirizine is a racemate, consisting of equal quantities of two enantiomers, levocetirizine [(R)-enantiomer] and dextrocetirizine [(S)-enantiomer]. In vitro and human pharmacodynamic studies (histamine-induced cutaneous and nasal responses) have provided evidence that levocetirizine is the more active enantiomer, accounting for most or all clinical antihistaminic activity of racemic cetirizine; this activity of levocetirizine is seen at half the dose of cetirizine.
In one in-vitro study, levocetirizine exhibited a 2-fold higher affinity for human H1-receptors than cetirizine, and was about 10-fold more potent than the (S)-enantiomer; levocetirizine dissociated more slowly from the H1-receptor than the (S)-enantiomer.
Oral levocetirizine 5 milligrams (mg) was reported more effective than oral loratadine 10 mg in preventing histamine-induced cutaneous responses (i.e. wheal, flare) in a small double-blind, pharmacodynamic study involving healthy subjects.
Racemic cetirizine [Zyrtec(R)], a metabolite of hydroxyzine, is a selective H1-antagonist which has shown efficacy in allergic rhinitis and chronic urticaria, with a relatively low propensity for adverse effects. No advantage of levocetirizine over racemic cetirizine was observed in pharmacodynamic comparisons in healthy subjects.
Pharmacokinetics: Levocetirizine is well-absorbed after single oral doses, with peak plasma levels occurring in about 1 hour; a volume of distribution of 0.3 L / kg and clearance of 0.6 ml / min / kg were reported. Similar to racemic cetirizine, hepatic metabolism is minimal, and most of a dose is excreted unchanged in the urine. A plasma elimination half-life of 7 hours has been reported after a single dose. Multiple-dose pharmacokinetic data are unavailable.
Toxicology: Preclinical Safety Data: Preclinical Data reveal no special hazard for humans based on conventional studies of pharmacology, repeated dose toxicity, genotoxicity and carcinogenic potential.
Levocetirizine is indicated for: the relief of nasal and ocular symptoms of seasonal and perennial allergic rhinitis; the relief of symptoms of chronic idiopathic urticaria.
Posology: Adults and children 12 years of age and older: The recommended dose of Levocetirizine is 5mg (1tablet) once daily in the evening.
Children 6 to 11 years of age: The recommended dose is 2.5mg (½ tablet) once daily in the evening.
In patients with both hepatic and renal impairment, adjustment of the dose is recommended.
LEVOCETIRIZINE IS NOT INDICATED FOR CHILDREN UNDER 6 YEARS OF AGE.
ROUTE OF ADMINISTRATION: Oral.
Overdose: Symptoms observed after an overdose of Levocetirizine are mainly associated with CNS effects or with effects that could suggest an anticholinergic effect.
Adverse events reported after an intake of at least 5 times the recommended daily dose are: confusion, diarrhoea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, restlessness, sedation, somnolence, stupor, tachycardia, tremor and urinary retention.
Management of overdose: There is no known specific antidote to Levocetirizine. Should overdose occur, symptomatic or supportive treatment is recommended. Gastric lavage should be considered following ingestion of a short occurrence. Levocetirizine is not effectively removed by dialysis.
Cetriliv is contraindicated in patients hypersensitive to Levocetirizine or any of its ingredients or to cetirizine. It is contraindicated in patients with severe renal impairment at less than 10 ml / min creatinine clearance.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose- galactose malabsorption should not take Levocetirizine Tablets.
Caution should be exercised when driving a car or operating potentially dangerous machinery. Concurrent use of Levocetirizine with alcohol or other CNS depressants should be avoided. Use of Levocetirizine in nursing mothers is not recommended. The use of Levocetirizine Dihydrochloride is not recommended in children aged less than 6 years.
Effects on Ability to Drive and Use Machines: Patients intending to drive, engaging in potentially hazardous activities or operating machinery should not exceed the recommended dose and should take their response to the medicinal product into account.
In these sensitive patients, concurrent use with alcohol or other CNS depressants may cause additional reduction in alertness and impairment of performance.
Very rare clinical data on exposed pregnancies are available. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development. Caution should be exercised when prescribing to pregnant or breast feeding women because Levocetirizine passes into breast milk.
Headache and fatigue have been reported occasionally. Skin rash has been reported rarely.
No clinically significant drug interactions have been found with theophylline at a low dose, azithromycin, pseudoephedrine, ketoconazole or erythromycin. There was a small decrease in the clearance of cetirizine caused by a 400 mg dose of theophylline; it is possible that larger theophylline doses could have a greater effect. The extent of absorption of Levocetirizine is not reduced with food, although the rate of absorption is decreased.
Store at a temperature not exceeding 30°C. Protect from light & moisture.
Shelf life: 36 Months from the date of manufacturing.
R06AE09 - levocetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.
FC tab 5 mg (white, circular, biconvex, plain on both sides) x 2 x 5 x 10's.
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