Philcet

Light yellow coloured, circular, biconvex, film-coated tablet, plain on both the sides.
Each film-coated tablet contains: Levocetirizine 5 mg.

Pharmacology: Pharmacodynamics: Levocetirizine, the active enantiomer of cetirizine, is an antihistamine; its principal effects are mediated via inhibition of H1 receptors. The antihistaminic activity of Levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that Levocetirizine has an affinity for the human H1-receptor, 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs. 6 nmol/L, respectively). The clinical relevance of this finding is unknown.
Pharmacokinetics: Absorption: Levocetirizine is rapidly and extensively absorbed following oral administration. In adults, peak plasma concentrations are achieved 0.9 hour after dosing. The accumulation ratio following daily oral administration is 1.12 with steady state achieved after 2 days. Peak concentrations are typically 270 ng/mL and 308 ng/mL following a single and a repeated 5 mg once daily dose, respectively. Food has no effect on the extent of exposure (AUC) of the Levocetirizine tablet, but Tmax was delayed by about 1.25 hours and Cmax was decreased by about 36% after administration with a high fat meal; therefore, Levocetirizine can be administered with or without food.
Distribution: The mean plasma protein binding of Levocetirizine in vitro ranged from 91 to 92%, independent of concentration in the range of 90-5000 ng/mL, which includes the therapeutic plasma levels observed. Following oral dosing, the average apparent volume of distribution is approximately 0.4 L/kg, representative of distribution in total body water.
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 hepatic drug metabolizing 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 involves multiple and/or unidentified CYP isoforms.
Elimination: The plasma half-life in adult healthy subjects was about 8 hours and the mean oral total body clearance for Levocetirizine was approximately 0.63 mL/kg/min. The major route of excretion of Levocetirizine and its 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. Renal clearance of Levocetirizine correlates with that of creatinine clearance. In patients with renal impairment the clearance of Levocetirizine is reduced.

Levocetirizine is indicated for the symptomatic relief of allergic conditions including rhinitis & chronic urticaria.

In adults and children aged 6 years and over, Levocetirizine hydrochloride is given by mouth in a dose of 5 mg once daily. The dose should be reduced in patients with renal impairment. The recommended dose in patients with moderate renal impairment (creatinine clearance 30 to 49 mL per minute) is 5 mg every 2 days.
Special dosage instructions for specific populations: Renal and hepatic impairment: Patients who have severe impairment of kidney function must not take Levocetirizine. Patients who only have impaired liver function should take the usual prescribed dose. Patients who have both impaired liver and kidney function may be given a lower dose depending on the severity of the kidney disease, and in children the dose will also be chosen on the basis of body weight; the dose will be determined by your doctor.
Elderly patients aged 65 years and above: No adaptation of the dose is necessary in elderly patients, provided their renal function is normal.
Use in children: Levocetirizine is not recommended for children under 6 years of age.
Or as prescribed by the physician.

Symptoms of overdose may initially include agitation and restlessness, followed by drowsiness. There is no known specific antidote to Levocetirizine. Should overdose occur, symptomatic or supportive treatment is recommended.
Levocetirizine is not effectively removed by dialysis, and dialysis will be ineffective unless a dialyzable agent has been concomitantly ingested.

Patients with known hypersensitivity to Levocetirizine or any of the ingredients of Levocetirizine, or to cetirizine.
Patients with end-stage renal disease and patients undergoing dialysis.
Pediatric patients 6 to 11 years of age with impaired renal function.

Patients should be cautioned against engaging in hazardous occupations requiring complete mental alertness, and motor coordination such as operating machinery or driving a motor vehicle after ingestion of Levocetirizine. Concurrent use of Levocetirizine with alcohol or other central nervous system depressants should be avoided because additional reductions in alertness and additional impairment of central nervous system performance may occur.

Pregnancy: Levocetirizine should be used during pregnancy only if clearly needed.
Lactation: Since Levocetirizine is expected to be excreted in human milk, use of Levocetirizine in nursing mothers is not recommended.

Use of Levocetirizine has been associated with somnolence (little drowsiness), dry mouth, headache, fatigue, and asthenia (weakness).

In vitro data indicate that Levocetirizine is unlikely to produce pharmacokinetic interactions through inhibition or induction of liver drug-metabolizing enzymes. No in vivo drug-drug interaction studies have been performed with Levocetirizine. Drug interaction studies have been performed with racemic cetirizine.

Store at temperatures not exceeding 30°C. Protect from light.

Antihistamines & Antiallergics

R06AE09 - levocetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.

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