RiteMED Levocetirizine

RiteMED Levocetirizine

levocetirizine

Manufacturer:

RiteMED

Distributor:

United Lab
Full Prescribing Info
Contents
Levocetirizine dihydrochloride.
Description
Each film-coated tablet contains: Levocetirizine dihydrochloride 5 mg.
Action
Pharmacology: Pharmacodynamics: Levocetirizine, the active enantiomer or cetirizine, is a second generation antihistamine. It selectively antagonizes histamine H1-receptors. In vitrostudies have shown that levocetirizine has twice the H1-receptor affinity of cetirizine.
Levocetirizine (at half of cetirizine dosage) appears to be as potent as cetirizine in inhibiting histamine-induced sneezing, increased nasal airway resistance, and skin wheal and flare. Compared with other antihistamines (e.g., desloratadine, fexofenadine, loratadine), it exhibits greater and more consistent inhibition of histamine-induced wheal and flare.
Pharmacokinetics: Levocetirizine is rapidly and extensively absorbed after oral administration. Peak plasma concentrations are seen at 0.5 hours for oral solution and 0.9 hour for tablets following oral administration. Food has no effect on the extent of exposure of levocetirizine, but time to peak plasma concentration is delayed by approximately 1.25 hours and peak plasma concentration is decreased by approximately 36% after administration with a high fat meal. Levocetirizine can, therefore, be administered with or without food.
No tissue distribution data are available in humans, neither concerning the passage of levocetirizine through the blood-brain barrier. Levocetirizine is 90% bound to plasma proteins. The apparent volume of distribution is approximately 0.4 L/kg.
In humans, the extent of levocetirizine metabolism is less than 14% of the dose. 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. Due to its low metabolism and absence of metabolic inhibition potential, the interaction of levocetirizine with other substances, or vice-versa is unlikely.
The plasma elimination half-life of levocetirizine is approximately 8 to 9 hours following oral administration. Mean oral total body clearance is approximately 0.63 mL/kg/min. The major route of excretion of levocetirizine and its metabolites is via urine, accounting for a mean 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.
Indications/Uses
Allergic rhinitis: For the relief of symptoms associated with seasonal and perennial allergic rhinitis.
Chronic idiopathic urticaria: For the treatment of uncomplicated skin manifestations of chronic idiopathic urticaria.
Dosage/Direction for Use
Adults and children ≥12 years old: Orally, 1 tablet once a day, at bedtime, or, as prescribed by a physician.
Dosage in Patients with Renal Impairment: For adults and children 12 years old and above, dosage adjustment should be done according to the degree of renal impairment as follows:

Click on icon to see table/diagram/image

Dosage in Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with solely hepatic impairment.
Overdosage
Symptoms of levocetirizine overdose in adults may include drowsines. In children, symptoms are initially agitation and restlessness, followed by drowsiness. No specific antidote is known and overdose is addressed by symptomatic or supportive treatment. Following short-term ingestion, gastric lavage may be considered. Dialysis may be ineffective unless a dialyzable agent was concomitantly ingested.
Contraindications
Hypersensitivity to levocetirizine, cetirizine, other piperazine derivatives, or to any component of the product.
Patients with end-stage renal disease (creatinine clearance <10 mL/min) or undergoing hemodialysis.
Children 6 months up to 11 years of age with renal impairment.
Breastfeeding.
Special Precautions
Patients with predisposing factors of urinary retention (e.g., spinal cord lesion, prostatic hyperplasia) should use levocetirizine with caution.
Concomitant use of levocetirizine with alcohol or other central nervous system (CNS) depressants should be avoided (see Interactions).
Caution should be observed in epileptic patients at risk of convulsions.
Levocetirizine should only be used during pregnancy when clearly needed.
Renal Impairment: Levocetirizine is mainly excreted by the kidneys and the risk of adverse effects may be greater in patients with renal impairment (see Dosage & Administration).
Effects on Ability to Drive and Use Machine: Somnolence, fatigue and asthenia are associated with levocetirizine treatment. Patients should exercise caution when performing hazardous activities requiring mental alertness and physical coordination (e.g., driving, operating machinery).
Use in the Elderly: Clinical experience with levocetirizine has not identified differences in responses between the elderly patients, usually starting at the lowest dose should be carefully selected for elderly patients, usually starting at the lowest dose due to greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.
Use In Pregnancy & Lactation
Pregnancy: Pregnancy Category B. There are no adequate and well-controlled studies in pregnant women. Levocetirizine should only be used during pregnancy when clearly needed.
Lactation: The use of levocetirizine is not recommended in breastfeeding women as it is possibly distributed into milk (cetirizine is distributed into milk).
Adverse Reactions
The most frequently reported adverse effects with levocetirizine include diarrhea, constipation, otitis media, vomiting, cough, pyrexia, epistexis, asthenia, dry mouth, fatigue, headache, nasopharyngitis, pharyngitis, and somnolence.
Immune system disorders: Hypersensitivity (anaphylaxis).
Metabolism and nutrition disorders: Edema, increased appetite, weight gain.
Psychiatric disorders: Aggression, agitation, depression, hallucination, suicidal ideation.
Nervous system disorders: Convulsion, dizziness, dysgeusia, extrapyramidal symptoms, febrile seizure, insomnia, movement disorders (including dystonia and oculogyric crisis), myoclonus, orafacial dyskinesia, paresthesia, seizure, syncope, tic, tremor.
Eye disorders: Blurred vision, visual disturbances.
Ear and labyrinth disorders: Vertigo.
Cardiac disorders: Palpitations, tachycardia.
Vascular disorders: Severe hypotension.
Respiratory, thoracic and mediastinal disorders: Dyspnea.
Gastrointestinal disorders: Nausea.
Hepatobiliary disorders: Cholestasis, hepatitis.
Skin and subcutaneous tissue disorders: Acute generalized exanthematous pustulosis (AGEP), angioedema, fixed drug eruption, pruritus, rash, urticaria.
Musculoskeletal and connective tissue disorders: Arthralgia, myalgia.
Renal and urinary disorders: Dysuria, glomerulonephritis, urinary retention.
Pregnancy, puerperium and perinatal conditions: Stillbirth.
Investigations: Abnormal liver function tests, blood bilirubin increased, transaminases increased.
Drug Interactions
CNS Depressants (e.g., Alcohol): Avoid concomitant use due to possible additive effect (i.e., additional reduction in alertness, additional impairment of CNS performance).
Ritonavir: Ritonavir disposition is not altered but this may cause increased AUC (42%), increased half-life (53%) and decreased clearance (29%) of cetirizine.
Theophylline: Theophylline disposition is not altered but this may cause decreased clearance (16%) of cetirizine.
Ketoconazole: Concomitant administration with cetirizine caused prolongation of QTc interval (increase of 17.4 msec). However, this interaction was not considered clinically important.
Antipyrine, Azithromycin, Cimetidine, Erythromycin, Ketoconazole, Pseudoephedrine: No clinically important changes in electrocardiogram parameters and no pharmacokinetic interactions were observed with cetirizine.
Storage
Store at temperatures not exceeding 30°C.
ATC Classification
R06AE09 - levocetirizine ; Belongs to the class of piperazine derivatives used as systemic antihistamines.
Presentation/Packing
FC tab 5 mg (white, round, biconvex that is plain on both sides) x 50's.
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