Attributes
- Form
- Dosage mg
- Pack
- Description en
- Instructions for use LEVCETIN OD S 5 LEVCETHIN ODS 5 Levocetirizine oral disintegrating strip 5mg Trade name LEVCETIN ODS 5 International Nonproprietary Name Levocetirizine dihydrochloride Pharmaceutical form Oral disintegrating strip Composition: Each oral disintegrating strip contains: Levocetirizine dihydrochloride 5mg Pharmacotherapeutic group: Pharmacotherapeutic group: Antihistamine, for systemic use, piperazine derivatives. ATC code: RO6AE09 Pharmacological characteristics: Pharmacodynamics: Levocetirizine, the (R)-enantiomer of cetirizine, is a potent and selective peripheral H1 receptor antagonist. Binding studies have shown that levocetirizine has a high affinity for human H1 receptors (Ki = 3.2 nmol/L). Levocetirizine has an affinity 2 orders of magnitude higher than cetirizine (Ki = 6.3 nmol/L). Levocetirizine dissociates from H1 receptors with a half-life of 115±38 min. After a single dose, levocetirizine shows 90% receptor occupancy at 4 hours and 57% at 12 hours. Pharmacodynamic studies in healthy volunteers show that at half the dose, levocetirizine has comparable activity to cetirizine in the skin and nose. Levocetirizine inhibits the early phase of the histamine-mediated allergic reaction and also reduces the migration of certain types of inflammatory cells and the release of certain mediators associated with the late allergic response. Pharmacokinetics: The pharmacokinetics of levocetirizine are linear, dose and time-independent, and vary slightly between subjects. The pharmacokinetic profile is the same when administered as a single enantiomer and as cetirizine. No chiral inversion is observed during absorption and elimination. Absorption: Levocetirizine is rapidly and extensively absorbed after oral administration. Peak plasma concentration is reached 0.9 hours after dosing. Steady state is achieved within two days. Peak concentration is typically 270 ng/mL and 308 ng/mL after single and repeated 0.5 mg once daily dosing, respectively. The extent of absorption is dose-independent and is not affected by food, but the rate of absorption and time to peak concentration are reduced and delayed. Distribution: Tissue distribution data are not known in humans, nor is the penetration of levocetirizine across the blood-brain barrier. Levocetirizine is 90% bound to plasma proteins. The distribution of levocetirizine is limited, as the volume of distribution is 0.4 L/kg. Biotransformation: In humans, the extent of levocetirizine metabolism is less than 14% of the dose, and therefore, differences due to genetic polymorphism or intake of enzyme inhibitors are likely to be negligible. Metabolic pathways include aromatic oxidation, N- and O-dealkylation, and conjugation with taurine. The dealkylation pathways are mainly mediated by CYP3A4, while aromatic oxidation involves multiple and/or unidentified CYP isoforms. Levocetirizine does not affect the activity of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, 3A4 at peak concentrations achieved after oral dosing of 5 mg. Due to low metabolism and lack of potential for metabolic inhibition, drug interactions with levocetirizine are unlikely. Elimination: The plasma half-life in adults is 7.9±1.9 hours. The clearance from the whole body averages 0.63 mL/min/kg. Levocetirizine and its metabolites are mainly eliminated via urine, accounting for approximately 85.4% of the dose. Only 12.9% of the dose is excreted in feces. Levocetirizine is eliminated by glomerular filtration and active tubular secretion. Therapeutic indications: Levocetirizine is indicated for: Relief of nasal and ocular symptoms in seasonal and perennial allergic rhinitis. For the relief of symptoms of chronic idiopathic urticaria. Dosage and administration: Adults and children over 12 years of age: The recommended daily dose is 5 mg once daily. Children 6-12 years of age: The recommended daily dose is 5 mg once daily. Due to insufficient data on safety and efficacy, the use of levocetirizine in children under 6 years of age is not recommended. Elderly: Currently, there is no data to indicate that dose reduction is necessary in elderly individuals with normal renal function. Patients with hepatic impairment: Dose adjustment is not required in individuals with hepatic impairment alone. Patients with hepatic and renal impairment: Dose adjustment is recommended. Method of administration: The oral disintegrating strip should be taken orally, swallowed whole with water, with or without food. Contraindications: Hypersensitivity to levocetirizine or any of the excipients used in the formulation. Patients with severe renal impairment with a creatinine clearance of less than 10 mL/min. Patients with rare hereditary problems of fructose intolerance should not take levocetirizine oral disintegrating strip. Special warnings and precautions for use: Do not exceed the recommended dose. The use of levocetirizine dihydrochloride is not recommended in children under 6 years of age. Clinically significant interactions with alcohol (at blood alcohol levels of 0.5 g/L) have not been described at therapeutic doses. Nevertheless, caution should be exercised when consuming alcohol. Caution is advised in patients with epilepsy and in those who have a risk of seizures. Effects on ability to drive and use machines: Objective measurements of driving performance, sleep latency, and actigraphy have not revealed any clinically significant effects at the recommended dose of 5 mg. Patients planning to drive, perform potentially hazardous activities, or operate machinery should not exceed the recommended dose and should consider their response to the medical product. In these sensitive patients, the use of alcohol and other CNS depressants may cause further reduction in alertness and impairment of performance. Adverse effects: The frequency of adverse effects is defined as follows: Very common (≥1/10); Common (≥1/100 to <1/10); Uncommon (≥1/1000 to <1/100); Rare (≥1/10,000 to <1/1000). Unknown (cannot be estimated from available data). Common: Somnolence, dizziness, headache, pharyngitis, rhinitis*, abdominal pain, dry mouth, nausea, fatigue. Uncommon: Agitation, paresthesia, diarrhea, pruritus, rash, asthenia, weakness. Rare: Hypersensitivity, aggression, confusion, depression, hallucinations, insomnia, convulsions, movement disorders, tachycardia, edema, abnormal liver function (increased transaminases, alkaline phosphatase, Y-GT, and bilirubin, urticaria, weight gain). Very rare: Thrombocytopenia, anaphylactic shock, tics, dysgeusia, syncope, tremor, dystonia, dyskinesia, accommodation disorders, blurred vision, oculogyration, angioneurotic edema, fixed drug eruption, dysuria, enuresis. Interactions with other medicinal products and other forms of interaction: Due to the pharmacokinetic, pharmacodynamic, and tolerance profile of levocetirizine, interactions with this antihistamine are not expected. In particular, neither pharmacodynamic nor significant pharmacokinetic interactions have been described in drug interaction studies, mainly with pseudoephedrine or theophylline (400 mg/day). The extent of absorption of levocetirizine is not reduced by food, but the rate of absorption is reduced. Fertility, pregnancy and lactation: Very rare clinical data are available on exposed pregnancies. Animal studies do not show direct or indirect harmful effects on pregnancy, embryonic/fetal development, delivery, and postnatal development. Caution should be exercised when prescribing to pregnant and breastfeeding women, as levocetirizine is excreted in breast milk. Overdose: Symptoms: The effects observed after overdose of levocetirizine are mainly related to CNS effects or effects that may indicate anticholinergic events. At doses at least 5 times the recommended daily dose, the following side effects have been observed: confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, restlessness, sedation, somnolence, stupor, tachycardia, tremor, and urinary retention. Management of overdose: There is no specific antidote for levocetirizine. In case of overdose, symptomatic and supportive therapy is recommended. If it has been a short time since oral intake, gastric lavage should be considered. Levocetirizine is not effectively removed by dialysis. Preclinical safety data: Based on studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, and reproductive toxicity, no indicators of clinically significant risk to humans have been identified. Incompatibility: Unknown. Dosage form and packaging: 10x1 strips. Shelf life: 2 years. Special precautions for storage: Store at a temperature not exceeding 25°C, protected from light and moisture. Conditions for dispensing of the medicinal product: Pharmaceutical product group II, dispensed with prescription N3. Manufacturer: Zydus Lifesciences Limited B-21/22 MIDC Area, Kalmeshwar Nagpur 441 501, Maharashtra State India. Manufactured using Tinoral® technology.
- Active
- levocetirizine
What is it?
Instructions for use LEVCETIN OD S 5 LEVCETHIN ODS 5 Levocetirizine oral disintegrating strip 5mg Trade name LEVCETIN ODS 5 International Nonproprietary Name Levocetirizine dihydrochloride Pharmaceutical form Oral disintegrating strip Composition: Each oral disintegrating strip contains: Levocetirizine dihydrochloride 5mg Pharmacotherapeutic group: Pharmacotherapeutic group: Antihistamine, for systemic use, piperazine derivatives. ATC code: RO6AE09 Pharmacological characteristics: Pharmacodynamics: Levocetirizine, the (R)-enantiomer of cetirizine, is a potent and selective peripheral H1 receptor antagonist. Binding studies have shown that levocetirizine has a high affinity for human H1 receptors (Ki = 3.2 nmol/L). Levocetirizine has an affinity 2 orders of magnitude higher than cetirizine (Ki = 6.3 nmol/L). Levocetirizine dissociates from H1 receptors with a half-life of 115±38 min. After a single dose, levocetirizine shows 90% receptor occupancy at 4 hours and 57% at 12 hours. Pharmacodynamic studies in healthy volunteers show that at half the dose, levocetirizine has comparable activity to cetirizine in the skin and nose. Levocetirizine inhibits the early phase of the histamine-mediated allergic reaction and also reduces the migration of certain types of inflammatory cells and the release of certain mediators associated with the late allergic response. Pharmacokinetics: The pharmacokinetics of levocetirizine are linear, dose and time-independent, and vary slightly between subjects. The pharmacokinetic profile is the same when administered as a single enantiomer and as cetirizine. No chiral inversion is observed during absorption and elimination. Absorption: Levocetirizine is rapidly and extensively absorbed after oral administration. Peak plasma concentration is reached 0.9 hours after dosing. Steady state is achieved within two days. Peak concentration is typically 270 ng/mL and 308 ng/mL after single and repeated 0.5 mg once daily dosing, respectively. The extent of absorption is dose-independent and is not affected by food, but the rate of absorption and time to peak concentration are reduced and delayed. Distribution: Tissue distribution data are not known in humans, nor is the penetration of levocetirizine across the blood-brain barrier. Levocetirizine is 90% bound to plasma proteins. The distribution of levocetirizine is limited, as the volume of distribution is 0.4 L/kg. Biotransformation: In humans, the extent of levocetirizine metabolism is less than 14% of the dose, and therefore, differences due to genetic polymorphism or intake of enzyme inhibitors are likely to be negligible. Metabolic pathways include aromatic oxidation, N- and O-dealkylation, and conjugation with taurine. The dealkylation pathways are mainly mediated by CYP3A4, while aromatic oxidation involves multiple and/or unidentified CYP isoforms. Levocetirizine does not affect the activity of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, 3A4 at peak concentrations achieved after oral dosing of 5 mg. Due to low metabolism and lack of potential for metabolic inhibition, drug interactions with levocetirizine are unlikely. Elimination: The plasma half-life in adults is 7.9±1.9 hours. The clearance from the whole body averages 0.63 mL/min/kg. Levocetirizine and its metabolites are mainly eliminated via urine, accounting for approximately 85.4% of the dose. Only 12.9% of the dose is excreted in feces. Levocetirizine is eliminated by glomerular filtration and active tubular secretion. Therapeutic indications: Levocetirizine is indicated for: Relief of nasal and ocular symptoms in seasonal and perennial allergic rhinitis. For the relief of symptoms of chronic idiopathic urticaria. Dosage and administration: Adults and children over 12 years of age: The recommended daily dose is 5 mg once daily. Children 6-12 years of age: The recommended daily dose is 5 mg once daily. Due to insufficient data on safety and efficacy, the use of levocetirizine in children under 6 years of age is not recommended. Elderly: Currently, there is no data to indicate that dose reduction is necessary in elderly individuals with normal renal function. Patients with hepatic impairment: Dose adjustment is not required in individuals with hepatic impairment alone. Patients with hepatic and renal impairment: Dose adjustment is recommended. Method of administration: The oral disintegrating strip should be taken orally, swallowed whole with water, with or without food. Contraindications: Hypersensitivity to levocetirizine or any of the excipients used in the formulation. Patients with severe renal impairment with a creatinine clearance of less than 10 mL/min. Patients with rare hereditary problems of fructose intolerance should not take levocetirizine oral disintegrating strip. Special warnings and precautions for use: Do not exceed the recommended dose. The use of levocetirizine dihydrochloride is not recommended in children under 6 years of age. Clinically significant interactions with alcohol (at blood alcohol levels of 0.5 g/L) have not been described at therapeutic doses. Nevertheless, caution should be exercised when consuming alcohol. Caution is advised in patients with epilepsy and in those who have a risk of seizures. Effects on ability to drive and use machines: Objective measurements of driving performance, sleep latency, and actigraphy have not revealed any clinically significant effects at the recommended dose of 5 mg. Patients planning to drive, perform potentially hazardous activities, or operate machinery should not exceed the recommended dose and should consider their response to the medical product. In these sensitive patients, the use of alcohol and other CNS depressants may cause further reduction in alertness and impairment of performance. Adverse effects: The frequency of adverse effects is defined as follows: Very common (≥1/10); Common (≥1/100 to <1/10); Uncommon (≥1/1000 to <1/100); Rare (≥1/10,000 to <1/1000). Unknown (cannot be estimated from available data). Common: Somnolence, dizziness, headache, pharyngitis, rhinitis*, abdominal pain, dry mouth, nausea, fatigue. Uncommon: Agitation, paresthesia, diarrhea, pruritus, rash, asthenia, weakness. Rare: Hypersensitivity, aggression, confusion, depression, hallucinations, insomnia, convulsions, movement disorders, tachycardia, edema, abnormal liver function (increased transaminases, alkaline phosphatase, Y-GT, and bilirubin, urticaria, weight gain). Very rare: Thrombocytopenia, anaphylactic shock, tics, dysgeusia, syncope, tremor, dystonia, dyskinesia, accommodation disorders, blurred vision, oculogyration, angioneurotic edema, fixed drug eruption, dysuria, enuresis. Interactions with other medicinal products and other forms of interaction: Due to the pharmacokinetic, pharmacodynamic, and tolerance profile of levocetirizine, interactions with this antihistamine are not expected. In particular, neither pharmacodynamic nor significant pharmacokinetic interactions have been described in drug interaction studies, mainly with pseudoephedrine or theophylline (400 mg/day). The extent of absorption of levocetirizine is not reduced by food, but the rate of absorption is reduced. Fertility, pregnancy and lactation: Very rare clinical data are available on exposed pregnancies. Animal studies do not show direct or indirect harmful effects on pregnancy, embryonic/fetal development, delivery, and postnatal development. Caution should be exercised when prescribing to pregnant and breastfeeding women, as levocetirizine is excreted in breast milk. Overdose: Symptoms: The effects observed after overdose of levocetirizine are mainly related to CNS effects or effects that may indicate anticholinergic events. At doses at least 5 times the recommended daily dose, the following side effects have been observed: confusion, diarrhea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, restlessness, sedation, somnolence, stupor, tachycardia, tremor, and urinary retention. Management of overdose: There is no specific antidote for levocetirizine. In case of overdose, symptomatic and supportive therapy is recommended. If it has been a short time since oral intake, gastric lavage should be considered. Levocetirizine is not effectively removed by dialysis. Preclinical safety data: Based on studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, and reproductive toxicity, no indicators of clinically significant risk to humans have been identified. Incompatibility: Unknown. Dosage form and packaging: 10x1 strips. Shelf life: 2 years. Special precautions for storage: Store at a temperature not exceeding 25°C, protected from light and moisture. Conditions for dispensing of the medicinal product: Pharmaceutical product group II, dispensed with prescription N3. Manufacturer: Zydus Lifesciences Limited B-21/22 MIDC Area, Kalmeshwar Nagpur 441 501, Maharashtra State India. Manufactured using Tinoral® technology.