Malasiya Product

Lcet Tablets

Lcet Tablets

Why you have been prescribed this medicine?

You have been prescribed this medicine if you have any of the following:

When you should consult your doctor?

You should consult your doctor if you experience any of the following:
Usually the preparation is well tolerated. During a long-term usage of high doses there can be possible follow side effects:

GIT:
nausea, vomiting, heartburn, diarrhea.

CNS:
hyperexcitability of CNS, headache.

Urinary system:
formation of urinary, cystine and oxalate concernments.
Skin and subcutaneous tissue: allergic reactions.

Blood system:
It can cause erythrocyte hemolysis in patients with insufficiency of glucose-6-phosphatdehydrogenase of hematocytes.

What to do if you miss a dose?

If it is almost time for your next dose, skip the dose you missed and take your next dose when you are meant to. Otherwise take it as soon as you remember and then go back to taking it as you would normally.

Things you MUST NOT DO while on this medicine?

Ascozin® increases salicylates (increases a risk of crystalluria), ethynilestradiol, benzylpenicillin and tetracyclines concentrations in blood, and decreases per oral contraceptives concentration in blood. It reduces anticoagulation effect of coumarin derivatives. It improves iron drugs absorption in intestine. It increases general clearance of ethyl alcohol. Quinolone drugs, calcium chloride, salicylate, corticosteroid decrease vitamin C reserve when used for a long term. Corticosteroids (cortisone and prednisolone), which are administered in concrete diseases (arthritis, bronchial astma etc), also reduce vitamin C and zinc levels.
Concurrent usage of ascorbic acid and deferoxamine enhances tissue toxicity of iron, especially in cardiac muscle that can cause decompensation of blood circulatory system. It can be used only in 2 hours after deferoxamine injection. A long-term administration of high doses in patients, who are treated by disulfiram, inhibits disulfamide-alcohol reaction.
High doses of the preparation decrease efficacy of tricyclic depressants.

What to do if you accidentally take too much (overdose) of the medicine?

Symptoms:
nausea, vomiting, intestine spasm, diarrhea; it is possible allergic reaction, kidney dysfunction, blood pressure increase, hyperexcitability of CNS, sleep disturbance.

Treatment:
It is symptomatic.

Is it safe in pregnancy and breast-feeding?

Tell your doctor immediately if you become pregnant while taking this medication. For safety of any drug during pregnancy or breastfeeding – please consult your doctor.

Storage Conditions:

Store in a dry, protected from light place at a temperature not more than 25° C.
Keep it out of reach of children.

Drug Description

COMPOSITION:

Each film coated tablet contains: Levocetirizine dihydrochloride ………… 5 mg Other ingredients: Microcrystalline cellulose, croscarmellose sodium, colloidal anhydrous silica, magnesium stearate, opadry II 85G51300 green & purified water.

Indications and dosage.

INDICATIONS:
Allergic Rhinitis: Levocetirizine is indicated for the relief of symptoms associated with allergic rhinitis (seasonal and perennial) in adults and children 6 years of age and older. Chronic Idiopathic Urticaria: Levocetirizine is indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older. MODE OF ADMINISTRATION
The film-coated tablet must be taken orally, swallowed whole with liquid and may be taken with or without food. It is recommended to take the daily dose in one single intake. DOSAGE:
The daily recommended dose is 5 mg (1 film-coated tablet).
Elderly:
Adjustment of the dose is recommended in elderly patients with moderate to severe renal impairment (see Patients with renal impairment below). Children aged 6 to 12 years: The daily recommended dose is 5 mg (1 film-coated tablet). For children aged 2 to 6 years no adjusted dosage is possible with the film-coated tablet formulation. It is recommended to use a paediatric formulation of levocetirine. Patients with hepatic impairment:
No dose adjustment is needed in patients with solely hepatic impairment. In patients with hepatic impairment and renal impairment, adjustment of the dose is recommended (see Patients with renal impairment above). Patients with renal impairment: The dosing intervals must be individualized according to renal function. Refer to the following table and adjust the dose as indicated. To use this dosing table, an estimate of the patient's creatinine clearance (CLcr) in ml/min is needed. The CLcr (ml/min) may be estimated from serum creatinine (mg/dl) determination using the following formula: L-cet tab/MY/F 140-age (years) x weight (kg) CL = (x 0.85 for women) cr 72 x serum creatinine (mg/dl)

Side effects and drug interactions.

ADVERSE REACTIONS:

Central nervous system:
headache, drowse, fatiguability, weakness.

Cardio-vascular system:
palpitation sensation.

Visual organ:
visual impairment.

Hepatobiliary system:
hepatitis.

Immune system:
hypersensitivity, including anaphylaxis and angioneurotic edema.

Respiratory system:
short breath.

Digestive system: dry mouth, nausea.

Skin and subcutaneous tissue:
skin itch, rash and urticaria.

Others:
body weight enlargement; gastric pain; mialgia; liver function test can be increased.

Drug interactions:
No interaction studies have been performed with levocetirizine (including no studies with CYP3A4 inducers); studies with the racemate compound cetirizine demonstrated that there were no clinically relevant adverse interactions (with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam). A small decrease in the clearance of cetirizine (16%) was observed in a multiple dose study with theophylline (400 mg once a day); while the disposition of theophylline was not altered by concomitant cetirizine administration. The extent of absorption of levocetirizine is not reduced with food, although the rate of absorption is decreased. In sensitive patients the simultaneous administration of cetirizine or levocetirizine and alcohol or other CNS depressants may have effects on the central nervous system, although it has been shown that the racemate cetirizine does not potentiate the effect of alcohol

Warnings and precautions

Pregnancy and lactation:
There is no data indicating the safety of the preparation during pregnancy that's why the administration in pregnant women is contraindicated. Levocetirizine is secreted into the breast milk. If there is a need the usage of the preparation during the breast feeding should be stopped.
Children:
The preparation is not used in children under 16 years old.

PRECAUTIONS:
Precaution is recommended with intake of alcohol. Due to the lack of data in this population, the administration of the product to infants and toddlers aged less than 2 years is not recommended. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Overdosage and Contraindications

Overdose:
Symptoms: Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness, followed by drowsiness in children.

Treatment:
Management of overdoses: There is no known specific antidote to levocetirizine. Should overdose occur, symptomatic or supportive treatment is recommended. Gastric lavage should be considered following short-term ingestion. Levocetirizine is not effectively removed by haemodialysis.


CONTRAINDICATIONS:
The use of Levocetirizine tablet is not recommended in children aged less than 6 years. Precaution is recommended with intake of alcohol. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine. Hypersensitivity to levocetirizine, to any piperazine derivative, methyl parahydroxybenzoate, propyl parahydroxybenzoate, or any of the other excipients. Severe renal impairment at less than 10 ml/min creatinine clearance.

Clinical pharmacology.

PHARMACOLOGICAL PROPERTIES:

Pharmacotherapeutic group:
antihistamine for systemic use, piperazine derivative. Mechanism of Action: Levocetirizine, the active enantiomer of cetirizine, is an anti-histamine; 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. The pharmacokinetics of levocetirizine are linear with dose- and time-independent with low inter-subject variability. The pharmacokinetic profile is the same when given as the single enantiomer or when given as cetirizine. No chiral inversion occurs during the process of absorption and elimination. Levocetirizine, the (R) enantiomer of cetirizine, is a potent and selective antagonist of peripheral H1-receptors. Binding studies revealed that levocetirizine has high affinity for human H1-receptors (Ki = 3.2 nmol/l). Levocetirizine has an affinity 2-fold higher than that of cetirizine (Ki = 6.3 nmol/l). Levocetirizine dissociates from H1-receptors with a half-life of 115 ± 38 min. Pharmacodynamic studies in healthy volunteers demonstrate that, at half the dose, levocetirizine has comparable activity to cetirizine, both in the skin and in the nose. In-vitro studies (Boyden chambers and cell layers techniques) show that levocetirizine inhibits eotaxin-induced eosinophil transendothelial migration through both dermal and lung cells. A pharmacodynamic experimental study in vivo (skin chamber technique) showed three main inhibitory effects of levocetirizine 5 mg in the first 6 hours of pollen-induced reaction, compared with placebo in 14 adult patients: inhibition of VCAM-1 release, modulation of vascular permeability and a decrease in eosinophil recruitment. The efficacy and safety of levocetirizine have been demonstrated in several double-blind, placebo controlled, clinical trials performed in patients suffering from seasonal allergic rhinitis or perennial allergic rhinitis. Clinical experience with 5 mg levocetirizine as a - tablet formulation is currently available for a 6-month treatment period. For chronic urticaria and chronic allergic rhinitis, up to one year's clinical experience is available for the racemate, and up to 18 months in patients with pruritus associated with atopic dermatitis. A 6- month clinical study in 551 patients (incl. 276 levocetirizine-treated patients) suffering from PAR (symptoms present 4 days a week for at least 4 consecutive weeks) and sensitized to house dust mites and grass pollen demonstrated that levocetirizine 5 mg was clinically and statistically significantly more potent than placebo on the relief from the total symptom score of allergic rhinitis throughout the whole duration of the study, without any tachyphylaxis. During the whole duration of the study, levocetirizine significantly improved the quality of life of the patients. Nonclinical Toxicology
Carcinogenesis, Mutagenesis, Impairment of Fertility: No carcinogenesis studies have been performed with levocetirizine. However, evaluation of cetirizine carcinogenicity studies are relevant for determination of the carcinogenic potential of levocetirizine. In a 2-year carcinogenicity study, in rats, cetirizine was not carcinogenic at dietary doses up to 20 mg/kg (approximately 16 times the maximum recommended daily oral dose in adults and approximately 20 times the maximum recommended daily oral dose in children on a mg/m2 basis). In a 2-year carcinogenicity study in mice, cetirizine caused an increased incidence of benign hepatic tumors in males at a dietary dose of 16 mg/kg (approximately 7 times the maximum recommended daily oral dose in adults and approximately 8 times the maximum recommended daily oral dose in children on a mg/m2 basis). No increased incidence of benign tumors was observed at a dietary dose of 4 mg/kg (approximately 2 times the maximum recommended daily oral dose in adults and children on a mg/m2 basis). The clinical significance of these findings during long-term use of Levocetirizine is not known. Levocetirizine was not mutagenic in the Ames test, and not clastogenic in the human lymphocyte assay, the mouse lymphoma assay, and in vivo micronucleus test in mice. In a fertility and general reproductive performance study in mice, cetirizine did not impair fertility at an oral dose of 64 mg/kg (approximately 25 times the recommended daily oral dose in adults on an mg/m² basis). Preclinical Safety Data
Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, toxicity to reproduction, genotoxicity or carcinogenicity. PHARMACOKINETIC PROPERTIES
Absorption: Levocetirizine is rapidly and extensively absorbed following oral administration. In adults, peak plasma concentrations are achieved 0.9 h after dosing. Steady state is achieved after two days. Peak concentrations are typically 270 ng/ml and 308 ng/ml following a single and a repeated 5 mg o.d. dose, respectively. The extent of absorption is dose-independent and is not altered by food, but the peak concentration is reduced and delayed. Distribution: No tissue distribution data are available in humans, neither concerning the passage of the blood-brain-barrier. In rats and dogs, the highest tissue levels are found in liver and kidneys, the lowest in the CNS compartment. In humans, levocetirizine is 90% bound to plasma proteins. The distribution of levocetirizine is restrictive, as the volume of distribution is 0.4 l/kg. Biotransformation: 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 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 involved multiple and/or unidentified CYP isoforms. Levocetirizine had no effect on the activities of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 at concentrations well above peak concentrations achieved following a 5 mg oral dose. Due to its low metabolism and absence of metabolic inhibition potential, the interaction of levocetirizine with other substances, or vice-versa, is unlikely. Elimination: The plasma half-life in adults is 7.9 ± 1.9 hours. The half-life is shorter in small children. The mean apparent total body clearance in adults is 0.63 ml/min/kg. The major route of excretion of levocetirizine and metabolites is via urine, accounting for a mean of 85.4% of the dose. Excretion via faeces accounts for only 12.9% of the dose. Levocetirizine is excreted both by glomerular filtration and active tubular secretion. Renal impairment: The apparent body clearance of levocetirizine is correlated to the creatinine clearance. It is therefore recommended to adjust the dosing intervals of levocetirizine, based on creatinine clearance in patients with moderate and severe renal impairment. In anuric end stage renal disease subjects, the total body clearance is decreased by approximately 80% when compared to normal subjects. The amount of levocetirizine removed during a standard 4-hour hemodialysis procedure was < 10%.
Shelf-life:
3 years.

Storage:
Store below 30°C.
Keep all medicines out of reach of children

Package:
10 tablets are in a blister, 1 or 3 blisters are in a carton pack.

Conditions of supply:
Without prescription.

CERTIFICATES

KEEP IN TOUCH

Kusum Healthcare
Kusum Healthcare Pvt. Ltd. SP 289(A), RIICO Indl. Area, Chopanki, Bhiwadi (Rajasthan), India