Bell-Kenz Pharma


Euro Generics
Full Prescribing Info
Each film-coated tablet contains Atorvastatin (as Calcium) 20 mg, 40 mg or 80 mg.
Atorvastatin is a synthetic lipid-lowering agent. It is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate limiting step of cholesterol biosynthesis.
Pharmacology: Pharmacokinetics: Atorvastatin is rapidly absorbed after oral administration; maximum plasma concentrations occur within 1 to 2 hours. Extent of absorption increases in proportion to atorvastatin dose. The absolute bioavailability of atorvastatin (parent drug) is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%. The low systemic availability is attributed to presystemic clearance in gastrointestinal mucosa and/or hepatic first-pass metabolism. Although food decreases the rate and extent of drug absorption by approximately 25% and 9%, respectively, as assessed by Cmax and AUC, LDL-C reduction is similar whether atorvastatin is given with or without food. Plasma atorvastatin concentrations are lower (approximately 30% for Cmax and AUC) following evening drug administration compared with morning. However, LDL-C reduction is the same regardless of the time of day of drug administration.
Distribution: Mean volume of distribution of atorvastatin is approximately 381 liters. Atorvastatin is ≥98% bound to plasma proteins. A blood/plasma ratio of approximately 0.25 indicates poor drug penetration into red blood cells. Based on observations in rats, atorvastatin is likely to be secreted in human milk.
Metabolism: Atorvastatin is extensively metabolized to ortho- and parahydroxylated derivatives and various beta-oxidation products. In vitro inhibition of HMG-CoA reductase by ortho- and parahydroxylated metabolites is equivalent to that of atorvastatin. Approximately 70% of circulating inhibitory activity for HMG-CoA reductase is attributed to active metabolites. In vitro studies suggest the importance of atorvastatin metabolism by cytochrome P450 3A4, consistent with increased plasma concentrations of atorvastatin in humans following co-administration with erythromycin, a known inhibitor of this isozyme .In animals, the ortho-hydroxy metabolite undergoes further glucuronidation.
Excretion: Atorvastatin and its metabolites are eliminated primarily in bile following hepatic and/or extra-hepatic metabolism; however, the drug does not appear to undergo enterohepatic recirculation. Mean plasma elimination half-life of atorvastatin in humans is approximately 14 hours, but the half-life of inhibitory activity for HMG-CoA reductase is 20 to 30 hours due to the contribution of active metabolites. Less than 2% of a dose of atorvastatin is recovered in urine following oral administration.
Atorvastatin as Calcium (ITORVAZ) is indicated in: Hypercholesterolaemia: Adjunct to diet for reduction of elevated total cholesterol, LDL-cholesterol, apolipoprotein B, and triglycerides in adults and children aged 10 years and older with primary hypercholesterolaemia , heterozygous familial hypercholesterolaemia or combined (mixed) hyperlipidaemia when response to diet and other pharmacological measures is inadequate.
Raises HDL-cholesterol and lowers the LDL/HDL and total cholesterol/HDL ratios.
Adjunct to diet and non-dietary measures in reducing elevated total cholesterol, LDL-cholesterol, and apolipoprotein B in patients with homozygous familial hypercholesterolaemia when response to these measures is inadequate.
Primary Prevention in Type II Diabetes Mellitus: Reducing the risk of cardiovascular events in diabetic patients with at least 1 additional risk factor, without clinically evident coronary heart disease irrespective of whether cholesterol is raised.
Dosage/Direction for Use
Primary Hypercholesterolaemia and Combined Hyperlipidaemia: Adult: Usually 10 mg once daily.
Familial Hypercholesterolaemia: Initially 10 mg daily, increased at intervals of at least 4 weeks to 40 mg once daily; if necessary, further increased to a maximum of 80 mg once daily.
Children and Adolescents aged 10-17 years with Heterozygous Familial Hypercholesterolaemia: Initial dose of 10 mg once daily, adjusted according to response to a maximum of 20 mg daily.
Or as directed by the physician.
Active liver disease or unexplained persistent elevations of serum transaminases.
Hypersensitivity to any component of this medication.
Special Precautions
General: Before instituting therapy with atorvastatin, an attempt should be made to control hypercholesterolemia with appropriate diet, exercise and weight reduction in obese patients and to treat other underlying medical problems.
Information to Patients: Patients should be advised to report promptly unexplained muscle pain, tenderness or weakness, particularly if accompanied by malaise or fever.
Use In Pregnancy & Lactation
Atorvastatin is contraindicated in pregnancy. Women of childbearing potential should use adequate contraceptive measures. Atorvastatin should be administered to women of childbearing age only when such patients are highly unlikely to conceive and have been informed of the potential hazards to the fetus.
Atorvastatin is contraindicated while breast-feeding. It is not known whether this drug is excreted in human milk. Because of the potential for adverse reactions in nursing infants, women taking atorvastatin should not breast-feed.
Drug Interactions
The risk of myopathy during treatment with drugs of this class is increased with concurrent administration of cyclosporin, fibric acid derivatives, niacin (nicotinic acid), erythromycin and azole antifungals.
Antacid: Co-administration of atorvastatin with an oral antacid suspension containing magnesium and aluminum hydroxides, decreased atorvastatin plasma concentrations approximately 35%. However, LDL-C reduction was not altered.
Antipyrine: Interactions with other drugs metabolized via the same cytochrome isozymes are not expected because atorvastatin does not affect the pharmacokinetics of antipyrine.
Colestipol: Plasma concentrations of atorvastatin decreased approximately 25% when colestipol and atorvastatin were co-administered. However, LDL-C reduction was greater when atorvastatin and colestipol were co-administered than when either drug was given alone.
Cimetidine: Atorvastatin plasma concentrations and LDL-C reduction were not altered by co-administration of cimetidine.
Digoxin: When multiple doses of atorvastatin and digoxin were co-administered, steady-state plasma digoxin concentrations increased by approximately 20%. Patients taking digoxin should be monitored appropriately.
Erythromycin/Clarithromycin: Co-administration of atorvastatin and erythromycin (500 mg four times daily), or clarithromycin (500 mg twice daily) known inhibitors of cytochrome P450 3A4, was associated with higher plasma concentrations of atorvastatin.
Oral Contraceptives: Co-administration of atorvastatin and an oral contraceptive increased AUC values for norethisterone and ethinyl estradiol by approximately 30% and 20%. These increases should be considered when selecting an oral contraceptive for a woman taking atorvastatin.
Warfarin: Atorvastatin had no clinically significant effect on prothrombin time when administered to patients receiving chronic warfarin treatment.
Store at temperatures not exceeding 30°C. Protect from light.
MIMS Class
Dyslipidaemic Agents
ATC Classification
C10AA05 - atorvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
Itorvaz FC tab 20 mg
30's (P450/box, P15/film-coated tab)
Itorvaz FC tab 40 mg
30's (P645/box, P21.5/film-coated tab)
Itorvaz FC tab 80 mg
30's (P795/box, P26.5/film-coated tab)
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