Adivast

Each Film-coated Tablet contains: Atorvastatin (as calcium) 20 mg and 40 mg, respectively.
Atorvastatin, a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor (a statin), is a lipid regulating drug with actions on plasma lipids.

Pharmacology: Pharmacodynamics: Atorvastatin as well as some of its metabolites, are pharmacologically active in humans. The liver is the primary site of action and the principal site of cholesterol synthesis and LDL clearance. Drug dosage, rather than systemic drug concentration, correlates better with LDL-C reduction individualization of drug dosage should be based on therapeutic response.
Pharmacokinetics: Atorvastatin is rapidly absorbed from the gastrointestinal tract. It has low absolute bioavailability of about 12% due to presystemic clearance in the gastrointestinal mucosa and/or first-pass metabolism in the liver, its primary site of action. Atorvastatin is metabolized by the P45O isoenzyme CYP3A4 to a number of compounds which are also active inhibitors of HMG-CoA reductase. The mean plasma elimination of atorvastatin is about 14 hours, although the half-life of inhibitory activity for HMG-CoA reductase is approximately 20 to 30 hours due to the contribution of the active metabolites. It is 98% to plasma proteins. Atorvastatin is excreted as metabolites primarily in the bile.

Atorvastatin is used to reduce LDL-cholesterol, apolipoprotein B, and triglycerides; and to increase HDL-cholesterol in the treatment of hyperlipidaemias, including hypercholesterolaemias and combined (mixed) hyperlipidaemias (type IIa or IIb hyperlipoproteinaemia). It can also be effective as adjunctive therapy in patients with homozygous familial hypercholesterolaemia who have some LDL-receptor dysfunction.

The usual initial dose is 10 mg to 20 mg daily which may be adjusted at intervals of 4 weeks up to a maximum of 80 mg daily or as prescribed by the physician.

In the event of an overdose, the patient should be treated symptomatically, and supportive measures instituted as required. Due to extensive drug binding to plasma proteins, hemodialysis is not expected to significantly enhance Atorvastatin clearance.

Statins are contraindicated in active liver disease (on persistently abnormal liver function test).
Use in Pregnancy & Lactation: Statins are contraindicated in pregnancy (adequate contraception required during treatment and for one month afterwards) and breast feeding.

Atorvastatin should not be given to patients with active liver disease or unexplained persistent raised serum-aminotransferase concentrations occur. It should be avoided during pregnancy since there is a possibility that it could interfere with fetal sterol synthesis; there have been a number of reports of congenital abnormalities associated with statins. Statins may cause myopathy and rhabdomyolysis, especially at higher doses and they should be used with caution in patients at risk of rhabdomyolysis and particularly in patients taking drugs that increase plasma concentrations of the statin; the statin should be discontinued if creatine phosphokinase increases significantly or if myopathy is diagnosed. Some statins, such as fluvastatin, pravastatin, rosuvastatin, and simvastatin, should be used with caution in patients with severe renal impairment.

Statins are contraindicated in pregnancy (adequate contraception required during treatment and for one month afterwards) and breast feeding.

The most common adverse effects therapy with Atorvastatin and other statins are gastrointestinal disturbances. Other adverse effects reported include headache, skin rashes, dizziness, blurred vision, insomnia, and dysgeusia. Reversible increases in serum-aminotransferase concentrations may occur and liver function should be assessed before treatment is initiated and then monitored periodically until one year after last elevation in dose. Hepatitis and pancreatitis have been reported. Hypersensitivity reactions including anaphylaxis and angioedema have also occurred. Myopathy, characterized by myalgia and muscle weakness and associated with increased creatinine phosphokinase concentrations, has been reported, especially in patients taking statins concurrently with cyclosporine fibric acid derivatives, or nicotinic acid. Rarely, rhabdomyolysis with acute renal failure may develop.

The most serious consequence of drug interactions with Atorvastatin and other statins is the development of myopathy and rhabdomyolysis. Drugs that can cause myopathy when given alone increase the risk of myopathy with all statins: these drugs include fibric acid derivatives (fibrates or gemfibrozil) and nicotinic acid. Atorvastatin is metabolized by Cytochrome P450 isoenzyme CYP3A4 as are simvastatin and lovastatin, and interactions may occur with drugs that inhibit this enzyme, including cyclosporine, itraconazole, ketoconazole, erythromycin, clarithromycin, HIV-protease inhibitors, nefazodone, amiodarone, and verapamil; there may also be similar interaction with grapefruit juice.

Avoid excessive consumption (>1L/day) of grapefruit juice.

Store at temperatures not exceeding 30°C.

Dyslipidaemic Agents

C10AA05 - atorvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.

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