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BAL PHARMA LIMITED Plot No. 1, 2, 3 & 69, Sector -4, IIE SIDCUL Pantnagar, Rudrapur. Distt, Udhom Singh Nagar Uttarakhand, INDIA.
Dosage Form, Composition & NAFDAC Registration Number (NRN)
Tablet (NRN:B4-1790): Each film coated tablet contains: Atorvastatin Calcium BP equivalent to Atorvastatin 10 mg. Colours: Titanium Dioxide BP
Pack size: Strip of 10 tablets.
Atorvastatin is an inhibitor of 3-hydroxy-3-Methylglutaryl-coenzyme A (HMG-CoA) reductase. Atorvastatin calcium is [R-(R*, R*)]-2-(4-fluorophenyl)-b, d -dihydroxy-5-(1-methylethyl)-3-phenyl-4 [(phenylamino) carbonyl]-1H-pyrrole -1-heptanoic acid, calcium salt (2:1) trihydrate. The empirical formula of Atorvastatin calcium is (C33H34FNO2)52 Ca.3HO2 and its molecular weight is 1209.42.
Mechanism of action
Atorvastatin is a selective, competitive inhibitor of HMG-CoA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coen-zyme A to mevalonate, a precursor of sterols, including cholesterol, In animal models, Atorvastatin lowers plasma cholesterol and lipoprotein levels by inhibiting HMG CoA reductase and cholesterol synthesis in the liver and by increasing the number of hepatic LDL receptors on the cell-surface to enhance uptake and catabolism of LDL; Atorvastatin also reduces LDL production and the number of LDL particles.
Atorvastatin is rapidly absorbed after oral administration; maximum plasma concentrations occur within 1 to 2 hours. The absolute bioavailability of Atorvastatin (parent drug) is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%. Mean volume of distribution of Atorvastatin is approximately 381 liters.
Atorvastatin is 98% bound to plasma proteins. Atorvastatin is extensively metabolized to ortho and parahydroxylate derivatives and various beta-oxidation products. Approximately 70% of circulative inhibitory activity for HMG-CoA reductase is attributed to active metabolites.
Atorvastatin and its metabolites are eliminated primarily in bile following: hepatic and/or extra-hepatic metabolism. 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.
As an adjunct to diet to reduce elevated total cholesterol and triglyceride level in patients with primary hypercholesterolemia and mixed dyslipoproteinemia (Type IIA and Type IIB).
Acute liver disease or unexplained persistent elevations of serum transaminases;
Hypersensitivity to any component of this medication; pregnancy and lactation.
Should be used with caution in patients with liver dysfunction.
Atorvastatin therapy should be temporarily withheld or discontinued in any patient with an acute, serious condition suggestive of a myopathy or having a risk factor predisposing to the development of renal failure secondary to rhabdomyolysis (eg, severe acute infection, hypotension, major surgery, trauma, severe metabolic, endocrine and electrolyte disorders, and uncontrolled seizures).
The risk of myopathy during treatment with drugs of this class is increased with concurrent administration of cyclosporine, fibric acid derivatives, niacin (nicotinic acid), erythromycin, azole antifungals.
Should be used with caution when given concomitantly with digoxin, erythromycin and oral contraceptives.
Can be safely administered with antipyrine, cimetidine and warfarin.
Lipofix is generally well tolerated.
Adverse reactions have usually been mild and transient.
The most frequent adverse events are constipation, flatulence, dyspepsia, and abdominal pain.
Dosage & Administration
The recommended starting dose of Atorvastatin is 10 mg once daily.
The dosage range is 10 to 80 mg once daily.
Atorvastatin can be administered as a single dose at any time of the day, with or without food.
There is no specific treatment for Atorvastatin over-dosage.
In the event of an overdose, the patient should be treated symptomatically and supportive measures instituted as required.
Store in a cool & dry place. Protect from light.