Atorvastatin Calcium

A-Statin is indicated as an adjunct to diet to reduce elevated total cholesterol, LDL cholesterol, apolipoprotein B (Apo-B) and triglycerides levels in following diseases when response to diet and other non-pharmacological measures is inadequate.
To reduce total cholesterol and LDL cholesterol in patients with heterozygous and homozygous familial hypercholesterolemia.
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A-Statin is indicated as an adjunct to diet to reduce elevated total cholesterol, LDL cholesterol, apolipoprotein B (Apo-B) and triglycerides levels in following diseases when response to diet and other non-pharmacological measures is inadequate.
To reduce total cholesterol and LDL cholesterol in patients with heterozygous and homozygous familial hypercholesterolemia.
To reduce elevated cholesterol and triglycerides in patient with mixed dyslipidemia (Fredrickson Type Ia and Ib).
For the treatment of patients with elevated serum triglyceride levels in hypertriglyceridaemia (Fredrickson Type IV).
For the treatment of patients with dysbetalipoproteinaemia (Fredrickson Type III).
To reduce cardiac ischaemic events in patients with asymptomatic or mild to moderate symptomatic coronary artery disease with elevated LDL-cholesterol level.
To reduce total and LDL-cholesterol concentrations patients with hypercholesterolemia associated with or exacerbated by diabetes mellitus or renal transplantation.

Dosage & Administration

Primary hypercholesterolaemia and combined hyperlipidaemia-
Adults
: Usually 10 mg once daily; if necessary, may be increased at intervals of at least 4 weeks to max. 80 mg once daily.
Child (10-18 years)
: Initially 10 mg once daily, increased if necessary at intervals of at least 4 weeks to usual max. 20 mg once daily.
Familial hypercholesterolaemia-
Adults
: Initially 10 mg daily, increased at intervals of at least 4 weeks to 40 mg once daily; if necessary, further increased to max. 80 mg once daily (or 40 mg once daily combined with anion-exchange resin in heterozygous familial hypercholesterolaemia).
Child (10-18 years)
: Initially 10 mg once daily, increased if necessary at intervals of at least 4 weeks to usual max. 80 mg once daily.
Prevention of cardiovascular events-
Adults
: Initially 10 mg once daily adjusted according to response.
Another guideline
: The patient should be placed on a standard cholesterol-lowering diet before receiving Atorvastatin and should continue on this diet during treatment with Atorvastatin. The recommended starting dose of Atorvastatin is 10 or 20 mg once daily. Patients who require a large reduction in LDL-C (more than 45%) may be started at 40 mg once daily. The dosage range of Atorvastatin 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. After initiation of Atorvastatin lipid levels should be analyzed within 2 to 4 weeks and dosage adjusted accordingly.
In hypercholesterolemia in Pediatric Patients (10-17 years of age) the recommended starting dose of Atorvastatin is 10 mg/day; the maximum recommended dose is 20 mg/day (doses greater than 20 mg have not been studied in this patient population). Doses should be individualized according to the recommended goal of therapy. Adjustments should be made at intervals of 4 weeks or more.

A-Statin is generally well-tolerated. The most frequent side effects related to A-Statin are constipation, flatulence, dyspepsia, abdominal pain. Other side effects includes infection, headache, back pain, rash, asthenia, arthralgia, myalgia.

Atorvastatin is a selective inhibitor of HMG-CoA reductase. This enzyme is the rate-limiting enzyme responsible for the conversion of HMG-CoA to mevalonate, a precursor of sterols, including cholesterol. Atorvastatin lowers plasma cholesterol and lipoprotein levels by inhibiting HMG-CoA reductase and cholesterol synthesis in the liver and increases the number of hepatic LDL receptors on the cell surface for enhanced uptake and catabolism of LDL.
Absorption
: 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%.
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 coadministration with erythromycin, a known inhibitor of this isozymes. 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.