Generic

Atorvastatin Calcium

Indications

Primary hypercholesterolemia is a condition in which there is an abnormally high level (heterozygous familial and nonfamilial), Dyslipidemia with a mix of lipids, Homozygous familial hypercholesterolemia, Hypertriglyceridemia, Familial hypercholesterolemia, Preventing cardiovascular events, Primary dysbetalipoproteinemia

Pharmacology

Atorvastatin is a selective HMG-CoA reductase inhibitor. This enzyme is responsible for the rate-limiting 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, as well as increasing the number of hepatic LDL receptors on the cell surface, allowing for improved LDL uptake and catabolism.

Dosage & Administration

Adults with primary hypercholesterolemia and mixed hyperlipidemia:

• Usually, 10 mg once a day; if necessary, may be raised at least every 4 weeks to a maximum of 80 mg once daily.
• Child (10-18 years): Start with 10 mg once daily, then gradually raise to the normal maximum of 20 mg once a day at least 4-week intervals.

Adults with familial hypercholesterolemia:

• Start with 10 mg daily and gradually increase to 40 mg once daily over at least 4 weeks; if required, increase to a maximum of 80 mg once daily (or 40 mg once daily combined with anion-exchange resin in heterozygous familial hypercholesterolemia).
• Child (10-18 years): Start with 10 mg once day and gradually raise to the normal maximum of 80 mg once daily at at least 4-week intervals.
  Adults: Start with 10 mg once day and gradually increase based on response.

Interaction

May increase risk of myopathy and rhabdomyolysis w/ CYP3A4 potent inhibitor (e.g. HIV or HCV protease inhibitors, itraconazole, clarithromycin), fenofibrate, colchicines, fixed combination of lopinavir/ritonavir. With a CYP3A4 inducer, plasma concentrations may be reduced (e.g. rifampicin, efavirenz). Digoxin AUC and peak plasma concentrations may be significantly increased. AUC for norethindrone and ethinyl estradiol has increased.

Contraindications

Hypersensitivity, active liver disease or unexplained persistent serum transaminase elevations, porphyria, pregnancy, and lactation

Side Effects

In most cases, Frenvas 10 is well tolerated. Constipation, flatulence, dyspepsia, and stomach discomfort are the most common adverse effects of Atorvastatin. Infection, headache, back pain, rash, asthenia, arthralgia, and myalgia are some of the other adverse effects.

Pregnancy & Lactation

During pregnancy, Frenvas 10 is not recommended. Pregnant women’s safety has not been demonstrated. There have been no controlled clinical studies using atorvastatin in pregnant women. There have been a few instances of congenital abnormalities following intrauterine exposure to HMG-CoA reductase inhibitors. Animal investigations have revealed that it is harmful to reproduction. Maternal Frenvas 10 therapy may lower fetal levels of mevalonate, a precursor of cholesterol production. Frenvas 10 should not be taken in pregnant women, women who are attempting to get pregnant, or women who believe they are pregnant. Treatment with atorvastatin should be discontinued for the length of the pregnancy or until the woman is proven to be not pregnant.

The presence of atorvastatin or its metabolites in human milk is unknown. The plasma concentrations of atorvastatin and its active metabolites in rats are comparable to those found in milk. Women taking atorvastatin should not breastfeed their children due to the risk of significant adverse effects. Taking atorvastatin during nursing is not advised.

Precautions & Warnings

Patients who drink a large amount of alcohol. A family history of liver disease. Patients who are at risk for myopathy or rhabdomyolysis. Prior to beginning statin treatment, hypothyroidism should be well controlled. Children under the age of ten Females in their premenstrual period. Lactation: Because of the risk of adverse effects in nursing infants, women taking this medication should not breastfeed; nursing moms should avoid taking it.

Therapeutic Class

Statins and other anti-anginal and anti-ischemic medications

Storage Conditions

Keep away from light and heat in a dry area. Keep out of children’s reach.

Pharmaceutical Name

Radiant Pharmaceuticals Ltd.