Lipitor Indication:

For management as an adjunct to diet to reduce elevated total-C, LDL-C, apo B, and TG levels in patients with primary hypercholesterolemia and mixed dyslipidemia.

Lipitor Mechanism Of Action:

Lipitor selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. As HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, this results in a decrease in mevalonate, a precursor of cholesterol, and a subsequent decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol.

Lipitor Drug Interactions:

Amprenavir Amprenavir can possibly increase the statin
Atazanavir Atazanavir increases the effect and toxicity of the statin
Bosentan Bosentan could decrease atorvastatin
Carbamazepine Carbamazepine decreases the effect of the statin
Clarithromycin The macrolide possibly increases the statin toxicity
Cyclosporine Possible myopathy and rhabdomyolysis
Delavirdine The NNRT inhibitor increases the effect and toxicity of the statin
Diltiazem Diltiazem increases the effect and toxicity of atorvastatin
Efavirenz The NNRT inhibitor increases the effect and toxicity of the statin
Erythromycin The macrolide possibly increases the statin toxicity
Fenofibrate Increased risk of myopathy/rhabdomyolysis
Fluconazole Increased risk of myopathy/rhabdomyolysis
Fosamprenavir Amprenavir can possibly increase the statin toxicity
Gemfibrozil Increased risk of myopathy/rhabdomyolysis
Imatinib Imatinib increases the effect and toxicity of atorvastatin
Indinavir Indinavir increases the effect and toxicity of atorvastatin
Itraconazole Increased risk of myopathy/rhabdomyolysis
Josamycin The macrolide possibly increases the statin toxicity
Ketoconazole Increased risk of myopathy/rhabdomyolysis
Nefazodone Nefazodone increases the effect and toxicity of the statin drug
Nelfinavir Nelfinavir increases the effect and toxicity of the statin
Nevirapine The NNRT inhibitor increases the effect and toxicity of the statin
Quinupristin This combination presents an increased risk of toxicity
Rifabutin The rifamycin decreases the effect of the statin drug
Rifampin The rifamycin decreases the effect of the statin drug
Ritonavir Ritonavir increases the effect and toxicity of the statin
Saquinavir Saquinavir increases the effect and toxicity of atorvastatin
Tacrolimus Tacrolimus increases the effect and toxicity of the statin
Telithromycin Telithromycin may possibly increase statin toxicity
Verapamil Verapamil increases the effect and toxicity of the statin
Bezafibrate Increased risk of myopathy/rhabdomyolysis
Colchicine Increased risk of rhadbomyolysis with this combination

Lipitor Food Interactions:

Avoid drastic changes in dietary habit.
Avoid alcohol.
Avoid taking grapefruit or grapefruit juice throughout treatment.
Grapefruit can significantly increase serum levels of this product.
Take with low fat meal.
Food may decrease maximum plasma levels and area under the curve, but this is inconsequential according to the manufacturer.

Lipitor Generic Name:

Synonyms:

  • Atorvastatin calcium

Drug Type:

Small Molecule; Approved

Absorption:

Atorvastatin is rapidly absorbed after oral administration. The absolute bioavailability of atorvastatin (parent drug) is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%.

Toxicity (Overdose):

Symptoms of overdose include rhabdomyolysis, eye hemorrhages, and liver problems.

Protein Binding:

98%

Biotransformation:

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.

Half Life:

14 hours

Dosage Forms of Lipitor:

Tablet Oral

Chemical IUPAC Name:

(3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid

Organisms Affected:

Humans and other mammals

Lipitor to general, pharmacology

General, pharmacology..