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Atorvastatin

Atorvastatin, marketed under the trade name Lipitor among others, is a member of the drug class known as statins, which are used primarily as a lipid-lowering agent and for prevention of events associated with cardiovascular disease. More

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Description

Atorvastatin, marketed under the trade name Lipitor among others, is a member of the drug class known as statins, which are used primarily as a lipid-lowering agent and for prevention of events associated with cardiovascular disease.

Generic Name

Atorvastatin

Chemical names

Atorvastatin; Cardyl; Tozalip; Xavator

Brand names

Unitor (10mg), Stator (40mg), Lorisk (10mg/160mg/5mg), Etovas (20mg), Mactor (10mg), Genxvast (10mg), Noklot-CV, Atornet (5mg), Nustat (10mg), Atorva (80mg), Atarp (20mg), Zenolip (10mg), Redustat Plus (10mg/200m

IUPAC name

7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-(propan-2-yl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoate

Pharmacokinetics

  • Absorption: Oral
  • Distribution: 99% protein binding
  • Metabolism: Hepatic
  • Excretion: Feces

Actions

Atorvastatin selectively and competitively inhibits the hepatic enzyme HMG-CoA reductase. As HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate in the cholesterol biosynthesis pathway, this result in a subsequent decrease in hepatic cholesterol levels. A decreased hepatic cholesterol level stimulates upregulation of hepatic LDL-C receptors which increases hepatic uptake of LDL-C and reduces serum LDL-C concentrations.

Dosage/Dosage form

Initially, 10 or 20 mg/day may increase at 4-weekly intervals. 

Therapeutic uses

Coronary heart disease

Adverse effects/Side effects

Headache, diarrhoea, flatulence, nausea, vomiting, anorexia, xerostomia, angioedema, myalgia, rash/pruritus, alopecia, and allergy, infection, and chest pain.

Interaction

  • Increased AUC for norethindrone and ethinyl estradiol.
  • Co-admin with antacid suspensions and colestipol decreased atorvastatin levels.
  • Increased risk of rhabdomyolysis when used concurently with fibrates.
  • Concomitant multiple doses of digoxin and atorvastatin increased steady-state digoxin levels. 

Contraindications

Hypersensitivity, liver disease, porphyria, pregnancy, unexplained persistent elevations of serum transaminase and lactation.

Storage

Store it at room temperature

Information

Molecular weight

557.6319

Molecular formula

C33H34FN2O5

CAS number

134523-00-5

Precautions

  • Hypothyroidism should be properly managed prior to starting statin therapy.
  • History of liver disease.
  • Patients who consume substantial quantities of alcohol.
  • Patients with risk factors for myopathy or rhabdomyolysis.
  • Children <10 years.