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Tuesday, March 10, 2015

Side Effects Of Atorvastatin

What is atorvastatin?


Atorvastatin belongs to the Group of medicines which are called cholesterolsynthese inhibitors or statinen. It is a specific competitive inhibitor of HMG-CoA reductase, an enzyme that plays an essential role in the biosynthesis of cholesterol. Inhibition of this synthesis include increase in the number of LDL receptors in the liver to result; This results in lowering of LDL-cholesterol concentration. It lowers triglycerides and apolipoprotein B and also increases in varying degree the HDL cholesterol and apolipoprotein a.

About 70% of the activity is attributed to active metabolites. Operation: within 2 weeks, max. within 4 weeks.

Indications


  • Adjunct to diet in adults and children ≥ 10 years with primary hypercholesterolemia including familial hypercholesterolemia (heterozygous variant) or combined (mixed) hyperlipidemia when diet and other measures alone are not sufficient for reduction of elevated total cholesterol, LDL cholesterol, apolipoprotein B and triglycerides.
  • In adults with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments or if such treatments are available to reduce total and LDL cholesterol.
  • Not officially registered: Prevention of cardiovascular disease in adult patients with a high chance of a cardiovascular event, as an adjunct to correction of other risk factors.


Kinetic data

  • Resorption: fast.
  • Biological beschikbaarhied = 12% by large first-pass effect in intestinal mucosa and liver.
  • Maximum mirror = 1 – 2 hours.
  • Plasma protein binding: > 98%.
  • Partition volume = ca. 5,4 l/kg.


Plasma concentrations of atorvastatin and its active metabolites in chronic alcoholic liver disease increased. Metabolism: Because CYP3A4 to active ortho and parahydroxylated derivatives and various β-oxidation products.

  • Elimination mainly through the liver.
  • Elimination half-life = 14 hours (atorvastatin), longer (active metabolites).

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Atorvastatin side effects


At Times

  • Gastrointestinal symptoms (nausea, abdominal pain, constipation, flatulence, heartburn or diarrhea)
  • Headache, dizziness, blurred vision, fatigue, insomnia
  • Skin rash, itching, redness


Rarely

  • Severe hypersensitivity reaction
  • Muscle pain, joint pain, muscle weakness and muscle cramps
  • Weakness, chest pain or back pain


Very rare

  • Liver inflammation
  • Inflammation of the pancreas
  • Numbness or tingling in the limbs
  • Hair Loss
  • Weight gain
  • Impotence


In January 2005, Pfizer is the Pharmaceutical Advertising Code Commission (CGR) condemned because they had been advertising expressions that Lipitor on side effects is just as safe as a placebo and the deadly side effect rhabdomyolysis had concealed. The Code Commission also found that medical representatives from Pfizer misleading statements are made about the safety of Lipitor. The committee spoke of a "serious violation" of the Medicines Act, which Pfizer is charged heavily.

Interactions


Atorvastatin is a substrate for CYP3A4. The risk of myopathy is increased by concomitant use of drugs that increase CYP3A4 moderate to heavy braking and plasma concentration of ciclosporin, azole antifungal (itraconazole), macrolide antibiotics, large quantities of grapefruit juice and HIV protease inhibitors.

  • Cyclosporine (immunosuppressive agent)
  • Erythromycin, azithromycin and clarithromycin (antibiotics) and Imatinib (chemotherapy)
  • Efavirenz and Nevirapine, and other anti-HIV and AIDS
  • Diltiazem and verapamil (cardiovascular medicines)
  • Gemfibrozil (Lopid) = cholesterol and other lipid lowering agent)

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