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Atorvastatin Mechanism of Action side effects and PharmacoKinetics

Atorvastatin is used to treat high cholesterol, and to lower the risk of stroke, heart attack, or other heart complications in people with type 2 diabetes, coronary heart disease, or other risk factors.
Atorvastatin is used in adults and children who are at least 10 years old.
Atorvastatin may also be used for purposes not listed in this medication guide.

 Mechanism of Action
Atorvastatin decreases the production of LDL cholesterol by blocking the action of the enzyme in the liver (called HMG-CoA reductase) that is responsible for its production. This decreases the amount of cholesterol in the liver cells, which causes them to take up LDL cholesterol from the blood. The decreased cholesterol production and increased removal of LDL cholesterol from the blood ultimately results in lowered blood cholesterol levels.
As the body produces most cholesterol at night, statins are generally more effective if taken at night.
Atorvastatin also causes a small decrease in the production of other 'bad fats' in the blood called triglycerides, and a small increase in the level of HDL cholesterol. This results in lowered levels of 'bad fats' and raised levels of 'good fats' in the blood.

Atorvastatin side effects

Stop taking atorvastatin and call your doctor at once if you have any of these serious side effects:
  • unexplained muscle pain, tenderness, or weakness;
  • fever, unusual tiredness, and dark colored urine;
  • swelling, weight gain, urinating less than usual or not at all; or
  • nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).
Less serious atorvastatin side effects may include:

    mild muscle pain;

    diarrhea; or

    mild nausea.

PharmacoKinetics

Volume of distribution is found to be 5.4 and plasma protien binding is 98%. and metabolism is reported Hepatic. Renal Excretion accounts for 2% and plasma half life is 14 hr.

Pregnancy and breastfeeding

Certain medicines should not be used during pregnancy or breastfeeding. However, other medicines may be safely used in pregnancy or breastfeeding providing the benefits to the mother outweigh the risks to the unborn baby. Always inform your doctor if you are pregnant or planning a pregnancy, before using any medicine.

 This medicine should not be used during pregnancy because it may be harmful to a developing foetus. Pregnancy should also be avoided for one month after stopping treatment. Women who could get pregnant should use an effective method of contraception to prevent pregnancy both during treatment with this medicine and for one month after stopping treatment. Seek further medical advice from your doctor.
    It is not known if this medicine passes into breast milk. For this reason, the manufacturer states that it should not be used during breastfeeding. Seek medical advice from your doctor.

Usual Adult Dose for Hyperlipidemia

Initial dose: 10, 20 or 40 mg orally once a day. The 40 mg starting dose is recommended for patients who require a reduction in LDL-cholesterol of more than 45%.

Dose adjustments should be made at intervals of 2 to 4 weeks.

Maintenance dose: 10 to 80 mg orally once a day.
Usual Pediatric Dose for Heterozygous Familial Hypercholesterolemia

10 to 17 years:
10 mg per day (max dose is 20 mg per day). Adjustments should be made at intervals of 4 weeks or more.
Renal Dose Adjustments

No adjustment recommended
Liver Dose Adjustments

Atorvastatin is contraindicated in patients with active liver disease or with unexplained elevation of liver function enzyme levels.
Dose Adjustments

Adjustments in dosage should be made in intervals of 2 to 4 weeks.
Dialysis

Hemodialysis is not expected to significantly enhance clearance of atorvastatin
since the drug is extensively bound to plasma proteins.
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Ditulis oleh: Unknown - Wednesday 6 April 2011