What is Lipitor?
Lipitor is a brand name for drug atorvastatin, which is a newer selective and competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme (HMG-CoA) reductase that belongs to a group of drugs known as statins. Atorvastatin was synthesized in 1985 and its development was mostly based on molecular comparisons of fungal metabolites and other synthetic inhibitors.
Atorvastatin is approved for the reduction of elevated total cholesterol, LDL cholesterol, apo B and triglyceride levels, but its usage also leads to an increase of HDL cholesterol in individuals with primary hypercholesterolemia and mixed dyslipidemia. Furthermore, the drug is approved for use in patients with dysbetalipoproteinemia and elevated triglyceride levels, as well as for the prevention of cardiovascular diseases.
Lipitor tablets for oral administration are …show more content…
Still, its absolute bioavailabilty is low (approximately 12%), which is due to high hepatic first-pass metabolism, but also presystemic metabolism (primarily in the gut wall). Atorvastatin concentrations in plasma are lower after evening drug administration in comparison to morning administration.
Two active metabolites can be found in plasma - 2-hydroxy-atorvastatin and 4-hydroxy-atorvastatin - both of which are in equilibrium with their respective inactive lacotne forms. It must be emphasized that 70% of circulating inhibitory activity for the enzyme HMG-CoA reductase can be attributed to this pair of active metabolites.
The half-life of atorvastatin is approximately 20 hours, which is often increased in individuals with hepatic disease. The biliary tract represents the major route of elimination, and less than 2% of the drug is excreted as unchanged in urine; therefore changes in renal function have no significant effect on the pharmacokinetcis of
Lipitor is a brand name for drug atorvastatin, which is a newer selective and competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme (HMG-CoA) reductase that belongs to a group of drugs known as statins. Atorvastatin was synthesized in 1985 and its development was mostly based on molecular comparisons of fungal metabolites and other synthetic inhibitors.
Atorvastatin is approved for the reduction of elevated total cholesterol, LDL cholesterol, apo B and triglyceride levels, but its usage also leads to an increase of HDL cholesterol in individuals with primary hypercholesterolemia and mixed dyslipidemia. Furthermore, the drug is approved for use in patients with dysbetalipoproteinemia and elevated triglyceride levels, as well as for the prevention of cardiovascular diseases.
Lipitor tablets for oral administration are …show more content…
Still, its absolute bioavailabilty is low (approximately 12%), which is due to high hepatic first-pass metabolism, but also presystemic metabolism (primarily in the gut wall). Atorvastatin concentrations in plasma are lower after evening drug administration in comparison to morning administration.
Two active metabolites can be found in plasma - 2-hydroxy-atorvastatin and 4-hydroxy-atorvastatin - both of which are in equilibrium with their respective inactive lacotne forms. It must be emphasized that 70% of circulating inhibitory activity for the enzyme HMG-CoA reductase can be attributed to this pair of active metabolites.
The half-life of atorvastatin is approximately 20 hours, which is often increased in individuals with hepatic disease. The biliary tract represents the major route of elimination, and less than 2% of the drug is excreted as unchanged in urine; therefore changes in renal function have no significant effect on the pharmacokinetcis of