What is the pharmacodynamics of atorvastatin?
Atorvastatin competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. [2] By preventing the conversion of HMG-CoA to mevalonate, statin medications decrease cholesterol production in the liver. Atorvastatin also increases the number of LDL receptors on the surface of hepatic cells.
How is atorvastatin metabolised?
Atorvastatin acid is extensively metabolised in both the gut and liver by oxidation, lactonisation and glucuronidation, and the metabolites are eliminated by biliary secretion and direct secretion from blood to the intestine.
What is the mechanism of action of statin drugs?
Mechanism of Action Statins work by competitively blocking the active site of the first and key rate-limiting enzyme in the mevalonate pathway, HMG-CoA reductase. Inhibition of this site prevents substrate access, thereby blocking the conversion of HMG-CoA to mevalonic acid.
How quickly is atorvastatin metabolized?
The elimination half-life of atorvastatin is approximately 14 hours, but the half-life of inhibitory activity for HMG-CoA reductase is 20 to 30 hours due to the contribution from the active metabolites of atorvastatin.
What is the therapeutic class of atorvastatin?
Atorvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.
Is atorvastatin metabolized in the liver?
Atorvastatin is largely metabolized in the liver via CYP 3A4 and excreted in bile. The mild, self-limited ALT elevations are likely due to a toxic intermediate of drug metabolism and the reversal of these elevations due to adaptation.
What is the molecular weight of atorvastatin?
558.64 g/mol
Atorvastatin/Molar mass
What is the role of atorvastatin?
What is the cause behind action of statins?
How Statins Work. Statin drugs work by blocking the action of the liver enzyme that is responsible for producing cholesterol. Too much cholesterol in the blood can cause a buildup of plaque on the walls of the arteries.
Is Atorvastatin metabolized in the liver?
How is rosuvastatin metabolized?
Rosuvastatin is metabolized mainly by CYP2C9 and not extensively metabolized; approximately 10% is recovered as metabolite N-desmethyl rosuvastatin. It is excreted in feces (90%) primarily and the elimination half-life is approximately 19 hours.