The extent of LDL reduction depends on the dose of the drug rather than on the plasma drug concentration. The liver is the main target organ of action, being the principal site of cholesterol synthesis and LDL clearance. Study predicts that different statins exhibit divergent effects on host response to SARS-CoV-2 infectionĪtorvastatin and its active metabolites are all pharmacologically active.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. The elimination half-life of a drug is defined as the time required for the concentration of the drug in the body to be reduced to half. Less than 2% of the drug is passed in urine.
These active derivatives account for almost 70% of HMG-CoA reductase inhibitory activity.Įxcretion: Atorvastatin and its metabolites are eliminated by biliary secretion. Metabolism: Atorvastatin acid is extensively metabolized into its active derivatives in the gut and liver by chemical reactions such as oxidation, lactonisation and glucuronidation. Changes in rate of atorvastatin absorption are not expected to have a clinically significant effect hence atorvastatin can be taken with or without food.ĭistribution: Atorvastatin has a volume of distribution of approximately 381 litres and the drug is =98% bound to plasma proteins. This phenomenon is termed as first-pass metabolism.įood decreases the rate of drug absorption however, it doesn’t interfere much with the extent of drug absorption. Higher concentrations of the drug are found in older adults (age 65 years or older), women and patients with chronic alcoholic liver disease.Ītorvastatin undergoes metabolism in the gastrointestinal mucosa and the liver before it reaches the systemic circulation. Plasma concentrations of atorvastatin also depend on the population being treated. Maximum plasma concentrations occur within 1 to 2 hours and the extent of absorption increases with the increase in dose. PharmacokineticsĪbsorption: Atorvastatin is rapidly absorbed after oral administration. The drug’s chemical structure decides its water solubility, which ultimately influences the pharmacokinetic properties - absorption, distribution, metabolism and excretion. Image Credit: Ching Design / Shutterstock Pharmacokinetics and Pharmacodynamics of AtorvastatinĪll drugs belonging to the drug class statins share a common mechanism of action however, they differ in terms of their structures, pharmacokinetic profiles and efficacy. HDL cholesterol and LDL cholesterol in artery.
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