Pharmacodynamics and Pharmacokinetics of Lipitor Case Study

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Lipitor is a brand name of Atorvastatin, one of the most commonly prescribed medications in the United States. Atorvastatin belongs to the statin family of drugs, which react with specific enzymes in order to lower cholesterol in the body. Lipitor/atorvastatin inhibits HMG-CoA reductase, an enzyme that "converts 3-hydroxy-3methylglutaryl-coenzyme A to mevalonate, a precursor of sterols" like cholesterol ("Lipior," n.d.).

Elevated plasma levels of total cholesterol (both LDL-cholesterol or LDL-C and HDL) as well as levels of apolipoprotein B (apo B) are known precursors or risk factors in human atherosclerosis and are risk factors for developing cardiovascular disease. By reducing the amount of cholesterol in plasma as well as in the liver, the drug helps to prevent atherosclerosis and cardiovascular disease. Lipitor is effective in addressing elevated cholesterol due to hereditary hypercholesterolemia, as well as nonfamilial types. Lipitor is indicated for patients with increased risk of myocardial infarction, stroke, and angina.

The drug is primarily active in the liver, which is the primary site of cholesterol synthesis ("Lipitor," n.d.). After metabolism in the liver, Lipitor and its metabolites are eliminated in bile. Very little of the drug is eliminated in urine. The "mean plasma elimination half-life of Lipitor in humans is approximately 14 hours, but the half-life of inhibitory activity for HMG-CoA reductase is 20 to 30 hours due to the contribution of active metabolites," ("Lipitor," n.d.).

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Ideally, Lipitor is an adjunct to diet, but it can also be effective for patients whose cholesterol levels do not respond to dietary changes.

Lipitor is taken orally, and is rapidly absorbed; "maximum plasma concentrations occur within 1 to 2 hours," ("Lipitor," n.d.). Starting dose is 10-20mg taken once per day, but can be prescribed up to 80mg per day depending on the patient's response. The drug can be taken with or without food; food only slightly inhibits the rate of absorption but not the overall effectiveness of the drug in LDL-C reduction ("Lipitor," n.d.). Metabolism of Lipitor is rapid and relatively thorough, as it is "extensively metabolized to ortho -- and parahydroxylated derivatives and various beta-oxidation products," ("Lipitor," n.d.). The drug works by "increasing the number of hepatic LDL receptors on the cell surface to enhance uptake and catabolism of LDL," ("Lipitor," n.d.).

"The absolute bioavailability of atorvastatin (parent drug) is approximately 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%," ("Lipitor," n.d.). In terms of distribution, " LIPITOR….....

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