Pravastatin is a cholesterol lowering drug whose mechanism of action is the inhi

Question

Pravastatin is a cholesterol lowering drug whose mechanism of action is the inhibition of HMG-CoA reductase. If a patient takes a 40.0 mg dose of pravastatin, what is the concentration of pravastatin in the blood? Assume the patient has 5.0 L of blood. The molecular weight of pravastatin is 425. Pravastatin is a competitive inhibitor of HMG-CoA reductase with a Ki of 2.3 x 10^-3 MuM. What fraction of the enzyme will have a bound substrate under the conditions described above? Assume the concentration of HMG-CoA is 14 MuM, and the KM for HMG-CoA reductase is 1.4 MuM. After a period of time, all but 0.10% of the pravastatin in the blood is metabolized. What fraction of the enzyme will have bound substrate under these conditions?

Explanation / Answer

Concentration can be calculated as:

= mass/ volume X molecular weight

= 40/ 5 X 425

= 18.8235 micromolar

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