Effects of HMG CoA Reductase Inhibitors on Cholesterol Synthesis
| Autor: | Alfred W. Alberts |
|---|---|
| Rok vydání: | 1990 |
| Předmět: |
chemistry.chemical_classification
7-Dehydrocholesterol reductase biology Cholesterol General Medicine Prodrug chemistry.chemical_compound Enzyme chemistry Biochemistry Simvastatin HMG-CoA reductase medicine biology.protein lipids (amino acids peptides and proteins) Pharmacology (medical) Lovastatin Pravastatin medicine.drug |
| Zdroj: | Drug Investigation. 2:9-17 |
| ISSN: | 1179-1918 0114-2402 |
| DOI: | 10.1007/bf03258189 |
| Popis: | Lovastatin (mevinolin) and simvastatin (epistatin) are lactone prodrugs, which, after conversion to their respective dihydroxy open acids, are very active inhibitors of HMG CoA reductase, the key rate-limiting enzyme in cholesterol biosynthesis. After oral administration of these agents, they are preferentially concentrated in the liver, the primary site of cholesterol biosynthesis. In the liver, the lactone prodrugs are converted to the active species. This results in specific inhibition of hepatic cholesterol synthesis. Associated with this inhibition is a decrease in urinary and plasma levels of mevalonate and a concomitant decrease in plasma LDL-cholesterol in experimental animals and man. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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