30:718:409 Lecture Notes - Lecture 27: Pitavastatin, Lactone, Cyp3A4

• School: Rutgers University
• Department: Pharmacology and Toxicology
• Course: 30:718:409
• Professor: Dr. Lavoie and Dr. Chakalamanil

Document Summary

Pitavastatin (calcium salt, livalo : the drug substance is a single enantiomer, metabolism, the major metabolite in the plasma is the lactone formed via glucuronidation by udp- glucuronosyltrasferase (ugt, no major metabolism by cyp3a4. Therefore, it is not likely to have ddi with cyp3a4 metabolized drugs. The 40mg dose is restricted to only those who don"t respond to lower doses. (80mg dose has increased risk of rhabdomyolysis: rosuvastatin is not extensively metabolized. The major metabolite is n-desmethyl rosuvastatin, which is formed cyp2c9 which is less active than rosuvastatin: cyp 3a4 is not a major metabolizing enzyme for rosuvastatin. Outcome studies: primary prevention: rosuvastatin significantly reduced the risk of major cv events (mi, stroke) Indications: familial hypercholesterolemia, hypertriglyceridemia, primary prevention and secondary prevention of cv diseases, fluvastatin is metabolized by cyp2c9 and cyp3a4 to active hydroxylated metabolites, but they do. Therefore they are not likely to have ddi with drugs that alter the activity of this enzyme.