Metabolization of Simvastatin
Simvastatin is a statin drug used in combination with diet, weight loss and exercise to treat hypercholesterolemia and hypertriglyceridemia and to reduce mortality and the incidence of cardiovascular events in high-risk individuals.
Simvastatin is hydrolyzed in the liver to its ß-hydroxyacid active form, which is a potent HMG-CoA reductase inhibitor that catalyzes the conversion of HMG-CoA to mevalonate, the initial and limiting step of cholesterol biosynthesis.
Hypersensitivity, active liver disease or persistent and unexplained elevations of serum transaminases, pregnancy, lactation, concomitance with potent inhibitors of CYP3A4 (itraconazole, ketoconazole, posaconazole, voriconazole, HIV protease inhibitors (nelfinavir), boceprevir, telaprevir, erythromycin, clarithromycin, telithromycin, nefazodone, gemfibrozil, cyclosporin or danazol.
Cautions mut be taken when there is severe renal impairment and in patients who consume large amounts of alcohol. Monitor and discontinue the treatment if serum transaminases exceed 3 times ULN (upper limit of normal). Risk of muscle disorders (myalgia, myopathy, and rarely rhabdomyolysis), it is mandatory to watch for muscle sensitivity, muscle weakness or muscle cramps.
Warnings and precautions for patients with factors predisposing to rhabdomyolysis (IR, hypothyroidism, previous history of muscle toxicity by a statin or fibrate, personal or family history of hereditary muscular diseases or alcoholism, elderly patients, women), determine values of creatine kinase CK (do not start if CK> 5 times ULN).
Risk of developing immune-mediated necrotizing myopathy. Interrupt temporarily in case of major surgery.
Not recommended for children
Constipation, dyspepsia, flatulence, nausea, vomiting, abdominal pain, anorexia. Insomnia, fatigue, headache, depression, memory loss, blurred vision, tinnitus. Eruption, alopecia. Rhinosinusitis. Nasopharyngitis, flu-like syndrome.
Transitory elevation of transaminases and creatine kinase. Myalgias, myositis, rabdomiolisi. Thrombocytopenia. Chest pain, peripheral edema. Hyper / hypoglycemia.
There are pharmacological interactions associated with increased risk of myopathy / rhabdomyolysis.
Simvastatine increases the effect of oral anticoagulants (it is mandatory to determine prothrombin time before starting treatment and often at the beginning of treatment).
- Alcosin ®
- Arudel ®
- Belmalip ®
- Colemin ®
- Glutasey ®
- Histop ®
- Lipociden ®
- Pantok ®
- Zocor ®
GENE OR REGION STUDIED