Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027121 (myositis)
 4,538 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Fluvastatin sodium (Lescol; Sandoz) the first entirely synthetic 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor studied, is structurally distinct from the other HMG-CoA reductase inhibitors currently available, all of which are fungal metabolites and analogues of compactin. Fluvastatin's distinct structure may be responsible for the biopharmaceutical properties that result in its low systemic exposure and, subsequently, low incidence of peripheral adverse events, such as headache and myositis. Fluvastatin is rapidly absorbed from the gastrointestinal tract; has a 30-minute half-life, the shortest of any currently available HMG-CoA reductase inhibitor (lovastatin, 15 hours; pravastatin, 2 hours; simvastatin, 15.6 hours); is highly selective for the liver, undergoing extensive first-pass metabolism; has no active circulating metabolites; and does not penetrate the blood-brain barrier, unlike lovastatin and simvastatin. The low systemic exposure suggests that the occurrence of peripheral adverse events, such as myositis, central nervous system effects, and drug-drug interactions, may be less than what is currently observed with other HMG-CoA reductase inhibitors. Neither niacin nor propranolol had an effect on fluvastatin plasma levels when combined with fluvastatin. In contrast to other HMG-CoA reductase inhibitors, fluvastatin in combination with niacin resulted in no instances of myositis or other serious adverse events. Although the interaction of fluvastatin with cholestyramine resulted in a lower rate and extent of fluvastatin bioavailability, this reduction had no impact on clinical efficacy. Fluvastatin administered to patients chronically receiving digoxin had no effect on the area under the curve (AUC) of digoxin compared with controls.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Clinical implications of the biopharmaceutical properties of fluvastatin. 819 18

Fluvastatin was the first wholly synthetic statin to the market and is effective in reducing total and low density lipoprotein cholesterol, which translates into reductions in coronary heart disease events. The Lescol Intervention Prevention Study has established the effectiveness of the early use of statins in reducing recurrent events in high-risk patients with coronary heart disease post percutaneous coronary interventions. Fluvastatin is well-tolerated with few side effects. The occurrence of significant abnormalities in liver enzymes is infrequent, and the risk of myositis and rhabdomyolysis seems to be less than with other statins. There have been no reports of fatal rhabdomyolysis to date. The potential for drug interactions with fluvastatin is low. It seems safe in combination with cyclosporin and there have been few reports of rhabdomyolysis when using fluvastatin in combination with other lipid-lowering agents. It is nevertheless important to be vigilant for this potentially important side effect and, as with other statins, inform patients of the potential risk and suggestive symptoms. Fluvastatin provides a useful option in treating hypercholesterolaemia in patients at high risk of coronary heart disease.
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PMID:Fluvastatin. 1243 96

The management of dyslipidemia in adults with diabetes is receiving more attention. However, there is a paucity of large, prospective, randomized outcome trials designed for diabetic patients. Diabetic dyslipidemia is characterized by an increase in triglyceride levels, low high-density lipoprotein (HDL) cholesterol concentrations, and small, dense low-density lipoprotein (LDL) particles. The treatment goals include an LDL cholesterol less than 100 mg/dL, triglyceride level less than 150 mg/dL, and an HDL greater than 40 mg/dL for men and more than 50 mg/dL for women. In the Diabetic Atherosclerosis Intervention Study, fenofibrate resulted in a 42% less increase in the percent stenosis, as assessed by quantitative coronary arteriography. The Heart Protection Study documented the unambiguous benefit of simvastatin in reducing all-cause mortality among 5963 diabetic patients. The Lescol Intervention Prevention Study observed a reduction in major adverse cardiac events in diabetics undergoing percutaneous intervention who received fluvastatin. The Veterans Affairs HDL Cholesterol Intervention Trial reported a reduction in major coronary events among 627 diabetic patients with low HDL cholesterol who sustained a myocardial infarction. The Fenofibrate Intervention and Event Lowering in Diabetics (FIELD) Trial (n = 9795), the Action to Control Cardiovascular Risk in Diabetes (ACCORD, n = 10,000), the Atorvastatin Study for Prevention of Coronary Heart Disease Endpoints in Non Insulin Dependent Diabetes Mellitus (ASPEN, n = 2421), and the Collaborative Atorvastatin Diabetes Study (CARDS, n = 2140) will provide the prospective outcome data that are needed for the management of patients. Combination drug therapy will be necessary to achieve treatment goals. Careful monitoring will be required to avoid myositis and hepatotoxicity.
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PMID:Clinical trials and lipid guidelines for type II diabetes. 1505 51