Magazine article Drug Topics

Potent Stuff

Magazine article Drug Topics

Potent Stuff

Article excerpt

The more the merrier! exclaimed Frederick S. Mayer, R.Ph., MPh., Pharmacists Planning Service Inc., Sausalito, Calif. He was reading to the recent approval ot a third-generation HMG-CoA reductase inhibitor, BAYCOL (cerivastatin sodium). Mayer, who's involved in cholesterol counseling programs, is one of many health-care providers who have been welcoming the growing statins with open arms. The class, which inhibits cholesterol biosynthesis, has received much praise for its recently shown risk reductions of coronary events.

The new lipid buster, made by Bayer Pharmaceutical Division, West Haven, Conn., appears to be one of the more potent statins. According to Evan Stein, M.D., Ph.D., Metabolic & Atherosclerosis Research Center, Cincinnati, 0.3 mg of cerivastatin achieves the same reductions in LDL cholesterol as approximately 5 mg of atorvastatin, 10 mg of simvastatin, 20 mg of lovastatin, 20 mg to 30 mg of pravastatin, and 40 mg to 60 mg of fluvastatin. Doses of 0.2 mg to 0.3 mg of the new drug have been shown in clinical trials to produce a 28% reduction in LDL levels, a 13% reduction in triglycerides, and a 10% increase in HDL cholesterol.

But the drug-interaction department is where cerivastatin really comes out ahead. Unlike others, the new statin was not shown in clinical studies to interact with warfarin, digoxin, cimetidine, and antacids. Concomitant use of cerivastatin with certain antihypertensives and nonsteroidal anti-inflammatory drugs (NSAIDs) also showed no evidence of clinically significant adverse effects. The reason, as explained by Stein, is none other than an available detour. "Cerivastatin is able to use an alternative metabolic pathway if one is blocked by a drug such as warfarin."

But not all interactions have been eliminated. Steady-state cerivastatin AUC and C",a were reported to increase approximately 50% and 24%, respectively, after 10 days of coadministration with erythromycin. Concurrent use of other statins with cyclosporine, fibric acid derivatives, erythromycin, azole antifungals, and lipid-lowering doses of niacin, has been associated with a risk of myopathy. A warning to that effect is maintained with cerivastatin.

Liver function tests (LFTs) are a must, as with use of all statins, because the class has been associated with biochemical abnormalities of hepatic function. The actual effects of the statins on the liver are not really known, since no one has been kept on the drugs indefinitely, Stein said. …

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