[Dual inhibition of cholesterol using the drug combination ezetimibe/simvastatin?].
The latest clinical intervention studies of statins have shown that more aggressive reductions in LDL-cholesterol to values lower than existing target values for persons with a high risk of cardiovascular disease produce greater success in terms of halted progression and even regression of the atherosclerotic process and fewer cardiovascular events. This has lead to a series of international and national recommendations for a further reduction in target values for LDL-cholesterol, which is often difficult to achieve with the usual dosage of statins. The combination of a statin with ezetimibe, acting as a dual inhibition mechanism against the synthesis and absorption of cholesterol, reduces LDL-cholesterol significantly more than treatment with a statin in monotherapy. This allows many more patients to achieve the target value for LDL-cholesterol. At present a drug combination comprising ezetimibe 10 mg and simvastatin in all doses (10, 20, 40 and 80 mg) is being introduced into our market under the company name Inegy. In addition to reducing LDL-cholesterol by up to 61% this combination has a positive effect on a range of other parameters for lipid metabolism and inflamation. A typical initial dose of ezetimibe 10 mg/simvastatin 20 mg reduces LDL-cholesterol by around 50%, which is necessary for the stabilisation of atherosclerotic plaque. For patients requiring more aggressive reduction of LDL-cholesterol it is best to start with a dose of ezetimibe 10 mg/simvastatin 40 mg. The highest dose of 10 mg/80 mg is intended for patients with the highest level of risk and reduces LDL-cholesterol by around 60%. In all the studies that have been carried out so far, the combination of ezetimibe and statin was very well tolerated and the safety profile of this combination was the same a treatment with the statin alone. At present a wide range of large clinical studies are underway to test whether LDL-cholesterol reduction using the ezetimibe + statin combination will also lead to a lower risk of cardiovascular events.
Vaverková
H
H
III. interní klinika Lékarské fakulty UP a FN Olomouc. helena.vaverkova@fnol.cz
D000924:Anticholesteremic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D050197:Atherosclerosis / Q000517:prevention & control; D001384:Azetidines / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008078:Cholesterol, LDL / Q000097:blood*; D004338:Drug Combinations; D004359:Drug Therapy, Combination; D000069438:Ezetimibe; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics; D019821:Simvastatin / Q000008:administration & dosage* / Q000493:pharmacokinetics
D000924:Anticholesteremic Agents; D001384:Azetidines; D008078:Cholesterol, LDL; D004338:Drug Combinations; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D019821:Simvastatin; D000069438:Ezetimibe