Treatment of hypercholesterolaemia in cardiovascular diseases — what target, which statin, what dose?

Abstract

Low-density-lipoprotein cholesterol (LDL-C) is recommended as the primary target for treatment. In patients at very high cardiovascular risk (established cardiovascular disease [CVD], diabetes, moderate to severe chronic kidney disease or a SCORE level ≥ 10%), the LDL-C goal is < 70 mg/dL or a ≥ 50% LDL-C reduction, when target level cannot be reached. In patients at high cardiovascular risk (markedly elevated single risk factors, a SCORE level ≥ 5 to < 10%) a LDL-C goal < 100 mg/dL should be considered. In subjects at moderate risk LDL-C goal < 115 mg/dL should be considered. If drug treatment is indicated to decrease LDL-C, a statin is recommended, up to the highest tolerable dose, to reach the target level. Current available evidence suggests that the clinical benefit is largely independent of the type of statin but depends on the extent of LDL-C lowering; therefore, the type of statin used should reflect the degree of LDL-C reduction that is required to reach the target LDL-C in a given patient.

In the majority of patients with high and very high cardiovascular risk, the goal of therapy can be achieved using one of two statins available on the Polish pharmaceutical market: rosuvastatin or atorvastatin. Both statins are available in a wide range of doses (rosuvastatin 5 mg, 10 mg, 15 mg, 20 mg, 30 mg, 40 mg; atorvastatin 10 mg, 20 mg, 30 mg, 40 mg, 60 mg, 80 mg). The dose of 15 mg rosuvastatin allows of a reduction of LDL-C level by 49–50%, which is the target recommended by the Guidelines when using the smallest necessary dose.

Statins differ in their absorption, bioavailability, plasma protein binding, excretion and solubility. Many statins undergo significant hepatic metabolism via cytochrome P450 isoenzymes, except pravastatin, rosuvastatin and pitavastatin. Although statin treatment has beneficial effects in the prevention of CVD, interindividual variation exists in response to statin therapy, as well as in the incidence of adverse effects.