Mechanism | Reversibly inhibits HMG CoA reductase - the rate limiting enzyme in cholesterol synthesis by the liver Liver responds by increased LDL receptor expression taking in more LDL to plasma cholesterol |
Typical Dose | 40mg OD to be increased up to 80mg. Taking at night improves efficacy |
Indications | Hypercholesterolaemia |
Contra-indications | * Active liver disease/persistently deranged LFTs * Pregnancy/breast feeding * When taking clarithromycin |
Side-effects | * Myositis (achy muscles), may lead to rhabdomyolysis |
Interactions | * Clarithromycin - increased exposure to simvastatin * Cylcosporin - increased risk of myositis * Fibrate - increased risk of myositis * Warfarin - increased exposure to Warfarin |
Elimination | ABC transporter mediated biliary excretion |
Additional Notes | Only prescribe if diet modification has failed and secondary causes of hyperlipidaemia have been ruled out. Regular LFTs before/during treatment. |