Atorvastatin (Lipitor)

Atorvastatin is a statin. It inhibits HMG-CoA reductase, the rate-limiting enzyme of the body's own cholesterol production in the liver. Less own production means the liver cell puts more LDL receptors on its surface and thereby pulls more LDL out of the blood. The actual effect therefore comes from that second step, not directly from the inhibition.

In the context of this platform it matters because oral anabolics flatten HDL and drive LDL up at the same time. That shift is one of the best documented consequences of oral 17-alpha-alkylated compounds.

This information is for research and educational purposes only. No medical advice.

The body's own cholesterol synthesis peaks at night, hence the recommendation to take it in the evening. With atorvastatin that point is less critical than with the short-acting older statins, because the half-life of around 14 hours plus active metabolites covers a good part of the day anyway.

For dosing there is the so-called rule of six: each doubling of the dose lowers LDL by a further six percent. Going from 10 to 20mg therefore adds little, going from 10 to 80mg adds up, but the side effect price rises faster than the benefit. That is why the high dose only makes sense with a correspondingly high starting value.

ASCOT-LLA (Lancet 2003) was stopped after 3.3 instead of the planned 5 years because the advantage was too clear: in hypertensives with average or even below-average cholesterol, 10mg atorvastatin cut coronary events by 36 percent. The message was new, because what was treated was not a high value but a high risk.

CARDS (Lancet 2004) did the same in type 2 diabetes and was likewise stopped two years early, with 37 percent fewer cardiovascular events. TNT (NEJM 2005) compared 80mg against 10mg in stable coronary disease and found 22 percent fewer events on the high dose, though with more liver value abnormalities.

SPARCL (NEJM 2006) belongs here with a caveat: after stroke or TIA, 80mg atorvastatin cut the stroke rate by 16 percent, while slightly more haemorrhagic strokes occurred. The net effect was positive, the limitation belongs in the picture anyway.

• Muscle pain: the best known issue. Statins can cause muscle pain and in rare cases genuine muscle breakdown. Anyone training hard has elevated CK anyway, which makes telling them apart difficult. New, unfamiliar muscle pain on a statin needs checking, not training through.
• Liver values: small rises are common and usually harmless, clear rises need checking.
• Blood sugar: statins slightly raise the risk of new-onset diabetes. The cardiovascular benefit clearly outweighs it in the trials, but it is worth mentioning.
• Digestive complaints: common in the first weeks, usually temporary.

Store dry, at room temperature and protected from light. Keep out of reach of children.