Anticholesterol Drug/Lipid Lowering Drug /Statins Groups Drug

Anticholesterol Drug/Lipid Lowering Drug /Statins Groups Drug

Anticholesterol drug is also known as HMG-CoA reductase inhibitors, are a class of lipid-lowering medications. Statins have been found to reduce cardiovascular disease (CVD) and mortality in those who are at high risk of cardiovascular disease. The evidence is strong that statins are effective for treating CVD in the early stages of the disease (secondary prevention) and in those at elevated risk but without CVD (primary prevention)

The statins are divided into two groups: fermentation-derived and synthetic. They include, along with brand names, which may vary between countries:

Statin Image Brand name Derivation Metabolism
Atorvastatin
Atorvastatin.svg
Lipitor, Ator Synthetic CYP3A4
Cerivastatin
Cerivastatin.svg
Lipobay, Baycol (withdrawn from the market in August, 2001 due to risk of serious rhabdomyolysis) Synthetic various CYP3Aisoforms
Fluvastatin
Fluvastatin.svg
Lescol, Lescol XL Synthetic CYP2C9
Lovastatin
Lovastatin.svg
Mevacor, Altocor, Altoprev Naturally occurring, fermentation-derived compound. It is found in oyster mushroomsand red yeast rice CYP3A4
Mevastatin
Mevastatin.svg
Compactin Naturally occurring compound found in red yeast rice CYP3A4
Pitavastatin
Pitavastatin.svg
Livalo, Livazo, Pitava Synthetic CYP2C9 and CYP2C8(minimally)
Pravastatin
Pravastatin.svg
Pravachol, Selektine, Lipostat Fermentation-derived (a fermentation product of bacterium Nocardia autotrophica) Non-CYP
Rosuvastatin
Rosuvastatin structure.svg
Crestor Synthetic CYP2C9 and CYP2C19
Simvastatin
Simvastatin.svg
Zocor, Lipex Fermentation-derived (simvastatin is a synthetic derivate of a fermentation product of Aspergillus terreus) CYP3A4
Simvastatin + ezetimibe Vytorin, Inegy Combination therapy: statin + cholesterol absorption inhibitor
Lovastatin + niacin extended-release Advicor, Mevacor Combination therapy
Atorvastatin + amlodipine Caduet, Envacar Combination therapy: statin + calcium antagonist
Simvastatin + niacin extended-release Simcor Combination therapy

LDL-lowering potency varies between agents. Cerivastatin is the most potent, (withdrawn from the market in August 2001 due to the risk of serious rhabdomyolysis) followed by (in order of decreasing potency), rosuvastatin, atorvastatin, simvastatin, lovastatin, pravastatin, and fluvastatin. The relative potency of pitavastatin has not yet been fully established.

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The oyster mushroom, a culinary mushroom, naturally contains lovastatin.

Some types of statins are naturally occurring and can be found in such foods as oyster mushrooms and red yeast rice. Randomized controlled trials have found these foodstuffs to reduce circulating cholesterol, but the quality of the trials has been judged to be low. Due to patent expiration, most of the block-buster branded statins have been generic since 2012, including atorvastatin, the largest-selling branded drug.

Statin equivalent dosages
% LDL reduction (approx.) Atorvastatin Fluvastatin Lovastatin Pravastatin Rosuvastatin Simvastatin
10–20% 20 mg 10 mg 10 mg 5 mg
20–30% 40 mg 20 mg 20 mg 10 mg
30–40% 10 mg 80 mg 40 mg 40 mg 5 mg 20 mg
40–45% 20 mg 80 mg 80 mg 5–10 mg 40 mg
46–50% 40 mg 10–20 mg 80 mg*
50–55% 80 mg 20 mg
56–60% 40 mg
* 80-mg dose no longer recommended due to increased risk of rhabdomyolysis
Starting dose
Starting dose 10–20 mg 20 mg 10–20 mg 40 mg 10 mg; 5 mg if hypothyroid, >65 yo, Asian 20 mg
If higher LDL reduction goal 40 mg if >45% 40 mg if >25% 20 mg if >20% 20 mg if LDL >190 mg/dL (4.87 mmol/L) 40 mg if >45%
Optimal timing Anytime Evening With evening meals Anytime Anytime  

Evening

References

Anticholesterol Drug/Lipid Lowering Drug /Statins Groups Drugs

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