Statin lipid-lowering drugs
Statins, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, not only potently lower total cholesterol (TC) and low-density lipoprotein (LDL), but also It can reduce triacylglycerol (TG) to a certain extent, and can also increase high-density lipoprotein (HDL), so statins can also be called more comprehensive lipid-lowering drugs.
The mechanism of action of statins is to competitively inhibit the endogenous cholesterol synthesis rate-limiting enzyme HMG-CoA reductase, block the intracellular xyvalonate metabolic pathway, reduce intracellular cholesterol synthesis, and feedback stimulate the low level of cell membrane surface. The increase in the number and activity of density lipoprotein (LDL) receptors increases serum cholesterol clearance and lowers the level. Clinically, it is mainly used to reduce cholesterol, especially low-density lipoprotein-cholesterol (LDL-C), and to treat atherosclerosis. Become the most effective drug for coronary heart disease prevention and treatment.
Lovastatin and simvastatin: Lovastatin is the first statin to be marketed, and simvastatin is the second statin to be marketed. It is based on lovastatin and has a very small structure. change. The properties of the two are similar, the lipid-lowering intensity is moderate, and simvastatin is more commonly used.
Both are metabolized by the liver drug enzyme CYP3A4, and many drugs are metabolized by the same pathway, so there are many interactions with other drugs, and attention should be paid when combining drugs. Both of them have a short duration of action and need to be taken before going to bed to maximize the lipid-lowering effect.
Pravastatin: It is a medium-acting statin, which is not metabolized by liver drug enzymes, and has less interaction with other drugs, less adverse reactions, less impact on blood sugar, short-acting, and needs to be taken before going to bed.
Fluvastatin: It is a medium-acting statin, mainly metabolized by the liver drug enzyme CYP2C9, and interacts with some drugs. It is short-acting and needs to be taken before going to bed. It is less used now.
Atorvastatin: It is a potent statin with a long-acting effect and can be taken at a fixed time every day. It is mainly metabolized by the liver drug enzyme CYP3A4, and it has many interactions with other drugs.
Rosuvastatin: It is a potent statin and has a long-acting effect. It can be taken at a fixed time every day. It is mainly excreted through the feces, partly through the kidneys, and a small part is metabolized through the liver. It has few interactions with other drugs, and it has a high safety when used in combination.
Pitavastatin: It is a medium-acting statin and has a long-acting effect. It can be taken at a fixed time every day. Take the smallest dose of statins, which are mainly excreted in the feces, have fewer interactions with other drugs, have fewer side effects, and have the least impact on blood sugar.
In recent years, studies have found that statins have various non-lipid-lowering effects, including inhibiting atherosclerosis and thrombosis, relieving rejection after organ transplantation, treating osteoporosis, anti-tumor, and anti-senile dementia. and many other functions.
