What Are Statin Drugs?

Statins, that is, 3-hydroxy-3 methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, are currently the most effective lipid-lowering drugs, which not only can strongly reduce total cholesterol (TC) and low density Lipoprotein (LDL), and can lower triacylglycerol (TG) to a certain extent, 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 valproate metabolism pathway, reduce intracellular cholesterol synthesis, and thus feedback stimulate the low cell membrane surface. The increase in the number and activity of density lipoprotein (LDL) receptors increases serum cholesterol clearance and decreases levels. It is mainly used clinically to lower cholesterol, especially low density lipoprotein-cholesterol (LDL-C), and to treat atherosclerosis. Become the most effective drug for the prevention and treatment of coronary heart disease. In recent years, research has found that statins have a variety of non-lipid-lowering effects, including inhibiting atherosclerosis and thrombosis, and also alleviating rejection after organ transplantation, treating osteoporosis, antitumor, and anti-dementia And so on.

Basic Information

Chinese name

Statins

Foreign name

statins

Function

Reduces intracellular cholesterol synthesis

side effect

Have

Pharmacological effects of statins

Statins are mainly used to lower cholesterol in serum, liver, and aorta, and to reduce the levels of very low density lipoprotein cholesterol and low density lipoprotein cholesterol.

1. Lipid-lowering effect: It has obvious lipid-lowering effect, the effect of reducing LDL-C is the strongest, TC is the second, the effect of reducing TG is small, and HDL-C is slightly increased. Statins have similar chemical structure with HMC-coA, and their affinity with HMG-coA reductase is thousands of times higher than that of HMG-CoA. Therefore, hydroxymethylglutaric acid coenzyme A reductase competitively inhibits, Cholesterol synthesis is blocked.

2. Non-hyperlipidemic effects: improve vascular endothelial function, inhibit the proliferation and migration of vascular smooth muscle cells, antioxidant, anti-inflammatory, inhibit platelet aggregation and anti-thrombotic effects, etc., and help prevent the formation of arteriosclerosis or stabilize and shrink arteries Atherosclerotic plaque.

Application of statins

Suitable for hypercholesterolemia and mixed hyperlipidemia mainly with elevated cholesterol. Prevention and treatment of coronary heart disease, myocardial infarction and stroke, delay atherosclerosis.

Statin adverse reactions

The common adverse reactions of statins are closely related to the dosage. The main needs to be alert to myopathy and liver adverse reactions, other gastrointestinal reactions, skin flushing, headache and so on.

Clinical manifestations of statin-related myopathy include myalgia, myositis, and rhabdomyolysis. Cases of myositis and severe rhabdomyolysis are rare, and most often occur in patients with multiple diseases and / or multiple drugs. Rhabdomyolysis is often manifested by a significant increase in CK (phosphokinase) (more than 10 times the upper limit of normal), which may be accompanied by an increase in serum creatinine, and is often accompanied by myosinuria and myosinemia, and can cause Acute renal failure.

Impaired liver function is manifested by elevated serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. Among patients treated with statins, only about 1% -2% of patients with liver enzymes have a higher increase (more than The upper limit of the normal value is 3 times), the increase of liver enzymes is mostly transient, and most of them occur in the first 3 months of starting treatment or increasing the dose. Generally, liver enzyme levels can decrease after stopping treatment.

Statins precautions

Forbidden in active liver disease or unexplained transaminase continues to rise. Liver function should be monitored regularly during medication. If ALT or AST continues to rise more than three times the upper limit of normal, it is recommended to reduce the dose or stop the medication. Forbidden in pregnant and lactating women. Myalgia, fatigue, or unexplained fatigue always occur during the medication, and the medication should be stopped in time and go to the hospital for necessary examinations. This class of drugs should not be used together with cardiovascular drugs such as warfarin, verapamil, clopidogrel, digoxin, gefiprozil and other fibrate lipid-lowering drugs and amiodarone. If you must take it, you should follow your doctor's advice to reduce your statins and closely monitor adverse reactions. For elderly patients, the principle of individualized prevention and treatment must be followed during treatment, and the dose should be adjusted more carefully under the circumstances of closely monitoring liver enzymes and creatine kinase.

(Note: The above content is only for introduction, the drug use must be carried out by a regular hospital under the guidance of a doctor.)