Introduction to Statins lipid-lowering drugs

Statins Introduction:

Common Statins drugs include pravastatin, simvastatin, lovastatin, fluvastatin, and atorvastatin.

The lipid-lowering effects of Statins drugs are mainly manifested in two aspects:

1. Effectively inhibiting the synthesis of cholesterol in the body, reducing intracellular cholesterol, and feedback regulating the activity of cell surface LDL receptors, promoting the decrease of low-density lipoprotein (LDL) levels in the plasma.
2. Increasing high-density lipoprotein (HDL) levels. It is well known that elevated LDL levels are a direct risk factor for atherosclerosis, while increased HDL levels can counteract the atherogenic effects of hypercholesterolemia and elevated very-low-density lipoprotein (VLDL) levels.

From the overall lipid-lowering effects, statin drugs can effectively prevent the occurrence of atherosclerosis and slow down the progression of atherosclerotic lesions by reducing hypercholesterolemia, lowering VLDL and LDL levels, and increasing HDL levels.

Long-term clinical studies have provided ample evidence that these drugs can prevent and treat atherosclerosis, greatly reducing the occurrence or recurrence rate of myocardial infarction in patients with coronary heart disease, as well as significantly reducing the number of strokes and deaths. As a result, they have received widespread acclaim.

(1) Pravastatin (Statins Introduction):

• [Mechanism of Action] It effectively lowers serum total cholesterol and LDL-C levels, moderately reduces triglyceride levels, and increases HDL-C levels. Pravastatin has a mild inhibitory effect on smooth muscle cell proliferation, which is beneficial for stabilizing fibrous caps of atherosclerotic plaques and improving endothelial cell function, reversing the abnormal effects of acetylcholine on endothelial cell injury. It also lowers plasma levels of C-reactive protein and amyloid A, exhibiting anti-inflammatory effects, thus contributing to the prevention of atherosclerosis.
• [Dosage] Taken after dinner, starting at 10 mg/day, with a maximum dose of 30 mg/day. The dosage may be appropriately reduced when the condition improves.
• [Adverse Reactions] Mild elevation of transaminases, rash, myalgia, headache, nausea, diarrhea, fatigue, etc.
• [Precautions] Contraindicated in pregnancy, pregnant women, and lactating women. Contraindicated in individuals with known hypersensitivity to the drug, active liver disease, or abnormal liver function. Less effective in familial hypercholesterolemia. Caution should be exercised in individuals with a history of liver disease or alcohol abuse. Co-administration with bile acid sequestrants can reduce the efficacy of cholesterol-lowering, but the two medications should be taken at least 4 hours apart to avoid drug adsorption.

(2) Simvastatin (Statins Introduction):

• [Mechanism of Action] It significantly lowers total cholesterol and LDL-C levels, increases serum high-density lipoprotein levels, and reduces triglyceride levels. Long-term oral administration can alleviate and delay the progression of atherosclerosis, improve endothelial cell function, and reduce the incidence of cardiovascular events in patients with coronary heart disease.
• [Dosage] The usual initial dose is 10 mg/day, taken in the evening. The maximum dose is 80 mg/day. For patients with mild to moderate elevation of cholesterol levels, the initial dose is 5 mg/day. For patients concurrently taking immunosuppressive drugs or with severe renal impairment, the maximum dose is 10 mg/day. For patients with coronary heart disease, the initial dose is 20 mg/day, and the dose is adjusted according to the condition. Additionally, patients should follow a routine cholesterol-lowering diet before and during treatment with this medication.
• [Adverse Reactions] Common adverse reactions include abdominal pain, constipation, gastrointestinal bloating, fatigue, weakness, and headache. Rare reactions include hepatitis and hypersensitivity. Most adverse reactions are mild and transient.
• [Precautions] a. Women of childbearing potential and lactating women should not take this medication temporarily. b. If creatine kinase elevation is observed during treatment, the medication should be discontinued immediately. c. Caution should be exercised in patients with a history of liver disease or alcohol abuse. d. Patients with elevated transaminases before treatment should be closely monitored. If serum transaminase levels exceed three times the normal value, the medication should be discontinued immediately.

(3) Lovastatin (Statins Introduction):

• [Mechanism of Action] It can treat any type of high cholesterol, except for homozygous familial hypercholesterolemia, including mixed hyperlipidemia primarily characterized by elevated serum total cholesterol levels. It can also slow down the progression of coronary atherosclerosis and reduce the occurrence of new lesions.
• [Dosage] It is taken orally once daily, with a dose of 20 mg per dose, taken with dinner. The dosage is adjusted every 4 weeks based on the serum cholesterol levels, with a maximum daily dose of 80 mg.
• [Adverse Reactions] The most common adverse reactions are gastrointestinal discomfort, muscle pain, muscle weakness, headache, and rash, with an incidence rate of around 1%. Rare reactions include hepatitis, obstructive jaundice, myopathy, rhabdomyolysis, and hypersensitivity syndrome.
• [Precautions] a. It should be avoided in pregnant and lactating women, as well as patients with active hepatitis. b. Caution should be exercised in patients with a history of liver disease and alcohol abuse. c. It has an additive effect when used in combination with colestipol. d. Liver function should be rechecked after 4 to 6 weeks, and if transaminase activity increases to more than three times the normal value, the medication should be discontinued immediately.

(4) Fluvastatin (Statins Introduction):

• [Mechanism of Action] It can significantly lower total cholesterol and LDL-C levels, moderately lower plasma triglyceride levels, and slightly increase HDL-C levels. It also improves endothelial function and has antiplatelet aggregation effects.
• [Dosage] The initial dose is 20 mg/day, taken in the evening. After 4 to 6 weeks, it can be increased to 40 mg/day, divided into two doses. The maximum dose is 80 mg/day.
• [Adverse Reactions] Mild and transient digestive discomfort, nausea, abdominal pain, insomnia, headache, and abnormal liver function may occur.
• [Precautions] a. It is contraindicated in pregnant women, lactating women, and patients under 18 years of age. b. It is contraindicated in patients with active hepatitis or persistently elevated serum transaminase of unknown cause. c. Caution should be exercised in patients with liver disease and alcohol abuse.

(5) Atorvastatin (Statins Introduction):

• [Action] It is used for primary hypercholesterolemia, mixed hyperlipidemia, and homozygous familial hypercholesterolemia. Along with dietary control, taking atorvastatin can significantly reduce cholesterol levels.
• [Dosage] The initial dose is 10 mg/day, taken in the evening. The maximum dose is 80 mg/day.
• [Adverse Reactions] Muscle tenderness, transient mild increase in serum creatine kinase (CK) levels. Occasionally, rhabdomyolysis, a serious adverse reaction, occurs. Therefore, CK levels should be monitored regularly during medication. Additionally, a few patients may experience increased plasma alkaline phosphatase levels, gastrointestinal disorders, nausea, insomnia, muscle tenderness, and rash.
• [Precautions] a. Regular ophthalmic examinations should be performed to watch for the development of cataracts. b. This medication should not be used in combination with nicotinic acid, gemfibrozil, cyclosporin, and cyclophosphamide, as this may cause severe muscle, liver, and kidney damage.