This article is from "Nankai Sun Pharmacist", which is used for medical science popularization for reference. What is the difference between lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin, rosuvastatin, pitavastatin?What do I need to pay attention to when taking statins for a long time?
Statins are commonly used in clinical blood lipid regulating drugs, belonging to hydroxymethataryl-CoA reductase inhibitors, common drugs are simvastatin, pravastatin, atorvastatin, rosuvastatin, pitavastatin, etc., oxymethaglutar-CoA reductase is a rate-limiting enzyme for the synthesis of cholesterol, statins mainly combine with the enzyme through selectivity and competition, inhibit the activity of the enzyme, reduce liver cholesterol synthesis, play a lipid-regulating role, and can significantly reduce serum total cholesterol, LDL cholesterol and apolipoprotein B levels can also decrease triglyceride levels and slightly increase HDL cholesterol levels. In addition, statins also have anti-inflammatory, antioxidant, stabilizing and narrowing atherosclerotic plaque and other effects, currently mainly used in clinical hypercholesterolemia and mixed hyperlipidemia, long-term use can significantly reduce the risk of cardiovascular and cerebrovascular events such as myocardial infarction and stroke.
At present, the statins commonly used in clinical practice mainly include lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin, rosuvastatin and pitavastatin, among which natural statins are lovastatin, simvastatin and pravastatin, and the others are synthetic, various statins have many similarities, and also have their own characteristics
1.Lipid-regulating effect: various statins have different affinities with hydroxymethylglutaryl-CoA reductase, so the lipid-regulating effects are different, if low-density lipoprotein cholesterol (bad cholesterol) is used as the target of intervention, atorvastatin and rosuvastatin can reduce low-density lipoprotein cholesterol by more than 50%, therefore, these two statins should be preferred if there is a definite coronary heart disease, especially in patients who have had unstable angina, myocardial infarction, or patients with diabetes.
2.Taking time: The synthesis of cholesterol has a diurnal pattern, usually the most synthesized at night, for short-acting statins such as lovastatin, simvastatin, pravastatin, fluvastatin, etc., it is necessary to take it before going to bed to achieve the maximum lipid-regulating effect, while atorvastatin, Rosuvastatin and pitavastatin have a long half-life and strong lipid-regulating effect, can be taken at any fixed time of the day, medication adherence is better, food can promote the absorption of lovastatin and simvastatin, it is recommended that these two statins are best taken with dinner.
3.Interaction: Most statins need to be metabolized by the liver and are affected by liver enzymes, especially lovastatin, simvastatin and atorvastatin, which have extensive drug-drug interactions and are prone to induce serious adverse reactions such as myopathy, while pravastatin and pitavastatin are almost not metabolized by the liver, and are little affected by liver drug enzymes, and the incidence of interaction is low.
4.Safety: It has been statistically found that the incidence of muscular adverse reactions of rosuvastatin is significantly higher than that of simvastatin and atorvastatin, while the incidence of muscular adverse reactions of lovastatin, pravastatin and fluvastatin is lower. All kinds of statins, pravastatin is the safest, because it is a water-soluble statin, it is not easy to penetrate the blood-brain barrier, central adverse reactions are rare, plasma protein binding rate is low, it is not metabolized by the liver, drug-drug interactions rarely occur, metabolites are inactive, and the incidence of systemic adverse reactions is low, especially suitable for the elderly population.
Long-term use of statins requires attention:
1.Liver function should be measured before and after the start of ** 3 months after the start, if the serum aminotransferase elevation exceeds 3 times the upper limit of the normal range, the dose should be reduced or discontinued under the guidance of a doctor, and those with excessive drinking habits and a history of liver disease should be used with caution to avoid serious liver damage.
2.Long-term use of statins can lead to elevated blood sugar, especially fasting blood glucose and glycosylated hemoglobin, for high-risk groups such as elevated fasting blood glucose, excess weight, hypertension and hypertriglyceridemia, attention should be paid to monitoring blood glucose, blood lipids and blood pressure during the medication, and maintain a healthy weight.
3.Statin use increases the risk of rhabdomyolysis in people older than 70 years, hypothyroidism, renal impairment, alcohol abuse, or a family history of muscle disease, so statins should be used with caution. In the course of medication, once there is unexplained muscle weakness, pain or cramping, accompanied by general malaise or fever, the drug should be stopped immediately and the drug should be treated for medical attention.