At present, the drugs used clinically for the treatment of dyslipidemia include: statins, fibrates, niacin, resins, cholesterol absorption inhibitors and deep-sea fish oil preparations and antioxidants. The following is an explanation of the action characteristics, adverse reactions and precautions for taking various types of drugs.
1, statins: that is, 3 hydroxy 3 methyl glutaryl coenzyme A (HMG-CoA) reductase inhibitors. It mainly lowers cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C), but also lowers triglycerides (TG) and slightly increases high-density lipoprotein cholesterol (HDL-C). In addition, statins also have extra-lipid-regulating effects such as anti-inflammation and protection of vascular endothelial function, so they play an important role in the prevention and treatment of atherosclerotic diseases.
There are six main types of statins currently available in China.
①Atorvastatin (Lipitor, Aller).
②Simvastatin (Sulforaphane, Kybixin).
(iii) Lovastatin
(4) Pravastatin (Meperidine, Placid), (5) Fluvastatin (Lysergol) and (6) Rosuvastatin.
The following points should be noted when applying statins.
Although their lipid-lowering efficacy is dose-related, it is not linearly correlated. A 1-fold increase in drug dose only increases lipid-lowering by about 6% (5% for TC and 7% for LDL-C), so the dose should not be increased in pursuit of lipid-lowering.
② Main side effects of statins.
The milder and transient side effects include: headache, insomnia, depression, dyspepsia, diarrhea, abdominal pain, nausea and other gastrointestinal symptoms.
Elevated liver enzymes: Elevated alanine aminotransferase (ALT) and aspartate aminotransferase (AST) occur in about 0.5% to 2% of cases in a dose-dependent manner. Statins leading to liver failure are rare, but cholestasis and active liver disease are contraindications to the use of this class of drugs.
Myopathy: This includes myalgia (muscle pain, tenderness, and weakness), myositis (muscle symptoms with elevated creatine kinase), and rhabdomyolysis (muscle symptoms with significant creatine kinase elevation greater than 10 times the upper limit of normal and creatinine elevation), the latter being the most dangerous adverse reaction and can be fatal in severe cases.
The incidence of muscle discomfort with statins is generally around 5%, and in order to prevent the development of associated myopathy, attention should be paid to the following conditions that can increase the risk of its development.
Advanced age, especially in women
Thin, frail body size
Multisystem disease (e.g., chronic renal insufficiency)
Combined use of multiple medications
Perioperative period
Combination of the following special medications or diets.
Betablockers (especially gemfibezil), niacin (rare), cyclosporine, erythromycin, clarithromycin, pyrrole antifungals, nefazodone (antidepressants), verapamil, amiodarone, and large amounts of grapefruit juice and alcohol abuse.
Overdose. Statins should be discontinued if muscle symptoms or discharge of brown urine (myoglobinuria) with a creatine kinase (CK) elevation of 10-fold or more occur during statin administration.
③ General evaluation of the efficacy and safety of statins.
The role of statins in regulating lipids and reducing the occurrence of major ischemic events in high-risk patients is very positive, and this role has not yet been fully exploited, so more efforts should be made to promote the use of statins; but at the same time, with the increase in drug dose and/or other factors, the adverse drug reactions will also increase, so there is also strict monitoring and careful use of drugs to ensure safety.
2.Betainide: also known as phenoxyaromatic acid, mainly reduce triglycerides (TG) and increase HDL-C level, but also can make LDL cholesterol (LDL) subtype from small and dense particles to large and loose particles.
Clinical applications include fenofibrate (0.1 Tid or micronized 0.2 Qd), benzofibrate (0.2 Tid), and gemfibrozil (0.6 Bid). Adverse reactions are commonly dyspepsia, cholelithiasis, and also elevated hepatic transaminases and myopathy, and gefirozil has a poor safety profile. Absolute contraindications are serious kidney disease and serious liver disease.
3, niacin: niacin is a B vitamin, when the dosage exceeds the dose used as a vitamin, there is a significant lipid-regulating effect. It is suitable for hypertriglyceridemia, low HDLemia or mixed type of hyperhaemoglobinemia with mainly elevated TG. Generally, a derivative of niacin, acipimox (Yiping) 0.25g, 2-3 times/day; or niacin extended-release tablets, starting with a small dose (0.375-0.5, taken at bedtime) and gradually increasing to 1-2g/d after four weeks. adverse effects of niacin include facial flushing, hyperglycemia, hyperuricemia, upper gastrointestinal discomfort, etc. The adverse effects of acipimox are milder. The absolute contraindications of this class of drugs are chronic liver disease and severe gout, and the relative contraindications are ulcer disease, hepatotoxicity and hyperuricemia.
4.Bile acid chelator: It is alkaline anion exchange resin, mainly used for hypercholesterolemia. Commonly used are Kolayenan (bile elimination), 4 to 16 grams per day, divided into 3 doses; Kolaytipo (bile reduction), 5 to 20 grams per day, divided into 3 doses.
Common adverse reactions include gastrointestinal discomfort, constipation.
5, cholesterol absorption inhibitor: that is, ezetimibe, the principle of action is to inhibit the absorption of cholesterol, used for hypercholesterolemia. Commonly used dose of 10mg/d, can make LDL-C decreased by about 18%, safety and tolerability is good, common adverse reactions are headache and nausea.
6, deep-sea fish oil preparations: containing ω-3 fatty acids, polyunsaturated fatty acids. Mainly used for hypertriglyceridemia, can reduce TG and mildly increase HDL-C, generally no effect on TC and LDL-C. In addition to lipid regulation, it also has the effects of lowering blood pressure, inhibiting platelet aggregation, anti-inflammatory and improving vascular reactivity, etc. Recently, it has also been found to have the effect of preventing cardiac arrhythmia and sudden death. About 2-3% of patients develop gastrointestinal symptoms such as nausea, bloating, indigestion and constipation. A few show mild elevation of liver transaminases or CK, and occasionally bleeding tendency.
7, antioxidants: Probucol, also known as propofol, the trade name of the up. It is mainly used for hypercholesterolemia, especially pure-sibling familial hypercholesterolemia. Still has antioxidant effect. Although this drug lowers HDL, it changes the structure and metabolic function of HDL and improves its ability to reverse cholesterol transport, thus making it more conducive to HDL’s anti-atherosclerotic effect. Common side effects include nausea, vomiting, dyspepsia, etc., as well as eosinophilia and increased blood uric acid. The most serious adverse effect is the prolongation of QT interval, but it is rare. The most serious adverse effect is the prolongation of QT interval, but it is rare. Therefore, it is prohibited for those who have ventricular arrhythmia or QT interval prolongation. The usual dose is 0.5, 2 times/day.