Simvastatin Tablets

1. Simvastatin can reduce the concentration of normal and elevated low-density lipoprotein cholesterol (LDL-C). LDL is formed by very low-density lipoprotein (VLDL) and is mainly degraded by high-affinity LDL receptors. The mechanism of simvastatin in reducing LDL-C mainly includes: reducing the concentration of VLDL cholesterol, inducing LDL receptors, leading to a decrease in LDL cholesterol and increasing the catabolism of LDL-C. During simvastatin treatment, the level of apolipoprotein B (apoB) also decreased significantly. Since each LDL particle contains one molecule of apoB, and apoB rarely appears in other lipoproteins, this also suggests that simvastatin can not only cause cholesterol to be lost from LDL, but also reduce the concentration of circulating LDL particles. In addition, simvastatin can increase the concentration of high-density lipoprotein cholesterol (HDL-C) and reduce plasma triglycerides (TG). All of these can lead to a decrease in total cholesterol/HDL-C and LDL-C/HDL-C. 2. Animal experiments, pathological and clinical studies have demonstrated the role of LDL-C in atherosclerosis. Epidemiological studies have shown that high concentrations of total cholesterol, LDL-C, and apoB are risk factors for coronary heart disease, while higher levels of HDL-C and apoA-I reduce the risk. The oral LD50 of simvastatin is about 3.8 g/kg in mice and about 5 g/kg in rats. High doses of simvastatin and related analogs given to a variety of animals have shown some tissue changes. Given the large doses used, the efficacy of these drugs in inhibiting mevalonic acid synthesis, and the fundamental role of the target enzyme in maintaining the homeostasis of the cellular environment, the appearance of these changes is not unexpected. The large amount of data obtained from these changes shows that they are extraordinary manifestations of the biochemical effects of these drugs at the high end of the dose-effect curve. Therefore, morphological changes in rat liver, squamous epithelial hyperplasia of the cardiac sinus of rats and mice, and liver toxicity in rabbits have all been shown to be directly related to the inhibition of HMG-CoA reductase.

The main ingredients and their chemical names are: Simvastatin, [1S-[1a, 3a, 7b (2S*, 4S*) 8ab]]-1,2., 3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1-naphthyl-2,2-dimethylbutyrate. Molecular formula: C25H38O5, molecular weight: 418.57

Film-coated tablets appear white or off-white after removing the film coating.

1. Hyperlipidemia For patients with primary hypercholesterolemia, including heterozygous familial hypercholesterolemia, hyperlipidemia or mixed hyperlipidemia, when diet control and other non-drug treatments are not ideal, this product can be used to reduce elevated total cholesterol, low-density lipoprotein cholesterol, apolipoprotein B and triglycerides in combination with diet control, and can increase high-density lipoprotein cholesterol, thereby reducing the ratio of low-density lipoprotein cholesterol/high-density lipoprotein cholesterol and total cholesterol/high-density lipoprotein cholesterol. For patients with homozygous familial hypercholesterolemia, this product can be used to reduce elevated total cholesterol, low-density lipoprotein cholesterol and apolipoprotein B in combination with diet control and non-diet therapy. 2. Coronary heart disease For patients with coronary heart disease and hypercholesterolemia, this product is suitable for: reducing

Before patients receive this product, they should follow a standard cholesterol-lowering diet and continue to maintain it during treatment. The recommended starting dose is 20 mg per day, taken once in the evening. For patients who are at high risk for CHD events due to a history of coronary heart disease, diabetes, peripheral vascular disease, stroke or other cerebrovascular disease, the recommended starting dose is 20-40 mg/day. For patients who only need a moderate reduction in low-density lipoprotein cholesterol, the starting dose is 10 mg. For patients who are also taking cyclosporine, danazol, fibrates (except fenofibrate) or niacin drugs, amiodarone, verapamil, and severe renal insufficiency, the recommended doses are as follows. The recommended dosage range is 5-80 mg per day, taken once in the evening, and the dose used should be based on baseline low-density lipoprotein cholesterol.

This product is generally well tolerated, and most adverse reactions are mild and transient. In controlled clinical studies, less than 2% of patients discontinued the drug due to adverse reactions of this product. In pre-marketing controlled clinical studies, adverse reactions that researchers considered to be drug-related (classified as possible, very likely or certain) and with an incidence of ≥1% included abdominal pain, constipation and gastrointestinal bloating; adverse reactions with an incidence of 0.5-0.9% included fatigue and headache. Reports of myopathy are rare. In the HPS study (see Pharmacology and Toxicology), a total of 20,536 patients took 40 mg of this product (n=10,269) or placebo (n=10,267) daily, with an average observation time of 5 years, and the safety of the two groups was similar. This large trial only recorded serious adverse reactions and the number of people who withdrew from the study due to adverse reactions. The proportion of withdrawals due to adverse reactions was similar between the two groups (4.8% in the simvastatin group and 51% in the placebo group). The incidence of myopathy in the simvastatin group was less than 0.1%. The rates of elevated transaminases (three times or more of the upper limit of normal on repeated examination) were 0.21% (n=21) in the simvastatin group and 0.09% (n=9) in the placebo group. In the Nordic Simvastatin Survival Study (4S), 4444 patients took 20-40 mg (n=2221) or placebo (n=2223) daily for a median follow-up of 5.4 years and had similar safety and tolerability between the two groups. The following adverse reactions have been reported in uncontrolled clinical studies or post-marketing use: nausea, diarrhea, rash, dyspepsia, pruritus, alopecia, dizziness, muscle cramps, myalgia, pancreatitis, paresthesia, peripheral neuropathy, vomiting, and anemia. Rhabdomyolysis and hepatitis/jaundice rarely occur, and liver failure is extremely rare. Significant hypersensitivity syndromes including one or more of the following symptoms have been reported rarely: angioedema, lupus-like syndrome, polymyalgia rheumatica, dermatomyositis, vasculitis, thrombocytopenia, eosinophilia, elevated ESR, arthritis, arthralgia, urticaria, photosensitivity, fever, flushing, dyspnea, and malaise. 1. Laboratory tests have rarely reported significant and persistent elevations in serum transaminases. Elevations in alkaline phosphatase and gamma-glutamyl transpeptidase have been reported. Liver function test abnormalities were mild and transient. Elevations in serum creatine kinase (CK) from skeletal muscle have been reported (see Precautions). 2. Pediatric patients (ages 10-17 years) In a study of heterozygous familial hypercholesterolemia patients aged 10-17 years (n=175), the safety and tolerability of the ZOCOR treatment group was generally similar to that of the placebo treatment group. (See Precautions; Pediatric Use; Clinical Trials).

1. Those who are allergic to any component of this product. 2. Those with active liver disease or unexplained persistent elevation of serum transaminase. 3. Pregnant and lactating women (see Precautions, Use in Pregnant and Lactating Women).

Precautions for children: The safety and effectiveness of the drug for children have not been established. Simvastatin is not currently recommended for children. Pregnancy and lactation precautions: 1. Pregnant women This product is contraindicated for pregnant women. There is no safety data on the use of simvastatin by pregnant women. Controlled clinical trials of simvastatin have not been conducted in pregnant women. There are also few reports of birth defects caused by the use of HMG-CoA during pregnancy. However, in a retrospective analysis of approximately 200 patients who used simvastatin or other closely related HMG-CoA inhibitors in the first three months of pregnancy, it was found that the incidence of birth defects was similar to that of the general population. This number of patients reviewed has been statistically able to rule out the possibility that the incidence of birth defects is no more than 2.5 times or more than the normal occurrence. Although there is no clear evidence that the use of simvastatin by pregnant women will increase the incidence of birth defects, simvastatin can reduce fetal mevalonate (cholesterol). Note for the elderly: In controlled clinical trials of simvastatin in elderly patients (over 65 years old), its effect on lowering total cholesterol and low-density lipoprotein (LDL) cholesterol was the same as that of other populations, and there was no significant increase in the frequency of adverse reactions and laboratory test abnormalities.

1. Interaction with CYP3A4 Simvastatin is metabolized by CYP3A4 but does not have CYP3A4 inhibitory activity; therefore, it does not affect the plasma concentrations of other drugs metabolized by CYP3A4. Effective CYP3A4 inhibitors (as listed below) increase the risk of myopathy by reducing the elimination of simvastatin (see Precautions, Myopathy/Rhabdomyolysis). Itraconazole Ketoconazole Erythromycin Clarithromycin Telithromycin HIV protease inhibitor Nefazodone 2. Interaction with other lipid-lowering drugs that can cause myopathy when used alone The risk of myopathy is increased when the following lipid-lowering drugs are used in combination. Although these drugs are not effective CYP3A4 inhibitors, they can cause myopathy when used alone. See Precautions, Myopathy/Rhabdomyolysis.

Keep sealed and below 30℃. Avoid instantaneous temperature exceeding 50℃.

10mg

36 months.

Jiangsu Pingguang Pharmaceutical (Jiaozuo) Co., Ltd.

• Founded in:

  1998-03-11

• Address:

  Shenzhou Road, Jiaozuo City Urban-Rural Integration Demonstration Zone

• Tax NO.:

  91410800173475469M

• Registered Funds:

  11.065 million yuan

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