Product Overview
[Drug Name]
Generic Name: Simvastatin Tablets
Trade Name: Xinqi
English Name: Simvastatin Tablets
Chinese Pinyin: Simvastatin Tablets
[Ingredients]
The main ingredient and its chemical name 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
[Properties]
This product is a white or off-white tablet.
[Indications]
1. Hyperlipidemia (1) For patients with primary hypercholesterolemia, heterozygous familial hypercholesterolemia or mixed hypercholesterolemia, when dietary control and other non-drug treatments are not ideal, simvastatin can be used to reduce elevated total cholesterol, low-density lipoprotein cholesterol, apolipoprotein B and triglycerides. Simvastatin also increases high-density lipoprotein cholesterol, thereby reducing the ratio of low-density lipoprotein/high-density lipoprotein and total cholesterol/high-density lipoprotein. (2) For patients with homozygous familial hypercholesterolemia, when dietary control and non-dietary treatments are not ideal, simvastatin can be used to reduce elevated total cholesterol, low-density lipoprotein cholesterol and apolipoprotein B.
2. Coronary heart disease For patients with coronary heart disease, simvastatin is used to: (1) Reduce the risk of death.(2) Reduce the risk of death from coronary heart disease and non-fatal myocardial infarction. (3) Reduce the risk of stroke and transient ischemic attack. (4) Reduce the risk of myocardial revascularization surgery (coronary artery bypass grafting and percutaneous coronary angioplasty). (5) Delay the progression of atherosclerosis, including the occurrence of new lesions and complete blockage.
[Usage and Dosage]
Oral administration, can be broken up and taken if necessary. 1. Hypercholesterolemia: The general starting dose is 10 mg per day (5 mg specification: 2 tablets; 10 mg specification: 1 tablet), taken in the evening. For patients with mild to moderate cholesterol levels, the starting dose is 5 mg per day (5 mg specification: 1 tablet; 10 mg specification: half a tablet). If the dose needs to be adjusted, it should be adjusted at least four weeks later. The maximum dose is 40 mg per day (5 mg specification: 8 tablets; 10 mg specification: 4 tablets), taken in the evening. When the low-density lipoprotein cholesterol level drops to 75 mg/dL (1.94 mmol/L) or the total cholesterol level drops to below 140 mg/dL (3.6 mmol/L), the dose of simvastatin should be reduced. 2. Homozygous Familial Hypercholesterolemia: Based on the results of controlled clinical studies, the recommended dose of simvastatin for patients with homozygous familial hypercholesterolemia is 40 mg/day taken in the evening, or 80 mg/day divided into three doses: 20 mg in the morning, 20 mg at noon, and 40 mg in the evening. Simvastatin should be used in combination with other lipid-lowering therapies (such as low-density lipoprotein aspiration). When these methods are unavailable, simvastatin can be used alone. 3. Coronary Artery Disease: Patients with coronary artery disease can take 20 mg (5 mg: 4 tablets; 10 mg: 2 tablets) daily in the evening as a starting dose. If dose adjustment is necessary, refer to the instructions above (Usage and Dosage for Hypercholesterolemia). 4. Concomitant Therapy: Simvastatin is effective both alone and in combination with bile acid sequestrants. For patients taking concomitant immunosuppressants, the recommended dose of simvastatin is 10 mg (5 mg: 2 tablets; 10 mg: 1 tablet) daily. 5. Renal Impairment: Because simvastatin is not significantly excreted by the kidneys, no dose adjustment is required for patients with moderate renal impairment. However, for patients with severe renal impairment (creatinine clearance <30 ml/min), careful consideration should be given to using doses exceeding 10 mg per day (5 mg: 2 tablets; 10 mg: 1 tablet).
[Adverse Reactions]
Simvastatin is generally well tolerated, with most adverse reactions being mild and transient. In controlled clinical trials, fewer than 2% of patients discontinued simvastatin due to adverse reactions. In controlled clinical trials, adverse reactions (classified as possibly, suspected, or definitely) attributed to drug-relatedness with an incidence greater than or equal to 1% included abdominal pain, constipation, and flatulence. Adverse reactions with an incidence of 0.5% to 0.9% included fatigue, weakness, and headache. Reports of myopathy are rare. The following adverse reactions have been reported in uncontrolled clinical trials or postmarketing use: nausea, diarrhea, rash, dyspepsia, pruritus, alopecia, dizziness, muscle cramps, myalgia, pancreatitis, paresthesia, peripheral neuropathy, vomiting, and rarely anemia, rhabdomyolysis, and hepatitis/jaundice. Overt hypersensitivity syndromes including one or more of the following features have been reported rarely: angioedema, lupus-like syndrome, polymyalgia rheumatica, vasculitis, thrombocytopenia, eosinophilia, increased erythrocyte sedimentation rate (ESR), arthritis, arthralgia, urticaria, photosensitivity, fever, flushing, dyspnea, and malaise. Laboratory findings: Significant and persistent elevations of serum aminotransferases have been reported rarely. Liver function test abnormalities have been mild or transient. Elevations of serum creatine phosphokinase (CK), derived from skeletal muscle, have also been reported.
[Contraindications]
1. Hypersensitivity to any of the ingredients. 2. Active hepatitis or unexplained persistent elevations of serum aminotransferases. 3. Use in combination with the tetralin calcium channel blocker mibefradil.
[Precautions]
1. Patients should follow a standard cholesterol diet before simvastatin treatment and continue to do so during treatment. 2. Hepatic reactions. This drug should be used with caution in patients with heavy alcohol consumption and/or a history of liver disease. Simvastatin should be contraindicated in patients with active liver disease or unexplained elevations in aminotransferase levels. In clinical trials, a small number of patients taking simvastatin experienced significant, persistent elevations in serum aminotransferase levels (more than three times the normal value). However, after discontinuation of the drug, aminotransferase levels returned to pre-treatment levels, without jaundice or other concerning clinical signs or symptoms, and without allergic reactions. Patients with elevated aminotransferase levels should undergo increased testing and precautions before treatment. If the patient's aminotransferase levels continue to rise, particularly if the elevation exceeds three times the normal value and persists, the drug should be discontinued. As with other lipid-lowering drugs, moderate elevations in aminotransferases (less than three times the normal value) have been reported in patients treated with simvastatin. These changes typically occur shortly after treatment with simvastatin, are generally transient, and are not associated with any symptoms, so discontinuation of the drug is not necessary. 3. Muscle Reactions. Mild, transient elevations in creatine kinase (CK, derived from skeletal muscle) are common in patients treated with simvastatin, but these are not clinically significant. Diffuse myalgia, muscle weakness, and/or significant elevations in creatine kinase (CK) (greater than ten times the normal value) should be considered a myopathy. Patients should be advised to report any unexplained signs of myopathy to their doctor immediately. If a significant elevation in creatine kinase (CK) is observed or myalgia is diagnosed or suspected, simvastatin treatment should be discontinued immediately. Treatment with methylhydroxyglutaryl coenzyme A (HMG-CoA) reductase inhibitors should be discontinued in patients with acute or severe conditions suggestive of myopathy or those at risk for secondary acute renal failure due to rhabdomyolysis. 4. Ophthalmological examination. Even without any medication, the incidence of lens opacities increases with age. Long-term clinical studies have shown that simvastatin has no adverse effects on the human lens. 5. Homozygous familial hypercholesterolemia. Because patients with homozygous familial hypercholesterolemia completely lack low-density lipoprotein (LDL) receptors, simvastatin is less effective in treating this condition. 6. Hypertriglyceridemia. Simvastatin has only a moderate effect on lowering triglycerides and is not suitable for treating conditions characterized by elevated triglycerides (such as types I, IV, and V hyperlipidemia). 7. This drug should be used with caution in patients with excessive alcohol consumption and/or a history of liver disease.
[Use in Special Populations]
Precautions for use in children:
The safety and efficacy of this medication have not been established in children. Simvastatin is not currently recommended for use in children.
Precautions for pregnancy and lactation:
1. There are no data on the use of simvastatin in pregnant women. Simvastatin is contraindicated during pregnancy. Because atherosclerosis is a chronic process, discontinuing lipid-lowering medication during pregnancy has little effect on the long-term effectiveness of treating primary hypercholesterolemia. Furthermore, cholesterol and other products of its biosynthetic pathway are essential for fetal development, including the synthesis of steroids and cell membranes. Because HMG-CoA reductase inhibitors such as simvastatin reduce cholesterol synthesis and other products of the cholesterol biosynthetic pathway, simvastatin use during pregnancy may be harmful to the fetus. Among women of childbearing age, simvastatin should only be used in those with a low probability of pregnancy. If a woman becomes pregnant while taking simvastatin, she should discontinue simvastatin and be informed of the potential harm to the fetus. It is not known whether simvastatin and its metabolites are excreted in human milk. Because many drugs are excreted in human milk and have potentially serious side effects, women taking simvastatin should not breastfeed.
Elderly Precautions:
In controlled clinical trials of simvastatin in elderly patients (over 65 years of age), its efficacy in lowering total cholesterol and low-density lipoprotein (LDL) cholesterol was comparable to that observed in other populations, without a significant increase in the frequency of adverse reactions or laboratory abnormalities.
[Drug Interactions] 1. The risk of rhabdomyolysis is increased when simvastatin is coadministered with other drugs that significantly inhibit cytochrome P450 3A4 at therapeutic doses (e.g., cyclosporine, mibefradil, itraconazole, ketoconazole, erythromycin, clarithromycin, and nefazodone), or with fibric acid derivatives or niacin. 2. The incidence and severity of myopathy may be increased when simvastatin is coadministered with methylhydroxyglutaryl coenzyme A (HMG-CoA) reductase inhibitors, including gemfibrozil and other fibrates, as well as lipid-lowering doses of niacin (≥1 g/day). In addition, elevated plasma levels of HMG-CoA reductase inhibitors (HMG-CoA) can increase the risk of myopathy. Simvastatin and other HMG-CoA reductase inhibitors are metabolized by the cytochrome P450 isoenzyme 3A4. Several drugs that significantly inhibit this metabolic pathway at therapeutic doses can increase HMG-CoA reductase inhibitor plasma levels and, therefore, the risk of myopathy. These drugs include cyclosporine, tetralins, the calcium channel blocker mibefradil, itraconazole, ketoconazole, and other antifungal azoles, the macrolide antibiotics erythromycin and clarithromycin, and the antidepressant nefazodone. 3. Coumarin derivatives: Clinical studies have shown that simvastatin can moderately enhance the anticoagulant effect of coumarin anticoagulants. Therefore, when adults begin early anticoagulant therapy and concurrent simvastatin use, the prothrombin time should be monitored frequently to ensure that the prothrombin time has not significantly changed. Even after a stable prothrombin time has been achieved in patients taking coumarin derivatives, continued prothrombin time monitoring is recommended for a fixed period. The same procedure should be followed if the simvastatin dose is changed. Simvastatin therapy has not been reported to affect bleeding or prothrombin time in patients not taking anticoagulants.
[Pharmacological Action]
This product is a methylhydroxyglutaryl coenzyme A (HMG-CoA) reductase inhibitor, inhibiting endogenous cholesterol synthesis and acting as a lipid regulator. Literature indicates that it reduces cholesterol (TC) levels in the serum, liver, and aorta of hyperlipidemic rabbits, as well as very low-density lipoprotein cholesterol (VLDL-C) and low-density lipoprotein cholesterol (LDL-C).
[Storage] Store tightly closed below 30°C. Avoid sudden temperature increases above 55°C.
[Specification] 20mg
[Packaging] Aluminum-plastic packaging, 14 tablets/box
[Expiration Period] 24 months
[Approval Number] National Medicine Standard H20084420
[Manufacturer] Shandong Xinqi Pharmaceutical Co., Ltd.
