Product Overview
[Drug Name]
Generic Name: Simvastatin Tablets
Trade Name: Tianzekang Simvastatin Tablets 10mg*28 Tablets
[Main Ingredients]
Simvastatin.
[Indications/Main Functions]
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, this product 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, this product 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 transluminal coronary angioplasty). (5) Delay the progression of atherosclerosis, including the occurrence of new lesions and complete blockage.
[Precautions]
1. Patients should follow a standard cholesterol diet before receiving simvastatin treatment and continue to use it during treatment. 2. Liver reaction. This drug should be used with caution in patients who drink a lot of alcohol and/or have a history of liver disease. Simvastatin should be contraindicated in patients with active liver disease or unexplained elevated aminotransferase levels. In clinical trials, a small number of patients taking simvastatin tablets had significant and persistent elevations in serum aminotransferases (more than 3 times the normal value). However, after discontinuation of the drug, the aminotransferases returned to pre-treatment levels, but there was no jaundice or other related clinical symptoms or signs, nor any allergic reactions. Patients with elevated aminotransferase levels should be monitored closely and monitored prior to treatment. If aminotransferase levels continue to rise, particularly if they exceed three times the normal value and persist, the drug should be discontinued. As with other lipid-lowering drugs, moderate elevations in aminotransferase levels (less than three times the normal value) have also 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 elevations 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 these 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 condition-suggestive myopathy and those at risk for secondary acute renal failure due to rhabdomyolysis. 4. Ophthalmological examination. Even without any drug treatment, the incidence of lens opacities increases with age. Long-term clinical data show 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 such patients. 6. Hypertriglyceridemia. Simvastatin has only a moderate triglyceride-lowering effect and is not suitable for treating conditions characterized by elevated triglycerides (such as types I, IV, and V hyperlipidemia). 7. This product should be used with caution in patients with excessive alcohol consumption and/or a history of liver disease.
[Drug Interactions]
1. Hypersensitivity to any of the ingredients. 2. Patients with active hepatitis or unexplained persistent elevations in serum aminotransferase levels. 3. Use in combination with the tetralin calcium channel blocker mibefradil.
[Use in Elderly Patients]
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.
[Use in Pregnancy and Breastfeeding]
1. No data are available regarding the use of simvastatin in pregnant women. Simvastatin tablets are contraindicated in pregnant women. Because atherosclerosis is a chronic process, discontinuing lipid-lowering medications during pregnancy has little effect on the long-term efficacy of treatment for primary hypercholesterolemia. Furthermore, cholesterol and other products of its biosynthetic pathway are essential for fetal development, including steroid synthesis and cell membrane synthesis. Because methylhydroxyglutaryl coenzyme A (HMG-CoA) reductase inhibitors such as simvastatin can reduce cholesterol synthesis and other products of the cholesterol biosynthesis pathway, simvastatin may harm the fetus when taken by pregnant women. In women of childbearing age, simvastatin should only be used in women who are unlikely to become pregnant. If a woman becomes pregnant while taking the drug, simvastatin should be discontinued and the woman should be informed of the possible harm to the fetus. 2. It is not known whether simvastatin and its metabolites are secreted in human milk. Because many drugs are secreted in human milk and have potential serious side effects, women taking simvastatin should not breastfeed.
[Specification]
10mg*28 tablets
[Usage and Dosage]
Patients should follow a standard cholesterol-lowering diet before receiving this product and continue to maintain it during treatment. (1) Hypercholesterolemia: The initial dose is generally 10mg per day, taken in the evening. For patients with mild to moderately elevated cholesterol levels, the initial dose is 5mg per day. If the dose needs to be adjusted, it should be adjusted at least four weeks apart. The maximum dose is 40mg per day, taken in the evening. When the LDL 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, it is recommended that patients with homozygous familial hypercholesterolemia take 40 mg/d of simvastatin in the evening, or 80 mg/d divided into three doses of 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 LDL extraction). When these methods cannot be used, simvastatin tablets can also be used alone. (3) Coronary heart disease: Patients with coronary heart disease can take 20 mg every night as a starting dose. If dose adjustment is required, refer to the above instructions (Usage and Dosage for Hypercholesterolemia). (4) Concomitant therapy: Simvastatin is effective when used alone or in combination with bile acid sequestrants. For patients who are taking immunosuppressants at the same time, the recommended dose of simvastatin is 10 mg per day. (5) Renal insufficiency: Since simvastatin is not significantly excreted by the kidneys, patients with moderate renal insufficiency do not need to adjust the dose; for patients with severe renal insufficiency (creatinine clearance less than 30 ml/min), if the dose exceeds 10 mg per day, it should be carefully considered and used with caution.
[Adverse Reactions]
Simvastatin is generally well tolerated, and most adverse reactions are mild and transient. In controlled clinical trials, less than 2% of patients discontinued simvastatin due to adverse reactions. In clinical trials with control groups, adverse reactions (classified as possible, suspected, or certain) with an incidence greater than or equal to 1% of drug-related reactions include: abdominal pain, constipation, and gastrointestinal flatulence. Adverse reactions with an incidence of 0.5% to 0.9% include 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. Used in combination with the tetralin calcium channel blocker mibefradil.
[Pharmacology and Toxicology]
Simvastatin can lower normal and elevated low-density lipoprotein cholesterol (LDL-C) concentrations. LDL is formed from very low-density lipoprotein (VLDL) and is primarily catabolized through the high-affinity LDL receptor. The mechanisms by which simvastatin lowers LDL-C include: lowering VLDL cholesterol concentrations, inducing LDL receptors, leading to a decrease in LDL cholesterol and increased LDL-C catabolism. Apolipoprotein B (apo B) levels also decrease significantly during simvastatin treatment. Since each LDL particle contains one molecule of apo B and apo B is rarely found in other lipoproteins, this suggests that simvastatin not only removes cholesterol from LDL but also reduces circulating LDL particle concentrations. Furthermore, simvastatin can increase high-density lipoprotein cholesterol (HDL-C) concentrations and lower plasma triglycerides (TG). All of these can lead to lowering of total cholesterol/HDL-C and LDL-C/HDL-C.
[Pharmacokinetics]
Simvastatin is highly selective for the liver after oral administration, with liver concentrations significantly higher than in other non-target tissues. Simvastatin undergoes extensive first-pass absorption in the liver, acting primarily in the liver and subsequently excreted via the bile. Less than 5% of the active simvastatin fraction is found in the periphery, and 95% of this is bound to plasma proteins. The specific metabolic pathway of fusidic acid in the liver is unknown, but interactions with fusidic acid metabolized via CYP-3A4 to HMG-CoA reductase inhibitors are suspected.
