Product Overview
[Drug Name]
Generic Name: Simvastatin Tablets
Trade Name: LanKang Simvastatin Tablets 10mg*28 Tablets
Pinyin Full Code: LanKang XinFaTaTingPian 10mg*28Pian
[Main Ingredients]
Simvastatin.
[Properties]
Simvastatin tablets are white or off-white tablets.
[Indications/Main Functions]
1. Hyperlipidemia: (1) For patients with primary hypercholesterolemia, heterozygous familial hypercholesterolemia or mixed hypercholesterolemia, when diet 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 therapy are not ideal, simvastatin can be used to lower elevated total cholesterol, low-density lipoprotein cholesterol, and apolipoprotein B. 2. Coronary heart disease: (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. 3. Children with heterozygous familial hypercholesterolemia. For adolescent boys and girls aged 10-17 years (at least 1 year after menarche) with heterozygous familial hypercholesterolemia, combined with dietary control, this product can be used to lower total cholesterol, low-density lipoprotein cholesterol, apolipoprotein B, and triglycerides.
[Specifications]
10mg x 28 tablets
[Dosage and Administration]
Oral administration; may be broken into pieces if needed. 1. Hypercholesterolemia: The general starting dose is 10 mg daily, taken in the evening. For patients with mild to moderately elevated cholesterol levels, the starting dose is 5 mg daily. Dosage adjustments should be made at least four weeks apart, with a maximum dose of 40 mg daily, taken in the evening. The simvastatin dose should be reduced when the LDL cholesterol level drops to 75 mg/dL (1.94 mmol/L) or the total cholesterol level drops below 140 mg/dL (3.6 mmol/L). 2. Homozygous Familial Hypercholesterolemia: Based on controlled clinical studies, the recommended daily 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 a starting dose of 20 mg daily in the evening. 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 daily. 5. Renal Impairment: Because simvastatin is not significantly excreted by the kidneys, no dose adjustment is required in patients with moderate renal impairment. However, in patients with severe renal impairment (creatinine clearance less than 30 ml/min), the use of doses exceeding 10 mg daily should be carefully considered and used with caution.
[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 tablets due to adverse reactions. In controlled clinical trials, adverse reactions (classified as possibly, suspected, or definitely) attributed to the drug with an incidence greater than or equal to 1% included abdominal pain, constipation, and flatulence. Fatigue, asthenia, and headache occurred in 0.5% to 0.9% of patients. Reports of myopathy were 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. Rare reports have described a clear hypersensitivity reaction syndrome, including one or more of the following features: angioedema, lupus-like syndrome, polymyalgia rheumatica, vasculitis, thrombocytopenia, eosinophilia, elevated erythrocyte sedimentation rate (ESR), arthritis, arthralgia, urticaria, photosensitivity, fever, flushing, dyspnea, and malaise. Laboratory findings: Significant and persistent elevations in serum aminotransferases have been reported rarely. Liver function test abnormalities have been mild or transient. Elevations in serum creatine phosphokinase (CK), derived from skeletal muscle, have also been reported.
[Contraindications]
1. Hypersensitivity to any component of simvastatin tablets. 2. Active hepatitis or unexplained persistent elevation of serum aminotransferases. 3. Concomitant use with the tetralin calcium channel blocker mibefradil.
[Drug Interactions]
1. The risk of rhabdomyolysis is increased when simvastatin is used in combination with other drugs that significantly inhibit cytochrome P450 3A4 at therapeutic doses (e.g., cyclosporine, mibefradil, itraconazole, ketoconazole, erythromycin, clarithromycin, and nefazodone), or with fibrates or niacin. 2. Concomitant use of simvastatin with methylhydroxyglutaryl coenzyme A (HMG-CoA) reductase inhibitors, including gemfibrozil and other fibrates, and lipid-lowering doses of niacin (≥1g/day), may increase the incidence and severity of myopathy. Furthermore, 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, frequent prothrombin time monitoring is recommended to ensure that the prothrombin time does not change significantly. Even after a stable prothrombin time has been achieved in patients taking coumarin-based biologics, 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.
[Precautions]
1. Patients should follow a standard cholesterol diet before starting simvastatin therapy and continue it during treatment. 2. Hepatic Reactions. This drug should be used with caution in patients who consume significant amounts of alcohol and/or have 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 and persistent elevations in serum aminotransferases (more than three times the normal value). However, after discontinuation of the drug, aminotransferase levels can return to pre-treatment levels, without jaundice or other related clinical symptoms or signs, and without allergic reactions. It is recommended that patients with elevated aminotransferase levels should undergo more frequent examinations and pay more attention before treatment. If the patient's aminotransferase level continues to rise, especially if the increase exceeds 3 times the normal value and persists, the drug should be discontinued. As with other lipid-lowering drugs, moderate increases in aminotransferase levels (less than 3 times the normal value) have also been reported in patients treated with simvastatin. These changes usually occur shortly after treatment with simvastatin, but are generally transient and not accompanied by any symptoms, so discontinuation of the drug is not necessary. 3. Muscle reactions. Patients treated with simvastatin generally have a slight transient increase in creatine kinase (CK, which comes from skeletal muscle, but these have no clinical significance. Myopathy should be considered in cases of diffuse myalgia, muscle weakness or/and significant increase in creatine kinase (CK) (more than ten times the normal value). Therefore, patients should be asked to tell their doctors immediately if they find any unexplained signs of myopathy. If a significant increase in creatine kinase (CK) is found or myalgia is diagnosed or suspected, simvastatin treatment should be stopped immediately. Treatment with methylhydroxyglutaryl coenzyme A (HMG-COA) reductase inhibitors should be stopped for patients with acute or severe conditions suggesting myopathy and those who are prone to secondary acute renal failure due to rhabdomyolysis. 4. Ophthalmological examination. Even in the absence of any drug treatment, the incidence of lens opacity increases with age. Long-term clinical research data show that simvastatin treatment can improve the quality of life of patients. 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 triglyceride-lowering effect 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 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.
