Product Overview
[Drug Name]
Generic Name: Simvastatin Tablets
Trade Name: BiXinShu Simvastatin Tablets 10mg x 10 Tablets
Pinyin Full Code: BiXinShuXinFaTaTingPia10MG x 10Pia
[Main Ingredient]
Simvastatin.
[Properties]
This product is a film-coated tablet that appears white or off-white after removal of the coating.
[Indications/Main Functions]
Simvastatin is indicated for lowering elevated total cholesterol, low-density lipoprotein cholesterol, apolipoprotein B, and triglycerides in patients with primary hypercholesterolemia, heterozygous familial hypercholesterolemia, or mixed hypercholesterolemia when dietary control and other non-drug treatments are unsatisfactory.
[Specifications]
10mg x 10s
[Dosage and Administration]
Patients should follow a standard cholesterol-lowering diet before starting simvastatin therapy and continue to do so during treatment. 1. Hypercholesterolemia: The general starting dose is 10mg daily, taken in the evening. For patients with mild to moderately elevated cholesterol levels, the starting dose is 5 mg daily. Dose adjustments should be made at least four weeks apart, with a maximum dose of 40 mg daily, taken in the evening. Cholesterol levels should be monitored regularly, and if cholesterol levels are significantly below the target range, a dose reduction of simvastatin should be considered. 2. Coronary Artery Disease: Patients with coronary artery disease can start with 20 mg/day. Dose adjustments should be made at least four weeks apart, with a maximum dose of 40 mg daily, taken in the evening. 3. Concomitant Medication: Simvastatin is effective both alone and in combination with bile acid sequestrants. Concomitant use with fibrates or niacin should generally be avoided. For patients taking immunosuppressants (such as cyclosporine), the starting dose of simvastatin should be 5 mg/day, not exceeding 10 mg/day. 4. Patients with Renal Insufficiency: Since simvastatin is primarily excreted in the bile, with minimal renal excretion, no dose adjustment is necessary in patients with moderate renal insufficiency. This drug should be used with caution in patients with severe renal impairment (creatinine clearance <30 mg/min). The starting dose for such patients should be 5 mg/day, and close monitoring is required when the dose exceeds 10 mg/day.
[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 related to the drug) reported at an incidence of greater than or equal to 1% included abdominal pain, constipation, and flatulence. Adverse reactions reported at 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, elevated 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 are mild or transient. Elevations of serum creatine phosphokinase (CK) derived from skeletal muscle have also been reported.
[Contraindications]
1. Hypersensitivity to any component. 2. Active hepatitis or unexplained persistent elevations 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, erythrotoxin, clarithromycin, and nefazodone), or with fibric acid derivatives 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 (≥1 g/day), may increase the incidence and severity of myopathy. Furthermore, elevated plasma levels of HMG-CoA reductase inhibitors may also 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 blood levels and, therefore, increase 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, in adults beginning early anticoagulant therapy and concurrently taking simvastatin, frequent prothrombin time measurements should be performed to ensure that the prothrombin time does not significantly change. After patients taking coumarin derivatives have achieved a stable prothrombin time, 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-lowering diet before starting simvastatin therapy and continue this diet 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, persistent elevations in serum aminotransferases (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 be monitored and monitored closely before treatment. If a patient's 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 aminotransferases (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 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 therapy 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 in the absence of any medication, 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 these patients. 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 product should be used with caution in patients with excessive alcohol consumption and/or a history of liver disease.
[Children's Use]
Follow medical advice.
[Elderly Patients' Use]
Follow medical advice.
[Overdose]
There have been a few reports of overdoses, with patients experiencing no specific symptoms. All patients have recovered without sequelae. The maximum dose used was 450 mg. Conventional measures are generally used to manage overdoses.
[Pharmacology and Toxicology]
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 can reduce cholesterol (TC) levels in the serum, liver, and aorta of rabbits with hyperlipidemia, and lower very low-density lipoprotein cholesterol (VLDL-C) and low-density lipoprotein cholesterol (LDL-C) levels.
