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Simvastatin tablets

Product description
Approval date: June 21, 2006
 
Date of revision: September 30, 2010
 
         October 16, 2013
 
         November 30, 2015
 
Simvastatin tablets
 
Please read the instructions carefully and use them under the guidance of a physician.
 
 
 
【Drug Name】
 
Generic name: Simvastatin tablets
English name: Simvastatin Tablets
 
Pinyin: Xinfatating Pian
[Ingredients] The main component of this product is simvastatin. Its chemical name is: 2,2-dimethylbutyric acid (4R,6R) -6-[2-[(1S,2S,6R,8S,8aR) - 1,2,6,7,8,8a-hexahydro-8-hydroxy-2,6-dimethyl-1-naphthyl]ethyl]tetrahydro-4-hydroxy-2H-pyran-2-one -8-ester.
 
 
 
Molecular formula: C25H38O5
 
Molecular weight: 418.57
 
【Properties】 This product is a film-coated tablet, which is white or off-white after removal of the coating.
[indications]
    Hypercholesterolemia
 
(1) For patients with primary hypercholesterolemia, simvastatin can be treated when diet control and other non-drug treatments are not ideal. Simvastatin not only lowers total cholesterol, low-density lipoprotein cholesterol, apolipoprotein B and triglycerides, but also raises high-density lipoprotein cholesterol, thereby lowering low-density lipoprotein cholesterol/high-density lipoprotein cholesterol and total cholesterol / High density lipoprotein cholesterol ratio.
    (2) Simvastatin lowers cholesterol levels in patients with hypercholesterolemia and hypertriglyceridemia who are predominantly hypercholesterolemia.
    2. Coronary heart disease
 
For patients with coronary heart disease complicated with hypercholesterolemia, simvastatin is suitable for:
 
(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 myocardial recanalization (coronary artery bypass grafting and percutaneous balloon coronary angioplasty) due to coronary events;
 
(4) delay the progression of coronary atherosclerosis, including the reduction of new lesions and the formation of total occlusion.
[Specification] 10mg
 
【Dosage】
    Patients should receive a standard cholesterol-lowering diet and continue to maintain during the course of treatment with simvastatin.
    1. Hypercholesterolemia:
 
The general starting dose is 10mg (1 tablet) per day, and it is served in the evening. For patients with mild to moderately elevated cholesterol levels, the starting dose is 5 mg (1/2 tablet) per day. If you need to adjust the dose, it should be more than four weeks, the maximum dose is 40mg (4 tablets) per day, and served in the evening.
 
Cholesterol levels should be monitored regularly, and if the cholesterol level is significantly below the target range, consideration should be given to reducing the dose of simvastatin.
   2. Coronary heart disease:
 
Patients with coronary heart disease can take 20mg (2 tablets) per day as the starting dose. If the dose needs to be adjusted, it should be more than four weeks apart. The maximum dose is 40mg (4 tablets) per day.
   3. Combined medication:
 
Simvastatin is effective alone or in combination with a bile acid sequestrant. In general, avoid using it simultaneously with fibrates or niacin. In patients taking an immunosuppressant (such as cyclosporin), the initial dose of simvastatin should be 5 mg (1/2 tablet) per day and no more than 10 mg per day (1 tablet).
   4. Patients with renal insufficiency:
 
Since simvastatin is mainly excreted via the bile, and the amount excreted by the kidney is small, patients with moderate renal insufficiency do not have to adjust the dose. Patients with severe renal insufficiency (creatinine clearance less than 30ml / min) should be used with caution. The starting dose of such patients should be 5mg (1/2 tablet) per day, when the dose exceeds 10mg (1 tablet) per day, It should be closely monitored.
【Adverse reactions】
    Simvastatin is generally well tolerated and most of the adverse reactions are mild and transient. In the clinical control study, less than 2% of patients discontinued the drug due to the adverse reactions of simvastatin.
 
In clinical controlled studies, the incidence of drug-related ≥1% adverse reactions were abdominal pain, constipation, flatulence, and the incidence of 0.5% to 0.9% of adverse reactions were fatigue and headache.
 
Reports of myopathy are rare.
    The following adverse reactions have been reported in clinical observation and post-marketing applications: nausea, diarrhea, rash, indigestion, itching, hair loss, dizziness, muscle spasm, myalgia, pancreatitis, paresthesia, peripheral neuropathy, vomiting, and anemia , rhabdomyolysis and hepatitis / jaundice rarely occur.
 
Significant allergic reactions including one or more of the following symptoms are rarely reported: angioedema, lupus-like syndrome, rheumatic polymyalgia, vasculitis, thrombocytopenia, eosinophilia, ESR Elevation, arthritis, joint pain, urticaria, light sensitivity, fever, flushing, difficulty breathing, and discomfort.
 
Laboratory tests have found that significant and sustained elevations in serum transaminases are rarely reported. Alkaline phosphatase and gamma-glutamate transpeptidase have been reported to be elevated. Abnormal liver function tests are generally mild or transient. The rise of serum creatine kinase (CK) derived from skeletal muscle has been reported.
 
Post-marketing surveillance of statins has reports of hyperglycemia, impaired glucose tolerance, elevated glycated hemoglobin levels, new-onset diabetes, worsening glycemic control, and some statins have reports of hypoglycemia.
Post-marketing experience: There are rare cognitive impairment reports in the post-marketing surveillance of statins, which are characterized by memory loss, memory loss, confusion of thinking, etc., mostly non-severe, reversible reactions, which can be recovered after drug withdrawal. .
[taboo]
 
The following conditions are disabled:
1. Those who are allergic to any of the ingredients in this product.
2. Active liver disease or unexplained serum transaminase continues to rise.
 
3. Pregnant and lactating women.
4. It is forbidden to be combined with tetrahydrophenolic calcium channel blocker mbeidil.
 
【Precautions】
    Muscle function
 
HMG-CoA reductase inhibitors occasionally cause myopathy, manifested as muscle pain or weakness with a significant increase in CK (10 times higher than the upper limit of normal). Rhabdomyolysis of acute renal failure with or without secondary myoglobinuria is rarely reported. In the Nordic Simvastatin Survival Study, 1 case of myopathy occurred in 1399 patients taking simvastatin 20 mg daily, and 822 patients who received simvastatin 40 mg daily did not develop myopathy during the median 5.4 years. In two 6-month clinically controlled studies, 1 of 436 patients taking simvastatin 40 mg developed myopathy, and 699 patients with simvastatin 80 mg developed 5 myopathy. The combination of simvastatin and certain drugs increases the risk of myopathy, and some of these drugs were excluded from the study design.
 
Myopathy caused by drug interaction
 
HMG-CoA reductase inhibitors, when combined with drugs that cause myopathy alone, increase the incidence and severity of myopathy, including gemfibrozil and other fibrates, as well as lipid-lowering doses ( Niacin (nickic acid) ≥ 1 g/day.
 
In addition, an increase in the activity of HMG-CoA reductase inhibitors in plasma also increases the risk of myopathy. Simvastatin and other HMG-CoA reductase inhibitors are metabolized by cytochrome P450 isoenzyme 3A4 (CYP3A4). Some drugs that have a significant inhibitory effect on this metabolic pathway at therapeutic doses can increase the blood levels of HMG-CoA reductase inhibitors and thus may increase the risk of myopathy. These include cyclosporin, antifungal Itraconazole and ketoconazole, macrolide antibiotics (erythromycin, clarithromycin, telithromycin), fusidic acid, HIV protease inhibitors And the antidepressant nefazodone.
 
Reduce the risk of myopathy:
 
(1) General measures
 
Patients should be informed of the risk of myopathy at the start of simvastatin treatment and promptly report unexplained muscle pain, tenderness or weakness. A patient's CK level is 10 times higher than the upper limit of normal and accompanied by an unexplained muscle symptom indicating a myopathy. If diagnosed or suspected of myopathy, simvastatin should be discontinued. For most cases, muscle symptoms and CK increase will recover after timely termination of treatment.
 
Many patients with rhabdomyolysis have a history of comorbidities. Some patients have a history of renal insufficiency, which is usually the secondary cause of long-term diabetes. For such patients, caution should be exercised when increasing the dose. At the same time, simvastatin should be discontinued in the first few days before a larger surgery and in the case of a more serious acute medical or surgical disease, due to the inability to ascertain the poor secondary symptoms of short-term interruption of treatment.
 
(2) Measures to reduce the risk of myopathy caused by drug interactions (see above)
 
The pros and cons should be weighed when planning to use simvastatin in combination with any other interacting drug, and the patient's muscle pain, tenderness, or weakness signs and symptoms should be carefully monitored, especially during the first few months of treatment. Increase the dose period. In this case, consider checking CK regularly, but this does not ensure that myopathy can be prevented.
 
Simvastatin should be avoided in combination with fibrates or niacin unless the benefits of altered lipid levels are likely to exceed the increased risk of this combination. In small, short-term, and carefully monitored clinical studies, small doses of simvastatin in combination with fibrates or niacin did not cause myopathy. HMG-CoA reductase inhibitors in combination with these drugs generally do not lower HDL cholesterol, but can further reduce triglycerides and increase HDL cholesterol. Clinical practice shows that the risk of myopathy occurring with simvastatin in combination with niacin is lower than that of fibrates.
 
Because the risk of myopathy occurring at larger doses is significantly increased, the dose of simvastatin should not exceed 10 mg/day for patients taking cyclosporin, fibrate or niacin (see [Usage and Dosage] Combination therapy). Simvastatin is not recommended for use with itraconazole, ketoconazole, erythromycin, clarithromycin, telithromycin, fusidic acid, HIV protease inhibitor or nefazodone. Since there is no report of adverse effects on long-term lipid-lowering effects due to short-term withdrawal, it may be temporarily discontinued when it is necessary to use itraconazole, ketoconazole, erythromycin or clarithromycin for short-term treatment. Simvastatin. Simvastatin should be avoided in combination with other drugs that have a potential inhibitory effect on CYP3A4, unless the benefits of the combination therapy outweigh the increased risk.
    2. Liver function
 
In clinical studies, a small number of adult patients receiving simvastatin showed a sustained increase in serum transaminase (three times higher than the upper limit of normal). After discontinuation or discontinuation of these patients, transaminase levels are usually slowly reduced to pre-treatment levels. This elevated transaminase is not associated with jaundice or other clinical signs or symptoms, and no allergic manifestations. Some of these patients had abnormal liver function tests before simvastatin treatment and/or had consumed a large amount of alcohol.
 
It is recommended that all patients undergo a liver function test at regular intervals (eg, once every six months) before the start of treatment and during the first year after the start and after the dose is increased. For patients with elevated serum transaminases, liver function should be reviewed in a timely manner and the frequency of examination should be increased. If the transaminase level shows an upward trend, especially if it rises to 3 times the upper limit of normal and does not continue to fall, the drug should be discontinued.
 
This medicine should be used with caution in patients who drink large amounts of alcohol and/or have a history of previous liver disease. Simvastatin is contraindicated in patients with active liver disease or elevated levels of transaminase.
 
As with other lipid-lowering drugs, there was a report of elevated serum transaminase (three times lower than the upper limit) after simvastatin treatment. These changes occur shortly after the start of simvastatin treatment, but are often transient, without any symptoms and without interrupting treatment.
    3. Eye examination
 
Even in the absence of any medication, the incidence of lens opacity increases with age. Long-term clinical studies have shown that simvastatin has no adverse effects on the human lens.
    4. Hypertriglyceridemia
 
Simvastatin only moderately lowers triglycerides and is not suitable for the treatment of abnormalities characterized by elevated triglycerides (such as type I, IV and V hyperlipidemia).
    5. Patients who have heavy drinking and/or have a history of liver disease should use this product with caution.
[Pregnant women and lactating women]
    There are no data on the use of simvastatin in pregnant women. Because atherosclerosis is a chronic process, the use of lipid-lowering drugs during pregnancy has little effect on the long-term treatment of primary hypercholesterolemia. Cholesterol and other products of its biosynthetic pathway are essential components of fetal development, including the synthesis of steroids and cell membranes. Because HMG-CoA reductase inhibitors such as simvastatin reduce the synthesis of cholesterol and other products of its biosynthetic pathway, pregnant women ban simvastatin. Among women of childbearing age, simvastatin can only be used in women who are less likely to become pregnant. If a woman is pregnant while taking the drug, she should be discontinued and informed of possible damage to the fetus.
    It is not known whether simvastatin and its metabolites are secreted by human milk. Because many drugs are secreted by human milk and may cause serious adverse reactions, women who take simvastatin should not breastfeed (please refer to [taboo]).
[Children's medication]
    The safety and efficacy of medication for children has not been determined. Simvastatin is currently not recommended for children.
[Geriatric Use]
    In elderly patients (greater than 65 years), in a clinical controlled study using simvastatin, the effect of lowering total cholesterol and low-density lipoprotein (LDL) cholesterol was similar to that of other populations, and adverse reactions and laboratory abnormalities occurred. There is no significant increase in the rate.
【medicine interactions】
    Gemfibrozil and other fibrates, niacin (niacin) at a lipid-lowering dose (≥1 g/day): These drugs have an increased risk of myopathy when combined with simvastatin, probably because these drugs are separate It can cause myopathy when used (please refer to [Precautions] Muscle Effect). There is no evidence that these drugs have an effect on the pharmacokinetics of simvastatin.
 
Interaction with CYP3A4:
 
Simvastatin has no CYP3A4 inhibitory activity and, therefore, it is presumed that it does not affect the plasma levels of other drugs metabolized by CYP3A4. However, simvastatin itself is a substrate for CYP3A4. During the simvastatin treatment period, a strong inhibitor of CYP3A4 may increase the risk of myopathy by increasing plasma HMG-CoA reductase inhibitory activity. These strong inhibitors include cyclosporin, mibezil, itraconazole, ketoconazole, erythromycin, clarithromycin, telithromycin, fusidic acid, HIV protease inhibitors and nefazodone (See [Notes] Muscle Effect).
    Grapefruit juice contains one or more ingredients that inhibit CYP3A4 and increases plasma levels of drugs metabolized by CYP3A4. The conventional consumption (250 ml per day) produced little effect (by measuring the area under the concentration time curve, plasma HMG-CoA reductase inhibitory activity increased by 13%) and was of no clinical significance. However, such as
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