Buy Zocor® pills 20 mg, 28 pcs
  • Buy Zocor® pills 20 mg, 28 pcs

Simvastatin

Merck Sharp & Dohme
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2019-09-19
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Clinical Pharmacology

Zocor is a lipid-lowering drug obtained synthetically from the fermentation product Aspergillus terreus.

In the body, simvastatin (the active ingredient of the drug Zocor®), which is an inactive lactone, undergoes hydrolysis to form the corresponding hydroxy acid derivative. The latter is a major metabolite that has an inhibitory effect on 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) - reductase, an enzyme that catalyzes the initial and cholesterol biosynthesis stage (Cc). As a result, as shown in clinical studies, Zocor lowers total plasma cholesterol, low density lipoprotein (LDL) and very low density lipoprotein (VLDL). Zocor causes a decrease in plasma triglycerides, as well as a moderate increase in high-density lipoprotein (HDL) and, thus, reduces the ratio of LDL / HDL and total cholesterol / HDL.

Simvastatin, an active metabolite, is a specific inhibitor of HMG-CoA reductase, an enzyme catalyzing the formation of mevalonate from HMG-CoA. Since the conversion of HMG-CoA to mevalonat is an early stage of cholesterol biosynthesis, it is believed that the use of Zocor should not cause the accumulation of potentially toxic sterols in the body. In addition, HMG-CoA is easily metabolized to acetyl-Co-A, which is involved in many processes of biosynthesis in the body.

Studies were conducted therapeutic effect of Zocor on primary hypercholesterolemia, in which the appointment of a diet was insufficient. Zocor is highly effective in reducing total cholesterol and LDL in cases of heterozygous familial and non-familial forms of hypercholesterolemia, as well as in mixed hyperlipidemia, when elevated cholesterol is a risk factor. A noticeable effect was achieved within 2 weeks, the maximum therapeutic effect - within 4-6 weeks after the start of treatment. The effect persisted with continued treatment. At the termination of therapy with Zocor, the total cholesterol content returned to the initial level before the start of treatment.

In a study of the effect of simvastatin on survival (4S), the effect of Zocor therapy on total mortality (median patient participation time of 5.4 years) was evaluated in 4444 patients with coronary artery disease with baseline total cholesterol 212-309 mg / dL (5.5-8.0 mmol / l) In this multicenter, randomized, double-blind, placebo-controlled study Zocor reduced the risk of total mortality by 30%, death from coronary heart disease - by 42%, the incidence of myocardial infarction, confirmed in hospital conditions - by 37%. Moreover, Zocor reduced by 37% the risk of the need for surgery to restore coronary blood flow.

A multicenter, placebo-controlled study (Heart Protection Study / HPS) was conducted in the UK for 5.5 years. The study involved 20,536 patients with coronary artery disease or the risk of its development and the level of total cholesterol from 3.5 mmol / l and above. According to the results of the study, it was found that the use of Zocor reduced the risk of heart attack, stroke and reduced the frequency of revascularization operations by 1/3 (after allowing for non-compliance with the regimen) while maintaining the safety of using the drug. The study also found that the effectiveness of Zocor did not depend on the initial cholesterol level, the age and sex of the patients, and the simultaneous treatment of another therapy.

Indications

  • Coronary heart disease.
  • In order to reduce overall mortality.
  • In order to reduce the risk of coronary mortality and prevention of myocardial infarction.
  • To reduce the risk of stroke and transient cerebral circulatory disorders.
  • In order to reduce the likelihood of undergoing surgery to restore coronary blood flow (coronary artery bypass surgery and percutaneous transluminal coronary angioplasty).
  • In order to slow the progression of coronary atherosclerosis.
  • Reducing the elevated levels of total cholesterol and cholesterol / LDL in patients with primary hypercholesterolemia, when the use of diet therapy and other non-pharmacological measures did not bring an adequate effect. Zocor increases HDL and thus reduces the ratio of LDL / HDL and total cholesterol / HDL.
  • Reducing elevated cholesterol levels in patients with combined hypercholesterolemia and hypertriglyceridemia, when hypercholesterolemia is a risk factor.

Composition

1 tablet contains:

Active substance: Simvastatin 20 mg.

Simvastatin is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Zocor® Merck Sharp & Dohme USA pills
pills
Simvastatin Vertex Russia pills
Simvastatin Hemofarm Serbia pills
Simvastatin Zentiva KS Czech pills
Avenkor Ozon Russia pills
Simvahexal Hexal AG Germany pills
Vasilip Krka dd Novo mesto AO Slovenia pills

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Simvastatin

Dosage and Administration

InsideOnce a day, in the evening, drinking plenty of water. Drug intake time should not be associated with food intake.

Before treatment with Simvastatin, the patient should be prescribed a standard hypocholesterol diet, which should be followed during the entire course of treatment.

The recommended dose of simvastatin for the treatment of hypercholesterolemia varies from 10 to 80 mg once a day in the evening. The recommended initial dose for patients with hypercholesterolemia is 10 mg. The maximum daily dose is 80 mg.

Changes (selection) dose should be carried out at intervals of 4 weeks. In most patients, the optimal effect is achieved when taking the drug in doses up to 20 mg / day.

In patients with homozygous hereditary hypercholesterolemia, the recommended daily dose of simvastatin is 40 mg 1 time per day in the evening or 80 mg in 3 doses (20 mg in the morning, 20 mg in the afternoon and 40 mg in the evening).

When treating patients with coronary artery disease or high risk of developing coronary artery disease, the effective doses of Simvastatin are 20–40 mg / day. Therefore, the recommended initial dose in such patients is 20 mg / day. Changes (selection) of the dose should be carried out at intervals of 4 weeks, if necessary, the dose can be increased to 40 mg / day. If the content of LDL

Elderly patients and patients with mild or moderately severe degree of renal failure do not need to change the dosage of the drug.

In patients with CKD (Cl creatinine

For patients taking amiodarone or verapamil simultaneously with simvastatin, the daily dose should not exceed 20 mg.

Adverse reactions

From the digestive system: constipation, diarrhea, loss of appetite, flatulence, nausea, abdominal pain, pancreatitis, increased activity of ALT, AST, GGT, ALP.

From the side of the central nervous system and peripheral nervous system: headache, dizziness, muscle cramps, paresthesias, peripheral neuropathy.

Since the cardiovascular system: possible transient arterial hypotension.

From the musculoskeletal system: myalgia, myopathy, rhabdomyolysis, increased activity of CPK.

Allergic reactions: rarely - angioedema, lupus-like syndrome, vasculitis, thrombocytopenia, eosinophilia, increased ESR, arthritis, urticaria, fever, shortness of breath.

Dermatological reactions: photosensitivity, skin rash, itching, skin flushing, alopecia.

Other: anemia.

Contraindications

  • Hypersensitivity;
  • acute liver dysfunction;
  • severe renal failure.

Drug interactions

Cytotoxic agents, antifungal agents (ketoconazole, itraconazole), fibrates, high doses of nicotinic acid, immunosuppressants, erythromycin, clarithromycin, telithromytia, HIV protease inhibitors, nefazodone increase the risk of myopathy.

Cyclosporine or danazol: the risk of myopathy / rhabdomyolysis increases with co-administration of cyclosporine or danazol with high doses of simvastatin.

Other lipid-lowering drugs that can cause the development of myopathy: the risk of myopathy increases with the joint appointment of other lipid-lowering drugs that are not potent inhibitors of CYP3A4, but can cause myopathy in monotherapy. Such as gemfibrozil and other fibrates (except fenofibrate), as well as niacin (nicotinic acid) in a dose of> 1 g / day.

Amiodarone and verapamil: the risk of myopathy increases with co-administration of amiodarone or verapamil with high doses of simvastatin.

Diltiazem: the risk of myopathy is slightly increased in patients receiving diltiazem simultaneously with simvastatin at a dose of 80 mg.

Simvastatin potentiates the action of oral anticoagulants (eg, fenprocumon, warfarin) and increases the risk of bleeding, which requires the need to monitor blood clotting indicators prior to treatment, as well as quite often in the initial period of therapy.Once a stable level of prothrombin time or the International Normalized Attitude (MHO) is reached, its further monitoring should be carried out at intervals recommended for patients receiving anticoagulant therapy. When changing the dosage or discontinuing the administration of simvastatin, the prothrombin time or MHO should also be monitored as described above.

Simvastatin therapy does not cause changes in prothrombin time and the risk of bleeding in patients not taking anticoagulants. Increases digoxin levels in the blood plasma.

Kolestiramin and Kolestipol reduce bioavailability (use of simvastatin is possible 4 hours after taking these medicines, with an additive effect).

Grapefruit juice contains one or more components that inhibit CYP3A4 and can increase the plasma concentration of drugs metabolized by CYP3A4. An increase in the activity of HMG-CoA reductase inhibitors after consuming 250 ml of juice per day is minimal and has no clinical significance. However, consuming a large volume of juice (more than 1 l per day) while taking simvastatin significantly increases the level of inhibitory activity against HMG-CoA reductase in plasma. In this regard, it is necessary to avoid the consumption of grapefruit juice in large quantities.

Pregnancy and Lactation

Simvastatin may have an adverse effect on the fetus and is contraindicated in pregnant women. There are several reports of the development of anomalies in newborns whose mothers took simvastatin.
Women of reproductive age taking Simvastatin should avoid conception. The use of Simvastatin is not recommended for women of childbearing age who do not use contraceptives. If, in the course of treatment, the pregnancy does occur, Simvastatin should be canceled and the woman should be warned of the possible danger to the fetus.
Data on the allocation of Simvastatin with breast milk are not available. If necessary, the appointment of Simvastatin during breastfeeding should be borne in mind that many drugs are excreted in breast milk, and there is a risk of severe reactions, so breastfeeding while taking the drug is not recommended

Special instructions

At the beginning of therapy with simvastatin, a transient increase in liver enzymes is possible.

Before starting therapy and then regularly conduct a study of the function of the liver (monitor the activity of liver enzymes every 6 weeks for the first 3 months, then every 8 weeks for the remaining first year, and then once every six months), as well as with increasing doses should be a test on the definition of liver function. If you increase the dose to 80 mg, you need to test every 3 months. With a persistent increase in transaminase activity (3 times compared with the initial level), the intake of simvastatin should be stopped.

Simvastatin, like other HMG-CoA reductase inhibitors, should not be used with an increased risk of developing rhabdomyolysis and renal failure (against the background of severe acute infection, hypotension, planned major surgery, trauma, severe metabolic disorders).

Cancellation of hypolipidemic drugs during pregnancy does not have a significant impact on the results of long-term treatment of primary hypercholesterolemia.

Due to the fact that HMG-CoA reductase inhibitors inhibit cholesterol synthesis, and cholesterol and other products of its synthesis play a significant role in the development of the fetus, including the synthesis of steroids and cell membranes, simvastatin can have an adverse effect on the fetus when prescribing it to pregnant women (women reproductive age should avoid conception).If pregnancy occurs during treatment, the drug should be canceled, and the woman should be warned of the possible danger to the fetus.

The use of simvastatin is not recommended for women of childbearing age who do not use contraceptives.

In patients with low thyroid function (hypothyroidism) or in the presence of certain kidney diseases (nephrotic syndrome), with an increase in cholesterol level, the therapy underlying the disease should first be carried out.

Simvastatin is prescribed with caution to persons who abuse alcohol and / or have a history of liver disease.

Before and during treatment, the patient should be on a cholesterol diet.

The simultaneous intake of grapefruit juice may increase the severity of side effects associated with the intake of simvastatin, so their simultaneous intake should be avoided.

Simvastatin is not indicated in cases where there are hypertriglyceridemia types I, IV and V.

Treatment with simvastatin can cause myopathy, leading to rhabdomyolysis and renal failure. The risk of this disease increases in patients receiving simultaneously with simvastatin one or more of the following drugs: fibrates (gemfibrozil, fenofibrate), cyclosporine, nefazadon, macrolides (erythromycin, clarithromycin), antifungal agents from the group of azoles (ketoconazole, itraconazole) and inhibitors HIV proteases (ritonavir). The risk of myopathy is also increased in patients with severe renal failure.

All patients starting therapy with simvastatin, as well as patients who need to increase the dose of the drug, should be warned about the possibility of myopathy and the need for immediate medical attention in case of unexplained pain, muscle soreness, lethargy or muscle weakness, especially if this is accompanied by malaise or fever. Drug therapy should be immediately discontinued if myopathy is diagnosed or contemplated.

In order to diagnose the development of myopathy, it is recommended to regularly measure CPK values.

When treating with simvastatype, an increase in the serum CPK content is possible, which should be taken into account in the differential diagnosis of chest pain. The criterion for discontinuation of the drug is an increase in the content of CK in the serum of more than 10 times relative to the upper limits of the norm. In patients with myalgia, myasthenia and / or a pronounced increase in the activity of CPK, treatment with the drug is stopped.

The drug is effective both in the form of monotherapy, and in combination with bile acid sequestrants.

In case of missing the current dose, the drug should be taken as soon as possible.

If it is time to take the next dose, do not double the dose.

Patients with severe renal insufficiency are treated under the control of renal function.

The duration of the drug is determined by the attending physician individually.

Influence on ability to drive motor transport and control mechanisms

No adverse effect of simvastatin on the ability to drive and work with mechanisms was reported.

Overdosage

None of the known several cases of overdose (maximum dose of 450 mg) revealed any specific symptoms.

Treatment:induce vomiting, take activated charcoal. Symptomatic therapy. Liver and kidney functions, serum CK levels should be monitored.

With the development of myopathy with rhabdomyolysis and acute renal failure (a rare but severe side effect), the drug should be stopped immediately and a diuretic and sodium bicarbonate should be given to the patient (intravenous infusion). If necessary, hemodialysis is indicated.

Rhabdomyolysis can cause hyperkalemia, which can be eliminated by intravenous administration of calcium chloride or calcium gluconate, infusion of glucose with insulin, using potassium ion exchangers or, in severe cases, using hemodialysis.

Studies and clinical trials of Simvastatin (Click to expand)

  1. Comparison of Bezafibrate and Simvastatin in the Treatment of Dyslipidaemia in Patients with NIDDM
  2. Quantitation of simvastatin and its β-hydroxy acid in human plasma by liquid–liquid cartridge extraction and liquid chromatography/tandem mass spectrometry
  3. Simvastatin and plasma very-long-chain fatty acids in X-linked adrenoleukodystrophy
  4. Simvastatin-induced thrombocytopenia
  5. Simvastatin treatment in the SLO syndrome: A safe approach?
  6. Treatment with simvastatin in normocholesterolemic patients with Alzheimer's disease: A 26-week randomized, placebo-controlled, double-blind trial
  7. Simvastatin enhances learning and memory independent of amyloid load in mice
  8. Simvastatin therapy prevents brain trauma-induced increases in β-amyloid peptide levels
  9. Inhibition of systemic sclerosis dermal fibroblast type I collagen production and gene expression by simvastatin
  10. RhoA-mediated, tumor necrosis factor α–induced activation of NF-κB in rheumatoid synoviocytes: Inhibitory effect of simvastatin
  11. Simvastatin inhibits cytokine-stimulated Cyr61 expression in osteoblastic cells: A therapeutic benefit for arthritis
  12. Pharmacokinetics and bioequivalence evaluation of two simvastatin 40 mg tablets (Simvast & Zocor) in healthy human volunteers
  13. Pregnancy outcomes after maternal exposure to simvastatin and lovastatin
  14. Rational improvement of simvastatin synthase solubility in Escherichia coli leads to higher whole-cell biocatalytic activity
  15. Development of a large-scale continuous substrate feed process for the biotransformation of simvastatin by Nocardia s.p.
  16. Simvastatin impairs smad-3 phosphorylation and modulates transforming growth factor β1-mediated activation of intestinal fibroblasts
  17. Development and validation of a highly sensitive and robust LC-ESI-MS/MS method for simultaneous quantitation of simvastatin acid, amlodipine and valsartan in human plasma: application to a clinical pharmacokinetic study
  18. Analysis of five HMG-CoA reductase inhibitors— atorvastatin, lovastatin, pravastatin, rosuvastatin and simvastatin: pharmacological, pharmacokinetic and analytical overview and development of a new method for use in pharmaceutical formulations analysis and in vitro metabolism studies
  19. A selected ion monitoring method for quantifying simvastatin and its acid form in human plasma, using the ferroceneboronate derivative
  20. Determination of the HMG–CoA reductase inhibitors simvastatin, lovastatin, and pravastatin in plasma by gas chromatography/chemical ionization mass spectrometry
  21. Effects of simvastatin treatment on oxidant/antioxidant state and ultrastructure of streptozotocin-diabetic rat lung
  22. Simvastatin treatment prevents oxidative damage to DNA in whole blood leukocytes of dyslipidemic type 2 diabetic patients
  23. Geraniol and simvastatin show a synergistic effect on a human hepatocarcinoma cell line
  24. ChemInform Abstract: A Cost-Efficient Synthesis of Simvastatin via High-Conversion Methylation of an Alkoxide Ester Enolate.

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