Simgal
Simgal: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Simgal
ATX code: C10AA01
Active ingredient: Simvastatin (Simvastatin)
Producer: IVAX Pharmaceuticals sro, Teva Czech Industries sro (Czech Republic)
Description and photo update: 2019-05-08
Simgal is a hypolipidemic drug that inhibits HMG-CoA reductase action.
Release form and composition
Simgal is available in the form of film-coated tablets:
- 10 mg: biconvex, round, light pink (7 pieces in blisters, in a cardboard box 1 blister; 14 pieces in blisters, in a cardboard box 1, 2 or 6 blisters);
- 20 mg: biconvex, round, pink, on one side there is a risk (7 pieces in blisters, in a cardboard box 1 blister; 14 pieces in blisters, in a cardboard box 1, 2 or 6 blisters);
- 40 mg: biconvex, round, dark pink, on one side there is a risk (7 pieces in blisters, 1 blister in a cardboard box; 14 pieces in blisters, in a cardboard box 1, 2 or 6 blisters).
Composition of 1 tablet:
- active substance: simvastatin - 10, 20 or 40 mg;
- auxiliary components: citric acid, pregelatinized corn starch, ascorbic acid, magnesium stearate, butylhydroxyanisole, lactose monohydrate;
- film shell (Opadrai pink OY-B-34915 - dose 10 mg, Opadrai pink OY-B-34917 - dose 20 mg, Opadrai brown AMB 80W36564 - dose 40 mg): talc, xanthan gum, polyvinyl alcohol, lecithin, iron oxide dye red, titanium dioxide, dye iron oxide yellow; The composition of the shell Opadrai pink OY-B-34915 additionally contains indigo carmine, and the composition of the casings Opadrai brown AMB 80W36564 and Opadrai pink OY-B-34917 contains black iron oxide.
Pharmacological properties
Pharmacodynamics
Simvastatin is a lipid-lowering agent synthetically obtained from the fermentation product of Aspergillus terreus. In the body, it undergoes hydrolysis, which results in the formation of a hydroxy acid derivative. This active metabolite is able to inhibit the enzyme HMG-CoA reductase (3-hydroxy-3-methyl-glutaryl-CoA reductase), which catalyzes the starting reaction of mevalonate synthesis from HMG-CoA. Since the conversion of HMG-CoA to mevalonate occurs in the early stages of cholesterol formation, the use of the drug does not lead to the accumulation of potentially toxic sterols in the body. HMG-CoA is metabolized to acetyl-CoA, which is involved in many synthesis processes in the body.
Simvastatin reduces the content of low-density lipoproteins, very low-density lipoproteins, triglycerides and total cholesterol in blood plasma (with mixed hyperlipidemia and heterozygous non-familial and familial hypercholesterolemia, when high plasma cholesterol is a risk factor).
The drug also increases the level of high density lipoproteins and reduces the ratio of total cholesterol / high density lipoprotein and low density lipoprotein / high density lipoprotein.
The effect appears 2 weeks after the start of taking Simgal, and the maximum therapeutic effect is achieved after 4-6 weeks. With continued therapy, the effect persists. In the case of discontinuation of treatment, a gradual return of the cholesterol content to the initial value occurs.
Pharmacokinetics
Simvastatin is rapidly absorbed in the gastrointestinal tract. The maximum concentration is reached 1.3–2.4 hours after ingestion of the drug, and after 12 hours it decreases by 90%. Simvastatin is approximately 95% bound to plasma proteins.
The drug metabolism occurs in the liver, resulting in the formation of active and inactive metabolites. T 1/2 (half-life) of active metabolites of simvastatin is 1.9 hours.
About 60% of the drug is excreted in the form of metabolites with feces. Approximately 10-15% of simvastatin is excreted in an inactive form by the kidneys.
Indications for use
Simgal is prescribed for hypercholesterolemia and coronary heart disease (IHD).
With hypercholesterolemia, indications for use are:
- primary hypercholesterolemia type 2a and 2b according to Fredrickson (in addition to diet therapy and other methods of treatment, for example, correction of body weight and increase in general physical activity);
- combined hypertriglyceridemia and hypercholesterolemia, refractory to treatment with exercise and a special diet;
- hereditary homozygous hypercholesterolemia (in addition to diet and other methods of lowering lipid levels if they are not effective enough).
With ischemic heart disease, Simgal is used to achieve the following goals:
- reducing the risk of overall mortality by reducing the number of deaths in IHD;
- reducing the risk of dangerous coronary and vascular complications (stroke, nonfatal myocardial infarction, revascularization surgery, sudden coronary death);
- reducing the number of cases in which surgery is required to restore peripheral blood flow;
- reducing the risk of the need for surgical intervention to restore coronary blood flow (coronary artery bypass grafting, coronary angioplasty, etc.).
Contraindications
Absolute:
- active liver disease or increased activity of liver enzymes in serum, of unknown origin;
- a marked decrease in blood pressure;
- myopathy;
- severe acute infectious diseases;
- trauma;
- planned surgical intervention;
- severe metabolic disorders;
- simultaneous use with itraconazole, ketoconazole, clarithromycin, nefazodone, erythromycin, telithromycin, HIV protease inhibitors and other CYP3A4 inhibitors;
- lactase deficiency, lactose intolerance or glucose-galactose malabsorption syndrome (the drug contains lactose);
- children and adolescents up to 18 years old (safety and efficacy of using Simgal in children have not been established);
- period of pregnancy;
- period of breastfeeding;
- hypersensitivity to the main or auxiliary components, as well as other statin drugs.
Relative (Simgal is used with caution):
- conditions in which the development of severe renal failure is possible (acute infectious diseases of a severe course, disturbances in the water and electrolyte balance, arterial hypotension, severe endocrine disorders, etc.);
- the presence of risk factors for the development of rhabdomyolysis / myopathy [uncontrolled hypothyroidism, impaired renal function (creatinine clearance less than 30 ml / min), advanced age over 65 years, rhabdomyolysis / myopathy associated with taking fibrates and statins (history), use in women, alcoholism, family history of muscle disease];
- epilepsy;
- increased or decreased tone of skeletal muscles of unknown origin;
- postoperative period in patients after transplantation receiving immunosuppressants;
- drinking alcohol in large quantities;
- simultaneous use with gemfibrozil, danazol, cyclosporine and other fibrates (except fenofibrate), amiodarone, diltiazem, verapamil, fusidic acid, grapefruit juice and nicotinic acid (in lipid-lowering doses of ≥1 g per day).
Instructions for the use of Simgal: method and dosage
Simgal tablets are taken orally, once a day (in the evening), washed down with water in sufficient quantity.
The recommended dose of the drug varies in the range of 5–80 mg per day. Dose adjustment is carried out gradually, with an interval of at least 1 month. The maximum daily dose of 80 mg is prescribed only to those patients who have not achieved the desired therapeutic effect when taking simvastatin at a dose of 40 mg per day, as well as to those taking simultaneously with Simgal diltiazem. The rest of the patients should not take more than 40 mg of the drug per day.
In hypercholesterolemia, the initial daily dose of simvastatin is 10–20 mg. In cases where it is necessary to reduce the concentration of low density lipoprotein (LDL) by 45% or more, you can increase the initial dose to 20-40 mg per day.
With homozygous hereditary hypercholesterolemia, Simgal is prescribed at a dose of 40 mg once a day or 80 mg per day in three divided doses (20 mg in the morning and in the afternoon, and 40 mg in the evening).
Before starting therapy, the patient is prescribed a cholesterol diet, which he must adhere to throughout the entire course of treatment.
In IHD, the initial dose of simvastatin is 20 mg once a day (in the evening), then, if necessary, the dose is increased to 40 mg per day (gradually, every 4 weeks).
With simultaneous use with gemfibrozil, danazol, cyclosporine, other fibrates (except fenofibrate) and nicotinic acid in a daily dose of at least 1 g, the dose of Simgal should not exceed 10 mg per day. When combined with verapamil or amiodarone, Simgal 20 mg is prescribed.
Simvastatin should be taken separately from bile acid sequestrants (cholestyramine and colestipol) - 2 hours before taking them or 4 hours after taking these drugs.
Elderly patients and patients with mild to moderate renal insufficiency do not require dose adjustment. In severe renal insufficiency, the dose of the drug is no more than 10 mg per day, and the treatment is carried out under the supervision of a physician.
Side effects
- gastrointestinal tract, liver and biliary tract: rarely - nausea, acute pancreatitis, vomiting, abdominal pain, hepatitis, diarrhea or constipation, jaundice, flatulence; very rarely - liver failure;
- respiratory system: very rarely (with prolonged therapy) - interstitial lung disease;
- nervous system: very often - insomnia; rarely - paresthesia, dizziness, peripheral neuropathy, headache; very rarely - nightmares, sleep disturbances, depression, memory impairment;
- hematopoietic system: rarely - anemia;
- laboratory indicators: rarely - increased activity of creatine phosphokinase, alkaline phosphatase and liver enzymes;
- musculoskeletal system: rarely - muscle cramps, muscle pain, rhabdomyolysis, myopathy;
- skin: rarely - baldness;
- allergic reactions: rarely - urticaria, itching and rash on the skin, hypersensitivity (eosinophilia, thrombocytopenia, polymyalgia rheumatica, arthralgia, fever, angioedema, arthritis, flushing of the skin of the face, feeling unwell, lupus-like skin syndrome, hyperensitisation shortness of breath, increased erythrocyte sedimentation rate);
- other reactions: rarely - acute renal failure, asthenia, decreased potency, palpitations.
Overdose
In case of an overdose of the drug, specific symptoms have not been registered (several cases are known when Simgal was taken at a dose of 450 mg).
Treatment is standard: it is necessary to induce vomiting and give the patient activated charcoal. If necessary, symptomatic therapy is prescribed. Serum creatine phosphokinase levels and renal and hepatic function should also be monitored.
With the development of acute renal failure and the occurrence of myopathy with rhabdomyolysis, the drug should be immediately discontinued and the patient should be given sodium bicarbonate as an intravenous infusion and a diuretic. If necessary, hemodialysis is performed.
Hyperkalemia, which can be caused by rhabdomyolysis, is eliminated by intravenous administration of calcium gluconate or calcium chloride, infusion of glucose and insulin, the use of potassium ion exchangers, and in severe cases, hemodialysis.
special instructions
If during treatment with Simgal, muscle weakness or lethargy, muscle soreness, unexplained pain, especially accompanied by fever and malaise, occur, it is necessary to urgently consult a doctor, since the listed symptoms may be signs of developing myopathy.
According to the instructions, Simgal should be canceled a few days before the planned surgical intervention (including dental surgery) and not used in the postoperative period.
Before starting therapy, regularly during treatment, as well as at each dose increase, it is recommended to examine liver function.
In patients with nephrotic syndrome and certain other kidney diseases, as well as in those with hypothyroidism, the underlying disease is first treated.
Simgal is not indicated for hypertriglyceridemia of types 1, 4 and 5.
When a patient has forgotten to take the next dose, it should be taken as soon as possible, but if it is time for the next dose, the dose should not be doubled.
The duration of the course is determined by the attending physician.
During treatment with Simgal, care must be taken when driving a car and operating other potentially dangerous machinery.
Application during pregnancy and lactation
Simgal is contraindicated for use during pregnancy. Children whose mothers took the drug may develop anomalies (there is evidence of several such cases).
Women of reproductive age who take simvastatin should use reliable contraception and avoid conception.
Despite the fact that there are no data on the excretion of simvastatin in breast milk, the use of Simgal during breastfeeding is not recommended.
Pediatric use
The drug is contraindicated in children and adolescents under 18 years of age, since the safety and effectiveness of its use at this age have not been established.
With impaired renal function
For patients with chronic renal failure (with creatinine clearance of 30 ml / min) or patients receiving fibrates, cyclosporine and nicotinamide, Simgal is prescribed in an initial dose of 5 mg (the daily dose should not exceed 10 mg).
For violations of liver function
The drug is contraindicated in active liver diseases and a persistent increase in the activity of liver enzymes of unknown origin.
Use in the elderly
In elderly patients, a change in the dose of simvastatin is not required.
Drug interactions
The risk of developing myopathy increases with the simultaneous use of Simgal with antifungal drugs, immunosuppressants, HIV protease inhibitors, cytostatics, high doses of nicotinic acid, clarithromycin, nefazodone, gemfibrozil and other fibrates (with the exception of fenofibrate), erythromycin and telithromycin.
When danazol, cyclosporine, verapamil, amiodarone, diltiazem, or amlodipine are co-administered with high doses of simvastatin, the likelihood of rhabdomyolysis / myopathy increases.
Simgal potentiates the action of indirect anticoagulants and increases the risk of bleeding; increases the plasma concentration of digoxin.
During the period of treatment with simvastatin, you should avoid consuming large amounts of grapefruit juice.
Analogs
Simgala analogs are: Aterostat, Atrolin, Aldesta, Vasilip, Vasta, Vabadin, Vasostat-Health, Vastatin, Cardak, Zosta, Zokor, Simvageksal, Simvakol, Simvostat, Simvastatin, Simvastatin Zentiva, Simvakardvali, Simmitva Tad.
Terms and conditions of storage
Store in a dark place at a temperature of 10-25 ° C. Keep out of the reach of children.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Simgal
The available reviews about Simgala testify to the good tolerability of the drug and the rare occurrence of side effects (subject to the recommendations in the instructions for use of the drug).
Price for Simgal in pharmacies
The cost of the drug varies depending on the dosage and packaging. To date, the average prices for Simgal in pharmacies are as follows:
- tablets 10 mg, 28 pcs. in the package - 217-224 rubles;
- tablets 10 mg, 84 pcs. in the package - 591–611 rubles;
- tablets 20 mg, 28 pcs. in the package - 282–392 rubles;
- tablets 20 mg, 84 pcs. in the package - 593–880 rubles;
- tablets 40 mg, 28 pcs. in the package - 584–650 rubles;
- tablets 40 mg, 84 pcs. in the package - 1357 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
