To lower the concentration of cholesterol in the blood, the doctor may prescribe the medicine "Simgal". The product is considered effective and relatively safe, but only when used in accordance with the manufacturer's instructions. The doctor will tell you about all the features of the reception, frequency and dosage, duration of the consultation. It is important to follow these tips in order to prevent negative effects on the body, the occurrence of side effects.
general information
Simgal tablets are based on simvastatin, made in the form of thin-film capsules. On sale there are several dosage options for the active substance.
The minimum format is 10 mg of the active compound in a single dose. In addition to simvastatin, the composition contains auxiliary compounds - vitamin C, citric acid, starches and cellulose, lactose and some other components.
Twice more tablets are available containing 20 mg of simvastatin. In addition to the active compound, excipients also include lactose monohydrate and magnesium stearate. The shell is made of opadra.
The highest dose of simvastatin is presented in Simgal 40 mg. Butylhydroxyanisole and ascorbic, citric acid, starches and lactose are present in the tablets as auxiliary components.
Each of the formats is painted in its own unique shade. As indicated in the instructions for use, "Simgal" 10 mg has a light pink color, twice as much concentration of the active compound is available in pink, one of the sides is supplemented with risk. 40 mg are painted in a dark shade of pink and are also supplemented with risk. All release formats are round, convex on both sides.
What is this about?
Simgal tablets belong to the class of lipid-lowering, stopping the activity of reductase HMG-CoA. The tool is synthetic, made by processing Aspergillus terreus. This is a lactone that does not show activity. Once in the human body, the substance enters into metabolic reactions (hydrolysis), which leads to the formation of hydroxyacids. It is the metabolite that shows activity by stopping the action of HMG-CoA reductase, an enzyme that initiates the primary formation stage of HMG-CoA mevalonate. Since this reaction is inhibited, respectively, the early synthesis of cholesterol is disrupted. The use of drugs on simvastatin does not provoke the accumulation of sterols that can have a toxic effect on the body. Acetyl-CoA is formed on the basis of HMG-CoA, an element necessary for various biochemical reactions.
This material contains a photo of Simgala. The drug, packaged in such boxes, is sold in many modern pharmacies. When used wisely, the concentration of triglycerides, low-density, very low-density lipoproteins is reduced in the body. The total concentration of cholesterol is reduced, which is especially important for patients who are diagnosed:
- mixed form hyperlipidemia;
- hypercholesterolemia familial, non-familial.
At the same time, taking the drug provokes an increase in the concentration of high-density lipoproteins in the circulatory system. The concentration of LDL and total cholesterol against the background of HDL is reduced.
Everything has its time!
As noted in the reviews and in the instructions for use, "Simgal" shows a pronounced effect no earlier than half a month after the start of administration. The most striking result can be observed after a month and a half. The activity of the basic compound is present throughout the entire therapeutic program. Soon after discontinuation of the drug, cholesterol indicators again return to their original values.
Drug kinetics
As indicated in the instructions for use "Simgala" (10 mg and other dosage forms), the active compound of the drug is absorbed in the digestive tract in a short time. The average absorption level is 85%. The indicators are not dependent on food intake. The highest level in blood plasma is observed after one and a half hours (sometimes up to two and a half hours) from the moment of use. A 90% reduction is recorded after half a day. Active compounds bind to plasma proteins 95%.
The primary transformation of simvastatin occurs in liver cells. In this case, beta-hydroxy acid is formed, four more products are active in the human body, as well as some other compounds that have no effect. The cytochrome isoenzyme CYP3A4 takes part in the reaction. Instructions "Simgala" contains a reference to the dependence of the rate of transformation processes and the quality of blood circulation, in particular, the state of the hepatic portal vein. The bioavailability of the active component is estimated at less than 5%. The process of transformation of this substance is quite lengthy. A course involving repeated use of the drug does not provoke its accumulation in the cells of the body.
The elimination half-life is estimated at 1.9 hours for active metabolic products. Up to 60% leave the body through the intestinal tract, about 15% are excreted unchanged with urine.
Therapeutic course: to whom is it recommended?
The drug "Simgal" is used for hypercholesterolemia. If the primary form of the disease is diagnosed, according to the typology of Fredrickson belonging to the Pa or Pb groups, Simgal is indicated as an adjuvant supplementing the treatment with diet and other non-drug approaches to normalizing the patient's condition. At the same time, it is recommended to intensify physical activity and do procedures for normalizing weight. "Simgal" is prescribed only if non-pharmacological measures do not show the desired effect.
It is recommended to use the drug in the treatment of persons with:
- combined hypercholesterolemia;
- hyperlipoproteinemia;
- hypertriglyceridemia.
With all these diagnoses, treatment begins with a diet and lifestyle changes, and a medication is taken if such measures do not show a result.
The inherited hypercholesterolemia (in the homozygous form) also allows the use of Simgal, but only as an additional step in the therapeutic course. The main treatment is diet, LDL-apheresis, and other techniques that help normalize the blood fat profile.
Additional indications
The instructions for use of "Simgal" indicate that this medication can be prescribed for ischemia to reduce the risk of death. Studies have shown that the drug helps to slightly reduce the overall mortality rate. At the same time, the likelihood of severe coronary and vascular complications is reduced. This applies to:
- coronary death;
- non-fatal infarction;
- stroke.
"Simgal" is indicated for revascularization. The use of the composition in some cases helps to avoid surgical intervention to normalize coronary circulation - there is no need for angioplasty or bypass surgery. Simgal allows you to reduce the number of cases when necoronary revascularization is required.
When is it impossible?
The instructions for use "Simgala" lists a rather impressive list of contraindications. The most basic limitation is intolerance to the active component, as well as other compounds used in the manufacture of the drug. Do not use tablets if hypersensitivity to any statin compounds has been identified, that is, inhibiting the activity of HMG-CoA reductase. This applies to the entire medical history.
The instructions for use "Simgala" as contraindications also mentioned:
- myopathy
- acute liver pathology;
- hyperactivity of liver transaminases in the blood serum when it is not possible to establish the cause of this condition;
- lack of lactase;
- lactose intolerance;
- malabsorption syndrome;
- gestation and lactation;
- the use of drugs stopping the activity of CYP3A4;
- treatment with drugs that inhibit HIV protease;
- infectious pathologies in acute form, proceeding severely;
- low pressure;
- planned surgical intervention;
- recent injuries;
- metabolic problems.
Simgal should not be used for the treatment of minor patients: there is no official information on the effectiveness of this course, possible dangers for patients, long-term consequences.
Special occasion
In relation to some patients, the instructions for the use of Simgal contain mention of the possibility of using the drug, but only with careful monitoring by the doctor and regular check of vital indicators of the functioning of internal systems and organs. These cases include:
- increased likelihood of myopathy, rhabdomyolysis;
- elderly age;
- uncontrollable hypothyroidism;
- information on muscle pathologies in the family history of the disease;
- impaired renal function (creatine clearance 30 ml / min or less);
- passing treatment with some groups of medications;
- recent transplantation;
- the need for the use of immunosuppressants;
- arterial persistently low blood pressure;
- severe acute infectious lesion;
- metabolic disorders;
- insufficiency of the endocrine system;
- imbalance of electrolytes in the body;
- previous surgery (including dental);
- epilepsy.
Certain restrictions are imposed by the tone of skeletal muscle tissue above or below normal, especially in cases where it is not possible to identify the cause of such a violation.
Among the medicines that require special attention when combined with Simgal, it is necessary to mention cyclosporins, nicotinic acid and fusidic. In addition, restrictions include:
- gemfibrozil;
- amiodarone;
- diltiazem.
The instructions contain references to the need to regularly check the performance of the body when combining Simgal and verapamil, danazole, and other fibrates. The exception is fenofibrates. If possible, avoid grapefruit juice during the course of eating.
"Interesting" position
As indicated in the instructions, "Simgal" (analogues mainly also) can not be used during the period of gestation. Cases of the birth of babies with abnormalities of intrauterine development on the background of taking simvastatin during pregnancy have been recorded. Deviations are explained by the influence of the active substance on the production of mevalonate, which affects not only the mother's body, but also the embryo.
The instructions for Simgal and analogues based on simvastatin indicate that women who are of reproductive age should use the most reliable methods to prevent conception during treatment with this group of medicines. If pregnancy has occurred during the treatment period or there is at least the slightest suspicion of such a situation, the medicine is immediately canceled. Refusal of lipid-lowering drugs during gestation practically does not affect the results of a long course.
As noted in the reviews, "Simgal" during breastfeeding, doctors are also not recommended. This is due to the lack of accurate information about the possibility of penetration of the active compound into milk. When ingested, simvastatin and its metabolic products can cause severe negative consequences, so you have to adhere to strict restrictions. If there is a need for Simgal therapy, the child is transferred from breastfeeding to artificial feeding.
How to use?
In the instructions of "Simgala" (10 mg and other dosage forms) there is a description of the standard course of taking the medication. At the consultation, the doctor can recommend an excellent regimen, in which case the doctor's recommendations have priority. Usually the drug is used daily in the evening, the entire dose prescribed for the day is drunk at a time, drinking plenty of clean water. The recommended daily dosage varies widely enough: from 5 mg to 80 mg. If there is a need for adjustment, the change in volumes is made no more than once a month.
80 mg per day is recommended to be used only if necessary to combine the described medication and drugs containing diltiazem, as well as in the absence of a satisfactory result when consuming 40 mg of simvastatin daily (the LDL profile is analyzed). Simgal medicine and simvastatin-based analogues are usually used at a dosage of up to 40 mg per day of the active compound.
If hypercholesterolemia is diagnosed, first the patient undergoes diet therapy, and only with its ineffectiveness they decide to support the condition with medications. The use according to the instructions for use "Simgala" (and analogues on simvastatin) requires continued diet throughout the course. They start taking 10-20 mg of simvastatin per day, and increase the concentration as often as necessary no more than once a month.
Proper use is the key to a good result
If you need to lower the LDL content in the circulatory system by 45% (or more), the course begins with 20-40 mg of simvastatin per day, carefully following the instructions for use. According to reviews, Simgal (and analogues on simvastatin) shows a reliable result, but at first a negative response is possible from an organism that adapts to a therapeutic course.
If a homozygous form of inherited hypercholesterolemia is established, the optimal dosage of the drug for a day is 40 mg of simvastatin, used once or three times a day (80 mg is used in total). If you choose the format of three meals a day, the ratio is as follows: 20:20:40 mg. In addition, the course is supported by diet and other non-drug methods of improving the quality of the fat profile.
For cardiac ischemia, Simgal is recommended to start taking 20 mg in the evening, increasing the dosage once a month. The maximum daily volume is 40 mg.
A dose adjustment is required in a smaller direction, if LDL on the analyzes is displayed in an amount of 75 mg / dl or more, and total cholesterol - up to 140 mg / dl.
Combination therapy
The maximum permissible dose of Simgal for a day is 10 mg if the patient takes:
- cyclosporins;
- nicotinic acid;
- fibrates;
- danazol.
Twice as many are allowed if the patient is being treated with drugs containing amiodarone, verapamine.
If it is necessary to take bile sequestrants, Simgal is consumed a couple of hours before taking these medicines or four hours after them.
Special conditions and dosage
Simgal based on simvastatin, analogues (20 mg and a different dosage of the active compound) can be used for the treatment of the elderly, provided that vital signs of the functioning of the body are controlled. In this case, the drug is used in the recommended dose for the diagnosis, a specific decrease or increase in volumes is not required.
If kidney failure is found to be in mild, moderate form, the dosage is also not adjusted. In a difficult situation, when creatine clearance is less than 30 ml / min, simvastatin per day should be used in an amount of not more than 10 mg. Therapy requires a regular check with a doctor.
What to replace?
Of the analogues "Simgala" should be noted drugs:
- "Aldesta".
- "Zosta."
- "Simvakard."
The composition of "Symvostat" is distinguished by a good reputation.
Replacement of "Simgal" with analogues is carried out only at consultations with the treating doctor. If it is impossible to purchase the recommended remedy, you first need to find out which formulations will be useful - a lot depends on the individual condition of the patient. Sometimes doctors recommend staying at:
- "Vabadine."
- "Simvakole."
- Zokore.
In general, both Simgal and its analogues, based on simvastatin, have a good reputation and are easily tolerated by patients. Medicines are effective, give a pronounced effect.
Side effects
Most patients do not care about the negative response of the body. Relatively often, against the background of taking the drug, only sleep disturbances are observed. Other negative effects, if they appear, are only in a small percentage of cases, if you follow the instructions and use the drug taking into account indications and contraindications. Among the negative responses of the body, it is worth mentioning allergic reactions and active hair loss, stool disorders, flatulence. The head may hurt, nightmares, dizziness are possible, but all these phenomena are recorded in a vanishingly small percentage of cases. Occasionally, patients develop anemia.
With prolonged use of Simgal, there is a risk of developing interstitial pulmonary disease. Information on such consequences is known, but the likelihood of their occurrence is extremely small. Also, in a small percentage of cases, the patient can get hepatitis, myopathy, myalgia, neuropathy. Blood tests in the laboratory can show an increase in the activity of liver transaminases, an increase in CPK in the blood serum.
Occasionally, patients using Simgal noted increased heart rate, weakened sexual activity, and asthenia. Against the background of rhabdomyolysis, there is a risk of kidney failure in acute form.
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Against the background of rhabdomyolysis, accumulation of excess volumes of potassium in the blood is possible. To correct the patient's condition, calcium chloride or gluconate is injected, an dextrose solution, a short-acting insulin, is infused. In the most severe cases, hemodialysis is indicated.
Compatibility and mutual influence
The simultaneous use of Simgal and cytostatics, fibrates, immunosuppressants can cause myopathy. Similar consequences are possible when combining the described drug and drugs:
- for the treatment of fungal infection;
- containing erythro-, clarithro-, telithromycin;
- inhibitory HIV protease;
- based on nefazodone.
The likelihood of myopathy increases with the combination of Simgal and other compounds that lower the concentration of lipids in the circulatory system. This also applies to the simultaneous use of simvastatin, verapamil, amiodarone, especially in a situation where Simgal is prescribed in a high dosage.
Simgal therapy requires monitoring of blood coagulation quality indicators if the drug is used simultaneously with indirect coagulants, since the likelihood of bleeding increases. Coagulation tests must be done before the start of the course of simvastatin, then repeated during treatment. The frequency will be prescribed by a doctor.
The use of compounds on digoxin and simvastatin leads to an increase in the concentration of the former in the circulatory system. Under the influence of colestipol, colestyramine, the bioavailability of simvastatin is reduced. To prevent this, the time intervals between the use of drugs should be observed: from four hours or more.