Recently, more and more often doctors recommend that patients suffering from an increased concentration of cholesterol in the body take (of course, following the instructions) Simvastatin. At a relatively low price, the drug has a wide spectrum of effectiveness and a relatively narrow list of side effects. However, they should not practice self-medication - this can lead to the most undesirable consequences and harm to health.
general information
The drug "Simvastatin" is produced by several enterprises, both domestic and foreign. The cost of one package is from 40 rubles and more. Mostly, the goods of Russian manufacturers are somewhat cheaper, but those manufactured, for example, in the Czech Republic, will cost customers more expensive. "Simvastatin" belongs to the class of lipid-lowering drugs that can inhibit the activity of HMG-CoA reductase.
All manufacturers in the instructions for "Simvastatin" describe how the product looks. The medication is made in tablet form. Each specimen is round, convex on both sides, painted in different shades of yellow, and inside is filled with white matter. There are several dosage formats for the active ingredient: 10, 20, 40 mg. Manufacturers pack tablets in blisters or cans of polymers, usually opaque or dark. Simvastatin can also be stored in a glass jar.
The cardboard box contains instructions for "Simvastatin" and one can of tablets or several blisters. The specific number of doses, the content of the active compound must be indicated by the manufacturer on the outside of the pack. The buyer can see this information before settlement with the cashier in the pharmacy. The packaging also indicates the name of the manufacturer, the expiration date of the product and the rules for its dispensing. "Simvastatin" is sold strictly according to the prescription of the attending doctor. The document must be executed in the established manner, confirmed by the signature and seal of the doctor.
What is inside?
The instructions for "Simvastatin" indicate that one tablet contains an active compound, the name of which gave the name of the drug - this is simvastatin. The exact amount of this substance for one tablet is indicated on the package of the drug, bottle and blisters. The manufacturer also used auxiliary components that simplify the administration of the medication and increase its effectiveness. A complete list of substances must be studied by persons suffering from intolerance to any compounds used in the pharmaceutical industry. The current list for a specific release option can be found in the instructions for use of Simvastatin. Commonly used:
- lactose;
- starches;
- citric and ascorbic acid;
- cellulose;
- talc;
- magnesium stearate;
- aerosil;
- macrogol;
- alcohol;
- coloring matter.
Pharmacological Nuances
The tool belongs to the class of lipid-lowering. The starting material for its manufacture is aspergillus, processed using specific enzymes. The finished product of synthetic origin is inactive lactone. The instructions for use of "Simvastatin" indicate: only once in the body, the substance is soon subjected to processing (hydrolysis). This reaction leads to the formation of a specific metabolite showing pharmacological activity.
The product of simvastatin hydrolysis inhibits the activity of HMG-CoA reductase, which means that the substance initiating the formation of mevalonate is lost, that is, it is possible to control the early synthesis of cholesterol. In the instructions for use of "Simvastatin", the manufacturer draws attention to the specific effect of the compound on chemical reactions - despite the decrease in cholesterol production, the use of the medication does not provoke the accumulation of sterols, which can potentially poison a person.
HMG-CoA, not participating in the formation of cholesterol, is converted to acetyl-CoA, that is, a substance involved in a wide variety of biochemical reactions.
Features of the medication
Instructions for use of "Simvastatin" states that under the influence of the active compound, reactions that allow to obtain cholesterol are deactivated (these processes must occur in the liver). At the same time, the appearance of numerous receptors that are sensitive to low-density fatty structures (LDL) is stimulated, that is, the capture of these elements, their catabolism, is activated. Studies have shown that this leads to a decrease in the circulatory system of triglycerides, low-density fat structures, very low-density, as well as total cholesterol.
Clinical observations prove that with the proper use of Simvastatin, the relative rates of high-density lipoproteins increase. The active compound does not provoke gene mutations.
In the instructions for "Simvastatin" (20 mg and other dosage forms), the manufacturer indicates that the therapeutic effect can be observed by the end of the second week of taking the drug. The highest performance of the course can be seen on day 28-42 of the program. This effect persists for a long time while the patient is taking the drug. At the end of the program, indicators gradually return to their original values.
Kinetics of the drug
The instruction for tablets "Simvastatin" states that the absorption of the active compound is close to 100%. The maximum concentration in the circulatory system is achievable after 1.3-2.4 hours. After 12 hours, the plasma component of the blood of simvastatin becomes 90% less. Bioavailability is estimated at less than 5%, and the ability to communicate with plasma proteins reaches 95%.
The manufacturer in the instructions for use "Simvastatin" 40 mg, 10 and 20 mg indicates that the drug entering the body is a supplier of an inactive substance that undergoes hydrolysis in the tissues of the body. The reaction product is beta hydroxy acid. In addition, specific metabolites are formed that do not have a pharmacological effect.
The metabolic processes are localized mainly in the liver, proceed with the involvement of several isoenzymes. The half-life is estimated at 1.9 hours for the active reaction products. The instructions for use of Simvastatin (20 mg and other release options) indicate that 60% of the total amount is excreted through the intestinal tract, up to 15% - by the kidneys. These facts must be taken into account when prescribing the drug to people suffering from a lack of functionality and chronic diseases of different systems and organs.
When will it help?
According to the instructions, the medicine “Simvastatin” is indicated for different types of hypercholesterolemia (2a, 2b, mixed form), hereditary and not such, heterozygous, unless diet and other non-drug approaches are sufficient to control cholesterol in the patient’s blood.
Some are interested in what pressure "Simvastatin" should be taken according to the instructions for use. The drug does not help from high or low blood pressure, but is effective if a person has suffered a heart attack, the heart suffers from ischemia, as it prevents the recurrence of this situation.
"Simvastatin" is indicated if necessary to lose weight, if the diet, physical activity and other similar methods do not show a pronounced effect. Medication is allowed only if the likelihood of coronary atherosclerosis is estimated to be above average.
The instructions for use of "Simvastatin" (10 mg, 20 mg, 40 mg) indicate the effectiveness of using the drug with a combination of hypertriglyceridemia, hypercholesterolemia, if it is not possible to adjust the patient's condition with non-drug approaches, diet, loads.
"Simvastatin" allows you to reduce the rate of progress of atherosclerosis of coronary blood vessels, reduces the likelihood of disruption of the heart and blood vessels.
Strongly impossible!
Instructions for use of the pill "Simvastatin" are prohibited for people suffering from liver diseases in the acute phase, as well as persistent increased activity of liver transaminases when it is impossible to identify the cause of this fact. You can not use the drug for diseases of the muscular tissue of the skeleton, including myopathy.
The instructions for use of tablets "Simvastatin" indicate which substances used in the pharmaceutical industry, the tool can not be combined:
- ketoconazole;
- itraconazole;
- clarithro-, telitro-, erythromycin;
- nefazodone;
- all inhibitory isoenzyme CYP3A4 substances;
- inhibitory HIV protease compounds.
Contraindications for taking the drug include:
- lack of lactase;
- glucose-galactose malabsorption syndrome;
- bearing a child;
- lactation;
- minor age;
- hypersensitivity to statin drugs in the past;
- intolerance to any compounds used by the manufacturer in the manufacture of "Simvastatin".
Special occasion
If there is evidence for this, the instructions for use "Simvastatin" is allowed for people suffering from alcohol addiction. The use of the medication is possible only if it is possible to establish control over the patient's condition. Patients also deserve special attention if the medical history includes:
- impaired renal function;
- liver disease
- severe renal failure (creatinine clearance less than 30 ml / min);
- uncontrollable epilepsy;
- violation of the balance of water, severe electrolytes;
- low blood pressure;
- pronounced metabolic disorders, the functioning of the endocrine system;
- myopathy
- severe acute infectious diseases;
- necrosis of the muscles of the skeleton in acute form;
- major surgery, injury.
The use of fibrates imposes certain restrictions, but the drug in question is allowed if there are obvious indications for this. Instructions for use "Simvastatin" indicates that an exceptional case is the use of fenofibrate.
"Simvastatin" under the supervision of a doctor can be used in combination with grapefruit juice, verapamil, cyclosporine, nicotinic acid in an amount of a gram or more per day. "Simvastatin" is allowed for patients over 65 years of age, but only if it is possible to control the vital functions of the body. The same restrictions apply to combinations with:
Admission Rules
Like all simvastatin-based analogues, Simvastatin (instructions for use draws attention to this) is effective only if you adhere to a special diet during treatment, minimizing the intake of cholesterol. Strict restrictions apply to the entire therapeutic course.
"Simvastatin" is intended for oral administration. It is necessary to wash the capsule with water. No meals required. The duration of treatment and dosage are determined by the doctor, based on the characteristics of the diagnosis, the condition of the patient, individual specific requirements for the course.
With hypercholesterolemia, "Simvastatin" is prescribed in an amount of 5-80 mg per day. Usually start with 10 mg, use them for food at a time. It is recommended to take a pill in the evening. Duration of admission is four weeks. As a result, a blood test is done for the content of various fatty structures and a decision is made to lower or increase the dosage. In most cases, a dose of 20 mg is sufficient. According to similar rules, the drug "Simvastatin Alkaloid" is used. The instructions for it and the usual "Simvastatin" are extremely similar, since the active component is the same.
If the medication is taken in an amount of 40 g, but the clinical effect is not observed, it is reasonable to change the tool. As follows from the instructions for use, "Simvastatin Alkaloid", "Simvastatin", when used in a dosage above this, are highly likely to provoke myopathy.
80 mg of the active ingredient can be used if half the volumes do not allow to achieve a specific goal (LDL indicators).
Diagnoses and Doses
If familial hypercholesterolemia from the homozygous category is detected, then the instructions for use "Simvastatin Alkaloid", "Simvastatin" are recommended in an amount of 40 mg. The entire dose is used at a time, shortly before going to bed. If this amount is not enough, you can double the volumes taken, dividing them into three stages: 20 mg in the morning, the same amount in the afternoon and twice as much - before bedtime. To maximize the effectiveness of the course, the medication is combined with LDL apheresis, other methods and means of lowering the concentration of fat fractions in the circulatory system.
If ischemia is detected, Simvastatin can be used in case of hyperlipidemia, and in the absence of such a diagnosis. Admission rules are prescribed in the instructions for use. In reviews, "Simvastatin" is usually presented as a means of showing a pronounced effect even in a small dose, although therapy begins with 20 mg daily in the evening. If in a particular case this does not give the desired result, the volume used by the patient is doubled.
Both the reviews and the instructions for use of "Simvastatin" contain a mention of the need to withstand four weeks between dosage changes. It is possible to reduce the volumes consumed by the patient if low-density fatty structures are detected in an amount of less than 75 mg / dl. Indicators of total cholesterol, showing that it is possible to reduce the dose - 140 mg / dl and below.
Dosage and compatibility
If the patient is prescribed nicotinic acid, the patient undergoes a course of drugs, which contain cyclosporine, danazole, gemfibrozil, some other compounds, the maximum dose of simvastatin per day is 10 mg. To prevent the negative effects of treatment, you should inform the doctor about all the medicines that the patient uses. The doctor will adjust the dosage based on this information.
If the patient is prescribed diltiazem, "Simvastatin" for a day is allowed in an amount of up to 40 mg.
In combination with verapamil, amiodarone, the maximum daily dosage is 20 mg.
As noted in the reviews, the instruction of “Simvastatin” (quite understandable and detailed) contains indications of a specific approach to taking the drug by people who have established insufficient kidney function in expressed form. For moderate or mild impairment, volume adjustment is not required. It is not necessary to reduce the dose based on the old age of the patient. With creatinine clearance of less than 30 ml per minute, Simvastatin is prescribed in an amount of 10 mg per day. If this volume does not show the desired effect and requires a dosage increase, adjustment is allowed only if possible to monitor the patient's condition.
Negative consequences
Both the reviews and the instructions for “Simvastatin” contain references to the possibility of adverse reactions when taking the drug. Most often, sleep disturbances are noted. Some patients have headaches and dizziness. Simvastatin may cause:
- general weakness;
- asthenia;
- myasthenia gravis;
- neuropathy;
- disturbances in the perception of taste, visual image;
- stool disorders;
- pain in the stomach;
- nausea and vomiting
- increased gas formation;
- skin allergic reactions;
- hypersensitivity, expressed by various manifestations;
- activation of liver transaminases ;
- myopathy
- myalgia;
- shortness of breath
- arthritis;
- arthralgia;
- hypersensitivity to light;
- kidney failure in acute form.
Some noted violations of the frequency, heart rate, and a decrease in potency while taking Simvastatin. In the instructions, the manufacturer gives a complete list of all possible negative reactions. The doctor also introduces them, writing out the composition to the patient. The doctor immediately introduces the course of how to behave, if the body reacts negatively to tablets, in which case you need to stop taking it, and when - reduce the dose or leave it unattended, take measures to stop unpleasant manifestations.
Too much!
It is quite difficult to notice an overdose, since there are no specific symptoms indicating this. Studies were carried out using up to 450 mg of food, while it was not possible to identify any special manifestations. The active component of the medication does not have an antidote. If it is revealed that the drug was taken in too much volume, it is necessary to rinse the stomach, provoke vomiting. These measures are effective in the near future after using the drug, while it has not yet been absorbed. The patient is shown activated charcoal, taking laxatives.
Based on what symptoms an overdose provokes, therapy is prescribed for their relief. Additionally, they put the patient under control by regularly checking the functioning of the liver and kidneys. In blood serum, indicators of creatine phosphokinase are checked, and general measures are prescribed at the discretion of the doctor in order to adjust and maintain the functionality of the body.
If an overdose has caused myopathy, rhabdomyolysis, kidney failure in the acute form, sodium bicarbonate and diuretics should be dripped into a vein. If elevated potassium levels are detected, calcium chloride or gluconate should be used in the vein. There is a patient’s condition is very serious, hemodialysis is prescribed.
Application Nuances
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If the patient "Simvastatin" is prescribed in the amount of 80 mg per day, a liver function test is done every three months. If the activity of liver enzymes exceeds the norm threefold, while the nature of the changes is assessed as persistent, the medication should be discontinued.
The likelihood of rhabdomyolysis, liver failure in the acute form is higher if Simvastatin is used against the background of:
- acute infectious diseases;
- low blood pressure;
- severe metabolic disorders;
- injuries
- major operations.
If high cholesterol is accompanied by hypothyroidism, renal pathologies, you must first take measures to eliminate the underlying disease, only then start therapy to normalize cholesterol levels in the blood (if it will still be necessary).
The use of "Simvastatin" is always accompanied by the likelihood of myopathy, which, in turn, can cause rhabdomyolysis, kidney failure in acute form. To a greater extent, this risk is exposed to persons already suffering from renal failure, especially in severe form, as well as patients undergoing fibrates, macrolides, and some other medications.
It is believed that the risk of myopathy is increased in women, patients older than 65 years of age and those who have established hypothyroidism that is not amenable to correction. When prescribing the course, the doctor explains to the patient what the primary signs of myopathy are, indicates the need for an urgent visit to the clinic, if he is worried about a fever, pain, muscle weakness.
Course Features
There is a higher chance of side effects if the patient consumes grapefruit juice while taking Simvastatin.
The tablets described should not be used if hypertriglyceridemia of the first, fourth or fifth type is established.
In order to identify myopathy in time, it is important to constantly undergo examinations to identify the parameters of creatine phosphokinase in the blood serum. If the values are higher than normal ten times or more, the medication is canceled.
As tests have shown, "Simvastatin" is effective both as a primary treatment and as an auxiliary if the patient uses sequestrants of bile acids.
If the patient accidentally missed the next appointment, you need to immediately compensate for the missed, as soon as the fact was noticed. If it was possible to notice a pass only a day after the set time, use a single dosage (two doses are prohibited at the same time).
What to replace: analogues
The instruction to "Simvastatin" indicates that the active component of the drug is simvastatin. When choosing analogues, medications based on the same compound are primarily studied. Currently in demand are:
The medicines Avenkor and Actalipid have a good reputation. Sometimes doctors recommend, if it is not possible to purchase the prescribed drug, to stop using Sinkard, Aterostat.
The choice of analogue must be agreed with the attending doctor. Self-replacement can cause course inefficiency, a source of harm to the patient.