Aterostat

General characteristics. Structure:

Active agent: simvastatina 20 mg

Excipients: potato starch, lactose monohydrate, ascorbic acid, butylate hydroxytoluene, citric acid anhydrous, starch prezhelatinizirovanny, magnesium stearate.

Cover: talc, gipromelloza, hydroxypropyl cellulose, titanium dioxide, dye red acid.

Pharmacological properties:

Pharmacodynamics. The hypolipidemic means received in the synthetic way from Aspergillus terreus fermentation product is an inactive lactone, in an organism is exposed to hydrolysis with formation of hydroxyacid derivative. The active metabolite inhibits 3-гидрокси-З-метил-глутарил-КоА-редуктазу (HMG-CoA reductase), the enzyme catalyzing initial reaction of formation of a mevalonat from GMG-KOA. As transformation GMG-KOA in мевалонат represents an early stage of synthesis of cholesterol, use of a simvastatin does not cause accumulation in an organism of potentially toxic sterol. GMG-KOA it is easily metabolized to atsetil-KOA which participates in many processes of synthesis in an organism. Reduces the content of triglycerides (TG), lipoproteids of the low density (LPNP), lipoproteids of very low density (LPONP) and the general cholesterol in a blood plasma (in cases of heterozygous family and single forms of a hypercholesterolemia, at the mixed lipidemia when the increased content of cholesterol is risk factor). Reduces a ratio of LPNP/of lipoproteids of the high density (LPVP) and the general cholesterol / LPVP.
The beginning of action - in 2 weeks from the beginning of reception, the maximum therapeutic effect is reached in 4-6 weeks. Action remains at treatment continuation; at the therapy termination the content of cholesterol is returned to initial level (prior to treatment).

Pharmacokinetics. Absorption of a simvastatin high. After intake the maximum concentration in a blood plasma is reached in 1,3-2,4 hours and decreases by 90% in 12 hours. Communication with proteins of a blood plasma makes 95%.
Simvastatin is metabolized in a liver, has effect of "the first passing" through a liver (it is generally hydrolyzed in the active form beta hydroxyacid, also other active, and also inactive metabolites are found). The elimination half-life of active metabolites makes 1,9 h.
It is removed generally with a fecal masses (60%) in the form of metabolites. About 10-15% are removed by kidneys in an inactive form.

Indications to use:

Primary hypercholesterolemia of IIA and IIb of type (at inefficiency of a dietotherapy at patients in the increased risk of developing of coronary atherosclerosis), the combined hypercholesterolemia and a gipertriglitseridemiya, the giperlipoproteinemiya which is not giving in to correction by a special diet and an exercise stress.
Prevention of a myocardial infarction (for delay of progressing of coronary atherosclerosis), a stroke and passing disturbances of cerebral circulation.

Route of administration and doses:

Pill is taken inside, once, in the evening. At an easy or moderate hypercholesterolemia the initial dose makes 5 mg; at the expressed hypercholesterolemia an initial dose - 10 mg/days; if necessary the dose can be increased not earlier than in 4 weeks, the maximum daily dose - 80 mg.
At coronary heart disease the initial dose makes 20 mg (once, in the evening); in need of it gradually increase every 4 week up to 40 mg. If the maintenance of LPNP less than 75 mg/dl (1,94 mmol/l), and the content of the general cholesterol - less than 140 mg/dl (3,6 mmol/l), a dose of drug it is necessary to reduce.
At patients with a chronic renal failure (clearance of creatinine less than 30 ml/min.) or receiving cyclosporine, fibrata, niacinamide, the initial dose makes 5 mg, the maximum daily dose - 10 mg.
Against the background of immunodepressive therapy the recommended initial dose of 5 mg a day, the maximum daily dose makes 5 mg a day.
In case of the admission of the current dose drug needs to be accepted as soon as possible. If came time of the following dose, a dose not to double.

Features of use:

Before an initiation of treatment it is necessary to conduct a research of function of a liver (to control activity of "hepatic" transaminases each 6 weeks within the first 3 months, then each 8 weeks within the remained first year, and then 1 time in half a year).
To the patients receiving Aterostat in a daily dose of 80 mg, function of a liver is controlled 1 time in 3 months. When activity of "hepatic" transaminases increases (exceeding by 3 times of the upper bound of norm), treatment is cancelled.
At patients with a mialgiya, a myasthenia and/or the expressed increase in activity of KFK treatment with drug is stopped.
Aterostat (as well as other inhibitors of GMG-KOA-reduktazy) should not be applied at the increased risk of emergence of a rabdomioliz and a renal failure (owing to a heavy acute infection, arterial hypotension, big surgery, injuries, heavy metabolic disturbances).
Cancellation of hypolipidemic means during pregnancy has no significant effect on results of prolonged treatment of primary hypercholesterolemia.
Because inhibitors of GMG-KOA-reduktazy slow down cholesterol synthesis, and cholesterol and other products of its synthesis play an essential role in fetation, including synthesis of steroids and cellular membranes, симвастатин can make an adverse effect on a fruit at appointment to his pregnant women (women of reproductive age have to avoid conception). If in the course of treatment there is pregnancy, drug has to be cancelled, and the woman is warned about possible danger to a fruit.
Aterostat is not shown when there is a gipertriglitseridemiya I, IV and V types.
Drug is effective both in the form of monotherapy, and in combination with sekvestrant of bile acids.
Prior to the beginning of and during a course of treatment the patient has to be on a hypocholesteric diet.
To patients with a heavy renal failure treatment is carried out under control of function of kidneys.
Patients is recommended to report immediately about inexplicable muscle pains, slackness or weakness, especially if it is followed by an indisposition or fever.

Side effects:

From the alimentary system: dyspepsia (nausea, vomiting, gastralgia, abdominal pains, lock or diarrhea, meteorism), hepatitis, jaundice, increase in activity of "hepatic" transaminases, alkaline phosphotazy and kreatininfosfokinaza (KFK); seldom - acute pancreatitis.
From a nervous system and sense bodys: asthenic syndrome, dizziness, headache, sleeplessness, spasms, paresthesias, peripheral neuropathy, sight vagueness, disturbance of flavoring feelings.
From a musculoskeletal system: myopathy, mialgiya, muscular weakness; seldom - рабдомиолиз.
Allergic and immunopathological reactions: a Quincke's disease, a volchanochnopodobny syndrome, a rheumatic polimialgiya, a vasculitis, thrombocytopenia, an eosinophilia, increase SOE, arthritis, an arthralgia, a small tortoiseshell, a photosensitization, fever, a dermahemia, "inflows" of blood to face skin, an asthma.
Dermatological reactions: skin rash, itch, alopecia.
Others: anemia, heartbeat, an acute renal failure (owing to a rabdomioliz), decrease in a potentiality.

Interaction with other medicines:

Strengthens effect of indirect anticoagulants and increases risk of developing of bleedings.
Cytostatics, antifungal drugs (кетоконазол, интраконазол), fibrata, high doses of niacin, immunodepressants, erythromycin, кларитромицин, inhibitors of proteases increase risk of development of a rabdomioliz.
Simvastatin promotes increase concentration of digoxin in a blood plasma.
Colestyraminum and колестипол reduce bioavailability (Aterostat's use is possible in 4 hours after reception of the specified drugs, at the same time the additive effect is noted).

Contraindications:

Hypersensitivity to drug components, hypersensitivity to other drugs of a statinovy row (HMG-CoA reductase inhibitors) in the anamnesis, a liver failure, acute diseases of a liver, increase in activity of "hepatic" transaminases of not clear genesis; pregnancy; the lactation period, age up to 18 years (safety and efficiency of use are not established).
With care appoint the patient who is abusing alcohol and/or having in the anamnesis of a disease of a liver; to patients after organ transplantation which carries out therapy by immunodepressants (in connection with the increased risk of emergence of a rabdomioliz and a renal failure); at states which can lead to development of the expressed insufficiency of function of kidneys, such as: arterial hypotension, acute infectious diseases of a heavy current, the expressed metabolic and endocrine disturbances, disturbances of water and electrolytic balance, surgical interventions (including dental) or injuries; to patients with the lowered or raised tone of skeletal muscles of not clear etiology; at epilepsy.

Overdose:

Treatment: at overdose it is necessary to cause vomiting, to accept absorbent carbon, symptomatic therapy. It is necessary to control functions of a liver and kidneys, concentration of KFK in blood serum.

Storage conditions:

List B. In the dry place at a temperature not above 30 °C.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 20 mg. On 10 tablets in a blister strip packaging. On 30 tablets in bank polymeric or a bottle polymeric. 1, 2, 3, 4 or 5 blister strip packagings, to one bank or one bottle together with the application instruction place in a cardboard pack.