Simwastol

Roman name

Simvastol

Characteristics

Gipolipidemicescoe vehicle produced by synthetic product of the fermentation Aspergillus terreus.

Pharmacokinetics

Absorption simwastatina high. Once inside C_max achieved through 1,2-2,4 h is reduced by 90% after 12 hours Relationship with blood plasma proteins is 95%. Simwastatin metabolised in the liver, has the effect <pervogo prokhojdenia> through the liver (mainly hydrolyses in its active form beta-gidrokshikislotu found and the other active and inactive metabolites). T_1/2 active metabolites is 1.9 C.v largely withdrawn from the masses urine (60%) in the form of metabolites. About 10-15% of output in the memory inactive form.

Farmakodinamika

Simwastatin reduces the triglycerides engineers, and LPONP total cholesterol in the plasma (in cases heterozygous family and nesemeina of NCEP, with a mixed Moyle when elevated cholesterol is a risk factor). Increases LPVP content and reduces the ratio of engineers / LPVP and total cholesterol. The effect of in 2 weeks from the beginning of the reception, the maximum therapeutic effect was achieved through the 4-6 weeks. The remains for continuing treatment : with a therapy cholesterol gradually returning to the original (pre-treatment) level.

Indications

Primary giperholesterinemia IIa and IIb type (with inefficiency nutrition in patients with increased risk of coronary atherosclerosis), combined giperholesterinemia and gipertriglitzeridemia, hyperlipoproteinemy not easily correction special diet and physical нагрузкой.Профилакти��а myocardial infarction (to slow progression of coronary atherosclerosis), stroke and transient disturbance of cerebral circulation.

Contraindications

Hypersensitivity to the drug component, increased sensitivity to other drugs statinovogo stimulants (inhibitors G-koa-reduktaza) in the disease, liver failure, acute liver disease, the increase in the liver transaminaz ambiguous genesis, pregnancy, lactation period, before age 18 years (the safety and effectiveness of the unknown). Be wary appoint sick, misuse of alcohol and / or have a history of liver disease; patients after organ transplantation, which the therapy immunosupressantami (as a result of the heightened risk of rabdomioliza and kidney failure); for conditions that could lead to failure expressed by the kidneys, such as : arterial hypertension, acute infectious diseases heavy currents expressed metabolic and endocrine disruption, violations �одно-электролитическ ого balance, surgery (including dental), or injury; patients with low or high tone skeletal muscles unclear etiology; with epilepsy.

Specific guidance

Before treatment to a study of the liver (monitor activity transaminaz liver every six weeks for the first 3 months, then every 8 weeks for the remainder of the first year and then every 6 months). Patients receiving Simwastol in daily dose of 80 mg, liver function monitored every three months. In cases where the transaminaz growing (over 3 times the upper limit of the rules) and the treatment of Otmenaut.u patients with mialgiei, myasthenia and / or expressed growing activism CPK drug treatment Prekrashchaut.simwastol (like other inhibitors G-koa-reduktaza) should not be applied to the increased risk of rabdomioliza and renal failure (in the face of severe acute infection, arterial hypotension planned surgery, trauma, severe metabolic disturbance). The removal of lipid during pregnancy does not have a significant impact on the long-term treatment of primary �иперхолестеринемии.В �back to the fact that inhibitors G-koa-reduktaza down cholesterol synthesis and cholesterol and other products of his house to play an essential role in fetal development, including synthesis of steroids and cell membranes, simwastatin can have adverse effects on fruit in the appointment of his pregnant women (women of reproductive age at the time of treatment should avoid conception). If the treatment is pregnancy, the drug must be cancelled and the woman warned of the possible danger to Ploda.simwastol not shown when there is gipertriglitzeridemia I, IV and V Tipov.preparat effective in the form alone, or in combination with biliary sekwestrantami acids. Before and during the course of treatment the patient should be gipoholesterinova diet. If this passes doses, the drug should be taken as soon as possible. If it is time to receive the next dose, double dose should be avoided. Patients with severe renal failure treatment are under the control of the kidney. Patients should immediately report unexplained pain in the muscles, weakness or weakness, particularly if accompanied by malaise or fever.

Patient interaction

Do the anti proximity and increases the risk of hemorrhage. Cytostatics, antifungals (ketokonazol, Itraconazole) fibrata, high doses of nicotinic acid, immunosuppressants erythromycin, klaritromicin, protease inhibitors increase the risk of developing рабдомиолиза.Симваст��тин enhances digoxin concentration in plasma Krovi.kolestiramin and colestipol reduce bioavailability (application simwastatina possibly through 6700 after taking the drugs), but with a joint appointment was an additive effect.

Overdosing

In overdose should cause vomiting, the activated carbon. Treatment-symptomatic. The control function of liver and kidney CPK levels in the serum.

Dosing and Administration

Take pills inwards one evening. In light or moderate NCEP initial dose of 5 mg; In the NCEP expressed in a dose of 10 mg / day; If necessary dose can be increased at least four weeks. The maximum daily dose of 80 mg. In IBS initial dose is 20 mg (one evening); With the need to gradually increase every four weeks to 40 mg. If the claimed less than 75 mg / m (1.94 mmol / l), and the total cholesterol is less than 140 mg / m (3.6 mmol / l), dose of the drug needs to be narrowed. In patients with chronic renal insufficiency (creatinine klirens less than 30 ml / min), or receiving ciclosporin, fibrata, nicotinamide initial dose of 5 mg maximum daily dose of 10 mg. While immunodepressivna therapy recommended initial dose of 5 mg / day with a maximum daily dose of 5 mg per day.

Storage conditions

List B. The temperature is not above 30 ° C

Shelf life

The registration

015147/01

The drug forms

Simwastatin 10 mg-pink tablets, coated film-coated, round, flat, with full points. At level two visible layer, the nucleus uniformly white with a thin red coating on Krau.simwastatin 20 mg-yellow tablets, coated film-coated, round, flat, with full points. At level two visible layer, the nucleus uniformly white, with a thin yellow coating on the edge.

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