Simvastatin

Chemical name

1,2,3,7,8,8a-Гексагидро-3,7-д иметил-8-[2-(тетрагидро- 4-гидрокси-6-оксо-2Н-пир ан- 2-ил)этил]-1-нафталенил- 2,2-диметилбутаноат

Gross

C25-H38-O5

Characteristics

White or no white crystalline powder. Virtually nerastvorim in water, it is readily soluble in chloroform, methanol and ethanol.

Of drugs

The drugs - гипохолестеринемичес кое. In oral hydrolyses education metabolita active, inhibition 3-гидрокси-3-метил-глют арил-КоА-редуктазу (Sunset catalyzes a719 the synthesis stage cholesterol). Decreases as high or normal cholesterol, the concentration of engineers and LPONP. Thus the ratio LPVP and engineers and reducyruetsa-cholesterol / LPVP. Increases LPVP content and reduces the concentration of triglycerides. In the absence of inheritance finds receptors (gomozigotnaya family giperholesterinemia) simwastatin ineffective. A reliable clinical result is two weeks after the start of treatment, and the maximum is four to six weeks. Long received 20-40 mg / day increases the survival of patients with giperholesterinemiei disease and reduces the progression ateroskleroticski defeat of the coronary arteries. Active in the poor diet, etc. nemedikamentozhnykh methods Lechenia.posle oral the concentration simwastatina and its metabolites (formed mainly in the liver) is the maximum through 6700, and decreased by 90% after 12 hours As simwastatin, and the products of biotransformation plasma 95% related to the protein. Гипохолестеринемичес кую activity remained 6'-gidroksi-, 6'-gidroximetil- 6'-exometilenove and derivatives. Place in the form of metabolites with jelchew (60%) and urine (13%).

Indications

Giperholesterinemia, in the absence of the effect of diet combined giperholesterinemia and triglitzeridemia, ischemic heart disease, prevention of myocardial infarction and stroke, arteriosclerosis.

Contraindications

Hypersensitivity, acute failure of the liver, severe kidney failure, pregnancy, breast-feeding (for the period of treatment stop breastfeeding), children's age.

Side-Effects

Diarrhoeal phenomenon, diarrhoea, flatulence, nausea, exacerbation of pancreatitis and hepatitis, raising transaminaz, disorders of the central nervous system (headache, parestesia, convulsions), mialgia, fatigue, miopatia, rabdomioliz, photosensitization, allergic reaction (vasculit, urticaria, arthralgia, thrombocytopenia, eozinofilia, angioneuroticeski swelling, symptoms similar to the red Lupus).

Patient interaction

Immunodepressus therapy, high doses of nicotinic acid, antifungals-derivatives azola (ketokonazol, Itraconazole) increase the risk of myo-and rabdomioliza. Do indirect effects anticoagulants, gepatotoksicnosti alcohol and drugs have on the liver.

Precautions

Before and during treatment to monitor liver function and carefully appointed with its violations.

Dosing and Administration

Inside : at the beginning of the course in one dose of 5-10 mg / day, if necessary up to 40 mg / day, depending on the content of cholesterol and LDL in the blood. In IBS initial dose of 20 mg / day once.

Directory → Metaboliki → Lipid means → Statins → Simvastatin