Lovastatin

Chemical name

[1S-[1альфа(R*),3альфа,7бет а,8бета [2S * ,4 S *) .8 and �ета]]-2-метилбутановой �islota 1 2,3,7,8,8а-гексагидро-3,7-д��метил-8-[2-(тетрагидро-4 -гидрокси- 6 - оксо-2Н-пиран-2-ил)этил] -1-нафталениловый �fir

Gross

C24-H36-O5

Characteristics

Negigroskopicny white crystalline powder; Nerastvorim water malorastvorim in alcohol.

Of drugs

The drugs-gipolipidemicescoe, гипохолестеринемичес кое. Stops early and intermediate stages of the biosynthesis of cholesterol in the liver. The body is free beta-gidrokshikislotu that competitive ingibiruet 3-гидрокси-3-метилглут��рил-коэнзим A-reduktazu (G-koa-reduktaza), and violates the transformation in the profile mevalonat, as a result of limited synthesis of cholesterol, increasing its catabolised falls plasma level decreases the concentration of engineers containing large quantities of cholesterol. Oppressing synthesis LPONP and triglycerides improves concentration LPVP. It reduces the amount of apoprotein B (part of the engineers), and other components of circulating blood LPONP.V absorbed slowly and incompletely (30% of dose), reception prandial reduces absorption by 30%. C_max achieved in 2 hours, but then the plasma is declining rapidly, at 24 h 10% of the maximum. As lovastatin, and the бета-гидроксикислотн��й metabolite in the sossoudistom with circulating in the blood plasma form (about 95%). Stable equilibrium concentration lovastatina (and its active derivatives), with a 1 per day for the night (cholesterol synthesis in the night) is the day 2-3-i therapy, and 1.5 times higher than the one posed by radiation. Penetrates the GEB and placental barrier accumulate in the liver where oxidized to beta-gidrokshikislota, its 6-oksi derivative etc. metabolites, some of which are still active (block G-koa-reduktazu). 10% displayed product news, 83% - intestinal. Expressed gipolipidemiceski effect develops in 2 weeks, the maximum for a period of 4-6 weeks.

Indications

Giperholesterinemia : primary high certainty (types IIa and IIb), with no effect of diet combined with the гипертриглицеридемие й ( гиперлипопротеинемия �ipa IIb); arteriosclerosis.

Contraindications

Hypersensitivity, violations of the kidney expressed liver failure resilient raising transaminaz in plasma, pregnancy, breast-feeding (at the end of treatment), children's age.

Side-Effects

Violation of the liver, raising transaminaz, neuralgia, flatulence, nausea, vomiting, flatulence, dry mouth, the taste, anorexia, constipation / diarrhea, hepatitis, headaches, muscle pain, myo, rabdomioliz, general weakness, pain in the chest, artralgia, insomnia, parestesia, dizziness, mental disorders, convulsions, muscle nerve membranes, development cataracts, allergic reactions (skin rashes, etc.).

Specific guidance

It may raise levels of CPK and transaminaza (should be considered in differential diagnosis zagrudinnah pain).

Patient interaction

Holestiramin and jelchne acid added effect. Ciclosporin increased plasma levels of active metabolites lovastatina. Fibrata, nioqin, Itraconazole, etc. containing the group azolov, erythromycin or ciclosporin increased risk of miopati, indirect combined (cumarins) bleeding.

Precautions

In patients taking immunosuppressants or severe renal dysfunction dose should not exceed 20 mg / sut. During treatment patients need to be available on a standard diet low in cholesterol. The carefully monitor overall (a muscle pain or weakness, particularly against the backdrop of fever, requires the lovastatina) periodically check cholesterol and the pechenocnae tests.

Dosing and Administration

Inside, at the time of delivery; In the NCEP - 10-20 mg once during dinner; In the farm-20-40 mg. The inefficiency dose increase (at intervals of no less than 4 weeks) to 80 mg in 1-2 reception.

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