Fluvastatin

Chemical name

[R*,S*-(E)]-({+})-7-[3-(4-Фторфен ил)-1-(1-метилэтил)-1H-инд ол-2-ил]-3,5- �игидрокси-6-гептенова я acid (as sodium salt)

Gross

C24-H26-F-N-O4

Characteristics

White or light gigroskopicny powder. Rat in the water, ethanol, methanol.

Of drugs

The drugs - гипохолестеринемичес кое. Competitive ingibiruet 3-гидрокси-метилглута��ил-коэнзим A (CoA) -reduktazu, turning blocks profile in mevalonat predecessor sterols (including cholesterol). Absorbed quickly and completely (98%), eating slows induction. Metabolised in the liver, incl. in the "first pass" through the liver; absolute bioavailability 24%, the volume of 34.4 litres, more than 98% of circulating drug binds to plasma proteins, regardless of the concentration. Key components circulating in the blood, fluvastatin and pharmacologically active metabolite N-dezizopropilnoe derivative; Gidrauxilirovanne metabolites have pharmacological activity, but did not enter the blood system; Excretion of 6% of the urine, 93% from faeces, and only 2% is allocated in an unmodified form. Plasma Cl-1.8 l / min; When administered orally 40 mg T_1/2 is 2.3 C.podavlet cholesterol biosynthesis reduces cholesterol in the liver cells, which stimulates previously oppressed vnutricletocnam hate fusion receptors to the engineers, and thus increases the taking of circulating particles engineers and their predecessors LPONP because receptors recognize apoprotein B and E, which are present in both lipoproteinah; the end result is to reduce the concentration of plasma cholesterol-friendly (in terms of reducing haemoglobin) changes density ratios and membrane transport proteins. The lower cholesterol reasonable depends on the dosage : 5 mg, 15%, 40 mg, 24%; In the admission once a day at night гипохолестеринемичес кий the effect is twice as high as in the admission of the morning because zircadnami jazz fusion cholesterol; effect of the same drugs as in patients with poligenna giperholesterinemiei, and the family heterozygous; �ипохолестеринемичес��ий effect is more evident in patients with higher levels of cholesterol; not efficient at giperlipoproteidemy V design, in which levels of cholesterol claimed not upgraded; dozozawisimo increased cholesterol LPVP (at 2.5-8%), reduces triglycerides (at 8-10,5%); reduces the haemoglobin by reducing apoprotein B and the apoprotein AI; initial therapeutic response develops within four weeks, rising to 12 weeks and continues with its long-term use; despite the decline in the total cholesterol in the cells retained enough cholesterol to ensure the smooth functioning; it is likely cumulation fluvastatina in patients with liver failure.

Indications

Primary gipoholesterinemia (with the exception of family gomozigotna), mostly IIA and IIb (with the poor diet for three to six months).

Restrictions on the use of

Increased concentration in the blood liver transaminaz and CPK ambiguous genesis, diffuse mialgii, increasing or reducing muscle spasms unknown genesis, severe kidney failure, liver disease, alcohol abuse, pregnancy, breast-feeding (a non-breast-feeding), Children and Youth age (up to 18 years).

Contraindications

Hypersensitivity, acute pathological processes in the liver.

Side-Effects

Diarrhoeal phenomenon, nausea, insomnia, pain in the abdomen, bloating, headache, dental pain, gipestesia, increasing transaminaz, myo.

Patient interaction

Effect beta-blokatora increase; Risk of myo increase ciclosporin and other immunosuppressants gemfibrosil, nikotinova acid, erythromycin; Bioavailability reduces rifampicin (50%) increase, zimetidin, or ranitidine omeprazol.

Precautions

Before and during the treatment process should be followed гипохолестеринемичес кой diet, the level of liver transaminaz (the increase is more than three times longer reception); periodically to explore fat profile, and according to the cholesterol engineers adjust dose; Appointment of women of childbearing age is contingent on the use of appropriate contraceptive methods. In conjunction with ion-exchange resins fluvastatin should appoint (at night) is not less than four hours after taking the drugs.

Dosing and Administration

Inside, beginning with the dose 5 mg / day evening, every two weeks dose can be gradually increased to 20 mg once a day, and then to 20 mg twice a day or 40 mg once a day evening; with very high levels of cholesterol dose may be increased to 40 mg twice a day.

Literature

Yuan J., Y. Tsai, J. Hegland et al. Effects of fluvastatin (XU 62-320), an HMG-CoA reductase inhibitor, on the distribution and composition of low density lipoprotein subspecies in humans / / Atherosclerosis 1991 .- .- V. 87 N .- 2.3 .- P. 147-157.

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