Mycophenolate mofetil

Chemical name

Морфолиноэтил(Е)-6-(4-ги дрокси-6-метокси-7-мети л-3-оксо-5-фталанил)-4- metil-4-gexenoat

Gross

C23-H31-N-O7

Characteristics

White or no white crystalline powder Low in the water (solubility increases if zakislenia environment), soluble in methanol, partially soluble in ethanol, well, in acetone.

Of drugs

The drugs-immunodepressivne. Yes ingibiruet инозинмонофосфатдеги дрогеназу and inhibits fusion guanosin nukletoida de novo. Provides zitostaticski pronounced effect on the blood, strangling them proliferatiou in response to mitogennouu or allospecificescuu stimulation. Oppressing education B-limfozitami antibodies. Prevents glikozilirovanie limfocitarnah and monocitarnah glikoproteinov involved in the dopamine with endoteliem, and reduces the migration of lymphocytes in the pockets of inflammation and transplant rejection, blocking mononuklearov impact on the synthesis of DNA and Proliferatiou.pri ingestion rapidly absorbed and fully presistemno hydrolyses, forming mikofenolovu acid (the active metabolite). Absolute bioavailability of a 94% (plasma little detected mofetila mycophenolate). Time to C_max (24.5 µ g / ml) is 0.8-0.9 hours In the early stages (the first 40 days after kidney allotransplantation) C_max and time reaching about 50%. Mikofenolovaya acid 97% linked to albuminom plasma. Average distribution 3,6-4,0 l / kg The tissues become glukuronid (contact albuminom-82%). The high concentration of plasma glukuronida possible competition for places bonding with the squirrels. After 12 h in the blood by the second peak due enterogepaticescoy circulation. T_1/2 was 17.9 h, plasma Cl-193 ml / min. Kidneys displayed about 87% imposed dose intestinal 6%. Экскретируется главным образом глюкуронид, в моче обнаруживаются еще 3 метаболита и менее 1% микофеноловой кислоты.В сочетании с азатиоприном и циклоспорином, а также с индукционным курсом антитимоцитарного глобулина уменьшает частоту неблагоприятных исходов в первые 6 мес после трансплантации.

Indications

Preventing rejection reactions, and treatment exclusion allogennogo kidney transplant (in conjunction with ziklosporinom A and glukokortikoidami).

Contraindications

Hypersensitivity, increased ulcers stomach and duodenal ulcers and other stomach diseases, pregnancy, breast-feeding (breast-feeding at the time of treatment out), child.

Side-Effects

Nausea, vomiting, diarrhea, constipation, or lakopenia leucocytosis, anemia, thrombocytopenia, and an increase in the frequency of infections and septic complications; Headaches, insomnia, tremor, fever, fatigue, lumbago, hypertension, cough, pharyngitis, dizziness, peripheral oedema, rotoglotocny candidiasis, gematuria, ka 15f8 naltsevy necrosis, impotence, acne, hyper or gipokaliemia, giperglikemia, gipofosfatemia, giperholesterinemia, allergic reactions, skin rashes, itchy skin.

Patient interaction

Probenecid and other drugs affecting the secretion kanalzevu increase plasma concentration mikofenolova acid. Antatsida containing magnesium hydroxide and aluminium reduce removals. Lexredstwa altering flora tract may violate enterogepaticescuu circulation. Impact on the oral contraceptive. Azathioprine increases the risk of cancer, especially skin.

Overdosing

Symptoms : an increase in the frequency of gastrointestinal and haematological (particularly neutropenia) by Effectov.lechenie : dose reduction or elimination of the drug. To expedite excretion possible appointment sekwestrantov biliary acids. Small quantities glukuronida may be removed by dialysis (mikofenolovaya acid dializuetsa not).

Precautions

There is a need to bear in mind the possibility of increasing the risk of limfoproliferativeh processes (about 1% of cases), and regularly monitor the peripheral blood, while lowering the number of Klebsiella below 1.3 x ^ 3 / l has direct doses or interruption of treatment (and appropriate therapy). In the case of reducing speed clubockova filtering below 25 ml / min is not recommended the use of more than 2 times a day. During and in the six weeks after the end of compulsory reliable contraception; If the pregnancy yet emerged, should consider the possibility of abortion.

Dosing and Administration

Inside, erh. To prevent transplant rejection by 1 g twice a day (the initial dose should be taken within three days after transplantation), in combination with korticosteroidami and ziklosporinom. To treat rejection reactions, refractor to other treatments, 1.5 g twice a day, also in combination.

Directory → Immunotropona funds → Immunosuppressants → Mycophenolate mofetil