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mikofenolna kislina
mycophenolic acid

mikofenolna kislina (mpa, aktivni metabolit):
mycophenolic acid (mpa, active metabolite) :

mikofenolna kislina (enkratni 1 g odmerek)
mycophenolic acid (1 g single dose)

aktivni presnovek mofetilmikofenolata je mikofenolna kislina (mfk).
mycophenolic acid (mpa) is the active metabolite of mycophenolate mofetil.

mikofenolna kislina (substrat udp- glukuronil- transferaze):
mycophenolic acid (udp-glucuronyl transferase substrate):

v klinično relevantnih koncentracijah je mikofenolna kislina 97 % vezana na plazemske albumine.
mpa at clinically relevant concentrations is 97 % bound to plasma albumin.

zdravljenje med zavrnitveno reakcijo: aktivni presnovek mofetilmikofenolata je mikofenolna kislina (mfk).
mpa (mycophenolic acid) is the active metabolite of mycophenolate mofetil.

zanemarljiva količina učinkovine (manj kot 1 % odmerka) se kot mikofenolna kislina izloča v urin.
a negligible amount of substance is excreted as mpa (< 1 % of dose) in the urine.

mikofenolna kislina se večinoma presnovi z glukuronilno transferazo v fenolni glukuronid mikofenolne kisline (mikofenolglukuronid), ki pa ni farmakološko aktiven.
mpa is metabolised principally by glucuronyl transferase to form the phenolic glucuronide of mpa (mpag), which is not pharmacologically active.

mikofenolna kislina ima večji citostatični učinek na limfocite kot na druge celice, ker je razmnoževanje limfocitov t in b odločilno odvisno od de novo sinteze purinov, medtem ko lahko drugi tipi celic uporabljajo rešilne sintezne poti.
because t and b lymphocytes are critically dependent for their proliferation on de novo synthesis of purines whereas other cell types can utilise salvage pathways, mpa has more potent cytostatic effects on lymphocytes than on other cells.

mikofenolna kislina se večinoma presnovi z glukuronilno transferazo (izoencim ugt1a9) v neaktivni fenolni glukuronid mikofenolne kisline (mikofenolglukuronid).
mpa is metabolised principally by glucuronyl transferase (isoform ugt1a9) to form the inactive phenolic glucuronide of mpa (mpag).

mikofenolna kislina je močan, selektivni, nekompetitivni in reverzibilni zaviralec inozin- monofosfat- dehidrogenaze in tako zavira de novo sintezo gvanozinskih nukleotidov, brez vključevanja v dna.
mycophenolate mofetil is the 2-morpholinoethyl ester of mycophenolic acid (mpa). mpa is a potent, selective, uncompetitive and reversible inhibitor of inosine monophosphate dehydrogenase, and therefore inhibits the de novo pathway of guanosine nucleotide synthesis without incorporation into dna.