riminofenazinis anti TB moqmedeba
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Transcript riminofenazinis anti TB moqmedeba
riminofenazinis
anti TB moqmedeba
marina gaCeCilaZe,
“samSabaToba”, 02.11.10
riminofenazini Seiqmna aqtiuri fenazinis naerTebis jgufidan, sadac
Semcvleli jgufi R CarTulia molekulis “imino” nawilSi
ZiriTadi Tvisebebi
ujredSida akumulaciis unari, fagocitebSi swrafi dagroveba;
anTebis sawinaaRmdego moqmedeba;
wamlis mimarT rezistentobis dabali sixSire;
organizmidan neli gamoyofa – didi naxevardaSlis periodi;
saerTaSoriso saxelwodeba – klofazimini;
savaWro saxelwodeba – lampreni;
sinonimebi: solasulfoni, cimetoni, nogotrini, solapsoni, sulferoni, sulfonazini;
mwarmoebeli qveyana- Sveicaria;
registrirebulia – 1989 wels;
gadis preklinikuri kvlevebis III stadias;
molekuluri masa - 473,4;
qimiuri saxelwodeba – 3 (P-chloroanilino) – 10 (n-qlorfenilin -2, 10 dihidro -
2-izopropil-iminofenazidi);
wiTeli, moyavisfro Seferilobis fxvnilia;
advilad ixsneba benzolSi;
ixsneba qloroformSi;
cudad ixsneba acetonSi;
wyalSi praqtikulad uxsnadia;
fuZea;
aqtiuria fiziologiuri PH-is pirobebSi;
klinikuri farmakologia
riminofenazini Trgunavs mikobaqteriis zrdas da gamravlebas;
ukavSirdeba M. tuberculosis dnm-is guaninis
nukleotids da axdens mis transkripcias;
farmakokinetika
plazmaSi ufro dabali koncentraciiTa vidre qsovilebSi;
wamlis kristalebi aris fagocitarul ujredSi;
lipofiluria, lagdeba cximovan qsovilSi da retikuloendoTelialur sistemaSi;
makrofagebiT STainTqmeba mTels sxeulSi;
organizmSi rCeba 70 dRe - naxevraddaSlis periodi xangrZlivia;
gverdiTi movlenebi:
icvleba kanis pigmentacia;
muclis tkivili;
diarea;
gulisreva;
Rebineba;
organizmidan preparati ZiriTadad gamoiyofa fekaluri masiT da SardiT; nerwyviT da rZiT
naklebad;
xangrZlivi gamoyenebisas kani da lorwovani narinjisfers iRebs;
fagocitur ujredebSi aris preparatis kristalis CanarTebi;
moqmedebis meqanizmi:
riminofenazinebi aZliereben fosforilazas (PLA2) aqtivobas, rac xels uwyobs
lizofosfolipidebis dagrovebas, rac Tavis mxriv ganapirobebs gram (+) baqteriebis
inhibirebas;
klofazamins sxva TB preparatebTan SedarebiT rezistentobis ganviTarebis dabali sixSire
axasiaTebs;
xels uSlis Stamis izoniazidis mimarT rezistentobis ganviTarebas;
klofaziminis analogebi:
klofazaminze meti in vitro aqtivoba aRmoaCnda xuT analogs: B746, B4100, B4101,
B4154, B4157;
B4100 – toqsiuria makrofagebis mimarT;
B4101 –is ujredSida aqtivoba klofazaminis msgavsia, Tumca ar aris Seswavlili misi in
vivo aqtivoba;
B746 da B4157, B4154 klofaziminTan SedarebiT naklebad iwvevs Sinagani organoebis
lorwovanis da cximovani ujredebis pigmentaciis Secvlas;
analogebis gamoyenebam ar gamoiwvia klofazaminis mimarT Stamis rezistentobis
ganviTareba;
M. Avium -ze moqmedeba:
HIV/AIDS pacientis makrofagSi aZlierebs Clr; da roqsitromicinis moqmedebas;
efeqturia Clr, rifabutinTan da etambutolTan kombinaciaSi;
ara aiv-inficirebul pacientebSi:
cfz(150)+rifabutini(300)+Am+H+S+E; naxvelis konversia 13-dan mxolod 2
SemTxvevaSi aRniSna;
cfz(50-100mg/dReSi)+Am(75mg/kg 12 sT-Si erTxel)+E (15-
25mg)+R(600mg dReSi) iyo efeqturi;
daskvna:
axali preparatis mizania ujredSida organizmebis ganadgureba;
klofaziminis gamoyeneba TB mkurnalobaSi miRebulia, vinaidan ar aris
gamovlenili mikobaqteriis arc erTi rezistentuli forma am wamlis mimarT;
riminofenazinebis unikaluri Tviseba wamlebis makrofagebSi transportirebis unaria.
gmadlobT
yuradRebisaTvis