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,
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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