Iimveliso

I-Telithromycin yaziswa okokuqala eJamani njengonyango lomlomo olulolwa kanye yonke imihla losulelo lokuphefumla oluquka inyumoniya efunyanwa luluntu, ukonyuka kwebhaktiriya ebukhali yebronchitis engapheliyo, sinusitis ebukhali kunye ne-tonsillitis/pharyngitis.Le derivative ye-semisynthetic ye-natural macrolide erythromycin yi-ketolide yokuqala yokuthengisa, iklasi entsha ye-antibiotics ene-C3-ketone endaweni yeqela le-L-cladinose.I-14-membered ring antibacterial agent inqanda iprotheyini ye-bacterial synthesis ngokuzibophelela kwiindawo ezimbini ze-50S subunit ye-ribosomes yebhakteria.Ibonisa umsebenzi onamandla we-in vitro ngokuchasene nezifo eziqhelekileyo zokuphefumla ezibandakanya iStreptococcus pneumoniae, Haemophilus influenzae, iMoraxella catarrhalis kunye neStreptococcus pyogenes kunye nezinye iintsholongwane ezingaqhelekanga.Iqela le-3-keto linika ukwanda kozinzo lwe-asidi kunye nokunciphisa ukunyanzeliswa kwe-macrolide-lincosamide-streptogramin B ukuxhathisa okubonwa rhoqo nge-macrolides.I-C11-C12 intsalela ye-carbamate efakwe endaweni ayibonakali nje ukwandisa ubudlelwane bendawo yokubopha i-ribosomal kodwa kunye nokuzinzisa i-compound ngokuchasene ne-esterase hydrolysis kwaye ugweme ukuxhathisa ngenxa yokupheliswa kwe-macrolides kwiseli ngepompo ye-efflux efakwe kwi-mef gene kwii-pathogens ezithile. .I-Telithromycin yomibini inhibitor ekhuphisanayo kunye ne-substrate ye-CYP3A4.Nangona kunjalo, ngokungafaniyo nama-macrolides amaninzi afana ne-troleandomycin, ayenzi i-inhibitory ezinzileyo ye-CYP P-450 Fe2 + -nitrosoalkane metabolite complex enokuthi ibe ne-hepatotoxic.Ichiza linyamezelwa kakuhle kwaye lisasazwe kakuhle kwizicubu ze-pulmonary, i-bronchial secretions, iitoni kunye namathe.Kuvela ukuba kugxininiswe kakhulu kwi-azurophil granules ye-polymorphonuclear neutrophils ngaloo ndlela iququzelela ukuhanjiswa kwayo kwiibhaktheriya ze-phagocytosed.