Awọn ọja

Telithromycin ni a kọkọ ṣe ifilọlẹ ni Ilu Jamani gẹgẹbi itọju ẹnu-ẹẹkan lojumọ fun awọn akoran atẹgun pẹlu aarun pneumonia ti agbegbe, awọn imukuro kokoro-arun nla ti bronchitis onibaje, sinusitis nla ati tonsillitis/pharyngitis.Itọsẹ semisynthetic yii ti macrolide erythromycin adayeba jẹ ketolide akọkọ ti o ta ọja, kilasi tuntun ti awọn egboogi ti o nfihan C3-ketone dipo ẹgbẹ L-cladinose.Aṣoju antibacterial oruka 14-membered ṣe idilọwọ iṣelọpọ amuaradagba kokoro-arun nipa sisopọ si awọn agbegbe meji ti ipin 50S ti awọn ribosomes kokoro-arun.O ṣe afihan iṣẹ ṣiṣe in vitro ti o lagbara lodi si awọn aarun atẹgun ti o wọpọ pẹlu Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis ati Streptococcus pyogenes ati awọn aarun alaiṣedeede miiran.Ẹgbẹ 3-keto n funni ni iduroṣinṣin ekikan ti o pọ si ati idinku idinku ti macrolide-lincosamide-streptogramin resistance ti o jẹ akiyesi nigbagbogbo pẹlu awọn macrolides.Aloku C11-C12 carbamate ti o rọpo han kii ṣe lati mu isunmọ pọ si fun aaye isunmọ ribosomal ṣugbọn tun lati ṣe iduroṣinṣin agbo naa lodi si esterase hydrolysis ati yago fun ilodisi nitori imukuro macrolides lati inu sẹẹli nipasẹ fifa efflux ti koodu nipasẹ mef pupọ ninu awọn pathogens kan. .Telithromycin mejeeji jẹ oludena ifigagbaga ati sobusitireti ti CYP3A4.Bibẹẹkọ, ko dabi ọpọlọpọ awọn macrolides bii troleandomycin, ko ṣe idawọle iduroṣinṣin CYP P-450 Fe2+-nitrosoalkane metabolite eka eyiti o jẹ hepatotoxic.Oogun naa ni ifarada daradara ati pinpin daradara si awọn iṣan ẹdọforo, awọn aṣiri ti bronchi, awọn tonsils ati itọ.O wa ni ifọkansi pupọ ni awọn granules azurophil ti awọn neutrophils polymorphonuclear nitorinaa irọrun ifijiṣẹ rẹ si awọn kokoro arun phagocytosed.