68278-23-9
68278-23-9 結(jié)構(gòu)式
基本信息
鹽酸依氟烏氨酸
鹽酸恩氟沙星
鹽酸依氟鳥(niǎo)氨酸無(wú)水物
2-(DIFLUOROMETHYL)-ORNITHINE HYDROCHLORIDE
DFMO
DFMO HCL
DFMO HYDROCHLORIDE
DL-ALPHA-DIFLUOROMETHYLORNITHINE HYDROCHLORIDE
EFLORNITHINE HCL
EFLORNITHINE HYDROCHLORIDE
RMI-71782
RMI-71782 HYDROCHLORIDE
2-(difluoromethyl)-dl-ornithinehydrochloridehydrate
alpha-difluoromethylornithinehydrochloridehydrate
dl-ornithine,2-(difluoromethyl)-,monohydrochloride,hydrate
eflornithinehydrochloridehydrate
DL-alpha-Difluoromethylonithine
EflornitineHCl
Eflornitinehydrochloride
2-(Difluoromethyl)-DL-Ornithine hydrochloride
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
依氟鳥(niǎo)氨酸：該分子比美拉胂醇的毒性小，于1990年獲得注冊(cè)。它僅對(duì)布氏岡比亞錐蟲(chóng)有效。療程復(fù)雜，而且難以施用。尤其是在昏睡病高發(fā)的非洲農(nóng)村地區(qū)，醫(yī)療設(shè)備和醫(yī)務(wù)人員的緊缺讓這種治療方案的實(shí)施面臨重重阻礙。
2009年，包括非營(yíng)利性藥物研發(fā)組織DNDi（被忽視疾病藥物倡議）、無(wú)國(guó)界醫(yī)生組織等在內(nèi)的國(guó)際合作組織開(kāi)發(fā)了一種稱(chēng)為NECT的聯(lián)合療法，由硝呋替莫和依氟鳥(niǎo)氨酸聯(lián)合使用，比單用依氟鳥(niǎo)氨酸簡(jiǎn)便，安全性和治療效果也大大改善。它通過(guò)減少治療的持續(xù)時(shí)間和靜脈輸液的次數(shù)，簡(jiǎn)化了依氟鳥(niǎo)氨酸的使用，但不幸的是，沒(méi)有研究它對(duì)布氏羅得西亞錐蟲(chóng)是否有效。硝呋替莫被注冊(cè)用于治療美洲錐蟲(chóng)病，但未注冊(cè)用于治療非洲人類(lèi)錐蟲(chóng)病。盡管如此，在臨床試用提供了安全性和有效性數(shù)據(jù)之后，該藥與依氟鳥(niǎo)氨酸的聯(lián)合使用已被列入世衛(wèi)組織基本藥物清單，而且目前建議作為岡比亞型感染的一線(xiàn)治療。世衛(wèi)組織為此目的免費(fèi)為地區(qū)性流行國(guó)家提供這兩種藥物和載有用法所需的所有材料的材料包。
Eflornithine is the only new molecule registered for the treatment of human African trypanosomiasis over the last 50 years. It is the drug used mainly as a back-up for melarsoprol refractory Trypanosoma brucei gambiense cases. In subjects with excessive, unwanted facial hair, eflornithine 15% cream is superior to placebo in reducing hair growth. After 24 weeks' treatment, 58% of eflornithine and 34% of placebo subjects have at least some improvement in facial hirsutism. The hair growth inhibitory activity of eflornithine is significantly enhanced when the eflornithine cream is applied onto a mouse skin area pretreated with microneedles. Treatment of coarctation hypertensive rats with eflornithine results in a normalization of the contractile intensity to KCI and norepinephrine and relaxations to acetylcholine by 14 days of hypertension.