171596-29-5 Tadalafil

Tadalafil, hamwe na formula ya molekuline C22H19N3O4 hamwe nuburemere bwa molekile 389.4, yakoreshejwe cyane mukuvura imikorere mibi yumugabo kuva 2003 mu izina ryubucuruzi Cialis.Muri 2008, Isosiyete ya Eli Lilly yagurishije uburenganzira bwo guteza imbere ubucuruzi bwo kuvura PAH muri United Therapeutics.Muri Kamena 2009, FDA yemeje Tadafil kuvura abarwayi bafite hypertension yimpyiko (PAH) muri Amerika ku izina ry’ubucuruzi Adcirca.Tadafil yakozwe mu 2003 nk'umuti wo kuvura ED, kandi ingaruka zagize ingaruka 30min nyuma yubuyobozi, ariko ingaruka nziza ni 2h nyuma yubuyobozi, kandi ingaruka zishobora kumara 36h, kandi ingaruka ntizatewe nibiryo.Igipimo cya tadafil ni 10 cyangwa 20mg, igipimo cyambere gisabwa ni 10mg, ukurikije uko umurwayi yitwaye ndetse ningaruka mbi.Ubushakashatsi bwakozwe mbere y’isoko bwerekanye ko nyuma yibyumweru 12 byubuyobozi bwo mu kanwa bwa 10 cyangwa 20mg ya tadafil, ibisubizo byatanzwe byari 67% na 81%.Ubushakashatsi bwinshi bwerekanye ko tadafil ifite imikorere myiza mukuvura ED.
Imikorere mibi ya Erectile: Tadanafil na sildenafil ni ubwoko bumwe bwa fosifodiyesterase yo mu bwoko bwa 5 (PDE5), ariko imiterere yabyo iratandukanye niyanyuma, kandi indyo yuzuye ibinure ntabwo ibangamira iyinjizwa ryabo.Mugihe cyo gukangura imibonano mpuzabitsina, synthase ya nitric oxyde (NOS) mumyanya ndangagitsina ya penile na selile endothelia selile itera synthesis ya nitric oxyde (OYA) iva muri substrate L-arginine.OYA ikora siklase ya guanylate, ihindura trifosphate ya guanosine na fosifike ya cyclica ya guanosine (cGMP), bityo igakora poroteyine kinase ya cyclicique ya guanosine, bigatuma igabanuka ryimyunyu ngugu ya calcium yimitsi yoroheje, bigatuma habaho kuruhura imitsi yoroshye yimboro. sponge no kwubaka.Ubwoko bwa Phosphodiesterase ubwoko bwa 5 (PDE5) butesha agaciro cGMP mubicuruzwa bidakora, bigatera intege nke zimboro.Muguhagarika kwangirika kwa PDE5, tardanafil itera kwirundanya kwa cGMP, iruhura imitsi yoroshye ya corpus cavernosum yimboro kandi iganisha ku gutera imboro.Kubera ko estrate estrate NTA baterankunga, guhuza hamwe na tadanafil birashobora kongera cyane urwego rwa cGMP kandi biganisha kuri hypotension ikabije, kubwibyo, kwanduza ivuriro byombi birabujijwe.
Tardanafil igira ingaruka mukubuza PDES.Kwangirika kwa GMP, iyo rero bikoreshejwe hamwe na acide ya nitric na vinegere bishobora gutera umuvuduko ukabije wumuvuduko wamaraso kandi byongera ibyago bya syncope.CY3PA4 agent induction irashobora kugabanya abiotic kuboneka kwa tadana, kandi hamwe na rifampicin, cimetidine, erythromycine, clarithromycin, itraconwa, ketoconwa na protease inhibitor za HVI bishobora kongera amaraso yibicuruzwa.Hagomba kwitonderwa guhindura igipimo.Kugeza ubu, nta raporo yigeze ivuga ku bipimo bya farumasi y’ibicuruzwa byibasiwe nimirire n'inzoga.
Ukoresheje D-tryptophan nkibikoresho fatizo, reaction ya mbere ya methyl ester, ibisubizo bya D-tryptophan methyl ester hydrochloride muri alcool ya isopropyl na piperaldehyde Pictet-spengler reaction kugirango ibone cis-tetra hydrocarboline, hanyuma reaction hamwe na chloroacetyl chloride na methylamine, byose hamwe. umusaruro ni 56%, nyuma yo kwisuzumisha, Glacial acetic acide yarushijeho kwezwa nkumuti wa rerystallisation.Ikigereranyo cyihariye cyo kugereranya nuburyo bukurikira:

Cialis ni Tadalafil, imiti yo mu kanwa yatunganijwe na Eli Lilly Pharmaceutical Company yo kuvura imikorere mibi yumugabo.Nibisekuru bya kabiri phosphodiesterase 5 inhibitor.Raporo yubushakashatsi yerekana ko ugereranije na sildenafil, Cialis itangira gukurikizwa vuba, iminota 15 kugeza kuri 20, kandi ingaruka zimara amasaha 36.T1 / 2 ni amasaha 17.5.Mu bushakashatsi bwakorewe ku bagabo 348 bafite imikorere idahwitse kandi ikomeye y’igitsina gabo batoranijwe gufata tadalafil 20mg cyangwa umwanya wa platbo, amasaha 24 na 36 nyuma yo gufata ibiyobyabwenge byateye imbere mu mibonano mpuzabitsina ugereranije na placebo, abagabo benshi bakaba bararyamanye kabiri mu masaha 36.Nta tandukanyirizo ryagaragaye nuburemere bwibiyobyabwenge bibi ugereranije na placebo.Abagabo barenga 5% mumatsinda ya Tadalafil barwaye umutwe hamwe no kutarya.[Reaction reaction] Nta reaction zikomeye zagaragaye, nko guhindagurika no kubona ibintu bidasanzwe.Rimwe na rimwe kubabara umutwe, dyspepsia.[Precautions] Abarwayi bafata nitrate, angina pectoris, indwara z'umutima, hypertension itagenzuwe cyangwa hypotension, hamwe n'abarwayi bagize ikibazo cy'ubwonko mu mezi 6 ashize ntibagomba kwemererwa.

Phosphodiesterase 5 inhibitor zikoreshwa mukuvura imikorere mibi yumugabo.Igisekuru cya kabiri phosphodiesterase 5 inhibitor zikoreshwa mukuvura imikorere mibi yumugabo.