171596-29-5 Tadalafil

I-Tadalafil, enefomula ye-molecular C22H19N3O4 kanye nesisindo se-molecular 389.4, esisetshenziswe kabanzi ukwelapha ukungasebenzi kahle kwe-erectile emadodeni kusukela ku-2003 ngaphansi kwegama lokuhweba elithi Cialis.Ngo-2008, i-Eli Lilly Company yathengisa amalungelo okuthuthukiswa kwezentengiselwano okwelashwa kwe-PAH kwa-United Therapeutics.NgoJuni 2009, i-FDA igunyaze i-Tadafil yokwelashwa kweziguli ezine-pulmonary arterial hypertension (PAH) e-United States ngaphansi kwegama lokuhweba elithi Adcirca.I-Tadafil yasungulwa ku-2003 njengesidakamizwa sokwelashwa kwe-ED, futhi umphumela wawusebenza kahle nge-30min ngemva kokuphathwa, kodwa umphumela omuhle kakhulu wawuyi-2h ngemva kokuphatha, futhi umphumela ungahlala ku-36h, futhi umphumela awuzange uthintwe ukudla.Umthamo we-tadafil yi-10 noma i-20mg, umthamo wokuqala onconyiwe ngu-10mg, kuye ngokuthi isiguli sisabela kanjani kanye nokusabela okubi.Ucwaningo lwangaphambi kwemakethe lubonise ukuthi ngemva kwamasonto angu-12 okulawulwa komlomo we-10 noma i-20mg ye-tadafil, izinga lokuphendula laliyi-67% ne-81%, ngokulandelana.Ucwaningo oluningi luye lwabonisa ukuthi i-tadafil iyasebenza kangcono ekwelapheni i-ED.
Ukungasebenzi kahle kwe-Erectile: I-Tadanafil ne-sildenafil ziyingxenye ye-5 ye-phosphodiesterase ekhethiwe efanayo (PDE5), kodwa isakhiwo sazo sihlukile kunesakamuva, futhi ukudla okunamafutha aphezulu akuphazamisi ukumuncwa kwawo.Ngaphansi kokugqugquzelwa ngokocansi, i-nitric oxide synthase (NOS) eziphethweni zenzwa ye-penile namaseli e-vascular endothelial igqugquzela ukuhlanganiswa kwe-nitric oxide (NO) kusuka ku-substrate L-arginine.I-NO yenza i-guanylate cyclase isebenze, eguqula i-guanosine triphosphate ibe yi-cyclic guanosine phosphate (cGMP), ngaleyo ndlela isebenze i-cyclic guanosine phospho-dependent protein kinase, okuholela ekwehleni kokugcwala kwe-intracellular calcium yemisipha ebushelelezi, okuholela ekuphumuleni kwemisipha ebushelelezi yepenile. isipontshi nokumiswa.I-Phosphodiesterase type 5 (PDE5) yehlisa isithunzi i-cGMP ibe yimikhiqizo engasebenzi, okubangela ubuthakathaka bomthondo.Ngokuvimbela ukuwohloka kwe-PDE5, i-tardanafil iholela ekuqoqweni kwe-cGMP, ekhulula imisipha ebushelelezi ye-corpus cavernosum yomthondo futhi iholele ekumisweni komthondo.Njengoba i-nitrate esters AKUKHO abanikeli, inhlanganisela yabo ne-tadanafil ingakhuphula kakhulu izinga le-cGMP futhi iholele ku-hypotension enzima, ngakho-ke, ukungqubuzana komtholampilo kokubili kuyaphikiswa.
I-Tardanafil ithinta lokhu ngokuvimbela i-PDES.Ukuwohloka kwe-GMP, ngakho-ke uma kusetshenziswa kuhlanganiswe ne-nitric acid noviniga kungase kubangele ukwehla okukhulu komfutho wegazi futhi kwandise ingozi ye-syncope.I-CY3PA4 induction agent inganciphisa ukutholakala kwe-abiotic ye-tadana, futhi inhlanganisela ne-rifampicin, i-cimetidine, i-erythromycin, i-clarithromycin, i-itraconwa, i-ketoconwa kanye ne-HVI protease inhibitors ingase inyuse ukugcwala kwegazi kulo mkhiqizo.Kufanele kuqashelwe ukulungisa umthamo.Kuze kube manje, akukabikho umbiko mayelana nemingcele ye-pharmacokinetic yalo mkhiqizo othintwa ukudla notshwala.
Kusetshenziswa i-D-tryptophan njengento eluhlaza, ukusabela kwe-methyl ester yokuqala, umphumela we-D-tryptophan methyl ester hydrochloride ku-isopropyl alcohol kanye ne-piperaldehyde Pictet-spengler reaction ukuze uthole i-cis-tetra hydrocarboline compound, bese isabela nge-chloroacetyl chloride ne-methylamine, inani eliphelele. isivuno singama-56%, ngemuva kokuhlolwa, i-Glacial acetic acid yaphinde yahlanzwa njenge-solvent recrystallization.I-equation ethize yokusabela imi kanje:

I-Cialis i-Tadalafil, isidakamizwa somlomo esakhiwe yi-Eli Lilly Pharmaceutical Company yokwelapha ukungasebenzi kahle kwe-erectile emadodeni.Kuyisizukulwane sesibili se-phosphodiesterase 5 inhibitor.Imibiko yocwaningo ibonisa ukuthi uma kuqhathaniswa ne-sildenafil, i-Cialis iqala ukusebenza ngokushesha kakhulu, mayelana ne-15 kumaminithi we-20, futhi umphumela uhlala kuze kube amahora angu-36.I-T1/2 amahora angu-17.5.Ocwaningweni lwamadoda angama-348 anokungasebenzi kahle kwe-erectile okuncane kuya kokuqina okungahleliwe ukuthatha i-tadalafil 20mg noma i-placebo, kokubili amahora angu-24 nama-36 ngemva kokuthatha lesi sidakamizwa kwathuthukisa impumelelo yezocansi uma kuqhathaniswa ne-placebo, namadoda amaningi aphumelela ukuya ocansini kabili ngamahora we-36.Kwakungekho mehluko ezenzakalweni nasebucayini bokusabela kwezidakamizwa ezimbi uma kuqhathaniswa ne-placebo.Abesilisa abangaphezu kuka-5% eqenjini le-Tadalafil babenekhanda elibuhlungu kanye nokugayeka kokudla.[Ukusabela Okubi] Akukho ukusabela okubi kakhulu okuphawuliwe, njengokuguquguquka nokungaboni kahle.Ngezinye izikhathi ubuhlungu bekhanda, i-dyspepsia.[Izixwayiso] Iziguli ezithatha ama-nitrate, i-angina pectoris, isifo senhliziyo, umfutho wegazi ophakeme noma umfutho wegazi ophakeme, kanye neziguli ezibe nesifo sohlangothi ezinyangeni eziyi-6 ezedlule akufanele zivunyelwe.

I-Phosphodiesterase 5 inhibitors isetshenziselwa ukwelapha ukungasebenzi kahle kwe-erectile emadodeni.Isizukulwane sesibili se-phosphodiesterase 5 inhibitors sisetshenziselwa ukwelapha ukungasebenzi kahle kwe-erectile emadodeni.