171596-29-5 Tadalafil

I-Tadalafil, kunye ne-molecular formula C22H19N3O4 kunye ne-molecular weight 389.4, esetyenziswe ngokubanzi ukuphatha ukungasebenzi kwe-erectile kumadoda ukususela kwi-2003 phantsi kwegama lezorhwebo elithi Cialis.Ngo-2008, i-Eli Lilly Company yathengisa amalungelo ophuhliso lwezorhwebo kunyango lwe-PAH kwi-United Therapeutics.NgoJuni 2009, i-FDA yavuma i-Tadafil yonyango lwezigulane ezine-pulmonary arterial hypertension (PAH) e-United States phantsi kwegama lokuthengisa i-Adcirca.I-Tadafil yaphuhliswa kwi-2003 njengeyeza lonyango lwe-ED, kwaye umphumo wawusebenza nge-30min emva kokulawula, kodwa umphumo ongcono kakhulu wawuyi-2h emva kokulawula, kwaye umphumo unokuhlala kwi-36h, kwaye umphumo awuzange uchaphazeleke kukutya.I-dosage ye-tadafil yi-10 okanye i-20mg, i-dose yokuqala ephakanyisiweyo yi-10mg, kuxhomekeke kwimpendulo yesigulane kunye neempendulo ezimbi.Izifundo zangaphambi kwemakethe zibonise ukuba emva kweeveki ze-12 zokulawulwa komlomo we-10 okanye i-20mg ye-tadafil, amazinga okuphendula ayengama-67% kunye ne-81%, ngokulandelanayo.Izifundo ezininzi zibonise ukuba i-tadafil inokusebenza okungcono ekuphatheni i-ED.
I-Erectile Dysfunction: I-Tadanafil kunye ne-sildenafil yohlobo olufanayo lwe-phosphodiesterase ye-5 (PDE5) ekhethiweyo, kodwa isakhiwo sabo sihluke kuleyo yokugqibela, kwaye ukutya okunamafutha aphezulu akuphazamisi ukufunxa kwabo.Ngaphantsi kokuvuselela ngokwesondo, i-nitric oxide synthase (NOS) kwi-penile nerve endings kunye neeseli ze-vascular endothelial catalyzes synthesis ye-nitric oxide (NO) ukusuka kwi-substrate L-arginine.I-NO isebenze i-guanylate cyclase, eguqula i-guanosine triphosphate ibe yi-cyclic guanosine phosphate (cGMP), ngaloo ndlela isebenze i-cyclic guanosine phospho-dependent protein kinase, ekhokelela ekunciphiseni kwe-intracellular concentration ye-calcium yemisipha egudileyo, okukhokelela ekuphumleni kwemisipha egudileyo yepenile. isipontshi kunye nokumisa.Uhlobo lwe-Phosphodiesterase 5 (PDE5) luthoba i-cGMP kwiimveliso ezingasebenziyo, ezibangela ubuthathaka bepenile.Ngokuthintela ukuthotywa kwe-PDE5, i-tardanafil ikhokelela ekuqokeleleni i-cGMP, ekhulula i-muscle epholileyo ye-corpus cavernosum ye-penis kwaye iholele kwi-penile erection.Ekubeni i-nitrate esters AKUKHO abanikeli, ukudibanisa kwabo kunye ne-tadanafil kunokunyusa kakhulu inqanaba le-cGMP kwaye kukhokelela kwi-hypotension enzima, ngoko ke, ukuchasana kweklinikhi zombini kuyaphikisana.
I-Tardanafil ichaphazela oku ngokuvimbela i-PDES.Ukuthotywa kwe-GMP, ngoko xa isetyenziswe ngokudibeneyo ne-nitric acid kunye neviniga inokubangela ukuhla okugqithisileyo kwengcinezelo yegazi kunye nokwandisa umngcipheko we-syncope.I-CY3PA4 induction agent inokunciphisa ukufumaneka kwe-abiotic ye-tadana, kwaye indibaniselwano ne-rifampicin, i-cimetidine, i-erythromycin, i-clarithromycin, i-itraconwa, i-ketoconwa kunye ne-HVI protease inhibitors inokunyusa ukuxinwa kwegazi kule mveliso.Ingqalelo kufuneka ihlawulwe ekulungiseni umthamo.Ukuza kuthi ga ngoku, akukho ngxelo kwiiparamitha ze-pharmacokinetic zale mveliso echaphazelekayo kukutya kunye notywala.
Ukusebenzisa i-D-tryptophan njengento ekrwada, impendulo yokuqala ye-methyl ester, isiphumo se-D-tryptophan methyl ester hydrochloride kwi-isopropyl yotywala kunye ne-piperaldehyde i-Pictet-spengler reaction ukuze ufumane i-cis-tetra hydrocarboline ikhompawundi, kwaye emva koko iphendule nge-chloroacetyl chloride kunye ne-methylamine iyonke, isivuno yi-56%, emva kokuhlolwa, i-Glacial acetic acid yahlanjululwa ngakumbi njenge-solvent recrystallization.Inxaki yokusabela ethile yile ilandelayo:

I-Cialis yi-Tadalafil, ichiza lomlomo eliphuhliswe ngu-Eli Lilly Pharmaceutical Company kunyango lwe-erectile dysfunction kumadoda.Sisizukulwana sesibini se-phosphodiesterase 5 inhibitor.Iingxelo zophando zibonisa ukuba xa kuthelekiswa ne-sildenafil, i-Cialis isebenza ngokukhawuleza, malunga ne-15 kwimizuzu ye-20, kwaye umphumo uhlala ukuya kwiiyure ze-36.T1/2 yi 17.5 iiyure.Kuphononongo lwamadoda angama-348 ane-erectile i-mild to erectile dysfunction e-randomized ukuthatha i-tadalafil 20mg okanye i-placebo, zombini i-24 kunye neeyure ze-36 emva kokuthatha ichiza liphucule impumelelo yesondo xa kuthelekiswa ne-placebo, kunye namadoda amaninzi aphumelele ngesondo kabini kwiiyure ze-36.Kwakungekho mahluko kwizehlo kunye nobukhali bezenzo ezigwenxa zeziyobisi xa kuthelekiswa ne-placebo.Ngaphezulu kwe-5% yamadoda kwiqela le-Tadalafil lalineentloko kunye nokugaya.[Iimpendulo ezingathandekiyo] Akukho ziziphumo zibi zibonweyo, ezinje ngokugungxulwa nokungaboni kakuhle.Ngamanye amaxesha intloko ebuhlungu, i-dyspepsia.[Amanyathelo okhuseleko] Izigulana ezithatha i-nitrate, i-angina pectoris, isifo sentliziyo, uxinzelelo lwegazi olungalawulekiyo okanye i-hypotension, kunye nezigulane ezibe ne-stroke kwiinyanga ezi-6 ezidlulileyo akufanele zivunyelwe.

I-Phosphodiesterase 5 inhibitors isetyenziselwa ukunyanga i-erectile dysfunction emadodeni.Isizukulwana sesibini se-phosphodiesterase 5 inhibitors sisetyenziselwa ukuphatha ukungasebenzi kakuhle kwe-erectile kumadoda.