171596-29-5 Tadalafil

Tadalafil, oo leh caanaha molecular C22H19N3O4 iyo miisaanka molecular 389.4, kaas oo si ballaaran loo isticmaalay si loogu daaweeyo cillad kacsi ee ragga tan iyo 2003 ee hoos yimaada magaca ganacsiga Cialis.Sannadkii 2008, Shirkadda Eli Lilly waxay ka iibisay xuquuqda horumarinta ganacsiga ee daaweynta PAH ee United Therapeutics.Bishii Juun 2009, FDA waxay ansixisay Tadafil daaweynta bukaanada qaba hypertension sambabada (PAH) ee Maraykanka oo hoos yimaada magaca ganacsiga Adcirca.Tadafil waxaa la soo saaray 2003 sida daawada loogu talagalay daaweynta ED, saameyntuna waxay ahayd wax ku ool ah 30min ka dib maamulka, laakiin saameynta ugu fiican waxay ahayd 2h ka dib maamulka, saameyntuna waxay socon kartaa 36h, saameyntuna ma saameynayso cuntada.Qiyaasta tadafil waa 10 ama 20mg, qiyaasta bilowga ah ee lagu taliyey waa 10mg, taas oo ku xidhan falcelinta bukaanka iyo falcelinta xun.Daraasadaha suuqa ka hor ayaa muujiyay in ka dib toddobaadyada 12 ee maamulka afka ee 10 ama 20mg ee tadafil, heerarka jawaab-celinta waxay ahaayeen 67% iyo 81%, siday u kala horreeyaan.Daraasado badan ayaa muujiyay in tadafil ay waxtar fiican u leedahay daaweynta ED.
Kacsiga kacsiga: Tadanafil iyo sildenafil waxay ka tirsan yihiin isla nooca fosfodiesterase ee la xushay 5 (PDE5), laakiin qaabdhismeedkoodu wuu ka duwan yahay kan dambe, iyo cuntada dufanku ku badan tahay ma faragelinayso nuugista.Marka la eego kicinta galmada, nitric oxide synthase (NOS) ee dareemaha dareemaha guska iyo unugyada xididada xididada xididada ayaa kicinaya isku dhafka nitric oxide (NO) ee ka soo baxa substrate L-arginine.MAYA waxay kicisaa cyclase guanylate, taas oo u beddesha guanosine triphosphate una beddelo guanosine phosphate (cGMP), taas oo kicinaysa cyclic guanosine phospho-based protein kinase, taasoo keentay hoos u dhac ku yimaada uruurinta calcium intracellular ee muruqa siman, taasoo keentay nasinta muruqa siman ee xubinta taranka. isbuunyo iyo kacsi.Nooca phosphodiesterase 5 (PDE5) wuxuu hoos u dhigaa cGMP inuu noqdo alaab aan firfircoonayn, taasoo keenta daciifnimo guska.Iyadoo la xakameynayo hoos u dhaca PDE5, tardanafil waxay keenaysaa ururinta cGMP, taas oo dejisa muruqa siman ee cavernosum corpus ee xubinta taranka waxayna u horseedaa kacsiga guska.Maaddaama esters-ka Nitrate-ku aanu ahayn deeq-bixiyeyaal, isku-darkooda tadanafil waxay si weyn u kordhin karaan heerka cGMP waxayna u horseedi karaan hypotension daran, sidaas darteed, iska-hor-imaadyada kiliinikada ee labadaba waa la mamnuucay.
Tardanafil wuxuu saameeyaa tan isagoo xakameynaya PDES.Burburinta GMP, markaa marka lagu daro nitric acid iyo khal waxay keeni kartaa hoos u dhac aad u weyn oo ku yimaada cadaadiska dhiigga waxayna kordhisaa halista isku-dhafka.Wakiilka soo saarista CY3PA4 wuxuu yarayn karaa helitaanka abiotic ee tadana, iyo isku darka rifampicin, cimetidine, erythromycin, clarithromycin, itraconwa, ketoconwa iyo HVI protease inhibitors waxay kordhin kartaa xoogga dhiiga badeecadan.Waa in fiiro gaar ah loo yeesho hagaajinta qiyaasta.Ilaa hadda, ma jiraan wax warbixin ah oo ku saabsan xuduudaha farmashiyaha ee alaabtan ay saameeyeen cuntada iyo khamriga.
Isticmaalka D-tryptophan sida walxo ceeriin ah, falcelinta methyl ester-ka ugu horreysa, natiijada D-tryptophan methyl ester hydrochloride ee khamriga isopropyl iyo piperaldehyde Pictet-spengler falcelinta si loo helo cis-tetra hydrocarboline compound, ka dibna falcelinta chloroacetyl chloride iyo methylamine, wadarta guud. wax-soo-saarku waa 56%, baadhista ka dib, Glacial acetic acid ayaa loo sii sifeeyay sidii dareere recrystalization ah.Isla'egta falcelinta gaarka ah waa sida soo socota:

Cialis waa Tadalafil, daawo afka laga qaato oo ay samaysay shirkadda dawooyinka ee Eli Lilly si loogu daweeyo cillad la'aanta ragga.Waa jiilka labaad ee fosfodiesterase 5 inhibitor.Warbixinnada cilmi-baaristu waxay muujinayaan in marka la barbardhigo sildenafil, Cialis ay si dhakhso ah u dhaqan gasho, qiyaastii 15 illaa 20 daqiiqo, saameyntuna waxay socotaa ilaa saacadaha 36.T1/2 waa 17.5 saacadood.Daraasad lagu sameeyay 348 rag ah oo qaba cillad kacsi fudud iyo mid daran oo loo kala soocay inay qaataan tadalafil 20mg ama placebo, labadaba 24 iyo 36 saacadood ka dib qaadashada daroogada ayaa wanaajisay guusha galmada marka loo eego placebo, iyadoo ragga intooda badan ay si guul leh u galmoodaan laba jeer saacadaha 36.Ma jirin farqi u dhexeeya dhacdooyinka iyo darnaanta falcelinta daroogada xun marka la barbar dhigo placebo.In ka badan 5% ragga kooxda Tadalafil waxay lahaayeen madax-xanuun iyo dheef-shiid kiimikaad.[Dareen-celinta xun] Ma jirin fal-celin xun oo halis ah, sida qulqulka iyo cilladaha aragga.Mararka qaarkood madax xanuun, dyspepsia.[Taxaddar] Bukaannada qaadanaya Nitrate-ka, angina pectoris, cudurrada wadnaha, dhiig-karka aan la xakameynin, iyo bukaannada uu ku dhacay istaroog 6-dii bilood ee la soo dhaafay waa in aan la oggolaan.

Fosfodiesterase 5 inhibitors waxaa loo isticmaalaa in lagu daaweeyo cillad kacsiga ragga.Jiilka labaad ee fosfodiesterase 5 inhibitors ayaa loo isticmaalaa in lagu daweeyo cillad la'aanta ragga.