171596-29-5 Tadalafil

Tadalafil, ine molecular formula C22H19N3O4 uye molecular weight 389.4, iyo yakashandiswa zvakanyanya kurapa erectile dysfunction muvarume kubvira 2003 pasi pezita rekutengeserana Cialis.Muna 2008, Eli Lilly Company yakatengesa kodzero dzekusimudzira kutengeserana dzePAH kurapwa kuUnited Therapeutics.Muna June 2009, FDA yakabvumira Tadafil kurapwa kwevarwere vane pulmonary arterial hypertension (PAH) muUnited States pasi pezita rekutengeserana Adcirca.Tadafil yakagadzirwa mu2003 semushonga wekurapa ED, uye mhedzisiro yacho yakashanda 30min mushure mekutungamira, asi iyo yakanakisa mhedzisiro yaive 2h mushure mekutonga, uye mhedzisiro yacho inogona kugara kwe36h, uye mhedzisiro yacho haina kukanganiswa nekudya.Muyero we tadafil ndeye 10 kana 20mg, iyo inokurudzirwa yekutanga dose ndeye 10mg, zvichienderana nekuita kwemurwere uye maitiro asina kunaka.Zvidzidzo zvepamberi-musika zvakaratidza kuti mushure memavhiki e12 ekutonga kwemuromo kwe10 kana 20mg ye tadafil, mhinduro dzemhinduro dzaive 67% uye 81%, maererano.Zvidzidzo zvakawanda zvakaratidza kuti tadafil ine zvirinani kushanda mukurapa ED.
Erectile dysfunction: Tadanafil uye sildenafil ndeyemhando imwechete yakasarudzwa phosphodiesterase type 5 (PDE5), asi maitiro avo akasiyana neayo ekupedzisira, uye kudya kwemafuta akawanda hakuvhiringidzi kutora kwavo.Pasi pekukurudzira zvepabonde, nitric oxide synthase (NOS) mupenile nerve endings uye vascular endothelial masero anokonzera kuumbwa kwe nitric oxide (NO) kubva kune substrate L-arginine.HAPANA inobatisa guanylate cyclase, inoshandura guanosine triphosphate kuita cyclic guanosine phosphate (cGMP), nokudaro ichiita cyclic guanosine phospho-inotsamira protein kinase, zvichikonzera kuderera kwe intracellular calcium concentration yess smooth muscle, zvichikonzera kuzorora kwemhasuru yepenile. chipanje uye erection.Phosphodiesterase type 5 (PDE5) inokanganisa cGMP kuita zvigadzirwa zvisingaite, zvichikonzera kupera simba kwepenile.Nekudzivisa kuparara kwePDE5, tardanafil inotungamirira kuunganidzwa kweCGMP, iyo inozorodza musuru wakatsetseka wecorpus cavernosum yepeni uye inotungamirira kupenile erection.Sezvo nitrate esters vari NO vanopa, kusanganiswa kwavo netadanafil kunogona kuwedzera zvakanyanya cGMP level uye kutungamirira kune yakanyanya hypotension, saka, kliniki contraindications yezvose zviri zviviri zvinopesana.
Tardanafil inokanganisa izvi nekudzivisa PDES.GMP degradation, saka kana ikashandiswa pamwe chete nenitric acid nevhiniga inogona kukonzera kuderera kwakanyanya muropa uye kuwedzera njodzi yesyncope.CY3PA4 induction agent inogona kuderedza kuwanikwa kweabiotic yetadana, uye kusanganiswa ne rifampicin, cimetidine, erythromycin, clarithromycin, itraconwa, ketoconwa uye HVI protease inhibitors inogona kuwedzera kuwanda kweropa rechigadzirwa ichi.Kuchenjerera kunofanira kubhadharwa pakugadzirisa dose.Kusvika ikozvino, hakuna kumbove neshumo pamusoro pema pharmacokinetic parameters yechigadzirwa ichi chakakanganiswa nekudya uye doro.
Uchishandisa D-tryptophan seyakabikwa, yekutanga methyl ester reaction, inoguma D-tryptophan methyl ester hydrochloride mu isopropyl doro uye piperaldehyde Pictet-spengler reaction kuti uwane cis-tetra hydrocarboline compound, uyezve kuita ne chloroacetyl chloride uye methylamine, iyo yakazara. goho ndeye 56%, mushure mekuongorora, Glacial acetic acid yakawedzera kucheneswa seyakagadziriswa recrystallization solvent.Iyo chaiyo reaction equation ndeiyi inotevera:

Cialis is Tadalafil, mushonga wemukanwa wakagadzirwa naEli Lilly Pharmaceutical Company yekurapa erectile dysfunction muvarume.Iyo yechipiri-chizvarwa phosphodiesterase 5 inhibitor.Mishumo yekutsvagisa inoratidza kuti kana ichienzaniswa ne sildenafil, Cialis inobata nekukurumidza, nezve 15 kusvika 20 maminetsi, uye mhedzisiro yacho inotora kusvika kumaawa makumi matatu nematanhatu.T1/2 maawa 17.5.Muchidzidzo chevarume ve348 vane unyoro kusvika kune zvakanyanya erectile dysfunction avo vakangoerekana vatora tadalafil 20mg kana placebo, zvose 24 uye maawa 36 mushure mekutora mushonga wakavandudza kubudirira kwepabonde kuenzaniswa ne placebo, nevarume vakawanda vakabudirira kuita zvepabonde kaviri pamaawa 36.Pakanga pasina mutsauko muchiitiko uye kuomarara kwemaitiro akashata ezvinodhaka zvichienzaniswa ne placebo.Vanopfuura 5% yevarume muboka reTadalafil vaive nemusoro uye indigestion.[Maitiro akashata] Hapana maitiro akashata akakomba akaonekwa, akadai sekuputika uye kusaona zvakanaka.Dzimwe nguva kutemwa nemusoro, dyspepsia.[Kungwarira] Varwere vari kutora nitrate, angina pectoris, chirwere chemwoyo, hypertension isingadzoreki kana hypotension, uye varwere vane sitiroko mumwedzi mitanhatu yapfuura havafaniri kubvumirwa.

Phosphodiesterase 5 inhibitors inoshandiswa kurapa erectile dysfunction muvarume.Chizvarwa chechipiri phosphodiesterase 5 inhibitors chinoshandiswa kurapa erectile dysfunction muvarume.