I-Tadalafil 171596-29-5 ukuPhatha i-Erectile Dysfunction kuMadoda
Iinkcukacha zeMveliso
| Igama | Tadalafil |
| Inombolo yeCAS | 171596-29-5 |
| Ifomula yemolekyuli | I-C22H19N3O4 |
| Ubunzima bemolekyuli | 389.4 |
| Inombolo ye-EINECS | 687-782-2 |
| Ukujikeleza okuthe ngqo | D20+71.0 ° |
| Ukuxinana | 1.51±0.1g/cm3(Kuxelwe kwangaphambili) |
| Imeko yokugcina | 2-8°C |
| Ifom | Umgubo |
| I-acidity coefficient | (pKa) 16.68±0.40 (Kuxelwe kwangaphambili) |
| Ukunyibilika kwamanzi | I-DMSO: enyibilikayo 20mg/mL, |
Izithethantonye
I-TADALAFIL; ICIALIS; IC 351;(6R,12AR)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido;GF 196960;ICOS 351;Tildenafil;
Isiphumo se-Pharmacological
I-Tadalafil (i-Tadalafil, i-Tadalafil) ine-formula ye-molecular ye-C22H19N3O4 kunye ne-molecular weight of 389.4. Isetyenziswe ngokubanzi kunyango lwe-erectile dysfunction ukususela ngo-2003, kunye negama lezorhwebo elithi Cialis (Cialis). NgoJuni 2009, i-FDA yavuma i-tadalafil e-United States yonyango lwezigulane ezine-pulmonary arterial hypertension (PAH) phantsi kwegama lokuthengisa i-Adcirca. I-Tadalafil yaziswa kwi-2003 njengeyeza lonyango lwe-ED. Ithatha imizuzu engama-30 emva kokulawula, kodwa umphumo wayo ongcono kakhulu ngu-2h emva kokuqala kwesenzo, kwaye umphumo unokuhlala kwi-36h, kwaye umphumo wayo awuchaphazeli ngokutya. I-dose ye-tadalafil yi-10 okanye i-20 mg, i-dose yokuqala ephakanyisiweyo yi-10 mg, kwaye i-dose ilungiswa ngokwempendulo yesigulane kunye neempendulo ezimbi. Izifundo zangaphambi kweemarike zibonise ukuba emva kokulawulwa komlomo we-10 okanye i-20 mg ye-tadalafil kwiiveki ze-12, amaxabiso asebenzayo yi-67% kunye ne-81%, ngokulandelanayo. Izifundo ezininzi zibonise ukuba i-tadalafil inokusebenza okungcono kunyango lwe-ED.
I-Erectile Dysfunction: I-Tadalafil yintlobo ye-phosphodiesterase ekhethiweyo ye-5 (PDE5) efana ne-sildenafil, kodwa isakhiwo sayo sihluke kule yokugqibela, kwaye ukutya okunamafutha amaninzi akuphazamisi ukufunxa kwayo. Ngaphantsi kwesenzo sokuvuselela 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 monophosphate (cGMP), ngaloo ndlela isebenze i-cyclic guanosine monophosphate-dependent protein kinase, ekhokelela ekunciphiseni koxinzelelo lwe-calcium ions kwiiseli ze-muscle ezigudileyo, ezibangela ukuba i-corpus cavernosum Erection yenzeka ngenxa yokuphumla kwezihlunu ezigudileyo. I-Phosphodiesterase type 5 (PDE5) ithoba i-cGMP kwiimveliso ezingasebenziyo, okwenza incanca ibe yimeko ebuthathaka. I-Tadalafil inqanda ukuthotywa kwe-PDE5, ekhokelela ekuqokeleleni i-cGMP, ekhulula i-muscle egudileyo ye-corpus cavernosum, ekhokelela kwi-penile erection. Ekubeni i-nitrate i-NO donors, ukusetyenziswa okudibeneyo kunye ne-tadalafil kuya kwandisa kakhulu inqanaba le-cGMP kwaye kukhokelela kwi-hypotension enzima. Ngoko ke, ukusetyenziswa okudibeneyo kwezi zibini kuchasene nokusebenza kweklinikhi.
I-Tadalafil isebenza ngokuthintela i-PDES. I-GMP ithotyiwe, ngoko ke ukusetyenziswa okudityanisiweyo kunye ne-nitrate kunokubangela ukuhla okugqithisileyo koxinzelelo lwegazi kunye nokwandisa umngcipheko we-syncope. I-CY3PA4 inducers iya kunciphisa i-bioavailability ye-tadanafil, kwaye indibaniselwano ne-rifampicin, i-cimetidine, i-erythromycin, i-clarithromycin, i-itracon, i-ketocon, kunye ne-HVI protease inhibitors inokunyusa Uxinzelelo lwegazi lwechiza kufuneka luhlengahlengiswe. Ukuza kuthi ga ngoku, akukho ngxelo yokuba iiparamitha ze-pharmacokinetic zale mveliso zichaphazeleka kukutya kunye notywala.
