Vardenafil Dihydrochloride na-agwọ ọrịa akwụrụ 224785-91-5

Ihe omume ọgwụ
Ọgwụ a bụ ihe mgbochi ụdị phosphodiesterase 5 (PDE5). Nlekọta ọnụ nke ọgwụ a nwere ike imeziwanye ogo na oge a na-arụ ọrụ nke ọma, ma melite ọganihu nke ndụ mmekọahụ na ndị nwoke nwere nkwarụ erectile. Mmalite na mmezi nke nrụpụta penile metụtara izu ike nke mkpụrụ ndụ akwara dị nro nke cavernosal, yana cyclic guanosine monophosphate (cGMP) bụ onye ogbugbo nke izu ike nke mkpụrụ ndụ akwara dị nro nke cavernosal. Ọgwụ a na-egbochi ire ere nke cGMP site na igbochi ụdị phosphodiesterase 5, si otú a na-eme ka mkpokọta cGMP, izu ike nke uru ahụ dị nro nke corpus cavernosum, na nrụnye nke amụ. E jiri ya tụnyere phosphodiesterase isozymes 1, 2, 3, 4, na 6, ọgwụ a nwere nhọrọ dị elu maka ụdị 5 phosphodiesterase. Ụfọdụ data na-egosi na nhọrọ ya na mmetụta mgbochi ya na ụdị phosphodiesterase 5 dị mma karịa ndị ọzọ phosphodiesterase ụdị 5 inhibitors. Ụdị phosphodiesterase inhibitors dị ole na ole.

Njirimara ọgwụ na ngwa

1. Mgbe ejiri ya na CYP 3A4 inhibitors (dị ka ritonavir, indinavir, saquinavir, ketoconazole, itraconazole, erythromycin, wdg), ọ nwere ike igbochi metabolism nke ọgwụ a n'ime imeju, ọ na-abawanye ụbara plasma, na-agbatị ọkara ndụ, ma na-abawanye ụba nke mmeghachi omume ọjọọ, mgbanwe ihu ihu, hypotcial (mmeghachi omume na-adịghị mma, isi ọwụwa, mgbanwe ihu igwe, mgbanwe ihu igwe, ọdịdị ihu ihu, mgbanwe ihu ihu, ọdịdị ihu, hypotcial. priapism). Ekwesịrị izere ọgwụ a na ritonavir na indinavir. Mgbe ejiri ya na erythromycin, ketoconazole na itraconazole, oke ọgwụ a ekwesịghị ịfe 5 mg, yana ketoconazole na itraconazole ekwesịghị gafere 200 mg.
2. Ndị ọrịa na-ewere nitrates ma ọ bụ na-anata ọgwụgwọ inye onyinye nitric oxide kwesịrị izere iji ọgwụ a na ngwakọta. Usoro ya nke ime ihe bụ ịbawanye ụba nkeitinye uche nke cGMP, na-ebute mmetụta antihypertensive na-abawanye na ụbara obi. Mgbe ejiri ya na ndị na-egbochi α-receptor, ọ nwere ike ịkwalite mmetụta antihypertensive ma bute hypotension. Ya mere, a machibidoro iji ọgwụ a maka ndị na-eji α-receptor blockers. Nri dị oke abụba (30% nke kalori abụba) enweghị mmetụta dị ukwuu na pharmacokinetics nke otu ọgwụ ọnụ nke 20 mg nke ọgwụ a, yana nri nwere oke abụba (karịa 55% nke kalori abụba) nwere ike ịgbatị oge kacha elu nke ọgwụ a ma belata mkpokọta ọbara nke ọgwụ a kacha elu bụ ihe dịka 18%.

Pharmacokinetics
A na-etinye ya ngwa ngwa mgbe nchịkwa ọnụ gasịrị, bioavailability zuru oke nke mbadamba ụrọ bụ 15%, na nkezi oge maka elu bụ 1h (0.5-2h). Ngwọta ọnụ 10mg ma ọ bụ 20mg, nkezi oge kacha elu bụ 0.9h na 0.7h, nkezi mkpokọta plasma kacha elu bụ 9µg / L na 21µg / L, n'otu n'otu, na oge mmetụta ọgwụ nwere ike iru 1h. Ọnụ ọgụgụ njikọ protein nke ọgwụ a bụ ihe dịka 95%. 1.5h mgbe otu mkpụrụ ọgwụ 20 mg gasịrị, ọdịnaya ọgwụ na semen bụ 0.00018% nke dose ahụ. A na-emepụta ọgwụ ahụ karịsịa n'ime imeju site na cytochrome P450 (CYP) 3A4, na obere ego na-emepụta site na CYP 3A5 na CYP 2C9 isoenzymes. Isi metabolite bụ M1 nke e guzobere site na dethylation nke usoro piperazine nke ọgwụ a. M1 nwekwara mmetụta nke igbochi phosphodiesterase 5 (ihe dị ka 7% nke mkpokọta arụmọrụ), yana ntinye ọbara ya dị ihe dịka 26% nke ntinye ọbara nne na nna. , na enwere ike imeziwanye metabolized. Ọnụego mwepu nke ọgwụ n'ụdị metabolites na feces na mmamịrị dị ihe dịka 91% ruo 95% na 2% ruo 6% n'otu n'otu. Ọnụego mkpochapụ n'ozuzu bụ 56 L kwa elekere, na ọkara ndụ nke ogige nne na nna na M1 bụ ihe dịka awa 4 ruo 5.