Vardenafil Dihydrochloride Kuvura Imikorere idahwitse 224785-91-5

Igikorwa cya farumasi
Uyu muti ni fosifisiyose yubwoko bwa 5 (PDE5) inhibitor. Gucunga umunwa uyu muti birashobora kuzamura neza ubwiza nigihe cyigihe cyo gutera, kandi bikazamura intsinzi yubuzima bwimibonano mpuzabitsina kubarwayi babagabo bafite imikorere mibi. Gutangiza no gufata neza imboro bifitanye isano no kuruhura ingirabuzimafatizo zoroheje za cavernosal, kandi cyclic guanosine monophosphate (cGMP) ni umuhuza wo kuruhura ingirabuzimafatizo zoroheje. Uyu muti urinda kwangirika kwa cGMP uhagarika fosifisiyose yubwoko bwa 5, bityo bigatuma habaho kwirundanya kwa cGMP, kuruhura imitsi yoroshye ya corpus cavernosum, no gushiraho igitsina. Ugereranije na foshodiesterase isozymes 1, 2, 3, 4, na 6, uyu muti ufite amahitamo menshi kubwoko bwa 5 bwa fosifori. Amakuru amwe yerekana ko guhitamo kwayo ningaruka zo guhagarika ubwoko bwa fosifodiyesterase ya 5 aruta izindi fosifisiyose yubwoko bwa 5 inhibitor. Andika fosiforiesterase inhibitor ni mbarwa.

Ibyiza byubuvuzi nibisabwa

1. Uyu muti ugomba kwirinda ufatanije na ritonavir na indinavir. Iyo ikoreshejwe ifatanije na erythromycine, ketoconazole, na itraconazole, igipimo ntarengwa cy’ibi biyobyabwenge ntigishobora kurenga mg 5, kandi ikinini cya ketoconazole na itraconazole ntigishobora kurenga mg 200.
2. Abarwayi bafata nitrate cyangwa bakira imiti ya nitric oxyde itanga imiti bagomba kwirinda gukoresha uyu muti hamwe. Uburyo bwibikorwa ni ugukomeza kongerakwibumbira hamwe kwa cGMP, bikavamo imbaraga zo kurwanya antivypertensive no kongera umuvuduko wumutima. Iyo ikoreshejwe hamwe na α-reseptor blokers, irashobora kongera imbaraga za antihypertensive kandi iganisha kuri hypotension. Kubwibyo, gukoresha uyu muti birabujijwe kubakoresha α-reseptor blokers. Indyo yuzuye ibinure (30% ya karori yibinure) nta ngaruka nini yagize kuri farumasi yubuvuzi bwa dose imwe yo mu kanwa ya mg 20 yibi biyobyabwenge, kandi indyo yuzuye ibinure byinshi (birenga 55% bya karori yibinure) irashobora kongera igihe cyigihe cyibiyobyabwenge kandi bikagabanya umuvuduko wamaraso wibiyobyabwenge Iyi mpinga igera kuri 18%.

Imiti ya farumasi
Ihindurwa vuba nyuma yubuyobozi bwo munwa, bioavailability ya tablet yo mu kanwa ni 15%, naho igihe cyo hejuru cyo hejuru ni 1h (0.5-2h). Igisubizo cyo mu kanwa 10mg cyangwa 20mg, impuzandengo yigihe cyo hejuru ni 0.9h na 0.7h, impuzandengo ya plasma yibipimo ni 9µg / L na 21µg / L, kandi igihe cyo gufata ibiyobyabwenge gishobora kugera kuri 1h. Igipimo cya poroteyine gihuza uyu muti ni 95%. 1.5h nyuma yumunwa umwe wa mg 20 mg, ibiyobyabwenge mumasohoro ni 0.00018% yumuti. Uyu muti ukoreshwa cyane mu mwijima na cytochrome P450 (CYP) 3A4, kandi umubare muto ukoreshwa na CYP 3A5 na CYP 2C9 isoenzymes. Metabolite nyamukuru ni M1 ikorwa na deethylation yimiterere ya piperazine yibi biyobyabwenge. M1 ifite kandi ingaruka zo kubuza fosifodiyesterase 5 (hafi 7% yingirakamaro zose), kandi amaraso yayo agera kuri 26% yibitekerezo byamaraso yababyeyi. , kandi birashobora gukomeza guhinduranya. Igipimo cyo gusohora ibiyobyabwenge muburyo bwa metabolite mumyanda ninkari bigera kuri 91% kugeza 95% na 2% kugeza 6%. Igipimo rusange cyo gukuraho ni 56 L ku isaha, naho kimwe cya kabiri cyubuzima bwababyeyi hamwe na M1 byombi ni amasaha 4 kugeza kuri 5.