ʻO Vardenafil Dihydrochloride e mālama ana i ka erectile dysfunction 224785-91-5

Hana lāʻau lapaʻau
ʻO kēia lāʻau lapaʻau he phosphodiesterase type 5 (PDE5) inhibitor. Hiki i ka hoʻokele waha o kēia lāʻau lapaʻau ke hoʻomaikaʻi maikaʻi i ka maikaʻi a me ka lōʻihi o ke kūkulu ʻana, a hoʻomaikaʻi i ka helu kūleʻa o ke ola wahine i nā kāne maʻi me ka erectile dysfunction. ʻO ka hoʻomakaʻana a me ka mālamaʻana i ka penile e pili ana i ka hoʻomahaʻana o nā puʻupuʻu puʻupuʻu maʻemaʻe o ka cavernosal, a me ka cyclic guanosine monophosphate (cGMP) he mea hoʻoponopono i ka hoʻomahaʻana o nā puʻupuʻu puʻupuʻu cavernosal. Ke pale nei kēia lāʻau lapaʻau i ka decomposition o cGMP ma ke kāohi ʻana i ka phosphodiesterase type 5, a laila e hoʻoulu ai i ka cGMP, ka hoʻomaha ʻana o ka ʻiʻo maʻemaʻe o ka corpus cavernosum, a me ke kūkulu ʻana o ka penis. Ke hoʻohālikelike ʻia me phosphodiesterase isozymes 1, 2, 3, 4, a me 6, he kiʻekiʻe ke koho ʻana o kēia lāʻau no ka type 5 phosphodiesterase. Hōʻike kekahi mau ʻikepili i kāna koho koho a me ka hopena inhibitory ma ka phosphodiesterase type 5 ʻoi aku ka maikaʻi ma mua o nā mea hoʻopaneʻe phosphodiesterase type 5. He liʻiliʻi nā ʻano phosphodiesterase inhibitors.

Nā Waiwai Lapaʻau a me nā noi

1. Ke hoʻohana pū ʻia me CYP 3A4 inhibitors (e like me ritonavir, indinavir, saquinavir, ketoconazole, itraconazole, erythromycin, a me nā mea ʻē aʻe), hiki ke kāohi i ka metabolism o kēia lāʻau i loko o ke ake, hoʻonui ia i ka ʻike plasma, hoʻolōʻihi i ka hapalua o ke ola, a hoʻonui i ka ulu ʻana o nā hopena ʻino, hoʻololi ʻana i nā ʻano like ʻole. priapism). Pono e pale ʻia kēia lāʻau lapaʻau me ka ritonavir a me indinavir. Ke hoʻohana pū ʻia me ka erythromycin, ketoconazole, a me itraconazole, ʻaʻole pono ka nui o ka nui o kēia lāʻau ma mua o 5 mg, a ʻaʻole pono ka nui o ka ketoconazole a me itraconazole ma mua o 200 mg.
2. Pono nā po'e ma'i e lawe ana i ka nitrate a i 'ole e loa'a ana i ka nitric oxide donor therapy e ho'ohana pū i kēia lā'au. ʻO kāna ʻano hana e hoʻonui hou i kaka nui o ka cGMP, ka hopena i ka hopena antihypertensive a hoʻonui i ka puʻuwai puʻuwai. Ke hoʻohana pū ʻia me nā blockers α-receptor, hiki iā ia ke hoʻonui i ka hopena antihypertensive a alakaʻi i ka hypotension. No laila, pāpā ʻia ka hoʻohana ʻana i kēia lāʻau lapaʻau no ka poʻe e hoʻohana ana i ka α-receptor blockers. ʻO ka meaʻai momona momona (30% o nā calorie momona) ʻaʻohe hopena koʻikoʻi i ka pharmacokinetics o ka waha waha hoʻokahi o 20 mg o kēia lāʻau lapaʻau, a ʻo ka meaʻai momona kiʻekiʻe (ʻoi aku ma mua o 55% o nā calorie momona) hiki ke hoʻolōʻihi i ka manawa kiʻekiʻe o kēia lāʻau a hoʻemi i ke kahe koko o kēia lāʻau ʻO ka piko ma kahi o 18%.

Pharmacokinetics
Hoʻopili koke ʻia ia ma hope o ka hoʻokele waha, ʻo ka bioavailability piha o ka papa waha he 15%, a ʻo ka manawa awelika e piʻi ai he 1h (0.5-2h). ʻO ka hopena waha 10mg a i ʻole 20mg, ʻo ka manawa kiʻekiʻe o ka manawa he 0.9h a me 0.7h, ʻo ka awelika kiʻekiʻe o ka plasma concentration he 9µg/L a me 21µg/L, a hiki i ka lōʻihi o ka hopena o ka lāʻau ke hiki i 1h. ʻO ka nui o ka hoʻopaʻa ʻana i ka protein o kēia lāʻau ma kahi o 95%. 1.5h ma hope o hoʻokahi waha waha o 20 mg, ʻo ka maʻi o ka lāʻau i loko o ka semen he 0.00018% o ka nui. Hoʻopili nui ʻia ka lāʻau lapaʻau i loko o ke ake e ka cytochrome P450 (CYP) 3A4, a he mea liʻiliʻi ka metabolized e CYP 3A5 a me CYP 2C9 isoenzymes. ʻO ka metabolite nui ka M1 i hoʻokumu ʻia e ka deethylation o ka piperazine structure o kēia lāʻau lapaʻau. Loaʻa i ka M1 ka hopena o ke kāohi ʻana i ka phosphodiesterase 5 (ma kahi o 7% o ka nui o ka pono), a ʻo kona ʻano koko ma kahi o 26% o ke koko koko makua. , a hiki ke hoʻololi hou ʻia. ʻO ka nui o ka excretion o nā lāʻau lapaʻau ma ke ʻano o nā metabolites i nā feces a me ka mimi ma kahi o 91% a 95% a me 2% a 6%, kēlā me kēia. ʻO 56 L ka nui o ka hoʻomaʻemaʻe ʻana i kēlā me kēia hola, a ʻo ka hapalua o ke ola o ka hui makua a me M1 he 4 a 5 mau hola.