I-Vardenafil Dihydrochloride Ukunyanga i-Erectile Dysfunction 224785-91-5

Isenzo se-Pharmacological
Eli chiza luhlobo lwe-phosphodiesterase 5 (PDE5) inhibitor. Ukulawulwa komlomo kweli chiza kunokuphucula ngokufanelekileyo umgangatho kunye nobude bexesha lokumiswa, kunye nokuphucula izinga lempumelelo yobomi besondo kwizigulane zamadoda ezine-erectile dysfunction. Ukuqaliswa kunye nokugcinwa kwe-penile erection kuhambelana nokuphumla kweeseli ze-cavernosal smooth muscle, kunye ne-cyclic guanosine monophosphate (cGMP) ngumlamli wokuphumla kweeseli ze-cavernosal smooth muscle. Eli chiza lithintela ukubola kwe-cGMP ngokuthintela uhlobo lwe-phosphodiesterase lwe-5, ngaloo ndlela lubangela ukuqokelela kwe-cGMP, ukuphumla kwe-muscle egudileyo ye-corpus cavernosum, kunye nokumiswa kwepenis. Xa kuthelekiswa ne-phosphodiesterase isozymes 1, 2, 3, 4, kunye ne-6, eli chiza linokukhethwa okuphezulu kohlobo lwe-5 phosphodiesterase. Ezinye iinkcukacha zibonisa ukuba ukhetho lwayo kunye nefuthe lokuthintela kwi-phosphodiesterase uhlobo lwe-5 lungcono kunezinye i-phosphodiesterase type 5 inhibitors. Uhlobo lwe-phosphodiesterase inhibitors lumbalwa.

Iipropati zonyango kunye nezicelo

1. Xa isetyenziswe kunye ne-CYP 3A4 inhibitors (efana ne-ritonavir, indinavir, saquinavir, ketoconazole, itraconazole, i-erythromycin, njl.), inokuthintela imetabolism yeli chiza kwisibindi , inyusa i-plasma concentration, yandisa i-half-life, kwaye yandisa i-half-life, kwaye yandisa i-hypotension, utshintsho olubonakalayo, utshintsho olubonakalayo ukugungxula, ipriapism). Eli chiza kufuneka liphetshwe lidibene ne-ritonavir kunye ne-indinavir. Xa isetyenziswe ngokudibeneyo ne-erythromycin, i-ketoconazole, kunye ne-itraconazole, umthamo ophezulu weli chiza akufanele udlule i-5 mg, kwaye umthamo we-ketoconazole kunye ne-itraconazole akufanele udlule i-200 mg.
2. Izigulane ezithatha i-nitrate okanye ezifumana unyango lwe-nitric oxide donor kufuneka zigweme ukusebenzisa eli chiza ngokudibeneyo. Indlela yayo yokwenza kukwandisa ngakumbiukuxinwa kwe-cGMP, okukhokelela ekuphuculweni kwempembelelo ye-antihypertensive kunye nokunyuka kwentliziyo. Xa isetyenziswe kunye ne-α-receptor blockers, inokunyusa umphumo we-antihypertensive kwaye ikhokelela kwi-hypotension. Ngoko ke, ukusetyenziswa kwesi sidakamizwa akuvumelekanga kulabo basebenzisa i-α-receptor blockers. Ukutya okunamafutha aphakathi (i-30% yeekhalori ezinamafutha) kwakungenayo impembelelo ebalulekileyo kwi-pharmacokinetics yedosi yomlomo omnye we-20 mg yeli chiza, kunye nokutya okunamafutha aphezulu (ngaphezu kwama-55% eekhalori ezinamafutha) kunokwandisa ixesha eliphakamileyo leli chiza kunye nokunciphisa uxinzelelo lwegazi lweli chiza Incopho malunga ne-18%.

Pharmacokinetics
Ifakwe ngokukhawuleza emva kokulawulwa komlomo, i-bioavailability epheleleyo ye-tablet yomlomo yi-15%, kwaye ixesha eliphakathi kwe-peak yi-1h (0.5-2h). Isisombululo somlomo i-10mg okanye i-20mg, ixesha eliphakathi kwe-0.9h kunye ne-0.7h, i-concentration ye-plasma ye-peak ye-avareji yi-9µg / L kunye ne-21µg / L, ngokulandelanayo, kunye nobude besiphumo seziyobisi sinokufikelela kwi-1h. Izinga lokubophelela kwiprotheyini kweli chiza limalunga nama-95%. I-1.5h emva komthamo omnye womlomo we-20 mg, umxholo weziyobisi kwi-semen yi-0.00018% yedosi. Ichiza lisetyenziswa kakhulu kwisibindi nge-cytochrome P450 (CYP) 3A4, kwaye ixabiso elincinci lihlanjululwe yi-CYP 3A5 kunye ne-CYP 2C9 isoenzymes. I-metabolite ephambili yi-M1 eyenziwa yi-deethylation yesakhiwo se-piperazine yeli chiza. I-M1 nayo inefuthe lokuvimbela i-phosphodiesterase 5 (malunga ne-7% ye-efficacy iyonke), kunye ne-concentration yayo yegazi malunga ne-26% yoxinaniso lwegazi lomzali. , kwaye inokuphinda isetyenziswe imetabolism. Amazinga okukhutshwa kweziyobisi ngendlela ye-metabolites kwi-feces kunye nomchamo malunga ne-91% ukuya kwi-95% kunye ne-2% ukuya kwi-6%, ngokulandelanayo. Ireyithi yokucoca iyonke yi-56 L ngeyure, kwaye isiqingatha-ubomi bekhomponi yomzali kunye ne-M1 zombini malunga ne-4 ukuya kwiiyure ze-5.