I-Vardenafil Dihydrochloride Ukuphatha I-Erectile Dysfuction 224785-91-5

Isenzo samakhemisi
Lesi sidakamizwa siyi-phosphodiesterase Type 5 (PDE5) inhibitor. Ukuphathwa ngomlomo kwalesi sidakamizwa kungathuthukisa ngempumelelo ikhwalithi nobude besikhathi sokwenziwa, futhi kuthuthukise inani lempumelelo yempilo yezocansi ezigulini zesilisa ezine-erectile dysfunction. Ukuqalwa kanye nokugcinwa kwe-penile erection kuhlobene nokuphumuza kwamangqamuzana ama-cavernosal abushelelezi emisipha, futhi i-cyclic Guanosine Monophosphate (CGMP) ngumlamuli wokuphumula kwamangqamuzana emisipha ama-cavernosal. Lesi sidakamizwa sivimbela ukubola kwe-CGMP ngokuvimbela i-phosphodiesterase yohlobo 5, ngaleyo ndlela kubangele ukunqwabelana kwe-CGMP, ukuphumula kwemisipha ebushelelezi ye-Corpus Casernosum, kanye nokwakhiwa kwepipi. Uma kuqhathaniswa ne-phosphodeesterase i-Isozymes 1, 2, 3, 4, no-6, lesi sidakamizwa sinokukhetha okuphezulu kohlobo 5 phosphodierase. Eminye imininingwane ikhombisa ukuthi ukukhethwa kwayo nokukhetha okuvinjelwe ku-phosphodiesterase uhlobo 5 kungcono kunezinye izinhlobo ze-phosphodiesterase. Thayipha ama-phosphodiesterase inhibitors ambalwa.

Izakhiwo zokwelapha kanye nezinhlelo zokusebenza

1. Lapho isetshenziswa kanye ne-CCPS 3A4 inhibitors (enjengeRitonavir, i-Indinavir, SAQUINAVIR, i-itrronazole, i-actifing, i-hycotension, njenge-hypotension, visual Izinguquko, ikhanda, ukugcwala kobuso, i-priapism). Lesi sidakamizwa kufanele sigwenywe ngokuhlanganiswa neRitonavir ne-Indinavir. Lapho isetshenziswa ngokuhlanganiswa ne-erythromycin, i-ketoconazole, ne-iTraconazole, umthamo omkhulu walesi sidakamizwa akufanele udlule ku-5 mg, futhi umthamo we-ketoconazole ne-iTraconazole akufanele ngedlule ama-200 mg.
2. Iziguli ezithatha ama-nitrate noma ukwamukela ukwelashwa kwe-nitric oxide donor kufanele zigweme ukusebenzisa lesi sidakamizwa ngokuhlanganiswa. Indlela yayo yesenzo ukuthuthukisaUkuhlushwa kwe-CGMP, okuholele ekuthuthukiseni umphumela we-antihypererance umphumela kanye nokukhuphuka kwenhliziyo. Lapho isetshenziswa kanye nama-α-receptor blockers, ingathuthukisa umphumela we-antihyperance futhi iholele kwi-hypotension. Ngakho-ke, ukusetshenziswa kwalesi sidakamizwa kuyenqatshelwe labo abasebenzisa ama-α-receptor blockers. Ukudla okunamafutha aphakathi nendawo (ama-30% ama-kilojoule amafutha) akuzange kube nomphumela obalulekile kuma-pharmacokinetics umthamo owodwa womlomo we-20 mg walesi sidakamizwa futhi unciphise ukugcwala kwegazi ngalesi sidakamizwa cishe i-18%.

Pharmacokinetics
Itholwa ngokushesha ngemuva kokuphathwa ngomlomo, i-Bioavailability ephelele yethebhulethi yomlomo ingu-15%, futhi isikhathi esiphakathi sokuphakama kwe-1h (0.5-2h). Isixazululo se-Oral 10mg noma i-20mg isikhathi esiphakeme esiphakeme ngu-0.9h no-0.7h, i-auppential plasma yokuhlushwa yi-9μg / l kanye ne-21μg / l, futhi isikhathi somphumela wezidakamizwa singafinyelela ku-1h. Izinga lokubopha lamaprotheni kwalesi sidakamizwa cishe ngama-95%. 1.5h ngemuva komthamo owodwa womlomo we-20 mg, okuqukethwe kwezidakamizwa ku-semin kungu-0.00018% wethamo. Lesi sidakamizwa ikakhulukazi sihlanjululwa esibindini nguCytochrome P450 (CCPE) 3a4, kanti inani elincane lihlaselwe yi-CCP 3A5 kanye ne-CUCK 2c9 Isoenzymes. I-metabolite eyinhloko ngu-M1 eyakhiwa ukugcwala kwesakhiwo sePiperArazine yalolu phore. I-M1 futhi inomphumela wokuvimbela i-phosphodiestase 5 (cishe ama-7% okusebenza ngokuphelele), futhi ukugxila kwegazi kwalo cishe kungu-26% wokuhlushwa kwegazi kwabazali. , futhi ingaphinde ihlanganiswe. Amanani entengo ezidakamizwa ngesimo se-metabolites ku-feeces kanye nomchamo cishe ama-91% kuya ku-95% no-2% kuya ku-6%, ngokulandelana. Izinga eliphelele lokuthola imvume lingu-56 l ngehora, futhi izimpilo ze-Half of the Parent Compound kanye ne-M1 zingamahora ama-4 kuye kwangama-5.