I-Varddial Dihydrochrochrocyer inyanga i-irefleunction ye-224785-51-5
Iinkcukacha zemveliso
| Igama | I-Varddenil Dihydrochrochrochrochrochloride |
| Inombolo ye-CAS | I-224785-90-4 |
| Ifomula yemolekyuli | C23h32n6s |
| Ubunzima bemolekyuli | 488.6 |
| Inombolo ye-einecs | 607-088-5 |
| Indawo yokunyibilika | 230-235 ° C |
| Ukuxinana | 1.37 |
| Imeko yokugcina | Itywinwe kwi-freezer, engaphantsi kwe-42 ° C |
| Ifom | Umgubo |
| Umbala | Mhlophe |
| I-acididity ilunge | (PKA) 9.86 ± 0.20 (iqikelele) |
Izithethantonye
IVarddenil (i-LovetictothatentFree); IVarddenilhyddrochridrachridDeridDrate (2- (2-ethoxy- 5- (4-Esyylpiperazin-1-YL-Sul-Sul-Sulyl-7-I-METHyL-7-I-MERPYL-3H-IMIDAZO (1,2,4) UTriazin-4-mnye; IVarddenilhydrochridricheridrate99%; IVarddenilhydrochridrizeridlidDractDract ye-CASS # 224785-90-40forsale; I-VoestRESSUSTECMULDULDECOMDDEREDDROMDHROFROCHYLDHYDKRHROIDRY224785-40CASno.24785.4- (1,4-(1-) methyl-4-oxo-7-propylimidazo[5,1-f][1,2,4]triazin-2-yl)-4-ethoxyphenyl]sulfonyl]-4-ethyl-piperazinehydrochloridetrihydrate
Isiphumo se-Pharmacociological
Inketho ye-Pharmacological
Eli chiza li-Phosphedtrase chwether 5 (PD5) i-inhibitor. Ulawulo lweli chiza elinokuphucula ngokufanelekileyo umgangatho kunye nexesha lolwakhiwo, kunye nokuphucula imigangatho yempumelelo yobomi besini kwizigulana ezingamadoda ezine-erectile. Ukuqaliswa kunye nokugcinwa kolwakhiwo lweNtlalondi kuhambelana nokuphumla kweeseli ze-cavernos, kunye ne-cyclic guanosine monophotele (CGMP) ngumlamli wokuphumla kweeseli ze-cavernossal. Eli chiza lithintela ukubola kwe-CGMP ngokuthintela uhlobo lwe-phosphodiesterase yohlobo lwesi-5, ngaloo ndlela kubangela ukuqokelelwa kwe-CGMP, ukucutha komsipha ogudileyo we-Corpus Clovernosum, kunye nokwakhiwa kwePeris. Xa kuthelekiswa ne-phosphodiesterase iboymes 1, 2, 3, 4, kunye ne-6, eli chiza linokukhetha okuphezulu kuhlobo 5 phosphodiesterase. Ezinye idatha zibonisa ukuba ukukhetha kwayo kunye nefhinitory kwiPhemidiesterase TraidTErase Chwether 5 kungcono kunezinye ii-phosphoidterase cuters. Chwetheza i-phosphodimedterase infistiesterase infiritors bambalwa.
Iipropathi zonyango kunye nezicelo
1. Xa isetyenziswa kunye ne-cyp 3aitors (i-ritonavir, i-Indinavir, i-Saquinavir, i-Itquinavin, inokuthintela isiqingatha sendlela, ikwandisa imeko yokuphendula phantsi (njengoko I-hypoteren, utshintsho olubonakalayo, intloko ebuhlungu, ukugungxulwa kobuso, iprintapism). Eli chiza lifanele lithintelwe ngokudibeneyo neRitonavir kunye ne-Indinavir. Xa isetyenziswa ngokudibeneyo ne-erythromycin, i-ketocozole, idosi ephezulu yeli chiza akufuneki idlule kwi-5 mg, kwaye idosi ye-ketoconazole kwaye i-Itraconale ayifanele idlule kwi-200 mg.
2. Izigulana ezithatha i-nitrate okanye ifumana unyango lwe-witric oxide oxide kufuneka likuphephe ukusebenzisa eli chiza kwindibaniselwano. Indlela yayo yesenzo kukwandisa ngakumbiUkugxininiswa kwe-CGMP, kukhokelela kwimpembelelo ephuculweyo ye-antihypergert kunye nokunyuka kwentliziyo. Xa isetyenziswa kunye ne-α-rector blockers, inokuphucula ifuthe elinamandla kwaye likhokelele kwi-hypoteren. Ke ngoko, ukusetyenziswa kwaloo machiza akuvumelekanga abo basebenzisa iibhloko ze-α-rectors. Ukutya okuphakathi kwamafutha (ama-30% eekhalori ezinamafutha) wayengenampembelelo kwi-pharmacokinetics yedomey enye yomlomo ye-20 mg (kunye ne-55% yeekhalori ezinamafutha) enokuyindisa i-Teak Litter libe malunga ne-18%.
I-pharmacokinetics
Kuyaqondakala ngokukhawuleza emva kolawulo lomlomo, i-biaaible yebhayili yetafile yomlomo yi-15%, kunye nexesha eliphakathi, kunye nexesha eliphakathi lokuyithoba yi-1h (0.5-2). Isisombululo somlomo i-10mg okanye i-20mg, ixesha eliphakathi le-0.9h kunye ne-0.7H, i-Platema yePlasma yePlasma yi-9μ2 kwi-21μg / ngokulandelelana, kwaye ngokulandelelana, kunye nexesha lokusebenza kweziyobisi linokufikelela kwi-1h. Ixabiso lokubopha leprotein lali liyeza limalunga ne-95%. 1.5h emva kwedosi enye yomlomo ye-20 mg, umxholo weziyobisi kwi-semen yi-0.00018% yedosi. Eli chiza liyimigqaliselo ikakhulu kwisibindi nge-cytochrome p450 (i-cyp) 3a -4, kunye nexabiso elincinci lifakwe kwi-cyp 3a5c9 isoebymes. I-metabolite ye-metabolite yi-M1 yenziwa yi-Demerating yobume be-piperazine yeli chiza. I-M1 ikwanempembelelo yokuvula i-phosphodiesterase 5 (malunga ne-7% yokusebenza kakuhle), kwaye uxinzelelo lwegazi lwayo lumalunga ne-26% yoxinzelelo lwegazi lomzali. , kwaye inokuqhubeka nemetriki. Amanqanaba okuzihlaziya amachiza akwimo yeMetabolites kwizitya kunye nomchamo malunga ne-91% ukuya kwi-95% ne-2% ukuya kwi-6%, ngokulandelelana. Ireyithi yeyonke i-56 L i-56 L i-56 l ngeyure, kwaye i-tid-ubomi bomzali kunye ne-M1 ziiyure ezingama-4 ukuya kwezi-5.
