Lub npe | Vardenafil daydrocide |
Tus lej | 22475-90-4 |
Molecular Cov Qauv | C23hn32n6o4s |
Molecular hnyav | 488.6 |
Einecs tooj | 607-088-5 |
Melting taw tes | 230-235 ° C |
Ceev | 1.37 |
Chaw Cia Khoom | Muab ntim rau hauv qhuav, khaws rau hauv lub freezer, hauv qab -20 ° C |
Puab | Hmoov |
Xim | Xim dawb |
Acidity Coefficient | (PMA) 9.86 ± 0.20 (kwv yees) |
Vardenafil (SporttomtTFree); Vardenafilhydrodrotiderhydrate (contoptopatentfree); 2- (2-uthoxy- 5- (4-Ethylppiperazin-1-YL-1-Sulfonyl) Phenylas Phenyl) -5-Imm-3H-F) (1,2,4) Triazin-4-Ib; Vardenafilhydrodrotidethydrate99; Vasgenafilhydrodrotidethihlidethirydrate CAS # 224785-90-4forsale; Chaw Tsim Tshuaj Tsim Kev Tsim Khoom Siv DetigrdalAralAriSrishydrate22475-90-4caso.224785-90-4; Fadinaf; 1 - [3- (1,4-Dihydrro-5- Methyl-4-Oxo-7-Propylimidazo [5,1,4] Triazin-ethylyl] -4-Ethyl-Piperazinehdroidetrihydrate
Pharmacological txiav txim siab
Cov tshuaj no yog hom phosphodiesterase 5 (PDE5) inhibitor. Kev tswj hwm qhov ncauj ntawm cov tshuaj no tuaj yeem txhim kho qhov zoo thiab ntev ntawm kev ua kom tiav, thiab txhim kho kev ua tiav ntawm kev ua kev sib deev hauv cov txiv neej ua haujlwm nrog erectile dysfunction. Kev pib thiab kev saib xyuas ntawm Cenpile erection yog cuam tshuam rau lub sijhawm so ntawm lub hlwb ua kom haum rau lub cev muaj zog ntawm lub cavernosal du cov hlwb hlwb. Cov tshuaj no tiv thaiv cov decomposition ntawm cgmp los ntawm inhibiting ntawm CGMP, cov so ntawm cov leeg du ntawm lub corpus cavernum, thiab erection ntawm tus qau. Piv nrog phosphodiesterase isozymes 1, 2, 3, 4, thiab 6, cov tshuaj no muaj kev xaiv siab rau hom 5 phosphodiesterase Qee cov ntaub ntawv qhia tias nws txoj kev xaiv thiab kev tiv thaiv kev ua haujlwm ntawm Phosphodiesterase Hom 5 yog qhov zoo dua li lwm yam phosphodiesterase hom 5 inibitors. Hom phosphodiesterorse inibitors muaj ob peb.
Medicinal thaj chaw thiab cov ntawv thov
1. Thaum siv ua ke nrog CYP 3A4 inibitors (xws li cov ntshav siab, thiab muaj peev xwm ua rau muaj kev sib raug zoo, thiab muaj peev xwm ua rau muaj kev cuam tshuam rau lub neej Hloov pauv, mob taub hau, ntsej muag flushing, iabism). Cov tshuaj no yuav tsum zam rau kev sib xyaw nrog ritonavir thiab indinavir. Thaum siv ua ke nrog erythromycin, ketoconazole, thiab koob ntau tshaj plaws ntawm cov tshuaj no yuav tsum tsis pub tshaj 5 mg, thiab cov koob tshuaj ntawm Ketoconazole thiab Itraconazole yuav tsum tsis pub tshaj 200 mg.
2. Cov neeg mob noj Nitrates lossis tau txais NITRum Oxide tus mob kev kho mob yuav tsum zam kev siv cov tshuaj no ua ke. Nws cov tshuab ntawm kev nqis tes ua yog kom nce ntxivconcentration ntawm CGMP, ua rau muaj kev txhim kho antihypertensive thiab nce lub plawv dhia. Thaum siv ua ke nrog α-receptor blockers, nws tuaj yeem txhim kho cov nyhuv antihizertive thiab ua rau hypotension. Yog li ntawd, kev siv cov tshuaj no raug txwv rau cov uas siv α-cov neeg siv nyiaj tau. Ib qho kev noj zaub mov nruab nrab (30% ntawm cov roj ntsha tsis muaj roj) tsis muaj cov tshuaj ntawm cov tshuaj no thiab muaj ntau dua 55% ntawm cov tshuaj muaj roj ua ke ntawm cov tshuaj no yog li 18%.
Pharmaconinetics
Nws yog nrawm dhau los tom qab kev tswj hwm qhov ncauj, qhov tseeb bioavailability ntawm cov ntsiav tshuaj yog 15%, thiab nruab nrab lub sijhawm rau ncov yog 1h (0.5-2h). Qhov ncauj daws 10mg lossis 20mg, lub sijhawm nruab nrab yog 0.30H thiab 0.30h, nruab nrab lub siab chim siab yog 9μg / l, thiab lub sijhawm ntawm cov tshuaj muaj peev xwm ncav cuag 1h. Cov protein khi tus nqi ntawm cov tshuaj no yog kwv yees li 95%. 1.5H tom qab ib qho ntawm ib qho ntawm 20 mg, cov ntsiab lus siv tshuaj nyob hauv cov phev yog 0.00018% ntawm koob tshuaj. Cov tshuaj feem ntau yog metabolized nyob rau hauv daim siab los ntawm cytochrome P450 (CYP) 3A4, thiab ib qho me me yog metabolized los ntawm CYP 3A5 thiab CYP 2C9 ISOZYYMES. Lub Metabolite tseem ceeb yog M1 tsim los ntawm Deethylation ntawm Piperazine qauv ntawm cov tshuaj no. M1 kuj muaj qhov cuam tshuam ntawm ehibitingase 5 (txog 7% ntawm tag nrho cov kev ua kom cov ntshav tau yog li 26% ntawm cov niam txiv cov ntshav siab. , thiab tuaj yeem txuas ntxiv metabolized. Tus nqi ua yeeb yam ntawm cov tshuaj nyob rau hauv daim ntawv ntawm cov metabolites hauv cov quav thiab cov zis yog li 91% rau 95% thiab 6%, feem. Tus lej tshem tawm tag nrho tus nqi yog 56 L toj ib teev, thiab ib nrab lub neej ntawm niam txiv qhov sib xyaw thiab M1 muaj ob txog 4 txog 5 teev.