Dzina | Vardenafil Dihydrochloride |
Nambala ya CAS | 224785-90-4 |
Mapangidwe a maselo | Chithunzi cha C23H32N6O4S |
Kulemera kwa maselo | 488.6 |
Nambala ya EINECS | 607-088-5 |
Melting Point | 230-235 ° C |
Kuchulukana | 1.37 |
Mkhalidwe wosungira | Yosindikizidwa mu youma, Sungani mufiriji, pansi pa -20 ° C |
Fomu | Ufa |
Mtundu | Choyera |
Acidity coefficient | (pKa) 9.86±0.20 (Zonenedweratu) |
VARDENAFIL(SUBJECTTOPATENTFREE);VARDENAFILHYDROCHLORIDETRIHYDRATE(SUBJECTTOPATENTFREE);2-(2-Ethoxy- 5-(4-ethylpiperazin-1-yl-1-sulfonyl)phenyl) -5-methyl-7-propyl-3H-imidazo (5,1-f) (1,2,4) triazin-4-imodzi; Vardenafilhydrochloridetrihydrate99%; VardenafilHydrochlorideTrihydrate Cas#224785-90-4ForSale; OpangaSupplybestqualityVardenafilhydrochloridetrihydrate224785-90-4CASNO.224785-90-4;FADINAF;1-[[3-(1,4-Dihydro-5-) methyl-4-oxo-7-propylimidazo[5,1-f][1,2,4]triazin-2-yl)-4-ethoxyphenyl]sulfonyl]-4-ethyl-piperazinehydrochloridetrihydrate
Pharmacological Action
Mankhwalawa ndi phosphodiesterase type 5 (PDE5) inhibitor. Kuwongolera pakamwa kwa mankhwalawa kumatha kuwongolera bwino komanso kutalika kwa nthawi yogona, komanso kupititsa patsogolo moyo wogonana mwa amuna omwe ali ndi vuto la erectile. Kuyambitsa ndi kukonza kwa penile erection kumagwirizana ndi kupumula kwa cavernosal smooth muscle cell, ndipo cyclic guanosine monophosphate (cGMP) ndi mkhalapakati wa kupumula kwa cavernosal yosalala minofu maselo. Mankhwalawa amalepheretsa kuwonongeka kwa cGMP mwa kuletsa phosphodiesterase mtundu wa 5, motero kumayambitsa kudzikundikira kwa cGMP, kupumula kwa minofu yosalala ya corpus cavernosum, ndi kukhazikika kwa mbolo. Poyerekeza ndi phosphodiesterase isozymes 1, 2, 3, 4, ndi 6, mankhwalawa ali ndi kusankha kwakukulu kwa mtundu wa 5 phosphodiesterase. Deta ina ikuwonetsa kuti kusankha kwake ndi kuletsa kwake pamtundu wa phosphodiesterase 5 kuli bwino kuposa zoletsa zina za phosphodiesterase mtundu 5. Mitundu ya phosphodiesterase inhibitors ndi yochepa.
Katundu Wamankhwala ndi Ntchito
1. Mukagwiritsidwa ntchito limodzi ndi CYP 3A4 inhibitors (monga ritonavir, indinavir, saquinavir, ketoconazole, itraconazole, erythromycin, etc.), imatha kulepheretsa kagayidwe ka mankhwalawa m'chiwindi , imawonjezera plasma ndende, imatalikitsa theka la moyo, ndikuwonjezera zochitika, kusintha kwa mutu, kusintha kwa mutu, kusintha kwa thupi, kusintha kwa thupi. kuwotcha, priapism). Mankhwalawa ayenera kupewa kuphatikiza ritonavir ndi indinavir. Mukagwiritsidwa ntchito limodzi ndi erythromycin, ketoconazole, ndi itraconazole, mlingo waukulu wa mankhwalawa sayenera kupitirira 5 mg, ndi ketoconazole ndi itraconazole sayenera kupitirira 200 mg.
2. Odwala omwe amatenga nitrates kapena kulandira chithandizo cha nitric oxide donor therapy ayenera kupewa kugwiritsa ntchito mankhwalawa pamodzi. Njira yake yochitirapo kanthu ndikuwonjezera mphamvundende ya cGMP, zomwe zimapangitsa kuti pakhale mphamvu ya antihypertensive komanso kuchuluka kwa mtima. Mukagwiritsidwa ntchito limodzi ndi α-receptor blockers, imatha kukulitsa mphamvu ya antihypertensive ndikuyambitsa kutsika kwa magazi. Choncho, kugwiritsa ntchito mankhwalawa ndikoletsedwa kwa omwe akugwiritsa ntchito α-receptor blockers. A sing'anga-mafuta zakudya (30% mafuta zopatsa mphamvu) analibe kwambiri zotsatira pa pharmacokinetics wa limodzi pakamwa mlingo wa 20 mg wa mankhwala, ndi kudya mafuta ambiri (zoposa 55% mafuta zopatsa mphamvu) akhoza kutalikitsa nthawi pachimake cha mankhwala ndi kuchepetsa ndende ya magazi a mankhwala Chimake ndi za 18%.
Pharmacokinetics
Imatengeka mwachangu pambuyo pa makonzedwe amkamwa, mtheradi wa bioavailability wa piritsi ndi 15%, ndipo nthawi yayitali kwambiri ndi 1h (0.5-2h). Oral solution 10mg kapena 20mg, nthawi yayitali kwambiri ndi 0.9h ndi 0.7h, pafupifupi nsonga yapamwamba ya plasma ndi 9µg/L ndi 21µg/L, motero, ndipo nthawi yamankhwala imatha kufika 1h. Kumanga kwa mapuloteni a mankhwalawa ndi pafupifupi 95%. 1.5h pambuyo pa mlingo umodzi wapakamwa wa 20 mg, mankhwala omwe ali mu umuna ndi 0.00018% ya mlingo. Mankhwalawa amapangidwa makamaka m'chiwindi ndi cytochrome P450 (CYP) 3A4, ndipo pang'ono amapangidwa ndi CYP 3A5 ndi CYP 2C9 isoenzymes. Metabolite yayikulu ndi M1 yopangidwa ndi deethylation ya piperazine ya mankhwalawa. M1 imakhalanso ndi zotsatira zoletsa phosphodiesterase 5 (pafupifupi 7% ya mphamvu yonse), ndipo magazi ake ali pafupi ndi 26% ya magazi a kholo. , ndipo imatha kusinthidwanso. The excretion mitengo ya mankhwala mu mawonekedwe a metabolites mu ndowe ndi mkodzo pafupifupi 91% mpaka 95% ndi 2% mpaka 6%, motero. Chilolezo chonse ndi 56 L pa ola, ndipo theka la moyo wa makolo ndi M1 onse ndi maola 4 mpaka 5.