Vardenafil Dihydrochloride Kurapa Erectile Dysfunction 224785-91-5

Pharmacological Action
Mushonga uyu iphosphodiesterase type 5 (PDE5) inhibitor. Kutungamirirwa nemuromo kwechirwere ichi kunogona kunyatso kuvandudza kunaka uye nguva ye erection, uye kugadzirisa kubudirira kwehupenyu hwepabonde muvarwere vechirume vane erectile dysfunction. Kutanga uye kuchengetedzwa kwepenile erection kwakabatana nekuzorora kwecavernosal smooth muscle cells, uye cyclic guanosine monophosphate (cGMP) murevereri wekuzorora kwecavernosal smooth muscle cells. Mushonga uyu unodzivirira kuparara kwecGMP nekudzivisa phosphodiesterase type 5, nokudaro zvichiita kuti kuunganidza cGMP, kusununguka kwemuviri wakatsetseka we corpus cavernosum, uye kumira kwepeni. Zvichienzaniswa ne phosphodiesterase isozymes 1, 2, 3, 4, uye 6, mushonga uyu une high selectivity yemhando 5 phosphodiesterase. Imwe data inoratidza kuti kusarudza kwayo uye inhibitory mhedzisiro pane phosphodiesterase type 5 zviri nani pane mamwe phosphodiesterase type 5 inhibitors. Type phosphodiesterase inhibitors vashoma.

Mishonga Properties uye Applications

1. Kana yakashandiswa pamwe chete neCYP 3A4 inhibitors (yakadai se ritonavir, indinavir, saquinavir, ketoconazole, itraconazole, erythromycin, nezvimwewo), inogona kudzivisa metabolism yechirwere ichi muchiropa , inowedzera kusanganiswa kweplasma, inowedzera hafu yeupenyu, uye inowedzera kuitika kwechiitiko, kushanduka kwemusoro, kuchinja kwemusoro, kuchinja kwehupikisi, kuchinja kwehupikisi. kurutsa, priapism). Mushonga uyu unofanirwa kudzivirirwa wakasanganiswa ne ritonavir ne indinavir. Kana inoshandiswa pamwe chete ne erythromycin, ketoconazole, uye itraconazole, chiyero chepamusoro chechirwere ichi hachifaniri kudarika 5 mg, uye ketoconazole uye itraconazole haifaniri kudarika 200 mg.
2. Varwere vanotora nitrate kana kugamuchira nitric oxide donor therapy vanofanira kudzivisa kushandisa mushonga uyu pamwe chete. Iyo nzira yekuita kwayo ndeyekuwedzera kuwedzerakuunganidzwa kweCGMP, zvichikonzera kukwidziridzwa kweantihypertensive athari uye kuwedzera kwemoyo. Kana yakashandiswa pamwe chete nea-receptor blockers, inogona kuwedzera iyo antihypertensive mhedzisiro uye kutungamirira ku hypotension. Nokudaro, kushandiswa kwechirwere ichi kunorambidzwa kune avo vari kushandisa α-receptor blockers. Chikafu chepakati-mafuta (30% yemafuta makoriyumu) ​​yakanga isina mhedzisiro yakakosha pa pharmacokinetics yemwero yemuromo ye20 mg yemushonga uyu, uye kudya kwakawanda-mafuta (kupfuura 55% yemafuta makoriyumu) ​​kunogona kurebesa nguva yepamusoro yechirwere ichi uye kuderedza kuwanda kweropa remushonga uyu Iyo yepamusoro inenge 18%.

Pharmacokinetics
Inokurumidza kutorwa mushure mekutonga kwemuromo, iyo yakakwana bioavailability yepiritsi yemuromo ndeye 15%, uye nguva yepakati yekukwira ndeye 1h (0.5-2h). Oral solution 10mg kana 20mg, avhareji yepamusoro nguva ndeye 0.9h uye 0.7h, muvhareji wepamusoro peak plasma concentration ndeye 9µg/L uye 21µg/L, zvichiteerana, uye nguva yemhedzisiro yezvinodhaka inogona kusvika 1h. Mapuroteni anosunga chiyero chemushonga uyu anenge 95%. 1.5h mushure mechikamu chimwe chete chemuromo che 20 mg, zvinodhaka zviri muurume ndeye 0.00018% yedhesi. Mushonga wacho unonyanya kushandiswa muchiropa ne cytochrome P450 (CYP) 3A4, uye zvishoma zvinogadziriswa neCYP 3A5 uye CYP 2C9 isoenzymes. Iyo huru metabolite ndeye M1 inoumbwa ne deethylation yepiperazine chimiro chemushonga uyu. M1 inewo mhedzisiro ye inhibiting phosphodiesterase 5 (inenge 7% yehuwandu hunobudirira), uye huwandu hwayo hweropa hunenge 26% yemubereki weropa. , uye inogona kuwedzeredzwa metabolized. The excretion rates yemishonga muchimiro chemetabolites mutsvina uye weti inenge 91% kusvika 95% uye 2% kusvika 6%, zvichiteerana. Iyo yakazara clearance rate ndeye 56 L paawa, uye hafu yehupenyu hwemubereki kompani uye M1 zvese zviri zviviri maawa mana kusvika mashanu.