Vardenafil Dihydrochloride Kho Erectile Dysfunction 224785-91-5

Pharmacological Action
Cov tshuaj no yog phosphodiesterase type 5 (PDE5) inhibitor. Kev tswj hwm qhov ncauj ntawm cov tshuaj no tuaj yeem txhim kho qhov zoo thiab lub sijhawm ntawm erection, thiab txhim kho qhov ua tiav ntawm kev sib deev lub neej hauv cov txiv neej cov neeg mob uas muaj erectile kawg. Kev pib thiab kev saib xyuas ntawm penile erection yog cuam tshuam nrog kev so ntawm cov leeg nqaij pob txha, thiab cyclic guanosine monophosphate (cGMP) yog tus neeg nruab nrab ntawm kev so ntawm cov leeg nqaij leeg. Cov tshuaj no tiv thaiv kev decomposition ntawm cGMP los ntawm inhibiting phosphodiesterase hom 5, yog li ua rau tsub zuj zuj ntawm cGMP, so ntawm cov nqaij mos ntawm lub corpus cavernosum, thiab erection ntawm noov. 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 cov kev xaiv thiab inhibitory cuam tshuam ntawm phosphodiesterase type 5 zoo dua li lwm cov phosphodiesterase type 5 inhibitors. Hom phosphodiesterase inhibitors muaj tsawg.

Cov cuab yeej tshuaj thiab kev siv

1. Thaum siv ua ke nrog CYP 3A4 inhibitors (xws li ritonavir, indinavir, saquinavir, ketoconazole, itraconazole, erythromycin, thiab lwm yam), nws tuaj yeem cuam tshuam cov metabolism ntawm cov tshuaj no hauv daim siab, ua rau kom cov ntshav siab, ua kom lub neej ib nrab ntev, thiab ua rau muaj qhov tshwm sim ntawm lub ntsej muag hloov pauv, qhov tsis zoo tshwm sim. priapism). Cov tshuaj no yuav tsum tau zam ua ke nrog ritonavir thiab indinavir. Thaum siv nrog erythromycin, ketoconazole, thiab itraconazole, qhov siab tshaj plaws ntawm cov tshuaj no yuav tsum tsis txhob ntau tshaj 5 mg, thiab koob tshuaj ntawm ketoconazole thiab itraconazole yuav tsum tsis txhob ntau tshaj 200 mg.
2. Cov neeg mob noj nitrates lossis tau txais kev kho mob nitric oxide pub dawb yuav tsum tsis txhob siv cov tshuaj no ua ke. Nws mechanism ntawm kev txiav txim yog kom ntxiv dag zogconcentration ntawm cGMP, ua rau muaj kev txhim kho cov nyhuv antihypertensive thiab nce lub plawv dhia. Thaum siv ua ke nrog α-receptor blockers, nws tuaj yeem txhim kho cov nyhuv antihypertensive thiab ua rau hypotension. Yog li, kev siv cov tshuaj no yog txwv tsis pub rau cov neeg uas siv α-receptor blockers. Kev noj zaub mov muaj roj nruab nrab (30% ntawm cov calories rog) tsis muaj txiaj ntsig zoo rau cov tshuaj pharmacokinetics ntawm ib koob tshuaj ntawm 20 mg ntawm cov tshuaj no, thiab kev noj zaub mov muaj roj (ntau dua 55% ntawm cov calories rog) tuaj yeem ua rau lub sijhawm ncov ntawm cov tshuaj no thiab txo cov ntshav siab ntawm cov tshuaj no, qhov siab tshaj plaws yog kwv yees li 18%.

Pharmacokinetics
Nws yog absorbed sai sai tom qab kev tswj qhov ncauj, qhov tseeb bioavailability ntawm lub qhov ncauj ntsiav tshuaj yog 15%, thiab lub sij hawm nruab nrab ntawm lub ncov yog 1h (0.5-2h). Kev daws qhov ncauj 10mg lossis 20mg, lub sijhawm nruab nrab ntawm qhov nruab nrab yog 0.9h thiab 0.7h, qhov nruab nrab ncov plasma concentration yog 9µg / L thiab 21µg / L, raws li, 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 koob tshuaj ntawm qhov ncauj ntawm 20 mg, cov ntsiab lus ntawm cov tshuaj hauv cov phev yog 0.00018% ntawm cov koob tshuaj. Cov tshuaj feem ntau yog metabolized hauv daim siab los ntawm cytochrome P450 (CYP) 3A4, thiab ib qho me me yog metabolized los ntawm CYP 3A5 thiab CYP 2C9 isoenzymes. Lub ntsiab metabolite yog M1 tsim los ntawm deethylation ntawm piperazine qauv ntawm cov tshuaj no. M1 kuj muaj cov nyhuv inhibiting phosphodiesterase 5 (kwv yees li 7% ntawm tag nrho cov kev ua tau zoo), thiab nws cov ntshav concentration yog kwv yees li 26% ntawm niam txiv cov ntshav concentration. , thiab tuaj yeem ua rau metabolized ntxiv. Cov kev tso tawm ntawm cov tshuaj nyob rau hauv daim ntawv ntawm metabolites nyob rau hauv quav thiab zis yog hais txog 91% mus rau 95% thiab 2% mus rau 6%, feem. Qhov kev tshem tawm tag nrho yog 56 L ib teev, thiab ib nrab-lub neej ntawm cov niam txiv sib xyaw thiab M1 yog ob qho tib si txog 4 mus rau 5 teev.