Vardenafil Dihydrochloride Ho phekola ho se sebetse ha Erectile 224785-91-5

Ketso ea Pharmacological
Setlhare sena ke inhibitor ea mofuta oa phosphodiesterase 5 (PDE5). Tsamaiso ea molomo ea sethethefatsi sena e ka ntlafatsa ka katleho boleng le nako ea ho emisa, le ho ntlafatsa sekhahla sa katleho ea bophelo ba thobalano ho bakuli ba banna ba nang le ho se sebetse ha erectile. Ho qala le ho hlokomeloa ha penile erection ho amana le ho phomola ha lisele tsa cavernosal smooth muscle, 'me cyclic guanosine monophosphate (cGMP) ke mokena-lipakeng oa ho phomola ha lisele tsa cavernosal smooth muscle. Setlhare sena se thibela ho bola ha cGMP ka ho thibela phosphodiesterase mofuta oa 5, ka hona ho baka ho bokella cGMP, ho phomola ha mesifa e boreleli ea corpus cavernosum, le ho emisa penis. Ha ho bapisoa le phosphodiesterase isozymes 1, 2, 3, 4, le 6, sethethefatsi sena se na le khetho e phahameng ea mofuta oa 5 phosphodiesterase. Lintlha tse ling li bonts'a hore khetho ea eona le phello ea ho thibela phosphodiesterase mofuta oa 5 li molemo ho feta li-inhibitors tse ling tsa mofuta oa 5 oa phosphodiesterase. Mofuta oa phosphodiesterase inhibitors o fokola haholo.

Thepa ea Meriana le Lisebelisoa

1. Ha e sebelisoa hammoho le li-inhibitors tsa CYP 3A4 (tse kang ritonavir, indinavir, saquinavir, ketoconazole, itraconazole, erythromycin, joalo-joalo), e ka thibela metabolism ea lithethefatsi ena sebeteng , e eketsa mahloriso a plasma, e lelefatsa halofo ea bophelo, 'me e eketsa ts'ebetso ea hypotension, phetoho ea maikutlo, phetoho ea maikutlo, phetoho ea maikutlo. ho phopholetsa, boikhabollo). Setlhare sena se lokela ho qojoa hammoho le ritonavir le indinavir. Ha e sebelisoa hammoho le erythromycin, ketoconazole le itraconazole, tekanyo e phahameng ea lithethefatsi ena ha ea lokela ho feta 5 mg, 'me tekanyo ea ketoconazole le itraconazole ha ea lokela ho feta 200 mg.
2. Bakuli ba nkang nitrate kapa ba fumanang phekolo ea bafani ba nitric oxide ba lokela ho qoba ho sebelisa lithethefatsi tsena hammoho. Mokhoa oa eona oa ts'ebetso ke ho eketsa ka ho eketsehilengCGMP, e lebisang ho matlafatseng a antihypertensive le ho eketseha ha sekhahla sa pelo. Ha e sebelisoa hammoho le α-receptor blockers, e ka ntlafatsa phello ea antihypertensive mme ea lebisa ho hypotension. Ka hona, tšebeliso ea sethethefatsi sena e thibetsoe ho ba sebelisang li-alpha-receptor blockers. Lijo tse nang le mafura a mahareng (30% ea lik'hilojule tse mafura) li ne li se na phello e kholo ho pharmacokinetics ea tekanyo e le 'ngoe ea molomo ea 20 mg ea moriana ona,' me lijo tse nang le mafura a mangata (ho feta 55% ea lik'hilojule tse mafura) li ka lelefatsa nako ea tlhōrō ea lithethefatsi ena le ho fokotsa khatello ea mali ea lithethefatsi ena Tlhōrō e ka bang 18%.

Pharmacokinetics
E kenngoa ka potlako ka mor'a tsamaiso ea molomo, bioavailability e feletseng ea letlapa la molomo ke 15%, 'me nako e tloaelehileng ea ho fihla holimo ke 1h (0.5-2h). Tharollo ea molomo 10mg kapa 20mg, nako e tloaelehileng ea tlhōrō ke 0.9h le 0.7h, karolelano ea tlhōrō ea plasma ea 9µg/L le 21µg/L, ka ho latellana, le nako ea phello ea lithethefatsi e ka fihla ho 1h. Sekhahla se tlamang protheine ea moriana ona ke hoo e ka bang 95%. 1.5h ka mor'a tekanyo e le 'ngoe ea molomo ea 20 mg, lihlahisoa tsa lithethefatsi ka har'a peō ke 0.00018% ea tekanyo. Setlhare sena se sebelisoa haholo sebeteng ke cytochrome P450 (CYP) 3A4, 'me chelete e nyane e sebelisoa ke CYP 3A5 le CYP 2C9 isoenzymes. Metabolite e ka sehloohong ke M1 e entsoeng ke deethylation ea sebopeho sa piperazine ea moriana ona. M1 e ​​boetse e na le phello ea ho thibela phosphodiesterase 5 (hoo e ka bang 7% ea katleho eohle), 'me khatello ea mali ea eona e ka bang 26% ea motsoako oa mali oa motsoali. , 'me e ka ntlafatsoa hape. Litekanyetso tsa ho ntšoa ha lithethefatsi ka mokhoa oa metabolites mantleng le moroto li ka ba 91% ho isa ho 95% le 2% ho isa ho 6%, ka ho latellana. Kakaretso ea tumello ke 56 L ka hora, 'me halofo ea bophelo ba motsoako oa motsoali le M1 ke lihora tse ka bang 4 ho isa ho tse hlano.