Magac | Vardenafil DIHYDROCHOORLOORLIID |
Lambarka CAS | 224775-90-4 |
Qaaciddada molika | C23h32n6o4s |
Miisaanka Moleculal | 488.6 |
Tirada EINECS | 607-088-5 |
Dhibcaha dhalaalaya | 230-235 ° C |
Cucid | 1.37 |
Xaaladda kaydinta | Ku xidhan qalalan, ku keydi qaboojiyaha, hoosta -20 ° C |
Qaab | Budo |
Midab | Cad |
Isutirka aashitada | (PKA) 9.86 ± 0.20 (saadaaliyay) |
Vardefil (Prowtopatentferend); Vardenafilhyhydrortroriketrate (mowduuca mowduuca); 2- (2-ethexyy- 5- 4-Ethylpiperazin-1-yl-1-sulfonyl) -5-methyl-resyl-7-lindar-3h-f) (1,1-f) (1,2,4) Triazin-4-ah; Vardenafilhydydrochlorigetrate99%; Vardenafilhhhhyddrortrate Cas # 224785-90-4fsole; Soo-saareyaasha u soo saarahaFarquilatictafilDortlafiidHytrate224785-98casno.224785-90-4; FADINAF; 1 - (1-4-DIHYDDro-5- 1- Methyl-4-oxo-7-propylimalidazo [5,2,4] Triazin-2-yl) -4-Ethoxyphenyl] -іylyl-piperrazinethroriidhytrate
Ficilka dawooyinka
Daawadan waa nooca fosfooraska ah ee fosfooraska 5 (PDE5) inhihitor. Maamulka afka ah ee daroogadani waxay si wax ku ool ah u wanaajin karaan tayada iyo muddada kacsanaanta, iyo hagaajinta heerka guusha nolosha galmada ee bukaannada ragga ah oo leh ciribtirka. Bilowga iyo dayactirka xiisaha ciqaabta ayaa la xiriirta nasashada unugyada muruqyada jilicsan ee camagosine-ka, CGMP) waa dhexdhexaadiye ku saabsan nasashada unugyada muruqyada jilicsan ee camafka. Dawadani waxay ka hortagtaa burburka cgmp-ka iyadoo ay ka horjoogsanayso fowphphiererase nooca 5, taas oo sidaas ku keena Ururinta CGMP, nasashada muruqyada jilicsan ee Corpus Caventosum, iyo ka saarista guska. Marka la barbar dhigo fosphodeereseresterase bemozys 1, 2, 3, 4, 4, iyo 6, daroogadani waxay leedahay xulasho aad u sareeya oo loogu talagalay nooca 5 fosfooristiisa. Xogta qaar ayaa muujinaya in xulasho uu u qaabilsan yahay iyo in saameynta xannibaya iyo waxtarka xannibaadda fosfooraska Nooca 5-aad ay ka fiican yihiin fosfooraska kale ee fosfooraska Nooca 5 ka hortagga. Nooca fosfooraska fosfooraska ah ee xakameeyayaashu waa yar yihiin.
Guryaha Dawooyinka iyo Codsiyada
1. When used together with CYP 3A4 inhibitors (such as ritonavir, indinavir, saquinavir, ketoconazole, itraconazole, erythromycin, etc.), it can inhibit the metabolism of this drug in the liver , it increases the plasma concentration, prolongs the half-life, and increases the incidence of adverse reactions (such as hypotension, Isbedelada muuqaalka, madax xanuun, wajiga wajiga, Priapist). Daawadan waa in laga fogaadaa marka lagu daro ritonaviir iyo Indinavir. Markii loo isticmaalo isku darka erythromycin, ketoconazycin, ketoconazycin, ketoconazycin, ketoconazycin, ketoconacoole, qiyaasta ugu badan ee dawadan waa inaysan ka badnayn 5 mg, iyo qaddarka ketoconazole iyo Itraconacoole waa inaysan dhaafin 200 mg.
2. Bukaanka qaadanaya Nitrates ama helitaanka daaweynta Nitric Oxide waa inay ka fogaadaan isticmaalka daroogadan isku darka. Habka loo maro ficilku waa in la sii kordhiyoU fiirsashada CGMP, taasoo dhalisay in la wanaajiyo saameynta antihyptional iyo kordhinta garaaca wadnaha. Markii lagu isticmaalo isku-darka 'Fanceptor', waxay kor u qaadi kartaa saameynta ka hortagga ah waxayna u horseedi kartaa hypotension. Sidaa darteed, isticmaalka dawadan waa ka mamnuuc kuwa adeegsanaya α-soo-saareyaasha xargaha. Cunto-dufan dhexdhexaad ah (30% kaloriyada dufanka leh) wax saameyn ah oo ku saabsan dawooyinka loo yaqaan 'pharessines' ee 20 mg ee daroogada, iyo in ka badan 55% kaloriyada dufanka leh) ee dawadaas iyo yareynta dhiigga dhiigga ee dawada ayaa ah 18%.
Farmashiyaha
Waxay si dhakhso leh u nuujisaa ka dib maamulka afka kadib, bioavailabbiska dhabta ah ee kiniiniga ah ee afka ah waa 15%, celcelis ahaan waqtiga ugu sarreeya ee ugu sarreeya waa 1h (0.5-2h). Xalka afka ah 10MG ama 20MG, celceliska waqtiga ugu sarreeya waa 0.9h iyo 0.7h, celcelis ahaan / L iyo 15μg / L, iyo muddada saameynta daroogada ayaa la gaari karaa 1h. Heerka saadaasha borotiinka ee dawadan waa qiyaastii 95%. 1.5h ka dib hal mar oo ah qiyaasta afka ah ee 20 mg, waxa ku jira daroogada ee shahwada waa 0,00018% qiyaasta. Dawada ayaa inta badan lagu dhajiyaa beerka iyada oo loo yaqaan 'cytochrome p450 (Cyp) 3a4, iyo qadar yar, iyo qadar yar ayaa waxaa qaada Cym 3A5 iyo Cym9 ISOZEZMYS. Metabolite-ka ugu weyn waa M1 oo uu sameeyay saqafka qaab dhismeedka piperrazine ee dawadan. M1 sidoo kale waxay leedahay saameynta ay ku xakameynayso fosfooraska 5 (qiyaastii 7% wadarta hufnaanta), iyo uruurinta dhiiga waxay ku dhawaad 26% ka mid ah uruurinta dhiigga ee waalidka. , waana la sii kordhin karaa. Heerarka excretion ee dawooyinka qaab dheecaan ah ee saxarada iyo kaadida ayaa qiyaastii ah 91% ilaa 95% iyo 2% ilaa 6%, siday u kala horreeyaan. Heerka guud ee oggolaanshaha waa 56 l saacadii saacaddii, iyo badhka badhka ah xarunta waalidka iyo M1 waa labadaba qiyaastii 4 illaa 5 saacadood.