Vardenafil Dihydrochloride Maganin Rashin Matsala 224785-91-5

Ayyukan Pharmacological
Wannan magani shine mai hana nau'in phosphodiesterase 5 (PDE5). Gudanar da baka na wannan magani na iya inganta inganci da tsawon lokacin tsayuwa, da kuma inganta yawan nasarar rayuwar jima'i a cikin maza masu fama da rashin ƙarfi. Ƙaddamarwa da kuma kula da haɓakar penile yana da alaƙa da shakatawa na ƙwayoyin tsoka mai santsi na cavernosal, kuma cyclic guanosine monophosphate (cGMP) shine matsakanci na shakatawa na cavernosal santsi tsoka Kwayoyin. Wannan miyagun ƙwayoyi yana hana ɓarna na cGMP ta hanyar hana nau'in phosphodiesterase na 5, ta haka ya haifar da tarawar cGMP, shakatawa na tsoka mai santsi na corpus cavernosum, da haɓakar azzakari. Idan aka kwatanta da phosphodiesterase isozymes 1, 2, 3, 4, da 6, wannan magani yana da babban zaɓi don nau'in phosphodiesterase na 5. Wasu bayanai sun nuna cewa zaɓin sa da tasirin hanawa akan nau'in phosphodiesterase 5 sun fi sauran masu hanawa nau'in phosphodiesterase 5. Nau'in phosphodiesterase inhibitors kaɗan ne.

Abubuwan Magunguna da Aikace-aikace

1. Lokacin amfani da tare da masu hana CYP 3A4 (irin su ritonavir, indinavir, saquinavir, ketoconazole, itraconazole, erythromycin, da dai sauransu), zai iya hana metabolism na wannan miyagun ƙwayoyi a cikin hanta , yana ƙara yawan ƙwayar plasma, yana tsawaita rabin rayuwa, kuma yana ƙara yawan abin da ya faru na rashin lafiyan halayen, canje-canje na gani, ciwon kai, canje-canje na gani, ciwon kai, canje-canje na gani, ciwon kai, ciwon kai, canje-canje na gani. priapism). Ya kamata a guji wannan magani tare da ritonavir da indinavir. Lokacin amfani dashi tare da erythromycin, ketoconazole, itraconazole, matsakaicin adadin wannan maganin bai kamata ya wuce 5 MG ba, kuma adadin ketoconazole da itraconazole kada ya wuce 200 MG.
2. Marasa lafiya da ke shan nitrates ko karɓar maganin ba da gudummawar nitric oxide yakamata su guji amfani da wannan magani a hade. Tsarin aikinsa shine don ƙara haɓakamaida hankali na cGMP, yana haifar da ingantaccen tasirin antihypertensive da ƙara yawan bugun zuciya. Lokacin amfani dashi tare da masu hana masu karɓar α-receptor, yana iya haɓaka tasirin antihypertensive kuma yana haifar da hauhawar jini. Sabili da haka, an haramta amfani da wannan magani ga waɗanda ke amfani da masu hana α-receptor. Abincin mai matsakaici (30% na adadin kuzari) ba shi da wani tasiri mai mahimmanci a kan magungunan ƙwayoyi na kashi ɗaya na baki na 20 MG na wannan miyagun ƙwayoyi, da kuma cin abinci mai yawa (fiye da 55% na adadin kuzari) zai iya tsawaita lokacin kololuwar wannan miyagun ƙwayoyi kuma ya rage yawan jinin wannan miyagun ƙwayoyi Mafi girman shine kusan 18%.

Pharmacokinetics
Ana shayar da shi da sauri bayan gudanar da baki, cikakken bioavailability na kwamfutar hannu shine 15%, kuma matsakaicin lokacin zuwa ganiya shine 1h (0.5-2h). Magani na baka 10mg ko 20mg, matsakaicin lokacin mafi girma shine 0.9h da 0.7h, matsakaicin matsakaicin ƙwayar plasma mafi girma shine 9µg / L da 21µg / L, bi da bi, kuma tsawon lokacin tasirin miyagun ƙwayoyi na iya kaiwa 1h. Adadin daurin furotin na wannan magani shine kusan 95%. 1.5h bayan kashi ɗaya na baki na 20 MG, abun ciki na miyagun ƙwayoyi a cikin maniyyi shine 0.00018% na kashi. Maganin yana haɓakawa a cikin hanta ta hanyar cytochrome P450 (CYP) 3A4, kuma ƙaramin adadin yana haɓaka ta CYP 3A5 da CYP 2C9 isoenzymes. Babban metabolite shine M1 wanda aka kafa ta hanyar dethylation na tsarin piperazine na wannan magani. M1 kuma yana da tasirin hana phosphodiesterase 5 (kimanin 7% na jimlar inganci), kuma yawan jininsa shine kusan kashi 26% na mahaifar jinin mahaifa. , kuma za a iya ƙara metabolized. Yawan fitar da kwayoyi a cikin nau'in metabolites a cikin najasa da fitsari kusan 91% zuwa 95% da 2% zuwa 6%, bi da bi. Matsakaicin adadin izinin gabaɗaya shine 56 L a kowace awa, kuma rabin rayuwar mahallin mahaifa da M1 duka kusan awanni 4 zuwa 5 ne.