171596-29-5 Tadalafil

Tadalafil, yokhala ndi mamolekyu a C22H19N3O4 ndi molekyulu yolemera 389.4, yomwe yakhala ikugwiritsidwa ntchito kwambiri pochiza vuto la erectile mwa amuna kuyambira 2003 pansi pa dzina la malonda Cialis.Mu 2008, Eli Lilly Company idagulitsa ufulu wachitukuko wamalonda wa chithandizo cha PAH ku United Therapeutics.Mu June 2009, a FDA adavomereza Tadafil kuti azichiza odwala omwe ali ndi pulmonary arterial hypertension (PAH) ku United States pansi pa dzina la malonda Adcirca.Tadafil inapangidwa mu 2003 monga mankhwala ochizira ED, ndipo zotsatira zake zinali zogwira mtima 30min pambuyo pa utsogoleri, koma zotsatira zabwino zinali 2h pambuyo pa kayendetsedwe ka kayendetsedwe kake, ndipo zotsatira zake zikhoza kukhala kwa 36h, ndipo zotsatira zake sizinakhudzidwe ndi chakudya.Mlingo wa tadafil ndi 10 kapena 20mg, mlingo woyambira wovomerezeka ndi 10mg, malingana ndi momwe wodwalayo amachitira komanso zotsatira zake.Maphunziro oyambirira a msika amasonyeza kuti pambuyo pa masabata a 12 a makonzedwe a pakamwa a 10 kapena 20mg a tadafil, chiwerengero cha mayankho chinali 67% ndi 81%, motero.Kafukufuku wambiri wasonyeza kuti tadafil ili ndi mphamvu yabwino pochiza ED.
Erectile dysfunction: Tadanafil ndi sildenafil ali amtundu wa phosphodiesterase 5 (PDE5), koma mawonekedwe awo ndi osiyana ndi omaliza, ndipo zakudya zamafuta ambiri sizimasokoneza kuyamwa kwawo.Polimbikitsa kugonana, nitric oxide synthase (NOS) m'mitsempha ya mbolo ya mbolo ndi ma cell endothelial cell catalyzes kaphatikizidwe ka nitric oxide (NO) kuchokera ku gawo lapansi L-arginine.NO imayendetsa guanylate cyclase, yomwe imatembenuza guanosine triphosphate kukhala cyclic guanosine phosphate (cGMP), motero imayambitsa cyclic guanosine phospho-dependent protein kinase, zomwe zimapangitsa kuchepa kwa intracellular calcium ndende ya minofu yosalala, zomwe zimapangitsa kupumula kwa minofu yosalala ya penile. siponji ndi erection.Phosphodiesterase type 5 (PDE5) imasokoneza cGMP kukhala zinthu zosagwira ntchito, zomwe zimayambitsa kufooka kwa mbolo.Poletsa kuwonongeka kwa PDE5, tardanafil imayambitsa kudzikundikira kwa cGMP, yomwe imatulutsa minofu yosalala ya corpus cavernosum ya mbolo ndipo imatsogolera ku penile erection.Popeza ma esters a nitrate ndi NO opereka, kuphatikiza kwawo ndi tadanafil kumatha kukulitsa kwambiri cGMP mulingo ndikuyambitsa kutsika kwamphamvu kwamphamvu, chifukwa chake, zotsutsana zachipatala zonse zimatsutsana.
Tardanafil imakhudza izi poletsa PDES.Kuwonongeka kwa GMP, kotero mukagwiritsidwa ntchito limodzi ndi nitric acid ndi viniga kungayambitse kutsika kwambiri kwa kuthamanga kwa magazi ndikuwonjezera chiopsezo cha syncope.CY3PA4 induction agent imatha kuchepetsa kupezeka kwa tadana, ndipo kuphatikiza ndi rifampicin, cimetidine, erythromycin, clarithromycin, itraconwa, ketoconwa ndi HVI protease inhibitors kungapangitse kuchuluka kwa magazi a mankhwalawa.Chidwi chiyenera kuperekedwa pakusintha mlingo.Mpaka pano, sipanakhalepo lipoti la magawo a pharmacokinetic a mankhwalawa omwe amakhudzidwa ndi zakudya ndi mowa.
Pogwiritsa ntchito D-tryptophan ngati zopangira, methyl ester yoyamba, zotsatira zake D-tryptophan methyl ester hydrochloride mu isopropyl mowa ndi piperaldehyde Pictet-spengler reaction kuti atenge cis-tetra hydrocarboline pawiri, kenako amachitira ndi chloroacetyl chloride ndi methylamine, zokolola ndi 56%, pambuyo powunika, Glacial acetic acid inayeretsedwanso ngati zosungunulira recrystallization.The specific reaction equation ndi motere:

Cialis ndi Tadalafil, mankhwala apakamwa opangidwa ndi Eli Lilly Pharmaceutical Company pofuna kuchiza erectile dysfunction mwa amuna.Ndi m'badwo wachiwiri phosphodiesterase 5 inhibitor.Malipoti ofufuza akuwonetsa kuti poyerekeza ndi sildenafil, Cialis imagwira ntchito mwachangu kwambiri, pafupifupi 15 mpaka mphindi 20, ndipo zotsatira zake zimatha mpaka maola 36.T1/2 ndi maola 17.5.Pakafukufuku wa amuna a 348 omwe ali ndi vuto lochepa kwambiri la erectile lomwe linasinthidwa mwachisawawa kuti atenge tadalafil 20mg kapena placebo, maola onse a 24 ndi 36 atatha kumwa mankhwalawa amapindula bwino pogonana poyerekeza ndi placebo, ndipo amuna ambiri amatha kugonana kawiri pa maola a 36.Panalibe kusiyana pakati pa zochitika ndi kuopsa kwa zotsatira zoyipa za mankhwala poyerekeza ndi placebo.Oposa 5% mwa amuna omwe ali mu gulu la Tadalafil anali ndi mutu komanso kusanza.[Zoyipa] Palibe zoyipa zoyipa zomwe zidawonedwa, monga kukomoka komanso kusawoneka bwino.Nthawi zina mutu, dyspepsia.[Ndemanga] Odwala omwe akumwa ma nitrates, angina pectoris, matenda a mtima, kuthamanga kwa magazi kosalamulirika kapena kutsika kwa magazi, komanso odwala omwe adwala sitiroko m'miyezi 6 yapitayi sayenera kuloledwa.

Phosphodiesterase 5 inhibitors amagwiritsidwa ntchito pochiza vuto la erectile mwa amuna.M'badwo wachiwiri wa phosphodiesterase 5 inhibitors amagwiritsidwa ntchito pochiza vuto la erectile mwa amuna.