171596-29-5 Tadalafil

Tadalafil, nke nwere usoro molecular C22H19N3O4 na molecular arọ 389.4, nke ejirila mee ihe na-agwọ ọrịa erectile na ụmụ nwoke kemgbe 2003 n'okpuru aha ahia Cialis.Na 2008, Eli Lilly Company rere ikike mmepe azụmahịa maka ọgwụgwọ PAH na United Therapeutics.Na June 2009, FDA kwadoro Tadafil maka ọgwụgwọ nke ndị ọrịa nwere ọbara mgbali elu nke pulmonary arterial (PAH) na United States n'okpuru aha ahia Adcirca.E mepụtara Tadafil na 2003 dị ka ọgwụ maka ọgwụgwọ ED, na mmetụta ahụ dị irè 30min mgbe nchịkwa gasịrị, ma mmetụta kachasị mma bụ 2h mgbe nchịkwa gasịrị, mmetụta ahụ nwere ike ịdịru maka 36h, na nri adịghị emetụta mmetụta ahụ.Usoro nke tadafil bụ 10 ma ọ bụ 20mg, usoro mbụ a tụrụ aro bụ 10mg, dabere na mmeghachi omume onye ọrịa na mmeghachi omume ọjọọ.Nnyocha ọmụmụ tupu ahịa gosiri na mgbe izu iri na abụọ nke nchịkwa ọnụ nke 10 ma ọ bụ 20mg nke tadafil, nzaghachi nzaghachi bụ 67% na 81%, n'otu n'otu.Ọtụtụ nchọpụta egosila na tadafil nwere mmetụta dị mma n'ịgwọ ED.
Ngwọta erectile: Tadanafil na sildenafil so n'otu ụdị phosphodiesterase 5 (PDE5) ahọpụtara, mana usoro ha dị iche na nke ikpeazụ, na nri abụba dị elu anaghị egbochi nnabata ha.N'okpuru mkpali mmekọahụ, nitric oxide synthase (NOS) na njedebe akwara penile na sel endothelial vaskụla na-eme ka njikọ nke nitric oxide (NO) sitere na mkpụrụ L-arginine.NO na-arụ ọrụ guanylate cyclase, nke na-agbanwe guanosine triphosphate ka ọ bụrụ cyclic guanosine phosphate (cGMP), si otú ahụ na-arụ ọrụ cyclic guanosine phospho-dependent protein kinase, na-ebute mbelata na ntinye calcium intracellular nke anụ ahụ dị nro, na-eme ka izu ike nke uru ahụ dị nro nke penile. ogbo na erection.Ụdị phosphodiesterase 5 (PDE5) na-eweda cGMP n'ime ngwaahịa na-adịghị arụ ọrụ, na-akpata adịghị ike penile.Site na igbochi mmebi nke PDE5, tardanafil na-eduga n'ịgbakọta cGMP, nke na-eme ka ahụ dị nro nke corpus cavernosum nke amụ na-eduga na penile erection.Ebe ọ bụ na esters nitrate abụghị ndị na-enye onyinye, nchikota ha na tadanafil nwere ike ime ka ọkwa cGMP dịkwuo elu ma na-eduga na hypotension siri ike, ya mere, contraindications nke ụlọ ọgwụ nke abụọ bụ contraindicated.
Tardanafil na-emetụta nke a site na igbochi PDES.Mmebi GMP, yabụ mgbe ejiri ya na nitric acid na mmanya nwere ike ibute oke mbelata ọbara mgbali ma bulie ohere nke syncope.Ihe ntinye ntinye nke CY3PA4 nwere ike belata ohere nke tadana abiotic, yana nchikota ya na rifampicin, cimetidine, erythromycin, clarithromycin, itraconwa, ketoconwa na HVI protease inhibitors nwere ike ịbawanye mkpokọta ọbara nke ngwaahịa a.Ekwesịrị itinye nlebara anya maka ịhazigharị dose ahụ.Ka ọ dị ugbu a, enwebeghị akụkọ ọ bụla gbasara pharmacokinetic parameters nke ngwaahịa a metụtara nri na mmanya.
Iji D-tryptophan dị ka akụrụngwa, mmeghachi omume methyl ester mbụ, nsonaazụ D-tryptophan methyl ester hydrochloride na mmanya isopropyl na piperaldehyde Pictet-spengler mmeghachi omume iji nweta cis-tetra hydrocarboline compound, wee meghachi omume na chloroacetyl chloride na methylamine, mkpokọta. mkpụrụ bụ 56%, mgbe nyochachara, Glacial acetic acid na-asachapụ ọzọ dị ka ihe mgbaze recrystallization.Usoro mmeghachi omume a kapịrị ọnụ bụ nke a:

Cialis bụ Tadalafil, ọgwụ ọnụ nke Eli Lilly Pharmaceutical Company mepụtara maka ọgwụgwọ nke nrụrụ erectile na ụmụ nwoke.Ọ bụ ihe mgbochi phosphodiesterase 5 nke ọgbọ nke abụọ.Akụkọ nyocha na-egosi na e jiri ya tụnyere sildenafil, Cialis na-arụ ọrụ ngwa ngwa, ihe dị ka 15 ruo 20 nkeji, na mmetụta na-adịru ruo awa 36.T1/2 bụ awa 17.5.N'ime nnyocha nke ndị ikom 348 na-enwe mmetụta dị nro na nke siri ike erectile bụ ndị a na-ejikọtaghị na ha ga-ewere tadalafil 20mg ma ọ bụ placebo, ma 24 na 36 awa mgbe ịṅụchara ọgwụ ahụ mere ka ọganihu mmekọahụ dịkwuo mma ma e jiri ya tụnyere placebo, na ọtụtụ ndị ikom na-enwe mmekọahụ ugboro abụọ na 36 awa.Enweghị ihe dị iche na nhụta na ịdị njọ nke mmeghachi omume ọgwụ ọjọọ ma e jiri ya tụnyere placebo.Ihe karịrị 5% nke ndị ikom nọ na Tadalafil nwere isi ọwụwa na afọ ntachi.[Mmeghachi omume na-adịghị mma] Ọnweghị mmeghachi omume ọjọọ dị njọ a hụrụ, dị ka ịchafụ na ihe na-adịghị mma a na-ahụ anya.Mgbe ụfọdụ isi ọwụwa, dyspepsia.[Akpachara anya] Ndị ọrịa na-ewere nitrates, angina pectoris, ọrịa obi, ọbara mgbali elu na-achịkwaghị achịkwa, na ndị ọrịa nwere ọrịa strok n'ime ọnwa isii gara aga agaghị ekwe.

A na-eji ihe mgbochi phosphodiesterase 5 na-agwọ ọrịa erectile na ụmụ nwoke.Ọgbọ nke abụọ phosphodiesterase 5 inhibitors na-eji na-agwọ ọrịa erectile na ụmụ nwoke.