171596-29-5 Tadalafil

Tadalafil, e nang le foromo ea molek'hule C22H19N3O4 le boima ba molek'hule 389.4, e 'nileng ea sebelisoa haholo ho phekola ho se sebetse ha erectile ho banna ho tloha 2003 tlas'a lebitso la khoebo Cialis.Ka 2008, Eli Lilly Company e ile ea rekisa litokelo tsa nts'etsopele ea khoebo bakeng sa phekolo ea PAH ho United Therapeutics.Ka June 2009, FDA e amohetse Tadafil bakeng sa phekolo ea bakuli ba nang le khatello ea kelello ea methapo ea methapo (PAH) United States tlas'a lebitso la khoebo Adcirca.Tadafil e ile ea hlahisoa ka 2003 e le lithethefatsi bakeng sa phekolo ea ED, 'me phello e ne e sebetsa 30min ka mor'a tsamaiso, empa phello e ntle ka ho fetisisa e ne e le 2h ka mor'a tsamaiso,' me phello e ka tšoarella 36h, 'me phello e ne e sa amehe ke lijo.Tekanyo ea tadafil ke 10 kapa 20mg, tekanyo ea pele e khothalletsoang ke 10mg, ho itšetlehile ka karabelo ea mokuli le liketso tse mpe.Liphuputso tsa pele ho maraka li bontšitse hore ka mor'a libeke tsa 12 tsa tsamaiso ea molomo ea 10 kapa 20mg ea tadafil, litekanyetso tsa karabelo e ne e le 67% le 81%, ka ho latellana.Liphuputso tse ngata li bontšitse hore tadafil e na le katleho e ntle ea ho phekola ED.
Ho se sebetse ha Erectile: Tadanafil le sildenafil ke tsa mofuta o tšoanang oa phosphodiesterase 5 (PDE5), empa sebopeho sa bona se fapane le sa morao-rao, 'me lijo tse nang le mafura a mangata ha li kena-kenane le ho monya ha tsona.Tlas'a tšusumetso ea thobalano, nitric oxide synthase (NOS) lipheletsong tsa methapo ea penile le lisele tsa vascular endothelial li etsa hore ho be le motsoako oa nitric oxide (NO) ho tloha substrate L-arginine.NO e kenya tšebetsong guanylate cyclase, e fetolang guanosine triphosphate ho cyclic guanosine phosphate (cGMP), ka hona e kenya tšebetsong cyclic guanosine phospho-dependent protein kinase, e leng se bakang phokotseho ea khalsiamo ea intracellular ea mesifa e boreleli, e bakang phokoloho ea mesifa e boreleli ea penile. seponche le ho emisa.Phosphodiesterase type 5 (PDE5) e theola cGMP hore e be lihlahisoa tse sa sebetseng, e bakang bofokoli ba botoneng.Ka ho thibela ho senyeha ha PDE5, tardanafil e lebisa ho bokelleng ha cGMP, e khathollang mesifa e boreleli ea corpus cavernosum ea penis 'me e lebisa ho penile erection.Kaha li-nitrate esters ke NO bafani, ho kopana ha bona le tadanafil ho ka eketsa haholo boemo ba cGMP mme ba lebisa ho hypotension e matla, ka hona, li-contraindications tsa kliniki tsa bobeli li hanyetsanoa.
Tardanafil e ama sena ka ho thibela PDES.Ho senyeha ha GMP, kahoo ha ho sebelisoa hammoho le nitric acid le asene ho ka baka ho theoha ho feteletseng ha khatello ea mali le ho eketsa kotsi ea syncope.CY3PA4 induction e ka fokotsa ho fumaneha ha tadana, 'me motsoako le rifampicin, cimetidine, erythromycin, clarithromycin, itraconwa, ketoconwa le HVI protease inhibitors e ka eketsa khatello ea mali ea sehlahisoa sena.Ho lokela ho lebisoa tlhokomelo ho lokisa lethal dose.Ho fihlela joale, ha ho na tlaleho ka mekhahlelo ea pharmacokinetic ea sehlahisoa sena se anngoeng ke lijo le joala.
U sebelisa D-tryptophan e le lisebelisoa tse tala, karabelo ea pele ea methyl ester, sephetho sa D-tryptophan methyl ester hydrochloride ka isopropyl joala le piperaldehyde Pictet-spengler reaction ho fumana motsoako oa cis-tetra hydrocarboline, ebe o arabela ka chloroacetyl chloride le methylamine kaofela, lihlahisoa ke 56%, ka mor'a ho hlahloba, Glacial acetic acid e ile ea hloekisoa ka ho eketsehileng e le solvent recrystallization.Equation e khethehileng ea reaction ke e latelang:

Cialis ke Tadalafil, sethethefatsi sa molomo se entsoeng ke Eli Lilly Pharmaceutical Company bakeng sa phekolo ea ho se sebetse ha erectile ho banna.Ke moloko oa bobeli oa phosphodiesterase 5 inhibitor.Litlaleho tsa lipatlisiso li bontša hore ha li bapisoa le sildenafil, Cialis e sebetsa ka potlako haholo, hoo e ka bang 15 ho metsotso ea 20, 'me phello e nka lihora tse 36.T1/2 ke lihora tse 17.5.Phuputsong ea banna ba 348 ba nang le bothata ba ho se sebetse hantle ha erectile ka mokhoa o bonolo ho isa ho o matla ba neng ba sa sebetse ho nka tadalafil 20mg kapa sebaka sa placebo, lihora tse peli tsa 24 le 36 ka mor'a ho noa lithethefatsi li ile tsa ntlafatsa katleho ea thobalano ha li bapisoa le placebo, 'me banna ba bangata ba atleha ho kopanela liphate ka makhetlo a mabeli ka lihora tsa 36.Ho ne ho se phapang ketsahalong le botebong ba karabelo e mpe ea lithethefatsi ha e bapisoa le placebo.Ho feta 5% ea banna ba sehlopha sa Tadalafil ba ne ba e-na le hlooho e bohloko le indigestion.[Matšoenyeho a mabe] Ha ho na maikutlo a mabe a tebileng a ileng a bonoa, joalo ka ho hlatsa le ho se bone hantle.Ka linako tse ling ho tšoaroa ke hlooho, dyspepsia.[Litlhokomelo] Bakuli ba noang nitrate, angina pectoris, lefu la pelo, khatello ea mali e sa laoleheng kapa hypotension, le bakuli ba nang le stroke likhoeling tse 6 tse fetileng ha baa lokela ho lumelloa.

Phosphodiesterase 5 inhibitors e sebelisoa ho phekola ho se sebetse ha erectile ho banna.Moloko oa bobeli oa phosphodiesterase 5 inhibitors o sebelisetsoa ho phekola ho se sebetse ha erectile ho banna.