171596-29-5 Tadalafil

Tadalafil, nrog cov mis mos molecular C22H19N3O4 thiab molecular hnyav 389.4, uas tau dav siv los kho erectile kawg hauv cov txiv neej txij li xyoo 2003 raws li kev lag luam npe Cialis.Xyoo 2008, Eli Lilly Company tau muag cov cai tsim kev lag luam rau PAH kev kho mob rau United Therapeutics.Thaum Lub Rau Hli 2009, FDA pom zoo Tadafil rau kev kho mob ntawm cov neeg mob pulmonary arterial hypertension (PAH) hauv Tebchaws Meskas raws li lub npe lag luam Adcirca.Tadafil tau tsim nyob rau hauv 2003 raws li ib tug tshuaj rau kev kho mob ntawm ED, thiab cov nyhuv tau zoo 30min tom qab kev tswj hwm, tab sis qhov zoo tshaj plaws nyhuv yog 2h tom qab kev tswj hwm, thiab cov nyhuv yuav kav ntev li 36h, thiab cov nyhuv tsis cuam tshuam los ntawm cov khoom noj.Qhov koob tshuaj ntawm tadafil yog 10 lossis 20mg, qhov pom zoo thawj koob tshuaj yog 10mg, nyob ntawm tus neeg mob cov tshuaj tiv thaiv thiab kev tsis zoo.Kev tshawb fawb ua ntej kev lag luam pom tau tias tom qab 12 lub lis piam ntawm kev tswj qhov ncauj ntawm 10 lossis 20mg ntawm tadafil, cov lus teb yog 67% thiab 81%, feem.Ntau cov kev tshawb fawb tau pom tias tadafil muaj txiaj ntsig zoo hauv kev kho ED.
Erectile kawg: Tadanafil thiab sildenafil yog tib yam xaiv phosphodiesterase hom 5 (PDE5), tab sis lawv cov qauv txawv ntawm qhov kawg, thiab kev noj zaub mov muaj roj tsis cuam tshuam rau lawv txoj kev nqus.Raws li kev sib deev stimulation, nitric oxide synthase (NOS) nyob rau hauv penile paj endings thiab vascular endothelial hlwb catalyzes cov synthesis ntawm nitric oxide (NO) los ntawm substrate L-arginine.TSIS MUAJ activates guanylate cyclase, uas hloov guanosine triphosphate mus rau cyclic guanosine phosphate (cGMP), yog li ua kom cyclic guanosine phospho-dependent protein kinase, uas ua rau txo qis hauv intracellular calcium concentration ntawm cov nqaij mos, uas ua rau kom cov nqaij mos ntawm lub penile. daim txhuam cev thiab erection.Phosphodiesterase type 5 (PDE5) degrades cGMP rau hauv cov khoom uas tsis muaj zog, ua rau lub raum tsis muaj zog.Los ntawm inhibiting qhov degradation ntawm PDE5, tardanafil ua rau tsub zuj zuj ntawm cGMP, uas ua rau cov nqaij ntshiv ntawm lub corpus cavernosum ntawm noov thiab ua rau noov erection.Txij li thaum nitrate esters tsis yog tus neeg pub dawb, lawv cov kev sib xyaw ua ke nrog tadanafil tuaj yeem nce qib cGMP thiab ua rau muaj kev ntxhov siab hnyav, yog li ntawd, kev kho mob ntawm ob qho tib si yog contraindicated.
Tardanafil cuam tshuam qhov no los ntawm inhibiting PDES.GMP degradation, yog li thaum siv ua ke nrog nitric acid thiab vinegar yuav ua rau cov ntshav siab poob qis thiab ua rau muaj kev pheej hmoo ntawm syncope.CY3PA4 induction tus neeg sawv cev tuaj yeem txo qhov muaj abiotic muaj ntawm tadana, thiab kev sib xyaw nrog rifampicin, cimetidine, erythromycin, clarithromycin, itraconwa, ketoconwa thiab HVI protease inhibitors tuaj yeem ua rau cov ntshav siab ntawm cov khoom no.Kev saib xyuas yuav tsum tau them rau kev kho cov koob tshuaj.Txog tam sim no, tsis tau muaj lus ceeb toom txog cov tshuaj pharmacokinetic ntawm cov khoom no cuam tshuam los ntawm kev noj haus thiab cawv.
Siv D-tryptophan ua raw khoom, thawj methyl ester cov tshuaj tiv thaiv, qhov tshwm sim D-tryptophan methyl ester hydrochloride hauv isopropyl cawv thiab piperaldehyde Pictet-spengler cov tshuaj tiv thaiv kom tau txais cis-tetra hydrocarboline compound, thiab tom qab ntawd cov tshuaj tiv thaiv nrog chloroacetyl chloride thiab methylamine, tag nrho. yield yog 56%, tom qab kev tshuaj ntsuam, Glacial acetic acid tau ntxiv purified li recrystallization hnyav.Qhov kev sib npaug tshwj xeeb yog raws li hauv qab no:

Cialis yog Tadalafil, ib qho tshuaj qhov ncauj tsim los ntawm Eli Lilly Pharmaceutical Company rau kev kho mob ntawm erectile kawg hauv cov txiv neej.Nws yog ib tug thib ob tiam phosphodiesterase 5 inhibitor.Cov ntaub ntawv tshawb fawb qhia tau hais tias piv nrog sildenafil, Cialis siv tau sai heev, txog 15 mus rau 20 feeb, thiab cov nyhuv kav ntev txog 36 teev.T1/2 yog 17.5 teev.Hauv kev tshawb fawb ntawm 348 tus txiv neej uas muaj mob me me mus rau qhov hnyav erectile kawg uas tau randomized noj tadalafil 20mg lossis placebo, ob qho tib si 24 thiab 36 teev tom qab noj cov tshuaj txhim kho kev sib deev zoo dua piv rau cov placebo, nrog rau cov txiv neej feem ntau ua tiav kev sib deev ob zaug ntawm 36 teev.Tsis muaj qhov sib txawv ntawm qhov tshwm sim thiab qhov hnyav ntawm cov tshuaj tiv thaiv tsis zoo piv nrog cov placebo.Ntau tshaj 5% ntawm cov txiv neej hauv pawg Tadalafil tau mob taub hau thiab plab zom mov.[Qhov tshwm sim tsis zoo] Tsis pom muaj qhov tshwm sim tsis zoo, xws li dej ntws tawm thiab pom qhov txawv txav.Qee zaum mob taub hau, dyspepsia.[Kev ceev faj] Cov neeg mob uas noj nitrates, angina pectoris, kab mob plawv, tsis tswj ntshav siab lossis hypotension, thiab cov neeg mob uas tau mob stroke hauv 6 lub hlis dhau los yuav tsum tsis txhob tso cai.

Phosphodiesterase 5 inhibitors yog siv los kho erectile kawg hauv cov txiv neej.Qhov thib ob tiam phosphodiesterase 5 inhibitors yog siv los kho erectile kawg hauv cov txiv neej.