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Khoom Paub meej

Tadalafil Properties

Melting Point 298-300 degree; Kev sib hloov tshwj xeeb D20 +71.0℃; Boiling Point 679.1 ± 55.0℃(Tshaj tawm); Qhov ceev 1.51 ± 0.1 g / cm³ (Predicted); Flash Point 2 degree; Cia Lub Sijhawm: Muab ntim rau hauv qhuav, 2-8 degree; Solubility hauv DMSO: 20 mg / mL, ntshiab; Acidity Coefficient (pKa): 16.68 ± 0.40 (Predicted); Daim ntawv: hmoov; Xim: Dawb rau Beige; Optical Activity

Txheej txheem cej luam

Tadalafil (Tadalafil) muaj cov qauv molecular ntawm C22H19N3O4 thiab molecular hnyav ntawm 389.4. Nws tau dav siv los kho erectile kawg hauv cov txiv neej txij li xyoo 2003 raws li lub npe lag luam Cialis. Xyoo 2008, Eli Lilly thiab Tuam Txhab tau muag cov cai ua lag luam rau cov tshuaj no rau kev kho mob ntawm PAH rau United Therapeutics. Thaum Lub Rau Hli 2009, FDA pom zoo tadalafil hauv Tebchaws Meskas rau kev kho mob ntawm cov neeg mob pulmonary arterial hypertension (PAH) raws li lub npe Adcirca. Tadalafil, thawj zaug ua lag luam hauv xyoo 2003 raws li phau ntawv tshuaj rau kev kho mob erectile kawg (ED), muaj qhov pib ua haujlwm 30 feeb tom qab kev tswj hwm, tab sis nws cov txiaj ntsig tau kav ntev li 2 teev thiab kav ntev li 36 teev, tsis cuam tshuam los ntawm cov khoom noj. Tadalafil yog siv rau hauv koob tshuaj 10 lossis 20 mg, nrog rau kev pom zoo thawj zaug ntawm 10 mg. Kev kho tshuaj noj yog nyob ntawm tus neeg mob cov lus teb thiab cov tshuaj tsis zoo. Cov kev tshawb fawb ua ntej tau pom tias kev tswj hwm qhov ncauj ntawm 10 lossis 20 mg ntawm tadalafil rau 12 lub lis piam ua rau muaj txiaj ntsig zoo ntawm 67% thiab 81%, feem. Ntau cov kev tshawb fawb tau pom qhov ua tau zoo ntawm tadalafil hauv kev kho ED.

Cov lus qhia

Tadalafil yog siv los kho erectile kawg (ED) thiab pulmonary arterial hypertension hauv cov txiv neej.

Mechanism ntawm Action

Erectile Dysfunction: Tadalafil, zoo li sildenafil, yog xaiv rau phosphodiesterase type 5 (PDE5), tab sis nws cov qauv txawv ntawm sildenafil, thiab siab - cov zaub mov rog tsis cuam tshuam nrog nws qhov nqus. Raws li kev sib deev stimulation, nitric oxide synthase (NOS) catalyzes cov synthesis ntawm nitric oxide (NO) los ntawm lub substrate L-arginine nyob rau hauv penile paj endings thiab vascular endothelial hlwb. TSIS MUAJ activates guanylate cyclase, uas hloov guanosine triphosphate mus rau cyclic guanosine monophosphate (cGMP), yog li ua kom cGMP-nyob ntawm cov protein kinase, ua rau txo qis hauv calcium ion concentration nyob rau hauv cov leeg nqaij pob txha ntawm corpus cavernosum, ua kom cov leeg nqaij du thiab corpus. erection. Phosphodiesterase type 5 (PDE5) degrades cGMP rau hauv cov khoom uas tsis muaj zog, ua rau cov noov nkag mus rau hauv lub xeev flaccid. Tadalafil inhibits PDE5 degradation, ua rau cGMP tsub zuj zuj thiab so ntawm corpus cavernosum smooth nqaij, ua rau erection. Vim tias nitrates tsis yog tus neeg pub dawb, lawv siv ua ke nrog tadalafil tuaj yeem nce qib cGMP thiab ua rau mob hnyav heev. Yog li ntawd, lawv siv ua ke yog contraindicated nyob rau hauv kev kho mob xyaum.

Cialis, tseem hu ua tadalafil, yog ib qho tshuaj rau qhov ncauj rau erectile kawg tsim los ntawm Eli Lilly thiab Tuam Txhab. Nws yog thib ob - tiam phosphodiesterase 5 inhibitor. Cov ntaub ntawv tshawb fawb qhia tau hais tias piv rau sildenafil, Cialis muaj qhov pib ua haujlwm sai dua, siv sijhawm li 15-20 feeb, thiab cov nyhuv ntev ntev txog li 36 teev. Nws T1/2 yog 17.5 teev. Hauv kev tshawb fawb ntawm 348 tus txiv neej uas muaj mob me me mus rau qhov ua tsis taus pa hnyav, cov neeg mob tau randomized kom tau txais tadalafil 20mg lossis placebo. Cov txiaj ntsig tau pom tias piv rau cov placebo, tadalafil 20mg txhim kho kev sib deev ua tiav 24 thiab 36 teev tom qab noj. Cov txiv neej feem ntau muaj peev xwm muaj ob txoj kev sib raug zoo hauv 36 teev. Qhov tshwm sim thiab qhov hnyav ntawm cov kev tsis zoo tshwm sim zoo ib yam li cov uas tau pom nrog cov placebo. Mob taub hau thiab plab zom mov tshwm sim hauv ntau dua 5% ntawm cov txiv neej hauv pawg tadalafil. Kev Tiv Thaiv Tsis Zoo: Tsis muaj qhov tshwm sim tsis zoo tshwm sim, suav nrog dej ntws tawm thiab pom kev cuam tshuam. Mob taub hau thiab digestion tsis tshua muaj. [Kev ceev faj] Cov khoom no yog contraindicated nyob rau hauv cov neeg mob tam sim no noj nitrates, muaj angina pectoris, kab mob plawv, uncontrolled hypertension los yog hypotension, los yog leej twg muaj ib tug mob stroke nyob rau hauv 6 lub hlis dhau los.

Siv

Thib ob - tiam phosphodiesterase 5 inhibitor siv los kho erectile kawg hauv cov txiv neej.