Tadalafil 171596-29-5 los kho Erectile Dysfunction hauv Txiv neej
Product Detail
| Lub npe | Tadalafil |
| CAS nr | 171596-29-5 |
| Cov mis mos molecular | C22H19N3O4 |
| Molecular hnyav | 389.4 ib |
| EINECS Number | 687-782-2 ib |
| Kev sib hloov tshwj xeeb | D20+71.0° |
| Qhov ntom | 1.51 ± 0.1g / cm3 (Tshaj tawm) |
| Kev cia khoom | 2-8 ° C |
| Daim ntawv | Hmoov |
| Acidity coefficient | (pKa) 16.68 ± 0.40 (Predicted) |
| Dej solubility | DMSO: soluble 20mg / ml, |
Synonyms
TADALAFIL; CIALIS; IC 351;(6R,12AR)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido;GF 196960;ICOS 351;Tildenafil;
Pharmacological nyhuv
Tadalafil (Tadalafil, Tadalafil) muaj cov qauv molecular ntawm C22H19N3O4 thiab molecular hnyav ntawm 389.4. Nws tau siv dav hauv kev kho cov txiv neej erectile kawg txij li xyoo 2003, nrog lub npe lag luam Cialis (Cialis). 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 lag luam Adcirca. Tadalafil tau qhia hauv xyoo 2003 ua ib qho tshuaj rau kev kho mob ED. Nws yuav siv sij hawm 30 feeb tom qab kev tswj hwm, tab sis nws cov txiaj ntsig zoo tshaj plaws yog 2h tom qab pib ua, thiab cov nyhuv tuaj yeem kav ntev li 36 teev, thiab nws cov nyhuv tsis cuam tshuam los ntawm cov khoom noj. Cov koob tshuaj tadalafil yog 10 lossis 20 mg, qhov pom zoo thawj koob tshuaj yog 10 mg, thiab cov koob tshuaj raug kho raws li tus neeg mob cov lus teb thiab qhov tsis zoo tshwm sim. Kev tshawb fawb ua ntej kev lag luam tau pom tias tom qab kev tswj hwm qhov ncauj ntawm 10 lossis 20 mg ntawm tadalafil rau 12 lub lis piam, cov txiaj ntsig zoo yog 67% thiab 81%, feem. Ntau cov kev tshawb fawb tau pom tias tadalafil muaj txiaj ntsig zoo hauv kev kho ED.
Erectile Dysfunction: Tadalafil yog ib qho kev xaiv phosphodiesterase hom 5 (PDE5) zoo li sildenafil, tab sis nws cov qauv txawv ntawm qhov kawg, thiab kev noj zaub mov muaj roj tsis cuam tshuam nrog nws qhov nqus. Nyob rau hauv qhov kev txiav txim ntawm 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 lub substrate L-arginine. TSIS MUAJ activates guanylate cyclase, uas hloov guanosine triphosphate mus rau cyclic guanosine monophosphate (cGMP), yog li ua kom cyclic guanosine monophosphate-dependent protein kinase, ua rau txo qis hauv cov concentration ntawm calcium ions hauv cov leeg nqaij pob txha, ua rau lub cev nqaij daim tawv nqaij so kom txaus. Phosphodiesterase type 5 (PDE5) degrades cGMP rau hauv cov khoom tsis muaj zog, ua rau noov mus rau hauv lub xeev tsis muaj zog. Tadalafil inhibits qhov degradation ntawm PDE5, ua rau tsub zuj zuj ntawm cGMP, uas so cov leeg du ntawm corpus cavernosum, ua rau noov erection. Txij li thaum nitrates tsis yog tus neeg pub dawb, kev siv ua ke nrog tadalafil yuav ua rau nce qib ntawm cGMP thiab ua rau mob hnyav heev. Yog li ntawd, kev siv ua ke ntawm ob yog contraindicated nyob rau hauv kev kho mob xyaum.
Tadalafil ua haujlwm los ntawm inhibiting PDES. GMP yog degraded, yog li kev siv ua ke nrog nitrates tuaj yeem ua rau cov ntshav siab poob qis thiab ua rau muaj kev pheej hmoo ntawm syncope. CY3PA4 inducers yuav txo cov bioavailability ntawm tadanafil, thiab kev sib xyaw nrog rifampicin, cimetidine, erythromycin, clarithromycin, itracon, ketocon, thiab HVI protease inhibitors yuav ua rau kom cov ntshav concentration ntawm cov tshuaj yuav tsum tau kho. Txog tam sim no, tsis muaj ntawv ceeb toom tias cov tshuaj pharmacokinetic ntawm cov khoom no cuam tshuam los ntawm kev noj haus thiab cawv.
