0102
Mayelana ne-CAS 103-90-2 Acetaminophen
2024-05-10 09:37:28
| Iphoyinti lokuncibilika | 168-172 °C(lit.) |
| Iphuzu elibilayo | 273.17°C (isilinganiso esinzima) |
| ukuminyana | 1,293 g/cm3 |
| umfutho womhwamuko | 0.008Pa ku-25℃ |
| inkomba ye-refractive | 1.5810 (isilinganiso esinzima) |
| Fp | 11 °C |
| izinga lokushisa lokugcina. | Umkhathi ongenayo, izinga lokushisa legumbi |
| ukuncibilika | i-ethanol: i-soluble0.5M, icacile, ayinambala |
| pka | 9.86±0.13(Okubikezelwe) |
| ifomu | Amakristalu noma i-Crystalline Powder |
| umbala | Emhlophe |
Incazelo:
I-acetaminophen, eyaziwa nangokuthi i-paracetamol, iyikhemikhali enefomula ye-molecular C8H9NO2. Kuwumuthi owela ngaphansi kwekilasi le-analgesics (ukunciphisa ubuhlungu) kanye ne-antipyretics (i-fever reducers). Ngokwesakhiwo, i-acetaminophen iphuma ku-para-aminophenol. Mayelana nezakhiwo ezibonakalayo, i-acetaminophen iyimpushana emhlophe ecwebezelayo encibilika kancane emanzini. Ivamise ukutholakala ekwenziweni okuhlukahlukene, okuhlanganisa amaphilisi, amaphilisi, kanye nokumiswa okuwuketshezi, ukuze kuphathwe ngomlomo.
Ukusetshenziswa:
I-acetaminophen isetshenziswa kabanzi ukudambisa izinhlungu nokunciphisa imfiva. Kwaziwa ngokusebenza kwayo ngempumelelo ekudambiseni ubuhlungu obuncane kuya kobumaphakathi, obufana nekhanda elibuhlungu, ukuqaqamba kwemisipha, nokuqaqamba kwamazinyo. Ngokungafani nezidakamizwa ezingezona ukuvuvukala (ama-NSAID), i-acetaminophen ayinazo izinto ezibalulekile zokulwa nokuvuvukala.
Indlela eqondile yokusebenza kwe-acetaminophen ayiqondwa ngokugcwele, kodwa kukholakala ukuthi ihilela ukuvinjelwa kwe-enzyme ebizwa ngokuthi i-cyclooxygenase (COX) ohlelweni lwezinzwa oluphakathi. Le enzyme ibandakanyeka ekukhiqizweni kwe-prostaglandin, edlala indima ekuboneni ubuhlungu nasekulawuleni izinga lokushisa lomzimba.
I-acetaminophen ibhekwa njengenketho ephephile yokunciphisa ubuhlungu kubantu abangakwazi ukubekezelela ama-NSAID ngenxa yezici ezifana nezilonda zesisu noma ukuphazamiseka kwegazi.
Ucwaningo oluhlobene:
Izifundo ze-in vitro I-In vitro, i-acetaminophen ibangele ukukhetha kwe-4.4-fold for COX-2 inhibition (IC50 ye-COX-1, 113.7 μM; IC50 ye-COX-2, 25.8 μM). Ngemuva kokuphathwa ngomlomo, ukuvimbela okuphezulu kwe-ex vivo kwaba ngu-56% (COX-1) no-83% (COX-2). Ukugxila kwe-acetaminophen ku-plasma kwahlala kungaphezu kwe-in vitro IC50 ye-COX-2 okungenani amahora ama-5 ngemuva kokuthatha umthamo. Amanani e-ex vivo IC50 e-acetaminophen (COX-1: 105.2 μM; COX-2: 26.3 μM) aqhathaniseka kahle namanani ayo e-in vitro IC50. Ngokuphambene nemibono yangaphambilini, i-acetaminophen ivimbela i-COX-2 ngaphezu kuka-80%, izinga eliqhathaniswa nezidakamizwa ezingezona ukuvuvukala (ama-NSAID) kanye nama-COX-2 inhibitors akhethiwe. Kodwa-ke, akukho> 95% ukuvinjelwa kwe-COX-1 kuye kwahlotshaniswa nokuvinjelwa komsebenzi weplatelet [1]. Ukuhlolwa kwe-MTT kubonise ukuthi i-acetaminophen (APAP) ngethamo elingu-50mM kakhulu (p
Izifundo ze-vivo: Ukuphathwa kwe-acetaminophen (250 mg/kg, ngomlomo) kumagundane kuholele ekulimaleni okukhulu kwesibindi (p