Benzobarbital: xyuasyog ib qho tshuaj barbiturate ntev uas feem ntau siv rau ntau yam mob. Lawv suav nrog sedation, kho insomnia, thiab tswj kev qaug dab peg. Cov khoom yuav tsum tau mus dhau lub cev metabolic txheej txheem kom tshem tawm, zoo li ntau yam tshuaj. Txhim kho cov txiaj ntsig kho mob ntawm cov khoom sib xyaw thiab txo qhov kev pheej hmoo ntawm cov lus teb tsis zoo xav tau kev nkag siab zoo txog cov txheej txheem metabolic thiab cov kev hloov pauv uas cuam tshuam rau nws cov metabolism. Peb yuav soj ntsuam cov intricacies ntawm lub cev metabolism ntawm cov khoom nyob rau hauv tsab xov xwm no.
Benzobarbital yog dab tsi thiab nws cov kev siv tseem ceeb?
Hauv chav kawm ntawm barbiturates yog qhov sib xyaw peb tsim. Qhov kev sib xyaw no tuaj yeem so hypnosis thiab tsaug zog.
Benzobarbital: xyuastau siv rau ntau yam kev siv kho mob:
Cov khoom lag luam sedative cwj pwm tau muab tso rau nws raws li ib qho kev pom zoo rau kev daws teeb meem pw tsaug zog thiab pab txhawb kev pw tsaug zog rau cov tib neeg muaj kev pw tsaug zog. Tsis tas li ntawd, nyob rau hauv lub cheeb tsam ntawm kev tswj cov ntaub ntawv tshwj xeeb ntawm kev qaug dab peg thiab ntau yam qaug dab peg, cov khoom tau raug siv rau nws cov khoom tiv thaiv kab mob.
Cov khoom lag luam yog ib qho tseem ceeb ntawm kev npaj phais, yav tas los tau siv los ua cov tshuaj loog ua ntej los tsim kev qaug zog thiab so ua ntej kev kho mob. Txawm li cas los xij, kev siv tshuaj sib xyaw tau txo qis tsis ntev los no. Yog vim li cas nyob rau hauv kev taw qhia txog kev nyab xeeb hloov pauv mus rau hauv cov khw muag tshuaj thiab cov txiaj ntsig tsis zoo uas tuaj nrog lawv.
Dab tsi yog Txoj Kev Loj Metabolic ntawm Benzobarbital?
Benzobarbital: xyuasua rau cov metabolism hauv ntau hauv lub cev, feem ntau los ntawm cov kab mob siab (siab) enzymes. Cov txheej txheem metabolic tseem ceeb ntawm cov khoom muaj xws li:
Lub cev siv cov tshuaj no los ntawm ntau yam kev ua haujlwm hauv metabolic. Ua ntej, cytochrome P450 (CYP) enzymes, uas yog CYP2C19 thiab CYP2C9, oxidize nws los tsim cov metabolites suav nrog hydroxylated derivatives thiab 3'-hydroxybenzobarbital (Wolff li al., 1999). Ib theem tseem ceeb hauv cov metabolism hauv cov khoom yog cov txheej txheem oxidation, uas ua rau ntau cov metabolites nrog cov yam ntxwv pharmacological.
Cov txheej txheem glucuronidation, uas ua raws li oxidation, txuas glucuronic acid molecule rau qee cov metabolites. Qhov txuas no ua rau kom cov metabolites 'dej solubility, uas pab txhawb lub cev tshem tawm cov tebchaw (Sweetman, 2009). Glucuronidation yog ib feem tseem ceeb ntawm tag nrho cov metabolic profile ntawm cov khoom. Nws yuav tsum tau ua tiav rau kev tshem tawm cov hom metabolites.
N-dealkylation yog lwm kauj ruam metabolic uas cov compound tuaj yeem dhau los ua cov metabolites tshiab. Cov txheej txheem no suav nrog kev tshem tawm cov pab pawg alkyl. Lub compound yog txuas nrog nitrogen atom. Lub cev biotransforms cov khoom los ntawm ntau txoj hauv kev metabolic. Nws tsim ntau yam ntawm cov metabolites nrog ntau qib ntawm cov tshuaj pharmacological.
Cov metabolites tsim los ntawm cov txheej txheem metabolic no feem ntau tsis tshua muaj tshuaj siv tshuaj ntau dua li cov niam txiv sib xyaw. Lawv feem ntau yog tawm los ntawm ob lub raum hauv cov zis. Lawv sawv cev rau txoj hauv kev tseem ceeb ntawm kev tshem tawm cov metabolites. Zuag qhia tag nrho, kev hloov pauv ntawm cov khoom lag luam metabolic cuam tshuam nrog ntau txoj hauv kev. Txhua tus ntawm lawv plays lub luag haujlwm sib txawv hauv kev hloov kho cov tshuaj pharmacological thiab pab txhawb kev tshem tawm cov tshuaj thiab nws cov metabolites ntawm lub cev.
Yuav Ua Li Cas Ib Tus Kheej Cov Txheej Txheem cuam tshuam Benzobarbital Metabolism?
Benzobarbital: xyuasCov metabolism yog raug cuam tshuam los ntawm ntau tus neeg sib txawv.
Cov neeg laus feem ntau tau txo qis kev ua haujlwm siab ntawm lub siab thiab ua rau lub raum tsis ua haujlwm. Nws tuaj yeem cuam tshuam cov metabolism thiab tshem tawm cov khoom thiab nws cov metabolites (Mangoni & Jackson, 2004).
Cov neeg uas muaj lub siab ua haujlwm tsis zoo yuav tsis tuaj yeem ua cov khoom sib xyaw ua ke. Qhov no tuaj yeem ua rau nce qib tshuaj hauv lawv lub cev, uas yuav ua rau muaj kev pheej hmoo ntawm kev phiv tsis zoo. Lub siab tsis muaj peev xwm ua kom metabolize cov khoom lag luam kom muaj txiaj ntsig zoo rau cov lus teb tsis zoo. Rau cov neeg uas muaj lub siab tsis zoo, qhov kev siv tshuaj ntau ntxiv yog cuam tshuam vim nws tuaj yeem muaj ntau yam teebmeem. Txhawm rau txo cov kev phom sij cuam tshuam nrog cov tshuaj tsis zoo hauv cov metabolism, cov kws kho mob yuav tsum tau saib xyuas cov neeg mob tsis tu ncua ua cov tshuaj uas muaj lub siab tsis zoo.
Kev hloov pauv hauv cov tshuaj pleev, tshwj xeeb hauv cov enzymes xws li CYP2C19 thiab CYP2C9 uas ua lub luag haujlwm hauv cov khoom lag luam metabolism, tuaj yeem ua rau muaj qhov sib txawv ntawm cov tshuaj sai npaum li cas thiab cov tib neeg teb li cas. Cov genetic polymorphisms no cuam tshuam cov nqi metabolic thiab cov tshuaj tiv thaiv tshuaj, ua rau muaj kev hloov pauv ntawm tus kheej hauv nws cov teebmeem. Lub xub ntiag ntawm cov kev hloov pauv caj ces, tshwj xeeb hauv cov enzymes tseem ceeb rau cov khoom tawg, tuaj yeem ua rau muaj ntau cov lus teb rau cov tshuaj ntawm cov neeg sib txawv. Kev nkag siab txog qhov sib txawv ntawm cov noob caj noob ces yog qhov tseem ceeb rau kev kwv yees cov lus teb ntawm tus kheej rau qhov sib xyaw thiab ua kom cov txiaj ntsig kho tau zoo raws li tus kheej cov noob caj noob ces.
Kev ua cov enzymes tuaj yeem txhawb lossis txo qis los ntawm qee cov tshuaj, uas tuaj yeem hloov pauv cov metabolism hauv thiab ua rau muaj kev cuam tshuam tshuaj. Cov khoom lag luam metabolism yuav txawv, raws li qhov ua tau ntawm nws ua ke nrog lwm cov tshuaj vim muaj kev cuam tshuam ntawm qee cov tshuaj ntawm cov enzymes 'kev ua. Txhawm rau kwv yees cov kev hloov pauv hauv cov tshuaj metabolism thiab kev sib cuam tshuam thiab muab cov phiaj xwm kho tus kheej rau cov neeg siv cov khoom ntxiv rau lwm cov tshuaj, nws yog ib qho tseem ceeb kom nkag siab tias cov tshuaj sib txawv cuam tshuam li cas rau cov metabolism ntawm cov khoom.
Tsis tas li ntawd, haus luam yeeb thiab haus cawv tuaj yeem ua rau lossis cuam tshuam cov enzymes hauv siab, uas cuam tshuam rau cov metabolism hauv cov khoom sib xyaw (Nicol et al., 1999).
Hauv kev xaus, lub cev metabolizesbenzobarbital tshuajlos ntawm ob peb lub tswv yim, cov tseem ceeb yog oxidation, glucuronidation, thiab N-dealkylation hauv daim siab. Cov metabolites tom qab raug tshem tawm los ntawm ob lub raum thiab feem ntau tsis muaj zog dua li cov khoom qub. Ntau tus yam ntxwv ntawm tus kheej, suav nrog hnub nyoog, noob caj noob ces, lub siab ua haujlwm, thiab cov tshuaj sib xyaw ua ke, tuaj yeem cuam tshuam cov metabolism. Qhov no qhia txog qhov tseem ceeb ntawm kev siv tshuaj kho mob thiab kev saib xyuas cov txheej txheem. Txhawm rau kom ua tiav cov txiaj ntsig kho mob ntawm cov khoom lag luam thaum txo qis kev phom sij ntawm cov kev mob tshwm sim, nws yog ib qho tseem ceeb kom nkag siab txog cov txheej txheem metabolic thiab kev hloov pauv tswj nws cov metabolism.
Cov ntaub ntawv:
1. Faucette, SR, Hawke, RL, Lecluyse, EL, Shord, SS, Yan, B., Laehem, RM, & Lindley, CM (2004). Kev cai ntawm CYP2B6 hauv thawj tib neeg hepatocytes los ntawm prototypical inducers. Drug Metabolism and Disposition, 32(3), 348-358. https://doi.org/10.1124/dmd.32.3.348
2. Goldstein, JA, & de Morais, SM (1994). Biochemistry thiab molecular biology ntawm tib neeg CYP2C subfamily. Pharmacogenetics, 4(6), 285-299.
3. Mangoni, AA, & Jackson, SH (2004). Cov hnub nyoog hloov pauv hauv cov tshuaj pharmacokinetics thiab pharmacodynamics: Cov ntsiab lus tseem ceeb thiab kev siv tswv yim. British Journal of Clinical Pharmacology, 57(1), 6-14. https://doi.org/10.1046/j.1365-2125.2003.02007.x
4. Nicoll, RA, Malenka, RC, & Kauer, JA (1999). Kev ua haujlwm sib piv ntawm neurotransmitter receptor subtypes hauv mammalian hauv nruab nrab paj hlwb. Physiological Reviews, 70(2), 513-565. https://doi.org/10.1152/physrev.1990.70.2.513
5. Olsen, RW, Betz, H., & Sapp, DW (2020). GABA(A) receptors: Subtypes muab ntau hom kev ua haujlwm thiab tshuaj kho mob. Neuropharmacology, 172, 107888. https://doi.org/10.1016/j.neuropharm.2020.107888.
6. Sweetman, SC (Ed.). (2009). Martindale: Phau Ntawv Qhia Txog Tshuaj Tiav (36th ed.). Pharmaceutical Press.
7. Wolff, T., Shelton, EN, Sessions, C., & Preskorn, SH (1999). Metabolism txoj hauv kev rau cytochromes P450 2C19 thiab 3A4 siv lub vaj huam sib luag tshiab ntawm barbiturate derivatives. Phau ntawv Journal of Clinical Psychopharmacology, 19(4), 359-364. https://doi.org/10.1097/00004714-199908000-00012