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巴比妥(Barbital)類,濃度效力呈線性苯二氮平類(Benzodiazepines)類,濃度效力成非線性有cellingBarbiturates類取代基的不同主要包括pentobarbital、secobarbital和phenobarbital。(要背!!)較新型的藥Zolpidem安眠Zaleplon安眠\夢遊
triazolam和clorazepate是兩種吸收比較快desmethyldiazepam (nordiazepam)是一種代謝中間產物,是在胃裡酸水解成desmethyldiazepam的形式. (重要)Oxazepam, lorazepam, temazepam是三種屬於吸收比較慢全部都可以通過血腦屏障.
Barbiturates類的藥物大部分是在肝臟中代謝,只有Phenobarbital有部份可以以原型的形式代謝出去.帶有thio-group(SH-)的藥物(易被肝代謝),像是Thiobarbiturates,代謝會比較快,都是屬於短效的藥物,常用在麻醉輔助用藥上(誘導麻醉藥物).
GABAA屬於ligand-gated-ion channel;GABAB屬於G protein coupled receptorBenzodiazepines(BDZ)和Barbiturates等所有鎮靜安眠藥主要的受體是 GABAA receptor(重要)
Flumazenil則是GABAA receptor的拮抗劑(antagonist),結合到受體上阻斷BDZ的作用,卻不會對Barbiturate、Alcohol、Meprobamate的效果有影響。所以常用來急救吃安眠藥自殺的人(安眠藥含有BDZ),或是麻醉的催醒劑。(重要必考藥物)
Alprazolam可治療重度憂鬱症。重要!
問:小明今年22歲,平時沒有酗酒習慣,今飲用500毫升酒精濃度15%葡萄酒,請問小明需要多久才能將酒精完全代謝。(酒精代謝量平均為每小時7-10g)。答:500×0.15÷0.8(酒精密度要記得喔!)÷8(成人平均代謝量)=11.7小時。


酒精的代謝路徑有二:(教官說一定要背,考試必考!) 1.大部分利用酒精去氫酶(Alcohol dehydrogenase,ADH)氧化酒精成乙醛。 2.長期酗酒時活化MEOS,亦氧化酒精成乙醛,彌補ADH的不足。

抗癲癇的藥物一定要記住以下四項:Phenytoin、BDZ(可做鎮靜安眠藥)、Valproic acid(具脂肪酸結構的藥物)以及Tiagabine(GABA類藥物)。這四種藥物的蛋白結合率頗高!Sodium Valproate因為具有脂肪酸結構(本身為短鏈脂肪酸),和血漿蛋白結合的比率會和血漿中游離脂肪酸的濃度有關(因free form有效,故血中游離脂肪酸愈高愈有效)。(M105)Phenobarbital和 Carbamazepine會提升肝臟微小體酵素活性,若合併其他藥物使用時會使得其他藥物的代謝變快,所以其他藥物的劑量要提高。(背!!)
Benzodiazepines以”-pam”結尾,例外只有ChlordiazepoxideTriazolobenzodiazepines以”-lam”結尾:triazolam和alprazola

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