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* * * * * * * * * * * (芳香羥) (延長鹼基可延長效果) * * * * * * * * * * * * * * * * * n. * * * * * * * * Pharmacology --GABAA receptor of CNS: (1) enhancement of the synaptic actions of inhibitory neurotransmitters (2) blockade of the synaptic actions of excitatory neurotransmitters --GABA為擁有五個鍵結位子的氯離子通道. 只有GABAA 與barbiturates有關. 增加氯流入使細胞hyperpolarization. --也可抑制glutamate and acetylcholine等興奮性物質 Barbiturates Effects on Cerebral Metabolism --dose-related depression ?slowing of the EEG, reduction in the rate of ATP consumption , protection from incomplete cerebral ischemia --巴比妥可以降低代謝率(頂多50%).但不能降基礎代謝率 --decreased cerebral blood flow (CBF) and ICP, but reserving cerebral perfusion pressure Barbiturates Pharmacodynamics -- loss of consciousness, amnesia, and respiratory and cardiovascular depression -- 只有低劑量適合止痛 -- amnesic effect: less pronounced than that produced by the benzodiazepines Barbiturates Onset of Central Nervous System Effects -- 影響過BBB產生麻醉的能力:脂溶性.離子化.藥物濃度.蛋白結合度. --屬非離子態.速度快: methohexital Thiopental pentobarbital -- patients with acidosis require the administration of less barbiturate -- The degree of protein binding of a drug is influenced by the physiologic pH and disease state -- The two primary determinants of the plasma concentration are the dose administered and the rate (speed) of administration Barbiturates Termination of Effect --與影響onset因子同但Protein binding is less . --病人醒~thiopental :5 to 10 minutes --In the case of constant infusion or repeated dosing with saturation of all tissue sites, patients awake at a much delayed rate --小孩醒得早.代謝快 --Methohexital跟Thiopental相比.醒的時間差不多但是psychomotor較好.全麻超過八小時.中樞抑制的效果會持續一整天.但Methohexital較少如此…由於容易延長醒來.現多用propofol Barbiturates Uses -- induction and maintenance -- thiopental ~ onset (15 to 30 seconds), excellent hypnotic, amnesia, 無止痛 -- Methohexital 快速較不累積. 無止痛,可maintain, recovery from infusion titrated to maintain hypnosis is similar to propofol, --
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