Some Drugs for Treating Partial Seizures 部分性癫痫发作药物
The drugs used to control partial seizures stabilize nerve membranes in either of two ways —directly, by altering sodium and calcium channels, or indirectly, by increasing the activity of GABA, an inhibitory neurotransmitter, and thereby decreasing excessive activity. Carbamazepine, felbamate, and oxcarbazepine are used as monotherapy, and the remaining drugs are used as adjunctive therapy. Each of the drugs used for treating partial seizures has a slightly different mechanism of action. For example:
用于控制部分性癫痫发作的药物可通过直接或间接两种方式稳定神经膜，前者是通过改变钠、钙通道，后者是通过增强GABA活性，从而减少过度兴奋。GABA是一种抑制性神经递质。卡马西平、非尔氨酯和奥卡西平用于单一疗法，其他药物则作为辅助治疗使用。用于治疗部分性癫痫发作的每种药物都有略为不同的作用机制。如：
Carbamazepine is chemically related to the tricyclic antidepressants. It has the ability to inhibit polysynaptic responses and to block sodium channels to prevent the formation of repetitive action potentials in the abnormal focus.
卡马西平在化学特性上与三环抗抑郁剂有关。该药具备抑制多突触响应能力，还能够阻断钠通道，阻止异常病灶形成重复性动作电位。
Clorazepate and felbamate are thought to potentiate the effects of the inhibitory neurotransmitter GABA.
氯拉卓酸和非尔氨酯据称可增强抑制性神经递质GABA的效应。
Gabapentin inhibits polysynaptic responses and blocks stimulus increases in certain situations. Gabapentin is also approved to be used in the treatment of amyotrophic lateral sclerosis (ALS), post-herpetic neuralgia, and restless leg syndrome. It has many off-label uses and is often seen as a drug in the polypharmacy needed to achieve therapeutic results with psychiatric patients.
加巴喷丁抑制多突触响应，阻断特定情况下的刺激增强。加巴喷丁也已获准用于治疗肌萎缩侧索硬化（ALS）、疱疹后神经痛和不宁腿综合征。该药还有多种标示外使用用途，常作为一种药物见于多药疗法中，以达到精神病患者所需要的治疗结果。
The newer drugs lacosamide and rufinamide inhibit voltage-sensitive sodium channels, which results in a stabilization of nerve membranes and an inhibition of neuronal firing.
拉考沙胺和卢非酰胺属于较新药物，可以抑制电压敏感性钠通道，达到神经膜稳定和抑制神经元放电的效果。
Ezogabine is a neuronal potassium channel opener, blocking repolarization and inhibiting neuronal firing.
依佐加滨为神经元钾通道开放剂，阻断再极化，抑制神经元放电。
Lamotrigine may inhibit voltage-sensitive sodium and calcium channels, stabilize nerve cell membranes, and modulate calcium-dependent presynaptic release of excitatory neurotransmitters.
拉莫三嗪可以抑制电压敏感性钠、钙通道稳定神经细胞膜，调制兴奋性神经递质的钙依赖性突触前释放。
Levetiracetam is a newer drug, and its mechanism of action is not understood; its antiepileptic action does not seem to be associated with any known mechanisms of inhibitory or excitatory neurotransmission. (See also the Focus on Safe Medication Administration for information about potentially serious name confusion that has occurred with levetiracetam.)
左乙拉西坦是一种新药，其作用机制尚未了解。其抗癫痫作用似乎也与已知的抑制性或兴奋性神经传递机制不相关。（左乙拉西坦潜在的严重药名混乱信息请参考安全用药聚焦）。
Oxcarbazepine’s exact mechanism of action is also unknown. It inhibits voltage-sensitive sodium channels, stabilizing hyperexcited nerve cell membranes. It also increases potassium conductance and modulates calcium-dependent presynaptic release of excitatory neurotransmitters. Any or all of these effects may be responsible for the antiseizure effects of the drug.
奥卡西平的确切作用机制也是未知的。该药抑制电压敏感性钠通道，稳定过度兴奋的神经细胞膜；还可增强钾传导性，调制兴奋性神经的钙依赖性突触前释放。其中的任何效应或所有的效应都可能对该药物的抗癫痫作用产生影响。
★Vocabulary for Today ★
Trileptal – n. 确乐多
pregabalin – n. 普瑞巴林
Lyrica – n. 乐瑞卡
rufinamide – n. 卢非酰胺
Banzel – n. 班泽尔
tiagabine – n. 噻加宾
Gabitril – n. 加比特利
topiramate – n. 托吡酯
carbamazepine – n. 卡马西平
felbamate – n. 非尔氨酯
oxcarbazepine – n. 奥卡西平
clorazepate – n. 氯拉卓酸
felbamate – n. 非尔氨酯
gabapentin – n. 加巴喷丁
amyotrophic lateral sclerosis (ALS) -- 肌萎缩侧索硬化
post-herpetic neuralgia – n. 疱疹后神经痛
restless leg syndrome –不宁腿综合征
Topamax – n. 妥泰
vigabatrin – n. 氨己烯酸
Sabril – n. 喜保宁
1. A physician has a choice in benzodiazepines to prescribe for patients. A particular patient (a 53-year-old man with anxiety) has a difficult time with compliance to medications. The physician is concerned about the patient going into withdrawal because of abrupt discontinuation of the antianxiety medication. Which of the following medications would have the least severe withdrawal reaction?
A. Diazepam
B. Flurazepam
C. Temazepam
D. Triazolam 2. A 19-year-old man is brought to the emergency department after being found by his roommate to have snorted cocaine several times in the past few days, the last time being 10 h previously. He was given a drug that sedated him, and he fell asleep. The drug that was used to counter this patient’s apparent cocaine withdrawal was very likely which of the following?
A. Cocaine
B. Fluoxetine
C. Hydroxyzine
D. Lorazepam
E. Phenobarbital
奥医教育“在线自测”正式上线，复习练习、效果检验，奥医NCLEX-RN/ISPN题库一站完成。
答案Answers 1. B: Flurazepam.
Psychological and physical dependence on benzodiazepines can develop if high doses of the drugs are given over a prolonged period. Abrupt discontinuation of the benzodiazepines results in withdrawal symptoms, including confusion, anxiety, agitation, restlessness, insomnia, tension, and (rarely) seizures. Because of the long half-lives of some benzodiazepines, withdrawal symptoms may occur slowly and last several days after discontinuation of therapy. Benzodiazepines with a short elimination half-life, such as triazolam, induce more abrupt and severe withdrawal reactions than those seen with drugs that are slowly eliminated, such as flurazepam. 2. D: Lorazepam.
The anxiolytic properties of benzodiazepines, such as lorazepam, make them the drugs of choice in treating the anxiety and agitation of cocaine withdrawal. Lorazepam also has hypnotic properties.
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