PHA 4107 Lecture Notes - Lecture 10: Locus Coeruleus, Anxiolytic, Clonazepam
12 Jul 2018
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Document Summary
Benzodiazepines are positive allosteric modulators (pams) of gaba-a. Receptors: allosteric sites are all receptors sites where gaba itself does not bind, allosteric modulators can be positive or negative. Benzodiazepines: gabaergic anxiolytics diazepam (valium), lorazepam (ativan), clonazepam. Increase the effect of endogenous gaba: uses: Ventro-lateral preoptic nucleus of the hypothalamus (vlpo) the sleep. Promoter: vlpo nucleus contains gaba neurons that inhibit tmn and thus promote sleep, benzodiazepines augment the action of gaba in vlpo nucleus. Possible anterograde amnesia: prolonged usage can results in withdrawal , i. e. rebound insomnia, anxiety, tremors, Other anxiolytics: non benzodiazepines (zolpidem and zopiclone) Newer anxiolytics that do not share the same structure as benzodiazepines. Rapidly becoming first-line treatment for insomnia they induce sleep but, unlike benzodiazepines, they do not disrupt sleep cycle otherwise. These agents demonstrate less unwanted cognitive, memory and motor side effects. Better pharmacokinetics as well rapid onset and short duration of action.
