S6 Week 1 Pharmacology

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* Barbiturates increase duration of Cl- ion channel opening so they greatly increase GABA duration & they can mimic the effects of GABA so they have dramatic inhibitory effects (due to hyperpolarization). BZD merely increase the frequency of channel opening but they don’t mimic GABA – they facilitate GABA but don’t exert effects in the absence of GABA.

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BZD’s are becoming a 2nd line treatment for chronic anxiety; used mostly for acute symptoms while the SSRI is being started.
Which BZD is not metabolized by CYP34A? Oxazepam

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Which benzodiazapine would produce the most daytime sleepiness when taken at night?

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Chlordiazepoxide

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* Additional information: 5HT antagonists have additional mechanisms as 2nd line antidepressants = prototypical trazodone also inhibits serotonergic reuptake (bind to “SERT”) & act as partial 5HT agonist….trazodone also antagonizes a1 receptors (infamous but uncommon side effect =priapism) & is prototypical for this class----nefazodone is used less commonly due to potential hepatotoxicity so trazodone will prototypical for this session.

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DAT=Dopamine reuptake transporter; DA=dopamine

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