Pharm Ch 34 Sedative, hypnotics, BNZ
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| MOA of true BNZ | Bnz binds WITH GABA at receptor-->activates Cl- channel-->Cl- rushes in to make cell more negative (hyperpolarized) --> decreased firing --> inhibitory effect
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| do BNZs activate GABA receptors? | no - BNZ ONLY POTENTIATE the actions of GABA, which must be present
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| do BNZ cross BBB | yes, lipid soluble with long-acting metabolitesw
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| low dose of BNZ used in treatment of | anxiety, panic disorder, muscle spasms
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| higher dose of BNZ used in reatment of | insomnia, pre-op (+ anterograde amnesia), seizures
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| BNZ ADRs | CNS depression, resp depression, anterograde amnesia
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| unusual ADRs BNZ | paradoxical sundowning effect, esp in elderly
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| Special concerns BNZ | Category D, Interacts with CNS depressants, CYP 450 enzyme interactions
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| what is are BNZ-like that binds WITH GABA resulting in a built-in anti-overdose feature | zolpidem (zaleplon & eszoplicone ACT like BNZs but use different MOA)
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| zolpidem indicated for | ONLY sleep latency, prolongs duration somewhat. lacks muscle relaxant, anxiolytic, anti-seizure
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| zaleplon MOA | diff chemical class with MOA similar to BNZ
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| zaleplon indicated for | latency ONLY ---muscle relax, anxiolytic, anti-seizure
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| unique to zaleplon | half-life is 1 hour, very short acting, only for sleep latency
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| eszopiclone MOA | not chemically related to others in class, but has similar MOA at GABA receptor
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| indication for eszopiclone | sleep DURATION only - half-life of 6 hours
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| Class of drug - ramelteon | Melatonin-receptor agonist M1M2 in SCN suprachiasmatic nucleus (body's master circadian clock). Pineal gland increases melatonin at dark. this drug has 15 fold increase in affinity for MT1 receptors than melatonin
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| Unusual features ramelteon | Category C, metabolites half-life 2-5 hours where drug half life only 1-3 hours
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| Unusual ADRs ramelteon | potential for decreased testosterone, increase in prolactin
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| Barbiturates - why no longer used | can bind WITHOUT GABA which means OD possible which depresses CNS --> decreased resp --> coma, death
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| name one atypical antidepressent, with ADR of priaprism, used for hypnotic SE | trazadone
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| name 2 first generation antihistamines used for their sedative SE | diphenhydramine, doxylamine
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