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NURS 572 Ch 34
Pharm Ch 34 Sedative, hypnotics, BNZ
| Question | Answer |
|---|---|
| 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 |
| do BNZs activate GABA receptors? | no - BNZ ONLY POTENTIATE the actions of GABA, which must be present |
| do BNZ cross BBB | yes, lipid soluble with long-acting metabolitesw |
| low dose of BNZ used in treatment of | anxiety, panic disorder, muscle spasms |
| higher dose of BNZ used in reatment of | insomnia, pre-op (+ anterograde amnesia), seizures |
| BNZ ADRs | CNS depression, resp depression, anterograde amnesia |
| unusual ADRs BNZ | paradoxical sundowning effect, esp in elderly |
| Special concerns BNZ | Category D, Interacts with CNS depressants, CYP 450 enzyme interactions |
| 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) |
| zolpidem indicated for | ONLY sleep latency, prolongs duration somewhat. lacks muscle relaxant, anxiolytic, anti-seizure |
| zaleplon MOA | diff chemical class with MOA similar to BNZ |
| zaleplon indicated for | latency ONLY ---muscle relax, anxiolytic, anti-seizure |
| unique to zaleplon | half-life is 1 hour, very short acting, only for sleep latency |
| eszopiclone MOA | not chemically related to others in class, but has similar MOA at GABA receptor |
| indication for eszopiclone | sleep DURATION only - half-life of 6 hours |
| 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 |
| Unusual features ramelteon | Category C, metabolites half-life 2-5 hours where drug half life only 1-3 hours |
| Unusual ADRs ramelteon | potential for decreased testosterone, increase in prolactin |
| Barbiturates - why no longer used | can bind WITHOUT GABA which means OD possible which depresses CNS --> decreased resp --> coma, death |
| name one atypical antidepressent, with ADR of priaprism, used for hypnotic SE | trazadone |
| name 2 first generation antihistamines used for their sedative SE | diphenhydramine, doxylamine |
Created by:
lorrelaws
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