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NURS 572 Ch 34

Pharm Ch 34 Sedative, hypnotics, BNZ

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