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44 Cards in this Set
- Front
- Back
Sedatives actions?
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Reduces anxiety and causes sedative effects
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Hypnotics actions?
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Produces drowsiness, facilitates onset and maintenence of sleep
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EFFECTS OF GABA-A receptors?
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activates Cl- channels, hypopolarizes cell, cell is hypoactive
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Effects of GABA-B receptors?
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G-protein, presynaptic terminal controlling with Calium conductance
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Non-selective agonists of GABA-A receptors?
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Benzodiazepines(BZ1 and BZ2)
Imidazopyridines(BZ1) Eszopiclone |
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Flumazenil?
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GABA-A receptor Antagonists, blocks benzo's and Imidazopyridines but not the rest
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Benzo's that only do Phase II, prefered for elderly and those with hepatic involvement?
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Lorazepam, Oxazepam, Temazepam
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Alprazolam
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Benzo, Phase I and II but rapidly eliminated
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Diazepam
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Benzo, 99% plasma protien bound, interacts with phenytoin
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Flunitrazipam
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Benzo, Date rape drug
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Zolpidem?
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Non-benzo(BZ1), Imidazopyridines
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Zalephon?
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Non-benzo(BZ1), Imidazopyridines
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Eszoplicone?
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Non-benzo(BZ1)
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Benzo absorption?
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Lipidd soluble, variable
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Benzo Bioavailability?
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Very good, variable, plasma protein binding 70-99%
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Benzo MOA?
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increases affinity of GABA to GABA-A receptor,
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Benzo CI?
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Pregnancy, crosses BBB and decreases neonates vitals
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Other Effects of Benzo's?
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Affects respiration, and cardiovascular control
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Side Effects of Benzo's?
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Drowsiness, ataxia, amnesia, confusion, paradoxical rage reaction, tolerace and dependence, cross tolerance with alcohol
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Pentobarbital
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intermediate acting barbiturate
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Pentobarbital?
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Intermediate acting barbiturate, used for epilepsy
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Phenobarbital?
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Long acting barbiturate
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Thiopental?
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Short acting Barbiturate, used for induction anesthesia
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Barbiturate MOA?
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Bind GABA-A receptor and increases GABA acticity, at high doses they are GABA-mimetic
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Barbiturate Adverse Reactions?
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Low therapeutic window, respiratory depression especially with alcohol, physical dependence with life threatening withdrawal, stimulates CYP450
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Ramelteon?
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Melatonin receptor agonist(MT1, MT2), Treats insomnia, no dependence or abuse potential
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Therapeutic uses of Benzo's?
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Anticonvusant
Anesthesia Muscle relaxation Induction and maintanence of sleep |
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Benzo Insomnia treatment?
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Triazelam not used b/c of high abuse potential, used only for short time, long half-life so will accumilate
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Considerations in choosing benzodiazepines?
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Rapidity of onset of action
Duration of action Half-life of drug Route of metabolism |
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Factors affecting tolerance, dependence, addiction, withdrawal?
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drug potency, dose taken, t1/2, length of time drug taken
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Benzo's and withdrawal?
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Can be fatal, never withdraw abruptly, taper down or switch to different drug
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Zolpidem for sleep?
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no muscle relaxant, anxiolytic, anticonvulsand activity, anterograde amnesia, rebound insomnia
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Zaleplan for sleep?
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metabolized in liver, metabolism inhibited by cimetidine(H-2 blocker), less next day effects
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Flumazenil?
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Benzo antagonist, also blocks effects of Zolpidem and Zaleplan
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Eszopiclone for sleep?
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Can be used long term
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Mirtazapine?
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Alpha2 blocker(presynaptic on DA and 5-HT neurons), no sexual dysfunction of GI SE
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Amitryptyline for Sleep?
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TCA, SE: orthostatic hypotension, cardiotoxicity, confusion, CI: elderly
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Cyclobenzaprine?
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H-1 blocker for sleep
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Hydroxyzine?
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H-1 blocker for sleep
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Diphenhydramine
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H-1 blocker for sleep
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Nefazodone?
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5-HT2A antagonist and 5-HT reuptake inhibitor, mildly sedation, no sexual dysfunction
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Trazadone?
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Highly sedating, originally antidepressant
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Most non-prescription sleeping pills contain?
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pyralamin or methapyriline
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Herbal sleep aids?
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Valeriana Officinalis, Chamomile(apigenin), Kava, Passion flower(chrysin)
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