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44 Cards in this Set

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