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Neuro Exam 3 > Anxiolytics & Hypnotics > Flashcards

Anxiolytics & Hypnotics Flashcards

1
Q

GABA-A receptor

A

*when activated, the GABA receptor opens to allow Cl- to flow INTRAcellularly, causing HYPERpolarization
*the hyperpolarization is what causes the inhibitory effect of GABA

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2
Q

benzodiazepines MOA on GABA-A receptor

A

*benzos bind allosterically (same site as the z-drugs) to the GABA-A receptor, facilitating the binding of GABA to the receptor
*benzos increase the FREQUENCY of the channel being open

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3
Q

Z-drugs MOA on GABA-A receptor

A

*Z-drugs bind allosterically (same site as benzos) to the GABA-A receptor, facilitating the binding of GABA to the receptor
*Z-drugs increase the FREQUENCY of the channel being open

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4
Q

barbiturates MOA on GABA-A receptor

A

*barbs bind allosterically to the GABA-A receptor, facilitating the binding of GABA to the receptor
*barbs increase the DURATION of the channel being open

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5
Q

actions/uses of benzodiazepines

A

*sedation, sleep; conscious sedation, anesthesia adjuvant; acute anxiety
*muscle relaxation
*treatment of seizures
*alcohol withdrawal
*anterograde amnesia (loss of the ability to create new memories)

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6
Q

what characteristic can be used to distinguish the benzos from one another

A

wide variety in half-life

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7
Q

metabolism of benzos

A

*all metabolized in LIVER
-some undergo Phase I metabolism to ACTIVE metabolites
-long-acting agents can be even MORE long-acting in the elderly or those taking interacting meds

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8
Q

benzos - tolerance & dependence

A

*tolerance with repeated usage (mostly related to down-regulation of brain benzo receptors)
*psychological dependence
*physical dependence (need to take drug to prevent withdrawal symptoms); depends on:
-dose prior to cessation
-drug elimination (short half-life drugs are worse)

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9
Q

benzo’s effects on sleep

A

*reduction in sleep latency
*suppression of REM sleep
*decreases in all components of sleep EXCEPT STAGE 2
*development of tolerance to sleep effects with continued use
*can produce “REM rebound” upon abrupt discontinuation, especially for short-acting agents at high doses

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10
Q

alprazolam - half-life

A

short/medium

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11
Q

alprazolam - uses

A

commonly used for anxiety, acute panic

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12
Q

diazepam - half-life

A

very long

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13
Q

diazepam - uses

A

*alcohol withdrawal
*sedation
*IV or PO

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14
Q

lorazepam - half-life

A

short/medium

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15
Q

lorazepam - uses

A

*alcohol withdrawal
*sedation
*status epilepticus
*IV or PO

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16
Q

clonazepam - half-life

A

medium

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17
Q

clonazepam - uses

A

*seizures
*anxiety
*panic

18
Q

midazolam - half-life

A

very short

19
Q

midazolam - uses

A

*anesthesia
*conscious sedation
*status epilepticus
*sedation
*often given as IV infusion (but can also be IM)

20
Q

benzos - adverse effects

A

*sedation beyond what was intended (diminished motor skills, judgement, etc)
*anterograde amnesia (cannot retain new info)
*not very “toxic” given alone, but problems arise:
-respiratory depression in pts with pulmonary disease
-given with other drugs (alcohol, narcotics, other CNS depressants)
*be especially cautious with elderly (avoid if possible)

21
Q

zolpidem

A

*important “Z-drug” to know
*aka ambien

22
Q

important z-drug to know

A

zolpidem

23
Q

z-drugs - half-life

A

short

24
Q

z-drugs - use

A

*sleep/hypnotic
*less adverse effect on stages of sleep (compared to benzos)

25
Q

z-drugs - adverse effects

A

*similar to benzos
-less intensive withdrawal symptoms
-generally less tolerance and dependence
*rebound insomnia with higher doses
*perhaps a bit “safer” in the elderly, but not really “safe”

26
Q

what drug is used to reverse the actions of benzos/z-drugs

A

flumazenil

27
Q

flumazenil

A

*REVERSIBLE benzo-receptor antagonist (reverses effects of benzos and z-drugs)

28
Q

flumazenil - uses

A

*reverse benzo used in surgery or procedure
*treat overdose with benzos or z-drugs

29
Q

flumazenil - ADEs

A

*agitation, confusion, dizziness
*can precipitate abstinence symptoms

30
Q

flumazenil - half-life

A

*short (about 1 hour)
*may have to give repeated doses

31
Q

barbiturates - uses

A

*ANESTHESIA
*peds neuro
*some ICU sedation

32
Q

barbiturates - adverse effects

A

*sedation!!
*dependence (worse than benzos)
*tolerance
*induction of hepatic enzymes (drug interactions)
*respiratory depression

33
Q

barbiturates - key terms to associate with

A

*sedation
*seizures (peds)
*enzyme-induction
*GABA

34
Q

buspirone - MOA

A

*unique (but uncertain) MOA: hits some 5-HT and DA receptors

35
Q

buspirone

A

*relieves anxiety without much sedative or euphoric effect
*no rebound anxiety or withdrawal sx with abrupt discontinuation
*takes 2-4 weeks to see effects
*ADE: tachycardia, GI distress, paresthesias
*perhaps not as potent as you would like (often used as an adjunct with other meds)

36
Q

dual orexin receptor antagonists (DORAs) - MOA

A

*blocks OX1R and OX2R receptors (decreases the downstream action of the wake-promoting neurotransmitters that are overactive in pts with insomnia)

-Orexin A and B are peptides in hypothalamic neurons involved in control of wakefulness; they are silent during sleep

37
Q

dual orexin receptor antagonists (DORAs) - drugs in class

A

*suvorexant
*lemborexant
*daridorexant

38
Q

dual orexin receptor antagonists (DORAs) - uses and advantages

A

*used for sleep
*advantages: better daytime functioning; no rebound or withdrawal; little risk of abuse or dependence

*note - not used much

39
Q

remelteon

A

*melatonin receptor agonist
*improves sleep latency (a little); does not improve sleep maintenance
*ADEs: dizziness, somnolence, fatigue
*does not affect sleep architecture

40
Q

miscallaneous meds used for insomnia

A

*diphenhydramine (Benadryl - an H1 antagonist)
*Trazodone - sedating antidepressant
*gabapentin
*melatonin
*alcohol

41
Q

treating a patient with insomnia

A

*best treatment is improving sleep hygiene
*meds only play an adjunct role, especially for chronic insomnia
*drug-induced sleep just isn’t as good as natural sleep
*with continued med use, benefit often decreases as potential for ADEs increases

42
Q

treating a patient with anxiety

A

*counseling first (CBT)
*meds: usually treated with serotonergic-acting antidepressant
-buspirone and gabapentin can be adjuncts
-benzos second-line &/or when rapid action needed

Neuro Exam 3 (31 decks)

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