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Psych: Test 1 > Pharm: Sedatives/hypnotics > Flashcards

Pharm: Sedatives/hypnotics Flashcards

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1
Q

which drugs undergo oxidation reactions, thus requiring good hepatic function?

A

Alprazolam, Diazepam

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2
Q

which drug has longest half life?

A

Diazepam - distributes into CNS!

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3
Q

which drugs are best for those w/ hepatic impairment?

A

lorazepam, oxazepam, temezapam - these are all conjugated rather than oxidized

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4
Q

which drugs are best for sleep aids?

A

those with short half lives - Eszopiclone, Zaleplon, Zolpidem

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5
Q

flumazenil

A
  • benzodiazapine antagonist

MOA: competitive antagonist at benzodiazepine site on GABAA receptor

Blocks actions of – benzodiazepines, zolpidem, zaleplon, and eszopiclone

Does not block – barbiturates, buspirone, ramelteon

PK: short t1/2 0.7-1.3 hours (imp. b/c the benzodiazepine has longer 1/2 life, so must give repeat doses)

Use: reversing CNS depressant effects of benzodiazepine overdose and shorten recovery following anesthetic and diagnostic procedures

ADRs: agitation, confusion, dizziness, nausea

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6
Q

what can flumazenil block?

A

– benzodiazepines, zolpidem, zaleplon, and eszopiclone

Does not block:
– barbiturates, buspirone, ramelteon

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7
Q

buspirone

A

MOA: unknown; mediated through serotonergic or dopaminergic systems

PK: extensive first-pass effect, extensive metabolism (CYP3A4)

Use: generalized anxiety disorder (3-4 weeks to become established)

NOTE: does not produce sedation or hypnosis or euphoria!!!

ADRs: tachycardia, palpitations, nervousness, GI distress, paresthesias

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8
Q

ramelteon

A

MOA: agonist at MT­­1 and MT2 melatonin receptors

PK: extensive first-pass effect

Use: treatment of insomnia (difficulty with sleep onset)
ADRs: dizziness, somnolence, fatigue

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9
Q

what do you use sedatives for?

A

Relief of anxiety
Insomnia
Sedation and amnesia before and during medical surgical procedures
Treatment of epilepsy and seizure states
Component of balanced anesthesia (IV administration)
Control of ethanol or other sedative-hypnotic withdrawal states
Muscle relaxation in specific neuromuscular disorders
Diagnostic aids or for treatment in psychiatry

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10
Q

tx of acute anxiety and rapid tx of panic attacks?

A

benzodiazepine

Advantages:
High therapeutic index
Antagonist available for overdose (flumazenil)
Low risk of drug-drug interactions
Minimal effect on CV and autonomic function

Disadvantages:
Risk of dependence
CNS depression
Amnesic effects

** for more generalized and chronic relief you wouldn’t use this

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11
Q

what to use for sleep disorder tx?

A

Sleep aids should decrease sleep latency and provide sufficient sleep duration with minimal hangover effects

**Benzodiazepines used but daytime sedation a disadvantage- not as good

Zolpidem, zaleplon, and eszopiclone

  • Highly effective
  • Rapid onset with minimal hangover effects
    • Zolpidem in biphasic release formulation for sustained sleep maintenance
    • Zaleplon and zolpidem act rapidly
    • Eszopiclone has a longer half-life
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12
Q

what to use for sleep disorder tx?

A

Sleep aids should decrease sleep latency and provide sufficient sleep duration with minimal hangover effects

**Benzodiazepines used but daytime sedation a disadvantage- not as good

Zolpidem, zaleplon, and eszopiclone

  • Highly effective
  • Rapid onset with minimal hangover effects
    • Zolpidem in biphasic release formulation for sustained sleep maintenance
    • Zaleplon and zolpidem act rapidly
    • Eszopiclone has a longer half-life
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13
Q

sedative vs. hypnotic?

A

Sedative

  • Reduces anxiety, exerts calming effect
  • May be side effect of drugs which are not general CNS depressants (e.g., antidepressants, antihistamines, neuroleptics/antipsychotics)

Hypnotic

  • Produces drowsiness, facilitates onset & maintenance of sleep
  • More pronounced CNS depression
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14
Q

which drugs have a linear dose response curve?

A

barbiturates, alcohols, and older sedative-hypnotics

NOTE: benzodiazepines and newer sedative-hypnotics (plateau) — thus harder to reach the state of coma and death w/ dosing in these drugs

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15
Q

30 y/o ddx with generalized anxiety disorder. physician writes drug for lorazepam, what is its anxiolytic properties MOA?

A

its a benzo, it increases frequency of GABA channel opening –> increased Cl- influx –> increased hyperpolarization

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16
Q

30 y/o ddx with generalized anxiety disorder. physician writes drug for lorazepam, what is its anxiolytic properties MOA?

A

its a benzo, it increases frequency of GABA channel opening –> increased Cl- influx –> increased hyperpolarization

17
Q

25 y/o presents w/ c/o excessive anxiety, has difficulty concentrating, often tired, doesn’t sleep well, alcohol dependence hx, doesn’t want sexual performance problems… what agent is most appropriate?
- Busiprone, fluoxetine, impipramine, lorazepam?

A

Answer: Busiprone: doesn’t cause sedation, hypnosis or euphoria!! though this will take 3-4 weeks to work

  • Fluoxetine: SSRI - assoc. w/ sex dysfunction (though usually this is preferred for first line….)
  • Imipramine: TCA - assoc. w/ anticholinergic effects
  • Lorazepam: associated w/ physiologic dependence, thus d/t hx of alcohol dependence, wouldn’t want to put him on this that could produce dependence again
  • Propanolol: doesn’t work
18
Q

37 y/o w/ c/o diff. falling asleep. which of following is used to tx insomnia but has no affinity for GABA receptor complex?
- eszoplicone, ramelteon, temazepam, zaleplon, zolpidem?

A

Ramelteon doesn’t bind gaba complex - this works through melatonin receptors!

19
Q

37 y/o for insomnia, which isn’t metabolized extensively via hepatic oxidation to longer acting metabolite and would be good for NOT producing a hangover effect?
- chlorodiazepine, clorazepate, diazepam, flurazepam, lorazepam

A

** answer lorazepam - metabolized via conjugation and excreted via kidney

LOT drugs: lorazepam, oxazepam, tomazepam are conjugated before excretion w/ no active metabolites - these drugs would be useful for liver failure!!!!
* also useful in elderly who are more sensitive to sedative hypnotics, don’t want drugs w/ active metabolites that can cause cumulative toxicity

20
Q

44 y/o on hypnotic sleep aids, one week later she wakes up in her PJs in jail after enjoying a glass of wine - she wrecked her car and was under the influence. what drug did FDA req. add’n warnings d/t reports of “sleep-driving”?

A

Ambien/Zolpidem - increased reports of sleep walking!

21
Q

32 y/o y/o unresponsive w/ pill overdose. BP 115/74, slurred speech, RR 12, pupils normal size, normal bowel tones, impaired cognition?? which drug is most imp for this pt?
- atropine, ethanol, fluazenil, naloxone

A

sx point to benzo OD - confusion, blurred vision, drowsiness, unresponsiveness, slurred speech amnesia

(opioids cause constriction, use naloxone to reduce this….. ACHE inhibitors also cause constriction, would give atropine for this…)

Answer: Flumazenil

22
Q

alprazolam

A
  • benzodiazapine

MOA: promotes binding of GABA to GABAa receptor - increasing frequency of Cl - channel opening

USE: sedation, hypnosis, muscle relaxation, anxiolytic, and anticonvulsant effects

** high anxiolytic potency, w/ low capacity to cause fatal CNS depression (replaced barbituates)

ADR: hepatic excretion, need good liver!

23
Q

clonazepam

A
  • benzodiazapine

MOA: promotes binding of GABA to GABAa receptor - increasing frequency of channel opening

USE: sedation, hypnosis, muscle relaxation, anxiolytic, and anticonvulsant effects

** high anxiolytic potency, w/ low capacity to cause fatal CNS depression (replaced barbituates)

24
Q

diazepam

A
  • benzodiazapine

MOA: promotes binding of GABA to GABAa receptor - increasing frequency of channel opening

USE: sedation, hypnosis, muscle relaxation, anxiolytic, and anticonvulsant effects

** high anxiolytic potency, w/ low capacity to cause fatal CNS depression (replaced barbituates)

ADR: undergoes oxidation, need good liver function!

25
Q

midazolam

A
  • benzodiazapine

MOA: promotes binding of GABA to GABAa receptor - increasing frequency of channel opening

USE: sedation, hypnosis, muscle relaxation, anxiolytic, and anticonvulsant effects

** high anxiolytic potency, w/ low capacity to cause fatal CNS depression (replaced barbituates)

26
Q

triazolam

A
  • benzodiazapine

MOA: promotes binding of GABA to GABAa receptor - increasing frequency of channel opening

USE: sedation, hypnosis, muscle relaxation, anxiolytic, and anticonvulsant effects

** high anxiolytic potency, w/ low capacity to cause fatal CNS depression (replaced barbituates)

27
Q

phenobarbital

A

bartituate

MOA:
- potentiates GABA-induced Cl- currents through increasing the duration of channel opening –> hyperpolarizing

USE: mild sedation –> anesthesia, anxiolytic, hypnotic, and anticonvulsant effects
** possess narrow therapeutif index thus must be used cautiously

ADR: renal excretion (dose adjust for renal impairment)

28
Q

32 y/o y/o unresponsive w/ pill overdose. BP 115/74, slurred speech, RR 12, pupils normal size, normal bowel tones, impaired cognition?? which drug is most imp for this pt?
- atropine, ethanol, fluazenil, naloxone

A

sx point to benzo OD - confusion, blurred vision, drowsiness, unresponsiveness, slurred speech amnesia

(opioids cause constriction, use naloxone to reduce this….. ACHE inhibitors also cause constriction, would give atropine for this…)

Answer: Flumazenil

29
Q

most serious ADR of GABA sedatives?

A

respiratory depression, circulatory collapse (esp. in person w/ heart condition)

30
Q

which drug class are most of these drugs in ?

A

III or IV:

- III = medical use w/ moderate/low potential for physical dependence and high potential for psychologic dependence

31
Q

which drug class are most of these drugs in ?

A

III or IV:
Class III = medical use w/ moderate/low potential for physical dependence and high potential for psychologic dependence
Class IV = limited potential for dependnce

physiologic dependence: increased anxiety, insomnia, CNS excitability
psychologic component: w/drawal leads to cravings, irritability, insomnia, anorexia, depression, etc.

** imp. to taper sedative-hypnotics when w/drawing

32
Q

tx of acute anxiety attacks?

A

benzodiazepines

for panic disorders use alprazolam , lorazepam, or clonazeopam

33
Q

eszopiclone

A
  • “Lunesta” - sleep aid

MOA: GABAa receptor agonist

** best for pt. who awake early and have difficulty sleeping through night due to t1/2 being 6 hours

Note: long term use of hypnotics of more than 7-10 days may indicate presence of a primary psychiatric or medical illness - needs to be evaluated!

34
Q

ramelteon

A

MOA: agonist at MT­­1 and MT2 melatonin receptors

PK: extensive first-pass effect

Use: treatment of insomnia (difficulty with sleep onset)

ADRs: dizziness, somnolence, fatigue, endo changes (decreased cortisol and testosterone, increased prolactin)

35
Q

zaleplon

A
  • “sonata” - sleep aid

MOA: GABAa receptor agonist

acts rapidly, has short t1/2, thus is used for pts. woho awaken early in sleep cycle - causes less day after amnesia
** good for pt. who has trouble falling asleep d/t rapid action

Note: long term use of hypnotics of more than 7-10 days may indicate presence of a primary psychiatric or medical illness - needs to be evaluated!

36
Q

zolpidem

A
  • “ambien”
  • biphasic release, sleep aid

MOA: GABAa receptor agonist

    • good for pt. who has trouble falling asleep d/t rapid action
    • causes more day after amnesia

Note: long term use of hypnotics of more than 7-10 days may indicate presence of a primary psychiatric or medical illness - needs to be evaluated!

Psych: Test 1 (6 decks)

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