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NMSP Exam 1 > Sedative and Hypnotic Drugs - Iszard > Flashcards

Sedative and Hypnotic Drugs - Iszard Flashcards

1
Q
  • alprazolam
  • chlordiazepoxide
  • clonazepam
  • clorazepate
  • diazepam
  • flurazepam
  • lorazepam
  • midazolam
  • oxazepam
  • triazolam
A

benzodiazepines

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2
Q

flumazenil

A

benzodiazepine antagonist

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3
Q 
amobarbital
butaparbital
pentobarbital
phenobarbital
secobarbital
thiopental
A

barbiturates

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4
Q 
buspirone
chloral hydrate
eszopiclone
meprobamate
ramelteon
zaleplon
zolpidem
A

misc/newer sedative-hypnotic drugs

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5
Q

triazolam

A

short action benzo

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6
Q

alprazolam

A

intermediate action benzo

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7
Q

flurazepam

A

long action benzo

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8
Q

thiopental

A

ultra-short action barbiturate

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9
Q

secobarbital

A

short action barbiturate

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10
Q

phenobarbital

A

long action barbiturate

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11
Q

drug that decreases CNS activity, moderates excitement, calms the recipient

A

sedative

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12
Q

drug that produces drowsiness and facilitates the onset and maintenance of sleep, from which the recipient can be aroused easily

A

hypnotic

NOTE: hypnotic effects involve more pronounced depression of the CNS, which can be achieved with many drugs in this class by increasing the dose

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13
Q

what is the relationship between benzodiazepines and barbiturates on CNS effects?

A

benzodiazepines level off around anesthesia (don’t cause medullary depression or come like barbiturates can)

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14
Q
  • act on GABA-A receptors

- cause sedation, hypnotic effects, muscle relaxation, anxiolytic and anticonvulsant effects

A

benzodiazepines

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15
Q
  • act on GABA-A receptors

- cause a wide spectrum of effects: mild sedation to anesthesia

A

barbiturates

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16
Q
  • act on multiple receptor systems: GABA-A and melatonin

- used as sleep aides, treatment of delirium, anxiety, seizures

A

miscellaneous sedative-hypnotics

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17
Q

hepatic metabolism and excretion via kidney

  • CYP3A4 (phase I) ad glucuronidation (phase II)
  • binds the GABA-A receptors and enhances GABA’s effects
A

benzodiazepines

NOTE: risk of dependence and tolerance

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18
Q

what are the disadvantages of benzodiazepines?

A

risk of dependence, depression of CNS function (especially bad if combined with alcohol!), amnesia

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19
Q

what is the half life of diazepam?

A

> 100 hours KNOW this

  • has active metabolites
  • half life is increased in mild/moderate cirrhosis, can be up to 500 hours!
20
Q

what is the half life of alprazolam?

A

12-15 hours

- insignificant active metabolites

21
Q

extensively metabolized in humans, primarily CYP3A4

  • indicated in anxiety disorder and panic disorder
  • may be used in pts with open angle glaucoma
A

alprazolam

22
Q

which drug is contraindicated with ketoconazole and itraconazole?

A

alprazolam

- since these meds significantly impair CYP3A4

23
Q

given IM or IV as sedation agent prior to procedures

  • induction of general anesthesia
  • black box warning associated with respiratory depression/arrest, especially when used in noncritical care settings
A

midazolam

24
Q

this drug exerts anxiolytic, sedative, muscle relaxant, anticonvulsant and amnestic effects d/t GABA facilitation

  • indicated for management of anxiety
  • may be used in acute alcohol withdrawal
A

diazepam

25
Q

when is diazepam contraindicated?

A

myasthenia gravis, severe respiratory insufficiency, severe hepatic insufficiency, and sleep apnea syndrome

26
Q

what is the warning associated with dizepam?

A
  • NOT recommended in tx of psychotic patients

- pts should NOT take with alcohol (d/t CNS depressant)

27
Q

what drug is used in the treatment of anxiety, anxiety with depression and acute alcohol withdrawal?

A

oxazapam

28
Q

what drug is indicated for the short-term treatment of insomnia (generally 7-10 days)
- black box warning concomitant use with opioids can result in profound sedation, respiratory depression, coma and death

A

triazolam

29
Q

what drug is used from anxiety management, short term relief of sx of anxiety, withdrawal sx of acute alcoholism, and preoperative apprehension/anxiety

A

chlordiazepoxide

- also has black box warning against use with opioids

30
Q

what drug is a long acting hypnotic agents, useful for the treatment of insomnia characterized by difficulty falling asleep, frequent nocturnal awakenings and/or early morning awakening

A

flurazepam

NOT used long-term! if insomnia doesn’t stop after 7-10 days, it may indicate a primary psychiatric illness is present

31
Q

what drug is used in the treatment of seizure disorders (epilepsy)
- also used before surgery and medical procedures

A

lorazepam

32
Q
  • approved for the tx of generalized anxiety disorder
  • effects may take more than a week
  • does not cause sedation, hypnotic, euphoric, anticonvulsant or muscle relaxant effects
  • extensive metabolism by CYP3A4
A

buspirone

33
Q

what drug is indicated for the complete or partial reversal of the sedative effects of benzos, and the management of benzodiazepine overdose?

A

flumazenil (benzo antagonist)

- black box warning can cause seizures in patients showing signs of serious cyclic antidepressant overdose

34
Q

what are the specific conditions that barbiturates are limited to treating?

A
  • extreme insomnia
  • seizures unresponsive to other meds
  • induction of anesthesia
  • in combination w/acetaminophen and caffeine to relieve tension headaches
  • used to counteract the stimulant effects from coke and meth
35
Q

these drugs bind the GABA-A receptor, increasing the duration of GABA-gated channel openings
- can induce CYP450 enzymes

A

barbiturates

  • *risk of dependence and tolerance**
  • *overdose can cause death**
36
Q

given IV as sole anesthetic for brief (15 min) procedures or prior to administation of other anesthetic agents

A

thiopental (truth serum)

37
Q

what are the adverse reactions of thiopental?

A

respiratory depression, myocardial depression, cardiac arrhythmias, prolonged somnolence and recovery

38
Q

hypnotic, used for short-term treatment of insomnia or preanesthetic
- contraindicated in pts w/hypersensitivity to barbiturates, or a hx of manifest or latent porphyria, marked impairment of liver function, or respiratory disease

A

secobarbital

warning: failure of insomnia to remit after 7-10 days of treatment ay indicate psychiatric illness that should be evaluated

39
Q

what drug is indicated for use as a sedative or hypnotic

- contraindicated in patients with hx of manifest or latent porphyria

A

phenobarbital

NOTE: should be administered with cause to pts who are mentally depressed, have suicidal tendencies, or hx of drug abuse
**has been shown to induce liver microsomal enzymes, thus increasing or altering the metabolism of barbiturates and other drugs

40
Q

what drugs are used to treat insomnia?

A

benzodiazepines

NOTE: cause daytime sedation and patients may develop anterograde amnesia and tolerance

41
Q

tx of insonmia

- highly effective, rapid onset, minimal hangover effects

A

zolpidem, zaleplon, eszopiclone

  • zolpidem has biphasic release forumla for sustained sleep maintenance
  • eszopiclone has longest half life
42
Q

what drug is an agonist at melatonin receptors MT-1/2

- produces significant sedation

A

ramelteon

- metabolized by CYP1A2

43
Q

hepatic metabolism and excretion via kidney (CYP3A4)

  • relatively short half lives (<6hrs) so useful as hypnotics rather than sedatives
  • binds GABA-A that contain a1 subunit
  • ONLY approved for tx of sleep disorders
A

sleep aids

- eszopiclone, zolpidem, zaleplon

44
Q

nonbenzo hypnotic agent that interacts with GABA-BZ receptor complex
- indicated for short-term treatment of insomnia

A

zaleplon

NOTE: if it doesn’t cure insomnia after 7-10 days, consider psychiatric illness

45
Q

what drug is indicated for short-term treatment of insomnia characterized by difficulties with sleep initiation

A

zolpidem

NOTE: worsening depression or suicidal thoughts may occur. alcohol NOT recommended d/t CNS depressant effects

46
Q

what drug is indicated for the treatment of insomnia characterized by difficult with sleep onset

  • high affinity for MT-1/2 and selectivity over MT3
  • CYP1A2 is major isozyme
A

ramelteon

47
Q

what drug is indicated for treatment of insomnia, and has shown to decrease sleep latency and improve sleep maintenance

A

eszopiclone

  • do NOT take with alcohol d/t CNS depressant effects**
  • adverse rxns in pts with hepatic impairment, impaired respiratory function, impaired drug metabolism or hemodynamic response

NMSP Exam 1 (19 decks)

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