Pharm - Sedatives and Hypnotics Flashcards

1
Q

list the benzodiazepine antagonist

A

flumazenil

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2
Q

-pam suffix indicates what type of drug

A

benzodiazepines

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3
Q

-barbital indicate what type of drug

A

bartbiturates

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4
Q

compare sedatives to hypnotic drugs

A

sedatives: decrease CNS activity, moderates excitement, calms pt

hypnotic drug: produces drowsiness, facilitates onset and maintenance of sleep
- more pronounced depression of the CNS

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5
Q

MOA benzodiazepines

A

binds to GABA-A receptor and enhances GABA’s effects

–> chloride influx –> hyperpolarization –> fewer number of action potentials –> CNS depression

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6
Q

describe the advantages of benzos

A

1) high therapeutic index
2) antagonist available for OD
3) low risk of drug-drug interactions
4) minimal effect on CV or autonomic system

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7
Q

describe the disadvantages of benzos

A

1) risk of dependence
2) depression of CNS function
3) amnestic effects
4) bad when combined with alcohol

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8
Q

describe the half life, active metabolite status, and rate of onset for Diazepam

A

half life: >100 hours
active metabolites: yes
rate of onset: very fast

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9
Q

describe the half life, active metabolite status, and rate of onset for Alprazolam

A

half life: 12-15 hrs
active metabolites: insignificant
rate of onset: fast

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10
Q

list the short to intermediate acting benzos

A

1) alprazolam
2) oxazepam
3) temazepam
4) midazolam
5) traizolam

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11
Q

list the intermediate to long acting benzos

A

1) diazepam
2) lorazepam
3) clonazepam

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12
Q

indications for Alprazolam

A
  • anxiety disorder

- panic disorder

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13
Q

contraindications for Alprazolam

A
  • pts w/ acute narrow angle glaucoma

- w/ ketoconazole and itraconazole

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14
Q

indications for midazolam

A

preoperative sedation/anxiolysis/amnesia

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15
Q

black box warning for midazolam

A

respiratory depression

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16
Q

indications for diazepam

A
  • management of anxiety disorders and for short term relief of sx of anxiety
  • also used in acute alcohol withdrawal
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17
Q

how does milk to moderate cirrhosis affect use of diazepam

A

the average half-life is increased from 2-5 fold

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18
Q

contraindications for diazepam

A

1) peds pts under 6 months
2) myasthenia gravis
3) respiratory insufficiency
4) severe hepatic 3 insufficiency
5) sleep apnea
6) acute narrow angle glaucoma

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19
Q

warnings for diazepam

A

not recommended in tx of psychotic pts and don’t use w/ alcohol

20
Q

indications oxazapam

A

anxiety, anxiety w/ depression, and acute alcohol withdrawal

21
Q

indications triazolam

A

short term tx of insomnia (7-10 days)

22
Q

indications chlordiazepoxide

A

1) management of anxiety disorders or for short term relief of anxiety
2) alcohol withdrawal
4) preoperative apprehension and anxiety

23
Q

indications flurazepam

A

long acting hypnotic agent useful for tx of insomnia

24
Q

indications lorazepam

A

seizure disorders like epilepsy

- can also be used before surgery to relieve anxiety

25
Q

indications buspirone

A

tx of generalized anxiety disorder

***takes more than a week to become establihsed

26
Q

indications flumazenil

A

complete or partial reversal of sedative effects of benzos

- management of ODs

27
Q

MOA flumazenil

A

competitively inhibits activity at benzo recognition site on GABA receptor

28
Q

black box warning flumazenil

A

seizures most frequently in pts who have been on benzos for long time

29
Q

MOA barbituates

A

binds to GABA-A receptor and increases duration of GABA gated channel openings
–> chloride influx –> hyperpolarization –> decreased number of action potentials –> CNS depression

30
Q

compare the typical indications for ultra short acting, short acting, and long acting barbiturates

A

ultra short: anesthesia

short: insomnia
long: seizures

31
Q

indications thiopental

A

1) sole anesthetic agent for brief procedures
2) induction of anesthesia prior to other anesthetic agents
3) supplements regional anesthesia
4) hypnosis during balanced anesthesia w/ other agents
5) control convulsive states during or following anesthesia
6) increase intracranial pressure in neurosurgical pts

32
Q

indications secobarbital

A

hypnotic for the short term tx of insomnia (loses effectiveness after 2 weeks)

33
Q

contraindications secobarbital

A

marked impairment of liver, respiratory dz

34
Q

indications phenobarbital

A

sedative or hypnotic

35
Q

contraindications phenobarbital

A

pts with history of manifest or latent porphyria

36
Q

MOA ramelteon

A

full agonist at MT1 and MT2 melatonin receptors

37
Q

metabolism of ramelteon

A

metabolized by CYP1A2

38
Q

adverse effects ramelteon

A

dizziness, somnolence, fatigue, endocrine changes

39
Q

indications ramelteon

A

insomnia characterized by difficulty with sleep onset

40
Q

MOA zaleplon

A

interacts with GABA-benzodiazapine receptor complex (but is not a benzo)

41
Q

indications zaleplon

A

short term tx of insomnia

42
Q

indications zolpidem

A

short term tx of insomnia characterized by difficulties with sleep initiation

43
Q

indications eszopiclone

44
Q

indications meprobamate

A

anxiety disorders or for short term relief of sx of anxiety

45
Q

MOA meprobamate

A

slowing activity in brain to allow for relaxation

46
Q

indications chloral hydrate

A

short term use as sedative or sleep med