Sedatives/Hypnotics Flashcards

0
Q

chlordiazepoxide

A

chlordiazepoxide: Librium
Anxiety, alcohol withdrawal, pre-anaesthetic

long acting benzo
(active metabolites)

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1
Q

alprazolam

A

alazopram: Xanax
anxiety

intermediate acting benzo
(active metabolites)

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2
Q

clonazepam

A

clonazepam: Klonopin
SEIZURES, mania, movement disorders

intermediate acting benzo & centrally acting spasmolytic

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3
Q

diazepam

A

diazepam: Valium
anxiety, STATUS EPILEPTICUS,muscle relaxant, pre-anaesthetic

long acting benzo & centrally acting spasmolytic
(active metabolites)

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4
Q

estazolam

A

estazolam: Prosom
insomnia

intermediate acting benzo

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5
Q

flurazepam

A

flurazepam: Dalmane
insomnia

intermediate acting benzo
(active metabolites)

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6
Q

lorazepam

A

lorazepam: Ativan
anxiety, STATUS EPILEPTICUS, pre-anaesthetic

intermediate acting benzo

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7
Q

midazolam

A

midazolam: Versed
pre-anaesthetic, intraoperative medication

short acting benzo

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8
Q

quazepam

A

quazepam: Doral
insomnia

long acting benzo
(active metabolites)

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9
Q

temazepam

A

temazepam: Restoril
insomnia

intermediate acting benzo

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10
Q

triazolam

A

triazolam: Halcion
insomnia

short acting benzo
(active metabolites)

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11
Q

flunitrazepam

A

flunitrazepam: Rohypnol
date rape drug

long acting benzo

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12
Q

How do benzodiazepines work?

A
increase GABA(a) receptor-mediated inhibition
(increase Cl- conduction -> hyperpolarize neuron -> CNS depression)
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13
Q

Adverse effects of benzodiazepines

A
  • altered sleep
  • CNS depression: impaired mental/motor function, ataxia…
  • withdrawal sx: anxiety, nausea, seizures
  • tolerance
  • abuse
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14
Q

How are benzodiazepines metabolized?

A

hepatic: CYP3A4 glucuronidation –> urinary excretion

some are active metabolites

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15
Q

zolpidem

A

zolpidem: Ambien
increase sleep duration
- withdrawal: anxiety, tremor, agitation, rebound insomnia, seizures

short term (8-10d) non-benzo

16
Q

zaleplon

A

zaleplon: Sonata
help fall asleep
- risk of addiction in long term use

short term (<10d) non-benzo

17
Q

eszopiclone

A

eszopiclone: Lunesta
increase sleep duration
- potential for tolerance, dependence, abuse

long term (up to 6mo) non-benzo

18
Q

Advantages of non-benzodiazepines over benzodiazepines

A
  • less rebound insomnia/withdrawal symptoms

- lower potential for tolerance, dependence, abuse

19
Q

How do non-benzodiazepines (z-drugs) work?

A

bind BZ1 receptors of GABA receptor-Cl channel complex

20
Q

flumazenil

A

flumazenil: Romazicon
reverse action of benzodiazepines (competitive antagonist)

also cause:

  • agitation, confusion, dizziness, nausea
  • withdrawal sx, seizures in benzo overdose/dependence
21
Q

ramelteon

A

ramelteon: Rozeram
melatonin agonist (MT1/MT2)
no CNS depression
CYP1A2

22
Q

Advantages of Melatonin agonist

A
  • no CNS depression
  • no motor/cognitive impairment
  • little withdrawal sx/rebound insomnia
  • can be used long term
  • not controlled, no abuse potential
23
Q

Adverse effects of Melatonin agonist

A
  • increased serum prolactin

- decreased testosterone

24
Q

buspirone

A

partial agonist at serotonin receptor
: anxiolytic
less abuse potential than benzos
no CNS depression

25
Q

doxylamine

A

doxylamine: Unisom (and others)

OTC sleep aid

26
Q

diphendydramine

A

diphenhydramine: Benadryl (and others)

OTC sleep aid

27
Q

How does alcohol affect sleep?

A

hypnotic:

  • initial CNS depression
  • later rebound excitation (disrupts sleep)
28
Q

GHB

A

gamma-hydroxybutyrate/sodium oxybate:
metabolite and precursor for GABA
: cataplexy, narcolepsy

  • addictive, abuse risk: hallucinogenic, euphoric
29
Q

What do spasmolytics do and what conditions can they treat?

A

muslce relaxants: tx for spasms

  • MS
  • ALS
  • spinal cord transection
  • cerebral palsy
  • stroke
  • local muscle trauma
30
Q

Centrally acting spasmolytics

A
  • diazepam/clonazepam
  • baclofen
  • tizanidine
31
Q

baclofen

A

baclofen: Lioresal
centrally acting spasmolytic, less sedation than benzos

GABA(b) receptor agonist

32
Q

tizanidine

A

tizanidine: Zanaflex
centrally acting spasmolytic

alpha-2 adrenergic agonist (pre-/post-synaptic inhibition of motor neurons)

33
Q

dantrolene

A

dantrolene: Dantrium
direct acting spasmolytic

causes muscle weakness (not for ALS)
can treat malignant hyperthermia