Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PHAR 230 > M5 L3: Sedative-Hypnotics Agents > Flashcards

M5 L3: Sedative-Hypnotics Agents Flashcards

1
Q

what are sedatives

A
  • reduce anxiety
  • exert a calming effect w/o inducing sleep
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what are hypnotics

A
  • produce drowsiness
  • encourage onset and maintenance of sleep
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

is CNS depression worse for hypnotics or sedatives

A

hypnotics > sedatives

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

indications of sedative-hypnotics

A
  • anxiety
  • insomnia
  • amnesia + sedation
  • epilepsy and seizure
  • control of other drug withdrawal states
  • muscle relaxation
  • treatment in psychiatry
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

classes of sedative hypnotic drugs

A
  • benzodiazepines (ex: diazepam)
  • newer hypnotics: nonbenzodiazepines, z-drugs (ex: zolpidem)
  • barbiturates (ex: phenobarbital)

others: (can look on slide for ex)
- melatonin receptor agonists
- orexin antagonist
- 5-HT receptor agonists
- antihistaminics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

ion channels and NT receptors for sedative hypnotic drugs

A

**ligand-gated ion channel (ionotropic receptor)
- voltage gated ion channel
- G protein-coupled receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

what is a GABAa receptor

A

ligand: GABA
- mediated inhibitory synaptic transmission in CNS
- target of barbiturates, benzodiazepines, and new hypnotics
Ionotropic receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

what are benzodiazepines

A
  • widely used sedative hypnotic drugs
  • commonly used in 1990s
  • heterocyclic 1,4-benzodiazepine ring sys
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

sedative hypnotic drugs mech of action

A
  • act allosterically
  • bind specific site on GABAa receptor, distinct from GABA binding site
  • sedative hypnotics have a positive receptor affinity to GABA
  • they facilitate GABA-mediated Cl-channel opening frequency
  • this leads to an increase in membrane hyperpolarization
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

short acting ex of sedative hypnotic drugs

A

triazolam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

intermediate acting ex of sedative hypnotic drugs

A

alprazolam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

long acting ex of sedative hypnotic drugs

A

diazepam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

what is the absorption through GIT of sedative hypnotic drugs

A
  • variable rate - ex: triazolam is extremely rapid
  • gastric HCL converts clorazepate (prodrug) -> active form
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

what is the metabolism of sedative hypnotic drugs

A

in the liver:
phase 1 - oxidation by P450 isozymes specially CYP3A4
phase 2 - conjugation results in glucuronides

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

how are sedative hypnotic drugs excreted

A

in urine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

how is sedative hypnotic drugs administered

A

oral, IM, IV, rectal

17
Q

how are sedative hypnotic drugs metabolized

A

done thru phase 1/2 reactions. use active metabolites, and go primarily thru conjugation

18
Q

what are the effects of sedative hypnotic drugs

A
  • sedation, hypnosis, anaesthesia (decline when taken after 1-2 weeks)
  • anticonvulsant effect
  • muscle relaxation
  • respiratory depression, and cardiovascular depression (dangerous)
19
Q

what are common adverse effects of sedative hypnotic drugs

A
  • drowsiness, dizziness, deceased alertness and concentration
  • impaired coordination
  • decreased libido and ED
  • impaired memory
  • paradoxical reactions
  • overdose and acute toxicity
  • tolerance and dependence
20
Q

sedative hypnotic drug tolerance

A
  • develops w long-term use
  • shown mainly w sedative-hypnotic muscle relaxant and anticonvulsant effects
  • partial cross tolerance
  • mech: not understood well but in animals its thru a downregulation of receptors
21
Q

sedative hypnotic drug dependence

A
  • arises from perceived relief of anxiety, euphoria, disinhibition, and promotion of sleep
22
Q

what are ex of drug interactions that add to CNS depression with sedative hypnotic drugs

A
  • additive CNS depression
  • alcohol
  • opioids
  • anticonvulsants
  • antidepressants
  • antihistamines
23
Q

what is flumazenil

A

1,4-benzodiazepine derivative
* Competitive antagonist with high affinity to
benzodiazepine binding site on GABAA receptor
* Blocks many actions of benzodiazepines & Z-
drugs
* Used in the treatment of overdose (antidote)
* Administration: IV – dose should be repeated
(short t1/2)

24
Q

what are new hypnotic (Z-drugs)

A

Introduced in the late 80s / early 90s
* Strong hypnotics but weak sedatives
* Pharmacokinetics: refer to the table (look in slideshow)
* Less tolerance & dependence
* Administration: oral

25
Q

ex of new hypnotic (Z-drugs)

A
  • E.g., zolpidem, zaleplon, and eszopiclone
26
Q

what are newer hypnotic (z-drugs) mech of action, and effect similar too

A

benzodiazepines

27
Q

what have barbiturates mostly been replaced by

A

benzodiazepines
(bc of significant higher risk of overdose, lack of antidote)

28
Q

what are barbiturates derived from

A

barbituric acid

29
Q

barbiturates mech of action

A
  • act allosterically
  • bind to specific GABAa receptor
  • barbiturates have a +’ve receptor affinity to GABA
  • they increase the duration of GABA-mediated Cl- channel opening
  • this leads to an increase in membrane hyperpolarization
  • causes CNS depression associated w the effects of the drug
    (take a look at slideshow)
30
Q

medical uses of barbiturates

A
  • general anesthetics ( thiopental-IV)
  • anticonvulsants
  • insomnia (replaced by benzodiazepines) [phenobarbital - oral]
31
Q

adverse effects and drug interactions of barbiturates

A
  • similar to benzodiazepines
  • dependence > benzodiazepines
  • hepatic microsomal enzymes induction leads to an increased metabolism
  • more linear dose-response w barbiturates can increase toxicity
32
Q

what kind of drugs are sedative-hypnotics

A

lipophilic drugs

33
Q

sedative-hypnotics and pregnancy

A

avoid in:
- 1st trimester - teratogenic effect
- 3rd trimester - may induce premature labour
- Z-drugs are safer than benzodiazepines bc of lack of data
- antihistamines might b reasonable in early pregnancy

34
Q

sedative-hyponotics and dependence/withdrawal sympt

A
  • barbiturates > benzodiazepines > Z-drugs
  • short acting > long-acting
  • cross dependence can help prevent withdrawal sympt
    ex: long-acting alleviate withdrawal sympt by shorter-acting drugs

PHAR 230 (31 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions