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Pharmacology > Sedative Hynotics > Flashcards

Sedative Hynotics Flashcards

1
Q

Hypnotics uses?

A

produce drowsiness

encourages onset and maintenance of sleep

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2
Q

What are some sedative-hypnotics?

A
  1. benzodiazepines
  2. barbiturates
  3. non-benzodiazepine benzodiazepine recpetor agonists
  4. 5HT1A receptor partial agonists
  5. melatonin agonists
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3
Q

Benzodiazepines

MOA?

A

bind to GABAa receptors (chloride channel) b/w adjacent alpha and gamma subunit -> opens channel -> increase Cl influx.

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4
Q

What is benzodiazepine receptor AGONIST interaction?

A
  • positive allosteric modulators

- exert anxiolytic and anticonvulsant effects.

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5
Q

What is benzodiazepine receptor ANTAGONIST interaction?

A

flumazenil: blocks actions of benzodiazepines

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6
Q

What is benzodiazepine receptor INVERSE AGONIST interaction?

A
  1. negative allosteric modulators of GABA receptr function

2. cause anxiety and seizures.

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7
Q

what are the actions of benzodiazepines?

A
  1. reduction of anxiety
  2. sedative and hypnotic actions
  3. anticonvulsant
  4. muscle relaxant
  5. anesthesia
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8
Q

benzodiazepines

PK?

A

lipophilic
rapidly and completely absorbed after oral administration
distributed throughout body

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9
Q

what are long-acting benzodiazepines?

A
  1. diazepam

2. flurazepam

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10
Q

what are intermediate-acting benzodiazepines?

A
  1. alprazolam
  2. lorazepam
  3. temazepam
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11
Q

what are short-acting benzodiazepines?

A
  1. oxazepam

2. triazolam

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12
Q

how is desmethyldiazepam metabolized?

A

desmethyldiazepam = active metabolite of several benzo

- then metabolized to the active compound oxazepam

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13
Q

how is oxazepam, lorazepam, and temazepam metabolized?

A

oxazepam, lorazepam, temazepam are conj. directly (no P450)

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14
Q

how is flurazepam metabolized?

A

flurazepam is oxidized to active metabolites hydroxyethyl-flurazepam and desalkyl-flurazepam.

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15
Q

What are therapeutic uses of benzodiazepines?

A
  1. anxiety disorders
  2. muscular disorders
    - diazepam: skeletal muscle spasm, spasticity from degenrative disorders (MS or cerebral palsy)
  3. seizures
    - clonazepam: epileptic seizures
    - lorazepam & diazepam: status epilepticus
  4. drug withdrawal
    - diazepam & oxazepam: EtOH withdrawal
  5. anesthesia
  6. Sleep disorders
    - flurazepam (long), temazepam (intermediate), triazolam (short)
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16
Q

what are some benzodiazepines a.e’s?

A
  1. drowsiness and confusion
  2. ataxia
  3. cognitive impairment
  4. psychological effects
    - anxiety, irritability, hostility/rage, paranoia, depression, suicial ideation
  5. dependence
  6. withdrawal sx’s when d/c abruptly
    - confusion, anxiety, agitation, restlessness, insomnia, tension
17
Q

what is a benzo antagonist?

A

flumazenil

18
Q

flumazenil

uses?

A

reverse CNS depressant effects of benzo overdose

hasten recovery following use in anesthetic and diagnostic procedures.

19
Q

flumazenil

A.E?

A

precipitate withdrawal in physiologically dependent pts or

cause seizures if a benzodiazepine is used to control seizures.

20
Q

why has benzo replaced barbiturates?

A
  1. induced tolerance
  2. induced drug-metabolizing enzymes
  3. physical dependence
  4. severe withdrawal sx’s
  5. coma c high dose
21
Q

barbiturates

MOA?

A
  1. act on GABAa receptors -> increases duration of GABA-gated Cl channel openings.
  2. block glutamate receptors and Na channels
22
Q

barbiturates

actions?

A
  1. depression of CNS
    - low dose = sedation
    - high dose = hypnosis -> anesthesia -> coma, death
  2. respiratory depression
  3. enzyme induction (P450)
23
Q

barbiturates

uses?

A
  1. anesthesia (thiopental)
  2. anticonvulsant (phenobarbital)
    - tonic-clonic seizures, status epilepticus and eclampsia.
  3. anxiety
  4. hepatic metabolic
    - tx hyperbilirubinemia and kernicterus
24
Q

barbiturates

A.E?

A
  1. CNS - drowsy, impaired concentration, metnal/physical sluggishness
  2. paradoxical excitement
  3. hypersensitivity
  4. hangover
  5. increase porphyrin synthesis - contraindicated pts c porphyria.
  6. respiratory depression in pts c pulmonary insuff.
  7. pain
  8. dependence
  9. poisoning: respiratory depress and central CV depress.
25
Q

what is non-benzodiazepine benzodiazepine receptor agonists?

A

act only on the BZ1 subtype of benzo receptors.

  1. Zolpidem
  2. Zaleplon
  3. Eszopiclone
26
Q

eszopiclone

uses?

A

insomnia

decreases sleep latency and improves sleep maintenance.

27
Q

zolpidem

uses?

A

insomnia, difficulties c sleep initiation.

short action

28
Q

Zaleplon

uses?

A

short term tx of insomnia

29
Q

what is a 5HT1A partial agonists?

A

buspirone

30
Q

buspirone

uses?

A

anxiety disorders

analogous to antidepressants MOA.

31
Q

buspirone

advantages?

A
  1. less psychomotor impairment
  2. no rx interaction c EtOH
  3. no rx interactions c benzo and other sedative-hypnotics
  4. no rebound anxiety or withdrawal signs on abrupt d/c
  5. no dependence.
32
Q

what is a melatonin receptor agonist?

A

ramelteon

33
Q

ramelteon

uses?

A

agonist at MT1 and MT2 melatonin receptors

insomnia, difficulty c sleep onset.

34
Q

what are other sedative-hypnotics?

A
  1. hydroxyzine
    - relief anxiety
  2. propranolol
    - control performance anxiety
  3. clonidine
  4. diphenhydramine and doxylamine
    - mild insomnia
35
Q

Sedative uses?

A

reduce anxiety

calming effect c little or no effect on motor or mental functions.

Pharmacology (13 decks)

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