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521-Pharmacology > sedative-hypnotics > Flashcards

sedative-hypnotics Flashcards

1
Q

sedative-hypnotic class use

A

-cause sedation or to encourage sleep

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2
Q

sedative (anxiolytic) drugs use

A

reduce anxiety and produce a calming effect

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3
Q

hypnotic drug use

A

cause drowsiness and promote the onset and maintenance of a state of sleep

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4
Q

Barbiturates

A

-much older and less commonly used
-pentobarbital
-secobarbital
-phenobarbital

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5
Q

Sedative hypnotics with distinct features

A

-Glutethimide
-Meprobamate(Miltown)
-chloral hydrate
-ethanol

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6
Q

Benzodiazepines

A

-widely used
-most contain carboxamide group
-a halogen OR nitro group is required of activity

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7
Q

Triazolam and alprazolam structure

A

include triazole ring

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8
Q

z drugs

A

-zolpidem(Ambien)
-zaleplon(Sonata)
-Eszopiclone(Lunesta)

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9
Q

Where does GABA interact?

A
  • at two sites between alpha and beta subunits
    -this triggers chloride channel to open and hyperpolarize
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10
Q

Where do benzodiazepines and z drugs bind at the receptor?

A

between alpha and gamma subunits, but z drugs only interact with a1 subunits

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11
Q

Flumazenil

A

-competitive benzodiazepine antagonist
-binds between alpha and gamma subunit
-reverse benzo and z drug effects
-short half life so require multiple doses

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12
Q

True or False: Benzodiazepines directly activate GABA receptors

A

False.
-enhances GABA’s effects allosterically
-increased frequency of channel opening event

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13
Q

Barbiturates action at GABA receptor

A

-increase duration of the opening of GABA gated chloride channels
-at high conc., may directly open channels

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14
Q

Sedation

A

-overall calming effects
-produced euphoria, impaired judgement
-AMNESIA (benzodiazepines)

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15
Q

Hypnosis

A

-all sedative-hypnotics will induce sleep if high enough dose

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16
Q

effects of benzodiazepines on sleeps:

A

1)time to fall asleep decreased
2) Stage 2 NREM increased
3) REM decreased
4) Stage 4 NREM decreased

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17
Q

effects of zolpidem on sleep

A

decrease REM

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18
Q

effect of zaleplon on sleep

A

decrease the latency of sleep onset with little effect on total sleep time, NREM, or REM

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19
Q

effect of eszopiclone on sleep

A

-increase total sleep time: increase stage 2
-decreases REM at highest dose

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20
Q

Significance of sedative-hypnotics on sleep

A

-REM rebound: crazy dreams in older drugs
-rebound insomnia in zolpidem and zalpelon

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21
Q

Anesthesia

A

-benzodiazepines such as diazepam, lorazepam, and midazolam may be used for anestesia
-suitability is determined by rapidity of onset and duration of effect

22
Q

anticunvulsant

A

benzos: clonazepam, nitrazepam, lorazepam, diazepam
barbituates: phenobarbital(tonic-clonic)

23
Q

Muscle relaxation

A

certain benzodiazepines and meprobamate may depress transmission at the neuromuscular junction

24
Q

Respiration and cardiovascular function

A

-comparable to natural sleep
-significant effect in patients with pulmonary disease

25
Q

Buspirone

A

-relieves anxiety without causing sedative, hypnotic, or euphoric effects
-no anticonvulsant or muscle relaxant properties, no effect on GABA
-5-HT1a receptor agonist
-risk of serotonin syndrome with 3A4 inhibitors

26
Q

Ramelteon and tasimelteon

A

-melatonin receptor agonist
-no effect on GAM+BA
-Ramelteon reduces latency
-has longer half life than melatonin

27
Q

Suvorexant

A

-first orexin receptor antagonist to treat insomnia
-orexin A and B peptides involved in wakefulness

28
Q

Lemborexant (Dayvigo)

A

-Insomnia
-Orexin antagonist

29
Q

Daridorexant(Quviviq)

A

-Insomnia
-orexin receptor antagonist

30
Q

off label hypnotic drugs

A

-trazodone
-mirtazipine
-doxepin
-amitriptyline

31
Q

OTC hypnotic

A

-diphenhydramine
-doxylamine
-melatonin
-CNM (Cannabinol)

32
Q

PK of sedative-hypnotics

A

-all cross the placenta barrier

33
Q

Desmethyldiazepam

A

-active metabolite for clorazepate, chlordiazepoxide, diazepam, and prazepam
-LONG half life

34
Q

Triazolam

A

-short half life (2-5 hrs)
-favors use as hypnotic rater than sedative

35
Q

Alprazolam an Triazolam metabolism

A

-same mechanism due to similar structure
-alpha-hydroxylation results in short half life due to inactive glucuronides

36
Q

Metabolism of barbiturates

A

-oxidation via hepatic enzymes
-relatively slow

37
Q

Z Drugs PK

A

-absorbed rapidly
-biphasic release-metabolized to inactive metabolite by 3A4

38
Q

Phenobarbital PK

A

-long half life
-20-30% excreted unchanged in urine

39
Q

Tolerance

A

decreased responsiveness following repeated exposure
-common in sedative-hypnotics

40
Q

cross tolerance

A

can occur between sedative hypnotics and ethanol because of down regulation of GABA receptor?

41
Q

Psychologic component of dependence

A

-behavioral patterns
-compulsive

42
Q

Physiologic component of dependence

A

-altered state that requires continuous drug administration to prevent abstinence or withdrawal syndrome
-withdrawal symptoms are worse for meds with short half life

43
Q

Clinical uses for sedative hypnotics

A

-anxiety
-insomnia
-sedation and amnesia
-epilepsy
-withdrawal
-muscle relaxation

44
Q

secondary anxiety

A

-results from circumstances that are dealt with once or twice
-medical procedures

45
Q

Alprazolam

A

-panic disorder and agoraphobia
-more selective than other benzos
-more toxic in overdose

46
Q

choice of benzo for anxiety

A

1)onset of action
2) therapuetic index
3) risk for drug interactions
4) cardio or autonomic effects

47
Q

Disadvantages of benzodiazepines

A

-dependence
-depression of CNS functions
-amnesia effects
-newer SSRI first choice

48
Q

delirium tremens drug treatment

A

parenteral lorazepam

49
Q

muscle relaxants

A

meprobamate
diazepam: skeletal muscle spascity

50
Q

Toxic actions of sedative hypnotics

A

-low dose: drowsiness, impaired job perform and
-sleep walking with no memory
-amnesia
-hangover effects
-elderly more sensitive!

51
Q

drug interactions

A

other CNS depressant drugs

521-Pharmacology (11 decks)

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