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521-Pharmacology > sedative-hypnotics > Flashcards

sedative-hypnotics Flashcards

(51 cards)

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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

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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

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A

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

23
Q

Muscle relaxation

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A

certain benzodiazepines and meprobamate may depress transmission at the neuromuscular junction

24
Q

Respiration and cardiovascular function

Study These Flashcards
A

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

25
Buspirone
-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
Ramelteon and tasimelteon
-melatonin receptor agonist -no effect on GAM+BA -Ramelteon reduces latency -has longer half life than melatonin
27
Suvorexant
-first orexin receptor antagonist to treat insomnia -orexin A and B peptides involved in wakefulness
28
Lemborexant (Dayvigo)
-Insomnia -Orexin antagonist
29
Daridorexant(Quviviq)
-Insomnia -orexin receptor antagonist
30
off label hypnotic drugs
-trazodone -mirtazipine -doxepin -amitriptyline
31
OTC hypnotic
-diphenhydramine -doxylamine -melatonin -CNM (Cannabinol)
32
PK of sedative-hypnotics
-all cross the placenta barrier
33
Desmethyldiazepam
-active metabolite for clorazepate, chlordiazepoxide, diazepam, and prazepam -LONG half life
34
Triazolam
-short half life (2-5 hrs) -favors use as hypnotic rater than sedative
35
Alprazolam an Triazolam metabolism
-same mechanism due to similar structure -alpha-hydroxylation results in short half life due to inactive glucuronides
36
Metabolism of barbiturates
-oxidation via hepatic enzymes -relatively slow
37
Z Drugs PK
-absorbed rapidly -biphasic release-metabolized to inactive metabolite by 3A4
38
Phenobarbital PK
-long half life -20-30% excreted unchanged in urine
39
Tolerance
decreased responsiveness following repeated exposure -common in sedative-hypnotics
40
cross tolerance
can occur between sedative hypnotics and ethanol because of down regulation of GABA receptor?
41
Psychologic component of dependence
-behavioral patterns -compulsive
42
Physiologic component of dependence
-altered state that requires continuous drug administration to prevent abstinence or withdrawal syndrome -withdrawal symptoms are worse for meds with short half life
43
Clinical uses for sedative hypnotics
-anxiety -insomnia -sedation and amnesia -epilepsy -withdrawal -muscle relaxation
44
secondary anxiety
-results from circumstances that are dealt with once or twice -medical procedures
45
Alprazolam
-panic disorder and agoraphobia -more selective than other benzos -more toxic in overdose
46
choice of benzo for anxiety
1)onset of action 2) therapuetic index 3) risk for drug interactions 4) cardio or autonomic effects
47
Disadvantages of benzodiazepines
-dependence -depression of CNS functions -amnesia effects -newer SSRI first choice
48
delirium tremens drug treatment
parenteral lorazepam
49
muscle relaxants
meprobamate diazepam: skeletal muscle spascity
50
Toxic actions of sedative hypnotics
-low dose: drowsiness, impaired job perform and -sleep walking with no memory -amnesia -hangover effects -elderly more sensitive!
51
drug interactions
other CNS depressant drugs

521-Pharmacology (11 decks)

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