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PHRM 845 > L58 - Sedative, Hypnotics, and Anxiolytics. pt 1 > Flashcards

L58 - Sedative, Hypnotics, and Anxiolytics. pt 1 Flashcards

1
Q

Calms anxiety, decreases excitement and activity, does not produce drowsiness, or impair performance.
A. Sedative
B. Anxiolytic
C. Hypnotic
D. Narcotic

A

A

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2
Q

Antianxiety, relieves anxiety without sleep or sedation (not all anxiolytics are sedatives)
A. Sedative
B. Anxiolytic
C. Hypnotic
D. Narcotic

A

B

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3
Q

Induces sleep, implies restful, refreshing sleep, not “hypnotized!”, natural sleep (medial use term: sleeping-inducing)
A. Sedative
B. Anxiolytic
C. Hypnotic
D. Narcotic

A

C

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4
Q

Actually means “sleep producing”, now refers to opioids or illegal drugs
A. Sedative
B. Anxiolytic
C. Hypnotic
D. Narcotic

A

D

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5
Q

the reticular formation extends through the central core of what 3 brain structures

A

medulla oblongata, pons, and midbrain

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6
Q

3 stages of sleep (in order)

A

wakefulness
NonREM
REM

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7
Q

what neurotransmitters are biological regulators of sleep?

A

it says almost all and theres like so i aint typing all that just know its all of the major ones except dopamine

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8
Q

what neuromodulators are biological regulators of sleep? (5)

A

growth hormone
prolactin
cortisol
melatonin - no shit
endogenous peptides

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9
Q

what receptor is a pentameric structure comprised of 5 subunits from several polypeptide classes

A

GABA-A

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10
Q

~50% of total GABA-A receptors
A. GABA-A a1
B. GABA-A a2
C. GABA-A a3
D. GABA-A a5

A

A. GABA-A a1

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11
Q

Ubiquitous anatomical distribution.
A. GABA-A a1
B. GABA-A a2
C. GABA-A a3
D. GABA-A a5

A

A. GABA-A a1

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12
Q

Anatomical distribution is in hippocampus
A. GABA-A a1
B. GABA-A a2
C. GABA-A a3
D. GABA-A a5

A

D. GABA-A a5

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13
Q

Anatomical Distribution found in cortex, limbic system, spinal cord
A. GABA-A a1
B. GABA-A a2
C. GABA-A a3
D. GABA-A a5

A

B and C

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14
Q

is most closely affiliated with addiction properties
A. GABA-A a1
B. GABA-A a2
C. GABA-A a3
D. GABA-A a5

A

B. GABA-A a2

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15
Q

GABA-A Receptor/Chloride Ion Channel Complex:
Targets for _______-________

A

sedative-hypnotics

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16
Q

GABA-A Receptor/Chloride Ion Channel Complex:
what 2 receptors are at the orthosteric site?

A

GABA a1
GABA B2

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17
Q

GABA-A Receptor/Chloride Ion Channel Complex:
3 most common receptors

A

2a1, 2B2, 1y2

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18
Q

GABA-A Receptor/Chloride Ion Channel Complex:
what 2 receptors are at the allosteric site?

A

a1 and y2

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19
Q

Ligands Acting at the BZD Receptor:
Benzodiazepines: Facilitate _____ action, increase ________

A

GABA, frequency

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20
Q

Ligands Acting at the BZD Receptor:
Non-Benzos: (__________): zolpidem, zaleplon, eszopiclone - __ receptors of __ (sorry i didnt know how else to make this card)

A

Z-hypnotics
BZ1 of a1

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21
Q

BZD Antagonist: __________, overdose tx

A

Flumazenil

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22
Q

T or F: BZDs increase the duration of GABA-A channels opening

A

False, frequency

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23
Q

What drug class increases duration of channel opening?

A

Barbiturates

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24
Q

What drug class has DIRECT effects on GABA-A receptor in high doses

A

barbiturates

25
Q

SAR of Benzos:
what structural change is the source of active metabolites of benzos? **

A

1 position alkylation

26
Q

SAR of Benzos:
Annealing the 1-2 bond with an “electron rich” ring (triazole or imidazole) yields high affinity and decreased half-life

A

this isnt a question i just put it in here to read it so i understand wtf it means

27
Q

T or F: Diazepam has a long half-life

A

true

28
Q

Tx of convulsive disorders (seizures), accumulation of metabolites
A. Flurazepam
B. Quazepam
C. Diazepam
D. Chlordiazepoxide

A

C. Diazepam

29
Q

T or F: diazepam has a slow elimination rate

A

True

30
Q

T or F: Clonazepam has a rapid elimination rate

A

False, intermediate

31
Q

T or F: Midazolam has a rapid elimination rate

A

True

32
Q

Used as an anticonvulsant.
A. Alprazolam
B. Clonazepam
C. Oxazepam
D. Temazepam

A

B. Clonazepam

33
Q

Rapid Anesthesia
A. Clonazepam
B. Diazepam
C. Lorazepam
D. Midazolam

A

D. Midazolam

34
Q

Usage of slow elimination benzos (1 thing underlined)

A

active metabolites

35
Q

T or F: Benzos have more CNS effects as you increase dose than barbiturates do

A

False, barbiturates are much more dangerous

36
Q

T or F: Benzos decrease REM

A

True for some reason

37
Q

T or F: Benzos increase stage 3 and 4 of NREM sleep

A

False, decreases and i have no idea if this is a good or bad thing

38
Q

T or F: benzos have anticonvulsant activity

A

duh

39
Q

T or F: Side effects of benzos are dose dependent

A

no shit

40
Q

3 side effects listed under sedation for benzos

A

confusion, ataxia, daytime sedation

41
Q

precautions with benzos (3.5)

A

other sedatives
alcohol (another sedative)
Pregnancy and breastfeeding

42
Q

T or F: Barbiturates have higher abuse potential than benzos

A

true

43
Q

what drug is used to treat benzo overdose?

A

Flumazenil (romazicon)

44
Q

two side effects under flumazenil with a * next to them

A

panic attacks and induce convulsions

45
Q

where do z-hypnotics act

A

bzd binding site (BZ1 receptor)

46
Q

Short-term tx of insomnia
A. Zolpidem
B. Zaleplon
C. Eszopiclone

A

A and B

47
Q

Long term tx of insomnia
A. Zolpidem
B. Zaleplon
C. Eszopiclone

A

C. Eszopiclone

48
Q

T or F: Z-hypnotics cause more negative effects on sleep patterns vs BZD

A

False, less

49
Q

FDA warning to pts on z-hypnotics

A

sleep-driving
sleep-cooking
sleep-eating
sleep-sex

50
Q

Long acting anticonvulsant
A. Phenobarbital
B. Mephobarbital
C. Pentobarbital

A

A. Phenobarbital

51
Q

Short to intermediate acting sedative-hypnotic
A. Phenobarbital
B. Mephobarbital
C. Pentobarbital

A

C. Pentobarbital

52
Q

T or F: Barbiturates have a risk of respiratory depression

A

True

53
Q

Bind to all GABA-A a1-5 receptors
A. Barbiturates
B. Benzos
C. Z-hypnotics

A

A and B

54
Q

increase duration of GABA-A channel opening
A. Barbiturates
B. Benzos
C. Z-hypnotics

A

A. barbiturates

55
Q

increase frequency of GABA-A channel opening
A. Barbiturates
B. Benzos
C. Z-hypnotics

A

B. Benzos
C. Z-hypnotics

56
Q

has direct effects on GABA-A channel in high doses
A. Barbiturates
B. Benzos
C. Z-hypnotics

A

A. Barbiturates

57
Q

Bind to GABA-A BZD receptors of a1
A. Barbiturates
B. Benzos
C. Z-hypnotics

A

C. Z-hypnotics

58
Q
A

PHRM 845 (34 decks)

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