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D1 Spring > Pharmacology - Sedative-Hypnotics, Antianxiety Drugs, and Centrally Acting Muscle Relaxants (Exam 2) > Flashcards

Pharmacology - Sedative-Hypnotics, Antianxiety Drugs, and Centrally Acting Muscle Relaxants (Exam 2) Flashcards

1
Q

What are the sedative-hypnotics?

A

Benzodiazepines
Benzodiazepine-like
Barbiturates

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2
Q

What are the anxiolytics?

A

Benzodiazepines

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3
Q

What are the centrally acting muscle relaxants?

A

Benzodiazepines

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4
Q

A drug that reduces excitement and calms the patient without inducing sleep

A

Sedative

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5
Q

A drug that produces sleep resembling natural sleep

A

Hypnotic

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6
Q

Are sedatives and hypnotics analgesic?

A

NO

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7
Q

Some ________ may increase sensitivity to pain

A

Barbiturates

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8
Q

What do many sedatives induce?

A

Anterograde amnesia (no memories during tx)

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9
Q

Drug that decreases worriness manifested as the psychic awareness of anxiety, which is accompanied with increased vigilance, motor tension, and autonomic hyperreactivity

A

Anxiolytic

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10
Q

Drug that affects skeletal muscle function and decreases muscle tone; can alleviate symptoms such as muscle spasms, pain, and hyperreflexia

A

Muscle relaxant

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11
Q

Centrally acting muscle relaxants

A

Spasmolytics

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12
Q

Drug that reduces muscle tone by acting on various levels of the motor pathway within the central nervous system (cortex, brainstem, spinal cord)

A

Spasmolytic

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13
Q

Drug used to treat spasticity in a variety of neurological conditions

A

Spasmolytic

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14
Q

Sedative-hypnotics, antianxiety drugs, and centrally acting muscle relaxants act as _____ _________

A

CNS depressants

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15
Q

Name the spectrum of actions of sedative-hypnotics, antianxiety drugs, and centrally acting muscle relaxants

A

Anxiolysis
Sedation
Muscle relaxation
Anticonvulsant
Hypnosis
Anesthesia
Coma
Death

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16
Q

Various _______ dependent beneficial effects follow the CNS _______ spectrum. The deeper the depression, the closer to _______ ________

A

dose; depression; toxic overdose

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17
Q

Where are the anxiolytic sedative effects produced?

A

Limbic system (depressive action)

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18
Q

Where are hypnosis and deep sedation effects produced?

A

Reticular activating system in the brainstem

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19
Q

What happens to the brain in a coma?

A

General brain depression

(cerebral cortex first, and then autonomic centers in brainstem)

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20
Q

Dose response curve for barbiturates

A

Steep

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21
Q

Dose response curve for benzodiazepines

A

Flattens as dose increases

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22
Q

Which drug has a greater margin of safety, barbiturates or benzodiazepines?

A

Benzodiazepines

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23
Q

Benzodiazepines with psychopharmacologic activity have an electronegative group at _____, which confers the strongest CNS depressant activity

A

R7

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24
Q

A nitro moiety at R7 enhances ____________ properties

A

anti-seizure

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25
Q

Benzodiazepines enhance inhibitory neurotransmission mediated by _________

A

GABA

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26
Q

What are the 2 types of GABA receptors?

A

GABA-A and GABA-B

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27
Q

Benzodiazepines act on/modulate ________ receptors

A

GABA-A

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28
Q

GABA-A receptors are __________ forming a GABA-gated ___________ channel

A

pentamers; Cl-/HCO3-

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29
Q

What happens when benzodiazepine binds to GABA-A receptors:

  1. _________ frequency of Cl- channel opening when ______ is present
  2. _____________ of plasma membrane, increased duration of miniature _________ (postsynaptic GABA-A), decreased probability of synaptic _________ release (presynaptic GABA-A)
  3. Reduced probability of ________
A
  1. Increased; GABA
  2. Hyperpolarization; IPSPs; vesicle
  3. excitation
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30
Q

GABA is an ________

A

Agonist

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31
Q

Benzodiazepines are _________ _________

A

Allosteric modulators

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32
Q

Do benzodiazepines work in the absence of GABA or another agonist?

A

NO

(remember, benzodiazepines are allosteric modulators)

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33
Q

Which drugs promote positive regulation of GABA?

A

Barbiturates
Benzodiazepines
Alcohol, inhalational anesthetics, propofol

34
Q

Barbiturates ________ and ______ GABA action

A

facilitate; mimic

35
Q

Benzodiazepines ________ GABA action

A

facilitate

36
Q

Alcohol, inhalational anesthetics, and propofol ______ the Cl channel _______

A

open; directly

37
Q

Which drugs promote negative regulation of GABA?

A

Bicuculline
Flumazenil
Picrotoxin

38
Q

Which drug is the antidote for benzodiazepine?

A

Flumazenil

39
Q

Bicuculline is a _______ ________ at GABA Rc

A

Competitive antagonist

40
Q

Flumazenil is a __________ ________ at BZD site

A

Competitive antagonist

41
Q

Picrotoxin ________ Cl channel ________

A

blocks; non-competitively

42
Q

Which subunits of the GABA-A receptor are responsible for anxiolytic activity?

A

a2 and/or a3

43
Q

Which subunits of the GABA-A receptor are responsible for muscle relaxation?

44
Q

Which subunits of the GABA-A receptor are responsible for hypnotic activity, anticonvulsant activity (partially), and anterograde amnesia?

45
Q

What does the diversification of various combinations of subunits in the GABA-A receptors help explain?

A

Relative selectivity of some benzodiazepines to produce specific therapeutic effects

46
Q

Benzodiazepines are _______

A

lipophilic

47
Q

What happens after oral administration of benzodiazepines

A

Rapid and complete absorption

48
Q

Benzodiazepines penetrate into the _____

49
Q

Longer acting benzodiazepines form ______ metabolites with ______ half lives

A

active; long

50
Q

Benzodiazepines cross the _________ _________ and are excreted with ________

A

placental barrier; milk

51
Q

Some benzodiazepines are _______ absorbed, which _______ their action, despite rapid metabolism and post-absorption

A

slowly; prolongs

52
Q

Short acting benzodiazepines

A

Triazolam
Oxazepam
Midazolam

53
Q

Intermediate acting benzodiazepines

A

Alprazolam
Estazolam
Temazepam
Lorazepam
Nitrazepam

54
Q

Long acting benzodiazepines

A

Diazepam
Flurazepam
Clonazepam
Chlordiazepoxide

55
Q

Which benzodiazepines are safe to use in patients with liver disease?

A

Estrazolam
Temazepam
Lorazepam
Oxazepam

(non-oxidized benzodiazepines)

56
Q

Which benzodiazepines go through alpha-hydroxylation?

A

Alprazolam
Midazolam
Triazolam

57
Q

Why is alpha-hydroxylation something to be aware of?

A

Alpha-hydroxylation is done by hepatic CYP3A4 - must take caution in patients with liver disease!

58
Q

Which group of benzodiazepines form slowly eliminated active metabolites?

A

Long acting benzodiazepines

59
Q

Name the CYP3A4 inhibitors that cause an interaction with the benzodiazepines that undergo alpha-hydroxylation

A

Erythromyocin
Intraconazole
Verapamil, Diltiazem
Fluoxetine
Cimetidine
Grapefruit juice

60
Q

The anti-anxiety effects of benzodiazepines are _________ subject to tolerance than the sedative and hypnotic effects

61
Q

As tolerance and physiological dependence develop over time, _______ therapy with benzodiazepines should only be ________

A

anxiolytic; acute

62
Q

Which benzodiazepines are most useful to treat insomnia?

A

Short acting

(sleep phases are less disturbed)

63
Q

T/F benzodiazepines are usually not associated with respiratory depression and apnea

64
Q

T/F toxic side effects (respiratory depression, hypnosis, coma, death) may be enhanced if benzodiazepines are combined with other CNS depressants like alcohol, antihistamines, or opioids

65
Q

What is the paradoxic reaction of benzodiazepines that can occur in the elderly and young?

A

CNS excitation instead of depression

(nightmares, hyperactivity, insomnia, irritability, agitation, rage, hostility)

66
Q

Toxic side effects of benzodiazepines may also be enhanced by drugs that reduce their ___________ metabolism

Which benzodiazepines are used if this interaction cannot be avoided?

A

phase I

non-oxidized benzodiazepines

67
Q

What are the drugs that reduce phase I metabolism of benzodiazepines?

A

Cimetidine
Ca2+ channel blockers (Verapamil, Diltiazem)
Macrolids (Erythromyocin)
Protease inhibitors (Indinavir)
Antimycotics (Intraconazole)
Antidepressants (Fluoxetine)

68
Q

T/F toxic side effects of benzodiazepines may be enhanced by young age and liver disease

A

FALSE - old age and liver disease

69
Q

What effects are associated with benzodiazepine use in 3rd trimester of pregnancy?

A

Cleft palate
Baby benzo withdrawal
Infant hypotonia
Hypothermia respiratory depression

70
Q

Which benzo is classified as category X (meaning strong evidence of teratogenic effects - no use during pregnancy)

71
Q

What drug is used to speed up recovery from benzo-induced sedation?

A

Flumazenil (the benzo antagonist)

72
Q

Decreasing sensitivity to benzos with prolonged tx, caused by benzo-induced decrease in GABA-A expression

73
Q

Increased excitation and insomnia. Causes similar effects of tolerance

A

Withdrawal

74
Q

How soon does benzo withdrawal occur?

A

After 2 weeks of use

75
Q

Which benzos are more likely to cause withdrawal?

A

Short acting (Triazolam)

76
Q

T/F use of benzos may be associated with tolerance and dependence. Stopping may induce withdrawal

77
Q

What drugs have a non-benzodiazepine structure, but have action on the same site of the GABA-A receptor?

A

Z-hypnotics

78
Q

T/F Z-hypnotics are safe for short term use (even in pregnancy) and have less tolerance, but possible addiction after long term use

79
Q

Which drug is often combined with other sedatives to increase their effectiveness and also act as anti-emetics?

A

Anti-histaminics (hydroxizine, promethazine)

80
Q

When using diazepam as a central spasmolytic, effects on muscle tone are mostly ________

A

supraspinal

81
Q

What are the precautions while using CNS depressants?

A
  1. No driving for 24 hrs (drowsiness)
  2. No alcohol/other CNS depressants
  3. Adjust dose for elderly

D1 Spring (47 decks)

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