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Pharmacology II Exam 1 > BZD, barbiturates and buspirone > Flashcards

BZD, barbiturates and buspirone Flashcards

1
Q

What BZD is associated with procedural sedation and amnesia?

A

Midazoalm

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2
Q

What BZD is associated with use for muscle relaxation?

A

Diazepam

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3
Q

Which BZD is associated with use for drug and alcohol withdrawal symptoms?

A

Lorazepam

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4
Q

What BZD effects are associated with developed tolerance with chronic use?

A

Anti-seizure and hypnotic effects

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5
Q

Describe the tolerance to anti-anxiety effects of BZDs

A

Develops slowly or not at all

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6
Q

Describe the physiological dependence to BZDs; psychological?

A

Relatively little; more common than physiological (tendency to continue use when not needed)

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7
Q

What happens when someone discontinues using benzodiazepines after long-term use?

A

Symptom recurrence, rebound or withdrawal

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8
Q

Recurrence definition (BZDs)

A

Return of symptoms that required therapy (common with BZDs, weeks-months long)

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9
Q

Rebound definition (BZDs)

A

Symptoms are similar to before but with greater intensity (within hours or days of last dose)

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10
Q

T/F: Rebound symptoms are greater with long-acting BZDs than with short-acting.

A

False (short-acting have greater rebounds)

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11
Q

How is rebound intensity related to dose and duration of use (BZDs)

A

Proportionally

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12
Q

Withdrawal general symptoms (BZDs)

A

General anxiety, sensory disturbances, flu-like

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13
Q

Withdrawal autonomic sympathetic signs (BZDs)

A

Tachycardia/hypertension, tremors, abdominal distress, sweating

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14
Q

Withdrawal symptoms following abrupt DC after long-term use (BZDs)

A

Seizures and delirium

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15
Q

Explain how to discontinue BZDs

A

Switch to longer-acting drug (lorazepam, diazepam) and gradually taper dose by 10% per 1-2 weeks

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16
Q

How can BZDs, specifically longer-acting ones, suppress abstinence symptoms from other CNS depressants like alcohol and barbiturates?

A

Cross-dependence

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17
Q

Why should the use of BZDs be avoided in the elderly?

A

ADEs= confusion, anterograde amnesia are more common in elderly

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18
Q

Paradoxical ADEs of BZDs (2)

A

Hyperactivity, aggression (esp. in pediatric population)

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19
Q

BZD use in pregnancy

A

Chronic use is contraindicated (category D and X)

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20
Q

Toxicity presenting signs (BZDs)

A

Severe drowsiness and ataxia, vital signs usually normal

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21
Q

T/F: BZDs when taken orally do not cause fatal toxicity, but are potentially fatal when combined with alcohol or other CNS depressants.

A

True

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22
Q

Treatment: BZD toxicity

A

Supportive care (technically could use flumazenil)

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23
Q

Competitive antagonist at the BZD receptor sign on GABAa

A

Flumazenil (Romazicon)

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24
Q

Flumazenil blocks the effects of ____, but does NOT reverse the effects of ___(4).

A

BZDs and non-benzo BZD agonists; barbiturates, ethanol, general anesthetics, or opioids

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25
Q

Flumazenil administration, onset time, half-life

A

IV, 1-2 minutes, 1 hour (metabolized by liver)

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26
Q

2 uses of flumazenil:

A

Reverse sedation effect of BZDs after anesthesia, BZD overdose

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27
Q

T/F: Flumazenil is used to treat BZD overdose especially because it re-establishes the airway.

A

False- not a substitute for establishing airway-assisted ventilation

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28
Q

Boxed warning on flumazenil

A

Seizures (esp. in patients on long-term BZD therapy who have taken TCA)

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29
Q

ADEs= amnesia, agitation, dizziness, nausea, may precipitate withdrawal in dependency

A

Flumazenil (BZD receptor antagonist)

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30
Q

Phenobarbital and methohexital + CYP enzymes…

A

Strong inducers of CYP enzymes (multiple DDIs)

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31
Q

Onset of methohexital

A

Rapid (extremely lipid soluble)

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32
Q

What determines methohexital’s DOA after a single dose? Plasma half-life?

A

Redistribution; hepatic metabolism

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33
Q

What determines phenobarbital’s DOA? Plasma half-life?

A

Both determined by hepatic metabolism (less lipid soluble, so does not enter brain as rapidly)

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34
Q

Phenobarbital: % metabolized

A

75%

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35
Q

Phenobarbital: onset time

A

60 minutes

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36
Q

Phenobarbital: duration

A

10-12 h

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37
Q

Phenobarbital: lipid/water

A

3

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38
Q

T/F: Barbiturates have poor analgesic properties but DO relieve anxiety.

A

True

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39
Q

Main use and schedule of phenobarbital

A

Epileptic seizures (status epilepticus), CIV

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40
Q

Off-label use of phenobarbital

A

Treatment of alcohol and sedative/hypnotic withdrawal

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41
Q

Describe phenobarbital’s use as a sedative/hypnotic

A

No longer recommended (overdose is deadly)

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42
Q

Uses of methohexital (2)

A
  • Induction of general anesthesia

- procedural sedation

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43
Q

Tolerance to phenobarbital’s ____ effects occurs, but NOT to its ___ or ____ effects.

A

Sedative-hypnotic; respiratory depression or anti-seizure

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44
Q

What causes the tolerance seen with phenobarbital use?

A

Increased metabolic clearance of the drug (CYP autoinduction)

45
Q

Physical dependence on phenobarbital is a serious problem - what symptoms are seen 8-12 H after last dose?

A

Anxiety, tremors, restlessness, weakness, nausea, vomiting, insomnia

46
Q

Physical dependence on phenobarbital is a serious problem - what symptoms are seen 2 days after last dose?

A

Increased sympathetic activity, delirium, seizures, death

47
Q

How do you treat physical dependence to phenobarbital?

A

Supportive, switch to long-acting barbiturate and taper dose

48
Q

T.I. Of barbiturates (phenobarbital)

A

10

49
Q

ADEs= potentially fatal CNS/respiratory depression, hypotension, paradoxical stimulatory response (esp. in pediatrics), alkalinization of urine (enhances elimination)

A

Barbiturates (phenobarbital, methohexital)

50
Q

MOA of busprione:

A

Unclear, partial agonist at 5-HT1a and 5-HT2 receptors

51
Q

Does buspirone bind to any site on the GABAa receptors?

A

No

52
Q

Use of buspirone

A

Generalized anxiety disorder (less effective for other anxiety disorders like social or panic)

53
Q

ADEs of buspirone (4)

A

Dizziness, restlessness, tachycardia, palpitations (think CNS and CV)

54
Q

What occurs upon abrupt discontinuation of buspirone?

A

Nothing- no rebound anxiety or withdrawal symptoms

55
Q

Use of buspirone while pregnant

A

Safe during pregnancy (category B)

56
Q

Use of buspirone while driving

A

Fine- does not affect motor skills

57
Q

Does buspirone show any abuse potential?

A

No (not a controlled substance)

58
Q

What is the main advantage of buspirone in treating anxiety?

A

No sedative/hypnotic or euphoric effects, NOT additive with other CNS depressants

59
Q

What is the onset of buspirone?

A

3-4 weeks (until anti-anxiety effect becomes established)

60
Q

T/F: Buspirone reverses withdrawal from other CNS depressants.

A

False

61
Q

Buspirone anti-seizure effects

A

None

62
Q

Buspirone muscle relaxant effects

A

None

63
Q

Lipid solubility and ______ are directly proportional

A

onset of action

64
Q

After a single dose, ______ of highly lipid soluble drugs i dependent on the rate of ______ out of the CNS into another compartment

A

duration of action

redistribution

65
Q

Lipid solubility and ______ are inversely proportional

A

duration of action

66
Q

When given chronically, duration of action is dependent on ______

A

hepatic elimination

67
Q

How do AA and glucose readily cross the BBB?

A

L-amino acid transporter

GLUT1

68
Q

The _____ is the primary drug target of CNS drugs

A

neuron

69
Q

neurons are classified by what 3 things?

A

function
location
NT they release

70
Q

Function of neurons are supported by what?

A

glial cells

71
Q

Target selectivity in the CNS is based on what?

A
  • different functions of the brain are mediated by release of specific NTs in discrete regions of brain by distinct groups of neurons
  • specific functions of the brain can be targeted by using drugs highly selective for the receptor subtypes
72
Q

Major excitatory NT

A

glutamate

73
Q

Where does glutamate act?

A

AMPA, KA, NMDA ion channels

74
Q

major inhibitory NT

A

GABA

75
Q

GABA A

A

Cl ion channels

76
Q

GABA B

A

GPCRs

77
Q

nicotinic and muscarinic NT

A

acetylcholine

78
Q

4 amine NTs

A

Serotonin
DA
NE
histamine

79
Q

What NT is associated with Parkinson’s?

A

DA

80
Q

What NT is implicated in virtually all CNS functions?

A

Serotonin

81
Q

What NT modulates arousal and appetite?

A

Histamine

82
Q

Where is MOA-A expressed?

A

GI tract
liver
CNS

83
Q

1st pass metabolism of MOA-A

A

dietary tyramine

84
Q

MAO-A inactivation of

A

Epi
NE
5-Ht
DA

85
Q

MOA-A inhibitors are used to treat

A

depression

86
Q

Where is MOA-B expressed?

A

platelets

CNS

87
Q

MAO-B is selective inactivation of what?

A

DA

88
Q

MAO-B inhibitors are used to treat

A

Parkinson’s

89
Q

Major drug classes of CNS depressants

A

BZD
Barbiturates
Ethanol
General anesthetics

90
Q

Decreased responsiveness to external stimuli, but not asleep; anti-anxiety effect

A

sedation

91
Q

also referred to as dissociative anesthesia

A

sedation

92
Q

pharmacological definition of sleep-like state from which the individual can still be aroused

A

Hypnosis

93
Q

unresponsive to external stimuli but responsive to pain

A

unconsciousness

94
Q

state of unconsciousness where individual is unresponsive to external stimuli or pain, is paralyzed and amnestic

A

anesthesia

95
Q

Non-selective CNS depressants

A

ethanol
barbiturates
general anesthetics

96
Q

Selective CNS depressants

A

BZDs

97
Q

How do CNS depressants bind?

A

allosteric agonists of GABA A

98
Q

5 subunits of GABA-A

A

2alpha
2 beta
gamma

99
Q

Where is the GABA binding site?

A

between beta and alpha

100
Q

Binding of GABA leads to what pore opening?

A

Cl

101
Q

Where is the BZD binding site?

A

between alpha and gamma

102
Q

alpha 1 subunit mediates what functions?

A

sedation
amnesia
ataxia

103
Q

alpha 2,3 subunits mediates what functions?

A

anti-anxiety

muscle relaxing effects

104
Q

alpha 5 subunits mediates what functions?

A

long-term memory and learning effects

105
Q

Binding of BZDs locks the channel into a conformation that increases its affinity for GABA and increases the _____ of chloride channel opening

A

frequency

106
Q

T/f BZDs will produce sedation and hypnosis given orally by themself

A

false

107
Q

t/f barbiturates need the gamma subunit to bind

A

false

108
Q

Barbiturates increase the ____ of chloride channel opening

A

duration

109
Q

t/f at high doses, barbiturate binding can activate the receptor in the absence of GABA

A

true

Pharmacology II Exam 1 (9 decks)

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