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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
Benzodiazepines enhance inhibitory neurotransmission mediated by _________
GABA
26
What are the 2 types of GABA receptors?
GABA-A and GABA-B
27
Benzodiazepines act on/modulate ________ receptors
GABA-A
28
GABA-A receptors are __________ forming a GABA-gated ___________ channel
pentamers; Cl-/HCO3-
29
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 ________
1. Increased; GABA 2. Hyperpolarization; IPSPs; vesicle 3. excitation
30
GABA is an ________
Agonist
31
Benzodiazepines are _________ _________
Allosteric modulators
32
Do benzodiazepines work in the absence of GABA or another agonist?
NO (remember, benzodiazepines are allosteric modulators)
33
Which drugs promote positive regulation of GABA?
Barbiturates Benzodiazepines Alcohol, inhalational anesthetics, propofol
34
Barbiturates ________ and ______ GABA action
facilitate; mimic
35
Benzodiazepines ________ GABA action
facilitate
36
Alcohol, inhalational anesthetics, and propofol ______ the Cl channel _______
open; directly
37
Which drugs promote negative regulation of GABA?
Bicuculline Flumazenil Picrotoxin
38
Which drug is the antidote for benzodiazepine?
Flumazenil
39
Bicuculline is a _______ ________ at GABA Rc
Competitive antagonist
40
Flumazenil is a __________ ________ at BZD site
Competitive antagonist
41
Picrotoxin ________ Cl channel ________
blocks; non-competitively
42
Which subunits of the GABA-A receptor are responsible for anxiolytic activity?
a2 and/or a3
43
Which subunits of the GABA-A receptor are responsible for muscle relaxation?
a2
44
Which subunits of the GABA-A receptor are responsible for hypnotic activity, anticonvulsant activity (partially), and anterograde amnesia?
a1
45
What does the diversification of various combinations of subunits in the GABA-A receptors help explain?
Relative selectivity of some benzodiazepines to produce specific therapeutic effects
46
Benzodiazepines are _______
lipophilic
47
What happens after oral administration of benzodiazepines
Rapid and complete absorption
48
Benzodiazepines penetrate into the _____
CNS
49
Longer acting benzodiazepines form ______ metabolites with ______ half lives
active; long
50
Benzodiazepines cross the _________ _________ and are excreted with ________
placental barrier; milk
51
Some benzodiazepines are _______ absorbed, which _______ their action, despite rapid metabolism and post-absorption
slowly; prolongs
52
Short acting benzodiazepines
Triazolam Oxazepam Midazolam
53
Intermediate acting benzodiazepines
Alprazolam Estazolam Temazepam Lorazepam Nitrazepam
54
Long acting benzodiazepines
Diazepam Flurazepam Clonazepam Chlordiazepoxide
55
Which benzodiazepines are safe to use in patients with liver disease?
Estrazolam Temazepam Lorazepam Oxazepam (non-oxidized benzodiazepines)
56
Which benzodiazepines go through alpha-hydroxylation?
Alprazolam Midazolam Triazolam
57
Why is alpha-hydroxylation something to be aware of?
Alpha-hydroxylation is done by hepatic CYP3A4 - must take caution in patients with liver disease!
58
Which group of benzodiazepines form slowly eliminated active metabolites?
Long acting benzodiazepines
59
Name the CYP3A4 inhibitors that cause an interaction with the benzodiazepines that undergo alpha-hydroxylation
Erythromyocin Intraconazole Verapamil, Diltiazem Fluoxetine Cimetidine Grapefruit juice
60
The anti-anxiety effects of benzodiazepines are _________ subject to tolerance than the sedative and hypnotic effects
less
61
As tolerance and physiological dependence develop over time, _______ therapy with benzodiazepines should only be ________
anxiolytic; acute
62
Which benzodiazepines are most useful to treat insomnia?
Short acting (sleep phases are less disturbed)
63
T/F benzodiazepines are usually not associated with respiratory depression and apnea
True
64
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
True
65
What is the paradoxic reaction of benzodiazepines that can occur in the elderly and young?
CNS excitation instead of depression (nightmares, hyperactivity, insomnia, irritability, agitation, rage, hostility)
66
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?
phase I non-oxidized benzodiazepines
67
What are the drugs that reduce phase I metabolism of benzodiazepines?
Cimetidine Ca2+ channel blockers (Verapamil, Diltiazem) Macrolids (Erythromyocin) Protease inhibitors (Indinavir) Antimycotics (Intraconazole) Antidepressants (Fluoxetine)
68
T/F toxic side effects of benzodiazepines may be enhanced by young age and liver disease
FALSE - old age and liver disease
69
What effects are associated with benzodiazepine use in 3rd trimester of pregnancy?
Cleft palate Baby benzo withdrawal Infant hypotonia Hypothermia respiratory depression
70
Which benzo is classified as category X (meaning strong evidence of teratogenic effects - no use during pregnancy)
Triazolam
71
What drug is used to speed up recovery from benzo-induced sedation?
Flumazenil (the benzo antagonist)
72
Decreasing sensitivity to benzos with prolonged tx, caused by benzo-induced decrease in GABA-A expression
Tolerance
73
Increased excitation and insomnia. Causes similar effects of tolerance
Withdrawal
74
How soon does benzo withdrawal occur?
After 2 weeks of use
75
Which benzos are more likely to cause withdrawal?
Short acting (Triazolam)
76
T/F use of benzos may be associated with tolerance and dependence. Stopping may induce withdrawal
True
77
What drugs have a non-benzodiazepine structure, but have action on the same site of the GABA-A receptor?
Z-hypnotics
78
T/F Z-hypnotics are safe for short term use (even in pregnancy) and have less tolerance, but possible addiction after long term use
True
79
Which drug is often combined with other sedatives to increase their effectiveness and also act as anti-emetics?
Anti-histaminics (hydroxizine, promethazine)
80
When using diazepam as a central spasmolytic, effects on muscle tone are mostly ________
supraspinal
81
What are the precautions while using CNS depressants?
1. No driving for 24 hrs (drowsiness) 2. No alcohol/other CNS depressants 3. Adjust dose for elderly

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