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4. Pharm III > 1- Sedative-Hypnotics and Anxiolytics > Flashcards

1- Sedative-Hypnotics and Anxiolytics Flashcards

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1
Q

What is the primary use of sedative-hynotic and anxiolytic drugs?

A

Encourage calmness and produce sleep

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2
Q

GABA is the major inhibitory NT. Activation of it leads to what effect on the body?

A

Decreased anxiety and promotion of sleep

depression of electrical activity/ CNS depressant

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3
Q

HA, palpitaions, tremor, perspiration, GI effects and dizziness are manifestation of what class of disorders?

A

Anxiety disorders

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4
Q

What is a maladaptive response in a person w/ an anxiety disorder?

A

Chronic and psychological stress, organ dysfunction, physical sxs

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5
Q

What is the “ideal drug” for treating an anxiety disorder?

A

Relieves anxiety w/o sedation/ drowsiness, no physical/ psychological dependence

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6
Q

What is the tx for acute anxiety disorder (short term and self limited) vs generalized anxiety disorders (chronic)?

A

Acute- benzodiazepines

Generalized- benzodiazepines/ buspirone

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7
Q

What is the tx for anxiety in children and adolescents?

A

Antidepressants

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8
Q

What is the tx for panic disorder/ agoraphobia (episodic, severe attacks)?

A

SSRIs

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9
Q

What is the tx for OCD?

A

SSRIs

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10
Q

What is the tx for PTSD?

A

Antidepressants

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11
Q

What an “ideal” drug to tx insomnia?

A

Sedative hypnotic → fall asleep quickly and stay asleep for as long as want, wear off in the AM, no “hangover” effect

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12
Q

What is the tx for transient or short-term insomnia (occurs w/ situational stress)?

A

Sedative hypnotics

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13
Q

What is the tx for long-term insomnia (related to underlying psychiatric disease or chronic alcohol/drug abuse)?

A

Behavioral therapy and lifestyle changes

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14
Q

What is the tx for hypersomnia and narcolepsy?

A

Stimulants

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15
Q

Kleine-Levin Syndrome is aka what and falls under what class of disorders?

A

AKA: “Sleeping beauty”, sleep disorders

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16
Q

What is the DOC for enureisis?

A

Tricyclic Antidepressants

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17
Q

What is the tx for sleep apnea?

A

CPAP and lifestyle changes

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18
Q

What is the MOA for barbiturates?

A

Bind to GABAA receptor to produce Cl influx and inhibition independent of GABA

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19
Q

Why are barbiturates abuses?

A

Causes feelings of euphoria

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20
Q

Do barbiturates cross the BBB?

A

Yes

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21
Q

Where are barbiturates metabolized? What do they induce?

A

Liver, induce CYP450s (LOTS of drug interactions)

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22
Q

What are the SEs for barbituates? (7)

A 
CNS depression (toxic doses)
Paradoxical excitement
Severe dependence (psych + phys)
Vertigo
N/V/D
Allergic rxn
Respiratory depression
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23
Q

When are barbiturates C/i? (2)

A

Porphyria, in combo w/ alcohol (supra-additive effects)

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24
Q

Withdrawal from what medication will cause severe sx of restlessness, anxiety, weakness, seizure, but is not fatal?

A

Barbiturates

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25
Do barbiturates have a ceiling effect? Why? What does this mean for its margin of safety?
No, b/c functions independently of GABA. LOW margin of safety
26
Coma, espiratory depression and hypotension are overdose sx of what medication?
Barbiturates
27
What is the tx for barbiturate overdose?
Supportive care, diuresis, alkalization of the urine
28
What drug class is Thiopental?
Barbiturates
29
What is the duration of action for Thiopental?
Short acting
30
What is Thiopental used for?
Induction of anesthesis
31
What drug class is Phenobarbital?
Barbiturates
32
What is the duration of action for Phenobarbital?
Long acting
33
What is Phenobarbital used for?
Used as anticonvulsant to tx partial and generalized tonic-clonic seizures
34
What is the MOA for benzodiazepines?
Bind to GABAA receptor, ↑ affinity of receptor to GABA prolonging its actions (effect dependent on GABA)
35
Do Benzodiazepines have a ceiling effect?
Yes! (limited GABA pool = effect plateaus once all GABA is used up despite an ↑ dose)
36
How are benzodiazepines metabolized?
CYP3A4 in liver
37
When are IV benzodiazepines used?
Emergencies, pre-anesthesia
38
What are the SEs for benzodiazepines? (3)
CNS depression (toxic doses), paradoxical excitement (dis-inhibition of suppressed behavior), sleep-related behaviors (sleep driving, eating, walking, etc)
39
When are benzodiazepines C/i? (4)
pregnancy, sleep apnea, elederly (can’t metabolize well), w/ alcohol use (supre-additive effects),
40
Tolerance to benzodiazepines is common. What effect does this have on dose and abuse potential?
Doses are not typically increased. High abuse potential
41
What are the effects of abrupt cessation/withdrawal of benzodizepines? (7)
Rebound ↑ anxiety and insomnia, muscle weakness, tremor, hyperalgesia, vomiting, weight loss, convulsions
42
What is the recommendation for stopping chronic benzodiazepine use?
Taper very slowly
43
What are the sx of a benzodiazepine OD?
Long deep sleep (24-48 hrs). Overall drug is relatively safe.
44
Possible fatality from a benzodizepine OD can occur in what populations?
People w/ respiratory difficulties, children, combine w/ alcohol
45
When prescribing a benzodiazepine. What is the general recommendation for dose and duration?
Lowest effect dose for shortest possible duration (to limit SE)
46
What is a general SE of drugs used to tx insomnia?
Minor depression of REM sleep → “hangover” effect
47
Which benzodiazepines have a long duration of action? (4)
Diazepam, Flurazepam, Chlordiazepoxide, Clonazepam
48
Anti-anxiety/ sedative drugs with a long duration of action result in what?
Hangover effect
49
Which anti-anxiety/ sedative drugs have an intermediate duration of action? (3)
Alprazolam, Oxazepam/Lorazepam, Temazepam
50
What is the duration of action for Midazolam?
Short (No hangover effect)
51
What are the 2 DOCs for status epilepticus?
Diazepam and Lorazepam (given IV or rectally)
52
What is Diazepam used to tx? (3)
DOC for status epilepticus, acute muscle spasm/ pain as a result of injury, tapered withdrawal from alcohol and barbiturates
53
What is flurazepam used to tx?
Insomnia (hypnotic)
54
What is Chlordiazepoxide used to tx?
Tapered withdrawal from alcohol and barbituates
55
What is Clonazepam used to tx? (3)
Absence seizures, myoclonic seizures, infantiles spams (West syndrome)
56
What is Oxazepam/lorazepam used to tx? (2)
Status epilepticus, tapered withdrawal from alcohol and barbiturates
57
What is Temazepam used to tx?
Insomnia (hypnotic)
58
What is Midazolam used to for?
Preparation for anesthesia for short surgical procedures
59
How is Midazolam administered?
IV
60
What is a SE of Midazolam?
Can cause anterograde amnesia
61
What drug class is Diazpam?
Benzodiazepines
62
What drug is Flurazepam?
Benzodiazepines
63
What drug class is Chlordiazepoxide?
Benzodiazepines
64
What drug class is Clonazepam?
Benzodiazepines
65
What drug class is Alprazolam?
Benzodiazepines
66
What drug class is Oxazepam/Lorazepam?
Benzodiazepines
67
What drug class is Temazepam?
Benzodiazepines
68
What drug class is Midazolam?
Benzodiazepines
69
What is the MOA for Flumazenil?
Benzodiazepine antagonist- competes w/ BZ’s for GABA receptor and reverses BZ effects
70
What is the use of Flumazenil?
Reverses respiratory depression caused by Midazolam, hypersomnia conditions
71
What is the duration of action of Flumazenil? What does this mean for it's hangover effect?
Short duration of action. No hangover effect
72
What are the SE of flumazenil?
Triggers withdrawal and seizures in patients who are physically dependent on BZs
73
When is Flumazenil C/i?
HX of seizures
74
What are the "z" drugs?
Zolpidem, Zaleplon, Eszopiclone
75
What is the MOA for the "Z" drugs?
Bind to BZ1 subtype of GABA receptor → increase GABA-mediated inhibition
76
When are "Z" drugs used?
Used for insomnia (strong/ rapid sedative effects)
77
Do the "Z" drugs have anxiolytic, anticonvulsant, or muscle relaxant properties?
No
78
What is the duration of action for the Eszopiclone?
Long duration of action
79
What is the duration of action for Zaleplon and Zolpidem? What does this mean for it's hangover effect?
Short duration of action, no hangover effect
80
Where are the "Z" drugs metabolized?
Liver by CYP3A4
81
Where are the "Z" drugs excreted?
Kidney
82
If pt w/ severe liver disease, what effect does this have on the half life of the "z" drugs?
Prolongs half life
83
Which of the "Z" drugs is uded for long term tx?
Eszopiclone
84
The "Z" drugs have a very high margin of safety. What are the SEs?
GI, CNS depression, sleep-related behaviors
85
If the "Z" drugs are rapdily discontinued/withdrawn what are the SEs?
Rebound insomnia, withdrawal sxs
86
In what population are the "Z" drugs C/I?
Elderly (can cause confusion, memory loss, psychosis)
87
What is the MOA for Suvorexant?
Antagonist at orexin receptors (involved in regulating sleep-wake cycle and promote wakefulness)
88
What is Sovorexant metabolized by?
CYP3A4
89
What are the SE to Suvorexant? (2)
HA, abn dreams
90
When is Suvorexant C/I? (2)
Depression, narcolepsy
91
What is the MOA for Ramelteon?
Melatonin analogue, resets sleep-wake cycle, promotes sleepiness w/ no GABA effect
92
Where is Ramelteon metabolized?
Metabolized in liver by CYP450s
93
Ramelteon is absored orally. What does this mean for its first pass metabolism?
Extensive first pass metabolism
94
What are the SEs for Ramelteon?
Drowsiness, dizziness, nausea (high doses)
95
Ramelteon can have toxic additive sedation effects if combined with what?
Alcohol, other sedative hypnotics
96
What is the use for 1st gen antihistamines?
Sedation
97
What is a benefit to using 1st gen antihistamines for sedation?
No abuse potential
98
What drug class is Hydroxyzine and Benadryl?
Antihistamine
99
What are the uses of Hydroxyzine as a sedative-hypnotic? (3)
Anti-anxiety, prevents nausea/ emesis caused by motion sickness, anti-Parkinson effects (used to treat EPS)
100
When is Benadryl used as a sedative-hypnotic?
Useful for occasional insomnia, especially if hx of addiction to benzo or alcohol
101
What is the MOA for Chloral Hydrate?
Acts similarly to barbiturates on GABAA receptor
102
When and why is Chloral hydrate used?
CHEAP, sedation in pediatric dental procedures, nursing homes, chronic care institutions
103
Chloral Hydrate has a LOW margin of safety. What are potential SEs?
High doses induce respiratory and vasomotor depression, GI sx, allergic response, +/- cardiac arrhythmias
104
Chronic use of Choral hydrate can result in what? (2)
Liver damage and fatal intoxication
105
When is chloral hydrate C/I?
As a sedative-hypnotic
106
What is the MOA for Buspirone?
Partial agonist at postsynaptic serotonin (5-HT1A) receptor, full agonist at presynaptic serotonin receptor)
107
What is the benefit to using buspirone for the tx of anxiety?
Relieves anxiety w/o producing sedations (can be taken during the day)
108
When is Buspirone used?
To tx mild generalized anxiety and anxiety and depression, ADHD and autistic pts w/ anxiety, premenstrual syndrome
109
Why is Buspirone used in pts w/ hx of alcohol or benzodiazepine abuse?
Very low addiction potential | no muscle relaxant or anticonvulsant properties, does not potentiate CNS depression w/ alcohol or BZs
110
How long does Buspirone take to become effective?
2 weeks
111
Where is Buspirone metabolized?
Liver by CYP3A4
112
What are the SE of Buspirone? (5)
Light-headedness, restlessness, HA, drowsiness, N/V
113
What drugs are metabolised by CYP450?
Ramelteon
114
What drugs are CYP450 inducers
Barbituates (Thiopental, Phenobarbital)
115
What medications are classified as "other sedative-hypnotics"? (10)
Flumazenil, Zolipdem, Zaleplon, Eszopiclone, Suvorexant, Ramelteon, Hydroxyzine, Benadryl, Chloral Hydrate, Buspirone

4. Pharm III (16 decks)

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