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

1- Sedative-Hypnotics and Anxiolytics Flashcards

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
Q

Do barbiturates have a ceiling effect? Why? What does this mean for its margin of safety?

A

No, b/c functions independently of GABA. LOW margin of safety

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26
Q

Coma, espiratory depression and hypotension are overdose sx of what medication?

A

Barbiturates

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27
Q

What is the tx for barbiturate overdose?

A

Supportive care, diuresis, alkalization of the urine

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28
Q

What drug class is Thiopental?

A

Barbiturates

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29
Q

What is the duration of action for Thiopental?

A

Short acting

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30
Q

What is Thiopental used for?

A

Induction of anesthesis

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31
Q

What drug class is Phenobarbital?

A

Barbiturates

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32
Q

What is the duration of action for Phenobarbital?

A

Long acting

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33
Q

What is Phenobarbital used for?

A

Used as anticonvulsant to tx partial and generalized tonic-clonic seizures

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34
Q

What is the MOA for benzodiazepines?

A

Bind to GABAA receptor, ↑ affinity of receptor to GABA prolonging its actions (effect dependent on GABA)

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35
Q

Do Benzodiazepines have a ceiling effect?

A

Yes! (limited GABA pool = effect plateaus once all GABA is used up despite an ↑ dose)

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36
Q

How are benzodiazepines metabolized?

A

CYP3A4 in liver

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37
Q

When are IV benzodiazepines used?

A

Emergencies, pre-anesthesia

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38
Q

What are the SEs for benzodiazepines? (3)

A

CNS depression (toxic doses), paradoxical excitement (dis-inhibition of suppressed behavior), sleep-related behaviors (sleep driving, eating, walking, etc)

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39
Q

When are benzodiazepines C/i? (4)

A

pregnancy, sleep apnea, elederly (can’t metabolize well), w/ alcohol use (supre-additive effects),

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40
Q

Tolerance to benzodiazepines is common. What effect does this have on dose and abuse potential?

A

Doses are not typically increased. High abuse potential

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41
Q

What are the effects of abrupt cessation/withdrawal of benzodizepines? (7)

A

Rebound ↑ anxiety and insomnia, muscle weakness, tremor, hyperalgesia, vomiting, weight loss, convulsions

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42
Q

What is the recommendation for stopping chronic benzodiazepine use?

A

Taper very slowly

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43
Q

What are the sx of a benzodiazepine OD?

A

Long deep sleep (24-48 hrs). Overall drug is relatively safe.

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44
Q

Possible fatality from a benzodizepine OD can occur in what populations?

A

People w/ respiratory difficulties, children, combine w/ alcohol

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45
Q

When prescribing a benzodiazepine. What is the general recommendation for dose and duration?

A

Lowest effect dose for shortest possible duration (to limit SE)

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46
Q

What is a general SE of drugs used to tx insomnia?

A

Minor depression of REM sleep → “hangover” effect

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47
Q

Which benzodiazepines have a long duration of action? (4)

A

Diazepam, Flurazepam, Chlordiazepoxide, Clonazepam

48
Q

Anti-anxiety/ sedative drugs with a long duration of action result in what?

A

Hangover effect

49
Q

Which anti-anxiety/ sedative drugs have an intermediate duration of action? (3)

A

Alprazolam, Oxazepam/Lorazepam, Temazepam

50
Q

What is the duration of action for Midazolam?

A

Short (No hangover effect)

51
Q

What are the 2 DOCs for status epilepticus?

A

Diazepam and Lorazepam (given IV or rectally)

52
Q

What is Diazepam used to tx? (3)

A

DOC for status epilepticus, acute muscle spasm/ pain as a result of injury, tapered withdrawal from alcohol and barbiturates

53
Q

What is flurazepam used to tx?

A

Insomnia (hypnotic)

54
Q

What is Chlordiazepoxide used to tx?

A

Tapered withdrawal from alcohol and barbituates

55
Q

What is Clonazepam used to tx? (3)

A

Absence seizures, myoclonic seizures, infantiles spams (West syndrome)

56
Q

What is Oxazepam/lorazepam used to tx? (2)

A

Status epilepticus, tapered withdrawal from alcohol and barbiturates

57
Q

What is Temazepam used to tx?

A

Insomnia (hypnotic)

58
Q

What is Midazolam used to for?

A

Preparation for anesthesia for short surgical procedures

59
Q

How is Midazolam administered?

60
Q

What is a SE of Midazolam?

A

Can cause anterograde amnesia

61
Q

What drug class is Diazpam?

A

Benzodiazepines

62
Q

What drug is Flurazepam?

A

Benzodiazepines

63
Q

What drug class is Chlordiazepoxide?

A

Benzodiazepines

64
Q

What drug class is Clonazepam?

A

Benzodiazepines

65
Q

What drug class is Alprazolam?

A

Benzodiazepines

66
Q

What drug class is Oxazepam/Lorazepam?

A

Benzodiazepines

67
Q

What drug class is Temazepam?

A

Benzodiazepines

68
Q

What drug class is Midazolam?

A

Benzodiazepines

69
Q

What is the MOA for Flumazenil?

A

Benzodiazepine antagonist- competes w/ BZ’s for GABA receptor and reverses BZ effects

70
Q

What is the use of Flumazenil?

A

Reverses respiratory depression caused by Midazolam, hypersomnia conditions

71
Q

What is the duration of action of Flumazenil? What does this mean for it’s hangover effect?

A

Short duration of action. No hangover effect

72
Q

What are the SE of flumazenil?

A

Triggers withdrawal and seizures in patients who are physically dependent on BZs

73
Q

When is Flumazenil C/i?

A

HX of seizures

74
Q

What are the “z” drugs?

A

Zolpidem, Zaleplon, Eszopiclone

75
Q

What is the MOA for the “Z” drugs?

A

Bind to BZ1 subtype of GABA receptor → increase GABA-mediated inhibition

76
Q

When are “Z” drugs used?

A

Used for insomnia (strong/ rapid sedative effects)

77
Q

Do the “Z” drugs have anxiolytic, anticonvulsant, or muscle relaxant properties?

78
Q

What is the duration of action for the Eszopiclone?

A

Long duration of action

79
Q

What is the duration of action for Zaleplon and Zolpidem? What does this mean for it’s hangover effect?

A

Short duration of action, no hangover effect

80
Q

Where are the “Z” drugs metabolized?

A

Liver by CYP3A4

81
Q

Where are the “Z” drugs excreted?

82
Q

If pt w/ severe liver disease, what effect does this have on the half life of the “z” drugs?

A

Prolongs half life

83
Q

Which of the “Z” drugs is uded for long term tx?

A

Eszopiclone

84
Q

The “Z” drugs have a very high margin of safety. What are the SEs?

A

GI, CNS depression, sleep-related behaviors

85
Q

If the “Z” drugs are rapdily discontinued/withdrawn what are the SEs?

A

Rebound insomnia, withdrawal sxs

86
Q

In what population are the “Z” drugs C/I?

A

Elderly (can cause confusion, memory loss, psychosis)

87
Q

What is the MOA for Suvorexant?

A

Antagonist at orexin receptors (involved in regulating sleep-wake cycle and promote wakefulness)

88
Q

What is Sovorexant metabolized by?

89
Q

What are the SE to Suvorexant? (2)

A

HA, abn dreams

90
Q

When is Suvorexant C/I? (2)

A

Depression, narcolepsy

91
Q

What is the MOA for Ramelteon?

A

Melatonin analogue, resets sleep-wake cycle, promotes sleepiness w/ no GABA effect

92
Q

Where is Ramelteon metabolized?

A

Metabolized in liver by CYP450s

93
Q

Ramelteon is absored orally. What does this mean for its first pass metabolism?

A

Extensive first pass metabolism

94
Q

What are the SEs for Ramelteon?

A

Drowsiness, dizziness, nausea (high doses)

95
Q

Ramelteon can have toxic additive sedation effects if combined with what?

A

Alcohol, other sedative hypnotics

96
Q

What is the use for 1st gen antihistamines?

97
Q

What is a benefit to using 1st gen antihistamines for sedation?

A

No abuse potential

98
Q

What drug class is Hydroxyzine and Benadryl?

A

Antihistamine

99
Q

What are the uses of Hydroxyzine as a sedative-hypnotic? (3)

A

Anti-anxiety, prevents nausea/ emesis caused by motion sickness, anti-Parkinson effects (used to treat EPS)

100
Q

When is Benadryl used as a sedative-hypnotic?

A

Useful for occasional insomnia, especially if hx of addiction to benzo or alcohol

101
Q

What is the MOA for Chloral Hydrate?

A

Acts similarly to barbiturates on GABAA receptor

102
Q

When and why is Chloral hydrate used?

A

CHEAP, sedation in pediatric dental procedures, nursing homes, chronic care institutions

103
Q

Chloral Hydrate has a LOW margin of safety. What are potential SEs?

A

High doses induce respiratory and vasomotor depression, GI sx, allergic response, +/- cardiac arrhythmias

104
Q

Chronic use of Choral hydrate can result in what? (2)

A

Liver damage and fatal intoxication

105
Q

When is chloral hydrate C/I?

A

As a sedative-hypnotic

106
Q

What is the MOA for Buspirone?

A

Partial agonist at postsynaptic serotonin (5-HT1A) receptor, full agonist at presynaptic serotonin receptor)

107
Q

What is the benefit to using buspirone for the tx of anxiety?

A

Relieves anxiety w/o producing sedations (can be taken during the day)

108
Q

When is Buspirone used?

A

To tx mild generalized anxiety and anxiety and depression, ADHD and autistic pts w/ anxiety, premenstrual syndrome

109
Q

Why is Buspirone used in pts w/ hx of alcohol or benzodiazepine abuse?

A

Very low addiction potential

no muscle relaxant or anticonvulsant properties, does not potentiate CNS depression w/ alcohol or BZs

110
Q

How long does Buspirone take to become effective?

111
Q

Where is Buspirone metabolized?

A

Liver by CYP3A4

112
Q

What are the SE of Buspirone? (5)

A

Light-headedness, restlessness, HA, drowsiness, N/V

113
Q

What drugs are metabolised by CYP450?

114
Q

What drugs are CYP450 inducers

A

Barbituates (Thiopental, Phenobarbital)

115
Q

What medications are classified as “other sedative-hypnotics”? (10)

A

Flumazenil, Zolipdem, Zaleplon, Eszopiclone, Suvorexant, Ramelteon, Hydroxyzine, Benadryl, Chloral Hydrate, Buspirone

4. Pharm III (16 decks)

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