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Therapeutics III > Yang Sedatives and Hypnotics > Flashcards

Yang Sedatives and Hypnotics Flashcards

1
Q

Sedative definition

A

Calms anxiety, decreases excitement and activity, does not produce drowsiness, or impair performance

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2
Q

Anxiolytic definition

A

Antianxiety, relieves anxiety without sleep or sedation (not all anxiolytics are sedatives)

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3
Q

Hypnotic definition

A

Induces sleep, implies restful, refreshing sleep, not “hypnotized”, natural sleep (sleep-inducing)

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4
Q

Narcotic definition

A

Actually means “sleep-producing” now refers to opioids or illegal drugs

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5
Q

Stages of sleep

A

-Wakefulness
-Non-rapid eye movement (NREM) slow-wave sleep
-Rapid eye movement (REM) sleep

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6
Q

Stages of NREM sleep

A

-Stage 1: dozing
-Stage 2: unequivocal sleep
-Stage 3: voltage increase, frequency decrease
-Stage 4: delta waves

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7
Q

Factors that regulate sleep

A

-Age: decreases with age due to changes in activity of reticular formation
-Sleep history: rebound of REM sleep
-Drug ingestion: acute and withdrawal produce rebound effects
-Circadian rhythms: normal sleep cycle

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8
Q

Neurotransmitters that regulate sleep

A

-Catecholamines
-Serotonin
-Histamine
-Acetylcholine
-Adenosine
-GABA

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9
Q

Neuromodulators that regulate sleep

A

-Growth hormone
-Prolactin
-Cortisol
-Melatonin
-Endogenous peptides

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10
Q

Targets for sedative-hypnotics on the GABAa receptor/chloride ion channel complex

A

-Orthosteric site
-Allosteric site
-Channel pore

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11
Q

What binds to the orthosteric site on the GABAa receptor/chloride ion channel complex?

A

GABA

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12
Q

What binds to the allosteric sites on the GABAa receptor/chloride ion channel complex?

A

-Benzodiazepines
-Barbituates
-Ethanol
-Gluccocorticoid

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13
Q

What binds to the channel pore on the GABAa receptor/chloride ion channel complex?

A

Picrotoxin

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14
Q

Benzodiazepine mechanism of action

A

Facilitate GABA action, increase frequency, require intact GABA system

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15
Q

What do Z-Hypnotics target?

A

BZ1 receptors of alpha1

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16
Q

Benzodiazepine antagonists for overdose treatment

A

Flumazenil

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17
Q

Inverse benzodiazepine agonists

A

B carbolines

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18
Q

Z-hypnotics

A

-Zolpidem
-Zaleplon
-Eszopliclone

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19
Q

BZDs with slow elimination rates

A

All have active metabolites
-Chlordiazepoxide
-Diazepam (used for seizures, accumulation of metabolites)
-Flurazepam
-Clorazepate
-Quazepam
-Prazepam

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20
Q

BZDs with intermediate elimination rates

A

-Alprazolam
-Lorazepam
-Clonazepam (anticonvulsant)
-Oxazepam
-Temazepam

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21
Q

BZDs with rapid elimination rates

A

-Midazolam
-Triazolam

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22
Q

Characteristics of BZDs with slow elimination

A

-Active metabolites
-Accumulation
-Drowsiness and sedation
-Useful in patients who “wake up”

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23
Q

Characteristics of BZDs with intermediate to rapid elimination

A

-Preferable in patients with hepatic problems
-Preferable in elderly patients
-Drugs that alter liver enzymes
-Rapid tolerance
-Rebound insomnia

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24
Q

Benzodiazepine considerations

A

-Readily absorbed (can be delayed by food)
-Have active metabolites or are converted to active forms
-Increased lipid solubility will increase speed of delivery to brain
-Redistribution to highly perfused tissue may decrease duration of action
-Cross placental barrier and are detected in breast milk
-Extensive protein binding, but not clinically significant

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25
BZD pharmacologic properties
-Anxiolytic -Decrease in REM -Decrease stage 3 and 4 -Anticonvulsant activity -Muscle relaxant -Cardiovascular and respiratory depression -Anterograde amnesia -Unable to recall events that occurred
26
BZD side effects
-Sedation (confusion, ataxia, daytime sedation) -Weakness -Headache -Vertigo -Nausea -Paradoxical effects
27
BZD precaution and interactions
-Other sedatives -Alcohol -Pregnancy/breast-feeding
28
BZD abuse potential
-Low vs barbiturates -Small kick
29
Flumazenil therapeutic use
Treat BZD overdose
30
Flumazenil dosing
-0.2 mg IV over 30 seconds -If desired consciousness is not obtained, increase to 0.3 mg IV over 30 seconds
31
Flumazenil max cumulative dose
3 mg
32
Flumazenil side effects
-Induce convulsions -Panic attacks -Agitation -Confusion -Nausea an vomiting -Headache
33
Z-hypnotic site of binding
Act at BZD binding site
34
When to use zolpidem
-Short-term treatment of insomnia -With difficulty of sleep-onset -Ambien CR for sleep maintenance
35
Zaleplon clinical pearls
-Short-term treatment of insomnia (7-10 days) -Rapid acting, rapidly eliminated -Little tolerance or dependance
36
Eszopiclone clinical pearls
-Active enantiomer of zopiclone (50 times greater affinity) -Treatment of insomnia (approved for long-term use)
37
How are z-hypnotics metabolized?
CYP3A4 to some extent
38
Side effects of z-hypnotics
-Daytime drowsiness -Dizziness -Ataxia -Nausea -Vomiting Sleep-driving -Sleep-cooking -Sleep-eating -Sleep-sex -Less negative side effects on sleep-patterns vs BZDs
39
Illicit sedative/hypnotics that target the benzodiazepine binding site
-Flunitrazepam -Clonazepam -Zolpidem
40
Why is flunitrazepam considered illicit?
-Not available in the US -Roofies -DEA recommends changing it to a control schedule 1 -Anterograde amnesia (dangerous aid for sexual assault)
41
Why is zolpidem considered illicit?
-A-minus and zombie pills -Dangerous aid for sexual assault -Teen party drug
42
Long acting barbiturate use
Anticonvulsant
43
What are the long-acting barbiturates?
Phenobarbital
44
Short to intermediate acting barbiturate use
Sedative-hypnotics
45
What are the short to intermediate acting barbiturates?
Pentobarbital
46
Ultra short acting barbiturate use
IV anesthetics
47
Barbiturate sleep physiology
-Comparable to BZD -Decrease REM -Slow deep sleep
48
Barbiturate side effects
-Idiosyncratic excitement and pain -Cardiovascular depression at high doses -Respiratory depression leading to death -Enzyme interactions -Dependence -Tolerance -Abuse -Withdrawal -Overdose -Hangover -Accumulation
49
Barbiturate duration of action
Inversely proportional to lipid solubility
50
Barbiturate mechanism of action
-Bind to all GABAa alpha1-5 -Increase the duration of channel opening -Direct effects on GABAa channel (high doses) -Higher risk
51
Benzodiazepine mechanism of action
-Bind to all GABAa alpha1-5 -Increase frequency of GABAa channel opening -Medium risk
52
Z-hypnotic mechanism of action
-Bind to GABAa BZ1 receptors of alpha1 -Increase frequency of GABAa channel opening -Lower risk
53
What kind of coupled receptor is GABAb?
Gi/o-coupled receptor
54
Location of the GABAb receptors?
-Brain -Limbic system
55
What does inhibition of GABAb do?
-Presynaptic - decrease Ca2+ conductance -Postsynaptic - increase K+ conductance
56
GABAb agonists
-Baclofen -Gamma-hydroxybutyric acid (GHB)
57
GABAb antagonists
-Phaclofen -Saclofen -2-hydroxysaclofen
58
Xyrem (sodium oxybate, GHB) clinical pearls
-Liquid form is only used for medical use other forms for illicit use -Available only to prescribers enrolled in the Xyrem Patient Success Program
59
Actions of Xyrem
-Decreases excessive daytime sleepiness and increases daytime wakefulness with concomitant stimulant use -Decrease cataplexy
60
Xyrem receptor targets
GABAb, GABAa, and GHB rceptors
61
Concerns regarding Xyrem
-Questionable mechanism of action -Combined with other agents -Red tape -Abuse and misuse
62
GHB street names
-Liquid ecstasy -Liquid X -Juice -Grievous bodily harm -Scoops -Georgia home boy
63
GHB effects
-Dose-dependent CNS depression -Patients often awaken spontaneously
64
Acute effects of GHB
-Loss of consciousness -Amnesia -Nausea and vomiting -Headache -Seizures -Death
65
GHB concerns
-No antagonist -Use with other sedative-hypnotics - including alcohol -Amnesia -Date rape
66
What are the melatonin agonists?
-Ramelteon -Tasimelteon
67
Ramelteon mechanism of action
-High affinity for MT1 and MT2 melatonin receptors -Receptors located in the suprachiasmatic nucleus (SCN)
68
Ramelteon metabolism
CYP1A2 substrate
69
What does ramelteon treat?
Insomnia characterized by difficulty with sleep onset
70
Ramelteon clinical pearls
-Non-controlled substance sleep aid -No abuse, withdrawal, or dependency -Negligible risk for next-day "hangover" effects
71
Tasimelteon mechanism of action
High affinity for MT1 and MT2 melatonin receptors
72
What does tasimelteon treat?
Non-24-hour sleep wake disorder in blind individuals
73
Tasimelteon clinical pearls
Orphan product registration
74
Orexin receptor antagonists
Suvorexant
75
Suvorexant mechanism of action
-High affinity antagonist for OX1 and OX2 orexin receptors -Receptors located in the hypothalamus -Decrease arousal and attention via receptors in locus coeruleus and the raphe -Reduce rewarding stimuli (DA release) via receptors that modulate the mesolimbic projections between the VTA and the nucleus accumbens
76
What does suvorexant treat?
Insomnia
77
Suvorexant clinical pearls
-Morning impairment likely/possible (use the lowest dose possible) -Scheduled CIV
78
What information needs to be included on the labeling of all sleep disorder drug products?
-Sleep-driving -Cooking and eating food while sleeping -Making phone calls while sleeping
79
Miscellaneous sedative drugs
-Trazodone -Antihistamines
80
Herbal/natural sedative hypnotics
-Tryptophan -Melatonin -Lemon balm -Valerian -Chamomile -Kava kava
81
Causes of sedative-hypnotic overdose
-Suicide and suicide gesture -Drug abuse
82
Signs and symptoms of sedative-hypnotic overdose
-Depressed respiration -Blood pressure -Reflexes -Hypothermia
83
Treatment of sedative-hypnotic overdose
-Supportive treatment -Maintain respiration -Maintain cardiovascular function -Flumazenil for benzodiazepines or z-hypnotics
84
What is anxiety?
Fear or apprehension of something dreadful
85
When to treat anxiety
-When it interferes with normal life -When it interferes with part of another disease
86
Types of anxiety
-Generalized anxiety disorder -Panic disorder -Social anxiety disorder or social phobia -Obsessive-compulsive disorder -Post-traumatic stress disorder -Anxiety associated with other medical issues (autism, depression, etc.)
87
Drugs that can induce anxiety
-Cocaine -Beta agonists -Psychostimulants -Corticosteroids
88
Diseases that can induce anxiety
-CHF -COPD -Diagnosis of terminal diseases
89
What can cause anxiety from withdrawal?
-Antidepressants -Anxiolytics -Drugs of abuse -Cell phone/social media
90
How does norepinephrine effect anxiety?
-Over-active locus coeruleus-release NE -Stimulate autonomic nervous system -Dysregulated in GAD and other types of anxiety -Projects to the amygdala (fear center)
91
How does the GABAergic system effect anxiety?
-Normally counteracts/balances stimulatory effects of excess NE -Hypothesis proposes reduced GABAergic signaling. Agents that increase GABA signaling are anxiolytic -GABA/glutamate (inhibitory/excitatory) (glutamate is converted to GABA by glutamic acid decarboxylase - GAD in the CNS) -Involved in GAD and panic disorder
92
How does serotonin effect anxiety?
-May reflect tone at multiple receptors/SSRIs have efficacy -Partial agonist of 5HT1A receptors effective -May involve amygdala and balance with NE -GAD, panic, OCD, social anxiety
93
How does corticotropin-releasing factor and the HPA axis effect anxiety?
-Hyperregulation -Suppression after treatment in PTSD
94
Drugs used to treat anxiety
-BZDs (quick acting, effective) -Antidepressants (SSRIs, SNRIs, TCAs, takes weeks) -New breakthrough: ketamine (nasal spray esketamine, very quick acting, game changer) -Buspirone (Buspar) -Beta blockers
95
Buspirone mechanism of action
-Partial agonist on brain 5HT1A receptors -Moderate affinity for brain dopamine D2 receptors
96
Buspirone clinical pearls
-Low abuse potential, no or little withdrawal -Longer onset of action compared to BZD (adaptive response)
97
Uses of buspirone
-GAD, social anxiety, comorbid depression -Adjunct use with OCD, PTSD -Not good for panic disorders (BZD is much faster)
98
Which beta blockers are used in anxiety?
Propranolol
99
Uses of propranolol
-Social anxiety -Nightmares associated with PTSD
100
Propranolol clinical pearls
-CNS penetration - lipophilic -Decreased peripheral symptoms of anxiety -Monitor cardiovascular effects
101
Propranolol side effects
-Hallucinations -Vivid dreams -Lethargy -Impotence
102
Miscellaneous anxiolytics
-Hydroxyzine (H1 antagonist) -Clonidine (alpha2 agonist)
103
Investigational anxiolytics
-Ondansetron (5HT3 antagonist) -Ketanserin (5HT2 antagonist) -Tiagabine (GABA uptake blocker) -Partial benzodiazepine receptor agonists -NDMA receptor modulators: d-cycloserine, memantine (glutamatergic agent) -mGluR5 antagonist: fenobam (glutamatergic agent) -mGluR2/3 agonist: LY354740 (glutamatergic agent)

Therapeutics III (42 decks)

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