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Pharm III Unit I > 3 Sedative-Hypnotics and Anxiolytics > Flashcards

3 Sedative-Hypnotics and Anxiolytics Flashcards

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1
Q

Symptoms of anxiety

A

Palpitations, tremor, perspiration, GI effects, dizziness, and headache

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2
Q

_______ anxiety is an appropriate reaction to danger (fear, arousal)

A

Adaptive

Leads to increased sympathetic activity

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3
Q

______ anxiety is the result of chronic, psychological stress

A

Maladaptive

Leads to organ dysfunction (GI, cardiac), physical symptoms

Anxiety that becomes chronic and interferes with normal functioning should be treated

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4
Q

The “ideal” anti-anxiety drug should…

A

Relieve anxiety without sedation or drowsiness, no physical or psychological dependence

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5
Q

What are the different classifications of anxiety disorders?

A

Acute Anxiety

Generalized Anxiety Disorder

Panic Disorder

Phobias

Obsessive Compulsive

Post Traumatic Stress Disorder

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6
Q

Classify the anxiety disorder:

Short term, self limiting

A

Acute anxiety

Treat with benzos

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7
Q

Classify the anxiety disorder:

Chronic anxiety

A

Generalized Anxiety Disorders

Treat with benzos or buspirone

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8
Q

Classify the anxiety disorder:

Episodic, severe attacks of anxiety

A

Panic disorder

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9
Q

Classify the anxiety disorder:

Fear of specific things or circumstances

A

Phobias

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10
Q

Classify the anxiety disorder:

Recurrent, obsessive behaviors

A

Obsessive Compulsive

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11
Q

Classify the anxiety disorder:

Anxiety after a stressful event

A

Post Traumatic Stress Disorder

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12
Q

What are the different classifications of sleep disorders?

A

Insomnia - short term tx with sedative hypnotic

Hypersonic, Narcolepsy - tx with stimulants

Kleine-Levin Syndrome (“Sleeping beauty”)

Enuresis (bed wetting) - tx with TCA

Sleep apnea - tx with CPAP

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13
Q

DOC for enuresis

A

Tricyclic antidepressants

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14
Q

Difficulty falling asleep, early or frequent awakening, and unrefreshing sleep

A

Insomnia

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15
Q

__________ insomnia occurs with situational stress (bereavement, conflict at work or in the family, hospitalization)

A

Transient or Short-term

Sedative-hypnotics are most useful

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16
Q

_______ insomnia may be related to underlying psychiatric disease or chronic alcohol/drug use

A

Long-term

Best treated with behavioral therapy and lifestyle changes

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17
Q

Describe the “ideal” sedative-hypnotic

A

Causes one to fall asleep quickly, stay asleep as long as wanted, and wears off early in the morning with no hangover effect

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18
Q

How does GABA work to relieve anxiety and promote sedation?

A

Gamma-amino-butyric-acid

It’s the primary CNS inhibitory neurotransmitter - acts as a depressant and is widely distributed in the CNS

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19
Q

GABA receptors are ______ channels, and activation causes the membrane to _________

A

Cl-

Hyperpolarize

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20
Q

What are the major subtypes of GABA?

A

GABA-a

GABA-b

GABA-c

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21
Q

Activation of ________ receptor causes depression of electrical activity which decreases anxiety and promotes sleep

A

GABA-a

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22
Q

Hydroxyzine (Vistaril) is an antihistamine but is also used as …

A

Anti-anxiety medication

It’s a 1st gen antihistamine so SEDATION is big

No abuse potential so good for use in recovering addicts

Inhibits smooth muscle response and vasodilation

CNS depression or stimulation

Prevents nausea and emesis caused by motion sickness

Has some anti-Parkinson effects

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23
Q

Barbiturates bind to ______ and stimulate _______ to produce _______.

A

GABA receptor

Cl- influx

Inhibition INDEPENDENT of GABA

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24
Q

Barbiturates cause marked _______ and _______

A

CNS depression (hypnosis) and euphoria

Considered a drug of abuse (schedule II or III controlled substances)

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25
Uses for barbiturates
Thiopental (Pentothal) - short acting barbiturate used for induction of anesthesia Long-acting barbiturates such as phenobarbital (Luminal) are used as anticonvulsants
26
If you see phenobarbital on the exam, think...
DRUG INTERACTIONS They induce CYP450s with chronic use, so alters metabolism of alcohol, many hormones, and other barbiturates
27
Side effects of barbiturates
CNS depression**** - drowsiness, distortion of mood, impaired judgement and motor skills, can last 10-22 hours Paradoxical excitement (esp in elderly patients)**** Vertigo, nausea, vomiting, diarrhea, and allergic reactions May depress the vasomotor and respiratory centers of the medulla Severe physiological and psychological dependence****
28
Contraindications for the use of barbiturates
Porphyria - b/c they enhance porphyrin synthesis Pulmonary insufficiency - may cause resp depression Supra-additive effects when combined with other CNS depressants (ie alcohol, benzos)
29
What does barbiturate withdrawal look like?
Can be severe Restlessness, anxiety, weakness, orthostatic hypotension, hyperactive reflexes and seizures
30
What makes barbiturates so dangerous?
Low margin of safety (no “ceiling effect”) b/c not dependent on GABA Benzos are safer b/c their dose/effect curve plateaus When combined with alcohol, barbiturates can be Supra-additive
31
Overdose of barbiturates is marked by...
Coma, respiratory depression, and decreased BP Treatment is supportive Stimulants increase mortality rate
32
What is the best way to manage a barbiturate overdose?
Supportive care Cleared with diuresis and alkalization of the urine (ion trapping)
33
The most commonly used group of anxiolytics and sedative-hypnotics
Benzodiazepines Overprescribed in the 60s-80s (whomp whomp)
34
Main drawbacks of benzos
CNS depression - decrease in anxiety often accompanied by drowsiness Hypnosis can occur with high doses The elderly do not metabolize benzos as quickly so avoid as much as possible
35
Benzos are metabolized by ________ and converted to _________
CYP3A4 in the liver Active metabolites
36
Duration of action for different benzos depends upon...
The metabolites Active metabolites = long duration of action Short-acting metabolites = intermediate duration Inactive metabolites = intermediate duration
37
Benzos with long duration of action
(Long duration b/c active metabolites Diazepam is converted to desmthyldiazepam, then to oxazepam, for a total 1/2 life of ~75 hours Flurazepam also converted to long-acting metabolites (t1/2 = 74 hours)
38
Benzos with intermediate duration of action
Alprazolam Oxazepam/lorazepam
39
Benzo with very short duration of action
Midazolam
40
MOA for benzos
Bind to specific sites on the GABA-a receptor for an effect that is DEPENDENT on GABA Increases affinity of the receptor to GABA, prolonging its action B/c it’s dependent on GABA —> CEILING EFFECT (vs barbs that are GABA independent)
41
DOC for benzos is based largely on...
Duration of action
42
Anxiety disorders in which benzos are NOT used
Obsessive-compulsive disorder (treat with SSRI) Agoraphobia and panic disorders (treat with SSRI) PTSD (treat with antidepressants) Anxiety in children and adolescents (treat with antidepressants)
43
Benzos used in insomnia
Flurazepam and temazepam Minor depression of REM sleep so may cause hangover effect These two are shorter acting drugs so helpful for the person who has difficulty falling asleep but not staying asleep
44
Benzos used in epilepsy and seizures
Diazepam and lorazepam for Status Epilepticus (ongoing seizures >3 min)
45
Benzo used for sedation, amnesia, and anesthesia
Midazolam - used in prep for anesthesia for short surgical procedures Anterograde amnesia possible
46
Benzo used for muscle relaxation
Diazepam sometimes used for acute muscle spasm and pain as a result of injury
47
Use of benzos during withdrawal from alcohol/barbiturates
Long-term use of alcohol/barbiturates can produce physical dependence and result in withdrawal that is very severe and can be life threatening Benzos (chlordiazepoxide, diazepam, and lorazepam) are used to provide a more tapered withdrawal
48
Side effects of benzos
CNS depression: dizziness, drowsiness, excessive sedation, impaired motor coordination, confusion, memory loss Effects are most common in the first few weeks - will decrease as tolerance develops Less common are blurred vision and hallucinations Paradoxical excitement**** - due to disinhibition of suppressed behavior (more likely in the elderly***) Supra-additive CNS depression when combined with alcohol Sleep-related behaviors (sleep driving, eating, walking)
49
Contraindications for the use of benzos
Should not be given during pregnancy unless absolutely necessary (Cat D) Sleep apnea - may decrease tone of upper airway) Elderly
50
Abrupt discontinuation of benzos can cause...
Rebound increases in insomnia and anxiety Muscle weakness, tremor, hyperalgesia, N/V, weight loss, and convulsions Benzos should be tapered very slowly following chronic use
51
Overdose on benzos generally results in...
A long deep sleep (24-48 hours) Although Schedule IV, do have some abuse potential Fatalities may occur in people with respiratory difficulties in children, and when combined with alcohol
52
Benzodiazepine antagonist that competes with benzos for GABA receptor to reverse their effects
Flumazenil (Mazicon) Reverses the effect of midazolam (Versed), which sometimes causes resp depression Also reverses the effects of other drugs (“z-drugs”) that act on the benzo binding site Evidence showing effective treatment for hypersomnia conditions
53
Major adverse effect of Flumazenil
Triggers withdrawal and seizures in patients who are physically dependent on benzos DO NOT USE in patients addicted to benzos or with Hx of SEIZURES
54
What are the “z-drugs”?
Zolpidem (Ambien), Zaleplon (Sonata), Eszopiclone (Lunesta) Bind to the BZ1 subtype of the GABA receptor to increase GABA-mediated inhibition Very strong and rapid sedative effects NO anxiolytic, anticonvulsant, or muscle relaxant properties
55
Pharmacokinetics of the Z drugs
Well-absorbed orally, peak levels at 30-60 min Metabolized in liver (CYP3A4), excreted by kidney Short duration of action, so morning drowsiness unlikely (exception = eszopiclone - used for long-term treatment) Half-life may be prolonged in severe hepatic disease
56
Side effects of z drugs
VERY HIGH margin of safety GI - diarrhea and nausea CNS - drowsiness and dizziness Sleep-related behaviors Amnesia occurs with higher than recommended doses Confusion, memory loss, and psychosis in the elderly May increase the depressant effects of other sedative drugs REBOUND INSOMNIA may occur after rapid d/c WITHDRAWAL Sx with abrupt cessation
57
MOA for Suvorexant (Belsomra)
Antagonist at orexin receptors Orexins are involved in regulating the sleep-wake cycle and promote wakefulness Metabolized by CYP3A4 so drug interactions likely with inhibitors such as cimetidine
58
Side effects of suvorexant (belsomra)
HA and abnormal dreams Can cause sleep paralysis***, hallucinations, and muscle weakness while falling asleep or waking up Depression may worsen in patients with underlying depression Effects will be magnified if combined with other CNS depressants
59
Suvorexant (Belsomra) is contraindicated in ...
Patients with narcolepsy
60
MOA for Ramelteon (Rozerem)
Melatonin analogue - resets sleep-wake cycle Promotes sleepiness w/o GABA effect
61
Side effects of Ramelteon (Rozerem)
Additive sedation with alcohol and other sedative hypnotics Drowsiness, dizziness and nausea
62
Why are antihistamines in this lecture?
Not classical sedatives, but 1st gen antihistamines have sedative properties They are the active ingredient in the majority of OTC preparations for insomnia Useful for occasional insomnia and esp in someone who has been addicted to benzos/alcohol
63
MOA for Chloral Hydrate (Noctec)
Converted to trichloroethanol, which causes sedation Acts similarly to barbiturates on GABA-a LOW MARGIN OF SAFETY - high doses induce resp and vasomotor depression
64
Down sides of Chloral Hydrate (Noctec)
Causes gastric irritation, N/V, allergic responses, may produce cardiac arrhythmias Long-term use may cause liver damage and fatal intoxication
65
Why does anyone use Chloral hydrate (Noctec)
CHEAP • In children for sedation during pediatric dental procedures • In nursing homes and chronic care institutions Use as a sedative-hypnotic not recommended
66
MOA for Buspirone (BuSpar)
Relieves anxiety without producing sedation Partial agonist at the POST-SYNAPTIC 5-HT receptor —> inhibition of cell signaling FULL agonist for PRE-SYNAPTIC 5-HT receptors —> decreased release of 5-HT Good option for anxiety in recovering addicts b/c it works outside of GABA system Anxiolytic effect takes about 2 weeks to develop No muscle relaxant or anticonvulsant properties
67
Uses for Busprione (BuSpar)
Generalized anxiety and anxiety with depression ADHD and autistic patients with anxiety Premenstrual syndrome Very low addiction potential - GREAT CHOICE for recovering alcoholics/addicts with anxiety Not good for severe anxiety and/or panic disorder

Pharm III Unit I (9 decks)

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