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

3 Sedative-Hypnotics and Anxiolytics Flashcards

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
Q

Uses for barbiturates

A

Thiopental (Pentothal) - short acting barbiturate used for induction of anesthesia

Long-acting barbiturates such as phenobarbital (Luminal) are used as anticonvulsants

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26
Q

If you see phenobarbital on the exam, think…

A

DRUG INTERACTIONS

They induce CYP450s with chronic use, so alters metabolism of alcohol, many hormones, and other barbiturates

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27
Q

Side effects of barbiturates

A

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
Q

Contraindications for the use of barbiturates

A

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
Q

What does barbiturate withdrawal look like?

A

Can be severe

Restlessness, anxiety, weakness, orthostatic hypotension, hyperactive reflexes and seizures

30
Q

What makes barbiturates so dangerous?

A

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
Q

Overdose of barbiturates is marked by…

A

Coma, respiratory depression, and decreased BP

Treatment is supportive

Stimulants increase mortality rate

32
Q

What is the best way to manage a barbiturate overdose?

A

Supportive care

Cleared with diuresis and alkalization of the urine (ion trapping)

33
Q

The most commonly used group of anxiolytics and sedative-hypnotics

A

Benzodiazepines

Overprescribed in the 60s-80s (whomp whomp)

34
Q

Main drawbacks of benzos

A

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
Q

Benzos are metabolized by ________ and converted to _________

A

CYP3A4 in the liver

Active metabolites

36
Q

Duration of action for different benzos depends upon…

A

The metabolites

Active metabolites = long duration of action
Short-acting metabolites = intermediate duration
Inactive metabolites = intermediate duration

37
Q

Benzos with long duration of action

A

(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
Q

Benzos with intermediate duration of action

A

Alprazolam

Oxazepam/lorazepam

39
Q

Benzo with very short duration of action

A

Midazolam

40
Q

MOA for benzos

A

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
Q

DOC for benzos is based largely on…

A

Duration of action

42
Q

Anxiety disorders in which benzos are NOT used

A

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
Q

Benzos used in insomnia

A

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
Q

Benzos used in epilepsy and seizures

A

Diazepam and lorazepam for Status Epilepticus (ongoing seizures >3 min)

45
Q

Benzo used for sedation, amnesia, and anesthesia

A

Midazolam - used in prep for anesthesia for short surgical procedures

Anterograde amnesia possible

46
Q

Benzo used for muscle relaxation

A

Diazepam sometimes used for acute muscle spasm and pain as a result of injury

47
Q

Use of benzos during withdrawal from alcohol/barbiturates

A

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
Q

Side effects of benzos

A

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
Q

Contraindications for the use of benzos

A

Should not be given during pregnancy unless absolutely necessary (Cat D)

Sleep apnea - may decrease tone of upper airway)

Elderly

50
Q

Abrupt discontinuation of benzos can cause…

A

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
Q

Overdose on benzos generally results in…

A

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
Q

Benzodiazepine antagonist that competes with benzos for GABA receptor to reverse their effects

A

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
Q

Major adverse effect of Flumazenil

A

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
Q

What are the “z-drugs”?

A

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
Q

Pharmacokinetics of the Z drugs

A

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
Q

Side effects of z drugs

A

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
Q

MOA for Suvorexant (Belsomra)

A

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
Q

Side effects of suvorexant (belsomra)

A

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
Q

Suvorexant (Belsomra) is contraindicated in …

A

Patients with narcolepsy

60
Q

MOA for Ramelteon (Rozerem)

A

Melatonin analogue - resets sleep-wake cycle

Promotes sleepiness w/o GABA effect

61
Q

Side effects of Ramelteon (Rozerem)

A

Additive sedation with alcohol and other sedative hypnotics

Drowsiness, dizziness and nausea

62
Q

Why are antihistamines in this lecture?

A

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
Q

MOA for Chloral Hydrate (Noctec)

A

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
Q

Down sides of Chloral Hydrate (Noctec)

A

Causes gastric irritation, N/V, allergic responses, may produce cardiac arrhythmias

Long-term use may cause liver damage and fatal intoxication

65
Q

Why does anyone use Chloral hydrate (Noctec)

A

CHEAP
• In children for sedation during pediatric dental procedures
• In nursing homes and chronic care institutions

Use as a sedative-hypnotic not recommended

66
Q

MOA for Buspirone (BuSpar)

A

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
Q

Uses for Busprione (BuSpar)

A

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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