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Pharmacology III > Sedative Hypnotics & Anxiolytics > Flashcards

Sedative Hypnotics & Anxiolytics Flashcards

(49 cards)

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1
Q

Primary use of Sedative-Hypnotic/Anxiolytic Drugs

A

Encourage calmness (anxiolytic effect) and to produce sleep (sedative-hypnotic)

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2
Q

GABA - MoA

A 
 CNS depressants
 Gamma-amino-butyric-acid (GABA)
 Major inhibitory neurotransmitter
 Widely distributed in CNS
 Relieves anxiety, promotes sedation
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3
Q

GABA Receptors

A

 Cl-channels
 Activation allows Cl-to enter cell hyperpolarizing the
membrane
 Major subtypes - GABAa, GABAb and GABAc
 Activation GABAa receptor causes depression of
electrical activity, which decreases anxiety and
promotes sleep
 Some drugs work independently of GABA (ramelteon,
buspirone)

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4
Q

Hydroxyzine (Vistaril)

A
  • Antihistamine used as anti-anxiety medication
     Sedation! (1st generation)
     No abuse potential: good for use in recovering
    addicts
     Inhibit smooth muscle response
     Inhibit vasodilation
     CNS depression OR stimulation
     Prevents nausea and emesis caused by motion
    sickness (anticholinergic effects)
     Anti-Parkinson effects - used to treat EPS
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5
Q

Barbiturates - MoA

A

 Binds to GABA receptor and stimulates Cl-influx
 Produces inhibition independent of GABA
 Marked CNS depressant effect: hypnosis
 Cause euphoria; drugs of abuse
 Schedule II or III controlled drugs

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6
Q

Barbiturates - Uses

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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7
Q

Barbiturates - Pharmacokinetics

A

 Well absorbed orally; Crosses blood brain barrier
 Extensively metabolized by the liver
 Induce CYP450s with chronic use; alters metabolism
of other drugs, especially alcohol, many hormones,
and other barbiturates

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8
Q

Barbiturates - Side Effects

A

 CNS depression:drowsiness, distortion of mood,
impaired judgment and motor skills; can last 10-22
hours.
 Paradoxical excitement
 Vertigo, nausea, vomiting, diarrhea, and allergic
reactions
 May depress the vasomotor and respiratory centers in
the medulla
 Severe physiological and psychological dependence

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9
Q

Barbiturates - Contraindications

A

Enhance porphyrin synthesis - contraindicated in
porphyria (abnormal hemesynthesis).
 Pulmonary insufficiency - may cause respiratory
depression
 Supra-additive effects - When combined with other
CNS depressants (alcohol) the effects are more than
what is expected

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10
Q

Barbiturates - Withdrawal

A

 Withdrawal can be severe: restlessness, anxiety,
weakness, orthostatic hypotension, hyperactive
reflexes and seizures.

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11
Q

Barbiturates - Overdose & Toxicity

A

 Low margin of safety; No “ceiling effect”
 Combined with alcohol effects can be supra-additive
 Overdose is marked by coma, respiratory depression,
and decreased blood pressure
 Cleared with diuresis and alkalization of the urine

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12
Q

Benzodiazepines - MoA

A

 Benzodiazepines bind to specific sites on the GABAa
receptor
 Effect is dependent on GABA
 Increases affinity of the receptor to GABA prolonging
its action
 Ceiling effect

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13
Q

Benzodiazepine - Metabolism

A

 Metabolized by CYP3A4 in the liver; converted to active
metabolites
 Long duration of action
• Diazepam (t½ = 43 hrs), the half life of diazepam (and
metabolites) is ~75 hrs
• Flurazepam (t½= 74 hrs); converted to long-acting
metabolites
 Intermediate duration of action
• Alprazolam (t½< 6 hr); converted to short-acting
metabolites
• Oxazepam/lorazepam (t½6-24 hr); converted to inactive metabolites
 Very short duration of action - Midazolam (t½< 2 hr)

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14
Q

Uses of Benzodiazepines - Anxiety

A

 Use lowest effective dose for the shortest possible
duration, to provide maximum benefit with the fewest
side effects.
 DOC largely based on duration of action

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15
Q

Uses of Benzodiazepines - Insomnia

A

 Flurazepam and Temazepam are commonly used as
hypnotics.
 Minor depression of REM sleep; May cause a
“hangover” effect
 Shorter-acting drugs - helpful for the person who has
difficulty falling asleep, but then stays asleep.

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16
Q

Uses of Benzodiazepines - Epilepsy & Seizure

A

 Diazepam and Lorazepam are used for status

epilepticus.

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17
Q

Uses of Benzodiazepines - Sedation, Amnesia, & Anesthesia

A

 Midazolam - used in preparation for anesthesia for
short surgical procedures. Given IV.
 Anterograde amnesia

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18
Q

Uses of Benzodiazepines - Muscle Relaxation

A

 Diazepam is sometimes used for acute muscle spasm

and pain as a result of injury.

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19
Q

Uses of Benzodiazepines - Withdrawal from Alcohol and Barbiturates

A

 Long-term use of alcohol or barbiturates can produce
physical dependence and result in withdrawal that is
very severe and can be life threatening.
 Benzodiazepines such as Chlordiazepoxide,
Diazepam, and Lorazepam are used to provide a
more tapered withdrawal.

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20
Q

Anxiety disorders in which BZs are not used

Study These Flashcards
A
  • Obsessive-compulsive disorder: treated with SSRIs
  • Agoraphobia and panic disorders: treated with SSRIs
  • Post-traumatic stress: treated with antidepressants
  • Anxiety in children and adolescents: antidepressants
21
Q

Benzodiazepines - Side Effects

Study These Flashcards
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-stimulation, hyperactivity and
aggressive behavior may occur due to dis-inhibition
of suppressed behavior -more likely in the elderly.
 Supra-additive - CNS depression becomes much
more profound when BZs are combined with alcohol
 Sleep-Related Behaviors - Sleep driving, eating,
walking, etc

22
Q

Benzodiazepines - Tolerance

Study These Flashcards
A

 Common, but patients generally don’t increase dose Physical dependence may occur; high abuse potential
 Withdrawal can result in anxiety and insomnia

23
Q

Benzodiazepines - Contraindications

Study These Flashcards
A

 Should not be given during pregnancy unless
absolutely necessary. Some are Category D
 Sleep apnea - may decrease tone of upper airway
 Elderly

24
Q

Benzodiazepines - Withdrawal

Study These Flashcards
A

 Abrupt discontinuation can cause rebound increases
in insomnia and anxiety
 Muscle weakness, tremor, hyperalgesia, nausea,
vomiting, weight loss and convulsions
 BZs should be tapered very slowly following chronic
use

25
Benzodiazepines - Overdose
 BZs are relatively safe  Overdose 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.
26
Flumazenil (Mazicon) - MoA
 Benzodiazepine antagonist  Competes with BZs for GABA receptor; reverses the effects of BZs
27
Flumazenil (Mazicon) - Uses
 Example: reverses the effect of midazolam (Versed®), which sometimes causes respiratory depression  Also reverses the effects of other drugs (“z-drugs”) that act on BZ binding site  Evidence showing effective treatment for hypersomnia conditions
28
Flumazenil (Mazicon) - Pharmacokinetics
 Duration of action is ~30 minutes
29
Flumazenil (Mazicon) - Adverse Effects
Triggers withdrawal and seizures in patients who are physically dependent upon BZs.
30
Flumazenil (Mazicon) - Contraindications
 Do not use in patients with history of seizures
31
Zolpidem (Ambien®), Zaleplon (Sonata®), Eszopiclone (Lunesta®) - MoA
 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
32
Zolpidem (Ambien®), Zaleplon (Sonata®), Eszopiclone (Lunesta®) - Uses
Insomnia
33
Zolpidem (Ambien®), Zaleplon (Sonata®), Eszopiclone (Lunesta®) - Pharmacokinetics
• Well-absorbed orally; peak levels in 30-60 min • Metabolized in liver (CYP3A4), excreted by kidney • Short duration of action, thus morning drowsiness is unlikely • Exception: Eszopiclone has a long half life; long-term treatment • Half-life may be prolonged in severe hepatic disease
34
Zolpidem (Ambien®), Zaleplon (Sonata®), Eszopiclone (Lunesta®) - Adverse Effects
 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  Low incidence of tolerance and dependence  Rebound insomnia may occur after rapid discontinuation  Withdrawal symptoms (CNS stimulation, anxiety, seizures) with abrupt cessation after long-term use of eszopiclone
35
Suvorexant (Belsomra®) - MoA
Antagonist at orexin receptors  Orexins are involved in regulating the sleep-wake cycle and promote wakefulness
36
Suvorexant (Belsomra®) - Adverse Effects
headache 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
37
Suvorexant (Belsomra®) - Pharmacokinetics
Metabolized by CYP3A4, so drug interactions likely with inhibitors such as cimetidine Effects will be magnified if combined with other CNS depressants
38
Suvorexant (Belsomra®) - Contraindications
patients with narcolepsy
39
Ramelteon (Rozerem®) - MoA
 Melatonin analogue; Resets sleep-wake cycle |  Promotes sleepiness w/no GABA effect
40
Ramelteon (Rozerem®) - Pharmacokinetics
• Orally absorbed, with extensive first pass metabolism • Metabolized by CYP450s (3A4; 2C9) in liver • Additive sedation with alcohol and other sedative hypnotics
41
Ramelteon (Rozerem®) - Side Effects
Drowsiness, dizziness and nausea most common
42
Diphenhydramine (Benadryl®)
- Older antihistamines have sedative properties.  They are the active ingredient in the majority of OTC preparations for insomnia.  They are useful for occasional insomnia, and are especially useful in someone who has been addicted to benzodiazepines or alcohol.
43
Chloral Hydrate (Noctec®) - MoA
 Converted to trichloroethanol, which causes sedation |  Acts similarly to barbiturates on GABAa receptor
44
Chloral Hydrate (Noctec®) - Uses
• in children for sedation during pediatric dental procedures • in nursing homes and chronic care institution
45
Chloral Hydrate (Noctec®) - Adverse Effects
 Low margin of safety; high doses induce respiratory and vasomotor depression  Causes gastric irritation, nausea and emesis, allergic responses, may produce cardiac arrhythmias  Long-term use may cause liver damage and fatal intoxication  Use as a sedative-hypnotic not recommended
46
Buspirone (BuSpar®) - MoA
 Relieves anxiety without producing sedation  Partial agonist at the postsynapitc5-HT1A (serotonin) receptor -> inhibition of cell signaling  Full agonist for presynaptic5-HT1A receptors -> decreased release of 5-HT
47
Buspirone (BuSpar®) - Uses
 Generalized anxiety and anxiety with depression  ADHD and autistic patients with anxiety  Premenstrual syndrome  Very low addiction potential - excellent choice for anxiety in recovering alcoholics/addicts  Not good for severe anxiety and/or panic disorder
48
Buspirone (BuSpar®) - Pharmacokinetics
 Well-absorbed orally; significant first-pass metabolism  Metabolized in liver (CYP3A4)  Anxiolytic effect takes about 2 weeks to develop  No muscle relaxant or anticonvulsant properties  Does not potentiate CNS depression with alcohol or BZs
49
Buspirone (BuSpar®) - Side Effects
- Fairly safe even in high doses.  Light-headedness, restlessness, headache, drowsiness, and nausea/vomiting

Pharmacology III (10 decks)

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