Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology III > Sedative Hypnotics & Anxiolytics > Flashcards

Sedative Hypnotics & Anxiolytics Flashcards

1
Q

Primary use of Sedative-Hypnotic/Anxiolytic Drugs

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

GABA - MoA

A 
 CNS depressants
 Gamma-amino-butyric-acid (GABA)
 Major inhibitory neurotransmitter
 Widely distributed in CNS
 Relieves anxiety, promotes sedation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Barbiturates - Withdrawal

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Uses of Benzodiazepines - Epilepsy & Seizure

A

 Diazepam and Lorazepam are used for status

epilepticus.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Uses of Benzodiazepines - Sedation, Amnesia, & Anesthesia

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Uses of Benzodiazepines - Muscle Relaxation

A

 Diazepam is sometimes used for acute muscle spasm

and pain as a result of injury.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Anxiety disorders in which BZs are not used

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

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

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

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

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
Q

Benzodiazepines - Overdose

A

 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
Q

Flumazenil (Mazicon) - MoA

A

 Benzodiazepine antagonist
 Competes with BZs for GABA receptor; reverses the
effects of BZs

27
Q

Flumazenil (Mazicon) - Uses

A

 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
Q

Flumazenil (Mazicon) - Pharmacokinetics

A

 Duration of action is ~30 minutes

29
Q

Flumazenil (Mazicon) - Adverse Effects

A

Triggers withdrawal and seizures in patients who are physically dependent upon BZs.

30
Q

Flumazenil (Mazicon) - Contraindications

A

 Do not use in patients with history of seizures

31
Q

Zolpidem (Ambien®), Zaleplon (Sonata®), Eszopiclone (Lunesta®) - MoA

A

 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
Q

Zolpidem (Ambien®), Zaleplon (Sonata®), Eszopiclone (Lunesta®) - Uses

A

Insomnia

33
Q

Zolpidem (Ambien®), Zaleplon (Sonata®), Eszopiclone (Lunesta®) - Pharmacokinetics

A

• 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
Q

Zolpidem (Ambien®), Zaleplon (Sonata®), Eszopiclone (Lunesta®) - Adverse Effects

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
 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
Q

Suvorexant (Belsomra®) - MoA

A

Antagonist at orexin receptors

 Orexins are involved in regulating the sleep-wake
cycle and promote wakefulness

36
Q

Suvorexant (Belsomra®) - Adverse Effects

A

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
Q

Suvorexant (Belsomra®) - Pharmacokinetics

A

Metabolized by CYP3A4, so drug interactions likely with inhibitors such as cimetidine

Effects will be magnified if combined with other CNS depressants

38
Q

Suvorexant (Belsomra®) - Contraindications

A

patients with narcolepsy

39
Q

Ramelteon (Rozerem®) - MoA

A

 Melatonin analogue; Resets sleep-wake cycle

 Promotes sleepiness w/no GABA effect

40
Q

Ramelteon (Rozerem®) - Pharmacokinetics

A

• Orally absorbed, with extensive first pass metabolism
• Metabolized by CYP450s (3A4; 2C9) in liver
• Additive sedation with alcohol and other sedative
hypnotics

41
Q

Ramelteon (Rozerem®) - Side Effects

A

Drowsiness, dizziness and nausea most common

42
Q

Diphenhydramine (Benadryl®)

A
  • 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
Q

Chloral Hydrate (Noctec®) - MoA

A

 Converted to trichloroethanol, which causes sedation

 Acts similarly to barbiturates on GABAa receptor

44
Q

Chloral Hydrate (Noctec®) - Uses

A

• in children for sedation during pediatric dental
procedures
• in nursing homes and chronic care institution

45
Q

Chloral Hydrate (Noctec®) - Adverse Effects

A

 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
Q

Buspirone (BuSpar®) - MoA

A

 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
Q

Buspirone (BuSpar®) - Uses

A

 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
Q

Buspirone (BuSpar®) - Pharmacokinetics

A

 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
Q

Buspirone (BuSpar®) - Side Effects

A
  • Fairly safe even in high doses.

 Light-headedness, restlessness, headache, drowsiness, and nausea/vomiting

Pharmacology III (10 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions