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Pharmacology 3 > E1- Sedative-Hypnotics and Anxiolytics > Flashcards

E1- Sedative-Hypnotics and Anxiolytics Flashcards

1
Q

What is the major inhibitory neurotransmitter in the brain?

A

GABA

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2
Q

What is the general MOA of sedative-hypnotics/anxiolytics?

A

Bind to GABA, to either intensify or prolong the actions of GABA

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3
Q

What is an antihistamine used as an anti-anxiety medication that causes sedation that is a good option for recovering addicts and the elderly?

A

Hydroxyzine

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4
Q

What is the MOA of barbiturates?

A

Bind to GABA receptor to stimulate Cl- influx and produce inhibition independent of GABA (prolongs channel opening time)

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5
Q

What makes barbiturates a drug of abuse?

A

Causes euphorai

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6
Q

What long-acting barbiturate is used as an anticonvulsant?

A

Phenobarbital

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7
Q

Do barbiturates cross the BBB?

A

Yes, CNS depressant

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8
Q

How are barbiturates metabolized?

A

By the liver

Induce CYP450s

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9
Q

What are SE of barbiturates?

A

CNS depression
Paradoxical excitement
Severe physiological and psychological dependence

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10
Q

What are contraindications of barbiturates?

A

Porphyria
Pulmonary insufficiency
Combination with alcohol (supra-additive effects)

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11
Q

What is the safety margin of barbiturates?

A

Low margin of safety, no “ceiling effect”

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12
Q

How is barbiturate OD treated?

What should not be given?

A

Diuresis and alkalization of the urine

Stimulants increase mortality rate

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13
Q

What patient population should typically not be given benzodiazepines?

A

Elderly (do not metabolize BZs as quickly)

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14
Q

What benzodiazepines have a long duration of action?

A

Diazepam

Flurazepam

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15
Q

What benzodiazepines have an intermediate duration of action?

A

Alprazolam
Lorazepam
Oxazepam

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16
Q

What benzodiazepine has a short duration of action?

A

Midazolam

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17
Q

What is the MOA of benzodiazepines?

A

Bind to GABA receptor to increase the affinity of the receptor to GABA, prolonging its action; dependent on GABA

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18
Q

What is the safety margin of benzodiazepines?

A

High margin of safety, “ceiling effect”

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19
Q

What are the general uses of benzodiazepines?

A 
Anxiety
Insomnia
Status epilepticus
Sedation, amnesia, anesthesia
Muscle relaxation
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20
Q

In what anxiety disorders are benzodiazepines not used?

A

Panic disorder, phobias, obsessive compulsive

PTSD, anxiety in children and adolescents

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21
Q

What benzodiazepines are used for insomnia?

A

Flurazepam

Temazepam

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22
Q

What benzodiazepines are used for Status Epilepticus?

A

Diazepam

Lorazepam

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23
Q

What benzodiazepines is used in preparation for anesthesia for short surgical procedures?
What is a SE?

A

Midazolam (IV)

Anterograde amnesia

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24
Q

What benzodiazepines are used for muscle relaxation?

A

Diazepam

25
Q

What are SE of benzodiazepines?

A

CNS depression
Paradoxical excitement
Supra-additive with alcohol Sleep related behaviors Physical dependence may occur (high abuse potential)

26
Q

What are contraindications of benzodiazepines?

A

Pregnancy
Sleep apnea
Elderly

27
Q

Regarding BZs, what can cause rebound increases in insomnia and anxiety? How can this be avoided?

A

Abrupt discontinuation

Taper slowly

28
Q

What is the MOA of Fluemazenil?

A

Benzodiazepine antagonist; competes with BZs for GABA receptor

29
Q

What is the use of Fluemazenil? (2)

A

Hypoersomnia

Reverse the effects of BZs (Ex: Midazolam, which can sometimes cause respiratory depression)

30
Q

What are SE of Fluemazenil?

A

Triggers withdrawal and seizures in pts who are physically dependent upon BZs

31
Q

What is a contraindication of Fluemazenil?

A

Pts with hx of seizures

32
Q

What the the “z-drugs?”

A

Zolpidem, Zaleplon, Eszopiclone

33
Q

What is the MOA of the “z-drugs?”

A

Bind to the BZ1 subtype of the GABA receptor to increase GABA mediated inhibition

34
Q

What class of sedative-hypnotics have no anxiolytic, anticonvulsant, or muscle relaxant properties?

A

The “z-drugs?”

35
Q

What is the use of the “z-drugs?”

A

Insomnia

36
Q

Do most “z-drugs” have a short or long duration of action?

A

Short duration of action (morning drowsiness is unlikely )

37
Q

Which “z-drug” has a long half-life and can be used for long-term tx of insomnia?

A

Eszopiclone

38
Q

What is the margin of safety for the “z-drugs?”

A

High margin of safety

39
Q

What are SE of the “z-drugs?”

A

GI (diarrhea, nausea)
Drowsiness
Sleep related behaviors
Confusion, memory loss, and psychosis in elderly

40
Q

Regarding the “z-drugs,” what can use rebound insomnia?

A

Rapid discontinuation

41
Q

Abrupt cessation after long-term use of Eszopiclone can cause what?

A

Withdrawal sxs (CNS stimulation, anxiety, seizures)

42
Q

What is the MOA of Suvorexant?

A

Orexin receptor antagonist

43
Q

What is a possible drug interaction with Suvorexant?

A

Metabolized by CYP3A4 (Cimetidine inhibits CYP3A4)

44
Q

What are SE of Suvorexant?

A 
HA
Abnormal dreams
Sleep paralysis
Hallucinations
Worsening depression
45
Q

What is a contraindication of Suvorexant?

A

Narcolepsy

46
Q

What is the MOA of Ramelteon?

A

Melatonin analogue; resets sleep-wake cycle; promotes sleepiness with no GABA effect

47
Q

What are SE of Ramelteon?

A

Drowsiness, dizziness, nausea

48
Q

What is the use of Suvorexant?

A

Insomnia

49
Q

What is the use of Ramelteon?

A

Insomnia

50
Q

What is an antihistamine that can be used for occasional insomnia? (good option for addicts)

A

Diphenhydramine

51
Q

What is the MOA of Chloral Hydrate?

A

Converted to trichloroethanol which causes sedation

52
Q

What is the margin of safety of Chloral Hydrate?

A

Low margin of safety (high doses induce respiratory and vasomotor depression)

53
Q

What can long-term use of Chloral Hydrate cause?

A

Liver damage and fatal intoxication

54
Q

What are uses of Chloral Hydrate?

A

Sedation during pediatric dental procedures

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55
Q

What is the MOA of Buspirone?

A

Relieves anxiety without producing sedation; works independently of GABA at serotonin receptors

56
Q

What class of anxiolytic has no muscle relaxant or anticonvulsant properties?

A

Buspirone

57
Q

Why is Buspirone a good option for tx of anxiety in alcoholics/addicts?

A

Does not potentiate CNS depression with alcohol or BZs

58
Q

What are uses of Buspirone? (6)

A 
Generalized anxiety
Anxiety with depression
ADHD
Autistic pts with anxiety
PMS
Anxiety in recovering alcoholics/addicts

Pharmacology 3 (10 decks)

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