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PPI-2 > CNS Depressants and Psychostimulants > Flashcards

CNS Depressants and Psychostimulants Flashcards

1
Q

What is the MOA for benzodiazepines and barbiturates?

A
  • Bind to allosteric site on GABA-A receptors
  • Increase affinity of GABA-A receptor for GABA
  • Potentiation of GABAergic inhibition of neuronal activity
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2
Q

What are general therapeutic uses for benzodiazepines?

A

Insomnia, anesthesia, anxiety, seizures, essential tremor, and spasticity

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3
Q

What are general adverse effects of benzodiazepines?

A

Drowsiness, confusion (esp in older patients), anterograde amnesia, psychomotor impairment, substance use disorder (tolerance and withdrawal)

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4
Q

T/F: Patients that are elderly with liver disease should take lorazepam due to it being safer

A

True; This is also relevant if they asked about oxazepam or temazepam (also good for cyp inhibitors)

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5
Q

T/F: If BDZ has been used for <3 days taper dose gradually to avoid rebound insomnia or anxiety

A

False, this is if the BDZ is taken for at least greater than a month

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6
Q

What drug is a benzodiazepine antagonist?

A

Flumazenil

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7
Q

What is the MOA of flumazenil?

A

Competitive antagonist at BDZ binding site

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8
Q

What are the clinical uses for flumazenil?

A

Treats BDZ overdose and used in anesthesiology to reverse effects of BDZs

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9
Q

What are novel BDZ receptor agonists?

A

Zolpidem, zaleplon, and eszopiclone

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10
Q

What is the MOA of zolpidem, zaleplon, and eszopiclone?

A
  • Bind to allosteric site on GABA-A receptors
  • Increase affinity of GABA-A receptor for GABA
  • Potentiation of GABAergic inhibition of neuronal activity
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11
Q

What are the clinical uses for novel BDZ receptor agonists (zolpidem, zaleplon, and eszopiclone)?

A

Sleep onset and sleep maintenance insomnia–> approved for long-term use

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12
Q

T/F: Z-compounds have fewer adverse effects than BDZs

A

True

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13
Q

What drug is a melatonin receptor agonist?

A

Ramelteon

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14
Q

What is the MOA of ramelteon?

A

Agonist at MT1 (regulates sleep) and MT2 (regulates circadian rhythm) melatonin receptors

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15
Q

What are the clinical uses for ramelteon?

A

Sleep onset insomnia

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16
Q

T/F: Ramelteon is more efficacious than BDZs and Z compounds

A

False; It is less effective but is the only approved sedative-hypnotic drug that is not controlled

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17
Q

What drug is a orexin receptor antagonist?

A

Suvorexant

18
Q

What is the MOA of suvorexant?

A

Antagonist at OX1 and OX2 orexin receptors

19
Q

What are the clinical uses for suvorexant?

A

Sleep-onset and sleep-maintenance insomnia

20
Q

What are adverse effects of orexin receptor antagonists?

A

Daytime sedation, impaired driving, substance use disorder

21
Q

What are the therapeutic uses for the barbiturate pentobarbital?

A

Insomnia and seizures

22
Q

What are adverse effects of pentobarbital?

A

Tolerance, physical dependence, high addition potential, low therapeutic index, induces CYP enzymes, long half life

23
Q

What is the therapeutic indication and adverse effects seen with H1 antihistamines (diphenhydramine, doxylamine)

A
  • Used for insomnia
  • Adverse effects: significant daytime sedation (has a long half life) and anticholinergic effects (off target effects)
24
Q

What are clinical uses of psychostimulants?

A
  1. Treatment of excessive sleepiness and fatigue (narcolepsy)
  2. Improvement of attention (ADHD)
25
Q

What is the MOA of indirect acting sympathomimetic drugs?

A

Increase synaptic concentration of endogenous catecholamines–> increased NE, DA, and 5-ht

26
Q

What drug is part of the “releasing agents” class?

A

Amphetamine

27
Q

What drugs are part of the “reuptake inhibitors” class?

A

Cocaine, methylphenidate, and modafinil/armodafinil

28
Q

What are predictable effects of psychostimulants?

A

NE: Increased arousal and less need for sleep
DA: euphoria, reward, potential for abuse, abnormal movements, psychosis
5-HT: hallucinations and decreased appetite

29
Q

What is the MOA of amphetamine?

A

Displaces stored catecholamines: uptake via NET and VMAT-2 and replaces DA in vesicles which leads to DA release via DA

30
Q

What are the clinical uses for amphetamine?

A

ADHD and narcolepsy

31
Q

What adverse effects are seen with amphetamine?

A

From increased NE: higher bp, cardiac arrhythmias, insomnia
From increased DA: growth inhibition
From increased 5-HT: anorexia

32
Q

What adverse effects are seen with amphetamine?

A

From increased NE: higher bp, cardiac arrhythmias, insomnia
From increased DA: growth inhibition
From increased 5-HT: anorexia

33
Q

What is the MOA for methylphenidate?

A

Blocks NET and DAT which leads to higher levels of dopamine and norepinephrine

34
Q

What are the clinical uses for methylphenidate?

A

ADHD and narcolepsy

35
Q

T/F: Adverse effects of methylphenidate are similar to amphetamine

A

True

36
Q

What is the MOA of modafinil?

A

May block NET and DAT which leads to higher levels of dopamine and norepinephrine

37
Q

What are the clinical uses for modafinil?

A

Narcolepsy or other disorders that cause excessive sleepiness

38
Q

What are the adverse effects of modafinil?

A

Less adverse effects than amphetamine or methylphenidate (d/t less sympathomimetic effects)

39
Q

T/F: Bupropion and atomoxetine can be used to treat ADHD and is first line

A

False; Bupropion and atomoxetine are indeed used to treat ADHD but are not first line

40
Q

T/F: All reuptake inhibitors are stimulants

A

False; TCAs, SSRIs, and SNRIs have different indications like depression and are not used for ADHD

PPI-2 (7 decks)

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