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AIM - The Brain > Psychostimulants > Flashcards

Psychostimulants Flashcards

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1
Q

general drugs for ADHD

A
  • Amphetamines/Amphetamine-like agents (methylphenidate) (IR or XR)
  • Atomoxetine (NSRI)
  • Guanfacine and Clonidine (alpha-2 agonists)
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2
Q

amphetamines MOA

A

(ADHD)
Stimulate monoamine neurotransmitters (promote release of biogenic amines from storage sites)

Prevents storage of dopamine in vesicles in the axon terminal.
High levels of dopamine.
Transporters push domamine into synaptic cleft due to high concentration.

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3
Q

main concerns for amphetamines

A 
(ADHD)
STIMULANT EFFECTS
-increased CNS
-suppressed GI
-stimulated cardiovascular

PSYCHOSIS
-hallucinations/delusions with high doses

PSYCHOLOGICAL DEPENDENCE

WITHDRAWAL
-depressed mood, fatigue

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4
Q

Why are there cardiovascular concerns with amphetamines?

A

(ADHD)
Stimulants –> stimulate NE release.
NE most readily stimulates Alpha-1 receptors –> increased vasoconstriction, increased peripheral resistance –> increased blood pressure

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5
Q

management of overdose of amphetamines

A

(ADHD)
Control cardiovascular hemodynamics
-alpha blockers, nitrates

Sedatives
-benzodiazepines

Activated Charcoal
-ties up any drug still available to prevent further absorption

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6
Q

names of amphetamines & like agents

A 
(ADHD)
Amphetamine (Benzedrine)
-dextroamphetamine (dexedrine)
-amphetamine + detroamphetamine (Adderall, most common)
-lisdexfetamine (Vyvanse)

Methylphenidate (Ritalin)

  • dexmethylphenidate (focalin)
  • have fewer cardiovascular effects
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7
Q

black box label warnings for Adderall, amphetamines

A
  • high potential for abuse
  • lead to drug dependence
  • serious cardiovascular effects
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8
Q

schedule II drugs

A

High potential for abuse, currently accepted medical use

  • restricted quantities
  • highly controlled
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9
Q

atomoxetine (strattera) use and MOA

A

ADHD

Selective inhibitor of NE transport (NSRI)
NONSTIMULANT

Blocks NE reuptake so it is available in synapse for longer.

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10
Q

atomoxetine metabolism, schedule #

A 
(ADHD)
Hepatic metabolism (CYP2D6)

Schedule VI drug (non-stimulant)

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11
Q

atomoxetine concerns

A
  • CNS
  • GI
  • Cardiovascular
  • others:
  • –dry mouth, urinary retention (anti-muscarinic)
  • –priapism (prolonged, painful erection due to vasoconstriction)
  • –drug interactions (if they block 2D6 then lead to toxicity)
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12
Q

black box label warning for atomoxetine

A

Increased risk of suicidal ideation.

  • unclear why
  • confounding
  • overall very small risk
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13
Q

Guanfacine, Clonidine use/MOA

A

ADHD

MOA: alpha-2 receptor agonists –> prevents release of NTs (MOA for ADHD unclear)

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14
Q

side effects of Guanfacine, Clonidine

A

(ADHD)
Sedation
Dry mouth
Hypotension

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15
Q

what schedule # is Guanfacine and Clonidine?

A

(ADHD)

Schedule VI drugs

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16
Q

drugs for treatment of sleepiness, narcolepsy, cataplexy

A

Caffeine
Modafinil
Gammahydroxybutyrate

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17
Q

caffeine is an analog to ________

A

caffeine is an analog to ADENOSINE

18
Q

caffeine mechanism

A

(sleepiness)
MOA: adenosine receptor antagonist (same shape, but does not cause same effect, just blocks site)

Adenosine binding to PRESYNAPTIC receptor:

  • closes Ca++ channels
  • decreased NT release

Adenosine binding to POSTSYNAPTIC receptor:

  • open K+ channel
  • hyperpolarizes cell
  • decreased response to stimuli

If BLOCKED:

  • increased NT release
  • increased response to stimuli
19
Q

pharmacological effects of caffeine

A 
(sleepiness)
Effects: 
-increased arousal and alertness
-anorexia
-cardiac and smooth muscles effects
-diuresis
20
Q

concerns with caffeine

A
  • CNS (seizures)
  • suppressed GI
  • cardiovascular overstimulation
  • tolerance/withdrawal
  • be cognizant of guarana (natural caffeine) and presence in supplements
21
Q

metabolic byproducts of caffeine

A

All contain xanthine.

Paraxanthine is a prescription drug itself.

  • bronchodilator
  • narrow therapeutic window
  • increased adverse effects
22
Q

mechanism of Modafinil (provigil)

A

Blocks dopamine transporter (dopamine available in synapse longer).
Increases synaptic dopamine (DSRI).
Not entirely clear how it relates to sleep

23
Q

Modafinil uses

A

Excessive sleepiness.

  • narcolepsy
  • shift work
  • obstructive sleep apnea
24
Q

schedule # for Modafinil?

A

schedule IV

-potential for abuse, but minor

25
Q

gammahydroxybutyrate (GHB) is also known as

A

Sodium oxybate (Xyrem)

used for cataplexy/narcolepsy

26
Q

use of GHB (gammahydroxybutyrate)

A

Cataplexy (low muscle tone –> falls).
Narcolepsy.

Promotes profound sleep at night, so less likely to fall asleep the next day.

27
Q

MOA of gammahydroxybutyrate (GHB)

A

(narcolepsy, cataplexy)

  • potent enhancer of GABA (powerful sedative)
  • exhibits GABA and dopamine-like effects

date rape drug (conscious sedation)

28
Q

schedule # of GHB

A

(narcolepsy, cataplexy)

schedule III
bc date rape drug

29
Q

concerns with GHB (gammahydroxybutyrate)

A

(narcolepsy/cataplexy)

Fatal overdose due to respiratory depression.

30
Q

names/types of anorexiants

A
  • phentermine: NE transporter inhibition
  • lorcaserin: 5HT(2C) receptor agonist
  • bupropion + naltrexone: DA and NE reuptake inhibitor and opioid receptor antagonist
31
Q

anorexiants are used to

A

Treat obesity.
Moderate weight gain.

Have rebound effect when stop using so beware.

32
Q

phentermine (lonamin) MOA

A

anorexiant

NE transporter inhibition

  • NE stays in synapse longer, acts as stimulant
  • sympathetic NS activated, parasympathetic suppressed
33
Q

side effects of phentermine

A

(anorexiant)

  • increased BP
  • increased arousal
  • irritability

due to increased NE

34
Q

lorcaserin (belviq) use, MOA

A

anorexiant

5HT(2C) [serotonin] receptor agonist

  • more serotonin produced
  • change in hypothalamus
  • less hungry
35
Q

burpropion + Naltrexone use, MOA

A

Anorexiant

DA and NE reuptake inhibitor.
Opioid receptor antagonist.

36
Q

fenfluramine and dexfenfluramine: old use, current use, MOA

A

Previous: anorexiant
Currently: off market

  • serotonin modulation
  • carried over to cardiac valves –> pulmonary hypertension
37
Q

sibutramine: old use, current use, MOA

A

Previous: anorexiant
Currently: off market

NE, 5HT transport inhibition
-in periphery –> CV side effects

38
Q

main concerns with anorexiants

A
  • CNS
  • cardiovascular
  • rebound effects on discontinuation
  • commonly found undeclared in dietary supplements
39
Q

candidate for anorexiants if:

A
  • obese and unresponsive to lifestyle modification

- overweight with comorbidities (diabetes, hypertension, dyslipidemia)

40
Q

other agents used as anorexiants

A

OTC decongestants
GLP-1 analogs (non-stimulants)
Absorption inhibitors (non-stimulants)

AIM - The Brain (105 decks)

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