Brainscape's Knowledge GenomeTM

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


See full index

Emma H&N > Psychostimulants > Flashcards

Psychostimulants Flashcards

1
Q

general drugs for ADHD

A
  • Amphetamines/Amphetamine-like agents (methylphenidate) (IR or XR)
  • Atomoxetine (NSRI)
  • Guanfacine and Clonidine (alpha-2 agonists)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

amphetamines MOA

A

(ADHD)
Monoamine agonists –> stimulate monoamine NTs (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.

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

main concerns for amphetamines

A 
(ADHD)
STIMULANT EFFECTS
-increased CNS (insomnia)
-GI (suppressed appetite, fullness, nausea) 
-stimulated CV (NE release)

PSYCHOSIS

  • hallucinations/delusions with high doses
  • bc inc dopamine in mesolimbic path

PSYCHOLOGICAL DEPENDENCE
-Schedule II

WITHDRAWAL

  • depressed mood, fatigue
  • start w/ low dose and work up
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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 BP

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

Change pH of urine to much lower than pKa of drug (urine trapping since amphetamines are basic)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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 (NE effects are confined to brain)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

black box label warnings for Adderall, amphetamines

A
  • high potential for abuse
  • lead to drug dependence (limbic path path stimulated)
  • serious cardiovascular effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

schedule II drugs

A

High potential for abuse, currently accepted medical use

  • restricted quantities
  • highly controlled (need signature/DEA#, telephone for emergencies only, etc.)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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 in prefrontal cortex.

similar mech to anti-depressants.

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

atomoxetine metabolism, schedule #

A 
(ADHD)
Hepatic metabolism (CYP2D6)

Schedule VI drug (non-stimulant)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

atomoxetine concerns

A
  • CNS (insomnia)
  • GI (appetite suppression)
  • Cardiovascular (inc bp)
  • others:
  • –dry mouth, urinary retention (anti-muscarinic)
  • –priapism (prolonged, painful erection due to vasoconstriction)
  • –drug interactions (if they block 2D6 then lead to toxicity bc inhibits clearance)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

black box label warning for atomoxetine

A

Increased risk of suicidal ideation.

  • unclear why
  • confounding
  • overall very small risk
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Guanfacine, Clonidine use/MOA

A

ADHD

MOA: alpha-2 receptor agonists (sympatholytic) –> prevents release of NTs
(recall alpha-2 receptors - when stimulated - suppress release of transmitter)

(MOA for ADHD unclear)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

side effects of Guanfacine, Clonidine

A

(ADHD)
Sedation
Dry mouth
Hypotension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

what schedule # is Guanfacine and Clonidine?

A

(ADHD)

Schedule VI drugs

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

drugs for treatment of sleepiness, narcolepsy, cataplexy

A

Caffeine
Modafinil
Gammahydroxybutyrate

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

caffeine is an analog to ________

A

caffeine is an analog to ADENOSINE (an endogenously produced nucleoside that normally INHIBITS transmitter release)

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

caffeine mechanism

A

(sleepiness)
MOA: adenosine receptor antagonist (same shape, but does not cause same effect, just blocks site)
- ultimately inhibiting an inhibitor –> inc transmitter release

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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

pharmacological effects of caffeine

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

concerns with caffeine

A
  • CNS (seizures)
  • suppressed GI
  • cardiovascular overstimulation
  • tolerance/withdrawal (rebound effect, cranial vasodilation –> HA)
  • be cognizant of guarana (natural caffeine) and presence in supplements
21
Q

metabolic byproducts of caffeine

A

All contain xanthine.

Theophylline is a rx drug itself.

  • bronchodilator
  • narrow therapeutic window
  • increased adverse effects (more intense caffeine-like sx)
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

isomer: armodafinil

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)

date rape drug.

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 bc GABA is primary inhibitor)
-exhibits GABA and dopamine-like effects
^ DA/GABA agonism

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

Reduce appetite. 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

-similar receptor being modulated as fen-phen –> possibly future cardiomyopathy issues?

35
Q

burpropion + Naltrexone use, MOA

A

Anorexiant

DA and NE reuptake inhibitor.
Opioid receptor antagonist. (prevent reward pathways from being stimulated. No reward when people eat.)

36
Q

fenfluramine and dexfenfluramine: old use, current use, MOA

A

(fen-phen)
Previous: anorexiant
Currently: off market

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

sibutramine: old use, current use, MOA

A

Previous: anorexiant, stimulant drug
Currently: off market

NE, 5HT transport inhibition
- more NE 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, HTN, dyslipidemia)

40
Q

other agents used as anorexiants

A 
OTC decongestants (in sudafed prods, stim alpha-1-r or promote NE release)
GLP-1 analogs (non-stimulants)
Absorption inhibitors (non-stimulants)
41
Q

Methylphenidate (Ritalin) has lesser risk of cardiac side effects, why?

A

ability of NE to promote methylphenydate release seems to be confined to brain, not periphery or extremities

42
Q

MA schedule of drugs

A

schedule I: high abuse potential (no accepted med use (heroin, cocaine used illicitly)

schedule II: high abuse potential, accepted med use (amphetamines)

schedule III-IV: less potential for abuse

schedule VI: all other rx drugs (penicillin)

43
Q

Phentermine is sometimes used in combo w/ which med?

A

topiramate (Qsymia)

an anti-convulsant that promotes nausea.

44
Q

Are lorcaserin and buoprion+naltrexone stimulants?

A

NOT stimulants.

Rx’d for weight loss via acting in hypothalamus to suppress appetite.

45
Q

Order of pharmacological tx for ADHD

A
  1. stimulants (methylphenidate or amphetamine)
  2. stimulants (try another subtype)
  3. atomoxetine (Strattera)
  4. buproprion
  5. tricyclic antidepressants
  6. alpha agonists

Emma H&N (49 decks)

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