Stimulants B&B Flashcards

1
Q

what are the 2 physiological effects of cocaine?

A
  1. local anesthetic (Na+ channel blocker)
  2. inhibits monoamine reuptake (dopamine, 5HT, NE) —> sympathetic activation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what is the classic hallucination of cocaine intoxication?

A

tactile hallucination - “bugs crawling on skin”

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

what is the treatment for cocaine intoxication? what drugs should be avoided?

A

tx with benzodiazepines - CNS depressants, counteract stimulatory effect of cocaine

AVOID beta blockers - further increase unopposed alpha adrenergic activity, worsen HTN and chest pain

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

how do amphetamines increase synaptic NE and dopamine?

A

promote release AND inhibit reuptake

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

what is the treatment for amphetamine intoxication?

A

tx with benzodiazepines - CNS depressants, counteract stimulatory effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

caffeine is an antagonist of ______ receptors, which leads to…

A

caffeine (methylxanthine) is an antagonist of ADENOSINE receptors, which leads to release of dopamine and NE

also blocks renal adenosine receptors —> diuresis

[recall adenosine = vasodilator, used in chemical stress tests]

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

where are nicotinic ACh receptors found?

A
  1. between pre- and post- ganglionic neurons in sympathetic nervous system
  2. adrenal medulla
  3. between pre- and post- ganglionic neurons in parasympathetic nervous system
  4. post synaptic neurons in skeletal muscle
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

which antidepressant is used in smoking cessation? how does it work?

A

bupropion: antidepressant, blocks reuptake of NE and dopamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

what is the clinical use of varenicline?

A

partial nicotinic receptor agonist used for smoking cessation

agonists effects limit withdrawal symptoms, antagonist effects block nicotine

AE: nausea, sleep disturbance

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

What are the EEG findings of each of the sleep stages?

A

awake, eyes open = beta waves (low amplitude, high frequency)

Awake, eyes closed = alpha waves (increased amplitude, more synchronous)

N1 = lightest sleep, Theta waves
N2 = largest percentage of sleep, Theta waves + K complexes (sudden increase in amplitude) + sleep spindles (sudden increase in frequency)
N3 = deepest sleep, delta waves (lowest frequency, highest amplitude - “slow waves”) - sleepwalking/talking/bedwetting occurs here

REM = low voltage sawtooth pattern, coordinated by PPRF - muscle paralysis occur is here (sleep paralysis also occurs here)

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

what sleep changes occur in depression? (3)

A
  1. decreased REM latency – REM sleep starts quicker
  2. Increased total REM sleep
  3. decreased N3/slow wave sleep

[sleep rhythms normalize on antidepressants]

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the clinical use of modafinil?

A

treats narcolepsy by promoting wakefulness - controlled substance, risk of abuse

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Name two indirect sympathomimetics that treat both ADHD and narcolepsy

A
  1. methylphenidate
  2. amphetamines

both increase dopamine and NE in synapses

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

What is the clinical use of sodium oxybate?

A

Salt form of gamma hydroxybutyrate (GABA metabolite) that causes CNS depression

Reduces cataplexy caused by narcolepsy, also improves nocturnal sleep and reduces daytime sleepiness

Illegally used as date rape drug

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

describe the MOA of amphetamine, dextroamphetamine, methamphetamine, and lisdexamfetamine

A
  1. enter presynaptic dopaminergic neurons both directly and via DAT and NET transporters
  2. pumped inside intracellular vesicles via vesicular transporter (VT), displacing DA and NE
  3. this causes massive outflow of DA and NE into synaptic cleft

—> in prefrontal cortex, enhance alertness/ concentration + reduce hyperactivity/impulsivity/ appetite

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

for what conditions are amphetamine, dextroamphetamine, methamphetamine, and lisdexamfetamine used to treat?

A

increase synaptic DA and NE, tx:

  1. ADHD - first line, both short-acting and long-acting have rapid onset of action
  2. narcolepsy - off-label
17
Q

contrast the adverse effects of amphetamines in adults vs children

A

adults: dry mouth, insomnia, irritability, headaches, dysphoria (distress), weight loss; less commonly psychosis, priapism, tics; euphoric/psychoactive (Schedule II)

children: weight loss, poor growth, sleep disturbances, jitteriness, emotional lability, social withdrawal

18
Q

what is the MOA and clinical use of methylphenidate (MPH)?

A

NE-5HT reuptake inhibitor (NRDI) - block DAT and NET —> affect prefrontal cortex to enhance alertness/concentration, reduce hyperactivity/impulsivity, suppress appetite

tx ADHD (1st line) and narcolepsy (2nd line)

19
Q

name a NE-5HT reuptake inhibitor (NRDI) that treats both ADHD and narcolepsy

A

methylphenidate (MPH): block DAT and NET —> affect prefrontal cortex to enhance alertness/concentration, reduce hyperactivity/impulsivity, suppress appetite

schedule II controlled substance!

20
Q

what is the MOA and clinical use of modafinil and armodafinil?

A

weak inhibitor of DA reuptake —> promotes wakefulness

treats narcolepsy (first line)

AE: headache, nausea, decreased appetite, insomnia, anxiety, diarrhea, Schedule IV

21
Q

name an inhibitor of DA reuptake that is first-line for treating narcolepsy

A

modafinil, also armodafinil

MODify your sleep!

22
Q

what is the MOA of caffeine?

A

competitive antagonist of adenosine receptors

adenosine is NT that activates sleep-promoting ventrolateral preoptic (VLPO) nucleus in the brain; builds up throughout the day as byproduct of cellular metabolism and causes feeling of tiredness

23
Q

what are the effects (specifically) of caffeine on CNS, cardiovascular, renal, and GI systems?

A

CNS: decreases fatigue (antagonizes adenosine), mildly elevates DA and NE

cardiovascular: inotropic + chronotropic, short-term increase in BP

renal: mild diuretic

GI: increases acid (H+) secretion from gastric mucosa

24
Q

what is the function of adenosine?

A

adenosine: NT that activates sleep-promoting ventrolateral preoptic (VLPO) nucleus in the brain; builds up throughout the day as byproduct of cellular metabolism and causes feeling of tiredness

caffeine antagonizes adenosine receptors

25
Q

in whom should caffeine intake be limited? (6)

A
  1. pregnancy/nursing
  2. sleep disorders
  3. migraines
  4. peptic ulcers or GERD (causes increase in H+ secretion)
  5. cardiac arrhythmias
  6. HTN
26
Q

what are the CNS and peripheral effects of nicotine?

A

agonist at ACh nicotinic receptors in the brain

CNS: euphoria/reward, arousal, relaxation, appetite suppression, improved attention/learning/reaction time

peripheral: vasoconstriction, increased BP + HR

27
Q

what is the MOA of cocaine?

A

inhibits dopamine transporters (DAT) to prevent reuptake, also blocks NET (NE reuptake) and SERT (5-HT transporter)