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Neuro B5 - WLB > Stimulants - Lichtblau > Flashcards

Stimulants - Lichtblau Flashcards

1
Q

What are the CNS effects of sympathomimetics?

A
  • Less fatigue
  • More wakefulness/alertness
  • Increased initiative, confidence, & ability to concentrate
  • Increased motor and speech activity
  • Improved athletic performance
  • Increased speed performance of simple mental tasks
  • Decreased food consumption
  • Stimulation of medullary respiratory center
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2
Q

When do sympathomimetics have the greatest effect?

A

If performance is affected by fatigue or lack of sleep

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3
Q

What are the peripheral effects of sympathomimetics?

A
  • Increased systolic and dystolic BP
    • reflex decrease in HR
    • due to increased NE release
  • Arrhythmias (in higher doses)
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4
Q

In order of potency, what are the effects of sympathomimetics on neurotransmission?

A
  • Low dose:
    • Increased release of NE and DA @ jxn
      • increase amount of NT that can act on post-synaptic receptors
  • Medium dose:
    • Blocks NE and DA reuptake
      • further increase in [NE] & [DA] levels
  • High dose:
    • Inhibits monoamine oxidase (MAO) metabolism
      • increase NT levels even higher
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5
Q

What are the effects of acute amphetamine toxicity?

A

Acute = exaggerated therapeutic effects

  • Cardiovascular system
    • headaches, arrhythmias, palpitations, anginal pain, circulatory collapse, and hyperthermia
  • CNS
    • dizziness, agitation, confusion, insomnia, seizures, coma
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6
Q

What do higher doses of sympathomimetics produce?

A

Restlessness and tremor

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7
Q

What are the effects of chronic amphetamine toxicity?

A
  • Amphetamine psychosis
    • vivid hallucinations, paranoid delusions and compulsions
    • marked weight loss
    • will have positive drug screen clinically
    • symptoms will resolve in 7-10 days
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8
Q

What is the treatment for amphetamine caused toxicity?

A
  • Antipsychotic
    • treat psychotic symptoms
  • Acidify patient’s urine
    • Ammonium Chloride IV
    • drugs are weak bases
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9
Q

What are the therapeutic uses of sympathomimetics?

A
  • Attention deficit hyperactivity disorder (ADHD)
  • Narcolepsy

(Questionable use for fatigue/weight loss)

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10
Q

Is amphetamine dependence primarily physical or psychological?

A

Psychological

(person BELIEVES that they need the drug)

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11
Q

What are the central effects of cocaine?

A

Similar to amphetamines, but more potent (1 mg of cocaine = 10 mg of amphetamine)

(awake, alert, confident, speedy, etc.)

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12
Q

What are the peripheral effects of cocaine?

A

Peripheral IV administration or smoking free-base cocaine produces a very intense pleasureable sensation known as “rush” or “flash”

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13
Q

What are the toxic effects of cocaine?

A
  • cardiac arrhythmias
  • coronary/cerebral thrombosis
  • impairs in utero brain development leading to significantly decreased brain size and neurological manifestations
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14
Q

What is the potential MOA of methylxanthines?

A
  • Translocation of intracellular Ca2+ from the sarcoplasmic reticulum
  • Inhibition of phosphodiesterase
    • Elevated levels of second messenger cAMP
    • Nonselective adenosine receptor antagonist
      • inhibits sleepiness-inducing adenosine
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15
Q

How is MDMA similar/different to other sympathomimetics?

A
  • Derived from methamphetamine
    • added methyl group –> increases lipophilicity
    • very rapid entry into the brain
  • Stimulates (CNS) release and inhibits reuptake of
    • Epi
    • NE
    • DA
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16
Q

What are “bath salts”?

A
  • Often contain various amphetamine-like chemicals
  • Chemicals act in the brain like stimulants
  • Toxicity associated with ingesting or snorting “bath salts”
17
Q

How are “bath salts” being used?

A
  • Chemicals act in the brain like stimulant drugs
  • they are sometimes touted as cocaine substitutes
  • present a high abuse and addiction liability
    • oral ingestion
    • snorting
    • smoking
18
Q

What are the clinical uses for methylxanthines?

A
  • Cardiac stimulation in CHF (controversial)
    • dilates coronary arteries –> increased coronary blood flow
    • Increased inotropic and chronotropic forces
      • increased O2 demand by the hear
  • Paroxysmal dyspnea (associated with left heart failure)
  • Analeptic
  • Bronchial asthma
  • Plus ergot alkaloids for migraine
    • vasoconstriction of cerebral vasculature
19
Q

What are the adverse effects of methylxanthines?

A
  • Toxicity seen at doses near 1 gm
    • CNS:
      • insomnia, excitement, mild delirium, sensory disturbances (tinnitus)
      • convulsions
      • >10gm = clonic convulsions & death
    • Cardiovascular
      • increased HR, extra systoles, increased RR
      • decreased clotting time
    • Increased gastric secretions
20
Q

Compare/contrast tolerance of amphetamines, cocaine, and caffeine.

A
  • Amphetamine
    • Develops to effects on appetite and mood
  • Cocaine
    • may develop
    • users can take the same dose every day and get the same effect
  • Caffeine
    • Some (but not all) users develop tolerance to sleep-disrupting effects
21
Q

Compare/contrast dependence of amphetamines, cocaine, and caffeine based on withdrawal symptoms.

A
  • Amphetamines
    • Psychological: craving for drug, prolonged sleep, fatigue, excessive eating, depression
  • Cocaine
    • evidence of withdrawal (physical dependence) is controversial
  • Caffeine
    • May appear within 12-24 hours after discontinuation of caffeine intake
    • headache, irritability, inability to concentrate, drowsiness, insomnia, pain in stomach/upper body/joints
22
Q

What is the MOA of Modafinil & Armodafinil?

A
  • ​Monoamines
    • DA
      • Increase release in striatum
      • Increase release in nucleus accumbens
      • May block DA reuptake
    • NE
      • Increase release in hypothalamus
    • 5HT
      • Increase release in amygdala and frontal cortex
  • Elevates hypothalamic histamine levels
  • Activates glutamatergic circuits
  • Inhibits GABAergic neurotransmission
23
Q

What are common side effects of Modafinil & Armodafinil?

A
  • Headache
  • Nausea
  • Insomnia
  • Lack of appetite
  • Dizziness
  • Agitation
  • Anxiety
  • High BP
24
Q

What are the severe side effects of Modafinil & Armodafinil?

A

Severe dermatologic reactions to Modafinil requiring hospitalization

Neuro B5 - WLB (19 decks)

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