Stimulant medications

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Mechanism of Action - Dopa-Norepi Power-Up

  • Core Effect: Boosts Dopamine (DA) and Norepinephrine (NE) concentrations in the prefrontal cortex synaptic cleft. This enhances executive functions like attention, focus, and impulse control.
  • Dual Mechanisms:
    • Reuptake Blockade: Competitively inhibit Dopamine Transporters (DAT) and Norepinephrine Transporters (NET), leaving more neurotransmitter in the synapse.
    • Enhanced Release: Promote release of DA/NE from presynaptic vesicles (VMAT2 reversal).

Amphetamines vs. Methylphenidate: While both block reuptake, amphetamines are more potent at promoting dopamine/norepinephrine release from vesicles, whereas methylphenidate primarily acts as a reuptake inhibitor.

ADHD Synaptic Mechanisms: Untreated vs. Stimulant-Treated

Stimulant Classes & Agents - The Stimulant Squad

  • Two major classes act on dopamine (DA) and norepinephrine (NE) pathways.
  • 📌 Mnemonic: My Attention is Directed (Methylphenidates & Amphetamines).
ClassPrimary MechanismKey Agents
MethylphenidateBlocks DA & NE reuptake- Methylphenidate (Ritalin, Concerta)
- Dexmethylphenidate (Focalin)
AmphetamineBlocks reuptake AND ↑ presynaptic release- Dextroamphetamine (Dexedrine)
- Mixed Salts (Adderall)
- Lisdexamfetamine (Vyvanse)

Stimulant Mechanisms of Action on Dopamine Transporters

Adverse Effects & CIs - Handle With Care

  • Common Side Effects:

    • CNS: Insomnia, headache, irritability, nervousness.
    • GI: ↓ Appetite, weight loss, abdominal pain.
    • Monitor: Height & weight in children due to potential for growth suppression.
  • Cardiovascular ⚠️:

    • ↑ BP & HR.
    • ECG screening is debated but consider if positive personal/family history of cardiac disease.
  • Psychiatric:

    • New or worsened tics (motor or phonic).
    • May unmask or exacerbate psychosis/mania.
  • Contraindications:

    • Absolute:
      • Use with or within 14 days of MAOIs.
      • Symptomatic cardiovascular disease, hyperthyroidism, glaucoma.
      • History of psychosis or Tourette's syndrome.

Exam Favorite: Before starting stimulants, screen for personal and family history of sudden death, ventricular arrhythmia, and other significant cardiovascular conditions. An ECG is warranted for positive histories.

High‑Yield Points - ⚡ Biggest Takeaways

  • Stimulants (methylphenidate, amphetamines) are first-line for ADHD, acting by blocking dopamine (DA) and norepinephrine (NE) reuptake.
  • Most common side effects include insomnia, decreased appetite, and weight loss.
  • Monitor blood pressure and heart rate due to cardiovascular risk; consider a baseline EKG.
  • Can cause a temporary slowing of linear growth in children.
  • High potential for abuse and diversion (Schedule II drugs).
  • Contraindicated in patients with psychosis or severe cardiovascular disease.

Practice Questions: Stimulant medications

Test your understanding with these related questions

A 20-year-old college student presents to the emergency room complaining of insomnia for the past 48 hours. He explains that although his body feels tired, he is "full of energy and focus" after taking a certain drug an hour ago. He now wants to sleep because he is having hallucinations. His vital signs are T 100.0 F, HR 110 bpm, and BP of 150/120 mmHg. The patient states that he was recently diagnosed with "inattentiveness." Which of the following is the mechanism of action of the most likely drug causing the intoxication?

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Flashcards: Stimulant medications

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Attention-deficit hyperactivity disorder (ADHD) has an onset before age _____

TAP TO REVEAL ANSWER

Attention-deficit hyperactivity disorder (ADHD) has an onset before age _____

12

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