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Flashcards in Stimulants Deck (8)
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1
Q

What are the ‘desired’ effects of sympathomimetics?

A
  • Decreased fatigue
  • Increased wakefulness, alertness, initiative, confidence, ability to concentrate, motor & speech activity
  • Improved simple activity and athletic performance

Organ effects:

  • Increased systolic and diastolic BP
  • High doses cause arrhythmias
  • Palpitations, anginal pain, circulatory collapse, & hyperthermia
2
Q

What are the CNS effects of sympathomimetics?

A

Acute: dizziness, agitation, confusion, insomnia, seizures

Chronic: amphetamine psychosis: vivid hallucinations, paranoid delusions and compulsions, marked weight loss, resolve in 7-10 days

3
Q

What is the mechanism of action of sympathomimetics (all the same except MDMA aka ecstasy)?

A

Low dose: Increased release of NE and DA
Medium dose: Blocks NE & DA reuptake
High dose: inhibits monoamine oxidase

Ecstasy: directly stimulates 5HT 21A receptors - binds to norepinephrine transporter protein. Added methyl group to increase lipophilicity and thus easier access to brain

4
Q

What are the pharmocokinetics of sympathomimetics?

A
  • Amphetamine and Methylphenidate: tolerance develops to effects on appetite and mood; abrupt withdrawal results in craving, prolonged sleep, fatigue, eating
  • Cocaine: withdrawal effects consistently occurs with cocaine little tolerance
  • MDMA (ecstasy): Stimulates release & inhibits reuptake of serotonin, epi, NE, and DA
5
Q

What are the sympathomimetics?

A
  • Amphetamine (Benzedrine)
  • Methylphenidate (Ritalin)
  • Cocaine
  • MDMA (ecstasy)
6
Q

Bath salts (mephedrone)

A
  • Act in brain as “cocaine substitutes”
  • Often contain various amphetamine like substances
  • High abuse and addiction liability
7
Q

What are the effects and mechanisms of Xanthines (caffeine and theophylline)?

A
  • Stimulate cortex: clearer though, less fatigue, increased dexterity
  • Medullary centers: stimulate respiratory & vasomotor center
  • Smooth muscle relaxant (decreased peripheral vascular resistance, increase cerebral vascular resistance)
  • Withdrawal: headache, irritibility, inability to concentrate, insomnia
  • theophylline higher potency than caffeine
  • LD50 of caffeine is 150-200 mg/kg ~80-100 cups of coffee
8
Q

What are the effects and mechanisms of eugeroics (Modafinil & armodafinl)?

A
  • Treats narcolepsy and shift work sleep disorder (promoted as wakefulness agent); effective for ADHD
  • CNS effects: headache, insomnia, dizziness, agitation, anxiety
  • Can cause nausea, lack of appetite, high BP, severe derm reactions
  • Elevates hypothalamic histamine levels, activates glut circuits, inhibits GABA transmission. Increases DA & NE