Stimulants

Question 1

Amphetamine - MOA?

Answer 1

Stimulates the release of NE, DA, & 5HT from storage vesicles in presynaptic terminals

Question 2

Which of the 2 Amphetamine enantiomers are more potent?

Answer 2

D-isomer is ~4x more potent than the L-isomer

Benzedrine = Mix of L- & D-isomers
Dexedrine = D-isomer only

Question 3

What receptors are activated by small doses of Amphetamine vs. higher doses?

Answer 3

Small doses activate β-1 receptors

Higher doses activate both α- & β-receptors

(in general, amphetamine is a “dirty” drug, causing activation of α-1, α-2-, β-1-, and β-2 receptors)

Question 4

Amphetamine - CV effects?

Answer 4

↑HR (β-1)
&
↑BP (β-1 & α-1)

Question 5

Describe the dose-dependent effects of Amphetamine on neurotransmitters.

Answer 5

Lower doses = release NE & DA

Higher doses also cause release of 5HT

Question 6

Methamphetamine - MOA?

Answer 6

• Stimulates the release of NE, DA, & 5HT from storage vesicles in presynaptic terminals
• Also inhibits their reuptake
• Greater selectivity for CNS than amphetamine (overall more potent & addictive)

Question 7

Chronic methamphetamine use may cause damage to _____ neurons, leading to psychosis and/or Parkinson disease.

Answer 7

dopaminergic

Question 8

Of the stimulants, which is the most highly addictive?

Answer 8

Methamphetamine

Question 9

Top 3 indications that stimulants are used for?

Answer 9

• ADHD
• narcolepsy
• providing “increased energy” in the elderly