Stimulants:

Question 1

Caffeine:

Answer 1

-Natural stimulant
–>1,3,7-trimethylxanthine
-Metabolized by P450 CYP enzymes
-Easily crosses the BBB
–>CYP 1A2
Theophylline: Tea derivative
(1.3-dimethylxanthine)

• Caffeine acts as an adenosine antagonist
• Directly increases monoamine/ ACh release
• Inhibits phosphodiesterase which leads to increased cAMP
• 10g coffee= fatal (100 cups of coffee)

Question 2

Amphetamine:

Answer 2

-Synthetic stimulant 
T1/2= 20 hours
-Structurally similar to NE and DA
-Blocks the re-uptake of NE and DA 
-Inhibits MAO's at high concentrations (Can't break down DA and NE) 
-Direct agonist at NE receptors

Question 3

Methylphenidate:

Answer 3

-Used clinically
T1/2= 2 hours
-Neurochemically similar to amphetamine
-Blocks the re-uptake of NE and DA

Question 4

Atomoxetine:

Answer 4

• Used to treat ADHD
• Metabolized by CYP2D6 enzymes
• Inhibits NET, DAT and SERT
• NMDA receptor antagonist

Question 5

Modafinil:

Answer 5

Drug of choice in treating Narcolepsy
T1/2= 10-12 hours
-Promotes wakefulness (mechanisms of action remain unclear)
-Elevates hypothalamic histamine levels/ inhibits DA re-uptake

Question 6

Phentermine:

Answer 6

-Similar to amphetamine
T1/2= 2 hours (10 hours for sustained release)
-Promotes NE/ DA release
-Suppresses appetite through satiety centres in the hypothalamus
-Excreted unchanged by the kidneys
-Generally well tolerated

Question 7

Ephedrine:

Answer 7

-Sympathomimetic stimulant drug acting on the SNS
T1/2= 3-4 hours
-Directly increases activity of NE on adrenergic receptors

Question 8

AE’s of Amphetamines:

Answer 8

-Vertigo, Hypertension, Insomnia, Potential for Addiction, Nausea and Diarrhea

Question 9

Order of Steps in treating Narcolepsy:

Answer 9

-Methylphenidate was the drug of choice for treating narcolepsy (outdated)

1. Armodafinil (R- enantiomer of Modafinil)
   - Less likely to be abused
   - ->Dextoampthetamine and methylphenidate are often abused/ found on the street

Question 10

Drugs for treating ADHD:

Answer 10

Amphetamine- Dextroampetamine- Adderall 
Dexmethylphenidate- Focalin 
Methylphenidate- Ritalin 
Lisdexamfetamine- Vyvanse 
Dextroamphetamine- Dextrostat/ Dexedrine