Chapter 18 & 20: Stimulants and Obesity

Question 1

What is Caffeine?

Answer 1

Caffeine was first isolated from coffee in 1819
Caffeine is a CNS stimulant, World’s most popular drug

Caffeine: naturally in products such as coffee, tea, chocolate and cola soft drinks; variety of prescription and over-the-counter medications, cough, cold and pain remedies, Energy drinks may contain both naturally occurring and added caffeine.

Question 2

Explain Caffeine structure and its metabolism?

Answer 2

• Xanthine molecule + 3 methyl groups
• Metabolized (demethylated) by Liver CYP450 (CYP1A2):
• Plasma T1/2 is about 6 hours
• Metabolites excreted in Urine

Question 3

Explain Caffeine Pharmacodynamics?

Answer 3

• both water & lipid soluble so **easily crosses the BBB **
• Adenosine receptor antagonist (indirectly increases monoamine/acetylcholine release)
• Inhibits phosphodiesterase which leads to increased cAMP (similar to β-adrenergic receptors)

Question 4

How much Caffeine does it take to become toxic?

Answer 4

1 cup of coffee contains 100-200 mg caffeine

1.5 g (12-15 cups) → anxiety, shakiness (tremor)

10 g of Caffeine is lethal **(100 cups of coffee!)
**

Question 5

What stimulant is this?

Answer 5

Amphetamine

Question 6

What stimulant is this?

Answer 6

Methylphenidate

Question 7

What stimulant is this?

Answer 7

Atomoxetine

Question 8

What stimulant is this?

Answer 8

Modafinil

Question 9

What stimulant is this?

Answer 9

Phentermine

Question 10

What stimulant is this?

Answer 10

Ephedrine

Question 11

What are the adverse effects of stimulants?

Answer 11

Question 12

What is ADHD?

Answer 12

Question 13

What is the treatment for ADHD?

Answer 13

Medication and Behavioral Treatment

Stimulants most commonly used ADHD Drug - Provides Calming effect.

Amphetamine-Dextroamphetmaine

Dextroamphetamine

MethylPhenidate

Question 14

What is Narcolepsy?

Answer 14

Liked to Reduced hypocretin/orexin in the hypothalamus; Possible Autoimmune targeting hypocretin (H1N1 Vaccinations?)

Characterized By:

• Sleep attacks: enter REM sleep almost instantly (during day)
• Excessive daytime sleepiness (EDS)
• Hallucinations as falling asleep or waking up
• loss of muscle tone occurs without loss of consciousness in response to strong emotions (cataplexy)

Affects 0.3 - 0.5 % of population.

Question 15

What is the treatment for Narcolepsy?

Answer 15

Armodafinil - Tried first, Less likely to be abused than other stimulants.

Dextroamphetamine
Methylphenidate