Don’t Forget-What Information Will be Covered for EVERY Drug:

What is drug?

Why is it used?

How is it administered?

How much is used?

Metabolism?

Affects on the cell?

Addiction?

Benefits?

Harms?

Individual experience may vary

• Nicotine• Caffeine (it IS a drug!) Lesson 16 • Cocaine• Amphetamines• Ecstasy• Anti depressants

What is caffeine? Why is it used?Activity2

Alkaloid found in many plants, including coffee beans, cacao pods, kola nuts and tea leaves

Keeping us alert!!

What are some caffeine forms?

Justin from Lincoln Park, NJ

http://commons.wikimedia.org/wiki/File:Energy_drinks.jpg

Plen

tiful

in

grou

nd w

ater

!WHY?

How is caffeine administered? Activity 3

Parenteral or not?

Which has the highest caffeine dosage?

What about?

Why so little caffeine in chocolate!?

All are Xanthines

Caffeine Theobromine Theophylline

CH3 = methyl groupFor instance, arsenic is 25+ times more toxic if methylated!

Is there a lethal dosage of caffeine?

One caffeine death – 90 No-Doz pills (100mg each) approx = 250 cups coffee

No hard data on lethal dose, but seems to be about 10 g

How is Caffeine metabolized? Activity 4

http://apu.sfn.org/content/Publications/BrainBriefings/

CYP1A2

H

84% is paraxanthine- rest is theobromine and theophylline

Half life 3-7 hours

What happens to CYP1A2 as you continue to use caffeine day after day?

1. Your CYP2A1 gets used up2. Your CYP2A1 is produced in an

anticipatory way3. Your CYP2A1 works more and

more poorly4. You stop making CYP2A1

because your thrifty body realizes you’re drinking it instead

How does caffeine effect a cell? Activity 5

http://apu.sfn.org/content/Publications/BrainBriefings/

caffeine

adenosine

Adenosine receptors and alertness

Adenosine and alertness

caffeine

Excess RAS activity is

interpreted as stress

adenosine

Caffeine and alertness

STRETCH/POWER YOGA!!!

How does adenosine tell you when you’re sleepy?

Noon

Adenosine receptors

mostly unoccupied

8 pm

Adenosine receptors 60% full

Midnight

Adenosine receptors 90% full

Midnight (with caffeine)

Adenosine receptors filled with

caffeine, not adenosine

Caffeine works as a(n):

1. Receptor antagonist 2. Receptor agonist3. Adenosine catalyst4. Xanthine catalyst5. Reticular transporter

Is caffeine addictive? Activity 6

This excerpt is from DSM-IV, retrieved from http://www.behavenet.com/capsules/disorders/subdep.htm. Criteria for Substance Dependence

A maladaptive pattern of substance use, leading to clinically significant impairment or distress, as manifested by three (or more) of the following, occurring at any time in the same 12-month period: (1) tolerance, as defined by either of the following:

(a) a need for markedly increased amounts of the substance to achieve Intoxication or desired effect (b) markedly diminished effect with continued use of the same amount of the substance

(2) Withdrawal, as manifested by either of the following: (a) the characteristic withdrawal syndrome for the substance (refer to Criteria A and B of the criteria sets for Withdrawal from the specific substances) (b) the same (or a closely related) substance is taken to relieve or avoid withdrawal symptoms

(3) the substance is often taken in larger amounts or over a longer period than was intended (4) there is a persistent desire or unsuccessful efforts to cut down or control substance use (5) a great deal of time is spent in activities necessary to obtain the substance (e.g., visiting multiple doctors or driving long distances), use the substance (e.g., chain-smoking), or recover from its effects (6) important social, occupational, or recreational activities are given up or reduced because of substance use (7) the substance use is continued despite knowledge of having a persistent or recurrent physical or psychological problem that is likely to have been caused or exacerbated by the substance (e.g., current cocaine use despite recognition of cocaine-induced depression, or continued drinking despite recognition that an ulcer was made worse by alcohol consumption).

Is caffeine addictive?

tolerancereward

dependence

Adenosine is a dopamine receptor antagonist. Caffeine (double negative)…antagonist to the antagonist, therefore…

What genes influence caffeine habits?? Activity 9

Adenosine receptor

Binds caffeine as if it was adenosine – get the same response

PMID: 12825092

What genes influence caffeine side effects?

CYP1A2 metabolizes caffeine

CYP1A2

CYP1A2*1A = fast metabolizer alleleCYP1A2*1F = slow metabolizer allele

*1F allele (hetero or homozygous), who also consumes caffeine, has 36% increased risk of heart attack (2-3 cups a day)PMID: 16522833

The latest in benefits (and harms):

• On electronic device/computer, go to the following website: www.sciencenews.org/highschools/login

• 2. Enter the following (case sensitive): • Username: STADIUM-WA• Password: 7jv35ZFc33• Tracking Code: STADIUM-243• Keep this information somewhere accessible for future

projects.• • 3. Search for the following article: The Beneficial Bean

(10/3/15) Read and take notes. Question on Final.

Which of these groups SHOULD use caffeine regularly?

1. Families prone to strokes.2. Families with Alzheimer’s.3. People prone to addiction.4. Families who also use nicotine.5. Women who are pregnant.

Caffeine benefits (besides alertness)? Activity 7

http://static.howstuffworks.com/

PMID: 12629235

PMID: 12099922

PMID: 12099922

What are caffeine Risks? Activity 8

Michael Malta

http://www.fanatikriders.com/

~75% as addictive as

nicotine

PMID: 16207803

Wired!

Interesting contradictions about caffeine and cardiovascular health

43% increased risk (men)

PMID: 15333732PMID: 14747639

14

20

25% reduced risk (women)