A Small Dose of Caffeine

An Introduction To The
Health Effects of Caffeine

A Small Dose of Caffeine – 04/22/10

 What Is This?
O
CH3
CH3
N
N 7
1

3
O N
N
CH3
A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10
Caffeine – 1,3,7 Trimethylxanthine

O
CH3
CH3
N
N 7
1

3
O N
N
CH3
A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10
 History of Coffee
Date Event
~850 - Coffee beans discovered - The fable says that an Ethiopian goat
or sheepherder noticed that the goats were more alter after
eating the wild berries. He then sampled this new delicacy.
~1100 - First coffee trees and roasting of coffee beans.
1475 - Constantinople – the world’s first coffee house.
1600s - Coffee enters Europe and moves quickly to the Americas
1700s - Coffee house open throughout Europe.
1723 - First coffee plants are introduced into the Americas.
1822 - First espresso machine is created in France.
1938 - First instant coffee invented by the Nestlé company.
1971 - Starbucks opens its first location in Seattle, Washington's Pike
Place Market.
A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10
 Caffeine & Money

The coffee and cola industries owe

their wealth to the physiological
properties of the drug caffeine.

S.G. Gilbert (2001)

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 History of Tea
Date Event
3000 B.C. - Tea discovered in China or introduced form India
350 B.C. - First written description of Tea drinking in China.
450 A.D. - Turkish traders bargain for Tea and the Silk road is born.
800 - Tea introduced to Japan.
1450 - Japanese Tea ceremony created and popularized
1610 - Dutch bring Tea to Europe
1773 - Boston Tea party, rebellion against England’s tea tax
1776 - England sends first Opium to China to help pay for tea.
1835 - First experimental tea plantations in Assam, India.
1908 - Tea bags invented in New York.

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 History of Chocolate
Date Event
400 B.C. - Olmec people of Mexico made chocolate drinks
250 A.D. - Mayans of Mexico were cultivating cocoa crops
1528 - Cocoa was brought to Spain by Hernando Cortés
1600s - Chocolate drinks introduced into Europe
1657 - First English chocolate houses open
1828 - Screw press that extracted the cocoa butter from the
beans invented in Holland
1840s - Chocolate as solid developed

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Quote – Lovers of Coffee

Coffee
Black as hell, strong as death,
sweet as love.
Turkish proverb.

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Quote – Fear of Coffee

"Often coffee drinkers, finding

the drug to be unpleasant, turn
to other narcotics, of which
opium and alcohol are most
common.“

Morphinism and Narcomanias from Other

Drugs (1902) by T. D. Crothers, M.D.
A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10
 Quote – Love of Tea

“Tea, though ridiculed by those who

are naturally coarse in their nervous
sensibilities … will always be the
favorite beverage of the intellectual.”

Thomas De Quincey (1785–1859), English

author. Confessions of an English Opium-
Eater,“The Pleasures of Opium” (1822).

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Quote – Religion and Drugs

If Christianity is wine, and Islam

coffee, Buddhism is most
certainly tea.

Alan Watts, The Way of Zen, 1957

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Historical Events

Tea trade and opium

Opium War of 1839-42
Great Britain has a monopoly on the sale of
opium which it forces on China; eventually
gaining control of Hong Kong.

Consider our societies ongoing “war on

drugs”.

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Caffeine and Society

 Most widely consumed

stimulant drug in the world
 Many people start consuming
caffeine at an early age
 A great deal of money is made
from caffeine – why?

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Exposure

Most widely consumed

neuroactive compound
Coffee
Soda Products
Tea
Chocolate
A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10
 Caffeine Content

1 Cup of coffee – 65-175 mg

1 Cup of tea – 50 mg
Can of soda (12 oz) – 40-50 mg
Bar of chocolate (30 g) – 1-35 mg

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Exposure and Effects

Have you every drank

too much caffeine?

What are the effects?

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Aspects of Caffeine
Desirable effects
Stimulant, increased alertness, concentrate, energy,
bronchial dilator

Toxicity
Restlessness, jitters, anxiety, insomnia, elevated or irregular
heart rate

No tolerance
Most develop little or no tolerance to the nervous system
effects

Withdrawal effects
Transient but persistent, headache, low energy, in ability to
concentrate
A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10
 Absorption

Rapidly absorbed following

oral consumption

Peak blood (plasma) levels

usually with 30 minutes

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Distribution

Distributes into all body

compartments –
Pass easily into brain, breast
milk and crosses placenta

Does not accumulate

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10
 Metabolism/Elimination

 Metabolized in the liver

 Changed to di- and mon-
methylxanthines
 Excreted in the urine

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Half-life
How long it takes to leave the body

Average adult – 3-5 hrs

Child less that 6 months – 24 hrs
Pregnant – 7-8 hrs
Smoker – 2-3 hrs

Varies between individuals

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

Theophylline – 1,3 Dimethylxanthine

O
H
CH3
N
N 7
1

3
O N
N
CH3
A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10
 Mechanism Of Action

Blocks Adenosine receptor

Adenosine is a calming
neurotransmitter

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Parents Of Caffeine
PURINE XANTHINE
O
H
H
N H N
N 7 N 7
1 1

3 3 N
N O
N N
H

Parent of compounds Dioxypurine - Parent

found in RNA & DNA methylxanthines

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Normal Action of Adenosine

Adenosine
1 Adenosine
Receptor

Outside Cell
Cell
2 Membrane Inside Cell

Adenosine binds to receptor

Signal Protein 3

Positive Response
Calming effect

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Action of Caffeine

Caffeine
1
Adenosine
Receptor

2 Caffeine
inactivates
receptor
3 Adenosine
can not bind

Caffeine

No Response
Resulting in Stimulation

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

Why so many $$s from caffeine?

1. Pleasant stimulant effects

2. Short Half-life (you need to
back for more)
3. Can’t drink too much at any
one time (toxicity)
4. Headache when you stop
drinking it

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 A Small Dose of ™ Caffeine

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Additional Information

 Web Sites
• England – Department of Health – Statement on
the reproductive effects of caffeine. Online.
<http://www.doh.gov.uk/sacn/pdf/200106caffeine.
pdf> (accessed: 2 April 2003).
• U.S. Food and Drug Administration (FDA) -
Perplexities Of Pregnancy. Online.
<http://www.cfsan.fda.gov/~dms/wh-preg2.html>
(accessed: 9 April 2003).
• Caffeine – The Vaults of Erowid. Online.
<http://www.erowid.org/chemicals/caffeine/caffei
ne.shtml> (accessed: 2 April 2003).

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Authorship Information

This presentation is supplement to

“A Small Dose of Toxicology”

For Additional Information Contact

Steven G. Gilbert, PhD, DABT
E-mail: smdose@asmalldoseof.org
Web: www.asmalldoseof.org

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10

 Xanthine
O
H
H N
N 7
1

3 N
O N
H
A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10
 Purine

H
N
N 7
1

3 N
N

A Small Dose of Toxicology A Small Dose of Caffeine – 04/22/10