Nikki, Bryan, Kyla

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Nov 12, 2013 (3 years and 4 months ago)


Nikki, Bryan, Kyla


Caffeine is one of the most widely used
drugs in the world.

It is estimated that ______% of adults
in the United States regularly drink
caffeinated beverages.

It has also been estimated that the
average adult caffeine intake in the
United States is 200 to 400 mg per day.

Caffeine can be found in all sorts of
things like coffee, energy drinks, soft
drinks, chocolate, migraine medicine,
tea, dietary supplements, etc.

Caffeine is normally consumed orally
through the beverages or food in which
it is present.


Caffeine is a psychoactive drug that acts as a
CNS stimulant

Its chemical name is 1,3,7

Its generic name is Caffeine

Some brand names are_______________

Primary Uses

Caffeine has many uses

It does not affect all people in the same way

Most people who do consume caffeine do so on regular basis

Athletes use caffeine to improve their performance and be
on top of their game

_________ sufferers use caffeine to alleviate their pain

Night shift employees or truck drivers may use it to make
fewer mistakes as a result of being tired or to increase
alertness during sleep deprivation

Students may use caffeine to stay up late studying

It is primarily used as a mild CNS stimulant to aid in staying
awake and restore mental alertness

Behavioral Effects

There are numerous behavioral effects for primary use and
some major side effects

Studies demonstrated _________ effects in rodents

At low doses it had stimulant effects

At high doses rodents showed reduced activity levels.

Humans do not show behavioral depression but they do
experience tension and anxiety at higher doses

Caffeine does more than just increase arousal. There are a
variety of positive subjective effects, such as:

Feelings of well
being, enhanced energy or vigor, increased
alertness and ability to concentrate, self
confidence, increased
work motivation, enhanced sociability, and reduced tension

Undesirable Side Effects

There are multiple unwanted or undesirable side effects as
well, such as:

increased blood pressure and respiration rate, enhanced water
excretion, etc.

Caffeine has a positive ionotropic effect on the myocardium
and chronotropic effect on the sinoatrial node

Results in a transient increase in heart rate, force of contraction,
and cardiac output

Some additional side effects are as follows but not limited
to; nervousness, insomnia, restlessness, irritability,
confusion, agitation, delirium, twitching, tremors,
convulsions, tingling of face, flushing, palpitation, nausea,
vomiting, epigastric discomfort, gastric irritation, diarrhea,

Background and History of Coffee

, a coffee plant with berries

Arabian tale about Kaldi and his goats

This shows early evidence that coffee provides energy

They think that coffee crossed the Red Sea early in its
history, as early as A.D. 575

It arrived in England in the early 1600s as a medicine

First English coffeehouse opened in Oxford in 1650,
and others soon after in London

There was some time of political turmoil

It has been said that “England’s great struggle for political
liberty was fought and won in the coffeehouse

Background and History of Coffee

By 1690, coffeehouses were firmly established
in English life

Helped reduce drunkenness during the gin
epidemic in the early 1700s

However, coffee consumption decreased from
3.1 cups a day for adults in 1960 to only 1.75
cups per day in 1991

People were trying to be more health conscious

Mechanisms of Action

The mechanisms of action, neurotransmitter systems, and the
receptor subtypes are not completely clear, but much progress has
been made with time

Caffeine is rapidly absorbed

Reaches peak concentration within ______ minutes.

It is water
soluble and lipid
soluble, which allows it to cross the BBB

It has a wide distribution and an almost immediate effect on

Originally it was thought that it directly influenced catecholamine
systems, and that it was an inhibitor of cAMP phosphodiesterase. It
was thought that it blocked GABA(A) receptors and that it
stimulated CA++ release within cells

Mechanisms of Action

More recent studies have led us to believe that it
actually blocks A1 and _____ receptors for adenosine

Adenosine plays a role in energy via adenosine
triphosphate (ATP)

Adenosine in the brain can serve a neurotransmitter
like function

Caffeine reduces the effects of adenosine by binding to
adenosine receptors, but not activating them

There are four different adenosine receptor subtypes
A1, A2A, A2B, and A3

Mechanisms of Action

Caffeine is thought to block A1 and A2A receptor subtypes
in laboratory animals

These receptor subtypes are thought to mediate most of the
behavioral effects of caffeine

A1 and A2A receptors

A1 receptors thought to inhibit calcium uptake

A2A receptors are thought to play a role in behavioral control
and interact with the _____ system

_____ system is intertwined with reward and arousal

Growing evidence from animal studies demonstrate that
adenosine is a sleep

or drowsiness

inducing factor
released after a period of waking

Explains why caffeine use in humans causes increased alertness
and suppression of sleep

Absorption and Metabolism

There are several factors related to route of administration,
absorption, distribution, and fate

Caffeine is rapidly absorbed. It is actually peaks 15
minutes after administration

It is widely distributed throughout the body, and
metabolized in the liver

Metabolites account for almost all caffeine excretion

Only 1 to 2% is excreted unchanged

In humans approximately ____% of caffeine metabolites
are eliminated through urine, 2
5% through feces, and the
remainder through body fluids like saliva

Metabolism is influenced by prior ingestion of caffeine,
gender, smoking status, and other drugs

Interactions With Other Drugs

Cigarette smoke used repeatedly causes an
increase in a liver enzyme known as

This speeds up the rate of
biotransformation/metabolism of caffeine

People who are heavy smokers may need higher
doses of caffeine, because it is metabolized by the
same enzyme

Caffeine also interacts with other drugs

It increases the effects of cimetidine and
theophylline toxicity

Half Life

Caffeine’s half
life is _____ hours in adults

The half life in neonates ranges from 36 to 144

It is also excreted in small amounts in the breast

Caffeine is classified as a FDA pregnancy
category B, meaning it freely crosses the

Caffeine Tolerance

Regular caffeine use can lead to tolerance to
some of caffeine’s subjective effects as well as
disrupt sleep

Chronic caffeine use can produce tolerance to the
cardiovascular and respiratory effects of the drug

Some withdrawal symptoms are:

Headache, lethargy, fatigue, impaired concentration,
impaired psychomotor performance, and in some
cases mild anxiety or depression

Physiological Effects

Heavy coffee drinking has been linked with
increased blood pressure and a heightened
risk of coronary heart disease

High caffeine consumption has also been
reported to be associated with low infant birth

Other Effects

Chronic ingestion of excessive amounts of caffeine can lead
to a syndrome called ____________.

Caffeinism is characterized by restlessness, nervousness,
insomnia, and physiological disturbances, such as
tachycardia and gastrointestinal upset.

Extremely high doses of caffeine may produce even more
severe psychiatric effects.

Caffeine consumption causes physical dependence and can
also lead to a compulsive use pattern.

Caffeine is reinforcing to regular users. Caffeine
reinforcement is related to a combination of functional
enhancement and relief from withdrawal symptoms.


Components Model of Addiction (Griffiths)


Mood Modification?







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