Whenever they went, however, the European explorers from Columbus
onward found other mind-affecting drugs, and brought then home with them.
Tobacco was discovered on Columbus's first voyage. Cocaine was found in large
areas of South America. Caffeine and LSD-like drugs were found scattered all
over the world. During the next two centuries, the Europeans not only adopted
nicotine and caffeine but spread them everywhere. They also imported opium.
In a remarkably short space of time, western Europe was converted from an
alcohol-like culture to a multidrug culture.
The introduction of caffeine drinks into countries that had not
previously known them - like the introduction of other exotic drugs such
as nicotine and marijuana - aroused a sense of deep moral outrage and evoked
efforts to repress the new drugs. The Mohammedans of Arabia, for example,
first used the newly introduced coffee to help them stay awake during prolonged
religious vigils. This "use as a devotional antisporific" stirred up fierce
opposition on the part of the strictly orthodox and conservative section
of the priests. Coffee to them was held to be an intoxicating beverage, and
therefore prohibited by the Koran, and severe penalties were threatened
to those addicted to its use. An early Arabian writer summed up: "The sale
of coffee has been forbidden. The vessels used for this beverage... have
been broken to pieces. The dealers in coffee have received the bastinado,
and have undergone other ill-treatment without even a plausible excuse; they
have been punished by loss of their money. The husks of the plant... have
been more than once devoted to the flames, and in several instances persons
making use of it... have been severely handled." "Notwithstanding threats
of divine retribution and other devices", however, the coffee-drinking habit
spread among the Arabian Mohammedans, and the growth of coffee and its use
as a national beverage became as inseparably connected with Arabia as tea
is with China.
Dr. Robert S. de Ropp notes that when coffee was introduced into
Egypt in the sixteenth century, "the coffee bugaboo'... caused almost as
much fuss as the 'marijuana bugaboo' in contemporary North America. Sale of
coffee was prohibited; wherever stocks of coffee were found they were burned...All
this fuss only had the result of interesting more people in the brew and
its use spread rapidly."
In Europe, too, coffee became a popular drink despite (or perhaps
because of) efforts at repressions and medical warnings. Yet, caffeine can
be a dangerous drug. Contemporary scientists echo several of the early allegations
made against caffeine. A reliable summary of current scientific opinion
can be found in any modern pharmacological text. These texts should review
both the desirable and hazardous effects of the caffeine found in coffee,
tea, cocoa, cola drinks, and other popular drinks.
The desirable effects are remarkably similar to those of cocaine
and the amphetamines. Caffeine stimulates all portions of the cerebral cortex.
Its main action is to produce a more rapid and clearer flow of thought,
and to allay drowsiness and fatigue. After taking caffeine one is capable
of a greater sustained intellectual effort and a more perfect association
of ideas. There is also a keener appreciation of sensory stimuli, and reaction
time is diminished. This accounts for the hyperthesia, sometimes unpleasant,
which some people experience after drinking too much coffee. In addition,
motor activity is increased; typists, for example work faster and with fewer
errors. However, recently acquired motor skill in a task involving delicate
muscular coordination and accurate timing may..be adversely affected. These
effects may be brought on by the administration of 150 to 250 mg of caffeine,
the amount contained in one or two cups of coffee or tea.
In addition to its effects on the cerebral cortex and other portions
of the central nervous system, caffeine in modest doses (a few cupfuls of
coffee or tea) affects the heart rate, heart rhythm, blood vessel diameter,
coronary circulation, blood pressure, urination, and other physiological
functions. The secretion of gastric acids is stimulated, a matter of concern
in connection with peptic ulcers.
Is caffeine addicting? Opinions vary, depending on one's definition
of addiction. One feature of heroin addiction is tolerance, the gradual fading
of effects as the same dose is taken daily. An appreciable degree of tolerance
may develop to certain effects of caffeine.
Another feature of heroin addiction is the withdrawal syndrome
or physical tolerance. Caffeine unquestionably produces withdrawal symptoms
at some dosage levels. There is no doubt that the excitation of the CNS (central
nervous system) produced by large amounts of caffeine is followed by depression.
There has been considerable controversy, however, as to whether this is also
true after the mild physiological stimulation produced by the small amounts
contained in the average cup of tea or coffee. Findings from 1969 demonstrate
that physical dependence does occur with five or more cups of coffee a day.
When taken in very large doses, moreover, caffeine is a potent
poison. A fatal dose of caffeine given to an animal produces convulsions
because of the central stimulating effect. Early in the poisoning, these
are epileptiform in nature; as the actio of the drug on the spinal cord becomes
manifest, strychnine-like convulsions may appear. Death results from respiratory
failure. The fatal caffeine dose in man is estimated at 10 g. (70 to 100)
cups of coffee.
Even a single gram of caffeine (7 to 10 cups) produces acute
toxic effects. Insomnia, restlessness, and exfeine given to an animal produces
convulsions because of the central stimulating effect. Early in the poisoning,
these are epileptiform in nature; as the actio of the drug on the spinal
cord becomes manifest, strychnine-like convulsions may appear. Death results
from respiratory failure. The fatal caffeine dose in man is estimated at 10
g. (70 to 100) cups of coffee.
Even a single gram of caffeine (7 to 10 cups) produces acute
toxic effects. Insomnia, restlessness, and exe in tablet form is readily
available without a prescription at drugstores and some supermarkets throughout
this country. Sold under such trade names as NoDoz, it comes in 100 mg tablets
priced at about 75 cents for fifteen tablets. Many North American's use caffeine
in this concentrated form. How many, and how much of it they take at a time,
is unknown - but ten tablets contain a gram of caffeine, enough to produce
the symptoms of acute toxicity described above. Production of natural and
synthetic caffeine in the United States in 1963 was 2.3 million pounds valued
at $4,830,000. This amount is equivalent to over 10 billion, 100 mg does,
or about 55 per capita.
Thus we come to the coffee paradox. The question of how a drug
so fraught with potential hazard can be consumed in North America at the
rate of more than a hundred billion doses a year without doing intolerable
damage, and without arousing the kind of hostility, legal repression, and
social condemnation aroused by the illicit drugs.
The answer is quite simple. Coffee, tea, cocoa, and the cola
drinks have been domesticated. Caffeine has been incorporated into our way
of life in a manner that minimizes (though it does not altogether eliminate)
the hazards inherent in caffeine use. Instead of its being classified as
an illicit drug, thereby grossly amplifying caffeine's potential for harm,
ways to make caffeine safer have been searched for and found.
In the first place, people generally take caffeine in forms so
diluted as to make it unlikely that excessive doses, more than 300 to 400
mg at a sitting, will be ingested. The contrast here with alcohol is noteworthy.
Whisky, gin and other distilled spirits, in contrast to light wines and beer,
increase the likelihood that excessive amounts of alcohol will be ingested.
Again, coffee is customary served with cream or milk, which may
at least partially protect the lining of the stomach from the irritation
that caffeine might otherwise produce.
People have also developed the custom of drinking coffee and
tea after a meal, further protection for the stomach lining. Cocktails, in
contrast, are usually drunk before a meal, increasing the inherent hazards.
By keeping coffee legal, society has avoided extortionate black
market prices that might otherwise bankrupt coffee drinkers and lead them
into lives of crime. And coffee drinkers are not stigmatized as criminals,
driven into a deviant subculture with all that criminalization entails.
Caffeine is one of a large group of naturally occurring compounds
known as alkaloids, other examples being nicotine, cocaine, and morphine.
Most alkaloids show marked physiological activity, and crude extracts of
various alkaloid-bearing plants have been used since antiquity because of
their curative and poisonous effects. In fact it was the alkaloid oniine
contained in the hemlock extract which killed Socrates. Many alkaloids, however,
are of great value in medicine because of specific pharmacological actions.
Thus, morphine and some of its related compounds are the best known agents
for the relief of pain. The curare alkaloids produce paralysis of voluntary
muscles and often are used as an adjunct to anaesthesia in surgery. The belladonna
alkaloids prevent the normal response of smooth muscle to nervous impulses
and when placed in the eye cause dilation of the pupil (resulting in a softening
look of the eye, a cosmetic effect for which the belladonna alkaloids were
The first alkaloid, morphine, was discovered in 1804, and within
a few years it was recognized as the first member if a new class of substances,
originally called vegetable alkalies, and later alkaloids, meaning alkali-like,
since most alkaloids are basic. Today over 2000 alkaloids are known, extracted
from over 100 families of plants. Not all plants contain alkaloids - they
are found most frequently in the higher seed-bearing plants, and only very
rarely in the lower non-seed bearers. The function of the alkaloids in the
plant are still a subject of speculation. The alkaloids are generally concentrated
in the living tissue at points of intense cell activity, from which they
are often cast aside and stored in such dead tissues as the seed hulls or
outer bark. These facts have led to the view that the alkaloids are end products,
or by-products, of amino acid metabolism in plants. Other theories regard
the alkaloids as reserve materials stored for protein synthesis, protective
substances which discourage animals or insect attack, plant stimulants or
regulators similar to hormones, or detoxification products rendered harmless
by the plant's defense mechanisms.
Caffeine was first unambiguously isolated from coffee and named
by F.F. Runge in 1821. The same substance isolated from tea was known as
theine until it was shown to be identical to caffeine in 1838. In 1861 Adolf
Strecker correctly suggested that the molecular formula of caffeine was C8H10N4O2.
In 1882 Emil Fisher, later to become famous for his brilliant determination
of the structure of glucose, suggested a structure for caffeine which he
revised 15 years later to the correct form.
You may notice the similarity between caffeine and uric acid.
The isolation of caffeine from dried tea leaves provides a particularly
interesting and useful introduction to the principles and practise of extraction
in that use is made of both of the two basic forms: Solid-Liquid and Liquid-Liquid
By treatment of the solid tea leaves with hot water, caffeine
is extracted into the aqueous medium along with several other compounds
including related alkaloids and coloured tannins (glucose esters of phenolic
aromatic acids). Inclusion of calcium carbonate in the initial hot water
treatment precipitates the tannins as insoluble calcium salts which are
removed by filtration and discarded along with the residual tea leaves, thus
simplifying the subsequent isolation of the caffeine from the aqueous solution
by extraction with the solvent, chloroform. After the removal of the chloroform
solvent, the solid residue of crude caffeine is subjected to a final purification
In a 600 mL beaker, place 30 g of dry tea leaves, 300 mL of distilled
water and 15 g of powdered calcium carbonate. Add 2-3 boiling chips and boil
the mixture gently, with occasional stirring for 20 minutes over a wire gauze
During the heating periods, the following preparations for filtration
of the tea extract should be carried out. First, line the walls of a second
600 mL beaker with multilayered cheese cloth. This will be the primary filter.
Next prepare 2 or 3 long-necked filter funnels with fluted filter paper.
These will be the secondary filters.
When the heated solution is ready, let it cool until it is easily
handled, then pour it all in one pour into the cheese-cloth filter. Grab
the ends of the cheese cloth and squeeze the tea leaves to remove as much
water as possible. Discard your tea leaves but keep the cheese cloth.
Take your filtrate and start filtering it through the secondary
Transfer the cold filtrate to a 250 mL separatory funnel and
extract with three successive 30 mL portions of chloroform. Each extraction
must be done with care to avoid the formation of a tight emulsion. To minimize
emulsion formation, DO NOT SHAKE the contents of the separatory funnel vigorously,
but only GENTLY SWIRL the two immiscible layers together for a longer period
of time (eg. 5 minutes).
SOME EMULSIFICATION IS INEVITABLE! A BUBBLY FROTH WILL FORM IN
THE LOWER CHLOROFORM LAYER JUST BELOW THE WATER INTERFACE. DRAIN OFF THE
CLEAR CHLOROFORM INTO A 250 mL ERLENMEYER FLASK. ALLOW A FEW MINUTES FOR
MORE OF THE FROTH TO DISSIPATE. THIS IS USUALLY FACILITATED BY RAPIDLY ROTATING
THE STEM OF THE FUNNEL, BACKWARDS AND FORWARDS BETWEEN YOUR FINGERTIPS.
DRAIN OFF AS MUCH AS POSSIBLE OF THE REMAINING CHLOROFORM. TRANSFER OF A
SMALL AMOUNT OF FROTH IS OF LITTLE CONCERN BECAUSE IT WILL
BE REMOVED IN THE SUBSEQUENT FILTRATION.
Filter the chloroform extracts through a cotton wool plug in
a short stem funnel. Take the filtrate and in a water bath under the fume
hood evaporate the caffeine to dryness. (DO NOT BURN IT)
(TO SAVE ON TIME FILTER AND BEGIN EVAPORATING EACH 30 mL PORTION
AS IT IS OBTAINED!!!)
Dissolve the solid residue of crude caffeine (usually slightly
greenish in colour) in a minimum amount of boiling methanol (approximately
4-8 mLs will be required). Transfer the resultant solution to a small 25
mL Erlenmeyer flask by means of a small pipette. Cork the flask and allow
the solution to cool to room temperature. Complete the crystallization by
chilling the flask in an ice-bath. Collect the crystals of pure caffeine
by filtration and wash with one mL of ice cold methanol.
Weight the pure, recrystallized caffeine and calculate the percentage
caffeine contained in tea. Submit your sample of caffeine in a labelled baggie