IntroductionCaffeine is a bitter white crystalline compound that acts as a psychoactive stimulant drug and a mild urination stimulant in humans and other animals. Caffeine was discovered by a German chemist, Friedrich Ferdinand Runge, in 1819. The word "Caffeine" comes from the term "kaffein," a chemical compound in coffee. Caffeine has another name such as guaranine when found in guarana, mateine when found in mate, and theine when found in tea; all of these names are synonyms for the same chemical compound.
Caffeine can be found in the beans, leaves, and fruit in many plants such as coffee beans, cocoa, tea leaves, kola nut, and meta leaves. It acts as a natural pesticide that paralyzes and kills certain insects feeding on the plants. It is most commonly consumed by human from coffee, tea, soft drink and energy drinks. In human body, caffeine acts as a psychoactive drug that induces self alertness. A psychoactive drug is a chemical substance that acts primarily upon the central nervous system where it alters brain function, resulting in temporary changes in perception, mood, consciousness and behavior. In North America, 90% of adults consume caffeine daily. Caffeine is the most legal and unregulated drug among other drugs. The U.S. Food and Drug Administration lists caffeine as a "Multiple Purpose Generally Recognized as Safe Food Substance".
History of CaffeineHumans have consumed caffeine since Stone Age. Early human found that chewing the seeds, bark, or leaves of certain plants had the effects of easing fatigue, stimulating awareness, and elevating mood. Later then they found that the effect of caffeine was increased by steeping such plants in hot water. Many cultures have legends that attribute the discovery of such plants to people living many thousands of years ago. According to one popular Chinese legend, the Emperor of China Shennong, said to have reigned in about 3,000 BCE, accidentally discovered that when some leaves fell into boiling water, a fragrant and restorative drink resulted. Shennong is also mentioned in Lu Yu's Cha Jing, a famous early work on the subject of tea. The history of coffee has been recorded as far back as the ninth century. During that time, coffee beans were available only in their native habitat, Ethiopia. A popular legend traces its discovery to a goat herder named Kaldi, who observed his goats that became sleepless at night after eating some coffee shrubs and. He then tried some of the berries that the goats had been eating, and the experienced the same sleepless vitality. In around the end of 16th century, coffee came into general use in the Near East (Asian Region). In Europe, coffee was known as "Arabian wine". The first few Coffee Houses were opened in Constantinople and Venice. In Britain, the first coffee houses were opened in London in 1652, at St Michael's Alley, Cornhill. They soon became popular throughout Western Europe, and played a significant role in social relations in the 17th and 18th centuries. Kola nut was chewed in many West African cultures, individually or in a social setting, to help reducing hunger. The earliest use of cocoa was discovered by the founding of an ancient Mayan pot dated to 600 BCE. In the New World, chocolate was consumed in a bitter and spicy drink called xocoatl. Xocoatl was believed to fight fatigue. Cocoa beans were used as currency during ancient times. Chocolate was introduced to Europe by the Spaniards and became a popular beverage by 1700. They also introduced the cacao tree into the West Indies and the Philippines. Caffeine has become the world's most popular psychoactive substance with global consumptions of 120,000 tons per annum.
Mechanism of Caffeine Action
Caffeine is complete;y absorbed by the stomach within 45 minutes of intake. Then, it is distributed throughout all tissues of the body and then is eliminited. The half-life of caffeine—the time required for the body to eliminate one-half of the total amount of caffeine consumed at a given time—varies widely among individuals according to such factors as age, liver function, pregnancy, some concurrent medications, and the level of enzymes in the liver needed for caffeine metabolism. In healthy adults, caffeine's half-life is approximately 3–4 hours. In women taking oral contraceptives (some sort of medication to counter pregnancy), the caffeine’s half-life is increased to 5–10 hours, and in pregnant women the half-life is about 9–11 hours. Caffeine can accumulate in individuals with severe liver disease when its half-life can increase to 96 hours. In infants and young children, the half-life may be longer than in adults; half-life in a newborn baby may be as long as 30 hours. Other factors such as smoking can shorten caffeine's half-life. Caffeine is metabolized in the liver by the cytochrome P450 oxidase enzyme system (specifically, the 1A2 isozyme) into three metabolic dimethylxanthines, which each have their own effects on the body:
Paraxanthine (84%): Has the effect of increasing lipolysis, leading to elevated glycerol and free fatty acid levels in the blood plasma.
Theobromine (12%): Dilates blood vessels and increases urine volume. Theobromine is also the principal alkaloid in cocoa, and therefore chocolate.
Theophylline (4%): Relaxes smooth muscles of the bronchi, and is used to treat asthma. The therapeutic dose of theophylline, however, is many times greater than the levels attained from caffeine metabolism.
Each of these metabolites is further metabolized and then excreted in the urine.
The precise amount of caffeine necessary to produce effects varies from person to person depending on body size and degree of tolerance to caffeine. Each person has different amount of caffeine intake that they can accommodate with. It takes less than an hour for caffeine to begin affecting the body and a mild dose wears off in three to four hours. Consumption of caffeine does not eliminate the need for sleep: it only temporarily reduces the sensation of being tired. Caffeine is an ergogenic; an external source that affect the brain and physical performance. Caffeine increases the capacity for mental or physical labor. Some studies show that trained runners showed a 44% increase in "race-pace" endurance, as well as a 51% increase in cycling endurance, after a dosage of 9 milligrams of caffeine per kilogram of body weight.
Because caffeine is primarily an antagonist of the central nervous system's receptors for the neurotransmitter adenosine, the bodies of individuals who regularly consume caffeine adapt to the continual presence of the drug by substantially increasing the number of adenosine receptors in the central nervous system. This increase in the number of the adenosine receptors makes the body much more sensitive to adenosine, with two primary consequences. First, the stimulatory effects of caffeine are substantially reduced, a phenomenon known as a tolerance adaptation. Second, because these adaptive responses to caffeine make individuals much more sensitive to adenosine, a reduction in caffeine intake will effectively increase the normal physiological effects of adenosine, resulting in unwelcome withdrawal symptoms in tolerant users. In much simpler way of describing this; caffeine is not addictive if consumed infrequently, regularly and in small amounts. However, caffeine can be addictive if taken very frequently in an amount that a normal people would not take.
Effect of Caffeine Intake and Overuse of CaffeineIn large amounts, and especially over extended periods of time, caffeine can lead to a condition known as caffeinism. Caffeinism usually combines caffeine dependency with a wide range of unpleasant physical and mental conditions including nervousness, irritability, anxiety, tremulousness, muscle twitching (hyperreflexia), insomnia, headaches, respiratory alkalosis and heart palpitations. Furthermore, because caffeine increases the production of stomach acid, high usage over time can lead to peptic ulcers, erosive esophagitis, and gastroesophageal reflux disease. (I don’t really know this kinda stuff).
There are four caffeine-induced psychiatric disorders recognized by the Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition: caffeine intoxication, caffeine-induced anxiety disorder, caffeine-induced sleep disorder, and caffeine-related disorder not otherwise specified (NOS).
Caffeine intoxicationAn acute overdose of caffeine, usually in excess of 300 milligrams, can result in a state of central nervous system over-stimulation called caffeine intoxication. The symptoms of caffeine intoxication may include restlessness, nervousness, excitement, insomnia, flushing of the face, increased urination, gastrointestinal disturbance, muscle twitching, a rambling flow of thought and speech, irritability, irregular or rapid heart beat, and psychomotor agitation. In cases of much larger overdoses mania, depression, lapses in judgment, disorientation, and loss of social inhibition, delusions, hallucinations, psychosis, rhabdomyolysis, and death may occur. In cases of extreme overdose, death can result.
Anxiety and sleep disorders
Long-term overuse of caffeine can bring out a number of psychiatric disturbances. Two such disorders recognized by the American Psychiatric Association (APA) are caffeine-induced sleep disorder and caffeine-induced anxiety disorder.
In the case of caffeine-induced sleep disorder, an individual regularly consumes high doses of caffeine sufficient to induce a significant disturbance in his or her sleep.
Parkinson's diseaseSeveral large studies have shown that caffeine intake is associated with a reduced risk of developing Parkinson's disease (PD) in men, but studies in women have been inconclusive. The mechanism by which caffeine affects PD remains a mystery. In animal models, researchers have shown that caffeine can prevent the loss of dopamine-producing nerve cells seen in Parkinson's disease, but researchers still do not know how this occurs.
Effects on memory and learningCaffeine can induce certain changes in memory and learning. However, it is still not definitely clear whether the effect is negative or positive.
Effects on the heartCaffeine increases the levels of cAMP in the heart cells, mimicking the effects of epinephrine. cAMP diffuses through the cell and acts as a "secondary messenger," activating protein kinase A (PKA; cAMP-dependent protein kinase). According to one study, caffeine, in the form of coffee, significantly reduces the risk of heart disease in epidemiological studies. However, the protective effect was found only in participants who were not severely hypertensive (i.e. patients that are not suffering from a very high blood pressure). Furthermore, no significant protective effect was found in participants aged less than 65 years or in cerebrovascular disease mortality for those aged equal or more than 65 years
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Effects on children
It is commonly believed that caffeine consumption causes stunted growth in children, but this is not supported by scientific research. However, just as with adults, there may be legitimate reason to limit the amount consumed by children.
Caffeine intake during pregnancy
The Food Standards Agency has recommended that pregnant women should limit their caffeine intake to less than 300 mg of caffeine a day – the equivalent of four cups of coffee a day. A higher intake may be associated with miscarriage.

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