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Caffeine (1,3,7-trimethyl-1H-purine-2,6(3H,7H)-dione) is the world's most widely used ergogenic (external influences that positively affect mental or physical performance) pharmacological aid. Caffeine has been used for over 5,000 years, dating back to when the Chinese first discovered tea. Today, the substance is primarily consumed in the form of coffee and other beverages. Caffeine is found in coffee beans, the tea bush, the kola nut, guarana berries, yerba mate, and cocoa. Caffeine is commonly used in pill form (NoDoz), is sometimes used in combination with over-the-counter pain relief medication (Excedrin), and has recently been incorporated into the growing market of energy drinks (Red Bull, Monster). Historically, the stimulant has been used to increase alertness and reduce physical fatigue; however, more research is being done to elucidate the effects of caffeine on athletic performance.

The effective ergogenic dose of caffeine has been reported to be 3 to 9 milligrams/kilogram (mg/kg) of body weight. Caffeine is primarily absorbed in the stomach and small intestine and has peak blood concentrations at about 45 minutes after intake. The chemical is distributed throughout all tissues of the body and is capable of crossing the blood-brain barrier. In healthy adults, caffeine has a half-life of about 3 to 4 hours. However, oral contraceptives, pregnancy, and liver failure can extend the half-life substantially. Caffeine is metabolized in the liver by a cytochrome P450 oxidase enzyme system (1A2). The three metabolic by-products, paraxanthine (80%), theobromine (10%), and theophylline (4%), have various effects on the body. These metabolites are broken down and excreted in the urine.

General Cardiovascular Effects

Caffeine and its metabolites have effects on the cardiovascular system that are thought to enhance athletic performance. Theobromine is a vasodilator that helps increase oxygen and nutrient delivery to muscle and brain tissues. Theophylline increases heart rate and heart contractility and, therefore, increases cardiac output (the amount of volume pumped by the heart per unit time). Large overdoses of caffeine can create cardiac complications, including heart palpitations and heart attack.

General Respiratory Effects

In addition to the vascular effects, caffeine also contributes to an increase in respiratory function. Theophylline acts as a smooth muscle relaxant of the bronchioles and, thus, increases lung ventilation and oxygen saturation. Caffeine is being researched as a potential drug for use in athletes with exercise-induced asthma. Caffeine is also thought to stimulate the respiratory center of the medulla and, thus, increase the ventilation rate. Caffeine can therefore increase respiratory readiness and prepare the body for athletic activity by increasing overall blood oxygen concentrations.

Dehydration and Renal Effects

One of the common worries about the consumption of caffeine is dehydration. While caffeine has shown mild diuretic (water excretion) effects on the kidney, consuming caffeinated beverages does not show a significant increase in overall fluid loss in a 24-hour period. Therefore, athletes should not increase their fluid intake when using moderate amounts of caffeine (<456 mg). However, when large ergogenic doses are taken, the risk of fluid loss is higher, and more water should be consumed to prevent hypovolemia (a drop in blood pressure). Regardless of caffeine intake, athletes should always monitor fluid intake during heavy training regimens.

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