Caffeine is the world’s most widely consumed psychoactive substance, but unlike many others, it is legal and unregulated. Many consider it a drug of abuse.
The two brain functions most sensitive to caffeine are the neural structures regulating the sleep-wake cycle. The average daily dose of consumed caffeine is five to ten times higher than is necessary to stimulate the sleep-awake cycle. The most notable behavioral effects of caffeine occur after consumption of low to moderate doses (50-300 milligrams) and include increased alertness, energy, and ability to concentrate. Moderate caffeine consumption rarely leads to health risks. In contrast, higher doses of caffeine induce negative effects such as anxiety, restlessness, insomnia, and rapid heart rate. After sudden caffeine cessation, withdrawal symptoms may develop for a small portion of the population, but these symptoms are moderate and transient.
Classic psychoactive drugs, such as ampthetamines and cocaine cause dopamine release (a brain stimulator) in a part of the brain called the nucleus accumbens (NA). The nucleus accumbens is where the brain controls reward, motivation, and addiction. Caffeine at daily doses of human consumption, in contrast to classic drugs, does not induce a release of dopamine in the nucleus accumbens. It only increases blood sugar (glucose) usage. Glucose release stimulates most brain structures and reflects the effects linked to high caffeine ingestion.
Caffeine does cause a release of dopamine in another part of the brain, the prefrontal cortex. The pre-frontal cortex functions are differentiating conflicting thoughts, future consequences of current activities, and the ability to suppress urges that, if not suppressed, could lead to socially unacceptable outcomes. Although caffeine fulfills some of the criteria for drug dependence, it does not relate to reward, motivation, and addiction.
Coffee and caffeine consumptionCaffeine is present in a number of dietary sources including tea, coffee, cocoa beverages, candy bars, and soft drinks. The caffeine content of these food items varies. Using 150 milliliters as a standard volume (about one cup), caffeine ranges from 71-220 milligrams for coffee, 32-42 milligrams for tea, 32-70 milligrams for cola, and 4 milligrams for cocoa. The two major coffee types are Arabica and Robusta. In a standard cup, caffeine ranges from 71-120 milligrams for Arabica to nearly double that in Robusta (131-220 milligrams).
Average caffeine consumption from all sources is approximately 76 milligrams per person per day but reaches 210-238 milligrams per person per day in the United States and Canada and more than 400 milligrams per person per day in Sweden and Finland, where 80-100% of the caffeine intake is from coffee alone. In the United Kingdom, the consumption of caffeine is similar to that in Sweden and Finland, but 72% is from tea. The daily intake of caffeine from all sources in the United States is two thirds coming from coffee consumed by subjects older than 10 years. In American children, soft drinks represent 55%, chocolate foods and beverages represent 35-40%, and tea represents 6-10% of the total caffeine intake.
Pharmacology of caffeineCaffeine, or 1,3,7-trimethylxanthine, is related structurally to uric acid. There is no evidence suggesting that methylxanthines are converted to uric acid or that their ingestion can exacerbate gout.
The rate of bodily elimination of methylxanthines varies by individual due to both genetic and environmental factors, and people may exhibit an astounding four-fold difference in speed of ridding caffeine from one person to then next. The metabolism (elimination) of methylxanthines is also influenced by other consumed chemicals and even health conditions. Biochemicals from cigarette smoking and oral contraceptives produce a small increase in methylxanthine elimination.
When a substance is introduced into the body, its speed of delivering its properties to where it is supposed to and then be fifty percent eliminated is called its half-life. Caffeine has a half-life of three to seven hours. Methylxanthine’s half life increases up to fourteen hours in women during the later stages of pregnancy or with long-term use of oral contraceptive steroids.
Clinical trails on caffeine and central nervous system arousal In a Dutch study of subjects instructed to respond to stimuli that were either red or blue, reaction times revealed faster responses in subjects who had been administered caffeine. This study suggested that caffeine results in a higher overall arousal level, more profound processing of both attended and unattended information, and acceleration of motor processes (actively doing something).
The United Kingdom conducted two caffeine studies. Caffeine level was manipulated by preparing tea and coffee at different strengths. Beverage volume and temperature (55 degrees Celsius) were constant. Systolic blood pressure, diastolic blood pressure, heart rate, skin temperature, electrical skin conductance, and mood were monitored over three hour study sessions.
In study number one, tea and coffee produced mild stimulation and mood elevation. Effects were not related to tea versus coffee or caffeine dose, despite a fourfold variation in the strength of caffeine. Increasing beverage strength was associated with greater increases in diastolic blood pressure and significant arousal. In study number two, caffeinated beverages increased systolic blood pressure, diastolic blood pressure, and skin conductance, but lowered heart rate and skin temperature. Caffeine had significant effects on arousal but no exact dosage could be found that would give clear response effects. The authors concluded that caffeinated beverages acutely stimulate the autonomic nervous system (the “fight or flight” system ) and increase alertness.
Another research study gave 200 milligrams caffeine or placebo to young truck drivers. Caffeine significantly reduced sleep incidents for the first 30 minutes and reduced subjective (perceived) sleepiness for an hour. This caffeine dose (via coffee) effectively reduced early morning driver sleepiness for about 30 minutes following sleep deprivation and for approximately 2 hours after sleep restriction.
Single exposure to caffeine can produce cerebral stimulant effects. This is especially true in the areas that control locomotor activity (skeletal-muscle) and in the sleep-wake cycle. In humans, sleep seems to be the physiological function most sensitive to the effects of caffeine. In general, more than 200 mg of caffeine is required to significantly affect sleep. Caffeine prolongs sleep latency (the length of time it takes from full wakefulness to sleep, normally to the lightest sleep stage) and shorten total sleep duration with preservation of the dream phases of sleep. Evidence of tolerance to caffeine-related sleep disturbance exists, since heavy coffee drinkers appear to be less sensitive to caffeine-induced sleep disturbances than light coffee drinkers
Caffeine and dependence / withdrawalDrug dependence is defined as a pattern of behavior focused on the repetitive and compulsive seeking and taking of a psychoactive drug.
Caffeine withdrawal symptoms most often reported are headaches, fatigue, weakness, drowsiness, impaired concentration, work difficulty, depression, anxiety, irritability, increased muscle tension, and occasionally tremor, nausea, and vomiting. Withdrawal symptoms generally begin 12-24 hours after sudden cessation of caffeine and reach a peak after 20-48 hours. In some individuals, however, these symptoms can appear within 3-6 hours and can last for one week. Interestingly, withdrawal symptoms and its length do not relate to the quantity of caffeine routinely ingested.
Caffeine withdrawal symptoms disappear shortly after ingestion of caffeine. This effect is linked strongly to the psychological satisfaction related to the ingestion of caffeine; this is especially true for the first cup of the day. The reversal of a caffeine withdrawal-induced headache and other withdrawal symptoms has been known for more than 50 years. The beneficial effects of caffeine consumption on mood or alertness seem to encourage the consumption of coffee or caffeine-containing beverages.
Tolerance to caffeineTolerance to a drug refers to an acquired change in responsiveness after repeated exposure to the drug. Tolerance can be considered in two ways. First, the dose necessary to achieve the desired euphoria increases with time, thus encouraging increased consumption of the drug. Second, tolerance to the adverse effects of high doses of the drug, also leading to increased consumption of the drug over time since the undesirable side-effects become more easily tolerated.
Human tolerance to caffeine can occur as it affects blood pressure, heart rate, diuresis (increased urine flow) and adrenaline and noradrenaline levels (brain/nervous system neurotransmitters). Tolerance usually develops within a few days. Evidence of tolerance through research to caffeine-induced alertness and wakefulness is limited, since acute administration of 10 milligram/kilogram caffeine induced the same brain heightened metabolic increase whether the person was exposed to fifteen days of previous daily consumption of caffeine or salt water. Tolerance to the enhancement of arithmetic skills by caffeine has been shown, however – few good things last for long!