![]() Many complex analgesics with such a combination of active substances are available on the market, also without a prescription. Low doses of caffeine are used as a fortifying adjuvant in combination with antidepressants, paracetamol, acetaminophen and non-steroidal anti-inflammatory drugs. It has been found that adding small doses of caffeine to a standard dose of common painkillers reinforces their analgesic effect. Īs experimental data showed, caffeine administered in doses from 25 to 100 mg/kg has an intrinsic antinociceptive effect. These two mechanisms, i.e., receptor antagonism and a multi-site effect on eicosanoid pathways (mainly by modulating cyclooxygenase activity), may explain the antinociceptive and adjuvant effects of caffeine. Caffeine may also develop an analgesic effect due to its ability to inhibit the synthesis of leukotrienes and prostaglandins. Due to its similar structure to adenosine, caffeine may compete with adenosine for A2A receptors, causing their inhibition. Thus, for example, activation of A1 and A2A adenosine receptors in neuropathic pain results in antinociceptive activity. They are expressed in various parts of the human nervous system, both central and peripheral. Three subtypes of these receptors are known: A1, A2 (A2A and A2B) and A3 receptors. Adenosine causes different effects in the central and peripheral nervous system, related to its effect on adenosine receptors. Adenosine is an inhibitor of neuronal activity in the central (CNS) and peripheral nervous system (PNS). Ĭaffeine, whose structure is similar to that of adenosine, affects pain control. In addition, it freely penetrates the blood–brain and placental barriers, and its half-life varies between 4 and 9 h. ![]() ![]() Īfter oral administration, caffeine is absorbed quickly and completely its bioavailability is almost 100%. For example, filtered coffee contains 85 mg of caffeine per 125 mL of drink, instant coffee contains 65 mL of caffeine in the same volume, tea contains 32 mg of caffeine per 150 mL of drink, energy drinks contain 80 mg/330 mL, dark chocolate contains 60 mg of caffeine per 30 g and milk chocolate contains only 6 mg per 30 g. Ĭaffeine content varies depending on the type of food you consume. These statements do not apply to caffeine used occasionally, in small amounts. Even therapeutic doses of caffeine have been associated with atrial fibrillation and central nervous system toxicity and should be used with caution in high-risk patients. Therefore, caffeine, especially in excess, is not recommended for people with hypertension or a history of seizures and should not be recommended for them. However, high doses of caffeine (400–800 mg once) can have negative effects and evoke anxiety, nervousness, tremors, insomnia or tachycardia. It also improves physical fitness, short-term memory and cognitive performance. Caffeine consumed once in a dose of 50–100 mg increases energy, alertness, reaction accuracy and the ability to concentrate and focus attention, and it improves well-being and mood and reduces fatigue. Consuming moderate amounts of caffeine, i.e., 200–400 mg of caffeine per day (about 4–5 cups of coffee), is safe for healthy, non-pregnant adults. Caffeine is found primarily in coffee, but also in tea, chocolate and energy drinks. Caffeine, a naturally occurring methylxanthine, is probably the most commonly consumed psychoactive compound worldwide.
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