The clinical toxicology of caffeine: A review and case study

Abstract

Caffeine is a widely recognized psychostimulant compound with a long history of consumption by humans. While it has received a significant amount of attention there is still much to be learned with respect to its toxicology in humans, especially in cases of overdose. A review of the history of consumption and the clinical toxicology of caffeine including clinical features, pharmacokinetics, toxicokinetics, a thorough examination of mechanism of action and management/treatment strategies are undertaken. While higher (i.e., several grams) quantities of caffeine are known to cause toxicity and potentially lethality, cases of mainly younger individuals who have experienced severe side effects and death despite consuming doses not otherwise known to cause such harm is troubling and deserves further study. An attempted case reconstruction is performed in an effort to shed light on this issue with a focus on the pharmacokinetics and pharmacodynamics of caffeine.

Intake of Caffeine and Its Association with Physical and Mental Health Status among University Students in Bahrain

“…The pharmacology of caffeine and related methylxanthines is complex, as they modulate a variety of biological targets. Nevertheless, clinical and experimental investigations of caffeine pharmacology provide biological plausibility to some of these effects, as outlined in a recent comprehensive review [37]. At physiologically relevant concentrations, the predominant pharmacological effect is as a purinoceptor antagonist.…”

“…Indeed, positive allosteric modulators of A1A have been proposed as a therapeutic strategy for anxiety [38]. Based upon laboratory observations, it is often claimed that caffeine is a phosphodiesterase inhibitor, however, this action is unlikely to occur, at any but the very highest concentrations in vivo, and the relevance to anxiety is unclear [37].…”

Attenuation of Weight Gain and Prevention of Associated Pathologies by Inhibiting SSAO

“…It is noteworthy that histamine and caffeine might cause certain health pathologies in high concentrations, e.g., human pregnancy complications [100], urticaria [101], and cardiovascular diseases [102] respectively. Thus, the right doses need to be applied.…”

The Association Between Coffee Consumption and Local Anesthesia Failure: Social Beliefs and Scientific Evidence

“…Adults over the age of 25 years have an estimated consumption of approximately 2.4 mg/kg/day. In the literature, the average daily consumption of caffeine varied depending on the survey, year conducted, and the sources considered [28]. However, it has most recently (i.e., 2011 -2012) been reported as 142 mg per day for adults and children in the US, a decrease from previous years (e.g., the average consumption of 175 mg/day in 1999 -2000), which is largely attributed to a reduction in soda consumption.…”

“…However, it has most recently (i.e., 2011 -2012) been reported as 142 mg per day for adults and children in the US, a decrease from previous years (e.g., the average consumption of 175 mg/day in 1999 -2000), which is largely attributed to a reduction in soda consumption. Caffeine is known to have generally dosedependent effects with positive or desirable effects at lower doses (i.e., ≤ 400 mg) and undesirable effects generally above this level of intake [28].…”