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Theobromine
Theobromine is a dimethylxanthine alkaloid of cacao beans and is consumed in cocoa and chocolate foods.1 It acts as a mild heart stimulant and bronchodilator in humans, with limited effects on the central nervous system.2 It has been used in pharmaceutical products as a vasodilator, diuretic, and heart stimulant.3 Theobromine can cause fatal poisoning in dogs and cats because they metabolize it more slowly.
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Theobromine peaks in the blood 2-3 hours after ingestion due to its fat solubility, more slowly than caffeine, and its elimination half life is between 6 and 8 hours. At doses of 0.8-1.5 g/day (50-100 g cocoa), sweating, trembling and severe headaches were noted, with limited mood effects found at 250 mg/day.
Duration
Subjective Effects
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Theobromine produces little in the way of a distinct subjective experience at ordinary dietary exposures, acting mainly on the cardiovascular system rather than the central nervous system. Mood effects reported at low intakes are limited, and the compound is not a meaningful stimulant of the human CNS. At substantially higher intakes, the effects that emerge are predominantly physical and uncomfortable rather than perceptual or cognitive.
Physical
The physical profile centres on cardiac stimulation and vasodilation, with sweating, trembling, and severe headaches appearing at higher intakes.
Uncomfortable
Cardiovascular
Pharmacology
Pharmacodynamics
Theobromine acts principally by antagonizing adenosine receptors, with an additional inhibitory effect on cyclic nucleotide phosphodiesterases that is thought to be small and appears only at intakes far above those obtained from a normal diet. Both of these actions are weaker than those of caffeine. In humans it behaves as a mild cardiac stimulant, a diuretic, and a bronchodilator, and it relaxes vascular smooth muscle, while producing no significant stimulant effect on the central nervous system. It may also act on the esophageal sphincter muscle in a way that allows stomach acid to pass into the esophagus.
Pharmacokinetics
Theobromine is only slightly water-soluble and comparatively fat-soluble, and blood levels peak 2 to 3 hours after ingestion, more slowly than caffeine. It is metabolized in the liver into xanthine and subsequently into methyluric acid, with CYP1A2 and CYP2E1 among the important enzymes involved. The elimination half life is between 6 and 8 hours. Theobromine also arises endogenously as a metabolite of caffeine, which the liver converts into roughly 12% theobromine alongside 4% theophylline and 84% paraxanthine.
Interactions
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Harm Potential
Toxicity
The reported median lethal dose in dogs is 100–200 mg/kg.4 Dogs and cats metabolize theobromine more slowly than humans, and poisoning can be fatal, although fatal outcomes are described as uncommon.
In humans, theobromine at 0.8–1.5 g/day has produced trembling and severe headaches, accompanied by sweating.
Theobromine may contribute to heartburn in some people, and poisoning in dogs and cats can cause digestive disturbances and dehydration.
Theobromine poisoning in dogs and cats can cause a slow heart rate.
Seizure Risk
Advanced theobromine poisoning in dogs and cats can cause epileptic-like seizures and may progress to death.
History & Culture
Theobromine was first identified in 1841, when the chemist A. Woskresensky isolated it from cacao beans. It is the principal alkaloid of Theobroma cacao, the cacao plant, and gives the cacao bean much of its bitter taste. In 1882, Hermann Emil Fischer reported the first synthesis of theobromine…
Legality
References
Citations
Article Status
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