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Caffeine (200 mg)

University Hospital, Basel, Switzerland · FDA-approved active Small molecule

Caffeine blocks adenosine receptors in the central nervous system, preventing the accumulation of adenosine and reducing drowsiness while increasing alertness and mental focus.

Caffeine blocks adenosine receptors in the central nervous system, preventing the accumulation of adenosine and reducing drowsiness while increasing alertness and mental focus. Used for Fatigue and drowsiness (over-the-counter use), Adjunctive treatment in headaches and migraines, Apnea of prematurity (in neonates).

At a glance

Generic nameCaffeine (200 mg)
Also known ascoffeinum, methyltheobromine, 1,3,7-trimethyl-3,7-dihydro-1H-purin-2,4-dion, CAS No: 56-08-2, Ph.Eur: 6.0/027
SponsorUniversity Hospital, Basel, Switzerland
Drug classMethylxanthine; Central nervous system stimulant
TargetAdenosine receptors (A1, A2A, A2B, A3)
ModalitySmall molecule
Therapeutic areaNeurology; General wellness
PhaseFDA-approved

Mechanism of action

Caffeine is a non-selective adenosine receptor antagonist that crosses the blood-brain barrier and competitively inhibits adenosine binding at A1 and A2A receptors. By blocking adenosine—a neurotransmitter that promotes sleep and relaxation—caffeine increases neuronal firing, enhances dopamine and norepinephrine signaling, and produces stimulant effects including increased wakefulness, improved concentration, and elevated heart rate and blood pressure.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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