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CARDIOVASCULAR SYSTEM › DIURETICS › LOW-CEILING DIURETICS, EXCL. THIAZIDES › Xanthine derivatives
theobromine
C03BD01
Forms & Strengths
- Oral: Capsules (e.g., 500 mg)
- Oral: Tablets (e.g., 500 mg)
- Botanical/Dietary supplement preparations (variable strengths)
Adult Dosing
- Diuresis / Bronchodilation: 300 mg to 500 mg orally every 4 to 6 hours as needed
- Maximum daily dose: 1.5 g to 2 g daily to avoid toxicity
Pediatric Dosing
- Safety and efficacy not established in pediatric populations
- Not recommended for routine pediatric use due to narrow therapeutic index and risk of central nervous system stimulation
Indications
- Historically used as a mild diuretic
- Adjunctive treatment for bronchial asthma and bronchospasm
- Vasodilator properties in clinical research settings
Mechanism of Action
- Non-selective phosphodiesterase (PDE) inhibitor, increasing intracellular cAMP
- Competitive antagonism of adenosine receptors
- Produces smooth muscle relaxation (specifically bronchial and vascular), myocardial stimulation, and mild diuresis
Contraindications
- Hypersensitivity to theobromine, caffeine, or other methylxanthines
- Severe cardiovascular disease, unstable angina, or recent myocardial infarction
- Severe hepatic impairment
Adverse Reactions
- Central nervous system: Insomnia, nervousness, restlessness, tremors, headache
- Cardiovascular: Tachycardia, palpitations, flushing, hypotension
- Gastrointestinal: Nausea, vomiting, dyspepsia, increased gastric acid secretion
- Renal: Diuresis, mild urinary frequency
Drug Interactions
- Other methylxanthines (e.g., caffeine, theophylline): Additive stimulant and adverse effects
- CYP1A2 inhibitors (e.g., cimetidine, fluoroquinolones): May decrease theobromine clearance and increase toxicity risk
- Sympathomimetics: Enhanced cardiovascular stimulation and arrhythmia risk
Curated Content: Needs Vetting Before Put to Clinical Use