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NERVOUS SYSTEM › PSYCHOANALEPTICS › PSYCHOSTIMULANTS, AGENTS USED FOR ADHD AND NOOTROPICS › Xanthine derivatives
caffeine
N06BC01
Forms & Strengths
- Oral tablet: 100 mg, 200 mg
- Oral capsule, extended-release: 200 mg
- Intravenous injection: 20 mg/mL (as caffeine citrate)
- Oral solution: 20 mg/mL (as caffeine citrate)
Adult Dosing
- Apnea of prematurity: N/A (neonatal indication)
- Fatigue/Alertness: 100 mg to 200 mg orally every 3 to 4 hours as needed
- Maximal recommended daily adult dose: 400 mg/day
Pediatric Dosing
- Apnea of prematurity (Caffeine citrate): Loading dose 20 mg/kg IV or orally once
- Apnea of prematurity maintenance dose: 5 mg/kg IV or orally once daily starting 24 hours after loading dose
Indications
- Apnea of prematurity in neonates between 28 and 33 weeks gestational age
- Management of transient fatigue and promotion of wakefulness
Mechanism of Action
- Nonselective adenosine receptor antagonist (A1 and A2A subtypes)
- Stimulation of the central nervous system, particularly the medullary respiratory center
- Inhibition of phosphodiesterase, leading to increased intracellular cyclic AMP
Contraindications
- Hypersensitivity to caffeine or any component of the formulation
- Documented history of serious cardiac arrhythmias (in high-dose adult contexts)
Adverse Reactions
- Cardiovascular: Tachycardia, hypertension, cardiac arrhythmias
- Central nervous system: Insomnia, nervousness, jitteriness, agitation, seizure (in overdose)
- Gastrointestinal: Nausea, vomiting, gastric irritation
- Renal: Increased diuresis
Drug Interactions
- CYP1A2 inhibitors (e.g., ciprofloxacin, fluvoxamine): Decrease caffeine metabolism, increasing toxicity risk
- CYP1A2 inducers (e.g., smoking, phenytoin): Increase caffeine clearance
- Sympathomimetic agents: Enhance central nervous system and cardiovascular stimulation
- Theophylline: Additive pharmacodynamic stimulation
Curated Content: Needs Vetting Before Put to Clinical Use