Learning Center/Pharmacology/Caffeine Citrate

Caffeine Citrate

Cafcit

bronchodilator sabaIV · oralOnset: Loading dose: 30 minutes–4 hoursDuration: Half-life: 40–230 hours in neonates (wide variability)

Mechanism of Action

Methylxanthine. Competitively antagonizes adenosine receptors (A1 and A2A) in CNS → stimulates respiratory drive (chemoreceptor sensitivity to CO2). Also increases diaphragmatic contractility and reduces hypoxic depression of breathing.

Dosing

Neonatal

Loading dose: 20 mg/kg IV over 30 min. Maintenance: 5–10 mg/kg IV/oral once daily starting 24 hr after loading dose

Doses expressed as caffeine citrate (not base): 20 mg/kg caffeine citrate = 10 mg/kg caffeine base

Indications

Apnea of prematurity (AOP) — first-line treatment
Facilitation of extubation in premature neonates

Contraindications

Hypersensitivity to caffeine
Symptomatic cardiac arrhythmias

Side Effects

Tachycardia
Jitteriness / irritability
Feeding intolerance
Hyperglycemia
Diuresis (mild — caffeine is a weak diuretic)
Necrotizing enterocolitis (association, not causation)

Monitoring Parameters

Heart rate (tachycardia)
Apnea episodes (count per shift)
Serum caffeine levels if toxicity suspected (therapeutic 5–25 mcg/mL)
Feeding tolerance
Blood glucose

Drug Interactions

Theophylline (additive toxicity — methylxanthine overlap; avoid combination)
Cimetidine (increases caffeine levels via CYP1A2 inhibition)
Phenobarbital (decreases caffeine levels via CYP1A2 induction)

Clinical Pearls

Preferred methylxanthine over theophylline in neonates (wider therapeutic window, once-daily dosing)
CAP trial: caffeine reduces BPD, PDA, and neurodevelopmental delay in premature infants
Long half-life in neonates (immature CYP1A2 metabolism) — once daily dosing is sufficient
Oral and IV formulations bioequivalent — can switch from IV to oral when tolerating feeds
Typically continued until 34–36 weeks corrected gestational age
Doses stated as caffeine citrate — 20 mg/kg caffeine citrate = 10 mg/kg caffeine base

Mnemonic

💡 Caffeine = Chemo-receptor Amplifier For Fragile Infants Eliminating apNeas

NBRC High-Yield

First-line for apnea of prematurity
Loading 20 mg/kg IV; maintenance 5–10 mg/kg daily (as caffeine citrate)
Adenosine receptor antagonist → stimulates respiratory drive
Long half-life (40–230 hr) in neonates → once-daily dosing
CAP trial: reduces BPD and improves neurodevelopmental outcomes
Watch for tachycardia and jitteriness

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Clinical Pearls

Preferred methylxanthine over theophylline in neonates (wider therapeutic window, once-daily dosing)

CAP trial: caffeine reduces BPD, PDA, and neurodevelopmental delay in premature infants

Long half-life in neonates (immature CYP1A2 metabolism) — once daily dosing is sufficient

Oral and IV formulations bioequivalent — can switch from IV to oral when tolerating feeds

Typically continued until 34–36 weeks corrected gestational age

Doses stated as caffeine citrate — 20 mg/kg caffeine citrate = 10 mg/kg caffeine base

NBRC High-Yield

First-line for apnea of prematurity

Loading 20 mg/kg IV; maintenance 5–10 mg/kg daily (as caffeine citrate)

Adenosine receptor antagonist → stimulates respiratory drive

Long half-life (40–230 hr) in neonates → once-daily dosing

CAP trial: reduces BPD and improves neurodevelopmental outcomes

Watch for tachycardia and jitteriness