Caffeine citrate
Methylxanthines
Methylxanthines
The treatment of choice for apnea of prematurity: it stimulates breathing in preterm babies and lasts days because they clear it slowly.
Quick facts
- Group
- Methylxanthines
- Target
- Adenosine A1 and A2A receptors
- Used for
- Apnea of prematurity
- Key effects
- Feeding intolerance and vomiting · Tachycardia
- Monitor
- Number and length of apneas · Heart rate
- ATC
- N06BC01
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows caffeine bound to the human adenosine A2A receptor (stabilised crystal construct).
Caffeine is a methylxanthine that blocks adenosine A1 and A2A receptors. In preterm infants this stimulates the respiratory centre, increases minute ventilation, lowers the threshold to carbon dioxide, improves diaphragm contraction and raises metabolic rate. The citrate salt is used because it dissolves well; the active substance is caffeine.
- Adenosine depresses breathing in the immature brain
- Caffeine blocks adenosine A1 and A2A receptors
- The respiratory centre responds more to carbon dioxide
- Apnea episodes become fewer
Indications
- Apnea of prematurity Apnoea of prematurity →
Adverse effects
Common
- Feeding intolerance and vomiting
- Tachycardia
- Irritability, restlessness and jitteriness
- Increased urine output
Contraindications
- Hypersensitivity to any component
- Caution in seizure disorders, heart disease and kidney or liver impairment
Key interactions
- Theophylline
- The two interconvert in preterm neonates; not combined
- Cimetidine, ketoconazole
- Reported to slow caffeine elimination
- Phenobarbital and phenytoin
- Speed caffeine elimination
What is monitored
- Number and length of apneas, bradycardias and desaturations
- Heart rate; withhold and report marked tachycardia
- Abdominal distension, feeding tolerance and stools (enterocolitis)
- Serum caffeine levels in selected infants
Administration and safety
- Intravenous infusion with a syringe pump, or the oral solution
- Caffeine citrate and caffeine base are not the same amount: orders and labels are checked for which one is meant
- Single-use vials: unused portions are discarded
Pregnancy and breastfeeding
It is a neonatal medicine; in the mother, caffeine from drinks crosses the placenta and passes into milk.
Nursing care
- Record apneas, bradycardias and desaturations before and during treatment
- Check heart rate before each dose
- Assess the abdomen and feeding tolerance every shift
- Watch for jitteriness and seizures
Pharmacokinetics
- Absorption
- Given intravenously or by mouth; oral absorption is good
- Metabolism
- Very limited in preterm infants because liver enzymes are immature; some interconversion with theophylline
- Elimination
- Mostly unchanged in the urine in neonates
- Half-life
- About 3 to 4 days in neonates, shortening as the infant matures
Test yourself
Think of the answer, then tap the question to see it.
What is caffeine citrate used for in neonatal care?
Apnea of prematurity.
Why does caffeine last so long in preterm infants?
Their immature liver barely metabolises it, so it is eliminated slowly, mostly unchanged in urine.
Which receptors does caffeine block to stimulate breathing?
Adenosine A1 and A2A receptors.
Which gut complication is watched for during caffeine treatment?
Necrotising enterocolitis.
Connections
← Back to the class: Methylxanthines
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - CAFFEINE CITRATE- caffeine citrate injection, solution (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); eEML - Electronic Essential Medicines List (World Health Organization, 2025).
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Representative model, for educational purposes only.