[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Methylxanthines](https://durgical.com/en/pharmacology/classes/methylxanthines/) › Caffeine citrate

# 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.

Updated Nov 1, 2026

## Quick facts

**Group**
[Methylxanthines](https://durgical.com/en/pharmacology/classes/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.

On this page

- The basics Mechanism of action
- Indications
- Adverse effects
- Pharmacokinetics
- Memory aid

- Safety Contraindications
- Key interactions
- What is monitored
- Administration and safety
- Pregnancy and breastfeeding
- Nursing care

- Study Test yourself

- Connections Connections

## Mechanism of action

◎**Adenosine A1 and A2A receptors**Caffeine citrate

ⓘ The figure shows caffeine bound to the human adenosine A2A receptor (stabilised crystal construct).

**Target in 3D:** Adenosine A1 and A2A receptors. PDB structure 5MZP (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/5MZP) · Drag to rotate · pinch to zoom

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 →](https://durgical.com/en/conditions/apnoea-of-prematurity/)

## Adverse effects

### Common

- Feeding intolerance and vomiting
- Tachycardia
- Irritability, restlessness and jitteriness
- Increased urine output

### Serious (rare, important)

- Necrotising enterocolitis has been reported during treatment; a causal link is not established but infants are watched closely
- Seizures in overdose
- Arrhythmias in overdose

## 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

## Memory aid

CAFFeine for the Cot: Coffee for babies who Forget to breathe.

## 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.

[Add to my cards (4)](https://durgical.app/estudiar/?add=/en/pharmacology/caffeine-citrate/)

[More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology)

## Connections

## Related drugs 2

- [Theophylline](https://durgical.com/en/pharmacology/theophylline/)
- [Aminophylline](https://durgical.com/en/pharmacology/aminophylline/)

## Related conditions 1

- [Apnoea of prematurity](https://durgical.com/en/conditions/apnoea-of-prematurity/)

[← Back to the class: Methylxanthines](https://durgical.com/en/pharmacology/classes/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](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=279a43b8-9ff5-4792-ac19-441f3fa49269) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N06BC01) (WHO Collaborating Centre for Drug Statistics Methodology, 2026); [eEML - Electronic Essential Medicines List](https://list.essentialmeds.org/?query=caffeine) (World Health Organization, 2025).

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Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/caffeine-citrate/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/caffeine-citrate/