Caffeine

CAFCIT

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Pronunciation: KAF-een

Caffeine ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Caffeine ballicule

Caffeine CAFCIT mascot mnemonic cartoon — Visual mnemonic: Caffeine mascot
**“A dino sign (adenosine) antagonist”**

What it isAdenosine receptor antagonist; alertness, analgesic adjunct, and apnea of prematurity.

Why this oneIn neonates it reduces apnea and improves neurodevelopmental outcome, which is a genuine therapeutic use rather than a stimulant one.

What limits itTolerance and withdrawal headache. A CYP1A2 substrate, so fluvoxamine and ciprofloxacin raise levels sharply, and smoking lowers them.

Caffeine molecular structure (skeletal formula) — Molecular structure: Caffeine

FDA-approved for

apnea of prematurity (~1999)

Off-label

post-dural-puncture headache

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Apnea of prematurity	Preterm infants	Load 20 mg/kg (1 mL/kg) IV over 30 min, once	Maintenance 5 mg/kg (0.25 mL/kg) IV over 10 min or PO q24h, starting 24 h after load	Undefined (serious toxicity with serum levels >50 mg/L)

Renal Undefined

Hepatic Undefined

Measure baseline caffeine level if infant previously on theophylline or mother consumed caffeine before delivery; monitor levels periodically.

Instructions

Doses expressed as caffeine citrate (20 mg citrate = 10 mg caffeine base)
IV via syringe infusion pump: load over 30 min, maintenance over 10 min
Inspect for particulates/discoloration; single-dose vial — discard unused portion
Stable 24 h at room temp admixed with D5W, D50W, Intralipid 20%, Aminosyn 8.5%, dopamine, calcium gluconate, heparin, fentanyl

Available strengths

sol 30 mg/3 mL
inj 20, 125 mg/mL
tab 100, 200 mg
cream 6 g/100 mL
gel 1 g/108.27 g
paste 0.05 g/100 mL

Cautions

Necrotizing enterocolitis — monitor

Adverse reactions

Feeding intolerance (8.7%)
Rash (8.7%)
Sepsis (4.3%)
Necrotizing enterocolitis (4.3%)
CNS stimulation (irritability, jitteriness) — literature
Tachycardia — literature
Hypo-/hyperglycemia — literature
Increased gastric aspirate/GI intolerance — literature

Pregnancy Pregnancy Category C; teratogenicity not relevant to infant use; cleft palate/exencephaly in mice.

Cost

Caffeine (CAFCIT)

Strength		#/mo	CostPlus
30 mg/3 mL	sol	per unit	not offered
20 mg/mL	inj	per unit	not offered
125 mg/mL	inj	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Caffeine is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Available combined with: butalbital / acetaminophen / caffeine

NO BOXED WARNINGS

Principal riskWithdrawal headache; CYP1A2 interactions

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

Direct muscarinic antagonism0 / 4

Legacy pregnancy categoryC

Defining liabilityNeonatal accumulation and dosing-related tachycardia or seizures

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Memory aids: interaction avatars

CYP1A2 substrate

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