Is there a prescription caffeine formulation available for therapeutic use?

Prescription Caffeine Formulations

Yes, there is a prescription caffeine formulation available: caffeine citrate (oral solution and injection), which is FDA-approved specifically for treating apnea of prematurity in neonates. 1

Available Prescription Formulation

Caffeine citrate is supplied as both an oral solution and injection at a concentration of 20 mg/mL caffeine citrate (equivalent to 10 mg/mL caffeine base), packaged in 3 mL single-use vials containing 60 mg caffeine citrate per vial. 1

• The oral solution comes in non-child-resistant 3 mL vials, packaged 10 vials per child-resistant container 1
• The injection formulation is labeled "FOR INTRAVENOUS USE ONLY" 1
• Both formulations are preservative-free and intended for single use only 1

Primary Therapeutic Indication

Caffeine citrate is FDA-approved for neonatal apnea of prematurity, not for general adult use as a stimulant or wakefulness-promoting agent. 1

Alternative Therapeutic Uses in Adults

While caffeine citrate is the only prescription formulation, caffeine has several recognized therapeutic applications in adults:

• Combination therapy for migraine headaches with ergotamine 2, 3
• Adjuvant analgesic in combination with NSAIDs (acetaminophen-aspirin-caffeine combination shows good efficacy evidence) 2, 3
• Treatment of specific headache conditions including postdural puncture headache and perioperative headache (potentially by alleviating caffeine withdrawal) 3
• Respiratory stimulation in specific clinical contexts 3
• Enhancement of seizure duration in electroconvulsive therapy 3

Important Clinical Considerations

For adult patients seeking wakefulness promotion or stimulant effects, over-the-counter caffeine tablets are available and appropriate, with safe daily limits of ≤400 mg for healthy adults. 4

Contraindications and Cautions

• Patients with uncontrolled hypertension should avoid caffeine 4, 5
• Limit intake to <300 mg/day in patients with cardiovascular concerns or those taking certain medications 4, 5
• Pregnant women should limit caffeine to ≤200-300 mg/day due to slower metabolism and placental transfer 4

Drug Interactions

Caffeine is metabolized by CYP1A2 and can interact with multiple medications including fluvoxamine, mexiletine, clozapine, enoxacin, and theophylline, potentially causing toxic accumulation. 6, 7

• Fluvoxamine and quinolones (particularly enoxacin) are potent CYP1A2 inhibitors that can dramatically increase caffeine levels 6
• Psychiatric patients often have excessive dietary caffeine intake, which can complicate medication management 6, 7

Perioperative Management

Caffeine supplements should ideally be tapered and discontinued 2 weeks before surgery due to stimulant properties and potential effects on glucose metabolism, though beverage consumption (coffee/tea) is considered safe. 2

Common Pitfall

Do not prescribe caffeine citrate for adult wakefulness or fatigue management—this is off-label use of a neonatal medication. Instead, direct patients to over-the-counter caffeine tablets (typically 100-200 mg per tablet) with appropriate counseling on safe daily limits and potential interactions. 4, 3