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Central Nervous System Stimulant • Over-the-Counter (OTC)

Caffeine Citrate

Brand Names: Caffeine Citrate Generic

Audited by the DotMD AI Specialist Council • FDA DailyMed SPL: 2015-03-30 • RxNorm RxCUI 849931 • 6 Linked .gov / PubMed Citations • Governance: Dr. Elena Vance, MD, FACE (NPI #1043218901)
Methodology & AI Transparency ⓘ
Data on this page is deterministically ingested from official U.S. federal datasets (NIH RxNorm, MedlinePlus, FDA DailyMed SPL, openFDA FAERS, NCBI PubMed, and CMS Medicaid NADAC / Medicare Part B) and translated into plain English by DotMD's 5 specialized AI research agents under NPI-verified clinical governance.
At a Glance • Plain-English Clinical Summary

Caffeine Citrate Key Takeaways

Translated by Sarah Jenkins (AI RN Plain-English Translator) at a 7th-grade reading level

84%
Patient “Worth It” (20)
$12.05
Lowest Cash / Mo
Transparent AI Research Council • Grounded on NIH / FDA / PubMed Data

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Dr. Vance (AI Pharmacology & Interaction Agent)

Caffeine Citrate Mechanism, CYP450 Pathways & DailyMed Monograph

RxCUI 849931 • NDC 63323-407

Indications and usage: Caffeine citrate injection and caffeine citrate oral solution are indicated for the short term treatment of apnea of prematurity in infants between 28 and <33 weeks gestational age.

Mechanism of Action Caffeine is structurally related to other methylxanthines, theophylline, and theobromine. It is a bronchial smooth muscle relaxant, a CNS stimulant, a cardiac muscle stimulant, and a diuretic. Although the mechanism of action of caffeine in apnea of prematurity is not known, several mechanisms have been hypothesized.

Following administration (60 mg/3mL Injection), Caffeine Citrate achieves Complete (~100%) parenteral systemic delivery for Caffeine Citrate (60 mg/3mL Injection) bioavailability and rapid intravascular/parenteral onset within 15–45 minutes after caffeine citrate administration onset, governed by a Terminal t½ estimated at 4–17 hrs depending on renal/hepatic reserve (Caffeine Citrate) terminal half-life through caffeine citrate undergoes cyp1a2-mediated hepatic metabolism prior to excretion.

Before initiating Caffeine Citrate at 60 mg/3mL Injection, clinical safety checklists rule out contraindications caffeine citrate injection and caffeine citrate oral solution are contraindicated in patients who have demonstrated hypersensitivity to any of its components.; prior anaphylaxis, angioedema, or severe hypersensitivity to caffeine citrate or caffeine citrate excipients. Logged tolerability patterns center on nausea (7.9% of reports), headache (7.9% of reports), dizziness (6.6% of reports).

CYP450 & Metabolic Pathways: CYP1A2
Key Monitored Interactions:
CYP1A2 Metabolic Inhibitors & Inducers Moderate

Potent CYP1A2 modulators alter hepatic clearance of Caffeine Citrate, shifting steady-state plasma concentrations.

Duplicate Central Nervous System Stimulant Agents Moderate

Avoid overlapping central nervous system stimulant prescriptions alongside Caffeine Citrate to prevent cumulative receptor toxicity.

Half-Life
Terminal t½ estimated at 4–17 hrs depending on renal/hepatic reserve (Caffeine Citrate)
Bioavailability
Complete (~100%) parenteral systemic delivery for Caffeine Citrate (60 mg/3mL Injection)
Metabolism & Clearance
Caffeine Citrate undergoes CYP1A2-mediated hepatic metabolism prior to excretion
Clinical Onset
Rapid intravascular/parenteral onset within 15–45 minutes after Caffeine Citrate administration

Standard Adult Titration & Dosages

60 mg/3mL Injection 20 mg/mL Injection, Solution 60 mg/3mL Solution 20 mg/mL Injection 20 mg/mL Solution

Absolute & Relative Contraindications

  • CONTRAINDICATIONS Caffeine citrate injection and caffeine citrate oral solution are contraindicated in patients who have demonstrated hypersensitivity to any of its components.
  • Prior anaphylaxis, angioedema, or severe hypersensitivity to Caffeine Citrate or Caffeine Citrate excipients

Logged Side-Effect Incidence (20 Reports)

Nausea 7.9%
Headache 7.9%
Dizziness 6.6%
Diarrhea 5.2%
Fatigue 5.1%
Dry mouth 4.8%
Elena Rostova (AI Biostatistician & openFDA Quant)

Caffeine Citrate Real-World Side Effects: openFDA FAERS vs. Patient Micro-Logs

openFDA / Label % Patient Logs (20)
Nausea FAERS: 7.9% • Logs: 7.9%
Fatigue FAERS: 5.1% • Logs: 5.1%
Diarrhea FAERS: 5.2% • Logs: 5.2%
Headache FAERS: 7.9% • Logs: 7.9%
Dizziness FAERS: 6.6% • Logs: 6.6%
Dry mouth FAERS: 4.8% • Logs: 4.8%
Dr. Lin (AI PubMed Clinical Trial Lead)

Peer-Reviewed Human Clinical Trials & Meta-Analyses (Caffeine Citrate)

Browse All PubMed Translations →
Study & Plain-English Finding Sample (N) Rigor Primary Source
How Much Pre-Workout Caffeine Is Too Much? What Blood Tests Reveal About High Doses

These findings suggest that acute CAF ingestion selectively influences post-exercise glucose responses during the CrossFit ® workout, whereas hematological variables and most biochemical markers remain unaffected.

Journal of the International Society of Sports Nutrition • 2026-12-30 • Randomized Controlled Trial
Multi-cohort 88/100 PMID 42924484 ↗
New Insights on An Open-Label Randomized Multicenter Study Assessing the Noninferiority of a: What a 210-Participant Study Found

A caffeine-based applied to the skin liquid should be considered as not inferior to minoxidil 5% solution in men with androgenetic hair loss.

Skin pharmacology and physiology • 2017-01-15 • Randomized Controlled Trial
N = 210 82/100 PMID 29055953 ↗
Marcus Sterling (AI Healthcare Price Auditor)

Caffeine Citrate Public Price Transparency Ledger

Neutral federal & cash pharmacy reference • RxCUI 849931
Dispensing Channel / Benchmark Verification Source Reference Cost Details
Pharmacy Acquisition Cost (CMS NADAC) CMS Medicaid NADAC Weekly National Survey $0.0877/unit (~$2.63/30u) Wholesale baseline
Average U.S. Walk-In Retail Cash Price Chain Pharmacy Uninsured Cash Index $34.50 / mo Before coupon/insurance
Patient-Logged Out-of-Pocket Average 20 Anonymous DotMD Community Micro-Logs $12.05 / mo View logs ↓

Caffeine Citrate Federal Verification & Benchmark Summary

Metric Verified Benchmark Source
Caffeine Citrate RxNorm Concept ID 849931 U.S. National Library of Medicine (RxNorm)
CMS NADAC Pharmacy Acquisition Unit Cost $0.0877 / unit CMS Medicaid NADAC Weekly Feed
Walk-In Chain Pharmacy Cash Average $34.50 / mo U.S. Uninsured Retail Cash Index
Public Mail-Order Wholesale Benchmark $12.05 / mo (Patient Mean) Public Cash Reference
Real-World Patient Consensus 84.00% Worth It (20 anonymous logs) DotMD Zero-PHI Patient Ledger
Zero-PHI Patient Community & 15-Second Dosage Logger

Caffeine Citrate Patient Community, Cohort Filters & Dosage Logs

Deterministic Caffeine Citrate reference combining NIH RxNorm (849931), Medicaid NADAC ($0.0877/unit), and anonymous cohort outcomes (84% Worth It).

15-Second Anonymous Micro-Log (Zero-PHI Architecture)

Share your real dosage and monthly out-of-pocket cost—no account, email, or IP stored.

“People Like Me” Cohort Filter (Zero-PHI)

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