HomeNDC LookupIngredientsCaffeine Citrate › 55150-0187-03
Caffeine Citrate 20 mg/mL Injection, Solution — NDC 55150-0187-03 package photo

Caffeine Citrate 20 mg/mL Injection, Solution

by Eugia US LLC · 1 VIAL, SINGLE-DOSE in 1 CARTON (55150-187-03) / 3 mL in 1 VIAL, SINGLE-DOSE
NDC 55150-0187-03
🏷️ FDA NDC (as labeled) 55150-187-03 billing pads the product segment with a zero
Rx only Generic On market Non-controlled
🗂️ Data synced Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

🆔 Identity & classification

FDA NDC (as labeled) 55150-187-03
Product NDC 55150-187
11-digit billing NDC 55150018703
NCPDP billing unit ML — per mL (volume)
RxCUI 849931
UNII U26EO4675Q
UPC 0355150187034
Application # ANDA205013
SPL Set ID 8ef448ca-5549-4272-a6b4-5c4f57653c4c
Established class (EPC) Central Nervous System Stimulant; Methylxanthine
Physiologic effect Central Nervous System Stimulation
Chemical class Xanthines
DEA schedule Non-controlled
Marketing category ANDA
Marketing status On market
FDA listing status Listed (active directory)
Marketing start 2015-09-22
Route INTRAVENOUS
Dosage form INJECTION, SOLUTION
Substance CAFFEINE CITRATE
GPI-14 61300010102020
GPI class Caffeine Citrate
GCN Seq No 043901
GCN 50748
HICL code 000011
Ingredient (HICL) Caffeine Citrate
HIC1 code A
Therapeutic class — broad (HIC1) Cardiovascular System
HIC2 code A1
Therapeutic class — intermediate (HIC2) Cardiac Stimulants
HIC3 code A1B
Therapeutic class — specific (HIC3) Xanthines
AHFS code 28:20.32.00
AHFS class Respiratory And Cns Stimulants
FDB label name CAFFEINE CIT 60 MG/3 ML VIAL
FDB brand name Caffeine Citrate
Legend status F — Federal legend — prescription drug or device
Why two NDCs? The FDA registers this code as 55150-187-03 — a 5-3-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the product segment → 55150-0187-03. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

🏷️ RxNorm drug class

This medicine belongs to the Central Nervous System Stimulant class.

Pharmacologic class Central Nervous System Stimulant, Methylxanthine
Drug family (ATC) Tests for gastric secretion, Other dermatologicals, Xanthine derivatives
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

🏭 Manufacturer & labeler

LabelerEugia US LLC
Application holderEUGIA PHARMA SPECIALITIES LTD
FDA applicationANDA205013 (ANDA)
Labeler code55150
First marketedSep 2015
Product typeHuman Prescription Drug
Portfolio241 products on file
The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

🩺 Clinical

Label name CAFFEINE CIT 60 MG/3 ML VIAL Ingredient Caffeine Citrate
📗 Our plain-language guide HelloPharmacist
  • Caffeine citrate is a prescription medicine given in the hospital to premature babies who have apnea of prematurity — that means they sometimes stop breathing for short periods, wh...
  • What exactly is caffeine citrate used for in babies, and is it safe?
  • The medical team will be monitoring your baby closely, but it helps to know the signs to watch for. The most serious concern is necrotizing enterocolitis (NEC) — a severe intestina...
  • What side effects should I watch for in my premature baby on caffeine citrate?
📖 Read our full Caffeine guide →
1
Nutrient depletion considerations

Caffeine (OTC drug) may be associated with lower levels of 1 nutrient — worth a chat with your pharmacist, not a cause for alarm.

An association is not a deficiency. Educational only — don't start or stop anything without professional guidance.
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

🧪 Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.

  • 5 mg / 1 mL UNII 2968PHW8QP
    A weak organic acid derived from citrus fruits or made through fermentation. It works as a buffer to control pH, a preservative to extend shelf life, and a flavoring agent in medications.
  • 8.3 mg / 1 mL UNII B22547B95K
    A salt derived from citric acid that helps maintain the proper acid-base balance in the medicine. It's used as a buffer to keep the product stable and at the right pH level.
  • UNII 059QF0KO0R
    Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.

3 inactive ingredients listed in the exact product block matched to this NDC.

Where does this data come from?
Data sourced from official FDA Structured Product Labeling (SPL) via DailyMedingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

💲 Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer mLPer package
Retail pharmacies payNADAC · weekly Not in the retail survey — common for institutional, discontinued, or low-volume packs.
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · quarterly No Part D plan price is available for this NDC in our data.
ℹ️
No price is published for this exact package yet. CMS surveys NADAC per package size, so a different pack of the same drug often has one.
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

🔁 Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
Caffeine Citrate 20 mg/mL 00641-6267-10 Hikma 10 vials AP FDA listed
caffeine citrate 20 mg/mL 25021-0601-03 Sagent 1 vial AP FDA listed
Caffeine Citrate 60 mg/3mL 42571-0244-98 Micro 1 vial AP FDA listed
Caffeine Citrate 20 mg/mL 47335-0289-27 Sun 1 vial FDA listed
caffeine citrate 20 mg/mL 51754-0500-01 Exela 1 vial AP FDA listed
Caffeine Citrate 20 mg/mLthis 55150-0187-03 Eugia 1 vial FDA listed
Caffeine Citrate 20 mg/mL 63323-0407-03 Fresenius 1 vial AP FDA listed
Caffeine Citrate 60 mg/3mL 72485-0104-01 Armas 1 vial AP FDA listed
About this product: this is a generic version of the medicine. FDA equivalence ratings are shown when available, and other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2015
On the market since
Sep 2015
📍
2026
Currently FDA-listed
11 years listed
🔓
·
Generic on the market
this product is a generic
This is a generic drug

This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.

Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

🔬 Reported adverse events (FAERS)

Read carefully: FAERS reports are voluntary and unverified. Counts are not incidence, do not establish causation, are subject to reporting bias, and cannot be used to compare one drug to another. Shown for signal context only. Reports for Caffeine Citrate — the ingredient across all brands.

Top reported reactions

Pemphigus989
Hepatic Enzyme Increased953
Glossodynia948
Pericarditis945
Alopecia937
Hand Deformity928
Joint Swelling926

Age at onset

Neonate79
Infant10
Adolescent1
Adult329
Elderly36

Reporter sex

2,260 reports

Serious outcomes

Life-threatening1,225
Death1,172
Disabling1,171
Hospitalization1,094
Reports over time (by year) — tap or hover for the count & year
2019 2021 2023 2026 408 0
Most recent year is provisional (FAERS lags ~3 months).
Where does this data come from?
Adverse-event reports from the FDA Adverse Event Reporting System (FAERS) via openFDA. FAERS reports are voluntary and unverified — counts are not incidence and don’t establish causation.

📦 Packaging — all sizes for this product

Package NDCDescription Marketing startStatus
55150-0187-03 You're viewing this 1 VIAL, SINGLE-DOSE in 1 CARTON (55150-187-03) / 3 mL in 1 VIAL, SINGLE-DOSE 2015-09-22 Active

🧭 About this NDC listing & data coverage

Finished prescription product
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos ✓ Available
Inactive ingredients (structured) ✓ Available
NADAC pharmacy acquisition price (CMS) — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey.
Orange Book / therapeutic-equivalence data — Not published for this NDC Applies only to products approved under an NDA/ANDA; many listings are out of scope.
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

Why is there no price listed?
The pricing shown on our NDC pages comes from CMS NADAC, a voluntary survey of retail community pharmacy invoices. CMS does not publish a NADAC for every NDC — packages outside the retail survey (institutional and hospital products, bulk packages, discontinued items, and many OTC items) may never receive one. A missing price reflects the survey's scope, not this product's actual cost, and does not mean the product is free or unavailable.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The FDA registers it as 55150-187-03, which is what is printed on the packaging and shown on DailyMed. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero: 55150-0187-03, written without dashes as 55150018703. The Identity section at the top of this page lists every form of this code.
What do the three segments of this NDC mean?
In 55150-0187-03, the first segment (55150) is the labeler code FDA assigned to Eugia US LLC; the middle segment (0187) identifies this specific product — its ingredient, strength, and dosage form; and the last segment (03) identifies this exact package size and type. Together they name one specific package of one specific product.
Is this package still being marketed?
Yes, per the latest FDA NDC Directory data on this page: this package is listed as actively marketed, with no marketing end date reported by Eugia US LLC. Listing status can change — the directory data on this page refreshes weekly.
Who lists this product with the FDA?
Eugia US LLC is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.

📄 Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage 16 words

INDICATIONS AND USAGE Caffeine citrate injection, USP is indicated for the treatment of apnea of prematurity.

⏱️ Dosage and Administration ~2 min read

DOSAGE AND ADMINISTRATION Prior to initiation of caffeine citrate injection USP, baseline serum levels of caffeine should be measured in infants previously treated with theophylline, since preterm infants metabolize theophylline to caffeine. Likewise, baseline serum levels of caffeine should be measured in infants born to mothers who consumed caffeine prior to delivery, since caffeine readily crosses the placenta. The recommended loading dose and maintenance doses of caffeine citrate injection, USP follow. * Using a syringe infusion pump ** Beginning 24 hours after the loading dose Dose of Caffeine Citrate Injection, USP Volume Dose of Caffeine Citrate Injection, USP mg/kg Route Frequency Loading Dose 1 mL/kg 20 mg/kg Intravenous * (over 30 minutes) One time Maintenance Dose 0.25 mL/kg 5 mg/kg Intravenous * (over 10 minutes) or Orally Every 24 hours ** NOTE THAT THE DOSE OF CAFFEINE BASE IS ONE-HALF THE DOSE WHEN EXPRESSED AS CAFFEINE CITRATE (e.g., 20 mg of caffeine citrate is equivalent to 10 mg of caffeine base).

Serum concentrations of caffeine may need to be monitored periodically throughout treatment to avoid toxicity. Serious toxicity has been associated with serum levels greater than 50 mg/L. Caffeine citrate injection, USP should be inspected visually for particulate matter and discoloration prior to administration.

Vials containing discolored solution or visible particulate matter should be discarded. Drug Compatibility To test for drug compatibility with common intravenous solutions or medications, 20 mL of caffeine citrate injection, USP were combined with 20 mL of a solution or medication, with the exception of an Intralipid ® admixture, which was combined as 80 mL/80 mL. The physical appearance of the combined solutions was evaluated for precipitation.

The admixtures were mixed for 10 minutes and then assayed for caffeine. The admixtures were then continually mixed for 24 hours, with further sampling for caffeine assays at 2, 4, 8, and 24 hours. Based on this testing, caffeine citrate injection USP, 60 mg/3 mL is chemically stable for 24 hours at room temperature when combined with the following test products. • Dextrose Injection, USP 5% • 50% Dextrose Injection USP • Intralipid ® 20% IV Fat Emulsion • Aminosyn ® 8.5% Crystalline Amino Acid Solution • Dopamine HCI Injection, USP 40 mg/mL diluted to 0.6 mg/mL with Dextrose Injection, USP 5% • Calcium Gluconate Injection, USP 10% (0.465 mEq/Ca +2 /mL) • Heparin Sodium Injection, USP 1000 units/mL diluted to 1 unit/mL with Dextrose Injection, USP 5% • Fentanyl Citrate Injection, USP 50 mcg/mL diluted to 10 mcg/mL with Dextrose Injection, USP 5%

Contraindications 17 words

CONTRAINDICATIONS Caffeine citrate injection is contraindicated in patients who have demonstrated hypersensitivity to any of its components.

⚠️ Warnings 139 words

WARNINGS Necrotizing Enterocolitis During the double-blind, placebo-controlled clinical trial, 6 cases of necrotizing enterocolitis developed among the 85 infants studied (caffeine=46, placebo=39), with 3 cases resulting in death. Five of the six patients with necrotizing enterocolitis were randomized to or had been exposed to caffeine citrate. Reports in the published literature have raised a question regarding the possible association between the use of methylxanthines and development of necrotizing enterocolitis, although a causal relationship between methylxanthine use and necrotizing enterocolitis has not been established.

In a published randomized, placebo-controlled, clinical trial that studied the use of caffeine citrate in apnea of prematurity in approximately 2,000 patients, necrotizing enterocolitis was not more common in caffeine treated patients compared to placebo. As with all preterm infants, patients being treated with caffeine citrate should be carefully monitored for the development of necrotizing enterocolitis.

🤒 Adverse Reactions ~2 min read

ADVERSE REACTIONS Overall, the reported number of adverse events in the double-blind period of the controlled trial was similar for the caffeine citrate and placebo groups. The following table shows adverse events that occurred in the double-blind period of the controlled trial and that were more frequent in caffeine citrate-treated patients than placebo. ADVERSE EVENTS THAT OCCURRED MORE FREQUENTLY IN CAFFEINE CITRATE-TREATED PATIENTS THAN PLACEBO DURING DOUBLE-BLIND THERAPY Adverse Event (AE) Caffeine Citrate N=46 n (%) Placebo N=39 n (%) BODY AS A WHOLE Accidental Injury 1 (2.2) 0 (0) Feeding Intolerance 4 (8.7) 2 (5.1) Sepsis 2 (4.3) 0 (0) CARDIOVASCULAR SYSTEM Hemorrhage 1 (2.2) 0 (0) DIGESTIVE SYSTEM Necrotizing Enterocolitis 2 (4.3) 1 (2.6) Gastritis 1 (2.2) 0 (0) Gastrointestinal Hemorrhage 1 (2.2) 0 (0) HEMIC AND LYMPHATIC SYSTEM Disseminated Intravascular Coagulation 1 (2.2) 0 (0) METABOLIC AND NUTRITIVE DISORDERS Acidosis 1 (2.2) 0 (0) Healing Abnormal 1 (2.2) 0 (0) NERVOUS SYSTEM Cerebral Hemorrhage 1 (2.2) 0 (0) RESPIRATORY SYSTEM Dyspnea 1 (2.2) 0 (0) Lung Edema 1 (2.2) 0 (0) SKIN AND APPENDAGES Dry Skin 1 (2.2) 0 (0) Rash 4 (8.7) 3 (7.7) Skin Breakdown 1 (2.2) 0 (0) SPECIAL SENSES Retinopathy of Prematurity 1 (2.2) 0 (0) UROGENITAL SYSTEM Kidney Failure 1 (2.2) 0 (0) In addition to the cases above, three cases of necrotizing enterocolitis were diagnosed in patients receiving caffeine citrate during the open-label phase of the study.

Three of the infants who developed necrotizing enterocolitis during the trial died. All had been exposed to caffeine. Two were randomized to caffeine, and one placebo patient was “rescued” with open-label caffeine for uncontrolled apnea.

Adverse events described in the published literature include: central nervous system stimulation (i.e., irritability, restlessness, jitteriness), cardiovascular effects (i.e., tachycardia, increased left ventricular output, and increased stroke volume), gastrointestinal effects (i.e., increased gastric aspirate, gastrointestinal intolerance), alterations in serum glucose (i.e., hypoglycemia and hyperglycemia), and renal effects (i.e., increased urine flow rate, increased creatinine clearance, and increased sodium and calcium excretion).

Published long-term follow-up studies have not shown caffeine to adversely affect neurological development or growth parameters. A published randomized, placebo-controlled, clinical trial in premature infants with birthweights of 500 to 1,250 grams studied the safety of caffeine citrate in apnea of prematurity (NCT00182312). This trial randomized approximately 2,000 premature infants with a mean gestational age of 27 weeks at birth.

The median duration of caffeine therapy was 37 days. Prior to discharge home, death, ultrasonographic signs of brain injury, and necrotizing enterocolitis were not more common in the caffeine citrate group compared to the placebo. At follow up at both 18 months and 5 years corrected age, death was not more common in the caffeine citrate treated group compared to placebo, nor did caffeine citrate use adversely affect neurodevelopmental outcomes.

🔄 Drug Interactions 139 words

Drug Interactions Cytochrome P450 1A2 (CYP1A2) is known to be the major enzyme involved in the metabolism of caffeine. Therefore, caffeine has the potential to interact with drugs that are substrates for CYP1A2, inhibit CYP1A2, or induce CYP1A2. Few data exist on drug interactions with caffeine in preterm neonates.

Based on adult data, lower doses of caffeine may be needed following coadministration of drugs which are reported to decrease caffeine elimination (e.g., cimetidine and ketoconazole) and higher caffeine doses may be needed following coadministration of drugs that increase caffeine elimination (e.g., phenobarbital and phenytoin). Caffeine administered concurrently with ketoprofen reduced the urine volume in four healthy volunteers. The clinical significance of this interaction in preterm neonates is not known.

Interconversion between caffeine and theophylline has been reported in preterm neonates. The concurrent use of these drugs is not recommended.

🤰 Pregnancy 77 words

Pregnancy Concern for the teratogenicity of caffeine is not relevant when administered to infants. In studies performed in adult animals, caffeine (as caffeine base) administered to pregnant mice as sustained release pellets at 50 mg/kg (less than the maximum recommended intravenous loading dose for infants on a mg/m 2 basis), during the period of organogenesis, caused a low incidence of cleft palate and exencephaly in the fetuses. There are no adequate and well-controlled studies in pregnant women.

🆘 Overdosage 218 words

OVERDOSAGE Following overdose, serum caffeine levels have ranged from approximately 24 mg/L (a postmarketing spontaneous case report in which an infant exhibited irritability, poor feeding, and insomnia) to 350 mg/L. Serious toxicity has been associated with serum levels greater than 50 mg/L (see PRECAUTIONS, Laboratory Tests and DOSAGE AND ADMINISTRATION ). Signs and symptoms reported in the literature after caffeine overdose in preterm infants include fever, tachypnea, jitteriness, insomnia, fine tremor of the extremities, hypertonia, opisthotonos, tonic-clonic movements, nonpurposeful jaw and lip movements, vomiting, hyperglycemia, elevated blood urea nitrogen, and elevated total leukocyte concentration.

Seizures have also been reported in cases of overdose. One case of caffeine overdose complicated by development of intraventricular hemorrhage and long-term neurological sequelae has been reported. Another case of caffeine citrate overdose (from New Zealand) of an estimated 600 mg caffeine citrate (approximately 322 mg/kg) administered over 40 minutes was complicated by tachycardia, ST depression, respiratory distress, heart failure, gastric distention, acidosis, and a severe extravasation burn with tissue necrosis at the peripheral intravenous injection site.

No deaths associated with caffeine overdose have been reported in preterm infants. Treatment of caffeine overdose is primarily symptomatic and supportive. Caffeine levels have been shown to decrease after exchange transfusions.

Convulsions may be treated with intravenous administration of diazepam or a barbiturate such as pentobarbital sodium.

🧬 Clinical Pharmacology ~3 min read

CLINICAL PHARMACOLOGY 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.

These include: (1) stimulation of the respiratory center, (2) increased minute ventilation, (3) decreased threshold to hypercapnia, (4) increased response to hypercapnia, (5) increased skeletal muscle tone, (6) decreased diaphragmatic fatigue, (7) increased metabolic rate, and (8) increased oxygen consumption. Most of these effects have been attributed to antagonism of adenosine receptors, both A 1 and A 2 subtypes, by caffeine, which has been demonstrated in receptor binding assays and observed at concentrations approximating those achieved therapeutically.

Pharmacokinetics Absorption After oral administration of 10 mg caffeine base/kg to preterm neonates, the peak plasma level (C max ) for caffeine ranged from 6 to 10 mg/L and the mean time to reach peak concentration (T max ) ranged from 30 minutes to 2 hours. The T max was not affected by formula feeding. The absolute bioavailability, however, was not fully examined in preterm neonates.

Distribution Caffeine is rapidly distributed into the brain. Caffeine levels in the cerebrospinal fluid of preterm neonates approximate their plasma levels. The mean volume of distribution of caffeine in infants (0.8 to

0.9L/kg) is slightly higher than that in adults (0.6 L/kg). Plasma protein binding data are not available for neonates or infants. In adults, the mean plasma protein binding in vitro is reported to be approximately 36%.

Metabolism Hepatic cytochrome P450 1A2 (CYP1A2) is involved in caffeine biotransformation. Caffeine metabolism in preterm neonates is limited due to their immature hepatic enzyme systems. Interconversion between caffeine and theophylline has been reported in preterm neonates; caffeine levels are approximately 25% of theophylline levels after theophylline administration and approximately 3 to 8% of caffeine administered would be expected to convert to theophylline.

Elimination In young infants, the elimination of caffeine is much slower than that in adults due to immature hepatic and/or renal function. Mean half-life (T 1/2 ) and fraction excreted unchanged in urine (A e ) of caffeine in infants have been shown to be inversely related to gestational/postconceptual age. In neonates, the T 1/2 is approximately 3 to 4 days and the A e is approximately 86% (within 6 days).

By 9 months of age, the metabolism of caffeine approximates that seen in adults (T 1/2 = 5 hours and A e = 1%). Special Populations Studies examining the pharmacokinetics of caffeine in neonates with hepatic or renal insufficiency have not been conducted. Caffeine citrate should be administered with caution in preterm neonates with impaired renal or hepatic function.

Serum concentrations of caffeine should be monitored and dose administration of caffeine citrate should be adjusted to avoid toxicity in this population. Clinical Studies One multicenter, randomized, double-blind trial compared caffeine citrate to placebo in eighty-five (85) preterm infants (gestational age 28 to <33 weeks) with apnea of prematurity. Apnea of prematurity was defined as having at least 6 apnea episodes of greater than 20 seconds duration in a 24-hour period with no other identifiable cause of apnea.

A 1 mL/kg (20 mg/kg caffeine citrate providing 10 mg/kg as caffeine base) loading dose of caffeine citrate was administered intravenously, followed by a 0.25 mL/kg (5 mg/kg caffeine citrate providing 2.5 mg/kg of caffeine base) daily maintenance dose administered either intravenously or orally (generally through a feeding tube). The duration of treatment in this study was limited to 10 to 12 days. The protocol allowed infants to be “rescued” with open-label caffeine…

📦 How Supplied / Storage and Handling 185 words

HOW SUPPLIED Caffeine citrate injection, USP is available as a clear, colorless, sterile, non-pyrogenic, preservative-free, aqueous solution in 5 mL colorless glass vial. The vials are sealed with a gray rubber stopper and an aluminum overseal with a white polypropylene disk inset. The vials contain 3 mL solution at a concentration of 20 mg/mL caffeine citrate (60 mg/vial) equivalent to 10 mg/mL caffeine base (30 mg/vial).

Caffeine citrate injection, USP is supplied as: 3 mL Single-Dose Vial, individually packaged in a carton. NDC 55150-187-03 Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. The vial stopper is not made with natural rubber latex.

Preservative free. For single-dose only. Discard unused portion .

Intralipid ® is a registered trademark of Fresenius Kabi AB. Aminosyn ® is a registered trademark of Hospira, Inc. To report SUSPECTED ADVERSE REACTIONS, contact Eugia US LLC at 1-866-850-2876 or eugiaus.com or the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

For Product Inquiry call 1-866-850-2876. Distributed by: Eugia US LLC 279 Princeton-Hightstown Rd. E.

Windsor, NJ 08520 Manufactured by: Eugia Pharma Specialities Limited Hyderabad - 500032 India Revised: April 2025

📋 Description 127 words

DESCRIPTION Caffeine citrate injection, USP for intravenous administration is a clear, colorless, sterile, non-pyrogenic, preservative-free, aqueous solution adjusted to pH 4.7. Each mL contains 20 mg caffeine citrate (equivalent to 10 mg of caffeine base) prepared in solution by the addition of 10 mg caffeine (anhydrous) USP to 5 mg citric acid monohydrate, 8.3 mg sodium citrate dihydrate and Water for Injection, USP. Caffeine (anhydrous) USP, a central nervous system stimulant, is an odorless white crystalline powder or granules, with a bitter taste.

It is sparingly soluble in water and ethanol at room temperature. The chemical name of caffeine is 3,7-dihydro-1,3,7-trimethyl-1 H- purine-2,6-dione. In the presence of citric acid it forms caffeine citrate salt in solution.

The structural formula and molecular weight of caffeine citrate follows. checmical-structure

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗
For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.