Caffeine

FDA label, Hikma Pharmaceuticals USA Inc., intravenous, effective 2024-04-08. Full label on DailyMed

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From MedlinePlus, U.S. National Library of Medicine

Quoted from the FDA label. Product labels differ by manufacturer and change over time; confirm against the label for the product you are using.

Dosing in kidney impairment

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Preparation and administration

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Basis

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The recommended loading dose and maintenance doses of caffeine citrate follow. [See table below.] *Using a syringe infusion pump **Beginning 24 hours after the loading dose 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 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 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, 60 mg/3 mL is chemically stable for 24 hours at room temperature when combined with the following test products.

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% 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%

Dose of Caffeine Citrate VolumeDose of Caffeine Citrate mg/kgRouteFrequency
Loading Dose1 mL/kg 20 mg/kgIntravenous* (over 30 minutes)One time
Maintenance Dose0.25 mL/kg 5 mg/kgIntravenous* (over 10 minutes) or OrallyEvery 24 hours**

Drug interactions

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Label text (2 paragraphs)

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.

Contraindications

Caffeine Citrate Injection is contraindicated in patients who have demonstrated hypersensitivity to any of its components.

Pregnancy and lactation

Pregnancy

Pregnancy Pregnancy Category C 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.

For breastfeeding, also see LactMed (National Library of Medicine), which summarizes milk levels and infant effects.

Supply and cost

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