CAFFEINE CITRATE injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

CAFFEINE CITRATE (UNII: U26EO4675Q) (CAFFEINE - UNII:3G6A5W338E)

Available from:

American Regent, Inc.

INN (International Name):

CAFFEINE CITRATE

Composition:

CAFFEINE CITRATE 20 mg in 1 mL

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Caffeine citrate injection is indicated for the treatment of apnea of prematurity. Caffeine citrate injection is contraindicated in patients who have demonstrated hypersensitivity to any of its components.

Product summary:

Caffeine citrate injection, USP is available as a clear, colorless, sterile, non-pyrogenic, preservative-free, aqueous solution in 5 mL colored glass vials. The vials contain 3 mL solution at a concentration of caffeine citrate 20 mg/mL (60 mg/vial) equivalent to caffeine base 10 mg/mL (30 mg/vial). Caffeine Citrate Injection, USP is supplied as: NDC 0517-0020-10                3 mL Single Dose Vial                Packages of 10 NDC 0517-0020-25                3 mL Single Dose Vial                Packages of 25 Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature]. Not made with natural rubber latex. Preservative Free. For single-dose only. Discard unused portion. To report SUSPECTED ADVERSE REACTIONS, contact American Regent, Inc. at 1-800-734-9236 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. For Product Inquiry call 1-800-354-4855. IN0020 Rev. 9/2020 AMERICAN REGENT, INC. SHIRLEY, NY  11967

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CAFFEINE CITRATE- CAFFEINE CITRATE INJECTION, SOLUTION
AMERICAN REGENT, INC.
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CAFFEINE CITRATE INJECTION, USP
RX ONLY
DESCRIPTION
Caffeine citrate injection, USP for intravenous administration, is a
clear, colorless, sterile, non-
pyrogenic, preservative-free, aqueous solution adjusted to pH 4.2 to
5.2. Each mL contains caffeine
citrate 20 mg (equivalent to 10 mg of caffeine base) prepared in
solution by the addition of caffeine
anhydrous 10 mg to citric acid monohydrate 5 mg, sodium citrate
dihydrate 8.3 mg and water for
injection q.s.
Caffeine, a central nervous system stimulant, is an odorless white
crystalline powder or granule, 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:
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 and A
subtypes, by caffeine, which has been demonstrated in receptor binding
assays and observed at
concentrations approximating those achieved therapeutically.
PHARMACOKINETICS
1
2
_Absorption:_
After oral administration of 10 mg caffeine base/kg to preterm
neonates, the peak plasma level (C
)
for caffeine ranged f