CAFFEINE CITRATE solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Caffeine Citrate (UNII: U26EO4675Q) (Caffeine - UNII:3G6A5W338E)

Available from:

Exela Pharma Sciences, LLC

INN (International Name):

Caffeine Citrate

Composition:

Caffeine Citrate 20 mg in 1 mL

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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. Caffeine citrate injection and caffeine citrate oral solution are contraindicated in patients who have demonstrated hypersensitivity to any of its components.

Product summary:

Both caffeine citrate Injection and caffeine citrate oral solution are available as clear, colorless, sterile, nonpyrogenic, preservative-free, aqueous solutions in 3 mL colorless glass vials. The vials of caffeine citrate injection are sealed with a teflon-faced gray rubber stopper and an aluminum overseal with a white flip-off polypropylene disk inset. The vials of caffeine citrate oral solution are sealed with a teflon-faced gray rubber stopper and a peel-off aluminum overseal with a blue flip-off polypropylene disk inset. Both the injection and oral solution 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 NDC 51754-0500-1: 3 mL vial, individually packaged in a carton. Caffeine citrate oral solution, USP NDC 51754-0501-2: 3 mL vial (NOT CHILD-RESISTANT), 5 vials per white polypropylene child- resistant container. NDC 51754-0501-3: 3 mL vial (NOT CHILD-RESISTANT), 10 vials per white polypropylene child-resistant container. Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Preservative free. For single use only. Discard unused portion. ATTENTION PHARMACIST: Detach "Instructions for Use" from the package insert and dispense with caffeine citrate oral solution prescription. Manufactured and Distributed by: Exela Pharma Sciences, LLC Lenoir, NC 28645 USA Revised: May 2018

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

CAFFEINE CITRATE- CAFFEINE CITRATE SOLUTION
EXELA PHARMA SCIENCES, LLC
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DESCRIPTION
Both caffeine citrate injection for intravenous administration and
caffeine citrate oral solution are clear,
colorless, sterile, non-pyrogenic, preservative-free, aqueous
solutions 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 to 5.0 mg citric acid
monohydrate, 8.3 mg sodium citrate
dihydrate and Water for Injection.
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
Absorption
After oral administration of 10 mg caffeine base/kg to preterm
neonates, the peak plasma level (C
)
1
2
After oral administration of 10 mg caffeine b