caffeine citrate

Therapeutic Classification: central nervous system stimulants

Pharmacologic Classification: respiratory stimulants

Indications ⬆ ⬇

REMS

Short-term treatment of idiopathic apnea of prematurity in infants between 28 and <33 wk gestational age.

Action ⬆ ⬇

Increases levels of cyclic AMP by inhibiting phosphodiesterase.
Acts as a bronchial smooth muscle relaxant.
Suggested mechanisms of action include:
- Stimulation of the respiratory center,
- Increased minute ventilation,
- Decreased threshold to hypercapnea,
- Increased response to hypercapnea,
- Increased skeletal muscle tone,
- Decreased diaphragmatic fatigue,
- Increased metabolic rate,
- Increased oxygen consumption.

Therapeutic effects:

Decrease in periods of apnea.

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability; also absorbed after oral administration.

Distribution: Rapidly distributes to the brain; CSF levels in neonates are similar to plasma levels.

Metabolism/Excretion: Mostly metabolized by the liver by the CYP1A2 isoenzyme; 3–8% converted to theophylline.

Half-Life: Infants >9 mo, Children, and Adults: 5 hr; Neonates: 3–4 days.

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
IV	rapid	end of infusion	24 hr
PO	rapid	30 min–2 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity.

Use Cautiously in:

History of seizure disorders;
History of cardiovascular disease;
Pedi: ↑risk of toxicity in neonates with hepatic or renal impairment.

Adv. Reactions/Side Effects ⬆ ⬇

CV: tachycardia

Derm: dry skin, rash, skin breakdown

Endo: hyperglycemia, hypoglycemia

GI: GI bleeding, feeding intolerance, gastritis, NECROTIZING ENTEROCOLITIS

GU: increased urine output

MS: muscle tremors, twitches

Neuro: insomnia, irritability, jitteriness, restlessness

Interactions ⬆ ⬇

Drug-drug:

Cimetidine, fluconazole, and ketoconazole↓ metabolism (dose reduction of caffeine may be necessary).
Phenobarbital and phenytoin may ↑ caffeine metabolism (↑ doses of caffeine may be necessary).
Because caffeine is a significant metabolite of theophylline, concurrent administration is not recommended.

Route/Dosage ⬆ ⬇

IV (Neonates ): Loading dose: 20 mg/kg caffeine citrate (10 mg/kg caffeine base).
IV PO (Neonates ): Maintenance dose: starting 24 hr after loading dose 5 mg/kg caffeine citrate (2.5 mg/kg caffeine base) every 24 hr.

Availability ⬆ ⬇

(Generic available)

Solution for injection: 20 mg/mL caffeine citrate (10 mg/mL caffeine base)
Oral solution: 20 mg/mL caffeine citrate (10 mg/mL caffeine base)

Assessment ⬆ ⬇

Assess respiratory status frequently throughout therapy.
Monitor patient for signs of necrotizing enterocolitis (abdominal distension, vomiting, bloody stools, lethargy). May be fatal.

Lab Test Considerations:

Monitor serum caffeine levels before and periodically during therapy in infants previously treated with theophylline or in infants whose mothers consumed caffeine before delivery.
- Monitor serum glucose levels. May cause hypoglycemia or hyperglycemia.
Therapeutic range: 8–20 mcg/mL.

Toxicity and Overdose:

Serum caffeine levels of >50 mcg/mL have been associated with serious toxicity. Monitor serum levels and adjust dose in neonates with impaired hepatic or renal function to avoid toxicity.

Implementation ⬆ ⬇

PO: Maintenance doses may also be administered orally.

IV Administration:

Intermittent Infusion: Solution should be clear, without particulate matter.
Rate: Initial loading dose should be administered over 30 min. Maintenance doses may be administered over 10 min every 24 hr beginning 24 hr after loading dose. Syringe pump should be used to ensure accurate delivery.
Y-Site Compatibility:
- blinatumomab
- doxapram
- ketamine
- LR
- levofloxacin
- meropenem
- naloxone
Y-Site Incompatibility:
- ibuprofen lysine
- pantoprazole

Patient/Family Teaching ⬆ ⬇

Instruct parent on correct technique for administration. Measure oral dose accurately with a 1-mL syringe. If apnea events continue, consult health care professional; do not increase dose.
Advise parent to consult health care professional immediately if signs of necrotizing enterocolitis occur.

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Pronunciation ⬇

Classifications ⬆ ⬇