caffeine citrate

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caffeine citrate

(ka-feensi-trate) ,


(trade name)


Therapeutic: central nervous system stimulants
Pharmacologic: respiratory stimulants
Pregnancy Category: C


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


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.


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 and Excretion: Mostly metabolized by the liver (cytochrome P450 1A2) enzymes; 3–8% converted to theophylline.
Half-life: Infants >9 mo, Children, and Adults: 5 hr; Neonates—3–4 days.

Time/action profile

IVrapidend of infusion24 hr
POrapid30 min–2 hr24 hr


Contraindicated in: Hypersensitivity.
Use Cautiously in: History of seizure disorders;History of cardiovascular disease; Pediatric: Increased risk of toxicity in neonates with impaired hepatic or renal function.

Adverse Reactions/Side Effects

Central nervous system

  • insomnia
  • irritability
  • jitteriness
  • restlessness


  • tachycardia


  • necrotizing enterocolitis (life-threatening)
  • feeding intolerance
  • gastritis
  • GI bleeding


  • increased urine output


  • dry skin
  • rash
  • skin breakdown


  • hypoglycemia
  • hyperglycemia


  • muscle tremors
  • twitches


Drug-Drug interaction

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.


Intravenous (Neonates) Loading dose—20 mg/kg caffeine citrate (10 mg/kg caffeine base).
Intravenous Oral (Neonates) Maintenance dose—starting 24 hr after loading dose 5 mg/kg caffeine citrate (2.5 mg/kg caffeine base) q 24 hr.

Availability (generic available)

Solution for injection: 20 mg/mL caffeine citrate (10 mg/mL caffeine base) in 3-mL vials
Oral solution: 20 mg/mL caffeine citrate (10 mg/mL caffeine base) in 3-mL vials

Nursing implications

Nursing 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.
  • Lab Test Considerations: Therapeutic range: 8–20 mcg/mL.
  • 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.

Potential Nursing Diagnoses

Ineffective breathing pattern (Indications)


  • Oral: Maintenance doses may also be administered orally.
  • Intravenous Administration
  • pH: 4.7.
  • 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.
  • Syringe Compatibility: alprostadil, amikacin, aminophylline, calcium gluconate, cefotaxime, cimetidine, clindamycin, dexamethasone, dobutamine, dopamine, epinephrine, fentanyl, gentamicin, heparin, isoproterenol, lidocaine, metoclopramide, morphine, nitroprusside, pancuronium, penicillin G, phenobarbital, phenylephrine, sodium bicarbonate, vancomycin
  • Syringe Incompatibility: acyclovir, furosemide, lorazepam, nitroglycerin, oxacillin, pantoprazole
  • Y-Site Compatibility: doxapram, levofloxacin
  • Additive Compatibility: amino acids, calcium gluconate, D5W, D50W, dopamine, fat emulsion, heparin, fentanyl

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.

Evaluation/Desired Outcomes

  • Decrease in apneic episodes in premature infant.

caf·feine cit·rate

citrated caffeine, a mixture of equal parts of caffeine and citric acid; more water soluble than caffeine.
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Experts say they have no reports of Askit ingredients - aspirin, caffeine citrate and the antiinflammatory drug aloxiprin - causing physical addiction.
Theophylline has been most extensively used, but it has been suggested that caffeine citrate may be the agent of choice.
Spokeswoman Liz Griffith said: "The active ingredients include aspirin, aloxiprin and caffeine citrate.
Fein's formula is all-natural caffeine citrate and a suite of secret, 100-percent natural "taste erasers.
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Food and Drug Administration (FDA) of its Abbreviated New Drug Application (ANDA) for Caffeine Citrate Oral Solution, USP, 20 mg/ml, the equivalent of Bedford Laboratories' Cafcit([R]) Oral Solution.
Caffeine Citrate Oral Solution is indicated for the short term treatment of apnea of premature infants.
Food and Drug Administration (FDA) for its Abbreviated New Drug Application (ANDA) for Caffeine Citrate injection, USP, 20 mg/mL, the generic equivalent of Cafcit([R]) Injection manufactured by Mead Johnson and Company.
Caffeine Citrate Injection is indicated for the short term treatment of apnea of prematurity (AOP) in infants between 28 and <33 weeks gestational age.
This first-ever placebo-controlled study concluded that caffeine citrate proved significantly better than placebo in reducing apnea of prematurity episodes in infants between 28 to 32 weeks post-conception.
Each 3 mL single-dose vial contains a concentration of 20 mg/mL caffeine citrate (60 mg/vial).