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Mechanism of Action
Increases calcium permeability in sarcoplasmic reticulum, inhibiting phosphodiesterase-promoting accumulation of cyclic AMP.
99% absorbed orally. C max is 5 to 25 mcg/mL; T max is 15 to 120 min.
Rapidly distributed throughout tissues; crosses the blood-brain barrier and placenta; excreted in breast milk. 17% to 36% protein bound. Vd is 0.64 kg.
Rapidly metabolized in the liver to 1-methyluric acid, 1-methylxanthine, and 7-methylxanthine; CYP1A2 is involved in the biotransformation.
The t ½ is 3 to 5 h. Approximately 1% is excreted in the urine as unchanged drug.
Special PopulationsPregnancy, smoking, and cirrhosis
The t ½ is increased.
Indications and Usage
Fatigue and drowsiness; analgesia; apnea of prematurity; respiratory depression.
Caffeine and sodium benzoate solution in pediatrics.
Dosage and AdministrationFatigue/Drowsiness
Adults and children (older than 12 yr of age)
PO 100 to 200 mg every 3 to 4 h as needed.Apnea of Prematurity
Preterm infants Loading dose (caffeine citrate)
IV 20 mg/kg (1 mL/kg) over 30 min once.Maintenance dose (caffeine citrate)
IV (over 10 min) or PO 5 mg/kg (0.25 mL/kg) every 24 h.
Store capsules, tablets, lozenges, and oral solution at controlled room temperature (59° to 86°F). Keep oral solution tightly capped. Citrated caffeine parenteral solution may be stored for up to 24 h at room temperature following dilution.
Drug InteractionsAspirin, clozapine, theophylline
Plasma levels of these agents may be elevated by caffeine, increasing their pharmacologic effects and adverse reactions.Cimetidine, disulfiram, fluoroquinolones, mexiletine, oral contraceptives
May increase caffeine levels, enhancing the effects.Lithium
Plasma levels may be reduced by caffeine, decreasing the pharmacologic effect.Phenytoin, smoking
May decrease caffeine levels.
Laboratory Test Interactions
False-positive elevations in serum urate measured by Bittner method; may increase urine levels of vanillymandelic acid, catecholamines, and 5-hydroxyindoleacetic acid, resulting in false-positive diagnosis of pheochromocytoma and neuroblastoma.
Tachycardia; extrasystoles; palpitations; other cardiac arrhythmias.
Insomnia; restlessness; excitement; nervousness; tinnitus; scintillating scotoma; muscular tremor; headache; lightheadedness.
Urticaria; rash, dry skin, skin breakdown (caffeine citrate).
Retinopathy of prematurity (caffeine citrate).
Vomiting; nausea; diarrhea; stomach pain; necrotizing enterocolitis, gastritis, GI hemorrhage (caffeine citrate).
Diuresis; kidney failure (caffeine citrate).
Disseminated intravascular coagulation (caffeine citrate).
Hyperglycemia; acidosis (caffeine citrate).
Dyspnea, lung edema (caffeine citrate).
Hypersensitivity (eg, dermatitis, rhinitis, bronchial asthma); feeding intolerance, sepsis, accidental injury, hemorrhage, cerebral hemorrhage (caffeine citrate).
Category C .
Excreted in breast milk.
Caffeine and sodium benzoate injection is contraindicated in children.
Other methylxanthines have been associated with development of necrotizing enterocolitis.
Too-vigorous treatment with parenteral caffeine can worsen depression.
Caffeine may aggravate diarrhea in patients with irritable colon or exacerbate duodenal ulcers.
Seizures have been reported with caffeine overdose; use caffeine citrate with caution in infants with seizure disorders.
Caffeine can increase heart rate, left ventricular output, and stroke volume; use caffeine citrate with caution in infants with CV disease.
Caffeine stimulates glycogenolysis and lipolysis, which increases free fatty acids and produces hyperglycemia.
Bone mineral density
Caffeine is associated with decreased bone density.
Symptoms may occur within 12 h after cessation of chronic caffeine ingestion and persist up to 7 days.
Vomiting, myoclonus, agitation, myocardial irritability, cardiac arrhythmia, seizures, hematemesis, opisthotonus, decerebrate posturing, generalized muscular hypertonicity, rhabdomyolysis with renal failure, pulmonary edema, hyperglycemia; hypokalemia, leukocytosis, ketosis, metabolic acidosis, death.
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