Caffeine

Indications
 Oral
Migraine
Adult: 100 mg in combination with ergotamine.
Oral
Mild stimulant of the central nervous system
Adult: 50-100 mg up to 200 mg. Not to be taken more often than 3 hrly.
Max Dosage: 1 g daily.
Intravenous
Short-term treatment of neonatal apnoea of prematurity
Child: As citrate: 20 mg/kg (equivalent to 10 mg/kg caffeine) via IV infusion. Maintenance: 5 mg/kg daily. May also be given orally.
Contraindications
 Hypersensitivity.
Warnings / Precautions
 Peptic ulceration; symptomatic cardiac arrhythmias and/or palpitations; 1st several days to wk after an acute MI; neonates; pregnancy; lactation.
Adverse Reactions
 Insomnia, restlessness, nervousness, mild delirium; nausea, vomiting, gastric irritation.
Drug Interactions
 Concurrent use may reduce the sedative/anxiolytic effect of benzodiazepines. Reduced levels when used with aminoglutethimide, carbamazepine, phenobarbital or rifampin. Increased levels when used with fluvoxamine, ketoconazole, rofecoxib, ciprofloxacin, norfloxacin or ofloxacin. β-adrenergic agonists, disulfiram, aspirin.
See Below for More caffeine Drug Interactions
Lab Interactions
 False-positive elevations of serum urate; slight increases in urine levels of vanillylmandelic acid and catecholamines which give rise to false-positive diagnosis of pheochromocytoma or neuroblastoma; slight increases in urine levels of 5-hydroxyindoleacetic acid.
Mechanism of Actions
 Caffeine, a methylxanthine, is a phosphodiesterase inhibitor. It has an antagonistic effect at central adenosine receptors. It is a CNS and resp stimulant. It has bronchodilating and diuretic properties and it facilitates the performance of muscular work.
Absorption: Readily absorbed after oral admin.
Distribution: Widely distributed throughout the body.
Metabolism: Metabolised almost completely hepatically via oxidation, demethylation and acetylation.
Excretion: Excreted in the urine as 1-methyluric acid, 1-methylxanthine, 7-methylxanthine, 1,7-dimethylxanthine, 5-acetylamino-6-formylamino-3-methyluracil and other metabolites with only about 1% unchanged.
Administration
 May be taken with or without food.
ATC Classification
 N06BC01 - caffeine ; Belongs to the class of xanthine derivative agents. Used as CNS stimulant.
Available As
  • Caffeine 1.5 mg
  • Caffeine 10 mg
  • Caffeine 100 mg
  • Caffeine Citrate 1186 mg
  • Caffeine 15 mg
  • Caffeine Citrate 15 mg
  • Caffeine 16 mg
  • Caffeine 20 mg
  • Caffeine Citrate 20 mg
  • Caffeine 25 mg
  • Caffeine Citrate 30 mg
  • Caffeine 30 mg
  • Caffeine 32 mg
  • Caffeine 35 mg
  • Caffeine 36.48 mg
  • Caffeine 4 mg
  • Caffeine 40 mg
  • Caffeine Citrate 5 mg
  • Caffeine 5 mg
  • Caffeine 50 mg
  • Caffeine 65 mg

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