Caffeine

Intravenous
Short-term treatment of neonatal apnoea of prematurity

Oral
Migraine

Oral
Mild stimulant of the central nervous system

May be taken with or without food.

Hypersensitivity.

Peptic ulceration; symptomatic cardiac arrhythmias and/or palpitations; 1st several days to wk after an acute MI; neonates; pregnancy; lactation.

Insomnia, restlessness, nervousness, mild delirium; nausea, vomiting, gastric irritation.

IM/IV/Parenteral/PO: C

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.

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.

Description: 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.
Pharmacokinetics:
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.

Antimigraine Preparations