Indication: For management of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in infants.
Pharmacology: Caffeine, a naturally occurring xanthine derivative like theobromine and the bronchodilator theophylline, is used as a CNS stimulant, mild diuretic, and respiratory stimulant (in neonates with apnea of prematurity). Often combined with analgesics or with ergot alkaloids, caffeine is used to treat migraine and other headache types. Over the counter, caffeine is available to treat drowsiness or mild water-weight gain.
Mechanism Of Action: Caffeine stimulates medullary, vagal, vasomotor, and respiratory centers, promoting bradycardia, vasoconstriction, and increased respiratory rate. This action was previously believed to be due primarily to increased intracellular cyclic 3′,5′-adenosine monophosphate (cyclic AMP) following inhibition of phosphodiesterase, the enzyme that degrades cyclic AMP. It is now thought that xanthines such as caffeine act as agonists at adenosine-receptors within the plasma membrane of virtually every cell. As adenosine acts as an autocoid, inhibiting the release of neurotransmitters from presynaptic sites but augmenting the actions of norepinephrine or angiotensin, antagonism of adenosine receptors promotes neurotransmitter release. This explains the stimulatory effects of caffeine. Blockade of the adenosine A1 receptor in the heart leads to the accelerated, pronounced "pounding" of the heart upon caffeine intake.
Drug Category: Central Nervous System Stimulants; Anorexigenic Agents; Phosphodiesterase Inhibitors; ATC:N06BC01
Absorption: Readily absorbed after oral or parenteral administration. The peak plasma level for caffeine range from 6-10mg/L and the mean time to reach peak concentration ranged from 30 minutes to 2 hours.
Interactions:
DrugBank: Interactions for Caffeine
Interactions for Caffeine:
Cytochrome P450 1A2 (CYP1A2) is known to be the major enzyme involved in the metabolism of
caffeine. Therefore, caffeine has the potential to interact with drugs that are substrates for CYP1A2,
inhibit CYP1A2, or induce CYP1A2.
Few data exist on drug interactions with caffeine in preterm neonates. Based on adult data, lower doses of
caffeine may be needed following coadministration of drugs which are reported to decrease caffeine elimination (e.g.,
cimetidine and ketoconazole) and higher caffeine doses may be needed following coadministration of drugs that
increase caffeine elimination (e.g., phenobarbital and phenytoin).
Caffeine administered concurrently with ketoprofen reduced the urine volume in 4 healthy volunteers. The clinical
significance of this interaction in preterm neonates is not known.
Interconversion between caffeine and theophylline has been reported in preterm neonates. The concurrent use of
these drugs is not recommended.
Chemical IUPAC Name: 1,3,7-trimethyl-3,7-dihydropurine-2,6-dione
Chemical Formula: C8H10N4O2
Half Life: 3 to 7 hours in adults, 65 to 130 hours in neonates
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