Active ingredient: Caffeine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

• Central Nervous System Stimulants
• Anorexigenic Agents
• Phosphodiesterase Inhibitors

Dosage Forms

• Capsule
• Drops
• Liquid
• Pill
• Tablet

Brands / Synonyms

Acetaminophen, Caffeine and Dihydrocodeine; Alert-Pep; Anoquan; Butalbital, Acetaminophen and Caffeine; Butalbital, Acetaminophen, Caffeine, and Codeine; Butalbital, Aspirin, and Caffeine; Butalbital, Aspirin, Caffeine, and Codeine; Cafamil; Cafcit; Cafecon; Cafeina; Cafergot; Caffedrine; Caffedrine Caplets; Caffein; Caffeine Pure; Caffeine, Anhydrous; Caffeine, Monohydrate; Caffeine, Synthetic; Caffine; Cafipel; CFF; Coffein; Coffeine; Compound 65; Darvon Compound; Darvon Compound-65; Dasin; Dexitac; Dexitac Stay Alert Stimulant; Dhc Plus; Diurex; Durvitan; Eldiatric C; Enerjets; Ercatab; Ergotamine and Caffeine; Esgic; Esgic-Plus; Femcet; Fioricet; Fioricet with Codeine; Fiorinal; Fiorinal with Codeine; Guaranine; Hycomine; Invagesic; Invagesic Forte; Keep Alert; Kofein; Koffein; Lanorinal; Mateina; Maximum Strength Snapback Stimulant Powders; Medigesic Plus; Methyltheobromide; Methyltheobromine; Migergot; Miudol; Monomethyl Derivative of Theophylline; Natural Caffeinum; Nix Nap; No-Doz; Nodaca; Nodoz Maximum Strength Caplets; Norgesic; Norgesic Forte; Organex; Orphengesic; Orphengesic Forte; Pep-Back; Phensal; Propoxyphene Compound 65; Propoxyphene Compound-65; Quick Pep; Refresh'n; SK 65 Compound; Stim; Synalgos-Dc; Thein; Theine; Theobromine ME; Theophylline ME; Triad; Ultra Pep-Back; Vivarin; Wake-Up; Wigraine ; Zebutal

Indications

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.

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.

Toxicity

LD₅₀=127 mg/kg (orally in mice)

Biotrnasformation / Drug Metabolism

Hepatic cytochrome P450 1A2 (CYP 1A2) is involved in caffeine biotransformation. About 80% of a dose of caffeine is metabolized to paraxanthine (1,7-dimethylxanthine), 10% to theobromine (3,7-dimethylxanthine), and 4% to theophylline (1,3-dimethylxanthine).

Contraindications

CAFCIT® (caffeine citrate) is contraindicated in patients who have demonstrated hypersensitivity to any of its components.

Drug Interactions

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.