Koffein 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.
Koffein Contraindications
CAFCIT® (caffeine citrate) is contraindicated in patients who have demonstrated hypersensitivity to any of its
components.
Additional information about Koffein
Koffein Indication: For management of fatigue, orthostatic hypotension, and for the short term treatment of apnea of prematurity in infants.
Mechanism Of Action: Koffein 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 Interactions: Not Available
Food Interactions: Not Available
Generic Name: Caffeine
Synonyms: Caffeine, Anhydrous; Caffeine, Monohydrate; Caffeine, Synthetic; CFF; Cafeina; Caffein; Caffeine Pure; Compound 65; Methyltheobromide; Methyltheobromine; Monomethyl Derivative of Theophylline; Theobromine ME; Theophylline ME
Where to order Caffeine (and Koffein analogs) online:
Drug Category: Central Nervous System Stimulants; Anorexigenic Agents; Phosphodiesterase Inhibitors
Drug Type: Small Molecule; Approved
Other Brand Names containing Caffeine: Alert-Pep;
Anoquan;
Cafamil;
Cafcit;
Cafecon;
Cafergot;
Caffedrine;
Caffedrine Caplets;
Caffine;
Cafipel;
Coffein;
Coffeine;
Darvon Compound;
Darvon Compound-65;
Dasin;
Dexitac;
Dexitac Stay Alert Stimulant;
Dhc Plus;
Diurex;
Durvitan;
Eldiatric C;
Enerjets;
Ercatab;
Esgic;
Esgic-Plus;
Femcet;
Fioricet;
Fiorinal;
Guaranine;
Hycomine;
Invagesic;
Invagesic Forte;
Keep Alert;
Kofein;
Koffein;
Lanorinal;
Mateina;
Maximum Strength Snapback Stimulant Powders;
Medigesic Plus;
Migergot;
Miudol;
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;
Triad;
Ultra Pep-Back;
Vivarin;
Wake-Up;
Wigraine;
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 (Overdose): LD
50=127 mg/kg (orally in mice)
Protein Binding: Low (25 to 36%).
Biotransformation: 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).
Half Life: 3 to 7 hours in adults, 65 to 130 hours in neonates
Dosage Forms of Koffein: Pill Oral
Liquid Oral
Tablet Oral
Capsule Oral
Syrup Oral
Suppository Rectal
Elixir Oral
Solution / drops Oral
Solution Oral
Suspension Oral
Tablet, extended release Oral
Chemical IUPAC Name: 1,3,7-trimethylpurine-2,6-dione
Chemical Formula: C8H10N4O2
Caffeine on Wikipedia: http://en.wikipedia.org/wiki/Caffeine
Organisms Affected: Humans and other mammals
