Company InfoNewsInvestor InformationResearchDevelopmentCareersBusiness DevelopmentResourcesDrugs databaseBack to the home pageSearch  
Drugs database
Drugs A-Z

Brands A-Z

Drugs by categories

Drugs by manufacturer

Drugs by packager

Antibiotics for sale

Online Viagra bestellen in Nederland

Home / Drugs / Starting with C / Caffeine
 
Caffeine
 

A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes smooth muscle, stimulates cardiac muscle, stimulates diuresis, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide phosphodiesterases, antagonism of adenosine receptors, and modulation of intracellular calcium handling. [PubChem]
BrandsAlert-Pep
Cafamil
Cafcit
Cafecon
Caffedrine
Caffine
Cafipel
Coffein
Coffeine
Dasin
Dexitac
DHC Plus
Diurex
Durvitan
Eldiatric C
Enerjets
Ercatab
Fioricet
Guaranine
Hycomine
Keep Alert
Kofein
Koffein
Mateina
Miudol
Nix Nap
No-Doz
Nodaca
Norgesic Forte
Organex
Pep-Back
Phensal
Quick Pep
Refresh'n
Stim
Thein
Theine
Vivarin
Wake-Up
Wigraine
CategoriesCentral Nervous System Stimulants
Anorexigenic Agents
Phosphodiesterase Inhibitors
ManufacturersMead johnson and co
App pharmaceuticals llc
Luitpold pharmaceuticals inc
Paddock laboratories inc
Sun pharmaceutical industries ltd
PackagersActavis Group
Aidarex Pharmacuticals LLC
Alphagen Laboratories Inc.
American Regent
Amerisource Health Services Corp.
Amneal Pharmaceuticals
Apotheca Inc.
APP Pharmaceuticals
A-S Medication Solutions LLC
Athlon Pharmaceuticals Inc.
Atley Pharmaceuticals
Bedford Labs
Ben Venue Laboratories Inc.
Bioniche Pharma
Blansett Pharmacal Co. Inc.
Blenheim Pharmacal
Brighton Pharmaceuticals
Bristol-Myers Squibb Co.
Bryant Ranch Prepack
Cardinal Health
Carlisle Laboratories Inc.
Comprehensive Consultant Services Inc.
Concord Labs
Corepharma LLC
CVS Pharmacy
D.M. Graham Laboratories Inc.
Direct Dispensing Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
Everett Laboratories Inc.
Forest Pharmaceuticals
G & W Labs
Gilbert Laboratories
GlaxoSmithKline Inc.
Goldline Laboratories Inc.
Heartland Repack Services LLC
Hope Pharmaceuticals
Hospira Inc.
Innoviant Pharmacy Inc.
J T Baker
Kaiser Foundation Hospital
Keene Pharmaceuticals Inc.
Keltman Pharmaceuticals Inc.
Lannett Co. Inc.
Liberty Pharmaceuticals
Luitpold Pharmaceuticals Inc.
Lunsco Inc.
Major Pharmaceuticals
Mallinckrodt Inc.
Marlex Pharmaceuticals
Marnel Pharmaceuticals Inc.
MCR American Pharmaceuticals Inc.
Mikart Inc.
Murfreesboro Pharmaceutical Nursing Supply
Nexgen Pharma Inc.
Novartis AG
Nucare Pharmaceuticals Inc.
Paddock Labs
Palmetto Pharmaceuticals Inc.
Patient First Corp.
PCA LLC
PD-Rx Pharmaceuticals Inc.
Perrigo Co.
Pharmaceutical Utilization Management Program VA Inc.
Physicians Total Care Inc.
Poly Pharmaceuticals Inc.
Preferred Pharmaceuticals Inc.
Prepackage Specialists
Prepak Systems Inc.
Prescript Pharmaceuticals
Prometic Pharma Inc.
Qualitest
Rebel Distributors Corp.
Redpharm Drug
Resource Optimization and Innovation LLC
Rising Pharmaceuticals
Rite Aid Corp.
Sandhills Packaging Inc.
Sciele Pharma Inc.
Seatrace Pharmaceuticals Inc.
Southwood Pharmaceuticals
Stat Rx Usa
Talbert Medical Management Corp.
Teva Pharmaceutical Industries Ltd.
US Pharmaceutical Corp.
Va Cmop Dallas
Victory Pharma
Vintage Pharmaceuticals Inc.
Watson Pharmaceuticals
West-Ward Pharmaceuticals
Xanodyne Pharmaceuticals Inc.
SynonymsCafeina
Caffein
CFF
Methyltheobromide
Methyltheobromine
Theobromine ME
Theophylline ME

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 antagonists 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.

toxicity

LD50=127 mg/kg (orally in mice)

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).

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.

half life

3 to 7 hours in adults, 65 to 130 hours in neonates

route of elimination

In young infants, the elimination of caffeine is much slower than that in adults due to immature hepatic and/or renal function.

drug interactions

Adenosine: Caffeine may diminish the therapeutic effect of adenosine. Specific management recommendations vary slightly depending on specific adenosine product used (i.e., therapeutic vs. diagnostic use of adenosine). Significantly higher adenosine doses, or alternative agents, may be required. Monitor for decreased therapeutic effects of adenosine if the patient is already receiving caffeine. Discontinue caffeine in advance (5 half-lives, or approximately 24 hours, is specifically recommended) of scheduled diagnostic use of adenosine (e.g., for radionuclide imaging studies) whenever possible.

Ciprofloxacin: Ciprofloxacin may increase the effect and toxicity of caffeine.

Clozapine: Caffeine increases the effect and toxicity of clozapine

Conivaptan: Conivaptan may increase the serum concentration of CYP3A4 substrates such as caffeine. Upon completion/discontinuation of conivaptan, allow at least 7 days before initiating therapy with drugs that are CYP3A4 substrates.

Grepafloxacin: Grepafloxacin may increase the effect and toxicity of caffeine.

Lithium: Caffeine decreases serum levels of lithium

Norfloxacin: Norfloxacin may increase the effect and toxicity of caffeine.

Tamsulosin: Caffeine, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Caffeine is initiated, discontinued, or dose changed.

Terbinafine: Terbinafine may increase the plasma concentration of Caffeine.

Thiabendazole: The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Caffeine by decreasing Caffeine metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Caffeine if Thiabendazole is initiated, discontinued or dose changed.

Tolterodine: Caffeine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.