Pharmacology of caffeine

Benowitz, N. L., Clinical pharmacology of caffeine. Annual Review of Medicine 41, 277-288, 1990. 

Sources of Caffeine History of Caffeine Use Prevalence of Caffeine Consumption Pharmacology of Caffeine... 

Arnaud, M. J. Progress in Drug Research, 31, 1987, 273-313. (Pharmacology of caffeine)... 

Arnaud MJ (1987) The pharmacology of caffeine. Progress in Drug Research 31 273-313. 

A detailed mechanistic understanding of the pharmacology of caffeine currently remains elusive but a key concept is based on the antagonism at adenosine receptors when considering normal doses of caffeine consumption (50 to 300 mg, one to three cups of coffee). Four adenosine receptors have been cloned and are classified as Ai,... 

C7HgN402. Occurs to a small extent in tea, but is chiefly prepared synthetically. Like caffeine, it is a very weak base which forms water-soluble compounds with alkalis. It has a similar pharmacological mechanism to that of caffeine and is used, in combination with ethy-lenediamine. as a diuretic and a bron-chodilator. 

Caffeine is also effective in the antagonism of peripheral adenosine (type I) receptors, which are known to inhibit lipolysis by subduing adenylate cyclase activity.28 The appeal of this mechanism of action is that the majority of the pharmacological effects of adenosine on the central nervous system can be inhibited by doses of caffeine that are well within physiologically non-toxic levels comparable to only a couple of cups of coffee.5... 

Hasenfratz, M., Bunge, A., Dal-Pra, G., Battig, K., Antagonistic effects of caffeine and alcohol on mental performance parameters. Pharmacology, Biochemistry and Behavior 46(2), 463-465, 1993. 

Foreman, N., Barraclough, S., Morre, C., Mehta, A., and Madon, M., High doses of caffeine impair performance of a numerical version of the Stroop task in men. Pharmacology, Biochemistry, and Behavior 32, 399-403, 1989. 

Clubley, M., Bye, C. E., Henson, T. A., Peck, A. W. and Riddington, C. J., Effects of caffeine and cyclizine alone and in combination on human performance, subjective effects and EEG activity. British Journal of Clinical Pharmacology 7 157-63, 1979. 

Chait, L. D., and Griffiths, R. R., Effects of caffeine administration on human cigarette smoking. Clinical Pharmacology and Therapeutics 34, 612-622, 1982. 

Kruger, A., Chronic psychiatric patients use of caffeine pharmacological effects and mechanisms. Psychol Rep 78(3), 915-923, 1996. 

Falk, J. L., Zhang, J., Chen, R., and Lau, C. E., A schedule induction probe technique for evaluating abuse potential Comparison of ethanol, nicotine and caffeine, and caffeine-midazolam interaction. Special Issue Behavioural pharmacology of alcohol. Behavioural Pharmacology 5(4-5), 513-520, 1994. 

Denaro, C. P., Brown, C. R., Jacob, P., Benowitz, N. L., Effects of caffeine with repeated dosing. European Journal of Clinical Pharmacology, 40, 273-278, 1991. 

Hofer, I., and Battig, K., Cardiovascular, behavioral, and subjective effects of caffeine under field conditions. Pharmacology, Biochemistry and Behavior 48(4), 899-908, 1994. 

Bruce, M., Scott, N., Lader, M. and Marks, V., The psychopharmacological and electrophysiological effects of a single dose of caffeine in healthy human subjects. British Journal of Clinical Pharmacology 22, 81-87, 1986. 

Balogh, A., Harder, S., Vollandt, R. and Staib, A.H. (1992) Intra-individual variability of caffeine elimination in healthy subjects. International Journal of Clinical Pharmacology, Therapy, and Toxicology, 30 (10), 383—387. 

Tarrus, E., Cami, J., Roberts, D.J., Spickett, R.G., Celdran, E. and Segura, J. (1987) Accumulation of caffeine in healthy volunteers treated with furafylline. British Journal of Clinical Pharmacology, 23 (1), 9-18. 

The major pharmacological constituents of tea are the purine alkaloids caffeine (2.9-4.2%), theobromine (0.15-0.2%), and theophylline (0.02-0.04%). Also present are triterpene saponins (including barringtogenol C and Rl-barringenol), catechins (theaflavine, theaflavin acid, thearubigine), and caffeic acid derivatives (chlorogenic acid and theogallin). A cup of brewed tea contains approximately 20-100 mg of caffeine... 

Sawynok J. (1995). Pharmacological rationale for the clinical use of caffeine. Drugs. 49(1) 37-50. Sawynok J. (1998). Adenosine receptor activation and nociception. Eur J Pharmacol. 347(1) 1-11. Schlaepfer TE, Strain EC, Greenberg BD, Preston KL, Lancaster E, Bigelow GE, Barta PE, Pearlson GD. (1998). Site of opioid action in the human brain mu and kappa agonists subjective and cerebral blood flow effects. Am J Psychiatry. 155(4) 470-73. 

Closely related methylxanthines include theophylline (1,3-dimethylxanthine), theobromine (3,7 dimethylxanthine) and paraxanthine (1,7-dimethylxanthine). Theobromine is found primarily in chocolate. These derivatives of caffeine are important because they are pharmacologically active and also are the common metabolites of caffeine. 

Beach, C. A., Mays, D. C., Sterman, B. M. and Gerber, N. 1985. Metabolism, distribution, seminal excretion and pharmacokinetics of caffeine in the rabbit. Journal of Pharmacology and Experimental Therapy, 233 18-23. 

Three xanthines are pharmacologically important caffeine, theophylline, and theobromine. All three alkaloids, which occur naturally in certain plants, are widely consumed in the form of beverages (infusions or decoctions) derived from these plants. Coffee primarily contains caffeine (about 100-150 mg per average cup) tea contains caffeine (30-40 mg per cup) and theophylline and cocoa contains caffeine (15-18 mg per cup) and theobromine. Cola drinks also contain significant amounts of caffeine (about 40 mg/12 oz). The CNS stimulation associated with these beverages is predominantly due to the caffeine. 

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