Therapeutically caffeine

Zhang, Y. and Wells, J., The effects of chronic caffeine administration on peripheral adenosine receptors, Journal of Pharmacology and Experimental Therapeutics, 254, 757, 1990. 

Rush, C., Sullivan, J. and Griffiths, R., Intravenous caffeine in stimulant drug abusers Subjective reports and physiological effects. Journal of Pharmacology and Experimental Therapeutics 273(1), 351-358, 1995. 

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

Carrillo, J. and Benitez, J., Caffeine metabolism in a healthy Spanish population N-Acetylator phenotype and oxidation pathways. Clinical Pharmacological Therapeutics 55, 293-304, 1994. 

Herbal medications are drugs in every sense of the word. They chemically modify bodily processes and can have therapeutic or harmful effects, depending on how they are used. However, there are a few general differences between herbal and pharmaceutical drugs (Tyler 1994). Herbal drugs tend to be more dilute than pharmaceutical drugs (table 1.1). For example, caffeine is available in 200 mg tablets to produce stimulation. Coffee contains 1-2% caffeine, so in order to get the same amount of caffeine one must use 20 g of coffee bean. Similarly, aspirin is... 

Caffeine and the related dimethylxanthines have similar pharmacological or therapeutic effects and similar toxic effects. The primary actions include stimulation of the central nervous system, relaxation of bronchial muscles, mild cardiac muscle stimulation, and diuretic effects on the kidney. 

Methylxanthines have a number of other effects, including effects on smooth muscles and the cardiovascular system. The most notable effect on smooth muscles is relaxing the bronchi of the lungs. Theophylline is prescribed to treat mild forms of asthma. While both caffeine and theophylline will relax the bronchial smooth muscles, theophylline is used therapeutically because of its longer half-life. This allows the drug to stay in the therapeutic range longer. 

Aranda JV. Maturational changes in theophylline and caffeine metahohsm and disposition clinical implications. Proceedings of the Second World Conference on Clinical Pharmacology and Therapeutics Bethesda, MD. American Society for Pharmacology and Experimental Therapeutics 1984. p. 868-77. 

Most drugs are administered to infants and children for the same therapeutic indications as for adults. However, a few drugs have found unique uses in children. Among these are theophylline and caffeine, which are used to treat apnea of prematurity indomethacin, which closes a patent ductus arteriosus and prostaglandin Ej, which maintains the patency of the ductus arteriosus. Paradoxically, drugs such as phenobarbital, which have a sedating action on adults, may produce hyperactivity in children, and some adult stimulant drugs, such as methyl-phenidate, are used to treat children with hyperactivity. 

Mecftanism of Action AGI Hj-blocker and gastric acid secretion inhibitor that inhibits histamine action at histamine 2 receptors of parietal cells Therapeutic Effect Inhibits gastric acid secretion when fasting, at night, or when stimulated by food, caffeine, or insulin. 

Apart from psychopharmaceuticals, there are many other substances that also affect subjective state and behavior social drugs such as alcohol and caffeine have little or no therapeutic applications in Western medicine but undoubtedly affect subjective state and behavior, whereas the use of drugs such as marijuana, LSD, cocaine and heroin involves risks that, according to today s opinion, outweigh the possible benefits. 

Other drugs, such as verapamil, caffeine, theophylline, osmotic diuretics, carbonic anhydrase inhibitors, or aminophylline, can increase lithium excretion, possibly dropping plasma levels below the therapeutic threshold ( 329). Further, if doses are increased to compensate for this effect, care must be taken to readjust the lithium downward when these concomitant agents are reduced or discontinued. 

Contradicting results were reported for GFJ when administered with caffeine. One study reported no changes in AUC, blood pressure, and heart rate (173). A second study reported increases in AUC and half-life. However, no assessment of pharmacodynamic parameters was performed (89). Furthermore, GFJ increased the fraction absorbed and the percentage of excreted dextromethorphan (28). The above-mentioned interactions can be considered weak regarding the overall exposure. Furthermore, dextromethorphan has a broad therapeutic window. The interactions of GFJ with caffeine and dextromethorphan do not seem to be of clinical relevance. 

The three methalated xanthine derivatives (methyixanthines) theophylline, theobromine, and caffeine are plant alkaloids. Theophylline is the only one of these which is widely used therapeutically. Three possible modes of action have been proposed ... 

The three important methylxanthines are theophylline, theobromine, and caffeine. Their major source is beverages (tea, cocoa, and coffee, respectively). The importance of theophylline as a therapeutic agent in the treatment of asthma has waned as the greater effectiveness of inhaled adrenoceptor agents for acute asthma and of inhaled anti-inflammatory agents for chronic asthma has been established, but theophylline s very low cost is an important advantage for economically disadvantaged patients in societies in which health care resources are limited. 

Theophylline is 1,3-dimethylxanthine theobromine is 3,7-dimethylxanthine and caffeine is 1,3,7-trimethylxanthine. A theophylline preparation commonly used for therapeutic purposes is aminophylline, a theophylline-ethylenediamine complex. The clinical use of theophylline is discussed below. The metabolic products, partially demethylated xanthines (not uric acid), are excreted in the urine. 

Caffeine has widespread therapeutic use. It is widely used in headache (migraine) remedies such as aspirin and other analgesics. Caffeine is a mild vasoconstrictor and its ability to constrict blood vessels serving the brain explains its use to relieve headache. Individuals who consume caffeine regularly through medications and food are susceptible to what is known as a rebound headache or caffeine rebound. This occurs when regular caffeine intake is suddenly reduced and the vessels dilate. Caffeine is a common substance in medications to treat apnea in premature infants. Apparently, the area of the brain controlling respiration in premature infants is not fully developed and caffeine helps to stimulate this portion of the... 

Certain foreign compounds may cause the retention or excretion of water. Some compounds, such as the drug furosemide, are used therapeutically as diuretics. Other compounds causing diuresis are ethanol, caffeine, and certain mercury compounds such as mersalyl. Diuresis can be the result of a direct effect on the kidney, as with mercury compounds, which inhibit the reabsorption of chloride, whereas other diuretics such as ethanol influence the production of antidiuretic hormone by the pituitary. Changes in electrolyte balance may occur as a result of excessive excretion of an anion or cation. For example, salicylate-induced alkalosis leads to excretion of Na+, and ethylene glycol causes the depletion of calcium, excreted as calcium oxalate. 

The xanthines caffeine (40 R1 = R2 = R3 = Me), theophylline (40 R1 = R2 = Me, R3 = H) and theobromine (40 R1 = R3 = Me, R2 = H), which are the stimulants present in tea, coffee, cocoa and many other beverages, have a number of therapeutic uses. They were formerly used as diuretics, theophylline being the most potent, and caffeine is a powerful CNS stimulant useful in treating cases of poisoning by CNS depressants. Caffeine has also been... 

As electroporation is still largely in the experimental stage and may possibly be never used clinically, many workers have employed model nontherapeutic molecules to demonstrate the feasibility of its use, such as sulforhodamine, calcein, and caffeine. However, more therapeutic and biotechnologically derived molecules have now been investigated for transdermal delivery, including, for example, fentanyl [22], metoprolol [21], timolol [36], flurbiprofen [37], cyclosporin [38], heparin [39], oligonucleotides [40], and genes [41]. 

Xanthine derivatives are a group of chemically similar compounds that exert a variety of pharmacologic effects. Common xanthine derivatives include theophylline, caffeine, and theobromine (Fig. 26-2) these compounds are frequently found in various foods and beverages (tea, coffee, soft drinks). Theophylline and several theophylline derivatives are also administered therapeutically to produce bronchodilation in asthma and other forms of reversible airway obstruction (bronchitis, emphysema).65,79 Theophylline and caffeine are also potent CNS stimulants, and some of the more common side effects of these drugs are related to this CNS excitation (see Adverse Side Effects, later in this chapter). 

Caffeine is used medicinally as a CNS stimulant, usually combined with another therapeutic agent, as in compound analgesic preparations. Theobromine is of value as a diuretic and smooth muscle relaxant, but is not now routinely used. Theophylline is an important smooth muscle relaxant for relief of bronchospasm, and is frequently dispensed in slow-release formulations to reduce side-effects. It is also available as aminophylline (a more soluble preparation containing theophylline with ethylenediamine) and choline theophyllinate (theophylline and choline). The alkaloids may be isolated from natural sources, or obtained by total or partial synthesis. 

Caffeine continues to be used therapeutically in analgesic combination preparations. It has superseded theophylline as the preferred drag for treatment of neonatal apnea because of its ease of administration and more predictable plasma concentrations. 

The therapeutic treatment of obesity with caffeine is another controversial area of interest. Many over-the-counter diet aids contain caffeine, but it has not yet been determined whether there is a medically safe way to use caffeine as a fat fighter. A 2000 study showed that a combination of herbal ephedra and caffeine lowered participants body weight by both decreasing fat and decreasing the body mass index (BMI). Losses were 15 and 7 pounds for those taking the herbal supplement and a placebo, respectively. 

Anyone who must take diuretics for therapeutic purposes should take the proper precautions when exercising. This includes adequate and regular intake of water, sports drinks, or other non-caffeinated fluids loose and comfortable clothing adequate rest periods and awareness of the signs of heat exhaustion (clammy and cool skin, fatigue, nausea, weakness, confusion, vision disturbances, and a possible loss of consciousness). 

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