Caffeine diuresis

Nussberger, J., Mooser, V., Maridor, G., Juillerat, L., Waeber, B. and Brunner, H., Caffeine-induced diuresis and atrial natriuretic peptides. J Cadiovasc Pharmacol 15(5), 685-691, 1990. 

These compounds competitively inhibit phosphodiesterase, resulting in an increase in cyclic AMP (see Box 14.3) and subsequent release of adrenaline. This leads to the major effects a stimulation of the central nervous system (CNS), a relaxation of bronchial smooth muscle, and induction of diuresis. These effects vary in the three compounds. Caffeine is the best CNS stimulant, and has weak diuretic action. Theobromine has little stimulant action, but has more diuretic activity and also muscle relaxant properties. Theophylline also has low stimulant action and is an effective diuretic, but it relaxes smooth muscle better than caffeine or theobromine. 

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. 

CNS, smooth muscle T diuresis X- pit aggregation Available forms Daily t doses w/ max 3 g PO daily Contra Avoid in PRG lactation, CAD, hyperthyroidism, anxiety disorders d/t high, caffeine content Notes/SE Insomnia, tach, anxiety, N/V, HA, HTN, Sz Interactions T Effects OF anticoagulants, anti-pits, BBs, bron-choclilators T risk of hypertensive crisis W/ MAOIs T effects W/ cimetidine, ciprofloxacin, ephedrine, hormonal contraceptives, dieophylline, cola, coffee X-effects OF adenosine, antihypertensives, benzodiazepines, Fe, X- effects W/ smoking EMS Tinctures contain EtOH may exacerbate GI disorders HTN T effects of anticoagulants and BBs... 

Large doses of caffeine cause diuresis. Daily consumption of caffeine citrate increased the mean urinary excretion rate of tubular cells and erythrocytes in volunteers (25). The nephrotoxicity of analgesic antipyretic drug combinations may result from a combined effect, in which aspirin, phenacetin, and caffeine all play a role (SEDA-4, 5). In 10 asymptomatic women and 20 women with confirmed detrusor instability, caffeine caused a significant increase in detrusor pressure on bladder filling in the latter, but no difference in volume at first contraction, height of contraction, or bladder capacity (26). 

The acute effects of caffeine include diuresis, stimulation of the heart and CNS, relaxation of smooth muscles, and stimulation of gastric acid. 

Caffeine causes several centrally mediated side effects including nervousness, irritability, and sleeplessness. Caffeine also acts on kidneys to increase diuresis. Convulsions and increased heart rate can occur with particularly high doses of the drug. 

Caffeine intoxication is the only official diagnosis associated with caffeinism in the DSM-IV-TR. Caffeine-induced anxiety may manifest as restlessness, nervousness, excitement, insomnia, diuresis, flushing, gastrointestinal disturbance, muscle twitching, irritability, and jitteriness. If caffeine-induced insomnia requires specific treatment, caffeine-induced sleep disorder (DSM-IV-TR) is an appropriate diagnosis." ... 

Overdosage of caffeine in a nontolerant individual causes insomnia, anxiety, diuresis, restlessness, excitement, nervousness, tinnitus, muscular tremor, headache, and scintillating scotoma. 

The drug produces CNS stimulation and skeletal muscles but to a much lesser extent as compared to caffeine however, it exhibits a greater effect on the coronary dilatation, smooth muscle relaxation, diuresis and cardiac stimulation than caffeine. 

W 0 (X X w Caffeine Adenosine receptor antagonist. High dose T Ca++ permeability in sarcoplasmic reticulum and T cAMP by inhibiting phosphodiesterase. Stimulates CNS, constricts cerebral arterioles, induces diuresis, stimulates heart, bronchodilates. Prolonged apnea in pre-term infants (unlabeled use). Included in some over-the counter analgesic preps, particularly headache remedies. Insomnia, restlessness, anxiety neurosis, nausea, tachycardia, diuresis. 

Theophylline Cellular mech like caffeine. More CNS stimulation than caffeine. Increased cardiac stimulation and diuresis. More effective bronchodilator. Bronchial asthma. Apnea and bradycardia in premature infants (unlabeled use). II M... 

Caffeine is the most widely consumed central-nervous-system stimulant. It also relaxes smooth muscles, stimulates the cardiac muscle, stimulates diuresis, and appears to be useful in the treatment of some types of headache. Moreover, it has potent antioxidant properties, helps in protecting cells against the UV radiation, and slows down the process of photo-aging of the skin [250]. Theobromine is used as a bronchodilator, as a vasodilator, as a diuretic, and in the treatment of angina pectoris and hypertension [251]. 

Xanthine derivatives have a number of pharmacological properties in common. Five major actions are observed (1) central nervous system and respiratory stimulation, (2) skeletal muscle stimulation, (3) diuresis, (4) cardiac stimulation, and (5) smooth-muscle relaxation. Caffeine (29) increases central nervous system activity and its main effect is on the cerebral cortex, where it acts to produce clear thought and reduce drowsiness and fatigue. The normal dose is 100-200 mg (Cordell, 1981). The oral LD50 in mouse is 127-137 mg/kg the oral LD50 in rat for theobromine (31) is 950... 

The phosphodiesterase which cleaves cyclic AMP to adenylate is found in both particulate and soluble fractions of tissue homogenates, and it is inhibited by pyrophosphate and ATP, as well as by caffeine, theophylline, and theobromine. These three methylated xanthines cause central nervous system and respiratory stimulation, smooth muscle relaxation, diuresis, coronary dilatation, cardiac stimulation, and skeletal muscle stimulation these effects are believed to be due to increased tissue concentrations of cyclic AMP resulting from inhibition of phosphodiesterase activity. 

Mechanism of action. Meihybcanihines stimulate the certral nervous system (CNS) and cardiac muscle, promote diuresis and irMiucx smootii misde rdaxatkm. Theobromirte is considered a less potent CNS mubnt than either caffeine or theophylline. 

The physiological activities of coffee are generally attributed to its caffeine. Caffeine is a powerful stimulant of the central nervous system, respiration, and skeletal muscles other activities include cardiac stimulation, coronary dilation, smooth muscle relaxation, and diuresis. 

In humans, the administration of a single dose of 4mgkg caffeine increases the urinary excretion of sodium, calcium, magnesium, potassium, chloride, and urine volume. The mechanism of this mild diuresis has been attributed to an increase in renal... 

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