Diuretics: Basic, Pharmacological, and Clinical Aspects

The need for adequate means by which to improve urine output is very old. Even in the "Scuola Salernitana", the oldest medieval medical school in Western Europe, about 1000 years ago it was taught how to improve urine output. The list of known "diuretica" included herbs, plants, roots, vegetables, in particular asparagus, fennel and carrot. The first diuretic drugs, however, were mercurial compounds. Thus, calomel, mercurous chloride, was initially used as a diuretic in the sixteenth century by Paracelsus, being one of the ingredients of the so-called "Guy's Hospital pill". But calomel had a cathartic effect so that it was replaced by organic mercurial compounds. These diuretics were clearly toxic. After the discovery of the car­ bonic anhydrase, in the early 1930s, and the introduction of sulfanilamide as a chemotherapeutic agent, it was observed that this drug was inhibiting carbonic anhydrase in vitro and urinary acidification in vivo thereby causing metabolic acidosis; urine output, however, appeared to increase. Subsequent studies led to the synthesis of more potent analogs, in particular acetazolamide. Studies on car­ bonic anhydrase inhibitors led to the synthesis of benzothiadiazides which disclosed much less inactivating action on carbonic anhydrase and much more diuretic effect through an inhibition of tubular transport of sodium and chloride. Chlorothiazide was the first member of this class of diuretics. Thiazides are still used in clinical practice.

Contenu

I. Historical Review..- Diuretics in the Salernitan medicine..- II. Effects of Diuretics on Ion Transport..- Ion transport and metabolism in renal cells..- Hydrogen secretion regulated by intracellular membrane potential: a hypothesis on the regulation of renal acidification..- Isolation and purification of the Amiloride-sensitive Na + channel from renal epithelia..- Blockers of active transport in the thick ascending limb of the loop of Henle..- The use of amiloride analogs to probe adaptations of the proximal tubular Na + /H + antiporter in response to a reduction in renal mass..- Red blood cell Na +-transport, Na-K-ATPase and phosphate ester metabolism in essential hypertension..- Correlation between blood pressure and K + fluxes in essential hypertensive patients treated for2 years with Cicletanine..- Effects of Muzolimine on cation transport ii human erythrocytes..- Effects of Xipamide on transmembranary potassium movements and prostacyclin production..- Lack of evidence for Na/K ATPase inhibition as a cause of low renin human hypertension..- Canrenone prevents Na,K pump inhibition induced by volume expansion in normal subjects..- Effect of Thiazides and Amiloride on the phosphorylation status of the red cell membrane anion carrier..- In vitro effects of d(+) and l(-)Ozolinone on sodium and potassium fluxes in human erythrocytes..- III. Effects of Diuretics on Tubular Transport..- The effects of diuretics on salt transport in renal diluting segments..- Estimation of free water back diffusion during water diuresis in man using Lithium clearance and furosemide effect: some unresolved questions..- Effect of Ouabain and Acetazolamide on proximal tubular transport in dogs..- Voltage-driven calcium reabsorption in diluting segment: inhibition by Furosemide but not by calcium antagonists..- Relationship between Na,K-ATPase activity and transcellular NaCl reabsorption in dog kidneys..- Dose dependence of inhibiton of proximal tubular sodium reabsorption by Furosemide in conscious rats..- Modification in renal handling of phosphate induced by Hydrochlorothiazide (HCTZ) and Amiloride (A)..- IV. Pharmacokinetics..- Influence of renal failure on the pharmacokinetics of Cicletanine..- Pharmacokinetics and -dynamics of Piretanide in chronic renal failure..- Changes in furosemide pharmacokinetics induced by dehydration..- Pharmacokinetics of Torasemide in man..- Furosemide blunts Hydrochlorothiazide (HCT) effect..- Influence of renal insufficiency on the pharmacokinetics and the renal effects of Cicletanine..- A comparison between Torasemide and Furosemide effects after application upon one kidney or after I.V. injection in the rat..- V. Endogenous Natriuretic Factors..- Receptor binding sites of Atrial Natriuretic Factor in bovine brain microvessels..- Intrarenal localization and photoaffinity labeling of receptors for ?-rat Atrial Natriuretic Polypeptide..- Atrial Natriuretic Peptide raises hematocrit in conscious nephrectomized rats..- Tubular effects of atrial extract and of Atriopeptin III in conscious rats..- Atrial Natriuretic Peptides and renin secretion..- Salt loading in spontaneously hypertensive rats further elevates blood pressure despite enhanced release of Atrial Natriuretic Peptides and exaggerated natriuresis..- Plasma cardionatrin and volume and the renin angiotensin aldosterone system in normotensive and hypertensive pregnancy..- Atrial Natriuretic Peptide as an indicator of cardiac and volume state..- Atrial Natriuretic Peptides (ANP) in rats with chronic renal failure..- Plasma levels of human Atrial Natriuretic Peptide in chronic uremic patients..- Atrial Natriuretic Peptide (ANP) and renal function: effect of posture and dietary sodium..- Involvement of Na + transport and Natruiretic hormones in the antihypertensive mechanism of Canrenone..- Inhibition of the erythrocyte Na +, K + - Pump by mammalian lignans: a possible link with endogenous digitalis..- Effects of human alpha Natriuretic Atrial Peptide on aldosterone secretion in vitro..- Interaction of platelet-activating factor with natriuresis and diuresis induced by the synthetic Atrial Natriurectic Factor (ser 99-Tyr 126) in anaesthetized dog..- Circulating Natriuretic Factor in the pathogenesis of genetic hypertension of renal origin..- Lack of correlation between plasma Ouabain-like Factor and urinary sodium excretion in essential hypertensive patients..- Atrial Natriuretic Peptide during water immersion in healthy volunteers..- VI. Aquaretics..- Symposium on aquaretics: introduction..- Some aquaretic agents other than vasopressin analogs..- Vasopressin antagonists: model aquaretic agents..- The anti-antidiuretic effect of a stable prostaglandin-E2 analog in conscious sheep and man..- Vasopression in patients with liver and cardiac disease..- Reversal of hyponatremia in experimental Schwartz-Bartter Syndrome with a vasopressin antagonist (SK&F101926)..- The vasopressin antagonist SK&F101926 is a selective aquaretic agent in dogs..- VII. Diuretics and Hypertension..- The antihypertensive mechanism of diuretics..- Metabolic effects of long-term diuretic treatment..- Anthihypertensive diuretics - old and new..- The physiology of natriuretic mechanisms in the kidney..- Intracellular electrolytes in essential hypertension during treatment with Torasemide..- The isolated perfused rat kidney as a model for the study of diuretics in hypertension..- Antihypertensive mechanisms of Muzolimine..- Indapamide: antihypertensive activity and renal effects..- In vitro effects of Furosemide on rabbit blood vessels..- Comparison of Torasemide and Indapamide in the treatment of essential hypertension..- Modifications in cardiovascular Norepinephrine responsiveness by diuretic treatment in mild renal parenchymal disease..- Muzolimine vs Captopril in Low and Mild Hypertension..- The hypotensive action of Indapamide..- Etozolin induced urine excretion of water and solutes in patients with hypertension..- Calcium metabolism in essential hypertensive patients treated with Etozolin..- Improvement in exercise-induced diastolic blood pressure changes by diuretic treatment..- Antihypertensive activity and tolerability of Thiobutizide alone or in fixed combination with potassium Canreonate in essential hypertension..- K-rich/Na-poor salt reduces blood pressure in hospitalized patients..- Combination of Nifedipine and Chlorthalidone in the treatment of hypertension..- Cardiovascular reflex and systemic hemodynamic relationship in…