The effect of renin and aldosterone inhibition by β-adrenergic blockade on the response to the new diuretic azosemide

Horký, K; Gregorová, I; Dvořáková, Jana

doi:10.1016/0014-2999(81)90447-7

Cited by 8 publications

(18 citation statements)

References 14 publications

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“…Nevertheless, time-averaged Cl CR values before and after administration of azosemide seemed to be comparable [55]. Consecutive administration of intravenous azosemide for 3 days was not accompanied by marked changes in Cl CR in benign essential hypertensive patients [8]. The time-averaged Cl IN was not significantly different (decreased slightly) after intravenous administration of azosemide to rats [32].…”

Section: Effects On Glomerular Filtration Rate and Renal Plasma Flowmentioning

confidence: 98%

“…Azosemide had a distinct stimulating activity on the renin-angiotensin-aldosterone system (RAAS) after intravenous infusion of the drug to benign essential hypertensive patients for consecutive 3 days [8]. The stimulation of RAAS might be responsible for the diminishing effectiveness with repeated azosemide infusion [8]. However, the plasma renin activity, heart rate and haematocrit were not affected by azosemide in patients with mild to moderate chronic congestive heart failure [10].…”

Section: Effects On Hormonesmentioning

confidence: 98%

“…Plasma ADH, serum prolactin, serum aldosterone and plasma renin activities rose with a resultant increase in urinary aldosterone excretion [55]. Azosemide had a distinct stimulating activity on the renin-angiotensin-aldosterone system (RAAS) after intravenous infusion of the drug to benign essential hypertensive patients for consecutive 3 days [8]. The stimulation of RAAS might be responsible for the diminishing effectiveness with repeated azosemide infusion [8].…”

Section: Effects On Hormonesmentioning

confidence: 99%

“…It is used clinically in the treatment of oedema and arterial hypertensions; specific indications for cardiac and renal oedema and ascites have been reported [2]. Its use in patients with oedema of various genesis [3][4][5], liver cirrhosis [6,7], benign essential hypertension [8], coexisting hypertension and oedema [9], congestive heart failure [10,11] and chronic syndrome of inappropriate secretion of antidiuretic hormone (SIADH) due to traumatic subarachnoidal haemorrhage [12] has been reported. The diuretic effects were also demonstrated in rats with various disease states: nephritis produced by anti-rat kidney serum [13], hepatic damage induced by carbon tetrachloride [13], partial hepatectomy [13], diabetes mellitus induced by streptozotocin (DMIS) [13], hypertension (spontaneously hypertensive rats, SHRs and deoxycorticosterone acetate (DOCA)-salt-induced hypertensive rats) [13], proteinÀcalorie malnutrition (PCM) [14], diabetes mellitus induced by alloxan (DMIA) [15] and acute renal failure induced by uranyl nitrate (U-ARF) [16] or mercuric chloride [17].…”

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confidence: 99%

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Pharmacokinetics and pharmacodynamics of azosemide

Suh¹,

Kim²,

Lee³

2003

Biopharm & Drug Disp

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Azosemide is used in the treatment of oedematous states and hypertension. The exact mechanism of action is not fully understood, but it mainly acts on both the medullary and cortical segments of the thick ascending limb of the loop of Henle. Delayed tolerance was demonstrated in humans by homeostatic mechanisms (principally an increase in aldosterone secretion and perhaps also an increase in the reabsorption of solute in the proximal tubule). After oral administration to healthy humans in the fasting state, the plasma concentration of azosemide reached its peak at 3-4 h with an absorption lag time of approximately 1 h and a terminal half-life of 2-3 h. The estimated extent of absolute oral bioavailability in humans was approximately 20.4%. After oral administration of the same dose of azosemide and furosemide, the diuretic effect was similar between the two drugs, but after intravenous administration, the effect of azosemide was 5.5-8 times greater than that in furosemide. This could be due to the considerable first-pass effect of azosemide. The protein binding to 4% human serum albumin was greater than 95% at azosemide concentrations ranging from 10 to 100 microg/ml using an equilibrium dialysis technique. The poor affinity of human tissues to azosemide was supported by the relatively small value of the apparent post-pseudodistribution volume of distribution (Vdbeta), 0.262 l/kg. Eleven metabolites (including degraded products) of azosemide including M1, glucuronide conjugates of both M1 and azosemide, thiophenemethanol, thiophencarboxylic acid and its glycine conjugate were obtained in rats. Only azosemide and its glucuronide were detected in humans. In humans, total body clearance, renal clearance and terminal half-life of azosemide were 112 ml/min, 41.6 ml/min and 2.03 h, respectively. Azosemide is actively secreted in the renal proximal tubule possibly via nonspecific organic acid secretory pathway in humans. Thus, the amount of azosemide that reaches its site of action could be significantly modified by changes in the capacity of this transport system. This capacity, in turn, could be predictably changed in disease states, resulting in decreased delivery of the diuretic to the transport site, as well as in the presence of other organic acids such as nonsteroidal anti-inflammatory drugs which could compete for active transport of azosemide. The urinary excretion rate of azosemide could be correlated well to its diuretic effects since the receptors are located in the loop of Henle. The diuretic effects of azosemide were dependent on the rate and composition of fluid replacement in rabbits; therefore, this factor should be considered in the evaluation of bioequivalence assessment.

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Section: Effects On Glomerular Filtration Rate and Renal Plasma Flowmentioning

confidence: 98%

Section: Effects On Hormonesmentioning

confidence: 98%

Section: Effects On Hormonesmentioning

confidence: 99%

mentioning

confidence: 99%

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Pharmacokinetics and pharmacodynamics of azosemide

Suh¹,

Kim²,

Lee³

2003

Biopharm & Drug Disp

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“…The properties of azosemide are very similar to those of furosemide and bumetanide. Its di uretic action has been observed in dogs [1], rats [2] and humans [3][4][5]. In humans, azo semide has been reported to be 5 times as potent as furosemide [4], Free-flow micropuncture in rats [2] and clearance studies in humans [3] indicate that the site of action of azosemide is the thick ascending limb of Henle's loop (TAL), the site where furosemide and bumetanide act.…”

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confidence: 99%

Effect of Azosemide on the in vitro Perfused Thick Ascending Limb of Henle’s Loop from the Mouse

Tsuchiya¹,

Sasaki²,

Marumo³

1990

Pharmacology

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Direct effect of azosemide on the mouse thick ascending limb of Henle’s loop was examined by the isolated tubules perfusion technique, and the effect was compared with that of furosemide. Azosemide added to the tubular lumen reversibly suppressed the lumen positive potential (PD_t) and decreased the net chloride reabsorption. Dose-response studies of these two drugs suggested that azosemide was about 5 times as potent as furosemide. The more potent effect of azosemide compared with furosemide was confirmed by a paired study in the same tubules. At a concentration of 10^–5 mol/l azosemide suppressed PD_t by 91.4%, furosemide by 65.6%.

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Effects of the rate and composition of fluid replacement on the pharmacokinetics and pharmacodynamics of intravenous azosemide

Park

Yoon

Shin

et al. 1997

Biopharm. Drug Dispos.

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The effects of differences in the rate and composition of intravenous fluid replacement for urine loss on the pharmacokinetics and pharmacodynamics of azosemide were evaluated using rabbit as the animal model. Each rabbit received a 4 h constant intravenous infusion of 1 mg kg−1 azosemide with 0% replacement (treatment I, n =4), 50% replacement (treatment II, n =5), and 100% replacement (treatment III, n =5) with lactated Ringer's solution, as well as with 100% replacement with 5% dextrose in water (D‐5‐W, treatment IV, n =5). Renal clearance and urinary excretion rate of the drug in treatment III were considerably higher than those in treatments I, II, and IV. In spite of the similarities in kinetic properties, diuretic and/or natriuretic effects of azosemide were markedly different among the four treatments. For example, the mean 8 h urine output values were 98·2, 178, 733, and 237 mL for treatments I–IV, respectively, and the corresponding values for sodium excretion were 11·1, 19·4, 76·4, and 14·2 mmol, and for chloride 13·4, 23·8, 78·9, and 17·1 mmol. Except for treatment III, diuresis and/or natriuresis were found to be time dependent, generally decreasing with time until reaching a low plateau during the later hours of infusion. The present findings also show that (i) no fluid replacement and 100% replacement with D‐5‐W both produce the same degree (not significantly different) of severe acute tolerance in natriuresis, indicating the insignificance of water compensation in tolerance development; (ii) in treatment II, where neutral sodium balance was achieved, the development of acute tolerance in diuresis can mainly be attributed to negative water balance under this special condition; and (iii) at steady state the hourly diuresis and natriuresis can differ up to about 6·87‐ and 5·21‐fold between treatments. Some implications for the bioequivalence evaluation of dosage forms of azosemide are discussed. © 1997 John Wiley & Sons, Ltd.

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The effect of renin and aldosterone inhibition by β-adrenergic blockade on the response to the new diuretic azosemide

Cited by 8 publications

References 14 publications

Pharmacokinetics and pharmacodynamics of azosemide

Pharmacokinetics and pharmacodynamics of azosemide

Effect of Azosemide on the in vitro Perfused Thick Ascending Limb of Henle’s Loop from the Mouse

Effects of the rate and composition of fluid replacement on the pharmacokinetics and pharmacodynamics of intravenous azosemide

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The effect of renin and aldosterone inhibition by β-adrenergic blockade on the response to the new diuretic azosemide

Cited by 8 publications

References 14 publications

Pharmacokinetics and pharmacodynamics of azosemide

Pharmacokinetics and pharmacodynamics of azosemide

Effect of Azosemide on the in vitro Perfused Thick Ascending Limb of Henle&rsquo;s Loop from the Mouse

Effects of the rate and composition of fluid replacement on the pharmacokinetics and pharmacodynamics of intravenous azosemide

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Effect of Azosemide on the in vitro Perfused Thick Ascending Limb of Henle’s Loop from the Mouse