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Chemical Compound Review

Eurelix     4-phenoxy-3-pyrrolidin-1-yl- 5-sulfamoyl...

Synonyms: Piretanido, Tauliz, piretanide, Arlix, Piretanidum, ...
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Disease relevance of Arelix

  • The study suggests that oral piretanide is a relatively safe and effective diuretic for treating congestive heart failure with a potential advantage of having potassium-sparing properties [1].
  • Only one patient treated with the highest allowed dose of piretanide developed mild hypokalemia [1].
  • BUN increased in nine piretanide-treated patients; two were discontinued from the study because of progressive azotemia [1].
  • Thus, piretanide appears to offer an effective alternative to other 'loop' diuretics for the treatment of oedematous diseases and to hydrochlorothiazide for the management of mild to moderate hypertension [2].
  • When used to treat oedema caused by liver disease, piretanide 12 to 24 mg/day was successful in only about 50% of patients, but spironolactone added to the treatment regimen greatly increased the response rate [2].

High impact information on Arelix

  • However, the addition of spironolactone, 150 mg/day, to piretanide was followed in these patients by a marked increase in diuresis and natriuresis [3].
  • Plasma renin activity (PRA) and plasma aldosterone concentration (PAC) were normal or only slightly increased in patients who responded to piretanide (PRA = 1.22 +/- 0.20 ng/ml/h; PAC = 12.25 +/- 2.20 ng/100 ml) and very high in patients who did not respond (PRA = 8.71 +/- 1.18 ng/ml/h; PAC = 84.6 +/- 16.2 ng/100 ml) (P < 0.001) [3].
  • The addition of digoxin for 2 wk after piretanide alone for 2 wk did not decrease serum potassium and TBK, but RCP fell under the influence of piretanide with digoxin [4].
  • Bumetanide, furosemide, and piretanide have similar pharmacokinetics, whereas the clearance of torasemide is less and the half-life concomitantly longer than the other 3 agents [5].
  • 5. Comparison of data from the vas and taenia showed that 36Cl efflux into Cl(-)-free, HCO3(-)-free solution was about twice as fast in the taenia, and that bumetanide or piretanide reduced this efflux to about the same rate as that observed in the vas with or without the loop diuretic [6].

Chemical compound and disease context of Arelix


Biological context of Arelix

  • The effect of the loop diuretic, piretanide (12 mg/day on blood pressure and intracellular electrolyte composition in red blood cells during a six-week treatment period was studied in 14 previously untreated essential hypertensive patients [11].
  • Acute and chronic effects of the loop diuretic, piretanide, on baroreflex set point and sensitivity in hypertensive man [12].
  • In in vitro experiments piretanide leads to effective inhibition of ADP-induced platelet aggregation with complete inhibition at 5 mM concentration [13].
  • Pretreatment with probenecid produced significant increases in absolute peak and plasma diuretic concentrations, t1/2 and mean residence time while decreasing steady-state volume of distribution, total clearance, renal clearance and fraction of unchanged drug excreted without affecting the bioavailability of piretanide [14].
  • The present results indicate that tubular secretion of piretanide is important for the diuretic response and that piretanide inhibits the fluid absorption in the loop of Henle and the tubuloglomerular feedback control which would otherwise blunt the diuretic response with a reduction in glomerular filtration rate [15].

Anatomical context of Arelix

  • Piretanide is a potent 'loop' diuretic whose principal site of action is in the thick ascending limb of the loop of Henle [2].
  • The demonstrated anionic selectivity, dependence on extracellular Na+ and susceptibility to blockade by the diuretic piretanide would strongly suggest that a coupled Na+-K+-Cl- co-transport system operates in submandibular glands as it does in other transporting epithelia to achieve K+ uptake [16].
  • In cells which have normally directed gradients of Na+ and K+, chronic incubation in piretanide (10(-4) M) for up to 24 hr has no significant effect on the internal ion contents of HeLa (human carcinoma), MDCK (dog kidney epithelium) or BC3H1 (mouse smooth muscle) cell lines [17].
  • Piretanide abolished the dorsal root potential elicited by ventral root stimulation [18].
  • Characterization of a high affinity piretanide receptor on kidney membranes [19].

Associations of Arelix with other chemical compounds


Gene context of Arelix

  • The inhibitory action of SRIF on basal SCC was suppressed by piretanide and diphenylamine-2-carboxylate, compatible with the assumption that the Na+K+2Cl- co-transporter and Cl- channels, respectively, may be involved in this antisecretory action of SRIF [22].
  • RESULTS: Independent of the basal TPMT activity, lowest IC50 values were calculated for furosemide (15-19 microM), followed by testosterone (30-72 microM), piretanide (300-313 microM) and AZA (430-532 microM) [23].
  • TBK and RCP were measured before treatment to establish baseline values, after which all subjects received 6 mg piretanide a day for 14 days [4].
  • 4. Responses to both peptides were inhibited by the presence of transport inhibitors, particularly diphenylamine-2-carboxylate (DPC, a chloride channel blocker) and piretanide (Na+-K+-2Cl- co-transport inhibitor) [24].
  • 4. In both cell lines r alpha-CGRP-elevated short-circuit current was inhibited by the loop diuretic piretanide (200 microM) and by somatostatin (100 nM) [25].

Analytical, diagnostic and therapeutic context of Arelix


  1. Piretanide, a potent diuretic with potassium-sparing properties, for the treatment of congestive heart failure. Sherman, L.G., Liang, C.S., Baumgardner, S., Charuzi, Y., Chardo, F., Kim, C.S. Clin. Pharmacol. Ther. (1986) [Pubmed]
  2. Piretanide. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy. Clissold, S.P., Brogden, R.N. Drugs (1985) [Pubmed]
  3. Use of piretanide, a new loop diuretic, in cirrhosis with ascites: relationship between the diuretic response and the plasma aldosterone level. Arroyo, V., Bosch, J., Casamitjana, R., Cabrera, J., Rivera, F., Rodés, J. Gut (1980) [Pubmed]
  4. Potassium balance in piretanide and digoxin treatment. Muller, F.O., Meyer, B.H., de Waal, A., van Reenen, O.R., Grigoleit, H.G. Clin. Pharmacol. Ther. (1982) [Pubmed]
  5. Clinical pharmacology of loop diuretics. Brater, D.C. Drugs (1991) [Pubmed]
  6. The effect of loop diuretics on Cl- transport in smooth muscle of the guinea-pig vas deferens and taenia from the caecum. Aickin, C.C., Brading, A.F. J. Physiol. (Lond.) (1990) [Pubmed]
  7. Usefulness of piretanide plus ramipril for systemic hypertension: a multicenter trial. Homuth, V., Faulhaber, H.D., Loose, U., Löffler, K., Luft, F.C. Am. J. Cardiol. (1993) [Pubmed]
  8. Acute effect of high dose (48 mg) of piretanide in advanced renal insufficiency. Hadj Aissa, A., Pozet, N., Labeeuw, M., Pellet, M., Traeger, J. British journal of clinical pharmacology. (1981) [Pubmed]
  9. A decade of developments in diuretic drug therapy. Hutcheon, D.E., Martinez, J.C. Journal of clinical pharmacology. (1986) [Pubmed]
  10. Efficacy of penbutolol + piretanide combinations in the treatment of arterial hypertension. Verho, M., Rangoonwala, B., Pahnke, K., Freude, J., Häringer, E. Drugs under experimental and clinical research. (1985) [Pubmed]
  11. Intracellular electrolytes during antihypertensive treatment with a loop diuretic. Zidek, W., Losse, H., Schmidt, W., Fehske, K.J., Vetter, H. J. Hypertens. (1984) [Pubmed]
  12. Acute and chronic effects of the loop diuretic, piretanide, on baroreflex set point and sensitivity in hypertensive man. Young, M.A., Watson, R.D., Littler, W.A. J. Hypertens. (1985) [Pubmed]
  13. Piretanide: a new synthetic fibrinolytic and anti-platelet agent. Chohan, I.S. Thromb. Haemost. (1986) [Pubmed]
  14. Renal responses and pharmacokinetics of piretanide in humans: effect of route of administration, state of hydration and probenecid pretreatment. Noormohamed, F.H., McNabb, W.R., Dixey, J.J., Lant, A.F. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  15. Renal tubular secretion of piretanide and its effects on electrolyte reabsorption and tubuloglomerular feedback mechanism. Odlind, B., Beermann, B., Selén, G., Persson, A.E. J. Pharmacol. Exp. Ther. (1983) [Pubmed]
  16. Potassium uptake in the mouse submandibular gland is dependent on chloride and sodium and abolished by piretanide. Exley, P.M., Fuller, C.M., Gallacher, D.V. J. Physiol. (Lond.) (1986) [Pubmed]
  17. An effect of piretanide upon the intracellular cation contents of cells subjected to partial chronic (Na-K) pump blockade by ouabain. Aiton, J.F., Simmons, N.L. Biochem. Pharmacol. (1984) [Pubmed]
  18. Selective action of piretanide on primary afferent GABA responses in the frog spinal cord. Wojtowicz, J.M., Nicoll, R.A. Brain Res. (1982) [Pubmed]
  19. Characterization of a high affinity piretanide receptor on kidney membranes. Giesen-Crouse, E.M., Welsch, C., Imbs, J.L., Schmidt, M., Schwartz, J. Eur. J. Pharmacol. (1985) [Pubmed]
  20. Effects of furosemide, piretanide, and water loading on urinary excretion of cefazolin in humans. Morgant, C., Contrepois, A., Chau, N.P., Romaru, A., Fourtillan, J.B., Carbon, C. Antimicrob. Agents Chemother. (1984) [Pubmed]
  21. Vascular effects of loop diuretics: an in vivo and in vitro study in the rat. Barthelmebs, M., Stephan, D., Fontaine, C., Grima, M., Imbs, J.L. Naunyn Schmiedebergs Arch. Pharmacol. (1994) [Pubmed]
  22. Somatostatin receptors mediating inhibition of basal and stimulated electrogenic ion transport in rat isolated distal colonic mucosa. McKeen, E.S., Feniuk, W., Humphrey, P.P. Naunyn Schmiedebergs Arch. Pharmacol. (1995) [Pubmed]
  23. Thiopurine S-methyltransferase as a target for drug interactions. Xin, H.W., Fischer, C., Schwab, M., Klotz, U. Eur. J. Clin. Pharmacol. (2005) [Pubmed]
  24. The effect of neuropeptide Y and peptide YY on electrogenic ion transport in rat intestinal epithelia. Cox, H.M., Cuthbert, A.W., Håkanson, R., Wahlestedt, C. J. Physiol. (Lond.) (1988) [Pubmed]
  25. Calcitonin gene-related peptide receptors in human gastrointestinal epithelia. Cox, H.M., Tough, I.R. Br. J. Pharmacol. (1994) [Pubmed]
  26. Bumetanide stimulation of sodium permeability of the apical membrane of toad urinary bladder. Li, J.H., Kau, S.T. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  27. The pharmacokinetics and diuretic effects of piretanide in chronic renal insufficiency. Berg, K.J., Walstad, R.A., Bergh, K. British journal of clinical pharmacology. (1983) [Pubmed]
  28. A single dose comparison of piretanide and bumetanide in congestive cardiac failure. Homeida, M., Roberts, C.J., Dombey, S.L. British journal of clinical pharmacology. (1979) [Pubmed]
  29. Quantitative evaluation of ototoxic side effects of furosemide, piretanide, bumetanide, azosemide and ozolinone in the cat--a new approach to the problem of ototoxicity. Göttl, K.H., Roesch, A., Klinke, R. Naunyn Schmiedebergs Arch. Pharmacol. (1985) [Pubmed]
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