Comparison of the pharmacodynamic effect of muzolimine and furosemide in patients with advanced chronic renal insufficiency

Schmidt, Paul; Loew, D.; Dycka, J.; Kopsa, H; Balcke, P; Zazgórnik, J; Deutsch, Erwin

doi:10.1007/bf00716380

Cited by 12 publications

(5 citation statements)

References 11 publications

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“…High ceiling diuretics such as furosemide block prostaglandin degradation in the kid ney by inhibiting prostaglandin dehydroge nase [55], Muzolimine, whose molecule is structurally closely related to nafazatrom, is also a high ceiling diuretic [56]. The possibil ity that nafazatrom likewise inhibits vessel wall prostaglandin dehydrogenase is at present being actively investigated.…”

Section: Inhibition Of Prostacyclin Degradationmentioning

confidence: 99%

A Pharmacological Approach to the Inhibition of Platelet Adhesion and Platelet Aggregation

Verstraete¹

1982

Pathophysiol Haemos Thromb

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A first level of pharmacological interference with platelet function is located at the site of the agonist-receptor interaction (receptors for collagen, adenosine diphosphate, serotonin, fibrinogen). A second level of interaction is to prevent the mobilization of intra-cellular calcium ions which can be obtained by inhibition of phosphodiesterase, activation of cAMP (e.g. with prostacyclin analogues), inhibition of thromboxane A₂ formation or blocking of its receptors. Compounds preventing the platelet contractile process or platelet secretion could theoretically also prevent some platelet functions.

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Section: Inhibition Of Prostacyclin Degradationmentioning

confidence: 99%

A Pharmacological Approach to the Inhibition of Platelet Adhesion and Platelet Aggregation

Verstraete¹

1982

Pathophysiol Haemos Thromb

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“…Muzolimine, lacking the sulfonamido radical and carbonic anhydrase inhibitory activity in vitro (B. Garthoff, unpublished observation), seems to have almost no effect on phosphate and bicarbonate excretion (51,93). Furthermore, the most unpleasant side effect of diuretic treatment, kaliuresis, was lower than with furosemide in animal studies (29) and man (6,21,51,86,99). Thus it is not surprising that during long-term treatment with muzolimine in hypertension, plasma potassium levels were not significantly different from those under the combination of hydrochlorothiazide with the potassium-sparing diuretic amiloride (100).…”

Section: Discussionmentioning

confidence: 94%

“…In patients with chronic cardiac failure and in those with a mild to moderate degree of renal insufficiency, the maximum effect generally occurred between 1 and 4 hr, and the duration of effect lasted for 12 hr (up to 24 hr) without any indication of a rebound phenomenon (6,7,21,43,47,80,93). In advanced renal insufficiency, maximum effect and duration of action were delayed, i.e., 3 to 5 and 24 hr and more (6,43,80,86,87). In patients with hepatic ascites and concomitant spironolactone treatment, the maximum effect was reached after 6 hr, and diuretic action persisted for up to 24 hr (54).…”

Section: Clinical Pharmacologymentioning

confidence: 97%

“…A dose of 40 mg for test subjects (36) and for patients with cardiac edema (6,21) showed a distinctly stronger effect on sodium, chloride, and water excretion than did 40 mg furosemide. In patients with advanced renal insufficiency-independent of hemodialysis-muzolimine at 240 mg was more effective than furosemide at 240 or even 500 mg (86,87,99). In healthy volunteers, muzolimine at 30 mg and furosemide at 40 mg proved to be equally effective, while the time-response curve showed different profiles.…”

Section: Clinical Pharmacologymentioning

confidence: 98%

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Muzolimine

Garthoff

Hanisch

1984

Cardiovascular Drug Reviews

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“…The main reasons are the different pharmacokinetics as well as the different sites of action on the nephron (15,16,17). Among the more modern diuretics only muzolimine seems to fulfil some of these desirable requirements such as high ceiling and protracted effect (18,23,24,28,31).…”

Section: Introductionmentioning

confidence: 99%

Bioavailability and elimination kinetics of the combination furosemide-retard/triamterene

Schuster¹,

Loew²,

Knoell³

1985

European Journal of Drug Metabolism and Pharmacokinetics

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In a pharmacokinetic study on 18 healthy male volunteers the bioavailability and elimination kinetics of furosemide-retard and the combination furosemide-retard/triamterene were investigated and compared with the non-retarded form and another retard form of furosemide. The relative bioavailability of the non-retarded form of furosemide was distinctly reduced by the retardation in the substances investigated. It varied between 42-66% in the plasma and between 37-73% in the urine. In the combination with triamterene the serum concentration time curve of furosemide was only slightly modified but the renal excretion of furosemide was more influenced (36% for furosemide-retard and 25% for furosemide-retard/triamterene). In comparison, the values for the renal excretion of triamterene and OH-TA sulfate were distinctly greater than those obtained after administration of triamterene alone. A renewed increase of the plasma concentration and renal excretion of furosemide were observed between 9 and 10.5 h after administration of furosemide-retard/triamterene. This observation suggests that a further absorption of furosemide occurs as a consequence of the delayed release from distal parts of the small intestine or from the large intestine.

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Comparison of the pharmacodynamic effect of muzolimine and furosemide in patients with advanced chronic renal insufficiency

Cited by 12 publications

References 11 publications

A Pharmacological Approach to the Inhibition of Platelet Adhesion and Platelet Aggregation

A Pharmacological Approach to the Inhibition of Platelet Adhesion and Platelet Aggregation

Muzolimine

Bioavailability and elimination kinetics of the combination furosemide-retard/triamterene

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