Canrenoate potassium

Spironolactone is the most clinically usehil steroidal aldosterone antagonist, and unlike GR antagonists, this compound is utilized much more frequendy than aldosterone agonists. Interfering with reabsorption and secretion in the late distal segment, this compound is predominantiy used with other diuretics. Canrenone, an olefinic metaboHte of spironolactone, and potassium canrenoate, in which the C-17 lactone has been hydrolyzed open, are also potent mineralocorticoid antagonists. 

Potassium canrenoate, 174 Potassium mexrenoate, 175 Potassium prorenoate, 175 Poultry, epidemics in, 366 Practolol, 106, 108 Pranolium chloride, 212 Prazepam, 405 Prazosin, 382 Prednisolone, 178 Prednival, 179 Probucol, 126 Procarbazine, 27 Prodolic acid, 459 Prodrug, 48, 50, 89, 198, 363... 

Spironolactone is poorly absorbed after oral administration and has a delayed onset of action it may take several days until a peak effect is produced. It has a somewhat slower onset of action than triamterene and amiloride (discussed later), but its natriuretic effect is modestly more pronounced, especially during long-term therapy. Spironolactone is rapidly and extensively metabolized, largely to the active metabohte canrenone. Canrenone and potassium canrenoate, its K+ salt, are available for clinical use in some countries outside the United States. Canrenone has a half-life of approximately 10 to 35 hours. The metabolites of spironolactone are excreted in both the urine and feces. New selective aldosterone receptor antagonists (SARA), such as eplerenone, have been developed but have not yet been introduced into clinical practice. Eplerenone and canrenone exhibit fewer steroidlike side effects (gynecomastia, hirsutism). 

Spironolactone (J. A. Cella et al., 1957) is deemed to be the preparation of first choice. Its clinical efficacy has been substantiated in numerous studies. The onset of effect is after 8 to 24 hours. The natriuretic/diuretic action is maintained for 1 or 2 days. A faster onset of effect is given by potassium canrenoate, available as an i.v. application, particularly when absorption is assumed to be impaired or if oral administration is not possible. Spironolactone is not primarily considered to be a diuretic agent, but more a substance with neurohumoral action. (107, 111, 114, 115, 117, 118, 129, 133, 135, 138 quot. 15)... 

The dosage of spironolactone is 100 to 400 mg/day in 2-3 single doses. That of potassium canrenoate amounts 100 to 800 mg/day. When therapy commences with potassium canrenoate, spironolactone should be administered orally 1-2 days prior to the intended termination of the i.v. application to ensure a smooth transition, since the onset of its effect is delayed. In 25-30% of male patients, long-term application leads to (generally reversible) potency disorders and gynaecomastia. 

The information presented in section 3.9.4 (s. p. 786) similarly provides a basis for adjuvant or unconventional treatment and for general care of tumour patients with metastases. (s. tab. 37.10) In addition, the perioperative use of galactose may be worth considering in surgical (or invasive) treatment of metastases, especially since it is without side effects and does not involve undue costs. Furthermore, we would like to point out that the administration of zinc and selenium as well as potassium canrenoate is useful when planning a resection of metastases. (s. p. 787)... 

The importance of an adequate supply of zinc is now accepted. In most cases, however, there is already a deficiency of this important trace element (unless previous medication has remedied the situation). Due to the scale of the operation, there is a considerable loss of zinc, which usually cannot be balanced even by intravenous substitution. Experience has shown that pronounced and extremely detrimental zincuria may be kept in check by i.v. application of potassium canrenoate. (s. p. 787 )... 

Emili M, Cuppone R, Ricci GL. Comparative clinical study of spironolactone and potassium canrenoate. A randomized... 

Datta P, Dasgupta A. A new turbidometric digoxm immunoassay on the AD VIA 1650 analyzer is free from interference by spironolactone, potassium canrenoate, and their common metabohte canrenone. Ther Drug Monit 2003 25(4) 478-82. 

ALDOSTERONE ANTAGONISTS (e.g. potassium canrenoate and spironolactone) work by blocking the action of the hormone aldosterone (a MINERALOCORTICOId), and this makes them suitable for treating oedema associated with aldosteronism, liver failure and certain heart conditions. 

Potaba aminobenzoic acid, potassium canrenoate canrenoicadd. POTASSIUM-CHANNEL ACTIVATORS are agents that modulate, activate or open one or other of the many types of potassium channels that are found in cell membranes. 

FIGURE 16.2 In vivo the inactive potassium canrenoate cycUzes to canrenone. ... 

Free acid potassium salt, C+dl KO. potassium canreno-ate, Kanrenot, Soldactone, Venactone. 

Potassium canrenoate. This is a water-soluble prodrug and can be administered parenterally (Fig. 14.2). It has no intrinsic activity, but it can exert its diuretic activity (as an aldosterone antagonist) because of its interconversion with... 

The canrenoate anion is not active per se but acts as an aldosterone antagonist because of its conversion to canrenone. which exists in the lactone form. Canrenone has been suggested to be the active form of spironolactone as an aldosterone antagonist. The formation of canrenone. however, cannot fully account for the total activity of spironolactone. Both canrenone and potassium canrenoate are used as diuretics in other countries, but they are not yet available in the United States. 

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