China
Africa
Explore chapters and articles related to this topic
Canrenone
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Canrenone is a synthetic pregnadiene compound and aldosterone antagonist with potassium-sparing diuretic activity. It is the major metabolite of spironolactone. The drug is indicated for the treatment of primary hyperaldosteronism, edematous conditions resulting from secondary hyperaldosteronism (congestive heart failure, ascitic liver cirrhosis, nephrotic syndrome) and therapy-resistant essential arterial hypertension (1). As canrenone inhibits 5α-dehydrotestosterone receptors in the pilosebaceous unit and thus has anti-androgenic properties, it has also been suggested for the treatment of acne, hirsutism and alopecia androgenetica (2). In pharmaceutical products, canrenone is usually employed as canrenoate potassium (CAS number 2181-04-6, EC number 218-554-9, molecular formula C22H29KO4) (1).
Kinetic Abnormalities of the Na+,K+ Pump in Essential Hypertension
Published in Antonio Coca, Ricardo P. Garay, Ionic Transport in Hypertension: New Perspectives, 2019
Previous studies suggest that canrenone, an antihypertensive drug, may interfere with the above mechanism. In fact, canrenone is able to interact with the Na+,K+ pump in vitro.173,174 This interaction is expected for a partial agonist at the digitalis receptor site. In addition, canrenone is able to partially antagonize in vivo the secondary effects of ouabain-like substances on cell Na+ handling and blood pressure in rats with reduced renal mass under excess Na+ intake.175 These results suggest that chronic administration of canrenone to patients with essential hypertension may induce a lowering of blood pressure by antagonism with circulating ouabain-like substances at the vascular wall.
Information on level of drugs into breastmilk
Published in Wendy Jones, Breastfeeding and Medication, 2018
Spironolactone is an aldosterone receptor antagonist used as a diuretic in various conditions associated with oedema, as well as in the treatment of hypertension. Its value is in sparing potassium loss. It is metabolised to canrenone, which was found in the breastmilk of one mother taking 25 mg four times a day by Phelps and Karim (1977). They suggested the amount absorbed by the baby would be 0.2% of the mother’s daily dose. Spironolactone is 90% plasma protein bound and has a bio-availability of 90% (Martindale 2017), 70% (Hale 2017).
An overview of mineralocorticoid receptor antagonists as a treatment option for patients with heart failure: the current state-of-the-art and future outlook
Published in Expert Opinion on Pharmacotherapy, 2022
Marta Lorente-Ros, Jose S Aguilar-Gallardo, Aayush Shah, Bharat Narasimhan, Wilbert S. Aronow
Interestingly, results of the TOPCAT trial demonstrated a significant variation based on randomization stratum and by region. Patients who had been enrolled with an elevated BNP/NT-proBNP had a reduction in the composite primary endpoint (HR 0.65, 95% CI 0.49–0.87), as did patients who were enrolled from the Americas (HR 0.82, 95% CI 0.69–0.98), as opposed to patients who were enrolled from Russia or Georgia (HR 1.10, 95% CI 0.79–1.51) [76]. Further analysis in this regional variation revealed differences in baseline characteristics between patients from the Americas and patients from Russia/Georgia, as well as differences in indication for enrollment (patients from Russia and Georgia were mostly enrolled with prior heart failure hospitalization rather than elevated BNP levels), daily dose of study drug, incidence of drug discontinuation, and changes in creatinine and potassium levels in response to spironolactone [77]. Moreover, canrenone (active metabolite of spironolactone) concentrations did not correlate with the reported study drug use and dosing during the trial, with higher prevalence of undetectable canrenone in patients from Russia and Georgia, in spite of the previously reported higher adherence and higher dosing [78].
Treatment of sleep apnea with a combination of a carbonic anhydrase inhibitor and an aldosterone antagonist: a patent evaluation of CA2958110 and IN6616DEN2012
Published in Expert Opinion on Therapeutic Patents, 2018
Andrea Angeli, Claudiu T. Supuran
Aldosterone is a hormone belonging to the mineralocorticoid family, and downstream effector of angiotensin II in the renin–angiotensin–aldosterone system. It is primarily synthesized by the adrenal cortex, but is also present in other tissues leading to local autocrine or paracrine effects [19]. The main activity is sodium reabsorption with concomitant potassium and hydrogen ion excretion and the more widespread effects of hyperaldosteronism include sympathetic nervous system activation, increased oxidant stress with inflammation, remodeling, and apoptosis [20]. Aldosterone antagonists are used for the treatment of several clinical pathologies, such as primary and resistant aldosteronism, heart failure, and chronic kidney disease. In this application, five clinically aldosterone antagonists with different pharmacological characteristics, such as spironolactone, canrenone, eplerenone, mexrenone, and prorenone (Figure 3) have been employed.
Assessment of adherence to diuretics and β-blockers by serum drug monitoring in comparison to urine analysis
Published in Blood Pressure, 2020
Sabrina Ritscher, Coralie Georges, Cora Wunder, Pierre Wallemacq, Alexandre Persu, Stefan W. Toennes
As found in the previous study [13] a rather high proportion of the measured concentrations (50%) failed to comply with published reference data on therapeutic concentrations. Of the 40 determined values 19 (47.5%) fell below the lower limit of the concentration range considered therapeutic [14,15], because these ranges may not reflect concentrations of low doses as part of complex antihypertension medication regimens [13]. This relates especially to the low doses of the β-blocker bisoprolol as well as the diuretics furosemide and spironolactone (assayed via its active metabolite canrenone) (Table 1). Therefore, the present study suggests that the evaluation of adherence using lower DRCs is the more appropriate approach.