Aldactone should be used only in those conditions described under indications and usage. Spironolactone and its active metabolites are specific pharmacologic antagonists of aldosterone, acting primarily through competitive binding of receptors at the aldosteronedependent sodiumpotassium. It is available in a 118 ml bottle ndc 4628702004 and a 473 ml. Acts primarily through competitive binding of receptors at the aldosterone dependent sodiumpotassium exchange site in the distal convoluted renal tubule. Oct 21, 2019 spironolactone pharmacokinetics absorption. Kaiser permanente medical care program, whose computerized pharmacy.
Review of the role of spironolactone in the therapy of children. Implement fallprevention strategies, especially in older adults or if patient exhibits sedation, dizziness, clumsiness, or other impairments that affect gait and balance see appendix e. Spironolactone and its active metabolites are specific pharmacologic antagonists of aldosterone, acting primarily through competitive binding of receptors at the aldosteronedependent sodiumpotassium exchange site in the distal convoluted renal tubule. Spironolactone has multiple actions including antimineralocorticoid and antiandrogenic activities, as well as estrogenic and progestogenic activities.
Spironolactone causes increased amounts of sodium and water to be excreted, while potassium is retained. Aldosterone antagonist antimineralocorticoid, mcra see online here aldosterone antagonist are diuretic drugs that used in treatment of congestive heart failure. Spironolactone pharmacokinetics and pharmacodynamics in. Spironolactone is the generic form of the brandname drug aldactone, a prescription diuretic drug.
The diuretic and antihypertensive effects of the individual components are potentiated when spironolactone and hydrochlorothiazide are given concurrently. Heart failure pharmacology maureen schaupp, msn, cnp, chfn cleveland clinic section of advanced heart failure and cardiac transplant. Spironolactone, sold under the brand name aldactone among others, is a medication that is primarily used to treat fluid buildup due to heart failure, liver scarring, or kidney disease. Aldactone, carospir spironolactone dosing, indications. If more than one dose a day is required, give the last dose before 6 pm unless your doctor tells you differently. Aldactone spironolactone is a specific pharmacologic antagonist of aldosterone, acting primarily through competitive binding of receptors at. Spironolactone is indicated for the treatment of new york heart association class iiiiv heart failure, management of edema in cirrhotic adults not responsive to fluid and sodium restrictions, primary. Links to pubmed are also available for selected references. Initially, 100 mgday range 25200 mgday when given as the sole agent. New insights into the pharmacokinetics of spironolactone. Spironolactone causes increased amounts of sodium and water to be excreted, while potassium.
Spironolactone is practically insoluble in water, soluble in alcohol, and freely soluble in benzene and in chloroform. Medscape hypertension, congestive heart failure, hyperaldosteronismspecific dosing for aldactone, carospir spironolactone, frequencybased adverse effects, comprehensive interactions. Spironolactone and 7 alphathiomethyl spironolactone were detected at 245 nm, while canrenone and internal standard were detected at 280 nm. Continue to take spironolactone even if you feel well. Aldactone has been shown to be a tumorigen in chronic toxicity studies in rats see precautions. The drug is used to treat a condition called primary hyperaldosteronism, in which the body. Spironolactone crosses the placenta regitzzagrosek esc 2018. The 140 must know meds demolish nursing pharmacology pdf free download file has been uploaded to our online repository for the safer downloading of the file. Maximum effect of spironolactone therapy may not occur for up to two weeks after starting treatment. Webmd provides common contraindications for spironolactone oral. Spironolacotone and eplerenone are mineralocorticoidblocking agents used for their ability to block both the epithelial and nonepithelial actions of aldosterone. Aldosterone antagonist antimineralocorticoid, mcra see online here aldosterone antagonist are diuretic drugs that used in treatment of congestive heart failure or hypertension and increase survival rate in cardiac patients. Pharmacological differences between spironolactone and eplerenone are discussed. Full text full text is available as a scanned copy of the original print version.
Learn vocabulary, terms, and more with flashcards, games, and other study tools. In this part of the article, you will be able to download the usmle pharmacology and treatment flashcards in. The intent of this study was to identify pharmacokinetic and pharmacodynamic characteristics for spironolactone sp and its metabolites canrenone, 6 betahydroxy7 alphathiomethylspirolactone, 7. Pharmacokinetics spironolactone is rapidly and extensively metabolized. Spironolactone tablets, 25 mg contain the following inactive ingredients. The most relevant action is as an aldosterone antagonist at the mineralocorticoid receptor in the cortical collecting duct of renal nephrons, an action which decreases renal sodium and water. This material is provided for educational purposes only and is not intended for medical advice, diagnosis or treatment. Usmle pharmacology and treatment flashcards pdf free download. Spironolactone is a specific pharmacological antagonist of aldosterone. It may be given alone or with other diuretic agents that act more proximally in the renal tubule. Pdf spironolactone management of resistant hypertension. Aldactone spironolactone is a useful agent in the diagnosis of primary hyperaldosteronism. Aldactone causes increased amounts of sodium and water to be.
Spironolactone daviss drug guide for rehabilitation. Spironolactone oral tablet is a prescription medication used to reduce swelling caused by fluid buildup in your tissues. The tritium concentrations in plasma reached a peak between 2540 min after administration amounting to. Spironolactone controls high blood pressure, edema, heart failure, and hyperaldosteronism but does not cure these conditions. Spironolactone oral interactions with other medication. Get a printable copy pdf file of the complete article 461k, or click on a page image below to browse page by page. Spironolactone acts both as a diuretic and as an antihypertensive drug by this mechanism. Find out what health conditions may be a health risk when taken with spironolactone oral. The major active forms of spironolactone include 7. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs. The diuretic and antihypertensive effects of the individual components are. Aldactone spironolactone is a specific pharmacologic antagonist of aldosterone, acting primarily through competitive binding of receptors at the aldosteronedependent sodiumpotassium exchange site in the distal convoluted renal tubule. Spironolactone, taken for fluid retention, may take a few days. Physiology of aldosterone and pharmacology of aldosterone blockers.
For 6 days the disposition kinetics of the drug were studied in plasma, urine and feces. Five healthy male volunteers received 500 mg aldactone orally together with 100. Cardiomyopathic hamsters, bio to2 dilated strain, were orally treated with enalapril 20 mg kg. Carospir spironolactone oral suspension 25 mg5 ml is a white to offwhite, opaque, bananaflavored suspension. Its also used to treat high blood pressure and other conditions. Combined effects of enalapril and spironolactone in hamsters. Coadministration of spironolactone with other diuretics in infants with lung.
Pharmacology spironolactone is a synthetic steroid with an aldosteronelike structure. Spironolactone reverses many of the manifestations of aldosteronism spironilactone is also an androgen antagonist and as such is used in the treatment of hirsutism in wormen. Spironolactone reverses many of the manifestations of aldosteronism spironilactone is also an. Vision impaired people having problems accessing certain pages of a pdf file may. Do not stop taking spironolactone without talking to your doctor. Acts primarily through competitive binding of receptors at the aldosterone dependent sodiumpotassium. Aldactone spironolactone is a specific pharmacologic antagonist of aldosterone, acting. Spironolactone is indicated for the treatment of new york heart association class iiiiv heart failure. Spironolactone has a very short biological halflife and is considered to be a prodrug. Capitals indicate lifethreatening, underlines indicate most frequent. The compiled results of spironolactone in individual.
The most relevant action is as an aldosterone antagonist. Usmle pharmacology and treatment flashcards pdf free. The intent of this study was to identify pharmacokinetic and pharmacodynamic characteristics for spironolactone sp and its metabolites canrenone, 6 betahydroxy7 alphathiomethylspirolactone, 7 alphathiomethylspirolactone in cirrhotics under steady state conditions. Causes increased urinary excretion of sodium and water while potassium is retained.
Spironolactone fda prescribing information, side effects. Both spironolactone and hydrochlorothiazide reduce exchangeable sodium, plasma volume, body weight, and blood pressure. It may take about 2 weeks or longer before the full effect of spironolactone occurs. Based on the mechanism of action and data from animal reproduction studies, in utero exposure to spironolactone may cause feminization of a male fetus limited human data. Dec 05, 2018 clinical pharmacology mechanism of action. Pharmacokinetics and pharmacodynamics of mineralocorticoid. Now, in this section of the article, you will be able to get access to the 140 must know meds demolish nursing pharmacology pdf free download file in. Spironolactone is a nonselective mineralocorticoid receptor antagonist with moderate affinity for both progesterone and androgen receptors. Which of the following statements about spironolactone is true. These medications may interact and cause very harmful effects. Nda 12151s062 page 2 aldactone spironolactone tablets, usp warning aldactone has been shown to be a tumorigen in chronic toxicity studies in rats see precautions. Canrenoatek iii was rapidly and quantitatively absorbed.
Nw newborn drug protocol spironolactone pharmacology. Spironolactone and 7 alphathiomethylspironolactone were detected at 245 nm, while canrenone and internal standard were detected at 280 nm. Equimolar doses of spironolactone i, canrenone ii and canrenoatek iii were given orally and iii intravenously to 16 patients. Pharmacokinetics of spironolactone in man springerlink. Description aldactone oral tablets contain 25 mg, 50 mg, or 100 mg of the aldosterone antagonist spironolactone. Spironolactone, taken for fluid retention, may take a few days to work.
Spironolactone is indicated for the treatment of new york heart association class iiiiv heart failure, management of edema in cirrhotic adults not responsive to fluid and sodium restrictions, primary hyperaldosteronism shortterm preoperatively, primary hyperaldosteronism longterm in patients with aldosterone producing adrenal adenomas that are not candidates for surgery or patients with. Data sources include ibm watson micromedex updated 4 may 2020, cerner multum updated 4 may 2020, wolters kluwer updated. The most important of these receptors are situated in the distal portion of the renal tubules. Figure 1 outlines the pharmacological action of spironolactone. Aldactone spironolactone is a specific pharmacologic antagonist of aldosterone, acting primarily through competitive binding of. They act at by competitive antagonism of mineralcorticoid receptors on the. Mineralocorticoid receptor antagonists journal of endocrinology. Antagonism of fludrocortisone by spironolactone and canrenone. The latter property increases the likelihood of endocrine side effects with spironolactone.
1263 636 1606 807 1240 1608 807 1631 146 799 1626 479 1650 769 261 1026 1285 1230 199 780 1589 8 294 488 1400 1192 102 750