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Namespace Prefixes

PrefixIRI
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Statements

Subject Item
n2:DB00421
rdf:type
n3:Drug
n3:description
A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827)
n3:dosage
n16:271B493C-363D-11E5-9242-09173F13E4C5 n16:271B493D-363D-11E5-9242-09173F13E4C5 n16:271B493E-363D-11E5-9242-09173F13E4C5 n16:271B4939-363D-11E5-9242-09173F13E4C5 n16:271B493A-363D-11E5-9242-09173F13E4C5 n16:271B493B-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Berardesca E, Gabba P, Ucci G, Borroni G, Rabbiosi G: Topical spironolactone inhibits dihydrotestosterone receptors in human sebaceous glands: an autoradiographic study in subjects with acne vulgaris. Int J Tissue React. 1988;10(2):115-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/2972662 # Pitt B, Zannad F, Remme WJ, Cody R, Castaigne A, Perez A, Palensky J, Wittes J: The effect of spironolactone on morbidity and mortality in patients with severe heart failure. Randomized Aldactone Evaluation Study Investigators. N Engl J Med. 1999 Sep 2;341(10):709-17. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/10471456 # Wandelt-Freerksen E: [Aldactone in the treatment of sarcoidosis of the lungs (author's transl)] Z Erkr Atmungsorgane. 1977 Jul;149(1):156-9. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/607621
n3:group
approved
n3:halfLife
10 minutes
n3:indication
Used primarily to treat low-renin hypertension, hypokalemia, and Conn's syndrome.
n3:manufacturer
n4:271B4925-363D-11E5-9242-09173F13E4C5 n4:271B4924-363D-11E5-9242-09173F13E4C5 n4:271B4926-363D-11E5-9242-09173F13E4C5 n4:271B4922-363D-11E5-9242-09173F13E4C5 n4:271B4923-363D-11E5-9242-09173F13E4C5 n4:271B4929-363D-11E5-9242-09173F13E4C5 n4:271B492A-363D-11E5-9242-09173F13E4C5 n4:271B4927-363D-11E5-9242-09173F13E4C5 n4:271B4928-363D-11E5-9242-09173F13E4C5 n4:271B491C-363D-11E5-9242-09173F13E4C5 n4:271B491D-363D-11E5-9242-09173F13E4C5 n4:271B491B-363D-11E5-9242-09173F13E4C5 n4:271B4920-363D-11E5-9242-09173F13E4C5 n4:271B4921-363D-11E5-9242-09173F13E4C5 n4:271B491E-363D-11E5-9242-09173F13E4C5 n4:271B491F-363D-11E5-9242-09173F13E4C5
owl:sameAs
n13:DB00421 n31:DB00421
dcterms:title
Spironolactone
adms:identifier
n15:50228080 n17:PA451483 n18:5833 n19:0781-1599-01 n20:SNL n21:46508525 n22:DB00421 n23:9241 n24:5628 n25:C07310 n26:D00443 n27:2875 n28:2875 n34:Spironolactone
n3:mechanismOfAction
Spironolactone is a specific pharmacologic antagonist of aldosterone, acting primarily through competitive binding of receptors at the aldosterone-dependent sodium-potassium exchange site in the distal convoluted renal tubule. Spironolactone causes increased amounts of sodium and water to be excreted, while potassium is retained. Spironolactone acts both as a diuretic and as an antihypertensive drug by this mechanism. It may be given alone or with other diuretic agents which act more proximally in the renal tubule. Aldosterone interacts with a cytoplasmic mineralocorticoid receptor to enhance the expression of the Na+, K+-ATPase and the Na+ channel involved in a Na+ K+ transport in the distal tubule . Spironolactone bind to this mineralcorticoid receptor, blocking the actions of aldosterone on gene expression. Aldosterone is a hormone; its primary function is to retain sodium and excrete potassium in the kidneys.
n3:packager
n4:271B4915-363D-11E5-9242-09173F13E4C5 n4:271B4912-363D-11E5-9242-09173F13E4C5 n4:271B4913-363D-11E5-9242-09173F13E4C5 n4:271B491A-363D-11E5-9242-09173F13E4C5 n4:271B48EC-363D-11E5-9242-09173F13E4C5 n4:271B48ED-363D-11E5-9242-09173F13E4C5 n4:271B48EA-363D-11E5-9242-09173F13E4C5 n4:271B48EB-363D-11E5-9242-09173F13E4C5 n4:271B48E8-363D-11E5-9242-09173F13E4C5 n4:271B48E9-363D-11E5-9242-09173F13E4C5 n4:271B48F4-363D-11E5-9242-09173F13E4C5 n4:271B4911-363D-11E5-9242-09173F13E4C5 n4:271B48F2-363D-11E5-9242-09173F13E4C5 n4:271B48F3-363D-11E5-9242-09173F13E4C5 n4:271B48F0-363D-11E5-9242-09173F13E4C5 n4:271B48F1-363D-11E5-9242-09173F13E4C5 n4:271B48EE-363D-11E5-9242-09173F13E4C5 n4:271B48EF-363D-11E5-9242-09173F13E4C5 n4:271B4910-363D-11E5-9242-09173F13E4C5 n4:271B4906-363D-11E5-9242-09173F13E4C5 n4:271B4907-363D-11E5-9242-09173F13E4C5 n4:271B4904-363D-11E5-9242-09173F13E4C5 n4:271B4905-363D-11E5-9242-09173F13E4C5 n4:271B4902-363D-11E5-9242-09173F13E4C5 n4:271B4903-363D-11E5-9242-09173F13E4C5 n4:271B4900-363D-11E5-9242-09173F13E4C5 n4:271B4901-363D-11E5-9242-09173F13E4C5 n4:271B490E-363D-11E5-9242-09173F13E4C5 n4:271B490F-363D-11E5-9242-09173F13E4C5 n4:271B490C-363D-11E5-9242-09173F13E4C5 n4:271B490D-363D-11E5-9242-09173F13E4C5 n4:271B490A-363D-11E5-9242-09173F13E4C5 n4:271B490B-363D-11E5-9242-09173F13E4C5 n4:271B4908-363D-11E5-9242-09173F13E4C5 n4:271B4909-363D-11E5-9242-09173F13E4C5 n4:271B48F6-363D-11E5-9242-09173F13E4C5 n4:271B48F7-363D-11E5-9242-09173F13E4C5 n4:271B48F5-363D-11E5-9242-09173F13E4C5 n4:271B48FE-363D-11E5-9242-09173F13E4C5 n4:271B48FF-363D-11E5-9242-09173F13E4C5 n4:271B48FC-363D-11E5-9242-09173F13E4C5 n4:271B48FD-363D-11E5-9242-09173F13E4C5 n4:271B48FA-363D-11E5-9242-09173F13E4C5 n4:271B48FB-363D-11E5-9242-09173F13E4C5 n4:271B48F8-363D-11E5-9242-09173F13E4C5 n4:271B48F9-363D-11E5-9242-09173F13E4C5 n4:271B4918-363D-11E5-9242-09173F13E4C5 n4:271B4919-363D-11E5-9242-09173F13E4C5 n4:271B4916-363D-11E5-9242-09173F13E4C5 n4:271B4917-363D-11E5-9242-09173F13E4C5 n4:271B4914-363D-11E5-9242-09173F13E4C5
n3:routeOfElimination
The metabolites are excreted primarily in the urine and secondarily in bile.
n3:synonym
Spironolattone Spironolactonum Spironolactone Espironolactona
n3:toxicity
The oral LD<sub>50</sub> of spironolactone is greater than 1,000 mg/kg in mice, rats, and rabbits. Acute overdosage of spironolactone may be manifested by drowsiness, mental confusion, maculopapular or erythematous rash, nausea, vomiting, dizziness, or diarrhea. Spironolactone has been shown to be a tumorigen in chronic toxicity studies in rats.
n10:hasAHFSCode
n11:24-32-20
n3:foodInteraction
Avoid alcohol. Food increases the bioavailability of spironolactone by almost 100%. Spironolactone may decrease the excretion of potassium. Salt substitutes containing potassium increase the risk of hyperkalemia.
n3:mixture
n30:271B48E3-363D-11E5-9242-09173F13E4C5 n30:271B48E6-363D-11E5-9242-09173F13E4C5 n30:271B48E7-363D-11E5-9242-09173F13E4C5 n30:271B48E4-363D-11E5-9242-09173F13E4C5 n30:271B48E5-363D-11E5-9242-09173F13E4C5
n3:proteinBinding
Spironolactone and its metabolites are more than 90% bound to plasma proteins.
n3:synthesisReference
Giuseppe Bernini, "Process for preparing micronized spironolactone." U.S. Patent US4332721, issued July, 1975.
foaf:page
n9:ald1010.shtml n29:spironolactone.html n32:spiron.htm
n3:IUPAC-Name
n5:271B4943-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B4949-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B4948-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B4945-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B4946-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B4947-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B4941-363D-11E5-9242-09173F13E4C5 n5:271B4959-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B495B-363D-11E5-9242-09173F13E4C5 n5:271B493F-363D-11E5-9242-09173F13E4C5 n5:271B4942-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B495C-363D-11E5-9242-09173F13E4C5 n5:271B4940-363D-11E5-9242-09173F13E4C5
n10:hasATCCode
n33:C03DA01
n3:H-Bond-Acceptor-Count
n5:271B494F-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B4950-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B494A-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B494B-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B494D-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B494C-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B494E-363D-11E5-9242-09173F13E4C5
n3:absorption
Fairly rapidly absorbed from the gastrointestinal tract. Food increases the bioavailability of unmetabolized spironolactone by almost 100%.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
52-01-7
n3:category
n3:containedIn
n6:271B4938-363D-11E5-9242-09173F13E4C5 n6:271B4936-363D-11E5-9242-09173F13E4C5 n6:271B4937-363D-11E5-9242-09173F13E4C5 n6:271B4934-363D-11E5-9242-09173F13E4C5 n6:271B4935-363D-11E5-9242-09173F13E4C5 n6:271B492B-363D-11E5-9242-09173F13E4C5 n6:271B4932-363D-11E5-9242-09173F13E4C5 n6:271B4933-363D-11E5-9242-09173F13E4C5 n6:271B4930-363D-11E5-9242-09173F13E4C5 n6:271B4931-363D-11E5-9242-09173F13E4C5 n6:271B492E-363D-11E5-9242-09173F13E4C5 n6:271B492F-363D-11E5-9242-09173F13E4C5 n6:271B492C-363D-11E5-9242-09173F13E4C5 n6:271B492D-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n5:271B4955-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B4957-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B4958-363D-11E5-9242-09173F13E4C5
n3:Melting-Point
n5:271B495A-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B4954-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B4953-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B4956-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B4944-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B4951-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B4952-363D-11E5-9242-09173F13E4C5