Spironolactone
Identification
- Name
- Spironolactone
- Accession Number
- DB00421
- Description
Spironolactone is a potassium sparing diuretic like eplerenone that competitively inhibits mineralocorticoid receptors in the distal convoluted tubule to promote sodium and water excretion and potassium retention.8. Spironolactone was originally developed purely for this ability before other pharmacodynamic properties of the drug were discovered.8,11 It is indicated to treat a number of conditions including heart failure, deem, hyperaldosteronism, adrenal hyperplasia, hypertension, and nephrotic syndrome.Label Off label uses of spironolactone involving its antiandrogenic activity include hirsutism, female pattern hair loss, and adult acne vulgaris.4 Spironolactone is also frequently used in medical gender transition.5
Spironolactone was developed in 1957, marketed in 1959, and approved by the FDA on January 21, 1960.10,12
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 416.573
Monoisotopic: 416.202130202 - Chemical Formula
- C24H32O4S
- Synonyms
- Espironolactona
- Spironolactone
- Spironolactonum
- Spironolattone
- External IDs
- NSC-150399
- SC-9420
Pharmacology
- Indication
Spironolactone is indicated for the treatment of New York Heart Association Class III-IV heart failure, management of edema in cirrhotic adults not responsive to fluid and sodium restrictions, primary hyperaldosteronism short-term preoperatively, primary hyperaldosteronism long-term in patients with aldosterone producing adrenal adenomas that are not candidates for surgery or patients with bilarteral micro/macronodular adrenal hyperplasia, as an add-on therapy in hypertension, and in nephrotic syndrome when treatment of the disease as well as fluid and sodium restriction with other diuretics is inadequate.Label
Spironolactone has antiandrogenic activity which leads to many of its off label uses. Spironolactone is used off label in the treatment of hirsutism, female pattern hair loss, and adult acne vulgaris.4
Spironolactone is also frequently used for its antiandrogenic effects in transgender female patients due to its low cost and reducing male-pattern hair growth.5
- Associated Conditions
- Acne
- Ascites
- Congestive Heart Failure (CHF)
- Edema
- High Blood Pressure (Hypertension)
- Hirsutism
- Hypokalemia
- Nephrotic Syndrome
- Primary Hyperaldosteronism
- Secondary hyperaldosteronism
- Chronic heart failure with reduced ejection fraction (NYHA Class III)
- Chronic heart failure with reduced ejection fraction (NYHA Class IV)
- Idiopathic hyperaldosteronism
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- Pharmacodynamics
Originally spironolactone was only studied for its potassium sparing diuretic effect.8 Spironolactone competitively inhibits mineralocorticoid receptors in the distal convoluted tubule to promote sodium and water excretion and potassium retention.8. Inhibition of this receptor leads to increased renin and aldosterone levels.8
Spironolactone is structurally similar to progesterone and as a result is associated with progestogenic and antiandrogenic effects.8
- Mechanism of action
Spironolactone competitively inhibits aldosterone dependant sodium potassium exchange channels in the distal convoluted tubule.Label This action leads to increased sodium and water excretion, but more potassium retention.Label The increased excretion of water leads to diuretic and also antihypertensive effects.Label
Target Actions Organism AMineralocorticoid receptor antagonistHumans UAndrogen receptor antagonistHumans UProgesterone receptor agonistHumans UGlucocorticoid receptor antagonistHumans UCytochrome P450 11B2, mitochondrial antagonistHumans USteroid 17-alpha-hydroxylase/17,20 lyase antagonistHumans U3-oxo-5-alpha-steroid 4-dehydrogenase antagonistHumans USex hormone-binding globulin binderHumans UVoltage-dependent calcium channel inhibitorHumans UNuclear receptor subfamily 1 group I member 2 Not Available Humans - Absorption
Spironolactone reaches a maximum concentration in 2.6 hours and an active metabolite (canrenone) reaches a maximum concentration in 4.3 hours.Label When taken with food, the bioavailability of spironolactone increases to 95.4%.Label
Giving spironolactone with food increases the maximum concentration from 209ng/mL to 301ng/mL.6 The time to maximum concentration also increases from 2.28 hours to 3.05 hours.6 The area under the curve varies from 2103ng/mL*hr to 4544ng/mL*hr.6
- Volume of distribution
Volume of distribution data is not readily available.Label,7
- Protein binding
- Metabolism
Spironolactone is deacetylated to 7α-thiospironolactone.2,3 7α-thiospironolactone is S-methylated to 7α-thiomethylspironolactone or undergoes an elimination reaction to canrenone.2,3 7α-thiomethylspironolactone is reduced to 3α-hydroxythiomethylspironolactone or 3β-hydroxythiomethylspironolactone.2,3
Canrenone was originally thought to be the primary circulating metabolite, however more recent studies have demonstrated that the primary metabolite is actually 7α-thiomethylspironolactone.8,9
Hover over products below to view reaction partners
- Route of elimination
Metabolites of spironolactone are excreted 42-56% in urine, and 14.2-14.6% in the feces.6 No unmetabolized spironolactone is present in the urine.6
- Half-life
-
Canrenone has a half life of 16.5 hours, 7-α-thiomethylspirolactone has a half life of 13.8 hours, and 6-ß-hydroxy-7-α-thiomethylspirolactone has a half life of 15 hours.Label,7
- Clearance
- Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
Patients experiencing an overdose may present with drowsiness, mental confusion, maculopapular or erythematous rash, nausea, vomiting, dizziness, or diarrhea. Vomiting is generally induced or a gastric lavage is performed.Label Supportive treatment involves maintining hydration, electrolyte balance, and vital functionsLabel.
The oral LD50 in mice, rats, and rabbits is >1g/kg.Label
Spironolactone should be avoided in pregnancy due to reports of feminization of male fetuses in animal studies.Label Active metabolites of spironolactone are present in breast milk and levels that are likely inconsequential, though the long term effects have not been studied.Label
In animal studies, spironolactone slowed follicle development, ovulation, and implantation.Label Spironolactone increased the incidence of benign adenomas in the testes of male rats, benign uterine endometrial stromal polyps in female rats, and thyroid follicular cell adenomas in both sexes of rats.Label Spironolactone and canrenone are generally not considered to be mutagenic in tests but canrenone occasionally tests positive for mutagenicity with metabolic activation and spironolactone has occasionally tested inconclusive though slightly positive for mutagenicity.Label
- Affected organisms
- Humans and other mammals
- Pathways
Pathway Category Spironolactone Action Pathway Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional DataAbacavir Spironolactone may increase the excretion rate of Abacavir which could result in a lower serum level and potentially a reduction in efficacy. Abiraterone The therapeutic efficacy of Abiraterone can be decreased when used in combination with Spironolactone. Acarbose Spironolactone may increase the excretion rate of Acarbose which could result in a lower serum level and potentially a reduction in efficacy. Acebutolol The risk or severity of hyperkalemia can be increased when Spironolactone is combined with Acebutolol. Aceclofenac The risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aceclofenac is combined with Spironolactone. Acemetacin The therapeutic efficacy of Spironolactone can be decreased when used in combination with Acemetacin. Acetaminophen Spironolactone may increase the excretion rate of Acetaminophen which could result in a lower serum level and potentially a reduction in efficacy. Acetyldigitoxin Spironolactone may decrease the excretion rate of Acetyldigitoxin which could result in a higher serum level. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Spironolactone which could result in a higher serum level. Aclidinium Spironolactone may increase the excretion rate of Aclidinium which could result in a lower serum level and potentially a reduction in efficacy. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Avoid alcohol.
- Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
- Take with or without food. Food increases the bioavailability of spironolactone by nearly 100%. It should be taken at a consistent time in regards to food.
Products
- Product Images
- International/Other Brands
- Osyrol / Spiresis / Spiretic / Spiroctan / Uractone / Verospiron / Xenalon
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataAldactone Tablet, film coated 25 mg/1 Oral REMEDYREPACK INC. 2018-08-31 2020-05-20 US Aldactone Tablet, film coated 50 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 1960-01-21 Not applicable US Aldactone Tablet, film coated 50 mg/1 Oral Physicians Total Care, Inc. 1995-04-24 2011-06-30 US Aldactone Tablet, film coated 25 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 1960-01-21 Not applicable US Aldactone Tablet, film coated 100 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 1960-01-21 Not applicable US Aldactone 100 mg Tablet Oral Pfizer Canada Ulc 1975-12-31 Not applicable Canada Aldactone 25 mg Tablet Oral Pfizer Canada Ulc 1959-12-31 Not applicable Canada CaroSpir Suspension 25 mg/5mL Oral Atlantic Biologicals Corp. 2018-08-22 Not applicable US CaroSpir Suspension 25 mg/5mL Oral Cmp Pharma, Inc. 2017-08-04 Not applicable US Spironolactone Tablet, film coated 50 mg/1 Oral Vintage Pharmaceuticals, LLC 2006-10-31 2006-10-31 US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataMint-spironolactone Tablet Oral Mint Pharmaceuticals Inc 2020-02-06 Not applicable Canada Mint-spironolactone Tablet Oral Mint Pharmaceuticals Inc 2020-02-06 Not applicable Canada Ntp-spironolactone Tablet Oral Nt Pharma Canada Ltd Not applicable Not applicable Canada Ntp-spironolactone Tablet Oral Nt Pharma Canada Ltd Not applicable Not applicable Canada Spironolactone Tablet, film coated 25 mg/1 Oral Ncs Health Care Of Ky, Inc Dba Vangard Labs 2006-08-29 Not applicable US Spironolactone Tablet, film coated 100 mg/1 Oral Denton Pharma, Inc. Dba Northwind Pharmaceuticals 2019-05-20 Not applicable US Spironolactone Tablet 100 mg/1 Oral REMEDYREPACK INC. 2019-10-24 Not applicable US Spironolactone Tablet 50 mg/1 Oral Amneal Pharmaceuticals LLC 2010-08-02 Not applicable US Spironolactone Tablet, film coated 100 mg/1 Oral Physicians Total Care, Inc. 2004-03-09 Not applicable US Spironolactone Tablet 25 mg/1 Oral Nucare Pharmaceuticals, Inc. 1986-07-23 2018-12-31 US Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Aldactazide Spironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1) Tablet, film coated Oral G.D. Searle LLC Division of Pfizer Inc 1978-01-01 Not applicable US Aldactazide Spironolactone (50 mg/1) + Hydrochlorothiazide (50 mg/1) Tablet, film coated Oral G.D. Searle LLC Division of Pfizer Inc 1978-01-01 Not applicable US Aldactazide 25 Spironolactone (25 mg) + Hydrochlorothiazide (25 mg) Tablet Oral Pfizer Canada Ulc 1960-12-31 2020-04-01 Canada Aldactazide 50 Spironolactone (50 mg) + Hydrochlorothiazide (50 mg) Tablet Oral Pfizer Canada Ulc 1983-12-31 2020-04-01 Canada Apo-spirozide Tab Spironolactone (25 mg) + Hydrochlorothiazide (25 mg) Tablet Oral Apotex Corporation 1991-12-31 2011-08-05 Canada Spironolactone and Hydrochlorothiazide Spironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1) Tablet Oral bryant ranch prepack 2020-06-10 Not applicable US Spironolactone and Hydrochlorothiazide Spironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1) Tablet Oral Mylan Pharmaceuticals Inc. 2012-07-26 2020-02-29 US Spironolactone and Hydrochlorothiazide Spironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1) Tablet Oral Mylan Institutional 1994-04-11 2018-11-30 US Spironolactone and Hydrochlorothiazide Spironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1) Tablet, film coated Oral Greenstone LLC 1978-01-01 Not applicable US Spironolactone and Hydrochlorothiazide Spironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1) Tablet Oral Physicians Total Care, Inc. 1993-05-26 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 011054 Niacinamide 4% / Spironolactone 5% Spironolactone (5 g/100g) + Nicotinamide (4 g/100g) Gel Topical Sincerus Florida, LLC 2020-07-02 Not applicable US 011218 Niacinamide 2% / Spironolactone 5% / Tretinoin 0.025% Spironolactone (5 g/100g) + Nicotinamide (2 g/100g) + Tretinoin (0.025 g/100g) Gel Topical Sincerus Florida, LLC 2020-07-02 Not applicable US 011220 Niacinamide 2% / Spironolactone 5% / Tretinoin 0.05% Spironolactone (5 g/100g) + Nicotinamide (2 g/100g) + Tretinoin (0.05 g/100g) Gel Topical Sincerus Florida, LLC 2020-07-02 Not applicable US 011503 Dapsone 6% / Niacinamide 2% / Spironolactone 5% Spironolactone (5 g/100g) + Dapsone (6 g/100g) + Nicotinamide (2 g/100g) Gel Topical Sincerus Florida, LLC 2020-07-02 Not applicable US Benzoyl Peroxide 5% / Clindamycin 1% / Niacinamide 2% / Spironolactone 2% Spironolactone (2 g/100g) + Benzoyl peroxide (5 g/100g) + Clindamycin phosphate (1 g/100g) + Nicotinamide (2 g/100g) Gel Topical Sincerus Florida, LLC 2019-05-11 Not applicable US Benzoyl Peroxide 5% / Clindamycin 1% / Niacinamide 2% / Spironolactone 2% / Tretinoin 0.025% Spironolactone (2 g/100g) + Benzoyl peroxide (5 g/100g) + Clindamycin phosphate (1 g/100g) + Nicotinamide (2 g/100g) + Tretinoin (0.025 g/100g) Gel Topical Sincerus Florida, LLC 2019-05-04 Not applicable US Benzoyl Peroxide 5% / Clindamycin 1% / Niacinamide 2% / Spironolactone 2% / Tretinoin 0.05% Spironolactone (2 g/100g) + Benzoyl peroxide (5 g/100g) + Clindamycin phosphate (1 g/100g) + Nicotinamide (2 g/100g) + Tretinoin (0.05 g/100g) Gel Topical Sincerus Florida LLC 2019-05-03 Not applicable US Clindamycin 1% / Niacinamide 4% / Spironolactone 2% / Tretinoin 0.025% Spironolactone (2 g/100g) + Clindamycin phosphate (1 g/100g) + Nicotinamide (4 g/100g) + Tretinoin (0.025 g/100g) Gel Topical Sincerus Florida, LLC 2019-05-04 Not applicable US Dapsone 6% / Niacinamide 2% / Spironolactone 5% Spironolactone (5 g/100g) + Dapsone (6 g/100g) + Nicotinamide (2 g/100g) Gel Topical Sincerus Florida, LLC 2019-05-11 Not applicable US Dapsone 8.5% / Niacinamide 2% / Spironolactone 5% Spironolactone (5 g/100g) + Dapsone (8.5 g/100g) + Nicotinamide (2 g/100g) Gel Topical Sincerus Florida, LLC 2019-05-10 Not applicable US
Categories
- ATC Codes
- C03DA01 — Spironolactone
- Drug Categories
- Agents causing hyperkalemia
- Antihypertensive Agents
- Antihypertensive Agents Indicated for Hypertension
- BSEP/ABCB11 Substrates
- Cardiovascular Agents
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (moderate)
- Cytochrome P-450 Enzyme Inhibitors
- Diuretics
- Fused-Ring Compounds
- Hormone Antagonists
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypotensive Agents
- Lactones
- Mineralocorticoid (Aldosterone) Receptor Antagonists
- Mineralocorticoid Receptor Antagonists
- Natriuretic Agents
- P-glycoprotein inducers
- Potassium-Sparing Diuretics
- Pregnanes
- Pregnenes
- Steroids
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as spironolactones and derivatives. These are steroid lactones with a structure based on the spironolactone skeleton.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Steroid lactones
- Direct Parent
- Spironolactones and derivatives
- Alternative Parents
- 3-oxo delta-4-steroids / Delta-4-steroids / Cyclohexenones / Gamma butyrolactones / Tetrahydrofurans / Thioesters / Carboxylic acid esters / Carbothioic S-esters / Sulfenyl compounds / Oxacyclic compounds show 3 more
- Substituents
- 3-oxo-delta-4-steroid / 3-oxosteroid / Aliphatic heteropolycyclic compound / Carbonyl group / Carbothioic s-ester / Carboxylic acid derivative / Carboxylic acid ester / Cyclic ketone / Cyclohexenone / Delta-4-steroid show 17 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- thioester, 3-oxo steroid, methyl ketone, oxaspiro compound, steroid lactone (CHEBI:9241) / Pregnane and derivatives [Fig] (C07310)
Chemical Identifiers
- UNII
- 27O7W4T232
- CAS number
- 52-01-7
- InChI Key
- LXMSZDCAJNLERA-ZHYRCANASA-N
- InChI
- InChI=1S/C24H32O4S/c1-14(25)29-19-13-15-12-16(26)4-8-22(15,2)17-5-9-23(3)18(21(17)19)6-10-24(23)11-7-20(27)28-24/h12,17-19,21H,4-11,13H2,1-3H3/t17-,18-,19+,21+,22-,23-,24+/m0/s1
- IUPAC Name
- (1'S,2R,2'R,9'R,10'R,11'S,15'S)-9'-(acetylsulfanyl)-2',15'-dimethylspiro[oxolane-2,14'-tetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadecan]-6'-ene-5,5'-dione
- SMILES
- [H][C@@]12CC[C@@]3(CCC(=O)O3)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])[C@@]([H])(CC2=CC(=O)CC[C@]12C)SC(C)=O
References
- Synthesis Reference
Giuseppe Bernini, "Process for preparing micronized spironolactone." U.S. Patent US4332721, issued July, 1975.
US4332721- General References
- Takamura N, Maruyama T, Ahmed S, Suenaga A, Otagiri M: Interactions of aldosterone antagonist diuretics with human serum proteins. Pharm Res. 1997 Apr;14(4):522-6. [PubMed:9144743]
- LaCagnin LB, Lutsie P, Colby HD: Conversion of spironolactone to 7 alpha-thiomethylspironolactone by hepatic and renal microsomes. Biochem Pharmacol. 1987 Oct 15;36(20):3439-44. [PubMed:3675606]
- Los LE, Pitzenberger SM, Ramjit HG, Coddington AB, Colby HD: Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites. Drug Metab Dispos. 1994 Nov-Dec;22(6):903-8. [PubMed:7895608]
- Kim GK, Del Rosso JQ: Oral Spironolactone in Post-teenage Female Patients with Acne Vulgaris: Practical Considerations for the Clinician Based on Current Data and Clinical Experience. J Clin Aesthet Dermatol. 2012 Mar;5(3):37-50. [PubMed:22468178]
- Millington K, Liu E, Chan YM: The Utility of Potassium Monitoring in Gender-Diverse Adolescents Taking Spironolactone. J Endocr Soc. 2019 Apr 4;3(5):1031-1038. doi: 10.1210/js.2019-00030. eCollection 2019 May 1. [PubMed:31065620]
- Karim A: Spironolactone: disposition, metabolism, pharmacodynamics, and bioavailability. Drug Metab Rev. 1978;8(1):151-88. doi: 10.3109/03602537808993782. [PubMed:363379]
- Carone L, Oxberry SG, Twycross R, Charlesworth S, Mihalyo M, Wilcock A: Spironolactone. J Pain Symptom Manage. 2017 Feb;53(2):288-292. doi: 10.1016/j.jpainsymman.2016.12.320. Epub 2016 Dec 23. [PubMed:28024992]
- Sica DA: Pharmacokinetics and pharmacodynamics of mineralocorticoid blocking agents and their effects on potassium homeostasis. Heart Fail Rev. 2005 Jan;10(1):23-9. doi: 10.1007/s10741-005-2345-1. [PubMed:15947888]
- Gardiner P, Schrode K, Quinlan D, Martin BK, Boreham DR, Rogers MS, Stubbs K, Smith M, Karim A: Spironolactone metabolism: steady-state serum levels of the sulfur-containing metabolites. J Clin Pharmacol. 1989 Apr;29(4):342-7. [PubMed:2723123]
- Menard J: The 45-year story of the development of an anti-aldosterone more specific than spironolactone. Mol Cell Endocrinol. 2004 Mar 31;217(1-2):45-52. doi: 10.1016/j.mce.2003.10.008. [PubMed:15134800]
- BOLTE E, VERDY M, MARC-AURELE J, BROUILLET J, BEAUREGARD P, GENEST J: Studies on new diuretic compounds: spirolactone and chlorothiazide. Can Med Assoc J. 1958 Dec 1;79(11):881-8. [PubMed:13608362]
- FDA Approved Drug Products: Spironolactone [Link]
- FDA Approved Drug Products: Aldactone (spironolactone) tablets [Link]
- External Links
- Human Metabolome Database
- HMDB0014565
- KEGG Drug
- D00443
- KEGG Compound
- C07310
- PubChem Compound
- 5833
- PubChem Substance
- 46508525
- ChemSpider
- 5628
- BindingDB
- 50228080
- 9997
- ChEBI
- 9241
- ChEMBL
- CHEMBL1393
- ZINC
- ZINC000003861599
- Therapeutic Targets Database
- DAP000297
- PharmGKB
- PA451483
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- SNL
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Spironolactone
- AHFS Codes
- 24:32.20 — Mineralocorticoid (Aldosterone) Receptor Antagonists
- PDB Entries
- 2ab2 / 2oax / 3vhu
- FDA label
- Download (204 KB)
- MSDS
- Download (72.6 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Basic Science Healthy Volunteers / Hypoglycemia 1 4 Active Not Recruiting Prevention Disorder Related to Renal Transplantation 1 4 Active Not Recruiting Treatment Acute Heart Failure (AHF) / Heart Failure; With Decompensation 1 4 Active Not Recruiting Treatment Atrial Fibrillation 1 4 Completed Diagnostic Heart Failure 1 4 Completed Diagnostic Heart Failure / Nonischemic Dilated Cardiomyopathy 1 4 Completed Prevention Anthracycline Induced Cardiotoxicity 1 4 Completed Prevention Chronic Renal Failure (CRF) / End-stage Renal Failure (ESRF) 1 4 Completed Prevention Liver Cirrhosis / Portal Hypertension 1 4 Completed Treatment Arrhythmia of ventricular origin 1
Pharmacoeconomics
- Manufacturers
- Gd searle llc
- Actavis elizabeth llc
- Amneal pharmaceuticals
- Ascot hosp pharmaceuticals inc div travenol laboratories inc
- Ivax pharmaceuticals inc
- Lederle laboratories div american cyanamid co
- Mutual pharmaceutical co inc
- Mylan pharmaceuticals inc
- Purepac pharmaceutical co
- Sandoz inc
- Superpharm corp
- Upsher smith laboratories inc
- Vangard laboratories inc div midway medical co
- Vintage pharmaceuticals llc
- Warner chilcott div warner lambert co
- Watson laboratories inc
- Packagers
- Actavis Group
- Advanced Pharmaceutical Services Inc.
- Amerisource Health Services Corp.
- A-S Medication Solutions LLC
- Cardinal Health
- Caremark LLC
- Comprehensive Consultant Services Inc.
- Dept Health Central Pharmacy
- DHHS Program Support Center Supply Service Center
- Direct Dispensing Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- GD Searle LLC
- Greenstone LLC
- Guna Inc.
- H and H Laboratories
- Heartland Repack Services LLC
- Innoviant Pharmacy Inc.
- Lake Erie Medical and Surgical Supply
- Liberty Pharmaceuticals
- Major Pharmaceuticals
- Mckesson Corp.
- Medisca Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Mutual Pharmaceutical Co.
- Mylan
- Neighborcare Repackaging Inc.
- Neuman Distributors Inc.
- Nucare Pharmaceuticals Inc.
- Palmetto Pharmaceuticals Inc.
- PD-Rx Pharmaceuticals Inc.
- Pfizer Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmacia Inc.
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Prepak Systems Inc.
- Professional Co.
- Qualitest
- Rebel Distributors Corp.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Richmond Pharmacy
- Sandhills Packaging Inc.
- Sandoz
- Southwood Pharmaceuticals
- UDL Laboratories
- Vangard Labs Inc.
- Vintage Pharmaceuticals Inc.
- Dosage Forms
Form Route Strength Tablet Oral 25 mg Pill 100 MG Capsule Oral 10 mg Capsule Oral 100 mg Tablet, coated Oral 25 mg Tablet Oral Tablet, coated Oral 50 mg Suspension Oral 25 mg/5mL Tablet, film coated Oral Capsule, coated Oral 50 mg Capsule Oral 25 MG Gel Topical Capsule Oral 20 mg Tablet, film coated Oral 20 mg Tablet Oral 20 mg Capsule Oral 50 MG Tablet, coated Oral 100 mg Tablet Oral 100 MG Tablet Oral 50 MG Tablet, film coated Oral 100 MG Tablet, film coated Oral 25 MG Tablet, film coated Oral 50 MG Suspension Oral 10 mg/1mL Suspension Oral 2 mg/1mL Suspension Oral 5 mg/1mL Tablet Oral 100 mg/1 Tablet Oral 25 mg/1 Tablet Oral 50 mg/1 Tablet, coated Oral 100 mg/1 Tablet, coated Oral 25 mg/1 Tablet, coated Oral 50 mg/1 Tablet, film coated Oral 100 mg/1 Tablet, film coated Oral 25 mg/1 Tablet, film coated Oral 50 mg/1 Tablet Oral Tablet, film coated Oral - Prices
Unit description Cost Unit Spironolactone powder 12.56USD g Aldactone 100 mg tablet 2.14USD tablet Aldactazide 50-50 mg tablet 2.02USD tablet Aldactazide 50-50 tablet 1.92USD tablet Aldactone 50 mg tablet 1.84USD tablet Spironolactone 100 mg tablet 1.45USD tablet Aldactazide 25-25 mg tablet 1.26USD tablet Aldactazide 25-25 tablet 1.04USD tablet Spironolactone 50 mg tablet 0.83USD tablet Aldactone 25 mg tablet 0.8USD tablet Spironolactone-HCTZ 25-25 mg tablet 0.57USD tablet Spironolactone 25 mg tablet 0.5USD tablet Novo-Spiroton 100 mg Tablet 0.25USD tablet Novo-Spiroton 25 mg Tablet 0.11USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region Unlock Additional DataUS9757394 No 2017-09-12 2036-10-28 US US10493083 No 2019-12-03 2036-10-28 US US10624906 No 2016-10-28 2036-10-28 US US10660907 No 2016-10-28 2036-10-28 US Additional Data Available- Filed OnFiled OnAvailable for Purchase
The date on which a patent was filed with the relevant government.
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Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 134.5 °C [MSDS] boiling point (°C) 201 [MSDS] logP 2.78 https://www.ncbi.nlm.nih.gov/pubmed/26642673 - Predicted Properties
Property Value Source Water Solubility 0.00198 mg/mL ALOGPS logP 3.1 ALOGPS logP 3.64 ChemAxon logS -5.3 ALOGPS pKa (Strongest Acidic) 18.01 ChemAxon pKa (Strongest Basic) -4.9 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 0 ChemAxon Polar Surface Area 60.44 Å2 ChemAxon Rotatable Bond Count 2 ChemAxon Refractivity 113.5 m3·mol-1 ChemAxon Polarizability 46.03 Å3 ChemAxon Number of Rings 5 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9912 Blood Brain Barrier + 0.932 Caco-2 permeable + 0.5432 P-glycoprotein substrate Substrate 0.5691 P-glycoprotein inhibitor I Inhibitor 0.6807 P-glycoprotein inhibitor II Inhibitor 0.8388 Renal organic cation transporter Non-inhibitor 0.727 CYP450 2C9 substrate Non-substrate 0.7897 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.6638 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.9276 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8681 Ames test Non AMES toxic 0.9158 Carcinogenicity Non-carcinogens 0.9288 Biodegradation Not ready biodegradable 0.9696 Rat acute toxicity 2.0150 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9427 hERG inhibition (predictor II) Non-inhibitor 0.7002
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Mass Spectrum (Electron Ionization) MS splash10-0006-9836000000-9f600bd39c3b914c0b17 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-014i-0000900000-5e2e1944e45fcef225d1 LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-014i-0000900000-406c100eed5b6cdc3286
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Zinc ion binding
- Specific Function
- Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates targ...
- Gene Name
- NR3C2
- Uniprot ID
- P08235
- Uniprot Name
- Mineralocorticoid receptor
- Molecular Weight
- 107066.575 Da
References
- Sitruk-Ware R: Progestogens in hormonal replacement therapy: new molecules, risks, and benefits. Menopause. 2002 Jan-Feb;9(1):6-15. [PubMed:11791081]
- Rogerson FM, Yao YZ, Smith BJ, Dimopoulos N, Fuller PJ: Determinants of spironolactone binding specificity in the mineralocorticoid receptor. J Mol Endocrinol. 2003 Dec;31(3):573-82. [PubMed:14664717]
- Gertner RA, Klein JD, Bailey JL, Kim DU, Luo XH, Bagnasco SM, Sands JM: Aldosterone decreases UT-A1 urea transporter expression via the mineralocorticoid receptor. J Am Soc Nephrol. 2004 Mar;15(3):558-65. [PubMed:14978157]
- Frishman WH, Stier CT Jr: Aldosterone and aldosterone antagonism in systemic hypertension. Curr Hypertens Rep. 2004 Jun;6(3):195-200. [PubMed:15128471]
- Rogerson FM, Yao Y, Smith BJ, Fuller PJ: Differences in the determinants of eplerenone, spironolactone and aldosterone binding to the mineralocorticoid receptor. Clin Exp Pharmacol Physiol. 2004 Oct;31(10):704-9. [PubMed:15554912]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
- Sica DA: Pharmacokinetics and pharmacodynamics of mineralocorticoid blocking agents and their effects on potassium homeostasis. Heart Fail Rev. 2005 Jan;10(1):23-9. doi: 10.1007/s10741-005-2345-1. [PubMed:15947888]
- Rossi G, Boscaro M, Ronconi V, Funder JW: Aldosterone as a cardiovascular risk factor. Trends Endocrinol Metab. 2005 Apr;16(3):104-7. [PubMed:15808807]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Zinc ion binding
- Specific Function
- Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription ...
- Gene Name
- AR
- Uniprot ID
- P10275
- Uniprot Name
- Androgen receptor
- Molecular Weight
- 98987.9 Da
References
- Ye P, Yamashita T, Pollock DM, Sasano H, Rainey WE: Contrasting effects of eplerenone and spironolactone on adrenal cell steroidogenesis. Horm Metab Res. 2009 Jan;41(1):35-9. doi: 10.1055/s-0028-1087188. Epub 2008 Sep 25. [PubMed:18819053]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Zinc ion binding
- Specific Function
- The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
- Gene Name
- PGR
- Uniprot ID
- P06401
- Uniprot Name
- Progesterone receptor
- Molecular Weight
- 98979.96 Da
References
- Fagart J, Hillisch A, Huyet J, Barfacker L, Fay M, Pleiss U, Pook E, Schafer S, Rafestin-Oblin ME, Kolkhof P: A new mode of mineralocorticoid receptor antagonism by a potent and selective nonsteroidal molecule. J Biol Chem. 2010 Sep 24;285(39):29932-40. doi: 10.1074/jbc.M110.131342. Epub 2010 Jul 22. [PubMed:20650892]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Zinc ion binding
- Specific Function
- Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
- Gene Name
- NR3C1
- Uniprot ID
- P04150
- Uniprot Name
- Glucocorticoid receptor
- Molecular Weight
- 85658.57 Da
References
- Fagart J, Hillisch A, Huyet J, Barfacker L, Fay M, Pleiss U, Pook E, Schafer S, Rafestin-Oblin ME, Kolkhof P: A new mode of mineralocorticoid receptor antagonism by a potent and selective nonsteroidal molecule. J Biol Chem. 2010 Sep 24;285(39):29932-40. doi: 10.1074/jbc.M110.131342. Epub 2010 Jul 22. [PubMed:20650892]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Steroid 11-beta-monooxygenase activity
- Specific Function
- Preferentially catalyzes the conversion of 11-deoxycorticosterone to aldosterone via corticosterone and 18-hydroxycorticosterone.
- Gene Name
- CYP11B2
- Uniprot ID
- P19099
- Uniprot Name
- Cytochrome P450 11B2, mitochondrial
- Molecular Weight
- 57559.62 Da
References
- Cheng SC, Suzuki K, Sadee W, Harding BW: Effects of spironolactone, canrenone and canrenoate-K on cytochrome P450, and 11beta- and 18-hydroxylation in bovine and human adrenal cortical mitochondria. Endocrinology. 1976 Oct;99(4):1097-106. [PubMed:976190]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Steroid 17-alpha-monooxygenase activity
- Specific Function
- Conversion of pregnenolone and progesterone to their 17-alpha-hydroxylated products and subsequently to dehydroepiandrosterone (DHEA) and androstenedione. Catalyzes both the 17-alpha-hydroxylation ...
- Gene Name
- CYP17A1
- Uniprot ID
- P05093
- Uniprot Name
- Steroid 17-alpha-hydroxylase/17,20 lyase
- Molecular Weight
- 57369.995 Da
References
- Authors unspecified: Spironolactone and endocrine dysfunction. Ann Intern Med. 1976 Nov;85(5):630-6. [PubMed:984618]
- Millington K, Liu E, Chan YM: The Utility of Potassium Monitoring in Gender-Diverse Adolescents Taking Spironolactone. J Endocr Soc. 2019 Apr 4;3(5):1031-1038. doi: 10.1210/js.2019-00030. eCollection 2019 May 1. [PubMed:31065620]
- Desai; Meena P.; Vijayalakshmi Bhatia & P.S.N. Menon (2001). Pediatric Endocrine Disorders. Orient Blackswan. [ISBN:978-81-250-2025-7]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Electron carrier activity
- Specific Function
- Converts testosterone into 5-alpha-dihydrotestosterone and progesterone or corticosterone into their corresponding 5-alpha-3-oxosteroids. It plays a central role in sexual differentiation and andro...
Components:
Name | UniProt ID |
---|---|
3-oxo-5-alpha-steroid 4-dehydrogenase 1 | P18405 |
3-oxo-5-alpha-steroid 4-dehydrogenase 2 | P31213 |
Polyprenol reductase | Q9H8P0 |
References
- Corvol P, Michaud A, Menard J, Freifeld M, Mahoudeau J: Antiandrogenic effect of spirolactones: mechanism of action. Endocrinology. 1975 Jul;97(1):52-8. [PubMed:166833]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Androgen binding
- Specific Function
- Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone...
- Gene Name
- SHBG
- Uniprot ID
- P04278
- Uniprot Name
- Sex hormone-binding globulin
- Molecular Weight
- 43778.755 Da
References
- Braunstein GD: Clinical practice. Gynecomastia. N Engl J Med. 2007 Sep 20;357(12):1229-37. [PubMed:17881754]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Voltage-gated calcium channel activity
- Specific Function
- This protein is a subunit of the dihydropyridine (DHP) sensitive calcium channel. Plays a role in excitation-contraction coupling. The skeletal muscle DHP-sensitive Ca(2+) channel may function only...
Components:
References
- Sorrentino R, Autore G, Cirino G, d'Emmanuele de Villa Bianca R, Calignano A, Vanasia M, Alfieri C, Sorrentino L, Pinto A: Effect of spironolactone and its metabolites on contractile property of isolated rat aorta rings. J Cardiovasc Pharmacol. 2000 Aug;36(2):230-5. [PubMed:10942165]
- Melander A, Danielson K, Schersten B, Thulin T, Wahlin E: Enhancement by food of canrenone bioavailability from spironolactone. Clin Pharmacol Ther. 1977 Jul;22(1):100-3. [PubMed:872489]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism an...
- Gene Name
- NR1I2
- Uniprot ID
- O75469
- Uniprot Name
- Nuclear receptor subfamily 1 group I member 2
- Molecular Weight
- 49761.245 Da
References
- Kretschmer XC, Baldwin WS: CAR and PXR: xenosensors of endocrine disrupters? Chem Biol Interact. 2005 Aug 15;155(3):111-28. [PubMed:16054614]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [PubMed:15601807]
- Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [PubMed:26721703]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Steroid 11-beta-monooxygenase activity
- Specific Function
- Has steroid 11-beta-hydroxylase activity. In addition to this activity, the 18 or 19-hydroxylation of steroids and the aromatization of androstendione to estrone have also been ascribed to cytochro...
- Gene Name
- CYP11B1
- Uniprot ID
- P15538
- Uniprot Name
- Cytochrome P450 11B1, mitochondrial
- Molecular Weight
- 57572.44 Da
References
- Cheng SC, Suzuki K, Sadee W, Harding BW: Effects of spironolactone, canrenone and canrenoate-K on cytochrome P450, and 11beta- and 18-hydroxylation in bovine and human adrenal cortical mitochondria. Endocrinology. 1976 Oct;99(4):1097-106. [PubMed:976190]
- Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Takamura N, Maruyama T, Ahmed S, Suenaga A, Otagiri M: Interactions of aldosterone antagonist diuretics with human serum proteins. Pharm Res. 1997 Apr;14(4):522-6. [PubMed:9144743]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Not Available
- Specific Function
- Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...
Components:
References
- Takamura N, Maruyama T, Ahmed S, Suenaga A, Otagiri M: Interactions of aldosterone antagonist diuretics with human serum proteins. Pharm Res. 1997 Apr;14(4):522-6. [PubMed:9144743]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- Johnson DR, Klaassen CD: Regulation of rat multidrug resistance protein 2 by classes of prototypical microsomal enzyme inducers that activate distinct transcription pathways. Toxicol Sci. 2002 Jun;67(2):182-9. [PubMed:12011477]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Rigalli JP, Ruiz ML, Perdomo VG, Villanueva SS, Mottino AD, Catania VA: Pregnane X receptor mediates the induction of P-glycoprotein by spironolactone in HepG2 cells. Toxicology. 2011 Jul 11;285(1-2):18-24. doi: 10.1016/j.tox.2011.03.015. Epub 2011 Apr 1. [PubMed:21459122]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- Kanai N, Lu R, Bao Y, Wolkoff AW, Schuster VL: Transient expression of oatp organic anion transporter in mammalian cells: identification of candidate substrates. Am J Physiol. 1996 Feb;270(2 Pt 2):F319-25. [PubMed:8779893]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [PubMed:24014644]
Drug created on June 13, 2005 07:24 / Updated on January 25, 2021 13:56