Spironolactone

Identification

Summary

Spironolactone is an aldosterone receptor antagonist used for the treatment of hypertension, hyperaldosteronism, edema due to various conditions, hirsutism (off-label) and hypokalemia.

Brand Names

Aldactazide, Aldactone, Carospir

Generic Name

Spironolactone

DrugBank Accession Number

DB00421

Background

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

Similar Structures

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

Reduce drug development failure rates

Build, train, & validate machine-learning models
with evidence-based and structured datasets.

See how

Build, train, & validate predictive machine-learning models with structured datasets.

See how

Associated Conditions

Contraindications & Blackbox Warnings

Avoid life-threatening adverse drug events

Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.

Learn more

Avoid life-threatening adverse drug events & improve clinical decision support.

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	antagonist	Humans
UAndrogen receptor	antagonist	Humans
UProgesterone receptor	agonist	Humans
UGlucocorticoid receptor	antagonist	Humans
UCytochrome P450 11B2, mitochondrial	antagonist	Humans
USteroid 17-alpha-hydroxylase/17,20 lyase	antagonist	Humans
U3-oxo-5-alpha-steroid 4-dehydrogenase	antagonist	Humans
USex hormone-binding globulin	binder	Humans
UVoltage-dependent calcium channel	inhibitor	Humans
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

>90%.^Label Canrenone is as much as 98% protein bound.⁶

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

Spironolactone
- 7alpha-thiospironolactone
  - 7alpha-thiomethylspironolactone
    - 3beta-hydroxythiomethylspironolactone
    - 3alpha-hydroxythiomethylspironolactone
  - Canrenone

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

1.4 hours.^Label,7

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

Clearance data is not readily available.^Label,7

Adverse Effects

Improve decision support & research outcomes

With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.

Learn more

Improve decision support & research outcomes with our structured 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 functions^Label.

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

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
Integrate drug-drug interactions in your software
Abacavir	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.
Acebutolol	The risk or severity of adverse effects 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.
Acrivastine	Spironolactone may increase the excretion rate of Acrivastine which could result in a lower serum level and potentially a reduction in efficacy.

Identify potential medication risks

Easily compare up to 40 drugs with our drug interaction checker.

Get severity rating, description, and management advice.

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

Drug product information from 10+ global regions

Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.

Access now

Access drug product information from over 10 global regions.

Access now

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
Aldactone	Tablet, film coated	50 mg/1	Oral	Pfizer Laboratories Div Pfizer Inc	1960-01-21	Not applicable
Aldactone	Tablet, film coated	50 mg/1	Oral	Physicians Total Care, Inc.	1995-04-24	2011-06-30
Aldactone	Tablet, film coated	25 mg/1	Oral	Pfizer Laboratories Div Pfizer Inc	1960-01-21	Not applicable
Aldactone	Tablet, film coated	100 mg/1	Oral	Pfizer Laboratories Div Pfizer Inc	1960-01-21	Not applicable
Aldactone	Tablet, film coated	25 mg/1	Oral	REMEDYREPACK INC.	2018-08-31	2020-05-20
Aldactone 100 mg	Tablet	100 mg	Oral	Pfizer Canada Ulc	1975-12-31	Not applicable
Aldactone 25 mg	Tablet	25 mg	Oral	Pfizer Canada Ulc	1959-12-31	Not applicable
CaroSpir	Suspension	25 mg/5mL	Oral	Atlantic Biologicals Corp.	2018-08-22	Not applicable
CaroSpir	Suspension	25 mg/5mL	Oral	Cmp Pharma, Inc.	2017-08-04	Not applicable
Spironolactone	Tablet, film coated	50 mg/1	Oral	Vintage Pharmaceuticals, LLC	2006-10-31	2006-10-31

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Jamp Spironolactone	Tablet	25 mg	Oral	Jamp Pharma Corporation	Not applicable	Not applicable
Jamp Spironolactone	Tablet	100 mg	Oral	Jamp Pharma Corporation	Not applicable	Not applicable
Mint-spironolactone	Tablet	100 mg	Oral	Mint Pharmaceuticals Inc	2020-02-06	Not applicable
Mint-spironolactone	Tablet	25 mg	Oral	Mint Pharmaceuticals Inc	2020-02-06	Not applicable
Ntp-spironolactone	Tablet	100 mg	Oral	Nt Pharma Canada Ltd	Not applicable	Not applicable
Ntp-spironolactone	Tablet	25 mg	Oral	Nt Pharma Canada Ltd	Not applicable	Not applicable
Spironolactone	Tablet, film coated	50 mg/1	Oral	PD-Rx Pharmaceuticals, Inc.	2017-06-02	Not applicable
Spironolactone	Tablet, film coated	50 mg/1	Oral	bryant ranch prepack	1986-07-23	Not applicable
Spironolactone	Tablet	25 mg/1	Oral	Unit Dose Services	1986-07-23	2017-12-31
Spironolactone	Tablet, film coated	100 mg/1	Oral	bryant ranch prepack	1986-07-23	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
AKTAZİD 25 MG/25 MG FİLM TABLET, 100 ADET	Spironolactone (25 mg) + Hydrochlorothiazide (25 mg)	Tablet, film coated	Oral	World Medicine Ilac San. Ve Tic. a.s.	2020-08-14	Not applicable
AKTAZİD 25 MG/25 MG FİLM TABLET, 20 ADET	Spironolactone (25 mg) + Hydrochlorothiazide (25 mg)	Tablet, film coated	Oral	World Medicine Ilac San. Ve Tic. a.s.	2020-08-14	Not applicable
AKTAZİD 25 MG/25 MG FİLM TABLET, 30 ADET	Spironolactone (25 mg) + Hydrochlorothiazide (25 mg)	Tablet, film coated	Oral	World Medicine Ilac San. Ve Tic. a.s.	2020-08-14	Not applicable
AKTAZİD 25 MG/25 MG FİLM TABLET, 50 ADET	Spironolactone (25 mg) + Hydrochlorothiazide (25 mg)	Tablet, film coated	Oral	World Medicine Ilac San. Ve Tic. a.s.	2020-08-14	Not applicable
AKTAZİD 50 MG/50 MG FİLM TABLET, 100 ADET	Spironolactone (50 mg) + Hydrochlorothiazide (50 mg)	Tablet, film coated	Oral	World Medicine Ilac San. Ve Tic. a.s.	2020-08-14	Not applicable
AKTAZİD 50 MG/50 MG FİLM TABLET, 20 ADET	Spironolactone (50 mg) + Hydrochlorothiazide (50 mg)	Tablet, film coated	Oral	World Medicine Ilac San. Ve Tic. a.s.	2020-08-14	Not applicable
AKTAZİD 50 MG/50 MG FİLM TABLET, 30 ADET	Spironolactone (50 mg) + Hydrochlorothiazide (50 mg)	Tablet, film coated	Oral	World Medicine Ilac San. Ve Tic. a.s.	2020-08-14	Not applicable
AKTAZİD 50 MG/50 MG FİLM TABLET, 50 ADET	Spironolactone (50 mg) + Hydrochlorothiazide (50 mg)	Tablet, film coated	Oral	World Medicine Ilac San. Ve Tic. a.s.	2020-08-14	Not applicable
Aldactazide	Spironolactone (50 mg/1) + Hydrochlorothiazide (50 mg/1)	Tablet, film coated	Oral	Pfizer Laboratories Div Pfizer Inc	1978-01-01	Not applicable
Aldactazide	Spironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1)	Tablet, film coated	Oral	Pfizer Laboratories Div Pfizer Inc	1978-01-01	Not applicable

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
011054 Niacinamide 4% / Spironolactone 5%	Spironolactone (5 g/100g) + Nicotinamide (4 g/100g)	Gel	Topical	Sincerus Florida, LLC	2020-07-02	Not applicable
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
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
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
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
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
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
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
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
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

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: (1R,3aS,3bR,4R,9aR,9bS,11aS)-4-(acetylsulfanyl)-9a,11a-dimethyl-2,3,3a,3b,4,5,7,8,9,9a,9b,10,11,11a-tetradecahydrospiro[cyclopenta[a]phenanthrene-1,2'-oxolane]-5',7-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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
Karim A: Spironolactone: disposition, metabolism, pharmacodynamics, and bioavailability. Drug Metab Rev. 1978;8(1):151-88. doi: 10.3109/03602537808993782. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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
RxNav: 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

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 Subjects (HS) / Hypoglycemia	1
4	Active Not Recruiting	Treatment	Acute Heart Failure (AHF) / Heart Failure; With Decompensation	1
4	Active Not Recruiting	Treatment	Atherosclerosis	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	Cirrhosis of the Liver / Portal Hypertension	1
4	Completed	Prevention	Disorder Related to Renal Transplantation	1
4	Completed	Prevention	End-stage Renal Failure (ESRF)	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
Capsule	Oral	25 MG
Pill		100 MG
Capsule	Oral
Capsule	Oral
Tablet, coated	Oral	50 mg
Tablet, coated	Oral
Suspension	Oral	25 mg/5mL
Tablet, film coated	Oral
Tablet, coated	Oral	100 mg
Capsule, coated	Oral
Gel	Topical
Tablet	Oral
Tablet	Oral	100 mg
Tablet	Oral	50 mg
Capsule	Oral	100 MG
Capsule	Oral	50 MG
Tablet, film coated	Oral	100 mg
Tablet, coated	Oral	25 mg
Tablet, delayed release	Oral	100 mg
Tablet, film coated	Oral	50 MG
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
Tablet	Oral	25 mg
Tablet, film coated	Oral	25 mg

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)
US9757394	No	2017-09-12	2036-10-28
US10493083	No	2019-12-03	2036-10-28
US10624906	No	2020-04-21	2036-10-28
US10660907	No	2020-05-26	2036-10-28
US10888570	No	2021-01-12	2036-10-28

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)	17.89	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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

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

Build, predict & validate machine-learning models

Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.

Learn more

Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.

Learn more

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	1.6	N/A	N/A	A28052
IC 50 (nM)	13	N/A	N/A	A28202
IC 50 (nM)	49	N/A	N/A	A28203
IC 50 (nM)	60	N/A	N/A	A28203
Ki (nM)	2.323	N/A	N/A	A28201

Details1. Mineralocorticoid receptor

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. [Article]
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. [Article]
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. [Article]
Frishman WH, Stier CT Jr: Aldosterone and aldosterone antagonism in systemic hypertension. Curr Hypertens Rep. 2004 Jun;6(3):195-200. [Article]
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. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
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. [Article]
Rossi G, Boscaro M, Ronconi V, Funder JW: Aldosterone as a cardiovascular risk factor. Trends Endocrinol Metab. 2005 Apr;16(3):104-7. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	120	N/A	N/A	A28203
IC 50 (nM)	523	N/A	N/A	A28202
Ki (nM)	39.4	N/A	N/A	A28201

Details2. Androgen receptor

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. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	>10000	N/A	N/A	A28202
IC 50 (nM)	650	N/A	N/A	A28203
Ki (nM)	399.7	N/A	N/A	A28201

Details3. Progesterone receptor

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. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	1400	N/A	N/A	A28203
IC 50 (nM)	6920	N/A	N/A	A28202
Ki (nM)	32.6	N/A	N/A	A28201

Details4. Glucocorticoid receptor

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. [Article]

Details5. Cytochrome P450 11B2, mitochondrial

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. [Article]

Details6. Steroid 17-alpha-hydroxylase/17,20 lyase

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. [Article]
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. [Article]
Desai; Meena P.; Vijayalakshmi Bhatia & P.S.N. Menon (2001). Pediatric Endocrine Disorders. Orient Blackswan. [ISBN:978-81-250-2025-7]

Details7. 3-oxo-5-alpha-steroid 4-dehydrogenase (Protein Group)

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. [Article]

Details8. Sex hormone-binding globulin

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. [Article]

Details9. Voltage-dependent calcium channel (Protein Group)

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:

Name	UniProt ID
Voltage-dependent calcium channel gamma-1 subunit	Q06432
Voltage-dependent calcium channel gamma-2 subunit	Q9Y698
Voltage-dependent calcium channel gamma-3 subunit	O60359
Voltage-dependent calcium channel gamma-4 subunit	Q9UBN1
Voltage-dependent calcium channel gamma-5 subunit	Q9UF02
Voltage-dependent calcium channel gamma-6 subunit	Q9BXT2
Voltage-dependent calcium channel gamma-7 subunit	P62955
Voltage-dependent calcium channel gamma-8 subunit	Q8WXS5
Voltage-dependent calcium channel subunit alpha-2/delta-1	P54289
Voltage-dependent calcium channel subunit alpha-2/delta-2	Q9NY47
Voltage-dependent calcium channel subunit alpha-2/delta-3	Q8IZS8
Voltage-dependent calcium channel subunit alpha-2/delta-4	Q7Z3S7
Voltage-dependent L-type calcium channel subunit alpha-1C	Q13936
Voltage-dependent L-type calcium channel subunit alpha-1D	Q01668
Voltage-dependent L-type calcium channel subunit alpha-1F	O60840
Voltage-dependent L-type calcium channel subunit alpha-1S	Q13698
Voltage-dependent L-type calcium channel subunit beta-1	Q02641
Voltage-dependent L-type calcium channel subunit beta-2	Q08289
Voltage-dependent L-type calcium channel subunit beta-3	P54284
Voltage-dependent L-type calcium channel subunit beta-4	O00305
Voltage-dependent N-type calcium channel subunit alpha-1B	Q00975
Voltage-dependent P/Q-type calcium channel subunit alpha-1A	O00555
Voltage-dependent R-type calcium channel subunit alpha-1E	Q15878
Voltage-dependent T-type calcium channel subunit alpha-1G	O43497
Voltage-dependent T-type calcium channel subunit alpha-1H	O95180
Voltage-dependent T-type calcium channel subunit alpha-1I	Q9P0X4

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. [Article]
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. [Article]

Details10. Nuclear receptor subfamily 1 group I member 2

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. [Article]

Enzymes

Details1. Cytochrome P450 11B1, mitochondrial

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. [Article]
Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]

Details2. Cytochrome P450 2C8

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. [Article]
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. [Article]

Carriers

Details1. Serum albumin

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. [Article]

Details2. alpha1-acid glycoprotein (Protein Group)

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:

Name	UniProt ID
Alpha-1-acid glycoprotein 1	P02763
Alpha-1-acid glycoprotein 2	P19652

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. [Article]

Transporters

Details1. Canalicular multispecific organic anion transporter 1

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. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	23600	N/A	N/A	A15871

Details2. P-glycoprotein 1

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. [Article]

Details3. Solute carrier organic anion transporter family member 1A2

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. [Article]

Details4. Bile salt export pump

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. [Article]

Drug created at June 13, 2005 13:24 / Updated at June 24, 2022 08:21

Spironolactone

Identification

Structure for Spironolactone (DB00421)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Targets

References

References

References

References

References

References

Components:

References

References

Components:

References

References

Enzymes

References

References

Carriers

References

Components:

References

Transporters

References

References

References

References