Identification

Name
Spironolactone
Accession Number
DB00421  (APRD01234)
Type
Small Molecule
Groups
Approved
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)

Structure
Thumb
Synonyms
  • Espironolactona
  • Spironolactone
  • Spironolactonum
  • Spironolattone
External IDs
NSC-150399 / SC-9420
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AldactoneTablet, film coated25 mg/1OralREMEDYREPACK INC.2018-08-31Not applicableUs
AldactoneTablet, film coated50 mg/1OralG.D. Searle LLC Division of Pfizer Inc1960-01-21Not applicableUs
AldactoneTablet, film coated50 mg/1OralPhysicians Total Care, Inc.1995-04-242011-06-30Us
AldactoneTablet, film coated25 mg/1OralG.D. Searle LLC Division of Pfizer Inc1960-01-21Not applicableUs
AldactoneTablet, film coated100 mg/1OralG.D. Searle LLC Division of Pfizer Inc1960-01-21Not applicableUs
Aldactone 100 mgTablet100 mgOralPfizer1975-12-31Not applicableCanada
Aldactone 25 mgTablet25 mgOralPfizer1959-12-31Not applicableCanada
CaroSpirSuspension25 mg/5mLOralCmp Pharma, Inc.2017-08-04Not applicableUs
CaroSpirSuspension25 mg/5mLOralAtlantic Biologicals Corp.2018-08-22Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ntp-spironolactoneTablet100 mgOralNt Pharma Canada LtdNot applicableNot applicableCanada
Ntp-spironolactoneTablet25 mgOralNt Pharma Canada LtdNot applicableNot applicableCanada
SpironolactoneTablet25 mg/1OralUnit Dose Services1986-07-23Not applicableUs50436 997320180907 15195 pcbo1v
SpironolactoneTablet, film coated50 mg/1OralCardinal Health2011-02-042018-11-30Us
SpironolactoneTablet100 mg/1OralZydus Pharmaceuticals Usa, Inc.2018-08-15Not applicableUs
SpironolactoneTablet, film coated25 mg/1OralPhysicians Total Care, Inc.1994-03-25Not applicableUs54868 070020180907 15195 1jfdnpn
SpironolactoneTablet, film coated50 mg/1OralMylan Institutional2002-02-20Not applicableUs
SpironolactoneTablet50 mg/1OralA-S Medication Solutions2010-08-022018-03-31Us50090 129220180913 8702 i8m0pt
SpironolactoneTablet, film coated100 mg/1OralGreenstone, Llc1960-01-212018-10-31Us
SpironolactoneTablet, film coated25 mg/1OralJubilant Cadista Pharmaceuticals Inc.2013-02-01Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AldactazideSpironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1)Tablet, film coatedOralG.D. Searle LLC Division of Pfizer Inc1978-01-01Not applicableUs
AldactazideSpironolactone (50 mg/1) + Hydrochlorothiazide (50 mg/1)Tablet, film coatedOralG.D. Searle LLC Division of Pfizer Inc1978-01-01Not applicableUs00025 1021 31 nlmimage10 b146d8b6
Aldactazide 25Spironolactone (25 mg) + Hydrochlorothiazide (25 mg)TabletOralPfizer1960-12-31Not applicableCanada
Aldactazide 50Spironolactone (50 mg) + Hydrochlorothiazide (50 mg)TabletOralPfizer1983-12-31Not applicableCanada
Apo-spirozide TabSpironolactone (25 mg) + Hydrochlorothiazide (25 mg)TabletOralApotex Corporation1991-12-312011-08-05Canada
Spironolactone and HydrochlorothiazideSpironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1)TabletOralSun Pharmaceutical Industries Limited1987-07-02Not applicableUs
Spironolactone and HydrochlorothiazideSpironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1)TabletOralMylan Pharmaceuticals2012-07-262020-02-29Us0378 014120180907 15195 1depn7u
Spironolactone and HydrochlorothiazideSpironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1)TabletOralMylan Institutional2017-05-12Not applicableUs
Spironolactone and HydrochlorothiazideSpironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1)TabletOralPhysicians Total Care, Inc.1993-05-26Not applicableUs54868 069920180907 15195 16vhh6y
Spironolactone and HydrochlorothiazideSpironolactone (25 mg/1) + Hydrochlorothiazide (25 mg/1)TabletOralAmerincan Health Packaging2015-03-312018-02-28Us53489 0144 01 nlmimage10 4f0ea785
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
SpironolactoneSpironolactone (25 mg/1)Tablet, film coatedOralVintage Pharmaceuticals, LLC2006-10-312006-10-31Us
SpironolactoneSpironolactone (100 mg/1)Tablet, film coatedOralVintage Pharmaceuticals, LLC2006-10-312006-10-31Us
SpironolactoneSpironolactone (50 mg/1)Tablet, film coatedOralVintage Pharmaceuticals, LLC2006-10-312006-10-31Us
International/Other Brands
Osyrol / Spiresis / Spiretic / Spiroctan / Uractone / Verospiron / Xenalon
Categories
UNII
27O7W4T232
CAS number
52-01-7
Weight
Average: 416.573
Monoisotopic: 416.202130202
Chemical Formula
C24H32O4S
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

Pharmacology

Indication

Used primarily to treat low-renin hypertension, hypokalemia, and Conn's syndrome.

Associated Conditions
Pharmacodynamics

Spironolactone is a synthetic 17-lactone steroid which is a renal competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics. On its own, spironolactone is only a weak diuretic, but it can be combined with other diuretics. Due to its anti-androgen effect, it can also be used to treat hirsutism, and is a common component in hormone therapy for male-to-female transgendered people. Spironolactone inhibits the effect of aldosterone by competing for intracellular aldosterone receptor in the distal tubule cells. This increases the secretion of water and sodium, while decreasing the excretion of potassium. Spironolactone has a fairly slow onset of action, taking several days to develop and similarly the effect diminishes slowly.

Mechanism of action

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.

TargetActionsOrganism
AMineralocorticoid receptor
antagonist
Human
UAndrogen receptor
antagonist
Human
UProgesterone receptor
agonist
Human
UGlucocorticoid receptor
antagonist
Human
UCytochrome P450 11B2, mitochondrial
antagonist
Human
U17alpha-hydroxylase
antagonist
Human
U17,20-desmolase
antagonist
Human
U3-oxo-5-alpha-steroid 4-dehydrogenase
antagonist
USex hormone-binding globulin
binder
Human
UVoltage-dependent calcium channel
inhibitor
Human
UDihydrotestosterone receptor
inhibitor
Human
UNuclear receptor subfamily 1 group I member 2Not AvailableHuman
Absorption

Fairly rapidly absorbed from the gastrointestinal tract. Food increases the bioavailability of unmetabolized spironolactone by almost 100%.

Volume of distribution
Not Available
Protein binding

Spironolactone and its metabolites are more than 90% bound to plasma proteins.

Metabolism

Rapidly and extensively metabolized. The metabolic pathway of spironolactone is complex and can be divided into two main routes: those in which the sulfur moiety is retained and those in which the sulfur moiety is removed by dethioacetylation. Spironolactone is transformed to a reactive metabolite that can inactivate adrenal and testicular cytochrome P450 enzymes. It also has anti-androgenic activity.

Route of elimination

The metabolites are excreted primarily in the urine and secondarily in bile.

Half life

10 minutes

Clearance
Not Available
Toxicity

The oral LD50 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.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Spironolactone Action PathwayDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
4-MethoxyamphetamineThe therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Spironolactone.
AbacavirSpironolactone may increase the excretion rate of Abacavir which could result in a lower serum level and potentially a reduction in efficacy.
AbediterolThe therapeutic efficacy of Abediterol can be decreased when used in combination with Spironolactone.
AbemaciclibThe serum concentration of Abemaciclib can be decreased when it is combined with Spironolactone.
AbirateroneThe therapeutic efficacy of Abiraterone can be decreased when used in combination with Spironolactone.
AcarboseSpironolactone may increase the excretion rate of Acarbose which could result in a lower serum level and potentially a reduction in efficacy.
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Spironolactone.
AceclofenacThe risk or severity of renal failure, hyperkalemia, and hypertension can be increased when Aceclofenac is combined with Spironolactone.
AcemetacinThe therapeutic efficacy of Spironolactone can be decreased when used in combination with Acemetacin.
AcetaminophenSpironolactone may increase the excretion rate of Acetaminophen which could result in a lower serum level and potentially a reduction in efficacy.
Food Interactions
  • 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.

References

Synthesis Reference

Giuseppe Bernini, "Process for preparing micronized spironolactone." U.S. Patent US4332721, issued July, 1975.

US4332721
General References
  1. 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:2972662]
  2. 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:10471456]
  3. 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:607621]
External Links
Human Metabolome Database
HMDB0014565
KEGG Drug
D00443
KEGG Compound
C07310
PubChem Compound
5833
PubChem Substance
46508525
ChemSpider
5628
BindingDB
50228080
ChEBI
9241
ChEMBL
CHEMBL1393
Therapeutic Targets Database
DAP000297
PharmGKB
PA451483
IUPHAR
2875
Guide to Pharmacology
GtP Drug Page
HET
SNL
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Spironolactone
ATC Codes
C03DA01 — Spironolactone
AHFS Codes
  • 24:32.20 — Mineralocorticoid (Aldosterone) Receptor Antagonists
PDB Entries
2ab2 / 2oax / 3vhu
FDA label
Download (395 KB)
MSDS
Download (72.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentPolycystic Ovaries Syndrome1
0RecruitingBasic ScienceHyperandrogenism / Polycystic Ovaries Syndrome / Puberty1
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedTreatmentHealthy Volunteers1
1CompletedTreatmentHeart Failure, Unspecified1
1CompletedTreatmentHigh Blood Pressure (Hypertension)1
1Not Yet RecruitingDiagnosticCardiomyopathy With Unknown Etiology1
1TerminatedBasic ScienceType 2 Diabetic Nephropathy1
1, 2CompletedTreatmentCentral Serous Chorioretinitis1
1, 2RecruitingOtherNASH - Nonalcoholic Steatohepatitis1
1, 2RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1, 2RecruitingTreatmentPulmonary Arterial Hypertension (PAH)1
2Active Not RecruitingTreatmentEnd-Stage Renal Disease (ESRD)1
2Active Not RecruitingTreatmentHyperkalemia / Resistant Hypertension1
2CompletedPreventionAcute Kidney Injury (AKI) / IHD / Prophylaxis of Contrast-induced nephropathy1
2CompletedPreventionCutaneous Atrophy Due to Corticosteroids1
2CompletedPreventionHeart Failure, Unspecified1
2CompletedSupportive CareAdvanced Malignant Neoplasm / Dermatologic Complication / Dermatologic Complications / Neoplasms, Malignant1
2CompletedTreatmentACTH / Cortisol Resistance / Glucocorticoid therapy / Mineralcorticoid / Negative Feedback1
2CompletedTreatmentAcanthosis Nigricans / Polycystic Ovaries Syndrome1
2CompletedTreatmentCardiovascular Disease (CVD) / Chronic Kidney Disease (CKD)1
2CompletedTreatmentChronic Kidney Disease (CKD) / High Blood Pressure (Hypertension) / Hyperkalemia1
2CompletedTreatmentCongenital Heart Disease (CHD) / Endomyocardial Fibrosis / Heart Failure, Unspecified1
2CompletedTreatmentEnd Stage Renal Disease / Hemodialysis1
2CompletedTreatmentFemale Pattern Hair Loss1
2CompletedTreatmentHeart Failure, Unspecified2
2CompletedTreatmentHigh Blood Pressure (Hypertension)1
2CompletedTreatmentHypertension,Essential1
2CompletedTreatmentPuberty, Precocious1
2RecruitingPreventionCardiovascular Disease (CVD) / Diabetes Mellitus (DM) / High Blood Pressure (Hypertension)1
2RecruitingTreatmentAlbuminuria / Chronic Kidney Disease (CKD)1
2RecruitingTreatmentCancers1
2SuspendedTreatmentTransplant, Kidney1
2TerminatedTreatmentHigh Blood Pressure (Hypertension)1
2WithdrawnTreatmentAcute Heart Failure (AHF)1
2, 3Active Not RecruitingDiagnosticDiabetic Nephropathies / Retinopathy, Diabetic1
2, 3CompletedPreventionDiabetic Nephropathies / Glomerulonephritis / Kidney Diseases / Proteinuria1
2, 3CompletedPreventionNonvalvular Atrial Fibrillation1
2, 3RecruitingPreventionCancers / Critically Ill1
2, 3RecruitingTreatmentChronic Lung Disease of Prematurity / Chronic Lung Diseases1
2, 3RecruitingTreatmentHeart Failure, Unspecified1
3Active Not RecruitingTreatmentGlucose tolerance impaired / Heart Failure, Unspecified / Type 2 Diabetes Mellitus1
3Active Not RecruitingTreatmentNonvalvular Atrial Fibrillation1
3CompletedPreventionCalcifications, Vascular / Coronary Artery Calcifications1
3CompletedPreventionEnd Stage Renal Disease (ESRD)1
3CompletedPreventionHeart Failure, Unspecified1
3CompletedTreatmentArterial Hypertension / Diabetes Mellitus (DM) / Hypertension, Resistant to Conventional Therapy1
3CompletedTreatmentAutosomal Dominant Polycystic Kidney Disease (ADPKD)1
3CompletedTreatmentCardiovascular Disease (CVD) / Congestive Heart Failure (CHF) / Heart Diseases1
3CompletedTreatmentCongestive Heart Failure (CHF) / Diastolic Heart Failure1
3CompletedTreatmentDuchenne's Muscular Dystrophy (DMD)1
3CompletedTreatmentHeart Failure, Unspecified1
3CompletedTreatmentHypertension,Essential1
3CompletedTreatmentMyocardial Infarction1
3Not Yet RecruitingPreventionAcute Kidney Injury (AKI)1
3Not Yet RecruitingTreatmentAldosterone Blockade / Nonvalvular Atrial Fibrillation / Surgery, Cardiac1
3RecruitingPreventionEndstage Renal Disease1
3RecruitingTreatmentAcne Vulgaris1
3RecruitingTreatmentEnd Stage Renal Failure on Dialysis1
3RecruitingTreatmentST Elevation Myocardial Infarction1
4Active Not RecruitingDiagnosticHeart Failure, Unspecified / Nonischemic Dilated Cardiomyopathy1
4Active Not RecruitingTreatmentCardio-Renal Syndrome / Renal Insufficiency,Chronic1
4Active Not RecruitingTreatmentHypertension, Resistant to Conventional Therapy1
4Active Not RecruitingTreatmentNonvalvular Atrial Fibrillation1
4CompletedDiagnosticHeart Failure, Unspecified1
4CompletedPreventionAnthracycline Induced Cardiotoxicity1
4CompletedPreventionEnd-stage Renal Failure (ESRF)1
4CompletedPreventionHigh Blood Pressure (Hypertension)1
4CompletedTreatmentArterial Elasticity / Arterial Stiffness1
4CompletedTreatmentAscites / Liver Cirrhosis1
4CompletedTreatmentChronic Renal Failure (CRF)1
4CompletedTreatmentDiabetes Mellitus (DM) / Hypertension, Resistant to Conventional Therapy1
4CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
4CompletedTreatmentDiabetic Nephropathies1
4CompletedTreatmentDiastolic Heart Failure1
4CompletedTreatmentHeart Failure, Unspecified1
4CompletedTreatmentHeart Failure, Unspecified / Ventricular Dysfunction, Left1
4CompletedTreatmentHigh Blood Pressure (Hypertension)2
4CompletedTreatmentStable Chronic Heart Failure2
4Enrolling by InvitationPreventionDisorder Related to Renal Transplantation1
4Not Yet RecruitingTreatmentFibrosis / Hypertrophic Cardiomyopathy1
4RecruitingBasic ScienceHealthy Volunteers / Hypoglycemia1
4RecruitingPreventionBlood Pressures / High Blood Pressure (Hypertension) / Strokes1
4RecruitingTreatmentAtherosclerosis1
4RecruitingTreatmentCardiomyopathy Right Ventricular / Chronic Right-Sided Heart Failure / Pulmonary Arterial Hypertension (PAH) / Pulmonary Hypertension, Primary, 2 / Pulmonary Hypertension, Primary, 3 / Pulmonary Hypertension, Primary, 41
4RecruitingTreatmentHeart Failure With Preserved Ejection Fraction (HFpEF)1
4RecruitingTreatmentHyperkalemia / Type2 Diabetes1
4RecruitingTreatmentHypertension Resistant To Conventional Therapy1
4RecruitingTreatmentLiver Cirrhosis / Portal Hypertension1
4RecruitingTreatmentPulmonary Hypertension (PH)1
4RecruitingTreatmentTransplantation, Liver1
4SuspendedTreatmentAlcoholism / Cardiomyopathy, Alcoholic1
4TerminatedPreventionPatients With Fungic Infections1
4Unknown StatusTreatmentChronic Renal Failure (CRF)1
4Unknown StatusTreatmentDiabetic Nephropathies1
4Unknown StatusTreatmentHigh Blood Pressure (Hypertension)3
4Unknown StatusTreatmentHypertrophic Cardiomyopathy / Myocardial Fibrosis1
4Unknown StatusTreatmentKnee Osteoarthritis (Knee OA)1
4Unknown StatusTreatmentLiver Cirrhosis / Portal Hypertension1
4Unknown StatusTreatmentRenal Failure1
4Unknown StatusTreatmentHemodialysis-dependent patients1
4WithdrawnTreatmentCongestive Heart Failure (CHF) / End Stage Renal Disease (ESRD)1
4WithdrawnTreatmentEnd Stage Renal Disease (ESRD) / Hemodialysis-dependent patients1
4WithdrawnTreatmentFemale Androgenetic Alopecia1
4WithdrawnTreatmentHeart Failure, Unspecified1
Not AvailableCompletedNot AvailableFractures, Bone / Type 2 Diabetes Mellitus1
Not AvailableCompletedDiagnosticCardiovascular Disease (CVD)1
Not AvailableCompletedPreventionBMI >30 kg/m2 / Insulin Resistance1
Not AvailableCompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases1
Not AvailableCompletedTreatmentAcute Decompensated Heart Failure (ADHF)1
Not AvailableCompletedTreatmentChronic Kidney Disease (CKD) / Proteinuria1
Not AvailableCompletedTreatmentCongenital Disorders1
Not AvailableCompletedTreatmentCongestive Heart Failure (CHF)1
Not AvailableCompletedTreatmentDiabetic Nephropathies1
Not AvailableCompletedTreatmentHyperaldosteronism / Obstructive Sleep Apnea (OSA) / Resistant Hypertension1
Not AvailableCompletedTreatmentHypertension,Essential1
Not AvailableCompletedTreatmentHypokalemia Caused by Thiazide Diuretics / Idiopathic Hypercalciuria1
Not AvailableCompletedTreatmentMajor Depressive Disorder (MDD)1
Not AvailableCompletedTreatmentPolycystic Ovaries Syndrome1
Not AvailableCompletedTreatmentType 2 Diabetes Mellitus / Vascular Diseases1
Not AvailableEnrolling by InvitationPreventionLong Qt Syndrome 1-2 / Sudden Cardiac Death1
Not AvailableNot Yet RecruitingTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableRecruitingNot AvailableAlport Syndrome / Familial Benign Hematuria / Hereditary Kidney Disease / Pediatric Kidney Disease / Thin Basement Membrane Disease1
Not AvailableRecruitingBasic ScienceBMI >30 kg/m2 / Hyperandrogenemia / Polycystic Ovaries Syndrome1
Not AvailableRecruitingBasic SciencePrimary Aldosteronism1
Not AvailableRecruitingTreatmentDiabetes, Diabetes Mellitus Type 11
Not AvailableTerminatedTreatmentCongestive Heart Failure (CHF)1
Not AvailableUnknown StatusPreventionAcute Kidney Injury (AKI) / Acute Renal Injury1
Not AvailableUnknown StatusPreventionDiabetes Mellitus (DM) / Endocrine System Diseases / Glucose Metabolism Disorders / Metabolic Diseases1
Not AvailableUnknown StatusTreatmentNonvalvular Atrial Fibrillation1
Not AvailableWithdrawnTreatmentCongestive Heart Failure (CHF)2
Not AvailableWithdrawnTreatmentDiastolic Heart Failure1
Not AvailableWithdrawnTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableWithdrawnTreatmentPulmonary Hypertension (PH) / Right Heart Failure1

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
FormRouteStrength
TabletOral
TabletOral100 mg
TabletOral25 mg
SuspensionOral25 mg/5mL
TabletOral100 mg/1
TabletOral25 mg/1
TabletOral50 mg/1
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral50 mg/1
Tablet, film coatedOral
Prices
Unit descriptionCostUnit
Spironolactone powder12.56USD g
Aldactone 100 mg tablet2.14USD tablet
Aldactazide 50-50 mg tablet2.02USD tablet
Aldactazide 50-50 tablet1.92USD tablet
Aldactone 50 mg tablet1.84USD tablet
Spironolactone 100 mg tablet1.45USD tablet
Aldactazide 25-25 mg tablet1.26USD tablet
Aldactazide 25-25 tablet1.04USD tablet
Spironolactone 50 mg tablet0.83USD tablet
Aldactone 25 mg tablet0.8USD tablet
Spironolactone-HCTZ 25-25 mg tablet0.57USD tablet
Spironolactone 25 mg tablet0.5USD tablet
Novo-Spiroton 100 mg Tablet0.25USD tablet
Novo-Spiroton 25 mg Tablet0.11USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US9757394No2016-10-282036-10-28Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)134.5 °CPhysProp
water solubility22 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.78HANSCH,C ET AL. (1995)
logS-4.28ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00198 mg/mLALOGPS
logP3.1ALOGPS
logP3.64ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)18.01ChemAxon
pKa (Strongest Basic)-4.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area60.44 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity113.5 m3·mol-1ChemAxon
Polarizability46.03 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9912
Blood Brain Barrier+0.932
Caco-2 permeable+0.5432
P-glycoprotein substrateSubstrate0.5691
P-glycoprotein inhibitor IInhibitor0.6807
P-glycoprotein inhibitor IIInhibitor0.8388
Renal organic cation transporterNon-inhibitor0.727
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6638
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9276
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8681
Ames testNon AMES toxic0.9158
CarcinogenicityNon-carcinogens0.9288
BiodegradationNot ready biodegradable0.9696
Rat acute toxicity2.0150 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9427
hERG inhibition (predictor II)Non-inhibitor0.7002
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0006-9836000000-9f600bd39c3b914c0b17
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-014i-0000900000-5e2e1944e45fcef225d1
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-014i-0000900000-406c100eed5b6cdc3286

Taxonomy

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
Spironolactone / 3-oxo-delta-4-steroid / 3-oxosteroid / Oxosteroid / Delta-4-steroid / Cyclohexenone / Gamma butyrolactone / Tetrahydrofuran / Carboxylic acid ester / Carbothioic s-ester
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)

Targets

Kind
Protein
Organism
Human
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
  1. Sitruk-Ware R: Progestogens in hormonal replacement therapy: new molecules, risks, and benefits. Menopause. 2002 Jan-Feb;9(1):6-15. [PubMed:11791081]
  2. 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]
  3. 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]
  4. Frishman WH, Stier CT Jr: Aldosterone and aldosterone antagonism in systemic hypertension. Curr Hypertens Rep. 2004 Jun;6(3):195-200. [PubMed:15128471]
  5. 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]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  7. Sica DA: Pharmacokinetics and pharmacodynamics of mineralocorticoid blocking agents and their effects on potassium homeostasis. Heart Fail Rev. 2005 Jan;10(1):23-9. [PubMed:15947888]
  8. 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]
Details
2. Androgen receptor
Kind
Protein
Organism
Human
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
  1. 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]
Details
3. Progesterone receptor
Kind
Protein
Organism
Human
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
  1. 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]
Details
4. Glucocorticoid receptor
Kind
Protein
Organism
Human
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
  1. 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
Human
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
  1. 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]
6. 17alpha-hydroxylase
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
References
  1. Authors unspecified: Spironolactone and endocrine dysfunction. Ann Intern Med. 1976 Nov;85(5):630-6. [PubMed:984618]
  2. Desai; Meena P.; Vijayalakshmi Bhatia & P.S.N. Menon (2001). Pediatric Endocrine Disorders. Orient Blackswan. [ISBN:978-81-250-2025-7]
7. 17,20-desmolase
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
References
  1. Authors unspecified: Spironolactone and endocrine dysfunction. Ann Intern Med. 1976 Nov;85(5):630-6. [PubMed:984618]
  2. 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
Not Available
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:
References
  1. 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
Human
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
  1. Braunstein GD: Clinical practice. Gynecomastia. N Engl J Med. 2007 Sep 20;357(12):1229-37. [PubMed:17881754]
Kind
Protein
Organism
Human
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...
Gene Name
CACNG1
Uniprot ID
Q06432
Uniprot Name
Voltage-dependent calcium channel gamma-1 subunit
Molecular Weight
25028.105 Da
References
  1. 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]
  2. 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]
11. Dihydrotestosterone receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
References
  1. 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:2972662]
Kind
Protein
Organism
Human
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
  1. 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
Human
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
  1. 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]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  3. 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
Human
Pharmacological action
Unknown
Actions
Inhibitor
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
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. 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]

Transporters

Kind
Protein
Organism
Human
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
  1. 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
Human
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
  1. 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
Human
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
  1. 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
Human
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
  1. 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 September 22, 2018 22:22