Identification

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Name
Furosemide
Accession Number
DB00695  (APRD00608, DB07799)
Type
Small Molecule
Groups
Approved, Vet approved
Description

Furosemide is a loop diuretic that acts on the kidneys to ultimately increase water loss from the body. An anthranilic acid derivative,7 furosemide is most commonly used for edema secondary to various clinical conditions, such as congestive heart failure exacerbation, liver failure, or renal failure, and high blood pressure.8 It mainly works by inhibiting electrolyte reabsorption from the kidneys and enhancing the excretion of water from the body. Furosemide has a fast onset and short duration of diuretic action and has been used safely and effectively in both pediatric and adult patient populations.1

Being a potent diuretic, the use of furosemide is thought to be particularly beneficial when an agent with greater diuretic potential is desired. Intramuscular and intravenous formulations of furosemide may be used in individuals with impaired gastrointestinal absorption or when oral administration of the drug is clinically unsuitable. It is proposed that parenteral use should be replaced with oral furosemide, in the form of tablets or oral solution, as soon as practical.7

Structure
Thumb
Synonyms
  • 2-Furfurylamino-4-chloro-5-sulfamoylbenzoic acid
  • 4-Chloro-5-sulfamoyl-N-furfuryl-anthranilic acid
  • 4-Chloro-N-(2-furylmethyl)-5-sulfamoylanthranilic acid
  • 4-Chloro-N-furfuryl-5-sulfamoylanthranilic acid
  • Frusemide
  • Furosemid
  • Furosemida
  • Furosemide
  • Furosemidu
  • Furosemidum
External IDs
LB-502 / NSC-269420
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
FuosemideTablet40 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs1983-11-10Not applicableUs
FurosemideTablet20 mg/1Oralbryant ranch prepack1981-08-27Not applicableUs
FurosemideTablet20 mg/1OralWest-Ward Pharmaceuticals Corp.1983-11-10Not applicableUs
FurosemideTablet20 mg/1OralClinical Solutions Wholsesale1983-11-102017-06-23Us58118 429720180913 8702 1d8a6ug
FurosemideInjection, solution10 mg/1mLIntramuscular; IntravenousHF Acquisition Co LLC, DBA HealthFirst2018-09-14Not applicableUs
FurosemideTablet20 mg/1OralA-S Medication Solutions1981-10-192018-06-30Us50090 015220180907 15195 13xy8w
FurosemideTablet20 mg/1OralCardinal Health2008-03-262019-01-31Us
FurosemideTablet40 mg/1OralREMEDYREPACK INC.2018-03-19Not applicableUs
FurosemideTablet20 mg/1OralCardinal Health1981-08-272014-06-30Us55154 627520180907 15195 37bosv
FurosemideInjection, solution10 mg/1mLIntramuscular; IntravenousHospira, Inc.2006-07-312006-07-31Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo Furosemide Tab 20mgTabletOralApotex Corporation1977-12-31Not applicableCanada
Apo Furosemide Tab 40mgTabletOralApotex Corporation1976-12-31Not applicableCanada
Apo Furosemide Tab 80mgTabletOralApotex Corporation1986-12-31Not applicableCanada
Ava-furosemideTabletOralAvanstra Inc2011-08-112014-08-21Canada
Ava-furosemideTabletOralAvanstra Inc2011-08-112014-08-21Canada
Ava-furosemideTabletOralAvanstra Inc2011-08-112014-08-21Canada
Bio-furosemideTabletOralBiomed Pharma2003-04-11Not applicableCanada
Bio-furosemideTabletOralBiomed Pharma2003-04-11Not applicableCanada
Dom-furosemideTabletOralBiomed Pharma2003-10-142013-08-02Canada
Dom-furosemideTabletOralBiomed Pharma2003-10-142013-08-02Canada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Active-Medicated specimen collection kitFurosemide (20 mg/1) + Benzalkonium chloride (0.0013 g/1mL)KitTopicalN.O.R.T.H., Inc.2013-10-31Not applicableUs
Diascreen 12-Panel Medicated Collection SystemFurosemide (20 mg/1) + Benzalkonium chloride (0.13 g/100g)KitTopicalIt3 Medical Llc2016-07-27Not applicableUs
Diuscreen Medicated Collection KitFurosemide (20 mg/1) + Benzalkonium chloride (0.0013 g/1mL)KitTopicalMaveron Health, LLC.2015-06-012016-10-28Us
Diuscreen Multi-Drug Medicated Test KitFurosemide (20 mg/1) + Benzalkonium chloride (0.0013 g/1mL)KitTopicalMaveron Health, LLC.2015-06-012016-10-28Us
Rx-Specimen Collection KitFurosemide (20 mg/1) + Benzalkonium chloride (0.0013 g/1mL)KitTopicalMas Management Group Inc.2015-07-23Not applicableUs
TOXYCOLOGY Medicated Collection SystemFurosemide (20 mg/1) + Benzalkonium chloride (0.13 g/100g)KitTopicalIt3 Medical Llc2016-07-27Not applicableUs
Urinx Medicated Specimen CollectionFurosemide (20 mg/1) + Benzalkonium chloride (0.0013 g/1mL)KitTopicalPharmaco Technology Llc2015-06-012015-12-31Us
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
FurosemideFurosemide (20 mg/1)TabletOralRemedy Repack2010-11-012011-02-10Us
Specimen Collection KitFurosemide (20 mg/1) + Benzalkonium chloride (0.13 mg/1mL)KitTopicalAlvix Laboratories2015-04-21Not applicableUs
International/Other Brands
Diurapid (Mibe Jena) / Diurin (Mylan) / Diurmessel (Biomep) / Eutensin (Sanofi) / Frumex / Frusenex / Frusol (Rosemont) / Furo-Puren (Actavis) / Seguril (Sanofi)
Categories
UNII
7LXU5N7ZO5
CAS number
54-31-9
Weight
Average: 330.744
Monoisotopic: 330.007719869
Chemical Formula
C12H11ClN2O5S
InChI Key
ZZUFCTLCJUWOSV-UHFFFAOYSA-N
InChI
InChI=1S/C12H11ClN2O5S/c13-9-5-10(15-6-7-2-1-3-20-7)8(12(16)17)4-11(9)21(14,18)19/h1-5,15H,6H2,(H,16,17)(H2,14,18,19)
IUPAC Name
4-chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid
SMILES
NS(=O)(=O)C1=C(Cl)C=C(NCC2=CC=CO2)C(=C1)C(O)=O

Pharmacology

Indication

Furosemide is indicated in adults and pediatric patients for the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome.

It is also indicated for the treatment of hypertension alone or in combination with other antihypertensive agents in adults who were not shown to be inadequately controlled with thiazides.

Parenteral therapy of furosemide should be reserved for emergency clinical situations or patients who cannot take oral medications.7

Associated Conditions
Pharmacodynamics

Furosemide is used to manage hypertension and edema associated with congestive heart failure, cirrhosis, and renal disease, including the nephrotic syndrome. Furosemide is a potent loop diuretic which works to increase the excretion of Na+ and water by the kidneys by inhibiting their reabsorption from the proximal and distal tubules, as well as the loop of Henle.7 It works directly acts on the cells of the nephron and indirectly modifies the the content of the renal filtrate.6 Ultimately, furosemide increases the urine output by the kidney.

Protein-bound furosemide is delivered to its site of action in the kidneys and secreted via active secretion by nonspecific organic transporters expressed at the luminal site of action.4,7 Furosemide works directly acts on the cells of the nephron and indirectly modifies the the content of the renal filtrate.6 Furosemide mediates its diuretic effect after 1 and 1.5 hours following oral administration 4 and within 5 minutes following intravenous administration.7 The duration of diuretic effect is approximately 2 hours.7

Mechanism of action

Furosemide promotes diuresis by blocking tubular reabsorption of sodium and chloride in the proximal and distal tubules, as well as in the thick ascending loop of Henle. This is achieved through competitive inhibition of sodium-potassium-chloride cotransporters (NKCC2) expressed along these tubules in the nephron, resulting in excretion of water along with sodium, chloride, magnesium, and calcium.8

in the nephron by blocking the sodium-potassium-chloride cotransporters (NKCC2) expressed in the thick ascending limb of the loop of Henle. This is achieved through competitive inhibition at the chloride binding site on the cotransporter, thus preventing the transport of sodium from the lumen of the loop of Henle into the basolateral interstitium. Consequently, the lumen becomes more hypertonic while the interstitium becomes less hypertonic, which in turn diminishes the osmotic gradient for water reabsorption throughout the nephron. Because the thick ascending limb is responsible for 25% of sodium reabsorption in the nephron, furosemide is a very potent diuretic.

It is proposed that the main mechanism of action of furosemide is independent of its inhibitory effect on carbonic anhydrase and aldosterone.7

TargetActionsOrganism
ASolute carrier family 12 member 1
inhibitor
Humans
NCarbonic anhydrase 2
inhibitor
Humans
Additional Data Available
Adverse Effects

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Blackbox Warnings

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Absorption

Following oral administration, furosemide is absorbed from the gastrointestinal tract. It displays variable bioavailability from oral dosage forms, ranging from 10 to 90%.4 The oral bioavailability of furosemide from oral tablets or oral solution is about 64% and 60%, respectively, of that from an intravenous injection of the drug.7

Volume of distribution
Not Available
Protein binding

Furosemide is more than 95% bound to plasma proteins,4 mainly binding to serum albumin.7

Metabolism

It is proposed that the metabolism of furosemide mainly occurs in the kidneys and in the liver to a smaller extent. The kidneys are responsible for about 85% of total furosemide total clearance, where about 40% involves biotransformation.5 Two major metabolites of furosemide are furosemide glucuronide and saluamine (CSA).2 Furosemide glucuronide is an active metabolite that also mediates a diuretic effect.8 Only a small amount is hepatically metabolized to the defurfurylated derivative, 4-chloro-5-sulfamoylanthranilic acid.

Route of elimination

The kidneys are responsible for 85% of total furosemide total clearance, where about 43% of the drug undergoes renal excretion.5 Significantly more furosemide is excreted in urine following the I.V. injection than after the tablet or oral solution. Approximately 50% of the furosemide load is excreted unchanged in urine, and the rest is metabolized into glucuronide in the kidney.4

Half life

The terminal half-life of furosemide is approximately 2 hours.7

Clearance
Not Available
Toxicity

Profound diuresis may cause fluid and electrolyte depletion. Excessive dehydration and potassium depletion may occur. Excessive diuresis may cause rapid weight loss, orthostatic hypotension or acute hypotensive episodes. May also cause tinnitus, reversible or permanent hearing loss or reversible deafness.

In rats, the oral LD50, intraperitoneal LD50, and subcutaneous LD50 is 2600 mg/kg, 800 mg/kg, and 4600 mg/kg, respectively. The Lowest published toxic dose (TDLo) in a female is 6250 μg/kg.9

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Furosemide Action PathwayDrug 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.
DrugInteraction
1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid may decrease the antihypertensive activities of Furosemide.
1-benzylimidazole1-benzylimidazole may decrease the antihypertensive activities of Furosemide.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Furosemide.
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Furosemide.
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Furosemide.
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Furosemide.
4-Methoxyamphetamine4-Methoxyamphetamine may decrease the antihypertensive activities of Furosemide.
5-fluorouridineThe therapeutic efficacy of Furosemide can be decreased when used in combination with 5-fluorouridine.
5-methoxy-N,N-dimethyltryptamine5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Furosemide.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Furosemide.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

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  • Action
    Action

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Food Interactions
  • Avoid alcohol.
  • Avoid excess salt/sodium unless otherwise instructed by your physician.
  • Increase potassium intake; add a banana or orange juice; unless instructed otherwise.
  • Take with food to reduce irritation.

References

Synthesis Reference

Angelo Signor, Alfredo Guerrato, Giovanni Signor, "Process for the preparation of furosemide." U.S. Patent US5739361, issued June, 1971.

US5739361
General References
  1. Prandota J: Clinical pharmacology of furosemide in children: a supplement. Am J Ther. 2001 Jul-Aug;8(4):275-89. [PubMed:11441327]
  2. Ponto LL, Schoenwald RD: Furosemide (frusemide). A pharmacokinetic/pharmacodynamic review (Part I). Clin Pharmacokinet. 1990 May;18(5):381-408. doi: 10.2165/00003088-199018050-00004. [PubMed:2185908]
  3. Prandota J: Furosemide: progress in understanding its diuretic, anti-inflammatory, and bronchodilating mechanism of action, and use in the treatment of respiratory tract diseases. Am J Ther. 2002 Jul-Aug;9(4):317-28. [PubMed:12115021]
  4. Oh SW, Han SY: Loop Diuretics in Clinical Practice. Electrolyte Blood Press. 2015 Jun;13(1):17-21. doi: 10.5049/EBP.2015.13.1.17. Epub 2015 Jun 30. [PubMed:26240596]
  5. Pichette V, du Souich P: Role of the kidneys in the metabolism of furosemide: its inhibition by probenecid. J Am Soc Nephrol. 1996 Feb;7(2):345-9. [PubMed:8785407]
  6. 28. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 352-354). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
  7. Furosemide - FDA Label [Link]
  8. Furosemide - StatPearls - NCBI Bookshelf [Link]
  9. Furosemide SAFETY DATA SHEET - Cayman Chemical [Link]
External Links
Human Metabolome Database
HMDB0001933
KEGG Drug
D00331
KEGG Compound
C07017
PubChem Compound
3440
PubChem Substance
46506779
ChemSpider
3322
BindingDB
25902
ChEBI
47426
ChEMBL
CHEMBL35
Therapeutic Targets Database
DAP000043
PharmGKB
PA449719
HET
FUN
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Furosemide
ATC Codes
C03EB01 — Furosemide and potassium-sparing agentsC03CA01 — FurosemideC03CB01 — Furosemide and potassiumG01AE10 — Combinations of sulfonamides
AHFS Codes
  • 40:28.08 — Loop Diuretics
PDB Entries
1z9y / 2xn5 / 3rf4 / 6de9

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentAcute Kidney Injury (AKI)1
0RecruitingBasic ScienceHeart Failure With Preserved Ejection Fraction (HFpEF)1
0RecruitingBasic ScienceInteraction Drug Food1
0RecruitingPreventionTransfusion-associated Circulatory Overload1
0RecruitingTreatmentInfants, Premature / Premature Births1
1CompletedNot AvailableSchizophrenic Disorders1
1CompletedBasic ScienceDrug Drug Interaction (DDI)1
1CompletedBasic ScienceDrug Interaction Potentiation1
1CompletedBasic ScienceDyspnea1
1CompletedBasic ScienceHealthy Volunteers2
1CompletedBasic ScienceHealthy Volunteers / Pharmacokinetics of Ipragliflozin1
1CompletedBasic ScienceRenal Hemodynamics1
1CompletedDiagnosticDehydration1
1CompletedOtherHealthy Volunteers1
1CompletedTreatmentAcute Heart Failure (AHF)1
1CompletedTreatmentCongestive Heart Failure (CHF) / Prophylaxis of cardiomyopathy1
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers1
1CompletedTreatmentGastroretentive Drug Formulation of Furosemide / Oedema1
1CompletedTreatmentHealthy Volunteers3
1CompletedTreatmentRenal Failure1
1CompletedTreatmentType 2 Diabetes Mellitus1
1Not Yet RecruitingTreatmentBody Weight Changes1
1RecruitingTreatmentDifficulty Breathing1
1TerminatedTreatmentHeart Failure / Impaired Renal Function1
1WithdrawnBasic ScienceMedication Absorption1
1, 2Active Not RecruitingBasic ScienceDyspnea / Healthy Volunteers1
1, 2Active Not RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1, 2CompletedSupportive CareDyspnea1
1, 2CompletedTreatmentHeart Failure1
1, 2CompletedTreatmentHeart Failure / Renal Function Abnormal1
1, 2Not Yet RecruitingBasic ScienceHigh Blood Pressure (Hypertension) / Inflammatory Reaction / Salt; Excess1
1, 2Not Yet RecruitingTreatmentCongestive Heart Failure (CHF)1
1, 2WithdrawnTreatmentAcute Decompensated Heart Failure (ADHF)1
2Active Not RecruitingOtherChronic Lung Disease of Prematurity1
2CompletedSupportive CarePulmonary Complications1
2CompletedTreatmentAcute Lung Injury (ALI)1
2CompletedTreatmentAscites / Liver Cirrhosis1
2CompletedTreatmentBronchiolitis1
2CompletedTreatmentCutaneous Warts1
2CompletedTreatmentHeart Failure2
2CompletedTreatmentTransient Tachypnoea of the Newborn1
2RecruitingPreventionHigh Blood Pressure (Hypertension)1
2RecruitingPreventionHypertension, Pregnancy-Induced1
2RecruitingTreatmentActinic Keratosis (AK)1
2RecruitingTreatmentCardiac Failure / Congestive Heart Failure (CHF) / Heart Decompensation / Myocardial Failure1
2RecruitingTreatmentHeart Failure1
2RecruitingTreatmentPolyps, Nasal1
2TerminatedTreatmentAcute Heart Failure (AHF) / Decompensated Heart Failure1
2TerminatedTreatmentMalignancies1
2WithdrawnTreatmentDelayed Graft Function1
2, 3Active Not RecruitingTreatmentLiver Cirrhosis / Refractory/Recurrent Ascites1
2, 3CompletedTreatmentCongestive Heart Failure (CHF)1
2, 3CompletedTreatmentHeart Failure2
2, 3RecruitingHealth Services ResearchAcute Heart Failure (AHF)1
2, 3RecruitingTreatmentHeart Failure1
2, 3TerminatedTreatmentAcute Renal Failure (ARF)1
3CompletedPreventionAtherosclerosis / Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / High Blood Pressure (Hypertension) / High Cholesterol / Type 2 Diabetes Mellitus1
3CompletedSupportive CareBronchiolitis1
3CompletedTreatmentCongestive Heart Failure (CHF) / Impaired Renal Function1
3CompletedTreatmentCutaneous Common Warts1
3CompletedTreatmentFluid Overload1
3CompletedTreatmentHeart Failure2
3CompletedTreatmentHypertension,Essential / Impaired Renal Function1
3CompletedTreatmentTransient Tachypnea of the Newborn1
3CompletedTreatmentChronic heart failure with reduced ejection fraction (NYHA Class III) / Chronic heart failure with reduced ejection fraction (NYHA Class IV)1
3Not Yet RecruitingTreatmentAcute Myocardial Infarction With Right Ventricular Extension1
3RecruitingDiagnosticChronic Kidney Disease (CKD)1
3RecruitingTreatmentFluid Balance of ICU Patients / Fluid Overload1
3RecruitingTreatmentHeart Failure2
3RecruitingTreatmentPulmonary Embolism With Right Ventricle Enlargement1
3SuspendedTreatmentCongestive Heart Failure (CHF)1
3TerminatedTreatmentCritically-ill Patients / Renal Failure1
3Unknown StatusPreventionContrast Induced Nephropathy (CIN)1
3Unknown StatusTreatmentChronic Lung Diseases1
3WithdrawnTreatmentHeart Failure1
3WithdrawnTreatmentRenal Function Disorder1
4Active Not RecruitingTreatmentAcute Heart Failure (AHF) / Fluid Overload1
4CompletedOtherCystoscopy1
4CompletedPreventionArterial Hypotension / Congestive Heart Failure (CHF) / High Blood Pressure (Hypertension) / Oedema1
4CompletedPreventionHigh Blood Pressure (Hypertension)1
4CompletedTreatmentAcute Decompensated Heart Failure (ADHF)1
4CompletedTreatmentAcute Heart Failure (AHF)1
4CompletedTreatmentAscites / Liver Cirrhosis2
4CompletedTreatmentChronic Heart Failure (CHF) / Congestive Heart Failure (CHF)1
4CompletedTreatmentChronic Kidney Disease (CKD)1
4CompletedTreatmentColorectal Disorders1
4CompletedTreatmentCongestive Heart Failure (CHF)2
4CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
4CompletedTreatmentGlomerulonephritis minimal lesion / Oedema1
4CompletedTreatmentHeart Failure2
4CompletedTreatmentHeart Failure, Diastolic1
4CompletedTreatmentHeart Failure / Type 2 Diabetes Mellitus1
4CompletedTreatmentHypertension Resistant To Conventional Therapy1
4CompletedTreatmentObstructive Sleep Apnea (OSA)1
4CompletedTreatmentPreeclampsia1
4CompletedTreatmentStable Chronic Heart Failure2
4Not Yet RecruitingTreatmentAcute Heart Failure (AHF) / Chronic Heart Failure (CHF) / Heart Failure1
4RecruitingDiagnosticEnd Stage Renal Disease (ESRD)1
4RecruitingTreatmentAcute Kidney Injury (AKI)1
4RecruitingTreatmentHeart Failure1
4RecruitingTreatmentProteinuria / Renal Insufficiency,Chronic1
4RecruitingTreatmentPulmonary Embolism (PE)1
4SuspendedTreatmentAcute Decompensated Heart Failure (ADHF)1
4TerminatedTreatmentAcute Decompensated Heart Failure (ADHF)2
4TerminatedTreatmentAcute Kidney Injury (AKI) / Critical Illness / Fluid Overload1
4TerminatedTreatmentCompensated Heart Failure1
4Unknown StatusPreventionDiabetic Nephropathies1
4Unknown StatusTreatmentAcute Heart Failure (AHF)1
4Unknown StatusTreatmentDiuresis Preserved / Hemodialysis Treatment / Kidney Insufficiency, Chronic1
4Unknown StatusTreatmentHealthy Male and Female Volunteers1
4WithdrawnTreatmentAcute Heart Failure (AHF)1
4WithdrawnTreatmentAcute Renal Failure (ARF)1
Not AvailableActive Not RecruitingNot AvailableAcute Heart Failure (AHF)1
Not AvailableActive Not RecruitingDiagnosticAcute Renal Failure (ARF)1
Not AvailableActive Not RecruitingTreatmentCritical Care / Fluid Shifts1
Not AvailableCompletedNot AvailableAcidosis, Renal Tubular / Calcium Nephrolithiasis / Vacuolar Proton-Translocating ATPases1
Not AvailableCompletedNot AvailableHealthy Volunteers1
Not AvailableCompletedNot AvailableHigh Blood Pressure (Hypertension)1
Not AvailableCompletedDiagnosticCardiorenal Syndrome1
Not AvailableCompletedDiagnosticChronic Kidney Disease (CKD)1
Not AvailableCompletedPreventionAcute Renal Failure (ARF)1
Not AvailableCompletedPreventionAcute Renal Failure (ARF) / Chronic Renal Failure (CRF) / Prophylaxis of Contrast-induced nephropathy1
Not AvailableCompletedTreatmentAcromegaly1
Not AvailableCompletedTreatmentAcute Kidney Injury (AKI)1
Not AvailableCompletedTreatmentCirrhosis, Decompensated1
Not AvailableCompletedTreatmentDiabetic Nephropathies1
Not AvailableCompletedTreatmentFluid Over-load1
Not AvailableCompletedTreatmentHeart Failure1
Not AvailableCompletedTreatmentInsulin Resistance1
Not AvailableCompletedTreatmentNeoplasms, Brain1
Not AvailableCompletedTreatmentObesity-induced Hyperfiltration1
Not AvailableCompletedTreatmentRenal Stones1
Not AvailableRecruitingDiagnosticDelayed Graft Function / Kidney Function / Kidney Transplant; Complications1
Not AvailableRecruitingDiagnosticHeart Failure1
Not AvailableRecruitingPreventionChronic Kidney Disease (CKD) / Hyperparathyroidism, Secondary1
Not AvailableRecruitingTreatmentGlomerulonephritis minimal lesion1
Not AvailableRecruitingTreatmentHeart Failure1
Not AvailableSuspendedTreatmentHeart Decompensation1
Not AvailableTerminatedDiagnosticAcute Decompensated Heart Failure (ADHF)1
Not AvailableTerminatedDiagnosticCritical Illness / Oliguria1
Not AvailableTerminatedTreatmentAcute Decompensated Heart Failure (ADHF) / Cardiac Failure / Heart Failure1
Not AvailableTerminatedTreatmentBrain Swelling / Dehydration1
Not AvailableTerminatedTreatmentHigh Blood Pressure (Hypertension)1
Not AvailableTerminatedTreatmentObesity-induced Hyperfiltration1
Not AvailableUnknown StatusNot AvailableHeart Failure1
Not AvailableUnknown StatusTreatmentIntra-Abdominal Hypertension1
Not AvailableUnknown StatusTreatmentLow-Renin Hypertension1
Not AvailableWithdrawnPreventionRenal Impairment After Cardiac Surgery1
Not AvailableWithdrawnTreatmentAnemia Treatment Among Patients Suffering From Left Ventricular Systolic Dysfunction1
Not AvailableWithdrawnTreatmentCongestive Heart Failure (CHF)2
Not AvailableWithdrawnTreatmentHypernatremia / Respiratory Failure / Volume Overload1
Not AvailableWithdrawnTreatmentLeukemias1

Pharmacoeconomics

Manufacturers
  • Abraxis pharmaceutical products
  • App pharmaceuticals llc
  • Astrazeneca lp
  • Baxter healthcare corp anesthesia and critical care
  • Hospira inc
  • International medication system
  • Luitpold pharmaceuticals inc
  • Marsam pharmaceuticals llc
  • Organon usa inc
  • Smith and nephew solopak div smith and nephew
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
  • Wockhardt ltd
  • Wyeth ayerst laboratories
  • Sanofi aventis us llc
  • Roxane laboratories inc
  • Wockhardt eu operations (swiss) ag
  • Dava pharmaceuticals inc
  • Excellium pharmaceutical inc
  • International medication systems ltd
  • Ipca laboratories ltd
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Kalapharm inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Superpharm corp
  • Vintage pharmaceuticals inc
  • County line pharmaceuticals llc
Packagers
  • Advanced Pharmaceutical Services Inc.
  • American Regent
  • Amerisource Health Services Corp.
  • Apotheca Inc.
  • APP Pharmaceuticals
  • A-S Medication Solutions LLC
  • Bryant Ranch Prepack
  • C.O. Truxton Inc.
  • Cardinal Health
  • Central Texas Community Health Centers
  • Comprehensive Consultant Services Inc.
  • Coupler Enterprises Inc.
  • CVS Pharmacy
  • DAVA Pharmaceuticals
  • Dept Health Central Pharmacy
  • DHHS Program Support Center Supply Service Center
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Excellium Pharmaceutical Inc.
  • General Injectables and Vaccines Inc.
  • Goldline Laboratories Inc.
  • Group Health Cooperative
  • H and H Laboratories
  • Heartland Repack Services LLC
  • Hospira Inc.
  • Intervet International
  • Ipca Laboratories Ltd.
  • Ivax Pharmaceuticals
  • Kaiser Foundation Hospital
  • Lake Erie Medical and Surgical Supply
  • Liberty Pharmaceuticals
  • Luitpold Pharmaceuticals Inc.
  • Macnary Ltd.
  • Major Pharmaceuticals
  • Mason Distributors
  • Mckesson Corp.
  • Medvantx Inc.
  • Merrell Pharmaceuticals Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Neighborcare Repackaging Inc.
  • Neuman Distributors Inc.
  • Norwich Pharmaceuticals Inc.
  • Nucare Pharmaceuticals Inc.
  • Ohm Laboratories Inc.
  • Palmetto Pharmaceuticals Inc.
  • Patheon Inc.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Qualitest
  • Ranbaxy Laboratories
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Remedy Repack
  • Roxane Labs
  • Sandhills Packaging Inc.
  • Sandoz
  • Sanofi-Aventis Inc.
  • Southwood Pharmaceuticals
  • Spectrum Pharmaceuticals
  • Stat Scripts LLC
  • Talbert Medical Management Corp.
  • Taylor Pharmaceuticals
  • Tya Pharmaceuticals
  • UDL Laboratories
  • United Research Laboratories Inc.
  • Va Cmop Dallas
  • Vangard Labs Inc.
  • Vatring Pharmaceuticals
  • Vedco Inc.
  • Vintage Pharmaceuticals Inc.
  • Watson Pharmaceuticals
  • Wockhardt Ltd.
Dosage forms
FormRouteStrength
KitTopical
InjectionIntramuscular; Intravascular10 mg/1mL
InjectionIntramuscular; Intravenous10 mg/2mL
InjectionIntramuscular; Intravenous10 mg/1mL
InjectionIntramuscular; Intravenous100 mg/10mL
InjectionIntramuscular; Intravenous20 mg/2mL
InjectionIntramuscular; Intravenous40 mg/4mL
InjectionIntravenous10 mg/1mL
Injection, solutionIntramuscular; Intravenous10 mg/1mL
Injection, solutionIntramuscular; Intravenous100 mg/10mL
Injection, solutionIntramuscular; Intravenous20 mg/2mL
Injection, solutionIntramuscular; Intravenous40 mg/4mL
Injection, solutionIntravenous10 mg/1mL
SolutionOral10 mg/1mL
SolutionOral40 mg/5mL
SolutionOral40 mg/4mL
TabletOral20 mg/1
TabletOral20 mg
TabletOral40 mg/1
TabletOral40 mg
TabletOral80 mg/1
TabletOral80 mg
LiquidIntramuscular; Intravenous
SolutionIntramuscular; Intravenous
SolutionIntravenous
TabletOral
LiquidOral
SolutionOral
LiquidIntravenous
Prices
Unit descriptionCostUnit
Hydro 40 40% Foam 150 gm Can182.52USD can
Hydro 40 40% Foam 70 gm Can148.99USD can
Furosemide 10 mg/ml Solution 60ml Bottle17.99USD bottle
Furosemide 10 mg/ml Solution 120ml Bottle15.98USD bottle
Furosemide powder3.51USD g
Lasix Special 500 mg Tablet3.25USD tablet
Urex 1 gm tablet2.47USD tablet
Furosemide 10 mg/ml cartrg1.45USD ml
Lasix 80 mg tablet1.0USD tablet
Furosemide 10 mg/ml Solution0.9USD ml
Furosemide 10 mg/ml0.75USD ml
Lasix 40 mg tablet0.53USD tablet
Furosemide 80 mg tablet0.45USD tablet
Lasix 20 mg tablet0.42USD tablet
Lasix 10 mg/ml Solution0.3USD ml
CVS Pharmacy diuretic 50 mg softgel0.17USD softgel capsule
Furosemide 40 mg tablet0.16USD tablet
Furosemide 20 mg tablet0.14USD tablet
Apo-Furosemide 80 mg Tablet0.13USD tablet
Novo-Semide 80 mg Tablet0.13USD tablet
Nat herbal diuretic tablet sa0.1USD tablet
Apo-Furosemide 40 mg Tablet0.07USD tablet
Natural herbal diuretic tablet0.07USD tablet
Novo-Semide 40 mg Tablet0.07USD tablet
Apo-Furosemide 20 mg Tablet0.05USD tablet
Novo-Semide 20 mg Tablet0.05USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)206U.S. Patent 3,058,882.
water solubility73.1 mg/L (at 30 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.03SANGSTER (1993)
logS-3.66ADME Research, USCD
Caco2 permeability-6.5ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.118 mg/mLALOGPS
logP2.71ALOGPS
logP1.75ChemAxon
logS-3.4ALOGPS
pKa (Strongest Acidic)4.25ChemAxon
pKa (Strongest Basic)-1.5ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area122.63 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity77.47 m3·mol-1ChemAxon
Polarizability30.55 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9155
Blood Brain Barrier-0.8833
Caco-2 permeable-0.6436
P-glycoprotein substrateNon-substrate0.8775
P-glycoprotein inhibitor INon-inhibitor0.9272
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterNon-inhibitor0.924
CYP450 2C9 substrateNon-substrate0.6878
CYP450 2D6 substrateNon-substrate0.8351
CYP450 3A4 substrateNon-substrate0.6789
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9602
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6885
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.6469
BiodegradationNot ready biodegradable0.9881
Rat acute toxicity2.1362 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9342
hERG inhibition (predictor II)Non-inhibitor0.8525
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
MS/MS Spectrum - Quattro_QQQ 10V, N/ALC-MS/MSsplash10-03dr-0090000000-da505a3f09285d049f34
MS/MS Spectrum - Quattro_QQQ 25V, N/ALC-MS/MSsplash10-0f89-2190000000-53c91100e89c81f0fa30
MS/MS Spectrum - Quattro_QQQ 40V, N/ALC-MS/MSsplash10-01ox-9660000000-83d8486cbca0dd3487c9
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 , negativeLC-MS/MSsplash10-000i-0090000000-f3a3dcb92cfcdff9f7dc
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0019000000-946089b12d2ab6fd05a4
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0090000000-04af1dec204d462d4bc4
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0udi-1090000000-1af70d23e1a0ebaa0878
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-9770000000-0c5cd578b5b69a1a61d4
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-9800000000-3303b20f9b23e24ae312
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-9400000000-23cfec716ac8fbcb092f
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-0019000000-e73aa1d969ab4255732b
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0090000000-33053544119c01ac6b45
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0udi-1090000000-7029ab63efa73a3ff88d
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-9670000000-4bad8928bbcfc85f431f
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-9800000000-2193e38e314f2b18be26
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004i-9600000000-e703f7ab6221182df156
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0090000000-f3645e993869ff3886ba
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0090000000-18400153a811f7100a2f
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0f79-0090000000-7e491b92dab050fb81c0
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0090000000-8e41d38fe799d96230a6
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0090000000-cfec4a54171c58245919
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-0ug0-0193000000-b55039ca13cbc3acd9a8
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0290000000-1f1017fe4370d9541f6d
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001i-9110000000-505f1e781d384073f688
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-001j-9000000000-cd886e0521fb4d1bdc82
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000t-9000000000-8a69e99643ee37bc1883
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000t-9000000000-f7ac3c9eea39ed725cfc
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000t-9000000000-8a294fd51a34073aa4a1
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-9000000000-b16e204dec9ae7938d40
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0f8a-9220000000-3bde836fe7e67c9b8755
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000t-9000000000-9025c2261c96ca3aa551
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-000t-9000000000-8d05f828403d0fe7cac4
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-9000000000-3cd4f8015eb5fafacacb
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-9000000000-34937031271e62c39c1f
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-9000000000-40e9966d335f71aedb96
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0290000000-586707fb0116e8b61643
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-001i-9000000000-f6727b05eb8ee02a6e7c
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00di-0090000000-51662bec1d461d0f0a5a
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00di-0090000000-8eea44e0dd27bb59939d
1H NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

Description
This compound belongs to the class of organic compounds known as aminobenzenesulfonamides. These are organic compounds containing a benzenesulfonamide moiety with an amine group attached to the benzene ring.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzenesulfonamides
Direct Parent
Aminobenzenesulfonamides
Alternative Parents
4-halobenzoic acids / Aminobenzoic acids / Halobenzoic acids / Benzenesulfonyl compounds / Benzoic acids / Aniline and substituted anilines / Benzoyl derivatives / Phenylalkylamines / Secondary alkylarylamines / Chlorobenzenes
show 15 more
Substituents
Aminobenzenesulfonamide / 4-halobenzoic acid or derivatives / Aminobenzoic acid / Aminobenzoic acid or derivatives / Halobenzoic acid or derivatives / 4-halobenzoic acid / Halobenzoic acid / Benzenesulfonyl group / Benzoic acid / Benzoic acid or derivatives
show 37 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
sulfonamide, furans, chlorobenzoic acid (CHEBI:47426)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Sodium:potassium:chloride symporter activity
Specific Function
Electrically silent transporter system. Mediates sodium and chloride reabsorption. Plays a vital role in the regulation of ionic balance and cell volume.
Gene Name
SLC12A1
Uniprot ID
Q13621
Uniprot Name
Solute carrier family 12 member 1
Molecular Weight
121449.13 Da
References
  1. Brater DC: Pharmacology of diuretics. Am J Med Sci. 2000 Jan;319(1):38-50. [PubMed:10653443]
  2. Davies DL, Wilson GM: Diuretics: mechanism of action and clinical application. Drugs. 1975;9(3):178-226. [PubMed:1092541]
  3. Vormfelde SV, Sehrt D, Toliat MR, Schirmer M, Meineke I, Tzvetkov M, Nurnberg P, Brockmoller J: Genetic variation in the renal sodium transporters NKCC2, NCC, and ENaC in relation to the effects of loop diuretic drugs. Clin Pharmacol Ther. 2007 Sep;82(3):300-9. Epub 2007 Apr 25. [PubMed:17460608]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
  5. Gimenez I: Molecular mechanisms and regulation of furosemide-sensitive Na-K-Cl cotransporters. Curr Opin Nephrol Hypertens. 2006 Sep;15(5):517-23. doi: 10.1097/01.mnh.0000242178.44576.b0. [PubMed:16914965]
  6. Limmer F, Schinner E, Castrop H, Vitzthum H, Hofmann F, Schlossmann J: Regulation of the Na(+)-K(+)-2Cl(-) cotransporter by cGMP/cGMP-dependent protein kinase I after furosemide administration. FEBS J. 2015 Oct;282(19):3786-98. doi: 10.1111/febs.13376. Epub 2015 Jul 30. [PubMed:26183401]
Details
2. Carbonic anhydrase 2
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Zinc ion binding
Specific Function
Essential for bone resorption and osteoclast differentiation (By similarity). Reversible hydration of carbon dioxide. Can hydrate cyanamide to urea. Involved in the regulation of fluid secretion in...
Gene Name
CA2
Uniprot ID
P00918
Uniprot Name
Carbonic anhydrase 2
Molecular Weight
29245.895 Da
References
  1. Ranjbar S, Ghobadi S, Khodarahmi R, Nemati H: Spectroscopic characterization of furosemide binding to human carbonic anhydrase II. Int J Biol Macromol. 2012 May 1;50(4):910-7. doi: 10.1016/j.ijbiomac.2012.02.005. Epub 2012 Feb 16. [PubMed:22343084]
  2. Supuran CT: Diuretics: from classical carbonic anhydrase inhibitors to novel applications of the sulfonamides. Curr Pharm Des. 2008;14(7):641-8. [PubMed:18336309]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Phosphogluconate dehydrogenase (decarboxylating) activity
Specific Function
Catalyzes the oxidative decarboxylation of 6-phosphogluconate to ribulose 5-phosphate and CO(2), with concomitant reduction of NADP to NADPH.
Gene Name
PGD
Uniprot ID
P52209
Uniprot Name
6-phosphogluconate dehydrogenase, decarboxylating
Molecular Weight
53139.56 Da
References
  1. Akkemik E, Budak H, Ciftci M: Effects of some drugs on human erythrocyte 6-phosphogluconate dehydrogenase: an in vitro study. J Enzyme Inhib Med Chem. 2010 Aug;25(4):476-9. doi: 10.3109/14756360903257900. [PubMed:20235752]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. Williams JA, Hyland R, Jones BC, Smith DA, Hurst S, Goosen TC, Peterkin V, Koup JR, Ball SE: Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8. doi: 10.1124/dmd.104.000794. Epub 2004 Aug 10. [PubMed:15304429]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
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
  1. Lebedev AA, Samokrutova OV: [Study of the binding of diuretics by serum proteins according to changes in tryptophan fluorescence]. Farmakol Toksikol. 1989 May-Jun;52(3):40-3. [PubMed:2792351]
  2. Furosemide - FDA Label [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Serine-type endopeptidase inhibitor activity
Specific Function
Major thyroid hormone transport protein in serum.
Gene Name
SERPINA7
Uniprot ID
P05543
Uniprot Name
Thyroxine-binding globulin
Molecular Weight
46324.12 Da
References
  1. Stockigt JR, Lim CF, Barlow JW, Wynne KN, Mohr VS, Topliss DJ, Hamblin PS, Sabto J: Interaction of furosemide with serum thyroxine-binding sites: in vivo and in vitro studies and comparison with other inhibitors. J Clin Endocrinol Metab. 1985 May;60(5):1025-31. doi: 10.1210/jcem-60-5-1025. [PubMed:2579968]
  2. CYTOMEL (liothyronine) FDA label [File]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
Molecular Weight
61815.78 Da
References
  1. Kim GH, Na KY, Kim SY, Joo KW, Oh YK, Chae SW, Endou H, Han JS: Up-regulation of organic anion transporter 1 protein is induced by chronic furosemide or hydrochlorothiazide infusion in rat kidney. Nephrol Dial Transplant. 2003 Aug;18(8):1505-11. [PubMed:12897087]
  2. Hosoyamada M, Sekine T, Kanai Y, Endou H: Molecular cloning and functional expression of a multispecific organic anion transporter from human kidney. Am J Physiol. 1999 Jan;276(1 Pt 2):F122-8. [PubMed:9887087]
  3. Lu R, Chan BS, Schuster VL: Cloning of the human kidney PAH transporter: narrow substrate specificity and regulation by protein kinase C. Am J Physiol. 1999 Feb;276(2 Pt 2):F295-303. [PubMed:9950961]
  4. Uwai Y, Saito H, Hashimoto Y, Inui KI: Interaction and transport of thiazide diuretics, loop diuretics, and acetazolamide via rat renal organic anion transporter rOAT1. J Pharmacol Exp Ther. 2000 Oct;295(1):261-5. [PubMed:10991988]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Symporter activity
Specific Function
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cat...
Gene Name
SLC22A5
Uniprot ID
O76082
Uniprot Name
Solute carrier family 22 member 5
Molecular Weight
62751.08 Da
References
  1. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. [PubMed:10525100]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. Cha SH, Sekine T, Fukushima JI, Kanai Y, Kobayashi Y, Goya T, Endou H: Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86. [PubMed:11306713]
  2. Kusuhara H, Sekine T, Utsunomiya-Tate N, Tsuda M, Kojima R, Cha SH, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. J Biol Chem. 1999 May 7;274(19):13675-80. [PubMed:10224140]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
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. Bakos E, Evers R, Sinko E, Varadi A, Borst P, Sarkadi B: Interactions of the human multidrug resistance proteins MRP1 and MRP2 with organic anions. Mol Pharmacol. 2000 Apr;57(4):760-8. [PubMed:10727523]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
May mediate the release of newly synthesized prostaglandins from cells, the transepithelial transport of prostaglandins, and the clearance of prostaglandins from the circulation. Transports PGD2, a...
Gene Name
SLCO2A1
Uniprot ID
Q92959
Uniprot Name
Solute carrier organic anion transporter family member 2A1
Molecular Weight
70043.33 Da
References
  1. Kanai N, Lu R, Satriano JA, Bao Y, Wolkoff AW, Schuster VL: Identification and characterization of a prostaglandin transporter. Science. 1995 May 12;268(5212):866-9. [PubMed:7754369]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
Gene Name
SLC22A11
Uniprot ID
Q9NSA0
Uniprot Name
Solute carrier family 22 member 11
Molecular Weight
59970.945 Da
References
  1. Cha SH, Sekine T, Kusuhara H, Yu E, Kim JY, Kim DK, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta. J Biol Chem. 2000 Feb 11;275(6):4507-12. [PubMed:10660625]

Drug created on June 13, 2005 07:24 / Updated on October 16, 2019 13:15