Furosemide

Summary

Furosemide is a loop diuretic used to treat hypertension and edema in congestive heart failure, liver cirrhosis, renal disease, and hypertension.

Brand Names

Lasix

Generic Name
Furosemide
DrugBank Accession Number
DB00695
Background

Furosemide is a potent loop diuretic that acts on the kidneys to ultimately increase water loss from the body. It is an anthranilic acid derivative.9 Furosemide is used for edema secondary to various clinical conditions, such as congestive heart failure exacerbation, liver failure, renal failure, and high blood pressure.10 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 action and has been used safely and effectively in both pediatric and adult patients.1 The use of furosemide is particularly beneficial in clinical settings that require a drug with a higher diuretic potential. In addition to oral formulations, the solution for intravenous and intramuscular administration is also available, which is typically limited to patients who are unable to take oral medication or for patients in emergency clinical situations.9

Type
Small Molecule
Groups
Approved, Vet approved
Structure

Thumb

Image

Weight
Average: 330.744
Monoisotopic: 330.007719869
Chemical Formula
C12H11ClN2O5S
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
Indication

Furosemide is indicated for the treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome, in adults and pediatric patients.9

Oral furosemide is indicated alone for the management of mild to moderate hypertension or severe hypertension in combination with other antihypertensive medications.12

Intravenous furosemide is indicated as adjunctive therapy in acute pulmonary edema when a rapid onset of diuresis is desired.9

Pharmacology

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Associated Conditions
  • Acute Pulmonary Edema
  • Ascites
  • Body Fluid Retention
  • Edema
  • High Blood Pressure (Hypertension)
  • Mild to Moderate Hypertension
Contraindications & Blackbox Warnings

Contraindications

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Pharmacodynamics

Furosemide manages hypertension and edema associated with congestive heart failure, cirrhosis, and renal disease, including the nephrotic syndrome. Furosemide is a potent loop diuretic that 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.9 It works directly acts on the cells of the nephron and indirectly modifies the content of the renal filtrate.8 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.4,9

Following oral administration, the onset of the diuretic effect is about 1 and 1.5 hours 9, and the peak effect is reached within the first 2 hours.10 The duration of effect following oral administration is about 4-6 hours but may last up to 8 hours.12 Following intravenous administration, the onset of effect is within 5 minutes, and the peak effect is reached within 30 minutes. The duration of action following intravenous administration is approximately 2 hours. Following intramuscular administration, the onset of action is somewhat delayed.9

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 diuretic effect is achieved through the competitive inhibition of sodium-potassium-chloride cotransporters (NKCC2) expressed along these tubules in the nephron, preventing the transport of sodium ions from the lumenal side into the basolateral side for reabsorption. This inhibition results in increased excretion of water along with sodium, chloride, magnesium, calcium, hydrogen, and potassium ions.10 As with other loop diuretics, furosemide decreases the excretion of uric acid.8

Furosemide exerts direct vasodilatory effects, which results in its therapeutic effectiveness in the treatment of acute pulmonary edema. Vasodilation leads to reduced responsiveness to vasoconstrictors, such as angiotensin II and noradrenaline, and decreased production of endogenous natriuretic hormones with vasoconstricting properties. It also leads to increased production of prostaglandins with vasodilating properties. Furosemide may also open potassium channels in resistance arteries.8 The main mechanism of action of furosemide is independent of its inhibitory effect on carbonic anhydrase and aldosterone.9

Target Actions Organism
ASolute carrier family 12 member 1

inhibitor

Humans
NCarbonic anhydrase 2

inhibitor

Humans
UG-protein coupled receptor 35

agonist

Humans
Absorption

Following oral administration, furosemide is absorbed from the gastrointestinal tract.12 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.9

Volume of distribution

The volume of distribution following intravenous administration of 40 mg furosemide were 0.181 L/kg in healthy subjects and 0.140 L/kg in patients with heart failure.6

Protein binding

Plasma concentrations ranging from 1 to 400 mcg/mL are about 91-99% bound in healthy individuals. The unbound fraction is about 2.3-4.1% at therapeutic concentrations.12 Furosemide mainly binds to serum albumin.9

Metabolism

The metabolism of furosemide occurs mainly in the kidneys and 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, which is pharmacologically active, and saluamine (CSA) or 4-chloro-5-sulfamoylanthranilic acid.2

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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 half-life from the dose of 40 mg furosemide was 4 hours following oral administration and 4.5 hours following intravenous administration. The terminal half-life of furosemide is approximately 2 hours following parenteral administration.9 The terminal half-life may be increased up to 24 hours in patients with severe renal failure.12

Clearance

Following intravenous administration of 400 mg furosemide, the plasma clearance was 1.23 mL/kg/min in patients with heart failure and 2.34 mL/kg/min in healthy subjects, respectively.6

Adverse Effects

Adverseeffects

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Toxicity

Clinical consequences from overdose depend on the extent of electrolyte and fluid loss and include dehydration, blood volume reduction, hypotension, electrolyte imbalance, hypokalemia, hypochloremic alkalosis,9 hemoconcentration, cardiac arrhythmias (including A-V block and ventricular fibrillation).12 Symptoms of overdose include acute renal failure, thrombosis, delirious states, flaccid paralysis, apathy and confusion. In cirrhotic patients, overdosage might precipitate hepatic coma.12

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.11

Pathways
Pathway Category
Furosemide Action Pathway Drug action
Pharmacogenomic Effects/ADRs
Not Available
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.

  • Approved
  • Vet approved
  • Nutraceutical
  • Illicit
  • Withdrawn
  • Investigational
  • Experimental
  • All Drugs
Drug Interaction

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Abacavir Furosemide may increase the excretion rate of Abacavir which could result in a lower serum level and potentially a reduction in efficacy.
Acamprosate The excretion of Acamprosate can be decreased when combined with Furosemide.
Acarbose The therapeutic efficacy of Acarbose can be decreased when used in combination with Furosemide.
Acebutolol Furosemide may increase the hypotensive activities of Acebutolol.
Aceclofenac The therapeutic efficacy of Furosemide can be decreased when used in combination with Aceclofenac.
Acemetacin Furosemide may increase the nephrotoxic activities of Acemetacin.
Acetaminophen Furosemide may increase the excretion rate of Acetaminophen which could result in a lower serum level and potentially a reduction in efficacy.
Acetazolamide Acetazolamide may increase the excretion rate of Furosemide which could result in a lower serum level and potentially a reduction in efficacy.
Acetohexamide The therapeutic efficacy of Acetohexamide can be decreased when used in combination with Furosemide.
Acetyldigitoxin The risk or severity of adverse effects can be increased when Furosemide is combined with Acetyldigitoxin.
Food Interactions
  • Avoid excessive or chronic alcohol consumption. Alcohol increases the risk of orthostatic hypotension.
  • Avoid natural licorice. Avoid licorice in large amounts, as it may lead to hypokalemia.
  • Increase consumption of potassium-rich foods. This medication may cause potassium depletion. Foods containing potassium include bananas and orange juice.

Products2

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Product Ingredients
Ingredient UNII CAS InChI Key
Furosemide sodium 101EM454S7 41733-55-5 DLFCAVBMDSKMEY-UHFFFAOYSA-M
Product Images
International/Other Brands
Diurapid (Mibe Jena) / Diurin (Mylan) / Diurmessel (Biomep) / Eutensin (Sanofi) / Frumex / Frusenex / Frusol (Rosemont) / Furo-Puren (Actavis) / Seguril (Sanofi)
Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Fuosemide Tablet 40 mg/1 Oral NCS HealthCare of KY, Inc dba Vangard Labs 1983-11-10 2022-10-31 US flag
Furosemide Tablet 40 mg/1 Oral REMEDYREPACK INC. 2017-10-27 2020-05-06 US flag
Furosemide Injection 10 mg/1mL Intravenous American Regent 1990-09-30 2017-01-18 US flag
Furosemide Injection, solution 10 mg/1mL Intramuscular; Intravenous HF Acquisition Co LLC, DBA HealthFirst 2018-09-14 Not applicable US flag
Furosemide Tablet 20 mg/1 Oral Vintage Pharmaceuticals, LLC 2007-09-13 2007-09-13 US flag
Furosemide Tablet 20 mg/1 Oral bryant ranch prepack 1983-11-10 2018-02-28 US flag
Furosemide Tablet 80 mg/1 Oral Ncs Health Care Of Ky, Inc Dba Vangard Labs 1981-10-19 Not applicable US flag 00615 157120210427 24843 1iwtn0r
Furosemide Injection, solution 10 mg/1mL Intramuscular; Intravenous HF Acquisition Co LLC, DBA HealthFirst 2021-06-28 Not applicable US flag
Furosemide Tablet 40 mg/1 Oral Mylan Pharmaceuticals Inc. 1981-08-27 Not applicable US flag 0378 021620180913 8702 rl1iv1
Furosemide Tablet 20 mg/1 Oral Cardinal Health 1983-11-10 2010-04-30 US flag
Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image
Apo Furosemide Tab 20mg Tablet 20 mg Oral Apotex Corporation 1977-12-31 Not applicable Canada flag
Apo Furosemide Tab 40mg Tablet 40 mg Oral Apotex Corporation 1976-12-31 Not applicable Canada flag
Apo Furosemide Tab 80mg Tablet 80 mg Oral Apotex Corporation 1986-12-31 Not applicable Canada flag
Ava-furosemide Tablet 80 mg Oral Avanstra Inc 2011-08-11 2014-08-21 Canada flag
Ava-furosemide Tablet 40 mg Oral Avanstra Inc 2011-08-11 2014-08-21 Canada flag
Ava-furosemide Tablet 20 mg Oral Avanstra Inc 2011-08-11 2014-08-21 Canada flag
Bio-furosemide Tablet 40 mg Oral Biomed Pharma 2003-04-11 Not applicable Canada flag
Bio-furosemide Tablet 20 mg Oral Biomed Pharma 2003-04-11 Not applicable Canada flag
Dom-furosemide Tablet 40 mg Oral Biomed Pharma 2003-10-14 2013-08-02 Canada flag
Dom-furosemide Tablet 20 mg Oral Biomed Pharma 2003-10-14 2013-08-02 Canada flag
Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
Active-Medicated specimen collection kit Furosemide (20 mg/1) + Benzalkonium chloride (0.0013 g/1mL) Kit Oral; Topical N.O.R.T.H., Inc. 2013-10-31 Not applicable US flag
Diascreen 12-Panel Medicated Collection System Furosemide (20 mg/1) + Benzalkonium chloride (0.13 g/100g) Kit Oral; Topical It3 Medical Llc 2016-07-27 Not applicable US flag
Diuscreen Medicated Collection Kit Furosemide (20 mg/1) + Benzalkonium chloride (0.0013 g/1mL) Kit Oral; Topical Maveron Health, LLC. 2015-06-01 2016-10-28 US flag
Diuscreen Multi-Drug Medicated Test Kit Furosemide (20 mg/1) + Benzalkonium chloride (0.0013 g/1mL) Kit Oral; Topical Maveron Health, LLC. 2015-06-01 2016-10-28 US flag
Rx-Specimen Collection Kit Furosemide (20 mg/1) + Benzalkonium chloride (0.0013 g/1mL) Kit Oral; Topical Mas Management Group Inc. 2015-07-23 Not applicable US flag
SEMİTONE 100/20 MG FILM TABLET, 10 ADET Furosemide (20 mg) + Spironolactone (100 mg) Tablet, film coated Oral World Medicine Ilac San. Ve Tic. a.s. 2020-08-14 Not applicable Turkey flag
SEMİTONE 100/20 MG FILM TABLET, 20 ADET Furosemide (20 mg) + Spironolactone (100 mg) Tablet, film coated Oral World Medicine Ilac San. Ve Tic. a.s. 2020-08-14 Not applicable Turkey flag
SEMİTONE 100/20 MG FILM TABLET, 30 ADET Furosemide (20 mg) + Spironolactone (100 mg) Tablet, film coated Oral World Medicine Ilac San. Ve Tic. a.s. 2020-08-14 Not applicable Turkey flag
SEMİTONE 50/20 MG FILM TABLET, 10 ADET Furosemide (20 mg) + Spironolactone (50 mg) Tablet, film coated Oral World Medicine Ilac San. Ve Tic. a.s. 2020-08-14 Not applicable Turkey flag
SEMİTONE 50/20 MG FILM TABLET, 20 ADET Furosemide (20 mg) + Spironolactone (50 mg) Tablet, film coated Oral World Medicine Ilac San. Ve Tic. a.s. 2020-08-14 Not applicable Turkey flag
Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image
Furosemide Furosemide (20 mg/1) Tablet Oral Remedy Repack 2010-11-01 2011-02-10 US flag
Specimen Collection Kit Furosemide (20 mg/1) + Benzalkonium chloride (0.13 mg/1mL) Kit Oral Alvix Laboratories, LLC 2015-04-21 2019-01-28 US flag
ATC Codes
C03EB01 — Furosemide and potassium-sparing agents
  • C03EB — High-ceiling diuretics and potassium-sparing agents
  • C03E — DIURETICS AND POTASSIUM-SPARING AGENTS IN COMBINATION
  • C03 — DIURETICS
  • C — CARDIOVASCULAR SYSTEM
C03CA01 — Furosemide
  • C03CA — Sulfonamides, plain
  • C03C — HIGH-CEILING DIURETICS
  • C03 — DIURETICS
  • C — CARDIOVASCULAR SYSTEM
G01AE10 — Combinations of sulfonamides
  • G01AE — Sulfonamides
  • G01A — ANTIINFECTIVES AND ANTISEPTICS, EXCL. COMBINATIONS WITH CORTICOSTEROIDS
  • G01 — GYNECOLOGICAL ANTIINFECTIVES AND ANTISEPTICS
  • G — GENITO URINARY SYSTEM AND SEX HORMONES
C03CB01 — Furosemide and potassium
  • C03CB — Sulfonamides and potassium in combination
  • C03C — HIGH-CEILING DIURETICS
  • C03 — DIURETICS
  • C — CARDIOVASCULAR SYSTEM
Drug Categories
  • Acids, Carbocyclic
  • Amides
  • Amines
  • Aminobenzoates
  • Aniline Compounds
  • Antihypertensive Agents
  • Antihypertensive Agents Indicated for Hypertension
  • Benzene Derivatives
  • Benzoates
  • Cardiovascular Agents
  • Diuretics
  • Drugs causing inadvertant photosensitivity
  • Drugs that are Mainly Renally Excreted
  • High-Ceiling Diuretics
  • High-Ceiling Diuretics and Potassium-Sparing Agents
  • Hyperglycemia-Associated Agents
  • Hypotensive Agents
  • Increased Diuresis at Loop of Henle
  • Membrane Transport Modulators
  • Natriuretic Agents
  • Nephrotoxic agents
  • Non Potassium Sparing Diuretics
  • OAT1/SLC22A6 inhibitors
  • OAT3/SLC22A8 Inhibitors
  • Ototoxic agents
  • Photosensitizing Agents
  • Sodium Potassium Chloride Symporter Inhibitors
  • Sulfanilamides
  • Sulfonamides
  • Sulfones
  • Sulfur Compounds
  • Thyroxine-binding globulin substrates
  • UGT1A1 Substrates
Chemical TaxonomyProvided by Classyfire
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 / Organosulfonamides / Aryl chlorides / Furans / Vinylogous amides / Aminosulfonyl compounds / Heteroaromatic compounds / Amino acids / Monocarboxylic acids and derivatives / Carboxylic acids / Oxacyclic compounds / Organic oxides / Organochlorides / Organooxygen compounds / Organopnictogen compounds / Hydrocarbon derivatives show 15 more
Substituents
4-halobenzoic acid / 4-halobenzoic acid or derivatives / Amine / Amino acid / Amino acid or derivatives / Aminobenzenesulfonamide / Aminobenzoic acid / Aminobenzoic acid or derivatives / Aminosulfonyl compound / Aniline or substituted anilines / Aralkylamine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Benzenesulfonyl group / Benzoic acid / Benzoic acid or derivatives / Benzoyl / Carboxylic acid / Carboxylic acid derivative / Chlorobenzene / Furan / Halobenzene / Halobenzoic acid / Halobenzoic acid or derivatives / Heteroaromatic compound / Hydrocarbon derivative / Monocarboxylic acid or derivatives / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organic sulfonic acid or derivatives / Organochloride / Organohalogen compound / Organoheterocyclic compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Organosulfonic acid amide / Organosulfonic acid or derivatives / Organosulfur compound / Oxacycle / Phenylalkylamine / Secondary aliphatic/aromatic amine / Secondary amine / Sulfonyl / Vinylogous amide show 37 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
sulfonamide, furans, chlorobenzoic acid (CHEBI:47426)
Affected organisms
  • Humans and other mammals
UNII
7LXU5N7ZO5
CAS number
54-31-9
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

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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  6. Andreasen F, Mikkelsen E: Distribution, elimination and effect of furosemide in normal subjects and in patients with heart failure. Eur J Clin Pharmacol. 1977 Aug 17;12(1):15-22. doi: 10.1007/bf00561400. [Article]
  7. Perez J, Sitar DS, Ogilvie RI: Biotransformation of furosemide in patients with acute pulmonary edema. Drug Metab Dispos. 1979 Nov-Dec;7(6):383-7. [Article]
  8. 28. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 352-354). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
  9. Furosemide - FDA Label [Link]
  10. Furosemide - StatPearls - NCBI Bookshelf [Link]
  11. Furosemide SAFETY DATA SHEET - Cayman Chemical [Link]
  12. Lasix Oral (furosemide) Product Monograph [Link]
Human Metabolome Database
HMDB0001933
KEGG Drug
D00331
KEGG Compound
C07017
PubChem Compound
3440
PubChem Substance
46506779
ChemSpider
3322
BindingDB
25902
RxNav
4603
ChEBI
47426
ChEMBL
CHEMBL35
ZINC
ZINC000000035804
Therapeutic Targets Database
DAP000043
PharmGKB
PA449719
PDBe Ligand
FUN
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Furosemide
PDB Entries
1z9y / 2xn5 / 3rf4 / 6de9 / 6sg0
Clinical Trials
Phase Status Purpose Conditions Count
4 Completed Other Cystoscopy 1
4 Completed Prevention Congestive Heart Failure (CHF) / Edema / High Blood Pressure (Hypertension) / Hypotension 1
4 Completed Prevention Diabetic Nephropathy 1
4 Completed Prevention High Blood Pressure (Hypertension) 1
4 Completed Treatment Acute Decompensated Heart Failure (ADHF) 1
4 Completed Treatment Acute Heart Failure (AHF) 1
4 Completed Treatment Ascites / Cirrhosis of the Liver 2
4 Completed Treatment Chronic Heart Failure (CHF) / Congestive Heart Failure (CHF) 1
4 Completed Treatment Chronic Kidney Disease (CKD) 1
4 Completed Treatment Colorectal Disorders 1
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
Form Route Strength
Kit Oral; Topical
Tablet Oral 20 mg
Tablet Oral 40 mg
Solution 10 mg/1ml
Tablet Oral
Tablet Oral
Tablet Oral 40.00 mg
Tablet Oral 250 MG
Injection, solution, concentrate Parenteral 250 mg
Injection, solution Intravenous 40 mg/4ml
Capsule, extended release Oral 120 MG
Tablet Oral 125 MG
Capsule, extended release Oral 30 MG
Injection, solution Parenteral 40 MG/4ML
Capsule, extended release Oral 60 MG
Solution Parenteral 10 MG/ML
Solution Parenteral 250 MG/25ML
Solution Intravenous 20 mg
Solution Parenteral 20 mg
Tablet, film coated Oral 40 mg
Capsule, coated Oral
Injection Intramuscular; Intravascular 10 mg/1mL
Injection Intramuscular; Intravenous 10 mg/2mL
Injection Intramuscular; Intravenous 10 mg/1mL
Injection Intramuscular; Intravenous 100 mg/10mL
Injection Intramuscular; Intravenous 20 mg/2mL
Injection Intramuscular; Intravenous 40 mg/4mL
Injection Intravenous 10 mg/1mL
Injection, solution Intramuscular; Intravenous
Injection, solution Intramuscular; Intravenous 10 mg/1mL
Injection, solution Intramuscular; Intravenous 100 mg/10mL
Injection, solution Intramuscular; Intravenous 20 mg/2mL
Injection, solution Intramuscular; Intravenous 40 mg/4mL
Injection, solution Intravenous 10 mg/1mL
Solution Oral 10 mg/1mL
Solution Oral 40 mg/4mL
Solution Oral 40 mg/5mL
Tablet Oral 20 mg/1
Tablet Oral 40 mg/1
Tablet Oral 80 mg/1
Tablet, film coated Oral
Injection, solution Parenteral 10 MG/ML
Injection, solution 10 MG/ML
Injection, solution Intravenous 20 mg/2ml
Injection, solution
Liquid Intramuscular; Intravenous 10 mg / mL
Solution Intramuscular; Intravenous 10 mg / mL
Solution Intramuscular; Intravenous 20 mg / 2 mL
Injection, solution 20 MG/2ML
Tablet Oral 25 MG
Solution Intravenous 250 mg / 25 mL
Liquid Intravenous 250 mg / 25 mL
Solution Intravenous 10 mg / mL
Tablet Oral 80 mg
Injection, solution Intramuscular; Intravenous 50 mg/5mL
Injection Intramuscular; Intravenous 10 mg/ml
Injection Intramuscular; Intravenous
Drug delivery system Topical 20 mg
Capsule, gelatin coated Oral
Capsule Oral
Injection, solution 250 MG/25ML
Solution Oral 10 MG/ML
Injection, solution, concentrate Intravenous 250 mg/25mL
Solution Parenteral 250 MG
Tablet Oral 80 mg / tab
Injection, solution Parenteral 20 MG/2ML
Liquid Oral 10 mg / mL
Solution Oral 10 mg / mL
Liquid Intramuscular; Intravenous 20 mg / 2 mL
Capsule Oral 30 mg
Capsule Oral 60 mg
Liquid Intravenous 10 mg / mL
Tablet, film coated Oral
Kit Oral
Injection, solution Parenteral
Injection
Solution Intramuscular; Intravenous
Kit Not applicable; Oral; Topical
Solution Intramuscular; Intravenous 20 mg
Solution Oral
Tablet, coated Oral 40 mg
Tablet Oral 500 mg
Injection, solution 10 mg/1ml
Prices
Unit description Cost Unit
Hydro 40 40% Foam 150 gm Can 182.52USD can
Hydro 40 40% Foam 70 gm Can 148.99USD can
Furosemide 10 mg/ml Solution 60ml Bottle 17.99USD bottle
Furosemide 10 mg/ml Solution 120ml Bottle 15.98USD bottle
Furosemide powder 3.51USD g
Lasix Special 500 mg Tablet 3.25USD tablet
Urex 1 gm tablet 2.47USD tablet
Furosemide 10 mg/ml cartrg 1.45USD ml
Lasix 80 mg tablet 1.0USD tablet
Furosemide 10 mg/ml Solution 0.9USD ml
Furosemide 10 mg/ml 0.75USD ml
Lasix 40 mg tablet 0.53USD tablet
Furosemide 80 mg tablet 0.45USD tablet
Lasix 20 mg tablet 0.42USD tablet
Lasix 10 mg/ml Solution 0.3USD ml
CVS Pharmacy diuretic 50 mg softgel 0.17USD softgel capsule
Furosemide 40 mg tablet 0.16USD tablet
Furosemide 20 mg tablet 0.14USD tablet
Apo-Furosemide 80 mg Tablet 0.13USD tablet
Novo-Semide 80 mg Tablet 0.13USD tablet
Nat herbal diuretic tablet sa 0.1USD tablet
Apo-Furosemide 40 mg Tablet 0.07USD tablet
Natural herbal diuretic tablet 0.07USD tablet
Novo-Semide 40 mg Tablet 0.07USD tablet
Apo-Furosemide 20 mg Tablet 0.05USD tablet
Novo-Semide 20 mg Tablet 0.05USD tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents
Not Available
State
Solid
Experimental Properties
Property Value Source
melting point (°C) 220 MSDS
water solubility 73.1 mg/L (at 30 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP 2.03 SANGSTER (1993)
logS -3.66 ADME Research, USCD
Caco2 permeability -6.5 ADME Research, USCD
Predicted Properties
Property Value Source
Water Solubility 0.118 mg/mL ALOGPS
logP 2.71 ALOGPS
logP 1.75 ChemAxon
logS -3.4 ALOGPS
pKa (Strongest Acidic) 4.25 ChemAxon
pKa (Strongest Basic) -1.5 ChemAxon
Physiological Charge -1 ChemAxon
Hydrogen Acceptor Count 5 ChemAxon
Hydrogen Donor Count 3 ChemAxon
Polar Surface Area 122.63 Å2 ChemAxon
Rotatable Bond Count 5 ChemAxon
Refractivity 77.47 m3·mol-1 ChemAxon
Polarizability 30.55 Å3 ChemAxon
Number of Rings 2 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 + 0.9155
Blood Brain Barrier - 0.8833
Caco-2 permeable - 0.6436
P-glycoprotein substrate Non-substrate 0.8775
P-glycoprotein inhibitor I Non-inhibitor 0.9272
P-glycoprotein inhibitor II Non-inhibitor 0.8382
Renal organic cation transporter Non-inhibitor 0.924
CYP450 2C9 substrate Non-substrate 0.6878
CYP450 2D6 substrate Non-substrate 0.8351
CYP450 3A4 substrate Non-substrate 0.6789
CYP450 1A2 substrate Non-inhibitor 0.9045
CYP450 2C9 inhibitor Non-inhibitor 0.907
CYP450 2D6 inhibitor Non-inhibitor 0.9231
CYP450 2C19 inhibitor Non-inhibitor 0.9025
CYP450 3A4 inhibitor Non-inhibitor 0.9602
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6885
Ames test Non AMES toxic 0.9132
Carcinogenicity Non-carcinogens 0.6469
Biodegradation Not ready biodegradable 0.9881
Rat acute toxicity 2.1362 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9342
hERG inhibition (predictor II) Non-inhibitor 0.8525

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

Mass Spec (NIST)
Not Available
Spectra
Spectrum Spectrum Type Splash Key
Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available
MS/MS Spectrum - Quattro_QQQ 10V, N/A LC-MS/MS splash10-03dr-0090000000-da505a3f09285d049f34
MS/MS Spectrum - Quattro_QQQ 25V, N/A LC-MS/MS splash10-0f89-2190000000-53c91100e89c81f0fa30
MS/MS Spectrum - Quattro_QQQ 40V, N/A LC-MS/MS splash10-01ox-9660000000-83d8486cbca0dd3487c9
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 , negative LC-MS/MS splash10-000i-0090000000-f3a3dcb92cfcdff9f7dc
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-004i-0019000000-946089b12d2ab6fd05a4
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-000i-0090000000-04af1dec204d462d4bc4
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-0udi-1090000000-1af70d23e1a0ebaa0878
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-004i-9770000000-0c5cd578b5b69a1a61d4
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-004i-9800000000-3303b20f9b23e24ae312
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-004i-9400000000-23cfec716ac8fbcb092f
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-004i-0019000000-e73aa1d969ab4255732b
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-000i-0090000000-33053544119c01ac6b45
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-0udi-1090000000-7029ab63efa73a3ff88d
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-004i-9670000000-4bad8928bbcfc85f431f
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-004i-9800000000-2193e38e314f2b18be26
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-004i-9600000000-e703f7ab6221182df156
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-000i-0090000000-f3645e993869ff3886ba
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-000i-0090000000-18400153a811f7100a2f
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-0f79-0090000000-7e491b92dab050fb81c0
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-000i-0090000000-8e41d38fe799d96230a6
LC-MS/MS Spectrum - LC-ESI-ITFT , negative LC-MS/MS splash10-000i-0090000000-cfec4a54171c58245919
LC-MS/MS Spectrum - LC-ESI-QFT , negative LC-MS/MS splash10-0ug0-0193000000-b55039ca13cbc3acd9a8
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-0udi-0290000000-1f1017fe4370d9541f6d
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-001i-9110000000-505f1e781d384073f688
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-001j-9000000000-cd886e0521fb4d1bdc82
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-000t-9000000000-8a69e99643ee37bc1883
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-000t-9000000000-f7ac3c9eea39ed725cfc
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-000t-9000000000-8a294fd51a34073aa4a1
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-0002-9000000000-b16e204dec9ae7938d40
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-0f8a-9220000000-3bde836fe7e67c9b8755
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-000t-9000000000-9025c2261c96ca3aa551
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-000t-9000000000-8d05f828403d0fe7cac4
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-0002-9000000000-3cd4f8015eb5fafacacb
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-0002-9000000000-34937031271e62c39c1f
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-0002-9000000000-40e9966d335f71aedb96
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-0udi-0290000000-586707fb0116e8b61643
LC-MS/MS Spectrum - LC-ESI-QFT , positive LC-MS/MS splash10-001i-9000000000-f6727b05eb8ee02a6e7c
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-00di-0090000000-51662bec1d461d0f0a5a
LC-MS/MS Spectrum - LC-ESI-ITFT , positive LC-MS/MS splash10-00di-0090000000-8eea44e0dd27bb59939d
1H NMR Spectrum 1D NMR Not Applicable
[1H,13C] 2D NMR Spectrum 2D NMR Not Applicable

Targets

Drugtargets2

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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. [Article]
  2. Davies DL, Wilson GM: Diuretics: mechanism of action and clinical application. Drugs. 1975;9(3):178-226. [Article]
  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. [Article]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
  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. [Article]
  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. [Article]
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. [Article]
  2. Supuran CT: Diuretics: from classical carbonic anhydrase inhibitors to novel applications of the sulfonamides. Curr Pharm Des. 2008;14(7):641-8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action

Unknown

Actions

Agonist

General Function
G-protein coupled receptor activity
Specific Function
Acts as a receptor for kynurenic acid, an intermediate in the tryptophan metabolic pathway. The activity of this receptor is mediated by G-proteins that elicit calcium mobilization and inositol pho...
Gene Name
GPR35
Uniprot ID
Q9HC97
Uniprot Name
G-protein coupled receptor 35
Molecular Weight
34071.89 Da
References
  1. Yang Y, Fu A, Wu X, Reagan JD: GPR35 is a target of the loop diuretic drugs bumetanide and furosemide. Pharmacology. 2012;89(1-2):13-7. doi: 10.1159/000335127. Epub 2012 Jan 10. [Article]
  2. Divorty N, Milligan G, Graham D, Nicklin SA: The Orphan Receptor GPR35 Contributes to Angiotensin II-Induced Hypertension and Cardiac Dysfunction in Mice. Am J Hypertens. 2018 Aug 3;31(9):1049-1058. doi: 10.1093/ajh/hpy073. [Article]
  3. Divorty N, Mackenzie AE, Nicklin SA, Milligan G: G protein-coupled receptor 35: an emerging target in inflammatory and cardiovascular disease. Front Pharmacol. 2015 Mar 10;6:41. doi: 10.3389/fphar.2015.00041. eCollection 2015. [Article]

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. [Article]
  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. [Article]
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. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action

No

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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
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. [Article]
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. [Article]
  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. [Article]
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. [Article]
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. [Article]
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. [Article]

Drug created at June 13, 2005 13:24 / Updated at December 21, 2021 15:24