0% found this document useful (0 votes)
152 views51 pages

Furosemide: A Comprehensive Guide

Furosemide is a loop diuretic used to treat hypertension and edema associated with congestive heart failure, cirrhosis, and renal disease. It works by inhibiting sodium and chloride reabsorption in the kidneys, increasing urine output. Common adverse effects include dehydration, electrolyte imbalances, and arrhythmias.

Uploaded by

Salihu Ibrahim
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd
0% found this document useful (0 votes)
152 views51 pages

Furosemide: A Comprehensive Guide

Furosemide is a loop diuretic used to treat hypertension and edema associated with congestive heart failure, cirrhosis, and renal disease. It works by inhibiting sodium and chloride reabsorption in the kidneys, increasing urine output. Common adverse effects include dehydration, electrolyte imbalances, and arrhythmias.

Uploaded by

Salihu Ibrahim
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd
You are on page 1/ 51

Read More!

NAV

Identification

Pharmacology

Indication

Associated Conditions

Contraindications & Blackbox Warnings

Pharmacodynamics

Mechanism of action

Absorption

Volume of distribution

Protein binding

Metabolism

Route of elimination

Half-life

Clearance

Adverse Effects

Toxicity

Pathways

Pharmacogenomic Effects/ADRs

Interactions

Products

Categories

Chemical Identifiers
References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Targets (3)

Enzymes (2)

Carriers (2)

Transporters (6)

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

Furoscix, 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

Weight

Average: 330.744

Monoisotopic: 330.007719869

Chemical Formula

C12H11ClN2O5S

Synonyms

Frusemide

Furosemid

Furosemida

Furosemide

Furosemidu

Furosemidum

External IDs

LB-502

NSC-269420

PHARMACOLOGY

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

Subcutaneous furosemide is indicated for the treatment of congestion due to fluid overload in adults
with NYHA Class II/III chronic heart failure. This drug formulation is not indicated for emergency
situations or in patients with acute pulmonary edema.13

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

Associated Conditions

Acute Pulmonary Edema

Ascites

Body Fluid Retention

Edema

Hypertension

Mild to Moderate Hypertension

Chest congestion

Contraindications & Blackbox Warnings

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

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
Hover over products below to view reaction partners

Furosemide

4-chloro-5-sulfamoylanthranilic acid

Furosemide glucuronide

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

Improve decision support & research outcomes with our structured adverse effects data.

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

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.

APPROVED

VET APPROVED

NUTRACEUTICAL

ILLICIT

WITHDRAWN

INVESTIGATIONAL

EXPERIMENTAL

ALL DRUGS

DRUG INTERACTION

INTEGRATE DRUG-DRUG INTERACTIONS IN YOUR SOFTWARE

Abacavir Furosemide may increase the excretion rate of Abacavir which could result in a lower
serum level and potentially a reduction in efficacy.
Abaloparatide The risk or severity of adverse effects can be increased when Furosemide is combined
with Abaloparatide.

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.

AcetaminophenFurosemide 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.

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.

PRODUCTS

Access drug product information from over 10 global regions.

Product Ingredients

INGREDIENT

UNII

CAS

INCHI KEY

Furosemide sodium
41733-55-5

Product Images

Previous

Next

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

Fuosemide Tablet 40 mg/1 Oral NCS HealthCare of KY, Inc dba Vangard Labs 1983-
11-10 2022-10-31 US flag

Furoscix Injection 8 mg/1mL Subcutaneous scPharmaceuticals Inc. 2022-11-14


Not applicable US flag

Furosemide Tablet 40 mg/1 Oral Cardinal Health 2010-10-12 2030-01-31 US flag

Furosemide Tablet 40 mg/1 Oral Teva Pharmaceuticals USA, Inc. 1983-11-30 2018-
02-28 US flag

Furosemide Tablet 40 mg/1 Oral Aphena Pharma Solutions - Tennessee, LLC 1983-
11-10 Not applicable US flag

Furosemide Tablet 20 mg/1 Oral Nucare Pharmaceuticals,inc. 1981-10-19 2019-


12-31 US flag

Furosemide Tablet 80 mg/1 Oral Vintage Pharmaceuticals, LLC 2007-09-13 2007-


09-13 US flag

Furosemide Injection 10 mg/1mL Intravenous American Regent 1990-09-30


2017-01-18 US flag

Furosemide Tablet 20 mg/1 Oral Avera McKennan Hospital 2015-06-09 2017-


05-24 US flag

Furosemide Tablet 40 mg/1 Oral Clinical Solutions Wholsesale 1983-11-10 2017-


06-23 US flag
Generic Prescription Products

NAME DOSAGE STRENGTH ROUTE LABELLER MARKETING START MARKETING


END

Apo-furosemide Tablet 80 mg Oral Apotex Corporation 1986-12-31 Not applicable


Canada flag

Apo-furosemide Tablet 20 mg Oral Apotex Corporation 1977-12-31 Not applicable


Canada flag

Apo-furosemide Tablet 40 mg Oral Apotex Corporation 1976-12-31 Not applicable


Canada flag

Ava-furosemideTablet 20 mg Oral Avanstra Inc 2011-08-11 2014-08-21 Canada flag

Ava-furosemideTablet 80 mg Oral Avanstra Inc 2011-08-11 2014-08-21 Canada flag

Ava-furosemideTablet 40 mg Oral Avanstra Inc 2011-08-11 2014-08-21 Canada flag

Bio-furosemide Tablet 20 mg Oral Biomed Pharma2003-04-11 2022-07-19 Canada flag

Bio-furosemide Tablet 40 mg Oral Biomed Pharma2003-04-11 2022-07-19 Canada flag

Dom-furosemide Tablet 20 mg Oral Biomed Pharma2003-10-14 2013-08-02 Canada


flag

Dom-furosemide Tablet 40 mg Oral Biomed Pharma2003-10-14 2013-08-02 Canada


flag

Mixture Products

NAME INGREDIENTS DOSAGE ROUTE LABELLER MARKETING START MARKETING


END

14-Panel Toxicology Medicated Collection System Furosemide (20 mg/1) + Benzalkonium chloride
(0.13 g/100g) Kit; Liquid; Tablet Oral; Topical Morkin Companies, Inc DBA Medical
Technologies, Inc 2022-01-26 Not applicable US flag

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

Furo-Spirobene - Filmtabletten Furosemide (20 mg) + Spironolactone (50 mg) Tablet, film coated
Oral Teva B.V. 1997-04-07 Not applicable Austria flag

Furo-Spirobene forte - Filmtabletten Furosemide (20 mg) + Spironolactone (100 mg) Tablet, film
coated Oral Teva B.V. 1997-04-07 Not applicable Austria flag

Lasilacton 20 mg/100 mg Kapseln Furosemide (20 mg) + Spironolactone (100 mg) CapsuleOral
Sanofi Aventis Gmb H 1981-12-07 Not applicable Austria flag

Lasilacton 20 mg/50 mg KapselnFurosemide (20 mg) + Spironolactone (50 mg) CapsuleOral Sanofi
Aventis Gmb H 1981-12-07 Not applicable Austria flag

OSYROL 100 LASIX Furosemide (20 mg) + Spironolactone (100 mg) CapsuleOral 2012-
04-01 Not applicable Germany flag

Unapproved/Other Products

NAME INGREDIENTS DOSAGE ROUTE LABELLER MARKETING START MARKETING


END

Furosemide Furosemide (20 mg/1) Tablet Oral Remedy Repack2010-11-01 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

CATEGORIES

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 Taxonomy

Provided 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 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 show 37 more

Molecular Framework

Aromatic heteromonocyclic compounds

External Descriptors

sulfonamide, furans, chlorobenzoic acid (CHEBI:47426)

Affected organisms

Humans and other mammals

CHEMICAL IDENTIFIERS
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-yl)methyl]amino}-5-sulfamoylbenzoic acid

SMILES

NS(=O)(=O)C1=C(Cl)C=C(NCC2=CC=CO2)C(=C1)C(O)=O

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

Prandota J: Clinical pharmacology of furosemide in children: a supplement. Am J Ther. 2001 Jul-


Aug;8(4):275-89. [Article]

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]

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]
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]

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]

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]

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]

28. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 352-354). Edinburgh: Elsevier/Churchill
Livingstone. [ISBN:978-0-7020-3471-8]

FDA Approved Drug Products: Furosemide Injection, for intravenous or intramuscular use [Link]

Furosemide - StatPearls - NCBI Bookshelf [Link]

Furosemide SAFETY DATA SHEET - Cayman Chemical [Link]

Lasix Oral (furosemide) Product Monograph [Link]

FDA Approved Drug Products: Furoscix (furosemide injection), for subcutaneous use (October 2022)
[Link]

External Links

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 / 7n3n / 7sfl / 8ste

CLINICAL TRIALS

Clinical Trials

PHASE STATUS PURPOSE CONDITIONS COUNT

4 Completed Other Cystoscopy 1

4 Completed Prevention Congestive Heart Failure (CHF) / Edema / Hypertension /


Hypotension 1

4 Completed Prevention Diabetic Nephropathy 1

4 Completed Prevention 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

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

FORM ROUTE STRENGTH

Kit Oral; Topical

Tablet Oral 20 mg

Solution Parenteral 20.000 mg

Tablet Oral 40 mg

Solution 10 mg/1ml

Tablet Oral 40.000 mg

Tablet Oral 20.000 MG

Tablet Oral

Tablet Oral

Solution Parenteral 20.00 mg

Tablet Oral 40.00 mg

Tablet Oral 250 MG

Injection, solution Intravenous 20 mg/2ml

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

Injection Subcutaneous 8 mg/1mL


Solution Parenteral 10 MG/ML

Injection, solution Parenteral 10 mg/ml

Solution Parenteral 250 MG/25ML

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 10 MG/ML

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

Injection, solution Intramuscular; Intravenous 50 mg/5mL

Injection Intramuscular; Intravenous 10 mg/ml

Injection Intramuscular; Intravenous

Drug delivery system Topical 20 mg

Solution Intramuscular 20.000 mg

Capsule, gelatin coated Oral

CapsuleOral

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

Solution Intravenous 20 mg

Injection, solution Parenteral 20 MG/2ML


Solution Oral 10 mg / mL

Liquid Oral 10 mg / mL

Liquid Intramuscular; Intravenous 20 mg / 2 mL

CapsuleOral 30 mg

CapsuleOral 60 mg

Liquid Intravenous 10 mg / mL

Injection 20 mg/2ml

Tablet Oral 20.01 mg

Tablet Oral 80 mg

Kit Oral

Tablet, film coated Oral

Injection, solution Parenteral

Solution Intravenous 20.000 mg

Kit; liquid; tablet Oral; Topical

Kit; swab; tablet Oral; Topical

Injection

Solution Intramuscular; Intravenous 20 mg/2ml

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

PATENT NUMBER PEDIATRIC EXTENSION APPROVED EXPIRES (ESTIMATED)

US11433044 No 2014-04-03 2034-04-03 US flag

US9884039 No 2018-02-06 2034-04-03 US flag

US10272064 No 2019-04-30 2034-04-03 US flag

PROPERTIES

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

Chemaxon

Hydrogen Donor Count

Chemaxon

Polar Surface Area

122.63 Å2
Chemaxon

Rotatable Bond Count

Chemaxon

Refractivity

77.47 m3·mol-1

Chemaxon

Polarizability

30.55 Å3

Chemaxon

Number of Rings

Chemaxon

Bioavailability

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

Blood Brain Barrier

Caco-2 permeable

P-glycoprotein substrate

Non-substrate

P-glycoprotein inhibitor I

Non-inhibitor

P-glycoprotein inhibitor II

Non-inhibitor

Renal organic cation transporter

Non-inhibitor

CYP450 2C9 substrate

Non-substrate

CYP450 2D6 substrate

Non-substrate
CYP450 3A4 substrate

Non-substrate

CYP450 1A2 substrate

Non-inhibitor

CYP450 2C9 inhibitor

Non-inhibitor

CYP450 2D6 inhibitor

Non-inhibitor

CYP450 2C19 inhibitor

Non-inhibitor

CYP450 3A4 inhibitor

Non-inhibitor

CYP450 inhibitory promiscuity

Low CYP Inhibitory Promiscuity

Ames test

Non AMES toxic

Carcinogenicity

Non-carcinogens

Biodegradation

Not ready biodegradable

Rat acute toxicity

2.1362 LD50, mol/kg

hERG inhibition (predictor I)

Weak inhibitor

hERG inhibition (predictor II)


Non-inhibitor

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

SPECTRA

Mass Spec (NIST)

Not Available

Spectra

SPECTRUM

SPECTRUM TYPE

SPLASH KEY

Predicted GC-MS Spectrum - GC-MS

MS/MS Spectrum - Quattro_QQQ 10V, N/A

MS/MS Spectrum - Quattro_QQQ 25V, N/A

MS/MS Spectrum - Quattro_QQQ 40V, N/A

Predicted MS/MS Spectrum - 10V, Positive (Annotated)

Predicted MS/MS Spectrum - 20V, Positive (Annotated)

Predicted MS/MS Spectrum - 40V, Positive (Annotated)

Predicted MS/MS Spectrum - 10V, Negative (Annotated)

Predicted MS/MS Spectrum - 20V, Negative (Annotated)

Predicted MS/MS Spectrum - 40V, Negative (Annotated)

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative


LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , negative

LC-MS/MS Spectrum - LC-ESI-QFT , negative

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive


LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-QFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

LC-MS/MS Spectrum - LC-ESI-ITFT , positive

1H NMR Spectrum

[1H,13C] 2D NMR Spectrum

TARGETS

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

1. Solute carrier family 12 member 1

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

Brater DC: Pharmacology of diuretics. Am J Med Sci. 2000 Jan;319(1):38-50. [Article]

Davies DL, Wilson GM: Diuretics: mechanism of action and clinical application. Drugs. 1975;9(3):178-226.
[Article]

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]

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
[Article]

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]

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]

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

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]

Supuran CT: Diuretics: from classical carbonic anhydrase inhibitors to novel applications of the
sulfonamides. Curr Pharm Des. 2008;14(7):641-8. [Article]

3. G-protein coupled receptor 35

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

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]

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]

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

1. 6-phosphogluconate dehydrogenase, decarboxylating

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

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]

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]

2. UDP-glucuronosyltransferase 1-1

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

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

1. Serum albumin
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

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]

FDA Approved Drug Products: Furosemide Injection, for intravenous or intramuscular use [Link]

2. Thyroxine-binding globulin
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

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]

CYTOMEL (liothyronine) FDA label [File]

TRANSPORTERS
1. Solute carrier family 22 member 6

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

InhibitorInducer

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

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]
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]

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]

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]

2. Solute carrier family 22 member 5

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

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]

3. Solute carrier family 22 member 8

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

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]

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]

4. Canalicular multispecific organic anion transporter 1

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

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]

5. Solute carrier organic anion transporter family member 2A1

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

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]

6. Solute carrier family 22 member 11

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

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 September 26, 2023 18:24

Stay up-to-date with the

latest from DrugBank!

Enter your email

About

About DrugBank Online

Blog

Wishart Research Group

License Agreement

Careers

Terms of Use

Privacy Policy

Support

Help Center

DrugBank Online FAQs

Contact Support

Downloads

Data LibraryBETA

Academic Downloads

Contact Sales
Website design by Educe Design & Innovation Inc.

// Start of HubSpot Embed Code // End of HubSpot Embed Code

You might also like