Furosemide: A Comprehensive Guide
Furosemide: A Comprehensive Guide
NAV
Identification
Pharmacology
Indication
Associated Conditions
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
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
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
Ascites
Edema
Hypertension
Chest congestion
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
Humans
NCarbonic anhydrase 2
inhibitor
Humans
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
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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
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
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.
Aceclofenac The therapeutic efficacy of Furosemide can be decreased when used in combination
with Aceclofenac.
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
Product Ingredients
INGREDIENT
UNII
CAS
INCHI KEY
Furosemide sodium
41733-55-5
Product Images
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Next
International/Other Brands
Diurapid (Mibe Jena) / Diurin (Mylan) / Diurmessel (Biomep) / Eutensin (Sanofi) / Frumex / Frusenex /
Frusol (Rosemont) / Furo-Puren (Actavis) / Seguril (Sanofi)
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 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
Mixture Products
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
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
C03 — DIURETICS
C — CARDIOVASCULAR SYSTEM
C03CA01 — Furosemide
C — CARDIOVASCULAR SYSTEM
G01AE — Sulfonamides
C03 — DIURETICS
C — CARDIOVASCULAR SYSTEM
Drug Categories
Acids, Carbocyclic
Amides
Amines
Aminobenzoates
Aniline Compounds
Antihypertensive Agents
Benzene Derivatives
Benzoates
Cardiovascular Agents
Diuretics
High-Ceiling Diuretics
Hyperglycemia-Associated Agents
Hypotensive Agents
Natriuretic Agents
Nephrotoxic agents
OAT1/SLC22A6 inhibitors
OAT3/SLC22A8 Inhibitors
Ototoxic agents
Photosensitizing Agents
Sulfanilamides
Sulfonamides
Sulfones
Sulfur Compounds
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
Sub Class
Benzenesulfonamides
Direct Parent
Aminobenzenesulfonamides
Alternative Parents
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
External Descriptors
Affected organisms
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
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]
FDA Approved Drug Products: Furoscix (furosemide injection), for subcutaneous use (October 2022)
[Link]
External Links
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
DAP000043
PharmGKB
PA449719
PDBe Ligand
FUN
RxList
Drugs.com
Wikipedia
Furosemide
PDB Entries
1z9y / 2xn5 / 3rf4 / 6de9 / 6sg0 / 7n3n / 7sfl / 8ste
CLINICAL TRIALS
Clinical Trials
4 Completed Treatment Chronic Heart Failure (CHF) / Congestive Heart Failure (CHF)
1
PHARMACOECONOMICS
Manufacturers
Astrazeneca lp
Hospira inc
Wockhardt ltd
Kalapharm inc
Sandoz inc
Superpharm corp
Packagers
American Regent
APP Pharmaceuticals
Cardinal Health
CVS Pharmacy
DAVA Pharmaceuticals
Dispensing Solutions
H and H Laboratories
Hospira Inc.
Intervet International
Liberty Pharmaceuticals
Macnary Ltd.
Major Pharmaceuticals
Mason Distributors
Mckesson Corp.
Medvantx Inc.
Mylan
Patheon Inc.
PCA LLC
Pharmedix
Prepackage Specialists
Qualitest
Ranbaxy Laboratories
Redpharm Drug
Remedy Repack
Roxane Labs
Sandoz
Sanofi-Aventis Inc.
Southwood Pharmaceuticals
Spectrum Pharmaceuticals
Taylor Pharmaceuticals
Tya Pharmaceuticals
UDL Laboratories
Va Cmop Dallas
Vatring Pharmaceuticals
Vedco Inc.
Wockhardt Ltd.
Dosage Forms
Tablet Oral 20 mg
Tablet Oral 40 mg
Solution 10 mg/1ml
Tablet Oral
Tablet Oral
Solution Parenteral 20 mg
Injection, solution
Tablet Oral 25 MG
Solution Intravenous 10 mg / mL
CapsuleOral
Solution Intravenous 20 mg
Liquid Oral 10 mg / mL
CapsuleOral 30 mg
CapsuleOral 60 mg
Liquid Intravenous 10 mg / mL
Injection 20 mg/2ml
Tablet Oral 80 mg
Kit Oral
Injection
Solution Oral
Prices
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
PROPERTIES
State
Solid
Experimental Properties
water solubility 73.1 mg/L (at 30 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
Predicted Properties
PROPERTY
VALUE
SOURCE
Water Solubility
0.118 mg/mL
ALOGPS
logP
2.71
ALOGPS
logP
1.75
Chemaxon
logS
-3.4
ALOGPS
4.25
Chemaxon
-1.5
Chemaxon
Physiological Charge
-1
Chemaxon
Chemaxon
Chemaxon
122.63 Å2
Chemaxon
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
PROPERTY
VALUE
PROBABILITY
Caco-2 permeable
P-glycoprotein substrate
Non-substrate
P-glycoprotein inhibitor I
Non-inhibitor
P-glycoprotein inhibitor II
Non-inhibitor
Non-inhibitor
Non-substrate
Non-substrate
CYP450 3A4 substrate
Non-substrate
Non-inhibitor
Non-inhibitor
Non-inhibitor
Non-inhibitor
Non-inhibitor
Ames test
Carcinogenicity
Non-carcinogens
Biodegradation
Weak inhibitor
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties.
(23092397)
SPECTRA
Not Available
Spectra
SPECTRUM
SPECTRUM TYPE
SPLASH KEY
1H NMR Spectrum
TARGETS
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
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
Molecular Weight
121449.13 Da
References
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]
2. Carbonic anhydrase 2
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
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
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
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
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
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
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
Molecular Weight
53139.56 Da
References
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
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
Specific Function
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]
TRANSPORTERS
1. Solute carrier family 22 member 6
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
InhibitorInducer
General Function
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
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]
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
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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
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
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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
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
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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Specific Function
Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
Gene Name
SLC22A11
Uniprot ID
Q9NSA0
Uniprot Name
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
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