Explore a selection of our essential drug information below, or:
Identification
- Summary
Fenoldopam is a dopamine D1 receptor agonist used for the short term management of hypertension.
- Brand Names
- Corlopam
- Generic Name
- Fenoldopam
- DrugBank Accession Number
- DB00800
- Background
A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Fenoldopam (DB00800)
- Weight
- Average: 305.756
Monoisotopic: 305.08187109 - Chemical Formula
- C16H16ClNO3
- Synonyms
- Fénoldopam
- Fenoldopam
- Fenoldopamum
- External IDs
- SKF 82526
- SKF 82526-J
Pharmacology
- Indication
For the in-hospital, short-term (up to 48 hours) management of severe hypertension when rapid, but quickly reversible, emergency reduction of blood pressure is clinically indicated, including malignant hypertension with deteriorating end-organ function.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Malignant hypertension •••••••••••• Treatment of Severe hypertension •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Fenoldopam is an agonist at D1-like dopamine receptors, binds to α2-adrenoceptors, increasing renal blood flow.
- Mechanism of action
Fenoldopam is a rapid-acting vasodilator. It is an agonist for D1-like dopamine receptors and binds with moderate affinity to α2-adrenoceptors. It has no significant affinity for D2-like receptors, α1 and β-adrenoceptors, 5HT1 and 5HT2 receptors, or muscarinic receptors. Fenoldopam is a racemic mixture with the R-isomer responsible for the biological activity. The R-isomer has approximately 250-fold higher affinity for D1-like receptors than does the S-isomer. In non-clinical studies, fenoldopam had no agonist effect on presynaptic D2-like dopamine receptors, or α or β -adrenoceptors, nor did it affect angiotensin-converting enzyme activity. Fenoldopam may increase norepinephrine plasma concentration.
Target Actions Organism AD(1B) dopamine receptor agonistHumans AD(1A) dopamine receptor agonistHumans UAlpha-1B adrenergic receptor inhibitorHumans UAlpha-1D adrenergic receptor inhibitorHumans UAlpha-1A adrenergic receptor inhibitorHumans UAlpha-2B adrenergic receptor antagonistHumans UAlpha-2C adrenergic receptor antagonistHumans UAlpha-2A adrenergic receptor antagonistHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Elimination is largely by conjugation, without participation of cytochrome P-450 enzymes. Methylation, glucuronidation, and sulfation are the main routes of conjugation.
- Route of elimination
Radiolabeled studies show that about 90% of infused fenoldopam is eliminated in urine, 10% in feces. Elimination is largely by conjugation, without participation of cytochrome P-450 enzymes. Only 4% of the administered dose is excreted unchanged.
- Half-life
The elimination half-life is about 5 minutes in mild to moderate hypertensives, with little difference between the R (active) and S isomers.
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The most likely reaction of overdose would be excessive hypotension which should be treated with drug discontinuation and appropriate supportive measures.
- Pathways
- Not Available
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Fenoldopam may decrease the excretion rate of Abacavir which could result in a higher serum level. Abaloparatide The risk or severity of adverse effects can be increased when Fenoldopam is combined with Abaloparatide. Acebutolol Fenoldopam may increase the hypotensive activities of Acebutolol. Aceclofenac The therapeutic efficacy of Fenoldopam can be decreased when used in combination with Aceclofenac. Acemetacin The therapeutic efficacy of Fenoldopam can be decreased when used in combination with Acemetacin. - Food Interactions
- Take on an empty stomach. Orally administered fenoldopam should be taken in a fasted state for optimal absorption.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Fenoldopam mesylate HA3R0MY016 67227-57-0 CVKUMNRCIJMVAR-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Corlopam Injection, solution 10 mg/1mL Intravenous Hospira, Inc. 2005-02-28 2021-01-01 US 
Corlopam Injection, solution 10 mg/1mL Intravenous Hospira, Inc. 2008-03-14 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Fenoldopam Mesylate Injection 10 mg/1mL Intravenous Bedford Pharmaceuticals 2004-10-14 2010-05-31 US Fenoldopam Mesylate Injection, solution 10 mg/1mL Intravenous Sandoz 2005-02-15 2009-05-31 US Fenoldopam Mesylate Injection 10 mg/1mL Intravenous Bedford Pharmaceuticals 2004-10-14 2010-05-31 US
Categories
- ATC Codes
- C01CA19 — Fenoldopam
- Drug Categories
- Adrenergic and Dopaminergic Agents
- Antihypertensive Agents
- Antihypertensive Agents Indicated for Hypertension
- Benzazepines
- Cardiac Stimulants Excl. Cardiac Glycosides
- Cardiac Therapy
- Cardiovascular Agents
- Dopamine Agents
- Dopamine Agonists
- Dopamine D1 Receptor Agonists
- Drugs that are Mainly Renally Excreted
- Heterocyclic Compounds, Fused-Ring
- Hypotensive Agents
- Neurotransmitter Agents
- Vasodilating Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as benzazepines. These are organic compounds containing a benzene ring fused to an azepine ring (unsaturated seven-membered heterocycle with one nitrogen atom replacing a carbon atom).
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzazepines
- Sub Class
- Not Available
- Direct Parent
- Benzazepines
- Alternative Parents
- Azepines / Aralkylamines / 1-hydroxy-2-unsubstituted benzenoids / Benzene and substituted derivatives / Aryl chlorides / Dialkylamines / Azacyclic compounds / Organopnictogen compounds / Organooxygen compounds / Organochlorides show 1 more
- Substituents
- 1-hydroxy-2-unsubstituted benzenoid / Amine / Aralkylamine / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Azepine / Benzazepine / Benzenoid show 12 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- benzazepine (CHEBI:5002)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- INU8H2KAWG
- CAS number
- 67227-56-9
- InChI Key
- TVURRHSHRRELCG-UHFFFAOYSA-N
- InChI
- InChI=1S/C16H16ClNO3/c17-15-11-5-6-18-8-13(9-1-3-10(19)4-2-9)12(11)7-14(20)16(15)21/h1-4,7,13,18-21H,5-6,8H2
- IUPAC Name
- 6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
- SMILES
- OC1=CC=C(C=C1)C1CNCCC2=C(Cl)C(O)=C(O)C=C12
References
- Synthesis Reference
- US4197297
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0014938
- KEGG Drug
- D00613
- KEGG Compound
- C07693
- PubChem Compound
- 3341
- PubChem Substance
- 46504963
- ChemSpider
- 3224
- BindingDB
- 60917
- 24853
- ChEBI
- 5002
- ChEMBL
- CHEMBL588
- Therapeutic Targets Database
- DAP000254
- PharmGKB
- PA164784034
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Wikipedia
- Fenoldopam
- FDA label
- Download (239 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Salt-sensitive Hypertension 1 somestatus stop reason just information to hide Not Available Terminated Prevention Partial Nephrectomy 1 somestatus stop reason just information to hide 4 Completed Prevention Cardiac Complications / Cardiopulmonary Bypass 1 somestatus stop reason just information to hide 4 Unknown Status Treatment Coronary Artery Disease (CAD) 1 somestatus stop reason just information to hide 4 Withdrawn Treatment Acute Renal Failure (ARF) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Hospira inc
- Bedford laboratories
- Pharmaforce inc
- Sandoz canada inc
- Teva parenteral medicines inc
- Packagers
- Baxter International Inc.
- Bedford Labs
- Ben Venue Laboratories Inc.
- Hospira Inc.
- Sandoz
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Injection, solution Intravenous; Parenteral 20 MG/2ML Injection, solution Intravenous; Parenteral 50 MG/5ML Injection Intravenous 10 mg/1mL Injection, solution Intravenous 10 mg/1mL - Prices
Unit description Cost Unit Fenoldopam 10 mg/ml ampule 213.75USD ml Corlopam 10 mg/ml ampul 81.9USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 4000 mg/L Not Available logP 2 Not Available - Predicted Properties
Property Value Source Water Solubility 0.272 mg/mL ALOGPS logP 2.39 ALOGPS logP 1.92 Chemaxon logS -3 ALOGPS pKa (Strongest Acidic) 8.12 Chemaxon pKa (Strongest Basic) 10.4 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 4 Chemaxon Polar Surface Area 72.72 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 82.68 m3·mol-1 Chemaxon Polarizability 30.89 Å3 Chemaxon Number of Rings 3 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 + 0.9972 Blood Brain Barrier + 0.7784 Caco-2 permeable - 0.5345 P-glycoprotein substrate Substrate 0.8329 P-glycoprotein inhibitor I Non-inhibitor 0.9142 P-glycoprotein inhibitor II Non-inhibitor 0.8567 Renal organic cation transporter Non-inhibitor 0.6062 CYP450 2C9 substrate Non-substrate 0.8216 CYP450 2D6 substrate Non-substrate 0.7124 CYP450 3A4 substrate Non-substrate 0.5301 CYP450 1A2 substrate Non-inhibitor 0.713 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Inhibitor 0.8931 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.8316 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7436 Ames test Non AMES toxic 0.7166 Carcinogenicity Non-carcinogens 0.9006 Biodegradation Not ready biodegradable 0.9935 Rat acute toxicity 2.7788 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.6864 hERG inhibition (predictor II) Inhibitor 0.8833
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 174.7425335 predictedDarkChem Lite v0.1.0 [M-H]- 169.59016 predictedDeepCCS 1.0 (2019) [M+H]+ 174.7947335 predictedDarkChem Lite v0.1.0 [M+H]+ 171.94818 predictedDeepCCS 1.0 (2019) [M+Na]+ 174.7466335 predictedDarkChem Lite v0.1.0 [M+Na]+ 178.04132 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase
- Specific Function
- dopamine binding
- Gene Name
- DRD5
- Uniprot ID
- P21918
- Uniprot Name
- D(1B) dopamine receptor
- Molecular Weight
- 52950.5 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Zeng C, Han Y, Huang H, Yu C, Ren H, Shi W, He D, Huang L, Yang C, Wang X, Zhou L, Jose PA: D1-like receptors inhibit insulin-induced vascular smooth muscle cell proliferation via down-regulation of insulin receptor expression. J Hypertens. 2009 May;27(5):1033-41. doi: 10.1097/HJH.0b013e3283293c7b. [Article]
- Dhasmana KM, Villalon CM, Zhu YN, Parmar SS: The role of dopamine (D2), alpha and beta-adrenoceptor receptors in the decrease in gastrointestinal transit induced by dopamine and dopamine-related drugs in the rat. Pharmacol Res. 1993 May-Jun;27(4):335-47. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase
- Specific Function
- arrestin family protein binding
- Gene Name
- DRD1
- Uniprot ID
- P21728
- Uniprot Name
- D(1A) dopamine receptor
- Molecular Weight
- 49292.765 Da
References
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Zeng C, Han Y, Huang H, Yu C, Ren H, Shi W, He D, Huang L, Yang C, Wang X, Zhou L, Jose PA: D1-like receptors inhibit insulin-induced vascular smooth muscle cell proliferation via down-regulation of insulin receptor expression. J Hypertens. 2009 May;27(5):1033-41. doi: 10.1097/HJH.0b013e3283293c7b. [Article]
- Dhasmana KM, Villalon CM, Zhu YN, Parmar SS: The role of dopamine (D2), alpha and beta-adrenoceptor receptors in the decrease in gastrointestinal transit induced by dopamine and dopamine-related drugs in the rat. Pharmacol Res. 1993 May-Jun;27(4):335-47. [Article]
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes
- Specific Function
- alpha1-adrenergic receptor activity
- Gene Name
- ADRA1B
- Uniprot ID
- P35368
- Uniprot Name
- Alpha-1B adrenergic receptor
- Molecular Weight
- 56835.375 Da
References
- Martin SW, Broadley KJ: Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade. Br J Pharmacol. 1995 May;115(2):349-55. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium
- Specific Function
- alpha1-adrenergic receptor activity
- Gene Name
- ADRA1D
- Uniprot ID
- P25100
- Uniprot Name
- Alpha-1D adrenergic receptor
- Molecular Weight
- 60462.205 Da
References
- Martin SW, Broadley KJ: Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade. Br J Pharmacol. 1995 May;115(2):349-55. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes
- Specific Function
- alpha1-adrenergic receptor activity
- Gene Name
- ADRA1A
- Uniprot ID
- P35348
- Uniprot Name
- Alpha-1A adrenergic receptor
- Molecular Weight
- 51486.005 Da
References
- Martin SW, Broadley KJ: Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade. Br J Pharmacol. 1995 May;115(2):349-55. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol
- Specific Function
- alpha2-adrenergic receptor activity
- Gene Name
- ADRA2B
- Uniprot ID
- P18089
- Uniprot Name
- Alpha-2B adrenergic receptor
- Molecular Weight
- 49953.145 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Martin SW, Broadley KJ: Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade. Br J Pharmacol. 1995 May;115(2):349-55. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins
- Specific Function
- alpha-2A adrenergic receptor binding
- Gene Name
- ADRA2C
- Uniprot ID
- P18825
- Uniprot Name
- Alpha-2C adrenergic receptor
- Molecular Weight
- 49521.585 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Martin SW, Broadley KJ: Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade. Br J Pharmacol. 1995 May;115(2):349-55. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol
- Specific Function
- alpha-1B adrenergic receptor binding
- Gene Name
- ADRA2A
- Uniprot ID
- P08913
- Uniprot Name
- Alpha-2A adrenergic receptor
- Molecular Weight
- 50646.17 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Martin SW, Broadley KJ: Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade. Br J Pharmacol. 1995 May;115(2):349-55. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 07, 2024 17:52