Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C16H16ClNO3 |
| Molecular Weight | 305.756 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC1=CC=C(C=C1)C2CNCCC3=C(Cl)C(O)=C(O)C=C23
InChI
InChIKey=TVURRHSHRRELCG-UHFFFAOYSA-N
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
| Molecular Formula | C16H16ClNO3 |
| Molecular Weight | 305.756 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
Fenoldopam (marketed under the brand name Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist. 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. Fenoldopam Mesylate Injection, USP is indicated 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.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 40.0 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | CORLOPAM Approved UseAdult Patients: Fenoldopam is indicated 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. Transition to oral therapy with another agent can begin at any time after blood pressure is stable during fenoldopam infusion. Pediatric Patients: Fenoldopam is indicated for the in-hospital, short-term (up to 4 hours) reduction in blood pressure. Launch Date8.7497277E11 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
10.9 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENOLDOPAM plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FED |
|
26.5 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENOLDOPAM plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
26.8 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENOLDOPAM plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FED |
|
44.7 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENOLDOPAM plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
2.6 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENOLDOPAM plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FED |
|
2.9 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/1673097 |
100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered: |
FENOLDOPAM plasma | Homo sapiens population: UNHEALTHY age: UNKNOWN sex: FEMALE / MALE food status: FASTED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
1.5 ug/kg/min single, intravenous Highest studied dose Dose: 1.5 ug/kg/min Route: intravenous Route: single Dose: 1.5 ug/kg/min Sources: Page: 1-61 |
unhealthy, 46±3 n = 9 Health Status: unhealthy Condition: Hypertension Age Group: 46±3 Sex: M+F Population Size: 9 Sources: Page: 1-61 |
|
0.8 ug/kg/min single, intravenous Recommended Dose: 0.8 ug/kg/min Route: intravenous Route: single Dose: 0.8 ug/kg/min Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Hypertension Sources: Page: p.1 |
Disc. AE: Tachycardia, Hypokalemia... AEs leading to discontinuation/dose reduction: Tachycardia Sources: Page: p.1Hypokalemia Anaphylactic reaction |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Anaphylactic reaction | Disc. AE | 0.8 ug/kg/min single, intravenous Recommended Dose: 0.8 ug/kg/min Route: intravenous Route: single Dose: 0.8 ug/kg/min Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Hypertension Sources: Page: p.1 |
| Hypokalemia | Disc. AE | 0.8 ug/kg/min single, intravenous Recommended Dose: 0.8 ug/kg/min Route: intravenous Route: single Dose: 0.8 ug/kg/min Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Hypertension Sources: Page: p.1 |
| Tachycardia | Disc. AE | 0.8 ug/kg/min single, intravenous Recommended Dose: 0.8 ug/kg/min Route: intravenous Route: single Dose: 0.8 ug/kg/min Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Hypertension Sources: Page: p.1 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Effect of fenoldopam on the acute and subacute nephrotoxicity produced by amphotericin B in the dog. | 1992 Jan |
|
| Evaluation of plasma von Willebrand factor as a biomarker for acute arterial damage in rats. | 2000 Sep-Oct |
|
| Design and rationale of CONTRAST--a prospective, randomized, placebo-controlled trial of fenoldopam mesylate for the prevention of radiocontrast nephropathy. | 2001 |
|
| Managing the high-risk patient: experience with fenoldopam, a selective dopamine receptor agonist, in prevention of radiocontrast nephropathy during percutaneous coronary intervention. | 2001 |
|
| Histopathological and immunohistochemical studies on arteritis induced by fenoldopam, a vasodilator, in rats. | 2001 Apr |
|
| [Fenoldopam: potential clinical applications in heart surgery]. | 2001 Dec |
|
| The effects of fenoldopam on coronary conduit blood flow after coronary artery bypass graft surgery. | 2001 Feb |
|
| Nonlinear analysis of partial dopamine agonist effects on cAMP in C6 glioma cells. | 2001 Jan-Feb |
|
| Reduced regional and global cerebral blood flow during fenoldopam-induced hypotension in volunteers. | 2001 Jul |
|
| D(1) dopamine receptor regulation of NHE3 during development in spontaneously hypertensive rats. | 2001 Jun |
|
| Preventing contrast-induced nephropathy with fenoldopam. | 2001 Mar |
|
| Renal blood flow changes induced with endothelin-1 and fenoldopam mesylate at quantitative Doppler US: initial results in a canine study. | 2001 May |
|
| [Regulation of NHE3 by D1 dopamine receptor during development of spontaneously hypertensive rats]. | 2001 May 10 |
|
| Fenoldopam: a selective peripheral dopamine-receptor agonist for the treatment of severe hypertension. | 2001 Nov 22 |
|
| Hemodynamic and sympathetic effects of fenoldopam and sodium nitroprusside. | 2001 Oct |
|
| Fenoldopam in the prevention of contrast media-induced acute renal failure. | 2001 Oct |
|
| Beneficial effects of fenoldopam treatment on renal function in streptozotocin-induced diabetic rats. | 2002 Apr |
|
| Changing trends in incidence and predictors of radiographic contrast nephropathy after percutaneous coronary intervention with use of fenoldopam. | 2002 Apr 15 |
|
| Management of patients with hypertensive urgencies and emergencies: a systematic review of the literature. | 2002 Dec |
|
| A protocol for prevention of radiographic contrast nephropathy during percutaneous coronary intervention: effect of selective dopamine receptor agonist fenoldopam. | 2002 Feb |
|
| The effects of fenoldopam on renal function in patients undergoing elective aortic surgery. | 2002 Jan |
|
| Immunohistochemical study on inducible type of nitric oxide (iNOS), basic fibroblast growth factor (bFGF) and tumor growth factor-beta1 (TGF-beta1) in arteritis induced in rats by fenoldopam and theophylline, vasodilators. | 2002 Jul |
|
| Fenoldopam mesylate blocks reductions in renal plasma flow after radiocontrast dye infusion: a pilot trial in the prevention of contrast nephropathy. | 2002 May |
|
| The therapeutic potential of dopamine modulators on the cardiovascular and renal systems. | 2002 May |
|
| Stability of fenoldopam mesylate in two infusion solutions. | 2002 May 1 |
|
| In vivo effects of fenoldopam on autonomic nervous system after inhibition or activation of ganglionic transmission. | 2002 May 31 |
|
| Contrast-associated nephropathy. | 2002 Nov-Dec |
|
| Using a dopamine type 1A receptor agonist in high-risk patients to ameliorate contrast-associated nephropathy. | 2002 Sep |
|
| New drugs: fenoldopam mesylate, glycoprotein IIb/IIIa antagonists, and K+ATP-channel agonists. | 2002 Winter |
|
| Hypertensive emergencies. Etiology and management. | 2003 |
|
| The role of the DA1 receptor agonist fenoldopam in the management of critically ill, transplant, and hypertensive patients. | 2003 |
|
| Pharmacologic identification of putative D1 dopamine receptors in feline kidneys. | 2003 Aug |
|
| The International Sepsis Forum's controversies in sepsis: my initial vasopressor agent in septic shock is dopamine rather than norepinephrine. | 2003 Feb |
|
| The vasodilatory effects of hydralazine, nicardipine, nitroglycerin, and fenoldopam in the human umbilical artery. | 2003 Feb |
|
| Compatibility of fenoldopam mesylate with other drugs during simulated Y-site administration. | 2003 Jan 1 |
|
| Dopamine D1 receptor-dependent inhibition of NaCl transport in the rat thick ascending limb: mechanism of action. | 2003 Jul 25 |
|
| Receptor mechanisms of prenodal lymphatic constriction by dopamine. | 2003 Jun 15 |
|
| Galpha12- and Galpha13-protein subunit linkage of D5 dopamine receptors in the nephron. | 2003 Mar |
|
| Radiocontrast-induced nephropathy. | 2003 Mar-Apr |
|
| Fenoldopam treatment improves peripheral insulin sensitivity and renal function in STZ-induced type 2 diabetic rats. | 2003 May |
|
| N-Acetylcysteine versus fenoldopam mesylate to prevent contrast agent-associated nephrotoxicity. | 2004 Aug 18 |
|
| Optimization of intestinal mucosal oxygenation in shock: a role for medical therapy? | 2004 Jan |
|
| Dopamine under alpha1-blockade, but not dopamine alone or fenoldopam, increases depressed gastric mucosal oxygenation. | 2004 Jan |
|
| Periprocedural hypertension: current concepts in management for the vascular surgeon. | 2004 Jul-Aug |
|
| Lessons in formulary management: the case of fenoldopam for radiographic contrast material-induced nephropathy. | 2004 Jun |
|
| Effects of short-term fenoldopam infusion on gastric mucosal blood flow in septic shock. | 2004 Sep |
Patents
Sample Use Guides
Adults: Initiate dosing at 0.01 to 0.3 mcg/kg/min by continuous infusion.
Dosing can be increased in increments of 0.05 to 0.1 mcg/kg/minute
every 15 minutes or longer until target blood pressure is reached.
Dilute prior to administration
Pediatrics: Initiate dosing at 0.2 mcg/kg/minute by continuous infusion
and titrate dose by 0.3 to 0.5 mcg/kg/min every 20-30 minutes to a
maximum dose of 0.8 mcg/kg/minute
Route of Administration:
Intravenous
| Substance Class |
Chemical
Created
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admin
on
Edited
Wed Jul 05 23:00:19 UTC 2023
by
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| Record UNII |
INU8H2KAWG
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| Record Status |
Validated (UNII)
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| Record Version |
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NCI_THESAURUS |
C66884
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WHO-ATC |
C01CA19
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NDF-RT |
N0000175580
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NDF-RT |
N0000000117
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WHO-VATC |
QC01CA19
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DTXSID0043896
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3341
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939
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FENOLDOPAM
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C61759
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M5280
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Fenoldopam
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CHEMBL588
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ENANTIOMER -> RACEMATE | |||
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BINDER->LIGAND |
BINDING
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ENANTIOMER -> RACEMATE | |||
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TARGET -> AGONIST | |||
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TARGET -> AGONIST |
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ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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| Biological Half-life | PHARMACOKINETIC |
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| Volume of Distribution | PHARMACOKINETIC |
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