Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C16H16ClNO3.ClH |
| Molecular Weight | 342.217 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.OC1=CC=C(C=C1)C2CNCCC3=C(Cl)C(O)=C(O)C=C23
InChI
InChIKey=NLMPGIXLXSPNFS-UHFFFAOYSA-N
InChI=1S/C16H16ClNO3.ClH/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;1H
| 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 | ( + / - ) |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 |
|---|---|---|
| Cardiovascular function during induced hypotension by fenoldopam or sodium nitroprusside in anesthetized dogs. | 1992 Jan |
|
| Effect of fenoldopam on the acute and subacute nephrotoxicity produced by amphotericin B in the dog. | 1992 Jan |
|
| Contrast nephropathy : an evidence-based approach to prevention. | 2003 |
|
| Hypertensive emergencies. Etiology and management. | 2003 |
|
| A review of pharmacologic interventions to prevent contrast-induced nephropathy. | 2003 |
|
| The role of the DA1 receptor agonist fenoldopam in the management of critically ill, transplant, and hypertensive patients. | 2003 |
|
| Improving perioperative outcomes in patients with end-stage heart failure. | 2003 |
|
| Contemporary strategies to preserve renal function during cardiac and vascular surgery. | 2003 |
|
| A review of contemporary prevention strategies for radiocontrast nephropathy: a focus on fenoldopam and N-acetylcysteine. | 2003 |
|
| Pharmacological profile of the vascular responses to dopamine in the canine external carotid circulation. | 2003 Apr |
|
| Fenoldopam for renal protection in patients undergoing cardiopulmonary bypass. | 2003 Aug |
|
| Pharmacologic identification of putative D1 dopamine receptors in feline kidneys. | 2003 Aug |
|
| Fenoldopam and N-acetylcysteine for the prevention of radiographic contrast material-induced nephropathy: a review. | 2003 Dec |
|
| Monitoring renal oxygen supply in critically-ill patients using urinary oxygen tension. | 2003 Dec |
|
| Amygdaloid D1 receptors are not linked to stimulation of adenylate cyclase. | 2003 Dec 15 |
|
| Malignant hypertension presenting as hemolysis, thrombocytopenia, and renal failure. | 2003 Fall |
|
| A case series of low-dose fenoldopam in seventy cardiac surgical patients at increased risk of renal dysfunction. | 2003 Feb |
|
| The International Sepsis Forum's controversies in sepsis: my initial vasopressor agent in septic shock is dopamine rather than norepinephrine. | 2003 Feb |
|
| Fenoldopam--but not dopamine--selectively increases gastric mucosal oxygenation in dogs. | 2003 Jul |
|
| Dopamine D1 receptor-dependent inhibition of NaCl transport in the rat thick ascending limb: mechanism of action. | 2003 Jul 25 |
|
| Acetylcysteine and fenoldopam. Promising new approaches for preventing effects of contrast nephrotoxicity. | 2003 Jun |
|
| 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 |
|
| Radiocontrast-induced nephropathy and percutaneous coronary intervention: a review of preventive measures. | 2003 May |
|
| Contrast agent--associated nephrotoxicity. | 2003 May-Jun |
|
| [Fenoldopam and kidney function in a case of abdominal aortic pseudoaneurysm with supra-renal clamping in an emergency protocol]. | 2003 Nov |
|
| The effects of intraoperative fenoldopam on renal blood flow and tubular function following suprarenal aortic cross-clamping. | 2003 Nov |
|
| Fenoldopam mesylate for the prevention of contrast-induced nephropathy: a randomized controlled trial. | 2003 Nov 5 |
|
| Effect of fenoldopam on renal function after nephrotomy in normal dogs. | 2003 Nov-Dec |
|
| Clinical review: the management of hypertensive crises. | 2003 Oct |
|
| Perturbation of D1 dopamine and AT1 receptor interaction in spontaneously hypertensive rats. | 2003 Oct |
|
| Effects of fenoldopam on renal blood flow and its function in a canine model of rhabdomyolysis. | 2003 Sep |
|
| Phlebotomy in the intensive care unit: strategies for blood conservation. | 2004 |
|
| In vitro effects of antihypertensive drugs on thromboxane agonist (U46619)-induced vasoconstriction in human internal mammary artery. | 2004 Aug |
|
| N-Acetylcysteine versus fenoldopam mesylate to prevent contrast agent-associated nephrotoxicity. | 2004 Aug 18 |
|
| American society of nephrology-36th annual meeting and renal week 2003. | 2004 Jan |
|
| 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 |
|
| Prevention of radiocontrast-induced nephropathy. | 2004 Jul |
|
| 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 |
|
| [Involvement of dopamine receptor in the pathogenesis of hypertension and hypertensive target-organ damage]. | 2004 Mar |
|
| Prophylaxis of iodinated contrast media-induced nephropathy: a pharmacological point of view. | 2004 Mar |
|
| Dopamine D1 receptor augmentation of D3 receptor action in rat aortic or mesenteric vascular smooth muscles. | 2004 Mar |
|
| Aberrant D1 and D3 dopamine receptor transregulation in hypertension. | 2004 Mar |
|
| Prevention of contrast media nephrotoxicity--the story so far. | 2004 May |
|
| Fenoldopam versus nitroprusside for the treatment of hypertensive emergency. | 2004 May |
|
| 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
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Edited
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| Record UNII |
425S22SN3P
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| Record Status |
Validated (UNII)
|
| Record Version |
|
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21642479
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181217-39-0
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DTXSID1042607
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425S22SN3P
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| Related Record | Type | Details | ||
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ENANTIOMER -> RACEMATE | |||
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ENANTIOMER -> RACEMATE |
