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Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D₁ receptor partial agonist.^[1] Fenoldopam is used as an antihypertensive agent.^[2] It was approved by the Food and Drug Administration (FDA) in September 1997.^[3]

Indications

Fenoldopam is used as an antihypertensive agent postoperatively, and also intravenously (IV) to treat a hypertensive crisis.^[4] Since fenoldopam is the only intravenous agent that improves renal perfusion, in theory it could be beneficial in hypertensive patients with concomitant renal insufficiency.^[5]

Pharmacology

Fenoldopam causes arterial/arteriolar vasodilation leading to a decrease in blood pressure by activating peripheral D₁ receptors.^[6] It decreases afterload and also promotes sodium excretion via specific dopamine receptors along the nephron. The renal effect of fenoldopam and dopamine may involve physiological antagonism of the renin-angiotensin system in the kidney.^[7] In contrast to dopamine, fenoldopam is a selective D₁ receptor agonist with no effect on beta adrenoceptors, although there is evidence that it may have some alpha-1 ^[8] and alpha-2 adrenoceptor antagonist activity.^[6] D₁ receptor stimulation activates adenylyl cyclase and raises intracellular cyclic AMP, resulting in vasodilation of most arterial beds, including renal, mesenteric, and coronary arteries.^[9] to cause a reduction in systemic vascular resistance. Fenoldopam has a rapid onset of action (4 minutes) and short duration of action (< 10 minutes) and a linear dose response relationship at usual clinical doses.^[10]

Side effects

Adverse effects include headache, flushing, nausea, hypotension, reflex tachycardia, and increased intraocular pressure.^[4]^[11]

Contraindications, warnings and precautions

Fenoldopam mesylate contains sodium metabisulfite, a sulfite that may rarely cause allergic-type reactions including anaphylactic symptoms and asthma in susceptible people. Fenoldopam mesylate administration should be undertaken with caution to patients with glaucoma or raised intraocular pressure as fenoldopam raises intraocular pressure.^[11] Concomitant use of fenoldopam with a beta-blocker should be avoided if possible, as unexpected hypotension can result from beta-blocker inhibition of sympathetic-mediated reflex tachycardia in response to fenoldopam.^[11]

References

^ Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. Pharmacol. Exp. Ther. 258 (1): 193–8. PMID 1677038.
^ Oliver WC, Nuttall GA, Cherry KJ, Decker PA, Bower T, Ereth MH (October 2006). "A comparison of fenoldopam with dopamine and sodium nitroprusside in patients undergoing cross-clamping of the abdominal aorta". Anesth. Analg. 103 (4): 833–40. doi:10.1213/01.ane.0000237273.79553.9e. PMID 17000789.
^ http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.Label_ApprovalHistory accessed November 14, 2011
^ ^a ^b Shen, Howard (2008). Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 9. ISBN 1-59541-101-1.
^ USMLE WORLD 2009 Step1 QBanks, Pharmacology, Pharma50q, Q NO 18
^ ^a ^b Nichols AJ, Ruffolo RR, Brooks DP (June 1990). "The pharmacology of fenoldopam". Am. J. Hypertens. 3 (6 Pt 2): 116S–119S. PMID 1974439.
^ Gildea JJ (January 2009). "Dopamine and angiotensin as renal counterregulatory systems controlling sodium balance". Curr. Opin. Nephrol. Hypertens. 18 (1): 28–32. doi:10.1097/MNH.0b013e32831a9e0b. PMC 2847451. PMID 19077686.
^ Martin SW, Broadley KJ (May 1995). "Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade". Br. J. Pharmacol. 115 (2): 349–55. doi:10.1111/j.1476-5381.1995.tb15884.x. PMC 1908310. PMID 7670737.
^ Hughes AD, Sever PS (1989). "Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries". Blood Vessels. 26 (2): 119–27. PMID 2474340.
^ Epstein, Murray MD, "Diagnosis and Management of Hypertensive Emergencies," clinical Cornerstone. Hypertension Vol2. No 1.
^ ^a ^b ^c NDA 19-922/S-005: Corlopam RA06497-R1-9/03 brand of Fenoldopam Mesylate Injection, USP

UpToDate Contents

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1. 虚血後（虚血性）の急性尿細管壊死において考え得る予防および治療 possible prevention and therapy of postischemic ischemic acute tubular necrosis
2. 高血圧緊急症の治療に用いる薬物 drugs used for the treatment of hypertensive emergencies
3. ドーパミンの腎臓作用 renal actions of dopamine
4. 小児における急性腎障害（急性腎不全）の予防およびマネージメント prevention and management of acute kidney injury acute renal failure in children
5. 成人における高血圧緊急症の評価および治療 evaluation and treatment of hypertensive emergencies in adults

English Journal

Expression and therapeutic targeting of dopamine receptor-1 (D1R) in breast cancer.

Borcherding DC1, Tong W2, Hugo ER1, Barnard DF1, Fox S1, LaSance K3, Shaughnessy E4, Ben-Jonathan N1.
Oncogene.Oncogene.2015 Oct 19. doi: 10.1038/onc.2015.369. [Epub ahead of print]
Patients with advanced breast cancer often fail to respond to treatment, creating a need to develop novel biomarkers and effective therapeutics. Dopamine (DA) is a catecholamine that binds to five G protein-coupled receptors. We discovered expression of DA type-1 receptors (D1Rs) in breast cancer, t
PMID 26477316

THE EFFECTS OF FENOLDOPAM ON RENAL FUNCTION AND METABOLISM IN AN OVINE MODEL OF SEPTIC SHOCK.

Post EH1, Su F, Taccone FS, Hosokawa K, Herpain A, Creteur J, Vincent JL, De Backer D.
Shock (Augusta, Ga.).Shock.2015 Oct 19. [Epub ahead of print]
INTRODUCTION: The importance of renal perfusion and metabolism in septic acute kidney injury (AKI) remains unclear. Prophylactic administration of the dopaminergic agent, fenoldopam, has been suggested to reduce the occurrence of AKI but its effects in septic shock are poorly defined.METHODS: Sepsis
PMID 26506071

Fenoldopam for the prevention of contrast-induced nephropathy (CIN)-do we need more trials? A meta-analysis.

Naeem M1, McEnteggart GE2, Murphy TP2, Prince E2, Ahn S2, Soares G2.
Clinical imaging.Clin Imaging.2015 Sep-Oct;39(5):759-64. doi: 10.1016/j.clinimag.2015.02.003. Epub 2015 Feb 12.
We conducted a pooled analysis of clinical trials comparing intravenous Fenoldopam (FP) with Saline/Placebo/N-acetyl cysteine (NAC) for the prevention of contrast-induced nephropathy (CIN). Five studies were eligible. Quantitative analyses were done with Review Manager (RevMan version 5.2.). A total
PMID 25709111

Japanese Journal

Fenoldopam mesylate in early acute tubular necrosis : a randomized, double-blind, placebo-controlled clinical trial

TUMLIN JA
Am J Kidney Dis 46, 26-34, 2005
NAID 30015141328

N-Acetylcysteine versus fenoldopam mesylate to prevent contrast agent-associated nephrotoxicity

BRIGUORI C
J Am Coll Cardiol 44, 762-765, 2004
NAID 30008101503

「フェノルドパム」

Fenoldopam
Systematic (IUPAC) name
	(RS)-6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
Clinical data
Trade names	Corlopam
AHFS/Drugs.com	Monograph
Pregnancy; category	US: B (No risk in non-human studies); ;
Routes of; administration	IV
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Metabolism	Hepatic (CYP not involved)
Biological half-life	5 minutes
Excretion	Renal (90%) and fecal (10%)
Identifiers
CAS Number	67227-57-0
ATC code	C01CA19 (WHO)
PubChem	CID 3341
IUPHAR/BPS	939
DrugBank	DB00800
ChemSpider	3224
UNII	HA3R0MY016
KEGG	D07946
ChEBI	CHEBI:5002
ChEMBL	CHEMBL588
Chemical data
Formula	C16H16ClNO3
Molar mass	305.76 g/mol
Chirality	Racemic mixture
	SMILES Clc1c3c(cc(O)c1O)C(c2ccc(O)cc2)CNCC3 ;
	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 ; Key:TVURRHSHRRELCG-UHFFFAOYSA-N ;
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