関: fenoldopam mesylate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/06/09 03:48:59」(JST)

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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. 高血圧緊急症の治療に用いる薬物 drugs used for the treatment of hypertensive emergencies
2. 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
3. ドーパミンの腎臓作用 renal actions of dopamine
4. 造影剤誘発性腎症の予防 prevention of contrast induced nephropathy
5. 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

English Journal

NEFM (Neurofilament Medium) Polypeptide, a Marker for Zona Glomerulosa Cells in Human Adrenal, Inhibits D1R (Dopamine D1 Receptor)-Mediated Secretion of Aldosterone.

Maniero C1, Garg S1, Zhao W1, Johnson TI1, Zhou J1, Gurnell M1, Brown MJ2.
Hypertension (Dallas, Tex. : 1979).Hypertension.2017 Aug;70(2):357-364. doi: 10.1161/HYPERTENSIONAHA.117.09231. Epub 2017 Jun 5.
PMID 28584012

Lengthening primary cilia enhances cellular mechanosensitivity.

Spasic M, Jacobs CR1.
European cells & materials.Eur Cell Mater.2017 Feb 20;33:158-168. doi: 10.22203/eCM.v033a12.
PMID 28217833

Frontline Science: D1 dopaminergic receptor signaling activates the AMPK-bioenergetic pathway in macrophages and alveolar epithelial cells and reduces endotoxin-induced ALI.

Bone NB1, Liu Z1, Pittet JF2, Zmijewski JW3.
Journal of leukocyte biology.J Leukoc Biol.2017 Feb;101(2):357-365. doi: 10.1189/jlb.3HI0216-068RR. Epub 2016 Oct 12.
PMID 27733575

Japanese Journal

Oxytocin and dopamine stimulate ghrelin secretion by the ghrelin-producing cell line, MGN3-1 in vitro.

Iwakura Hiroshi,Ariyasu Hiroyuki,Hosoda Hiroshi,Yamada Go,Hosoda Kiminori,Nakao Kazuwa,Kangawa Kenji,Akamizu Takashi
Endocrinology 152(7), 2619-2625, 2011-07
… The dopamine receptor D1 agonist fenoldopam stimulated ghrelin secretion, whereas the D2, D3 agonist bromocriptine did not. …
NAID 120004397870

ヨード造影剤による腎障害発現機序の解明とベラプロストの保護作用

矢野貴久
藥學雜誌 128(7), 1023-1029, 2008-07-01
… Although little is known about the mechanism of RCN, a direct toxic action on renal cells and/or decrease in renal blood flow are considered to be implicated in the pathogenesis of the disease/the condition, A large number of vasodilatory agents, including endothelin antagonists, adenosine antagonists, atrial natriuretic peptide, calcium channel blockers, dopamine, dopamine D1 receptor agonist fenoldopam, and prostaglandin E1 have been tried clinically to prevent RCN, however, most of them have failed. …
NAID 110006792632

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

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リンク元	「フェノルドパム」
拡張検索	「fenoldopam mesylate」

「フェノルドパム」

Fenoldopam
Clinical data
Trade names	Corlopam
AHFS/Drugs.com	Monograph
Pregnancy; category	US: B (No risk in non-human studies); ;
Routes of; administration	IV
ATC code	C01CA19 (WHO);
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
	IUPAC name (RS)-6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol;
CAS Number	67227-56-9 ;
PubChem CID	3341;
IUPHAR/BPS	939;
DrugBank	DB00800 ;
ChemSpider	3224 ;
UNII	INU8H2KAWG;
KEGG	D07946 ;
ChEBI	CHEBI:5002 ;
ChEMBL	CHEMBL588 ;
ECHA InfoCard	100.060.538
Chemical and physical data
Formula	C16H16ClNO3
Molar mass	305.76 g/mol
3D model (Jmol)	Interactive image;
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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