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Fenoldopam

From Wikipedia, the free encyclopedia
Antihypertensive agent
Pharmaceutical compound
Fenoldopam
Clinical data
Trade namesCorlopam
AHFS/Drugs.comMonograph
Routes of
administration
Intravenous
ATC code
Legal status
Legal status
Pharmacokinetic data
MetabolismHepatic (CYP not involved)
Eliminationhalf-life5 minutes
ExcretionRenal (90%) and fecal (10%)
Identifiers
  • (RS)-6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC16H16ClNO3
Molar mass305.76 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • Clc1c3c(cc(O)c1O)C(c2ccc(O)cc2)CNCC3
  • 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 checkY
  • Key:TVURRHSHRRELCG-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Fenoldopam, sold under the brand nameCorlopam, is adrug andsyntheticbenzazepinederivative which acts as aselectiveD1 receptorpartial agonist.[1] Fenoldopam is used as anantihypertensive agent.[2] It was approved by the USFood and Drug Administration (FDA) in September 1997.[3]

Medical uses

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Fenoldopam is used as an antihypertensive agent postoperatively, and alsointravenously to treat ahypertensive crisis.[4]Since fenoldopam is an intravenous agent with minimal adrenergic effects that improves renal perfusion, in theory it could be beneficial in hypertensive patients with concomitantchronic kidney disease.[5] It can cause reflextachycardia, but it is dependent on the infusion of the drug.

Contraindications

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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 withglaucoma or raisedintraocular pressure as fenoldopam raises intraocular pressure.[6] Concomitant use of fenoldopam with abeta blocker should be avoided if possible, as unexpected hypotension can result from beta-blocker inhibition of sympathetic-mediated reflex tachycardia in response to fenoldopam.[6]

Adverse effects

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Adverse effects includeheadache,flushing,nausea,hypotension,reflex tachycardia, and increasedintraocular pressure.[4][6]

Pharmacology

[edit]

Fenoldopam causes arterial/arteriolarvasodilation leading to a decrease inblood pressure by activating peripheral D1 receptors.[7] It decreasesafterload and also promotessodium excretion via specific dopamine receptors along thenephron. The renal effect of fenoldopam and dopamine may involve physiological antagonism of the renin-angiotensin system in the kidney.[8]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[9] and alpha-2 adrenoceptor antagonist activity.[7] D1 receptor stimulation activates adenylyl cyclase and raises intracellular cyclic AMP, resulting in vasodilation of most arterial beds, including renal, mesenteric, and coronary arteries.[10] 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 lineardose–response relationship at usual clinical doses.[11]

See also

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References

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  1. ^Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells".The Journal of Pharmacology and Experimental Therapeutics.258 (1):193–198.doi:10.1016/S0022-3565(25)20252-X.PMID 1677038.
  2. ^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".Anesthesia and Analgesia.103 (4):833–840.doi:10.1213/01.ane.0000237273.79553.9e.PMID 17000789.S2CID 23684353.
  3. ^"Drugs@FDA: FDA-Approved Drugs".www.accessdata.fda.gov. Archived fromthe original on July 2, 2010. RetrievedNovember 14, 2011.
  4. ^abShen H (2008).Illustrated Pharmacology Memory Cards: PharMnemonics. Minireview. p. 9.ISBN 978-1-59541-101-3.
  5. ^Szymanski MW, Richards JR (2021)."Fenoldopam".StatPearls. Treasure Island (FL): StatPearls Publishing.PMID 30252314. Retrieved2021-05-02.
  6. ^abc"Corlopam RA06497-R1-9/03 brand of Fenoldopam Mesylate Injection, USP"(PDF). NDA 19-922/S-005. Archived fromthe original(PDF) on September 5, 2015.
  7. ^abNichols AJ, Ruffolo RR, Brooks DP (June 1990). "The pharmacology of fenoldopam".American Journal of Hypertension.3 (6 Pt 2):116S –119S.doi:10.1093/ajh/3.6.116s.PMID 1974439.
  8. ^Gildea JJ (January 2009)."Dopamine and angiotensin as renal counterregulatory systems controlling sodium balance".Current Opinion in Nephrology and Hypertension.18 (1):28–32.doi:10.1097/MNH.0b013e32831a9e0b.PMC 2847451.PMID 19077686.
  9. ^Martin SW, Broadley KJ (May 1995)."Renal vasodilatation by dopexamine and fenoldopam due to alpha 1-adrenoceptor blockade".British Journal of Pharmacology.115 (2):349–355.doi:10.1111/j.1476-5381.1995.tb15884.x.PMC 1908310.PMID 7670737.
  10. ^Hughes AD, Sever PS (1989). "Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries".Blood Vessels.26 (2):119–127.doi:10.1159/000158760.PMID 2474340.
  11. ^Epstein, Murray MD, "Diagnosis and Management of Hypertensive Emergencies," clinical Cornerstone. Hypertension Vol2. No 1.
Sympatholytic (and closely related)antihypertensives (C02)
Sympatholytics
(antagonizeα-adrenergic
vasoconstriction)
Central
α2-Adrenergic receptor agonists
Adrenergic release inhibitors
Imidazoline receptor agonists
Ganglion-blocking/nicotinic antagonists
Peripheral
Indirect
Monoamine oxidase inhibitors
VMAT inhibitors
Tyrosine hydroxylase inhibitors
Direct
α1-Adrenergic receptor blockers
Non-selective α-adrenergic receptor blockers
Otherantagonists
Serotonin receptor antagonists
Endothelin receptor antagonists (forPHTooltip Pulmonary hypertension)
D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists
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