Fenoldopam

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Fenoldopam
Fenoldopam.svg
Fenoldopam 3d balls.png
Clinical data
Trade names Corlopam
AHFS/Drugs.com Monograph
Routes of
administration 		IV
ATC code
Legal status
Legal status
Pharmacokinetic data
Metabolism Hepatic (CYP not involved)
Elimination half-life 5 minutes
Excretion Renal (90%) and fecal (10%)
Identifiers
  • (RS)-6-chloro-1-(4-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C16H16ClNO3
Molar mass 305.76 g·mol−1
3D model (JSmol)
Chirality Racemic 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 Yes check.svgY
  • Key:TVURRHSHRRELCG-UHFFFAOYSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

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]

Contents

Indications

Fenoldopam is used as an antihypertensive agent postoperatively, and also intravenously (IV) to treat a hypertensive 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 concomitant chronic kidney disease. [5] It can cause reflex tachycardia, but it is dependent on the infusion of the drug.

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]

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References

  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. 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. Retrieved November 14, 2011.
  4. 1 2 Shen 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 . Retrieved 2021-05-02.
  6. 1 2 Nichols 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.
  7. ↑ 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.
  8. ↑ 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.
  9. ↑ 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.
  10. ↑ Epstein, Murray MD, "Diagnosis and Management of Hypertensive Emergencies," clinical Cornerstone. Hypertension Vol2. No 1.
  11. 1 2 3 "Corlopam RA06497-R1-9/03 brand of Fenoldopam Mesylate Injection, USP" (PDF). NDA 19-922/S-005.
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