Fenoldopam

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)
Legal status	US: ℞-only
Routes of administration	IV
Pharmacokinetic data
Metabolism	Hepatic (CYP not involved)
Biological half-life	5 minutes
Excretion	Renal (90%) and fecal (10%)
Identifiers
CAS Number	67227-57-0 Y
ATC code	C01CA19 (WHO)
PubChem	CID: 3341
IUPHAR/BPS	939
DrugBank	DB00800 Y
ChemSpider	3224 Y
UNII	HA3R0MY016 Y
KEGG	D07946 Y
ChEBI	CHEBI:5002 Y
ChEMBL	CHEMBL588 Y
Chemical data
Formula	C16H16ClNO3
Molecular mass	305.76 g/mol
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 Y Key:TVURRHSHRRELCG-UHFFFAOYSA-N Y
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Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D₁ receptor partial agonist. Fenoldopam is used as an antihypertensive agent. It was approved by the Food and Drug Administration (FDA) in September 1997.

Indications

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

Pharmacology

Fenoldopam causes arterial/arteriolar vasodilation leading to a decrease in blood pressure by activating peripheral D₁ receptors. 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. 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 and alpha-2 adrenoceptor antagonist activity. D₁ receptor stimulation activates adenylyl cyclase and raises intracellular cyclic AMP, resulting in vasodilation of most arterial beds, including renal, mesenteric, and coronary arteries. 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.

Side effects

Adverse effects include headache, flushing, nausea, hypotension, reflex tachycardia, and increased intraocular pressure.

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. 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.