Drug Groups

approved

Description

A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation. [PubChem]

Indication

For the in-hospital, short-term (up to 48 hours) management of severe hypertension when rapid, but quickly reversible, emergency reduction of blood pressure is clinically indicated, including malignant hypertension with deteriorating end-organ function.

Pharmacology

Fenoldopam is an agonist at D₁-like dopamine receptors, binds to α₂-adrenoceptors, increasing renal blood flow.

Toxicity

The most likely reaction of overdose would be excessive hypotension which should be treated with drug discontinuation and appropriate supportive measures.

Affected Organisms

Biotransformation

Elimination is largely by conjugation, without participation of cytochrome P-450 enzymes. Methylation, glucuronidation, and sulfation are the main routes of conjugation.

Half Life

The elimination half-life is about 5 minutes in mild to moderate hypertensives, with little difference between the R (active) and S isomers.

Elimination

Radiolabeled studies show that about 90% of infused fenoldopam is eliminated in urine, 10% in feces.
Elimination is largely by conjugation, without participation of cytochrome P-450 enzymes. Only 4% of the administered dose is excreted unchanged.

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