| Item |
Information |
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Drug Groups
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approved |
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Description
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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 |
| • |
Humans and other mammals |
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| 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. |
| External Links |
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