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Active ingredient: Fenoldopam - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Antihypertensive Agents
  • Dopamine Agonists
  • Vasodilator Agents

Dosage Forms

  • Solution

Brands / Synonyms

Corlopam; Fenodopam mesylate; Fenoldopam; Fenoldopam mesylate; Fenoldopamum [Latin]

Indications

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 antagonizes D1-like dopamine receptors, binds to α2-adrenoceptors, increasing renal blood flow.

Mechanism of Action

Fenoldopam is a rapid-acting vasodilator. It is an agonist for D1-like dopamine receptors and binds with moderate affinity to α2-adrenoceptors. It has no significant affinity for D2-like receptors, α1 and β-adrenoceptors, 5HT1 and 5HT2 receptors, or muscarinic receptors. Fenoldopam is a racemic mixture with the R-isomer responsible for the biological activity. The R-isomer has approximately 250-fold higher affinity for D1-like receptors than does the S-isomer. In non-clinical studies, fenoldopam had no agonist effect on presynaptic D2-like dopamine receptors, or α or β -adrenoceptors, nor did it affect angiotensin-converting enzyme activity. Fenoldopam may increase norepinephrine plasma concentration.

Absorption

Not Available

Toxicity

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

Biotrnasformation / Drug Metabolism

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

Contraindications

None known.

Drug Interactions

Drug Interactions with Beta-Blockers: Concomitant use of fenoldopam with beta-blockers should be avoided. If the drugs are used together, caution should be exercised because unexpected hypotension could result from beta-blocker inhibition of the sympathetic reflex response to fenoldopam.

Drug Interactions, General: Although there have been no formal interaction studies, intravenous fenoldopam has been administered safely with drugs such as digitalis and sublingual nitroglycerin. There is limited experience with concomitant antihypertensive agents such as alpha-blockers, calcium channel-blockers, ACE inhibitors, and diuretics (both thiazide-like and loop).

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