FENOLDOPAM MESYLATE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FENOLDOPAM MESYLATE (FENOLDOPAM MESYLATE).
Dopamine D1-like receptor agonist (D1 and D5) causing vasodilation in renal, mesenteric, coronary, and cerebral arteries; increases renal blood flow and natriuresis.
| Metabolism | Primarily hepatic via conjugation (glucuronidation and sulfation); CYP450 minimally involved. |
| Excretion | Renal (80% as metabolites, 10% as unchanged drug); fecal/biliary minor (10%) |
| Half-life | Terminal elimination half-life approximately 10 minutes (range 5–20 min) in healthy adults; clinically, continuous infusion is required to maintain therapeutic effect due to rapid clearance. |
| Protein binding | Approximately 90% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | 0.6–0.8 L/kg; moderate distribution consistent with limited tissue penetration. |
| Bioavailability | Intravenous: 100%; no oral bioavailability due to extensive first-pass metabolism (not administered orally). |
| Onset of Action | Intravenous: 5 minutes; rapid vasodilation and blood pressure reduction observed within 5 min of infusion initiation. |
| Duration of Action | Short duration; effects dissipate within 30–60 minutes after infusion cessation; some hemodynamic effects may persist up to 2 hours in patients with renal impairment. |
0.1 to 0.3 mcg/kg/min IV continuous infusion, titrated every 15-20 minutes by 0.05-0.1 mcg/kg/min; max dose 1.6 mcg/kg/min.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment; however, monitor for hypotension and electrolyte disturbances. |
| Liver impairment | No specific Child-Pugh based adjustments; use with caution in severe hepatic impairment due to increased risk of hypotension. |
| Pediatric use | Not FDA-approved for pediatric use; limited data: 0.2 mcg/kg/min IV infusion, titrated to effect; max 0.8 mcg/kg/min. |
| Geriatric use | Start at low end of dosing range (0.1 mcg/kg/min) due to increased sensitivity to hypotension; monitor blood pressure closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FENOLDOPAM MESYLATE (FENOLDOPAM MESYLATE).
| Breastfeeding | No data on presence in human milk; M/P ratio unknown. Caution advised; consider benefits of breastfeeding vs potential risk of infant exposure. |
| Teratogenic Risk | Risk in first trimester: No adequate human studies; animal studies show no teratogenic effects at clinically relevant doses. Risk in second and third trimesters: Potential for fetal hypotension and decreased uteroplacental perfusion; use only if clearly needed. Avoid in severe preeclampsia or eclampsia due to risk of significant maternal hypotension. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Known hypersensitivity to fenoldopam or any component","Patients with glaucoma"]
| Precautions | ["Hypotension risk: Monitor blood pressure closely; may cause excessive hypotension.","Tachycardia: Can increase heart rate; caution in patients with coronary ischemia or tachyarrhythmias.","Glaucoma risk: May increase intraocular pressure; avoid in patients with glaucoma.","Hypokalemia: Monitor potassium levels; may cause hypokalemia."] |
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| Fetal Monitoring |
| Monitor maternal blood pressure, heart rate, and signs of hypotension. Fetal heart rate monitoring recommended during infusion. Assess uteroplacental blood flow if prolonged use. |
| Fertility Effects | No human fertility studies; animal studies show no impairment of fertility at clinically relevant doses. |