FENOLDOPAM MESYLATE
Clinical safety rating
cautionComprehensive 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. |
| Molecular Weight | 401.44 |
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 | Fenoldopam is a dopamine D1-like receptor agonist used for hypertensive emergencies. Animal studies have not shown teratogenic effects, but no adequate human studies in first trimester. Use only if benefit outweighs risk. |
| 2nd trimester | Limited human data; no known teratogenicity. May be used if clearly needed. |
| 3rd trimester | May cause fetal hypotension, tachycardia, and potential uteroplacental hypoperfusion. Use only if maternal benefit justifies potential fetal risk. |
Clinical note
Comprehensive clinical and safety monograph for FENOLDOPAM MESYLATE (FENOLDOPAM MESYLATE).
| Placental transfer | Fenoldopam is a small molecule and likely crosses the placenta, though specific data are lacking. Animal studies indicate placental transfer. |
| Breastfeeding | Unknown if fenoldopam is excreted in human milk. Due to short half-life and IV use, exposure likely low. Use caution; consider benefits of breastfeeding vs. potential infant risk. |
| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| 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. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to fenoldopam or any componentPatients with glaucoma (may increase intraocular pressure)Concurrent use of beta-blockers (may cause paradoxical hypertension)
| 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. |
| Food/Dietary | No specific food interactions reported. However, patients should avoid excessive caffeine or stimulants as they may affect blood pressure. |
| Clinical Pearls | Fenoldopam is a dopamine D1-like receptor agonist used for severe hypertension and hypertensive emergencies. It causes rapid, titratable blood pressure reduction without the toxic metabolites seen with nitroprusside. It also increases renal blood flow and natriuresis, making it beneficial in patients with renal impairment. Avoid in patients with glaucoma (increases intraocular pressure) or sulfite allergy (contains sodium metabisulfite). |
| Patient Advice | This medication is given intravenously and is only used in a hospital setting. · You will have your blood pressure and heart rate monitored continuously during the infusion. · Report any headache, flushing, or dizziness to your nurse. · Do not stop the infusion suddenly; the dose will be gradually decreased. · Avoid consuming caffeine or other stimulants during treatment. · Tell your healthcare provider if you have glaucoma or a history of sulfite allergy. |
Loading safety data…