EPOPROSTENOL SODIUM

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EPOPROSTENOL SODIUM (EPOPROSTENOL SODIUM).

How it works

Prostacyclin (PGI2) analog; vasodilator and inhibitor of platelet aggregation via IP receptor activation, increasing cAMP in smooth muscle and platelets.

What the body does with it

Metabolism	Rapidly hydrolyzed at physiologic pH (t1/2 ~3-6 min); pH-dependent degradation; no significant hepatic metabolism.
Excretion	Renal (primarily as metabolites, <1% unchanged); biliary/fecal minimal.
Half-life	2-5 min (terminal); clinically administered via continuous IV infusion due to rapid elimination.
Protein binding	Approximately 60-70%, primarily to albumin.
Volume of Distribution	0.3-0.5 L/kg; confined primarily to intravascular space due to rapid metabolism.
Bioavailability	IV: 100%; inhaled: limited systemic absorption (approximately 10-20% of inhaled dose).
Onset of Action	IV: immediate (within 2-5 min); inhaled: 5-10 min.
Duration of Action	IV: 10-15 min post-infusion; inhaled: 30-60 min; continuous infusion required for sustained effect.

Classification & Brands

Dosing & administration

Initial: 2 ng/kg/min IV via continuous infusion, titrated by 1-2 ng/kg/min every 15 minutes or longer based on hemodynamic response. Typical maintenance: 20-40 ng/kg/min, range 10-50 ng/kg/min.

Dosage form	INJECTABLE
Renal impairment	No specific GFR-based dose adjustment required; epoprostenol is not significantly renally excreted. Use with caution in severe renal impairment due to potential fluid overload.
Liver impairment	Child-Pugh Class A: No adjustment. Class B: Consider starting at lower dose (1 ng/kg/min) and titrate slowly. Class C: Use with caution; limited data, consider starting at 1 ng/kg/min.
Pediatric use	Initial: 2 ng/kg/min IV continuous infusion, titrate by 1-2 ng/kg/min every 15 minutes. Maximum dose not established; typical range 20-50 ng/kg/min.
Geriatric use	No specific dose adjustment; start at low end of dosing range (2 ng/kg/min) and titrate cautiously due to age-related comorbidities and reduced organ function.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for EPOPROSTENOL SODIUM (EPOPROSTENOL SODIUM).

Breastfeeding

It is unknown whether epoprostenol or its metabolites are excreted in human milk. M/P ratio is not available. Due to the short half-life (approximately 6 minutes) and intravenous administration, systemic exposure in nursing infants is expected to be low. Caution is advised; benefit of therapy should outweigh potential risk.

Teratogenic Risk

In animal studies, epoprostenol sodium did not demonstrate teratogenicity at up to 50 times the human dose. However, no adequate and well-controlled studies in pregnant women exist. Because epoprostenol is a potent vasodilator, it may increase the risk of maternal hypotension and reduced uteroplacental perfusion, potentially causing fetal harm. - First trimester: Limited data; risk cannot be excluded. - Second trimester: Theoretical risk of impaired placental blood flow. - Third trimester: Potential for fetal distress due to maternal hypotension.

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Chronic use in patients with heart failure due to reduced left ventricular function (NYHA Class III-IV)","Known hypersensitivity to epoprostenol or related compounds"]

Clinical Precautions

Precautions

["Should not be abruptly discontinued due to risk of rebound pulmonary hypertension","Careful dose titration required; monitor for hypotension and bleeding","Use with caution in patients with pulmonary veno-occlusive disease, as pulmonary edema may occur","May exacerbate heart failure due to decreased left ventricular preload"]

Clinical Tips & Counseling

Drug interactions

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EPOPROSTENOL SODIUM

Clinical safety rating: caution

Comprehensive clinical and safety monograph for EPOPROSTENOL SODIUM (EPOPROSTENOL SODIUM).

How it works

Prostacyclin (PGI2) analog; vasodilator and inhibitor of platelet aggregation via IP receptor activation, increasing cAMP in smooth muscle and platelets.

What the body does with it

Metabolism	Rapidly hydrolyzed at physiologic pH (t1/2 ~3-6 min); pH-dependent degradation; no significant hepatic metabolism.
Excretion	Renal (primarily as metabolites, <1% unchanged); biliary/fecal minimal.
Half-life	2-5 min (terminal); clinically administered via continuous IV infusion due to rapid elimination.
Protein binding	Approximately 60-70%, primarily to albumin.
Volume of Distribution	0.3-0.5 L/kg; confined primarily to intravascular space due to rapid metabolism.
Bioavailability	IV: 100%; inhaled: limited systemic absorption (approximately 10-20% of inhaled dose).
Onset of Action	IV: immediate (within 2-5 min); inhaled: 5-10 min.
Duration of Action	IV: 10-15 min post-infusion; inhaled: 30-60 min; continuous infusion required for sustained effect.

Classification & Brands

Dosing & administration

Initial: 2 ng/kg/min IV via continuous infusion, titrated by 1-2 ng/kg/min every 15 minutes or longer based on hemodynamic response. Typical maintenance: 20-40 ng/kg/min, range 10-50 ng/kg/min.

Dosage form	INJECTABLE
Renal impairment	No specific GFR-based dose adjustment required; epoprostenol is not significantly renally excreted. Use with caution in severe renal impairment due to potential fluid overload.
Liver impairment	Child-Pugh Class A: No adjustment. Class B: Consider starting at lower dose (1 ng/kg/min) and titrate slowly. Class C: Use with caution; limited data, consider starting at 1 ng/kg/min.
Pediatric use	Initial: 2 ng/kg/min IV continuous infusion, titrate by 1-2 ng/kg/min every 15 minutes. Maximum dose not established; typical range 20-50 ng/kg/min.
Geriatric use	No specific dose adjustment; start at low end of dosing range (2 ng/kg/min) and titrate cautiously due to age-related comorbidities and reduced organ function.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for EPOPROSTENOL SODIUM (EPOPROSTENOL SODIUM).

Breastfeeding

Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Chronic use in patients with heart failure due to reduced left ventricular function (NYHA Class III-IV)","Known hypersensitivity to epoprostenol or related compounds"]