VENTAVIS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for VENTAVIS (VENTAVIS).
Ventavis (iloprost) is a synthetic prostacyclin analog that causes vasodilation by increasing cyclic adenosine monophosphate (cAMP) levels in vascular smooth muscle cells, leading to relaxation and inhibition of platelet aggregation.
| Metabolism | Iloprost is metabolized primarily via beta-oxidation to inactive metabolites. Enzymes involved include acyl-CoA synthetases and other beta-oxidation enzymes. No significant CYP450 involvement. |
| Excretion | Renal: ~6% as unchanged drug; biliary/fecal: minimal; extensive hepatic metabolism with metabolites primarily excreted in urine (50-60% of total clearance). No significant renal or biliary excretion of parent drug. |
| Half-life | Terminal elimination half-life: 0.45–1.0 hour (intravenous). Short half-life necessitates continuous intravenous or frequent nebulized administration for sustained effect. |
| Protein binding | Approximately 60%; primarily to albumin (HSA). |
| Volume of Distribution | 0.36–0.48 L/kg (central volume); moderate distribution into tissues. |
| Bioavailability | Inhaled: ~30-40% (relative to intravenous); systemic absorption via lungs. |
| Onset of Action | Inhaled (via nebulizer): within 5 minutes; effect peaks at 15–30 minutes. Intravenous: rapid (seconds to minutes). |
| Duration of Action | Inhaled: 30–60 minutes (hemodynamic effects); requires dosing 6–9 times daily due to short duration. Intravenous: effect duration correlates with dosing interval; continuous infusion typically used. |
Inhaled: 2.5 mcg or 5 mcg via I-neb AAD system, 6 to 9 times daily (maximum 45 mcg/day). Titrate based on response and tolerability.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No specific guidelines; use with caution in severe hepatic impairment (Child-Pugh C) due to limited data. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment; monitor for tolerability due to potential age-related comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for VENTAVIS (VENTAVIS).
| Breastfeeding | It is not known whether iloprost is excreted in human milk. Due to the potential for serious adverse reactions in nursing infants, a decision should be made to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother. M/P ratio is not established. |
| Teratogenic Risk | FDA Pregnancy Category C. In animal studies, iloprost (the active ingredient) was teratogenic at doses higher than the maximum recommended human dose. There are no adequate and well-controlled studies in pregnant women. Potential fetal risks include skeletal abnormalities and increased post-implantation loss. Risk cannot be ruled out; use only if potential benefit justifies potential risk to the fetus. |
■ FDA Black Box Warning
Ventavis is intended for inhalation only via the I-neb AAD system or the Prodose AAD system; fatal events may occur if administered intravenously.
| Serious Effects |
History of hypersensitivity to iloprost or any component of the formulation; patients with systolic blood pressure <85 mmHg; patients with conditions that might increase the risk of hemorrhage (e.g., active bleeding, peptic ulcer disease, trauma, or intracranial hemorrhage).
| Precautions | Risk of syncope and hypotension; use caution in patients with systolic blood pressure <85 mmHg. Avoid abrupt discontinuation. Use with caution in patients with hepatic impairment (Child-Pugh class B or C) or renal impairment (creatinine clearance <30 mL/min). Not recommended for use in patients with pulmonary veno-occlusive disease. |
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| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and signs of pulmonary hypertension exacerbation. Fetal monitoring includes ultrasound for fetal growth and amniotic fluid volume, and nonstress testing as clinically indicated. Assess for signs of preterm labor. Monitor for maternal bleeding risk due to antiplatelet effects. |
| Fertility Effects | No specific human studies on fertility. In animal studies, no adverse effects on fertility were observed at clinically relevant doses. Theoretical risk of impact on implantation due to vasodilatory effects; however, data are insufficient to draw conclusions. |