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| Clinical data | |
|---|---|
| Trade names | Ventavis, Ilomedine, Aurlumyn |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a612032 |
| License data | |
| Routes of administration | Inhalation,intravenous |
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| Pharmacokinetic data | |
| Bioavailability | Not determined[1] |
| Protein binding | 60%[1] |
| Metabolism | Viaβ-oxidation to inactive tetranor-iloprost[1] |
| Eliminationhalf-life | 20–30 minutes[1] |
| Excretion | Kidney (68%) and fecal (12%)[1] |
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| CAS Number | |
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| DrugBank |
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| UNII | |
| KEGG |
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| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.163.887 |
| Chemical and physical data | |
| Formula | C22H32O4 |
| Molar mass | 360.494 g·mol−1 |
| 3D model (JSmol) | |
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Iloprost, sold under the brand nameVentavis among others, is amedication used to treatpulmonary arterial hypertension (PAH),scleroderma,Raynaud's phenomenon,frostbite, and other conditions in which the blood vessels are constricted and blood cannot flow to the tissues.[4] Iloprost is a prostacyclin mimetic.[1]
For pulmonary arterial hypertension, iloprost is given via inhalation. Iloprost works by opening (dilating) the blood vessels to allow the blood to flow through them. It was developed by thepharmaceutical companySchering AG and is marketed byBayer Schering Pharma AG in the European Union and byActelion Pharmaceuticals in the US.
In the US, iloprost isindicated for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) to improve a composite endpoint consisting of exercise tolerance, symptoms (NYHA Class), and lack of deterioration.[1]
In the EU, iloprost is indicated for the treatment of people with primary pulmonary hypertension, classified as New York Heart Association functional class III, to improve exercise capacity and symptoms.[3]
In February 2024, the USFood and Drug Administration (FDA) approved iloprost (Aurlumyn) to treat severe frostbite to reduce the risk of finger or toe amputation.[2][5]
Iloprost is a synthetic analogue ofprostacyclin PGI2. Iloprost dilates systemic and pulmonary arterialvascular beds. It also affectsplatelet aggregation but the relevance of this effect to the treatment of pulmonary hypertension is unknown. The twodiastereoisomers of iloprost differ in their potency in dilating blood vessels, with the 4S isomer substantially more potent than the 4R isomer. While Iloprost is an analog of PGI2 that activates PGI2's receptor, theprostacyclin receptor, to stimulate vasodilation, it has little selectivity in that it binds to and activates all four receptors forprostaglandin E2 viz.,prostaglandin EP1 receptor,prostaglandin EP2 receptor,prostaglandin EP3 receptor, andprostaglandin EP4 receptor.[6] Activation of theEP2 andEP4 receptors cause vasodilation but activation of theEP3 receptor causes vasoconstriction.
Contraindications include: unstable angina; within 6 months of myocardial infarction; decompensated cardiac failure (unless under close medical supervision); severe arrhythmias; congenital or acquired heart-valve defects; within 3 months of cerebrovascular events; pulmonary veno-occlusive disease; conditions which increase risk of bleeding.
In clinical studies, common adverse reactions due to inhaled iloprost included:vasodilation (flushing, 27%), cough (39%), headache (30%), flu syndrome (14%), nausea (13%),neck spasms (12%),hypotension (11%), insomnia (8%), andfainting (syncope) (8%); other serious adverse events reported with the use of Ventavis includedcongestive heart failure, chest pain, supraventriculartachycardia,dyspnea,swelling of the limbs (especially around the ankles and feet), andkidney failure.
Serious adverse events reported with the use of inhaled iloprost includecongestive heart failure, chest pain,supraventricular tachycardia,shortness of breath,peripheral edema, and kidney failure.
{{cite journal}}: CS1 maint: DOI inactive as of July 2025 (link)