Iloprost, sold under the brand name Ventavis among others, is a medication used to treat pulmonary 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]
Quick Facts Clinical data, Trade names ...
Iloprost |
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Trade names | Ventavis, Ilomedine, Aurlumyn |
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AHFS/Drugs.com | Monograph |
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MedlinePlus | a612032 |
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Routes of administration | Inhalation, intravenous |
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Bioavailability | Not determined[1] |
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Protein binding | 60%[1] |
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Metabolism | Via β-oxidation to inactive tetranor-iloprost[1] |
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Elimination half-life | 20–30 minutes[1] |
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Excretion | Renal (68%) and fecal (12%)[1] |
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5-{(E)-(1S,5S,6R,7R)-7-hydroxy-6[(E)-(3S,4RS)-3-hydroxy-4-methyl-1-octen-6-ynyl]-bicyclo[3.3.0]octan-3-ylidene}pentanoic acid
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ECHA InfoCard | 100.163.887 |
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Formula | C22H32O4 |
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Molar mass | 360.494 g·mol−1 |
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CC#CCC(C)[C@@H](/C=C/[C@H]1[C@@H](C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)O
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InChI=1S/C22H32O4/c1-3-4-7-15(2)20(23)11-10-18-19-13-16(8-5-6-9-22(25)26)12-17(19)14-21(18)24/h8,10-11,15,17-21,23-24H,5-7,9,12-14H2,1-2H3,(H,25,26)/b11-10+,16-8+/t15?,17-,18+,19-,20+,21+/m0/s1 NKey:HIFJCPQKFCZDDL-ACWOEMLNSA-N N
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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 the pharmaceutical company Schering AG and is marketed by Bayer Schering Pharma AG in the European Union and by Actelion Pharmaceuticals in the US.
In the US, iloprost is indicated 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 US Food and Drug Administration approved iloprost (Aurlumyn) to treat severe frostbite to reduce the risk of finger or toe amputation.[2][5]
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%), and fainting (syncope) (8%); other serious adverse events reported with the use of Ventavis included congestive heart failure, chest pain, supraventricular tachycardia, dyspnea, swelling of the limbs (especially around the ankles and feet), and kidney failure.
Serious adverse events reported with the use of inhaled iloprost include congestive heart failure, chest pain, supraventricular tachycardia, shortness of breath, peripheral edema, and kidney failure.
- Olschewski H, Simonneau G, Galiè N, Higenbottam T, Naeije R, Rubin LJ, et al. (August 2002). "Inhaled iloprost for severe pulmonary hypertension". The New England Journal of Medicine. 347 (5): 322–329. doi:10.1056/NEJMoa020204. PMID 12151469.
- Meizer R, Meraner D, Meizer E, Radda C, Landsiedl F, Aigner N (January 2009). "Outcome of painful bone marrow edema of the femoral head following treatment with parenteral iloprost". Indian Journal of Orthopaedics. 43 (1): 36–39. doi:10.4103/0019-5413.45321 (inactive 24 April 2024). PMC 2739485. PMID 19753177.
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: CS1 maint: DOI inactive as of April 2024 (link)