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Iloprost 2D structure.svg
Clinical data
Trade namesVentavis, Ilomedine
License data
Routes of
Inhaled; Intravenous
ATC code
Legal status
Legal status
  • US: ℞-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
BioavailabilityThe absolute bioavailability of inhaled iloprost has not been determined.[medical citation needed]
MetabolismIloprost is metabolized principally via β-oxidation of the carboxyl side chain. The main metabolite is tetranor-iloprost, which is found in the urine in free and conjugated form. In animal experiments, tetranor-iloprost was pharmacologically inactive.[medical citation needed]
Elimination half-life20–30 minutes[medical citation needed]
  • 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
CAS Number
PubChem CID
CompTox Dashboard (EPA)
ECHA InfoCard100.163.887 Edit this at Wikidata
Chemical and physical data
Molar mass360.494 g·mol−1
3D model (JSmol)
  • 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
  • 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 ☒N
 ☒NcheckY (what is this?)  (verify)

Iloprost is a medication used to treat pulmonary arterial hypertension (PAH), scleroderma, Raynaud's phenomenon and other diseases in which the blood vessels are constricted and blood cannot flow to the tissues. This damages the tissues and causes high blood pressure.[1] There is ongoing research into using it as a frostbite treatment.[2] Iloprost works by opening (dilating) the blood vessels to allow the blood to flow through again. It was developed by the pharmaceutical company Schering AG and is marketed by Bayer Schering Pharma AG in Europe and Actelion Pharmaceuticals in the USA. Iloprost is given via inhalation, and a therapeautic benefit of the drug is that a very low dose is required because of the deposition in the lung. Iloprost has few systemic side effects for that reason.

Clinical pharmacology

Iloprost is a synthetic analogue of prostacyclin PGI2. Iloprost dilates systemic and pulmonary arterial vascular beds. It also affects platelet aggregation but the relevance of this effect to the treatment of pulmonary hypertension is unknown. The two diastereoisomers 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, the prostacyclin receptor, to stimulate vasodilation, it has little selectivity in that it binds to and activates all four receptors for prostaglandin E2 viz., prostaglandin EP1 receptor, prostaglandin EP2 receptor, prostaglandin EP3 receptor, and prostaglandin EP4 receptor.[3] Activation of the EP2 and EP4 receptors cause vasodilation but activation of the EP3 receptor causes vasoconstriction.

Dosage and administration


In the U.S., iloprost is inhaled specifically using the I-Neb AAD or Prodose AAD delivery systems. In Europe iloprost has been approved for use with two compressed air nebulizers with AAD delivery systems (Halolite and Prodose) as well as with two ultrasonic nebulizers Ventaneb and I-Neb.

Ventavis is supplied in 1 mL single-use glass ampules containing either 10 μg/mL or 20 μg/mL. The 20 μg/mL concentration is intended for patients who are maintained at the 5 μg dose and who have repeatedly experienced extended treatment times which could result in incomplete dosing. Transitioning patients to the 20 μg/mL concentration using the I-neb AAD System will decrease treatment times to help maintain patient compliance.[4]

The approved dosing regimen for iloprost is 6 to 9 times daily (no more than every 2 hours) during waking hours, according to individual need and tolerability. The significant clinical effects observed in the pivotal study of patients with PAH were achieved with a median dose of 30 μg per day (range: 12.5 to 45 μg delivered at the mouthpiece), corresponding to 6 daily inhalations of 5 μg. The majority of patients (> 80%) in the pivotal study used this median dose or a higher dose with an excellent treatment compliance after 12 weeks.

The first inhaled dose of iloprost should be 2.5 μg (as delivered at the mouthpiece). If this dose is well tolerated, dosing should be increased to 5 μg and maintained at that dose. Any patient who cannot tolerate the 5 μg dose should be maintained at 2.5 μg.

Each inhalation treatment requires one entire single-use ampule. Each single-use ampule delivers a concentration of 10 μg/mL to the medication chamber of either the I-Neb AAD or Prodose AAD System, and delivers a nominal dose of either 2.5 μg or 5.0 μg to the mouthpiece. After each inhalation session, any solution remaining in the medication chamber should be discarded. Use of the remaining solution, even if the reservoir is "topped off" with fresh medication, will result in unpredictable dosing. Patients should follow the manufacturer's instructions for cleaning the I-Neb AAD or Prodose AAD System components after each dose administration.

Complete information regarding use of iloprost in specific populations (e.g. nursing mothers, pediatrics, patients with hepatic or renal impairment), drug interactions, and overdosage can be found in full prescribing information.


Vial and box of IV iloprost
Vial and box of IV iloprost

Iloprost is also available in an intravenous form, developed and marketed by Schering AG under the trade name Ilomedine.[5] IV iloprost is usually administered diluted, via a peripheral vein or central venous catheter. The diluted iloprost should be delivered by an accurate rate delivery system such as a syringe driver. Doses vary with individuals as side effects are better tolerated by some patients than others. The duration of the treatment is typically 3 days. This is usually repeated every 8 to 12 weeks.[1]


Common side effects

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.


See also


  1. ^ a b "Iloprost Information" (PDF). Archived from the original (PDF) on 2016-04-06. Retrieved 2009-02-05.
  2. ^ "Fewer amputations in Yukon, thanks to pioneering frostbite treatment".
  3. ^ Moreno JJ (2017). "Eicosanoid receptors: Targets for the treatment of disrupted intestinal epithelial homeostasis". European Journal of Pharmacology. 796: 7–19. doi:10.1016/j.ejphar.2016.12.004. PMID 27940058. S2CID 1513449.
  4. ^ Ventavis Prescribing Information 2009[dead link]
  5. ^ "BIJSLUITER: INFORMATIE VOOR DE GEBRUIK(ST)ER" (PDF). Retrieved 2009-02-05.[permanent dead link] (in Dutch)