Drug Groups

approved; investigational

Description

Iloprost is a synthetic analogue of prostacyclin PGI2. Iloprost dilates systemic and pulmonary arterial vascular beds. It is used to treat pulmonary arterial hypertension (PAH).

Indication

Used for the treatment of pulmonary arterial hypertension.

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.

Toxicity

Overdoses can lead to hypotension, headache, flushing, nausea, vomiting, and diarrhea.

Affected Organisms

Biotransformation

Primarily hepatic. Iloprost is metabolized principally via beta-oxidation of the carboxyl side chain.

Absorption

Rapidly absorbed with bioavailability of 63%

Half Life

20-30 minutes

Protein Binding

60%

Distribution

* 0.7 to 0.8 L/kg

Clearance

* 20 mL/min/kg [Normal subjects]

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