Iloprost: Inhaled Prostacyclin

Iloprost is an inhalable form of prostacyclin, an analog (imitator) of our body's own vasodialator, prostaglandin. Prostaglandin prevents blood clots, and researchers believe that people with PH do not have enough of it. Thus prostacyclin, an artificial version of prostaglandin can help correct that imbalance. Studies have shown that in PH patients there is an abnormally low ratio of prostaglandin in relation to endogenous thromboxane A2 (a vasoconstrictor that serves the opposite function: stimulates platelet aggregation) that may be partially responsible for the development of pulmonary hypertension. Other prostacyclins such as epoprostenol (or Flolan) have been used to treat primary pulmonary hypertension with great sucess. Prostacyclins have been shown to improve survival rate, exercise capacity, and hemodynamics (blood circulation) of patients with severe PPH.

Iloprost is a stable form of prostacyclin that can be delivered via inhalation. The advantage of inhalation, is that the drug is introduced only to the lungs so that side effects that might affect the rest of the body are avoided.

Like Flolan (Epoprostenol), iloprost is very similar to naturally occurring prostaglandin with regard to its effect on blood vessels. When used intravenously its effects as well as its side effects are nearly identical to those of epoprostenol. Iloprost's chemical stability, however, is considerably superior.

Iloprost is stable at room temperature and is resistant to normal light, while in contrast, Flolan (Epoprostenol) has to be freshly dissolved, continuously cooled, and protected from light to preserve its full effectiveness. Iloprost has a 20-25 minute serum half-life in vivo, roughly five to six times longer than the quickly degenerating Epoprostenol.

The dosages used with continuous epoprostenol range between 10 and 50 ng/kg/min, while the dosages for continuous intravenous iloprost are much smaller and range between 1 and 5 ng/kg/min. This disparity is not yet fully understood by researchers believe it is probably due to the higher potency of iloprost and the efficacy of its delivery method.

Iloprost is effective and reduces shortness of breath, and may lower pulmonary pressures according to an August 2002 study that appeared in the New England Journal of Medicine, entitled, Inhaled Iloprost for Severe Pulmonary Hypertension. The study concluded: Inhaled iloprost is an effective therapy for patients with severe pulmonary hypertension.

So far Iloprost has only been approved for treatment of pulmonary arterial hypertension (PAH) in a few countries, and is not available for Primary Pulmonary Hypertension in the United States except through clinical trial.

See also: Ventavis



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