Iloprost

Iloprost Brand Name– Ventavis

What is Iloprost

Iloprost is an inhaled prostaglandin approved for the treatment of pulmonary hypertension.

It is a stable, second generation structural analog of the endogenous prostaglandin prostacyclin, with a potency which is ten-fold greater than first generation stable analogs (i.e., carbaprostacyclin). Intravenous prostacyclin was the first drug shown to reduce mortality in controlled trials in patients with severe pulmonary hypertension.

However, the agent requires continuous IV infusion and the effects are non-specific resulting in a lack of pulmonary specificity and peripheral vasodilation.

The advantage of iloprost is the ability of the drug to be given via inhalation aerosol, which may improve patient compliance and satisfaction.

The inhalation formulation also results in less systemic absorption and therefore has potential for an improved safety profile compared to intravenous prostacyclin analogs.

Compared to epoprostenol, iloprost has a longer elimination half-life, allowing intermittent dosing by the inhaled route.

Iloprost has advantages over inhaled nitrous oxide (N₂O). Inhaled nitrous oxide has less potent vasodilatory activity than prostacyclin in the pulmonary vasculature, and may result in rebound pulmonary hypertension if therapy is interrupted.

In a controlled clinical trial, inhalations of iloprost (inhaled 6—9 times per day with a median total daily dose 30 mcg/day) were compared with placebo in adult patients (n=203) with severe pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension (NYHA functional class III or IV).

Of patients receiving iloprost, 16.8% showed significant improvement in symptoms (noted by improvement by at least one NYHA class level), and improvements in exercise tolerance (>= 10% increase in 6-minute walking distance), compared with 4.9% of patients receiving placebo at the 3 month time period. Inhaled iloprost (Ventavis) was approved by the FDA for the treatment of pulmonary arterial hypertension (PAH) in adults in December 2004.

Indications

• pulmonary hypertension

For the treatment of pulmonary hypertension (pulmonary arterial hypertension WHO Group 1) to improve a composite endpoint consisting of exercise tolerance, symptoms (NYHA Class), and lack of deterioration

Side Effects

1. back pain
2. bronchospasm
3. chest pain (unspecified)
4. cough
5. diarrhea
6. dizziness
7. dysgeusia
8. dyspnea
9. elevated hepatic enzymes
10. epistaxis
11. flushing
12. headache
13. heart failure
14. hemoptysis
15. hypotension
16. influenza
17. insomnia
18. muscle cramps
19. nausea
20. palpitations
21. peripheral edema
22. peripheral vasodilation
23. rash
24. renal failure (unspecified)
25. supraventricular tachycardia (SVT)
26. syncope
27. thrombocytopenia
28. trismus
29. vomiting
30. wheezing

Monitoring Parameters

• arterial blood gases (ABGs)
• INR

Contraindications

• asthma
• breast-feeding
• children
• chronic obstructive pulmonary disease (COPD)
• driving or operating machinery
• geriatric
• hepatic disease
• hypotension
• ocular exposure
• pregnancy
• pulmonary edema
• renal failure
• renal impairment
• respiratory infection
• syncope

Interactions

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