Dosing & Uses
Dosage Forms & Strengths
single-use ampule
- 10mcg/mL (1mL)
- 20mcg/mL (1mL)
Pulmonary Arterial Hypertension
Initial: 2.5 mcg inhaled, if well-tolerated, THEN
5 mcg subsequent doses
6-9 times/day PRN; >q2hr while awake
Maintenance: 2.5-5 mcg/dose; not to exceed 45 mcg/day
Systemic Sclerosis (Orphan)
Orphan designation for treatment of systemic sclerosis
Orphan sponsor
- Eicos Sciences, Inc., a CiVi Biopharma, Inc. affiliated company; 200 Four Falls Corporate Center, Suite 107; West Conshohocken, Pennsylvania 19528
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
Flushing (18%)
Cough (39%)
Hypotension (11%)
Nausea (13%)
Headache (30%)
Jaw pain (12%)
Trismus (12%)
1-10%
Palpitations (7%)
Syncope (8%)
Insomnia (8%)
Vomiting (7%)
Tongue pain (4%)
Back pain (7%)
Muscle cramps (6%)
GGT elevated (6%)
Hemoptysis (5%)
Pneumonia (4%)
<1%
Kidney failure
Bronchospasm
Hypersensitivity
Supraventricular tachycardia
Warnings
Contraindications
None well documented
Cautions
Iloprost has been listed by the FDA as one of the drugs to monitor after having identified potential signs of serious risks or new safety information in the agency's Adverse Event Reporting System (AERS) database during the last 3 months of 2011. Hemoptysis has been reported with iloprost use. The FDA said that it is not suggesting that clinicians should stop prescribing any drugs on the watch list, or that patients should stop taking them. It advises patients with questions about watch-list drugs to discuss them with their clinician.
Use caution in patients experiencing other types of pulmonary diseases (i.e. COPD)
Syncope may occur with pulmonary arterial hypertension, particularly with physical exertion (adjust dose and reassess efficacy)
Risk of syncope - monitor vital signs when initiating
Use cautioin in patients with bleeding disorders
Rebound hypertension may occur with dose reductions or withdrawals
Administered only via the Prodose® AAD® System
Not for use in patients with hypotension (systolic BP <85 mm Hg)
Discontinue immediately if signs of pulmonary edema
Bleeding events are most commonly reported as epistaxis or hemoptysis
Pregnancy & Lactation
Pregnancy
Limited published data from case series and case reports in pregnant women have not identified drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes; there are risks to mother and fetus associated with pulmonary arterial hypertension
Pulmonary arterial hypertension in pregnancy increases risk for maternal heart failure, stroke and death, miscarriage, preterm delivery, low birthweight infants, and stillbirth
Animal data
- In animal reproductive studies, administration of continuous intravenous therapy to pregnant Han-Wistar rats during organogenesis at doses 2-times recommended human dose on a mg/m2 basis resulted in adverse developmental outcomes
- However, there were no adverse developmental outcomes with intravenous administration of iloprost to pregnant Sprague- Dawley rats, rabbits and monkeys at doses 1200-, 180-, and 14-times, respectively, the recommended human dose on a mg/m2 basis
Lactation
There are no data on presence of iloprost in human milk, effects on breastfed infant, or on milk production; drug is present in rat milk; when drug present in animal milk, it is likely drug will be present in human milk
Because of potential for serious adverse reactions, advise women not to breastfeed during treatment
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Synthetic analog of prostagladin PGI2, dilates systemic & pulmonary arterial beds; suppresses vascular smooth muscle proliferation and alters pulmonary vascular resistance when used long term
Pharmacokinetics
Vd: 0.7-0.8 L/kg
Protein Bound: 60%
Duration: 30-60 min
Metabolism: Principally via beta-oxidation of carboxyl side-chain
Metabolite: Tetranor-iloprost (inactive)
Half-life: 20-30 min
Peak serum time: Within 5 min (following inhalation)
Excretion: Urine (68%); feces (12%)
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Patient Handout
Formulary
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