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Drugs reference index «Iloprost»

Iloprost
Iloprost


Iloprost

Pronunciation: (EYE-low-prost)Class: Prostacyclin analog

Trade Names:Ventavis- Inhalation solution 20 mcg

Pharmacology

Dilates systemic and pulmonary arterial vascular beds.

Pharmacokinetics

Absorption

Absolute bioavailability of inhaled iloprost has not been determined. Following a 5 mcg inhalation, the C max is approximately 150 pg/mL in patients with pulmonary hypertension.

Distribution

Vd after IV infusion is 0.7 to 0.8 L/kg. Protein binding is approximately 60%, primarily to albumin.

Metabolism

Metabolized primarily by beta-oxidation of the carboxyl side chain to tetranoriloprost. The CYP-450 plays a minor role in iloprost metabolism.

Elimination

The t ½ is 20 to 30 min. Elimination is 68% in urine and 12% in feces.

Indications and Usage

Treatment of pulmonary arterial hypertension.

Unlabeled Uses

IV administration for treatment of severe Raynaud phenomenon associated with systemic sclerosis.

Contraindications

Standard considerations.

Dosage and Administration

Adults

Inhalation Start with 2.5 mcg (as delivered to the mouthpiece). If this dose is tolerated, increase dosing to 5 mcg and maintain that dose. Take 6 to 9 times/day but not more often than every 2 h (max, 45 mcg/day).

General Advice

  • For aerosol administration only. Not for parenteral or oral administration.
  • Do not administer iloprost inhalation solution with any aerosol-generating device other than the I-neb Adaptive Aerosol Delivery (AAD) or Prodose AAD system, or together with other aerosolized medications.
  • Do not allow iloprost solution to come into contact with the skin or eyes. If accidental skin or eye contact occurs, flush exposed areas with water.
  • Two ampule configurations, a 2 mL and 1 mL single-use glass ampule each containing 10 mcg per 1 mL, are available.
  • The 1 mL single-use ampule delivers 10 mcg to the medication chamber and must only be used with the I-neb AAD system.
  • The 2 mL single-use ampule delivers 20 mcg to the medication chamber of either of the AAD delivery systems. The 2 mL must be used with the Prodose AAD system and may be used with the I-neb AAD system.
  • The 2 mL and 1 mL ampules deliver a nominal dose of either 2.5 mcg or 5 mcg at the mouthpiece of the AAD delivery system for which they are labeled for use.
  • Each inhalation treatment requires 1 single-use ampule.
  • For each inhalation session, transfer the entire contents of 1 opened ampule into either the I-neb AAD system or the Prodose AAD system medication chamber (2 mL ampule only) immediately before use.
  • Open ampule by holding bottom of ampule with blue dot facing away from body, wrapping the included rubber pad around the entire ampule using other hand; then, using thumbs, break open the neck of the ampule by snapping the top of the ampule toward the body.
  • Administer iloprost according to instructions provided by the manufacturer for use with the I-neb AAD or Prodose AAD system.
  • Discard any remaining solution in the medication chamber following each inhalational session. Use of remaining solution for next inhalational session will result in unpredictable dosing.
  • Follow manufacturer instructions for cleaning the I-neb AAD or Prodose AAD system components after each inhalational session.

Storage/Stability

Store unopened ampules at controlled room temperature (59° to 86°F).

Drug Interactions

Anticoagulants

Because iloprost inhibits platelet function, the risk of bleeding may be increased.

Antihypertensive agents, vasodilators

The hypotensive effects of these agents may be increased by iloprost.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Vasodilation/flushing (27%); hypotension (11%); syncope (8%); palpitations (7%); chest pain, CHF, supraventricular tachycardia.

CNS

Headache (30%); insomnia (8%).

GI

Nausea (13%); vomiting (7%).

Genitourinary

Kidney failure.

Lab Tests

Increased alkaline phosphatase, increased gamma-glutamyltransferase (6%).

Musculoskeletal

Trismus (12%); back pain (7%); muscle cramps (6%).

Respiratory

Increased cough (39%); hemoptysis (5%); pneumonia (4%); dyspnea.

Miscellaneous

Flu syndrome (14%); tongue pain (4%); peripheral edema.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use with caution, usually starting at the low end of the dosage range because of the greater frequency of decreased cardiac, hepatic, or renal function, and of concomitant diseases or other drug therapy.

Renal Function

Use with caution in patients on dialysis.

Hepatic Function

Use with caution.

Special Risk Patients

Use has not been evaluated in patients with pulmonary hypertension, COPD, severe asthma, or acute pulmonary infections.

Pulmonary edema

Stop treatment immediately if pulmonary edema occurs when administered to patients with pulmonary hypertension; this may be a sign of pulmonary venous hypotension.

Syncope

Syncope may occur. Use with caution in patients with low systemic BP to avoid further hypotension; do not use in patients with systolic BP less than 85 mm Hg.

Overdosage

Symptoms

Extension of the pharmacologic effects, including diarrhea, flushing, headache, hypotension, nausea, and vomiting.

Patient Information

  • Advise patient or caregiver to use iloprost only as prescribed with the I-neb AAD or Prodose AAD system, pulmonary drug delivery devices, following the manufacturer instructions.
  • Ensure patient or caregiver has been trained in proper administration techniques, including dosing frequency, opening ampules, transferring solution, disposal of empty ampule, I-neb AAD or Prodose AAD system operation, and equipment cleaning and maintenance.
  • To avoid interruptions in therapy caused by equipment malfunction, ensure patient or caregiver has easy access to a backup I-neb AAD or Prodose AAD system.
  • Caution patient or caregiver to avoid oral ingestion or skin or eye contact with iloprost. Advise patient if accidental skin or eye contact occurs to flush the exposed area with water.
  • Caution patient or caregiver not to put any other medications in the I-neb AAD or Prodose AAD system while using iloprost.
  • Advise patient or caregiver that iloprost should be inhaled at intervals of no less than 2 h and that the beneficial effects of iloprost may not last 2 h. Caution patient or caregiver against increasing the frequency of administration if beneficial effects do not last the entire time between treatments.
  • Caution patient not to change the dose or stop taking unless advised by health care provider.
  • Caution patient or caregiver that BP may fall during or shortly after iloprost administration and that dizziness or fainting can occur. Advise patient to stand up slowly when getting out of a chair or bed. Advise patient or caregiver to notify health care provider if dizziness gets worse or if fainting occurs.
  • Advise patient or caregiver that the most common side effects of iloprost therapy (aside from low BP and fainting) include reddening of the face caused by widening of blood vessels (flushing), increased cough, headache, nausea, and spasms of the jaw muscles that cause trouble opening the mouth. Advise patient or caregiver to notify health care provider if any of these develop and are intolerable.

Copyright © 2009 Wolters Kluwer Health.

  • Iloprost MedFacts Consumer Leaflet (Wolters Kluwer)
  • iloprost Inhalation, oral/nebulization Advanced Consumer (Micromedex) - Includes Dosage Information
  • Ventavis Prescribing Information (FDA)
  • Ventavis Consumer Overview

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