Iloprost

Brand Names: Aurlumyn

Drug Class: Prostacycline

Overview

11 DESCRIPTION AURLUMYN contains iloprost, a synthetic analog of prostacyclin PGI 2 . The chemical name for iloprost is (5 E )-[3a S ,4 R ,5 R ,6a S )-5-hydroxy-4-[(1 E )-(3 S ,4 RS )-3-hydroxy-4-methyloct-1-en-6-ynyl]-hexahydropentalen-2(1 H )-ylidene]pentanoic acid. Iloprost consists of a mixture of the 4R and 4S diastereoisomers at a ratio of approximately 53:47.

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Iloprost is a synthetic analog of prostacyclin PGI 2 . Iloprost is a vasodilator and inhibits platelet aggregation. 12.3 Pharmacokinetics General Iloprost administered intravenously has linear pharmacokinetics over the dose range of 1 to 3 ng/kg/min. The half-life of iloprost is 20 to 30 minutes. Absorption and Distribution Following intravenous infusion, the apparent steady-state volume of distribution was 0.7 to 0.8 L/kg in healthy subjects. Iloprost is approximately 60% protein-bound, mainly to albumin, and this ratio is concentration-independent in the range of 30 to 3000 pg/mL. Metabolism and Excretion In vitro studies reveal that cytochrome P450-dependent metabolism plays only a minor role in the biotransformation of iloprost.

Indications

  • 1 INDICATIONS AND USAGE AURLUMYN is a prostacyclin mimetic indicated for the treatment of severe frostbite in adults to reduce the risk of digit amputations. Effectiveness was established in young, healthy adults who suffered frostbite at high altitudes ( 1.1 ). 1.1 Frostbite AURLUMYN is indicated for the treatment of severe frostbite in adults to reduce the risk of digit amputations. Effectiveness was established in young, healthy adults who suffered frostbite at high altitudes.

Common Doses

  • 30 mL
  • 1 mL
  • 100 mcg
  • 100 mL

Dosage

2 DOSAGE AND ADMINISTRATION Initiate intravenous infusion at 0.5 ng/kg/minute and titrate in 0.5 ng/kg/minute increments based on tolerability at intervals of 30 minutes to a maximum of 2 ng/kg/minute ( 2.1 ). Administer as continuous infusion for 6 hours each day up to a maximum of 8 consecutive days ( 2.1 ). Patients with moderate or severe hepatic impairment (Child-Pugh Class B or C): initiate infusion at 0.25 ng/kg/minute and titrate as described above ( 2.3 ). Patients with renal impairment with eGFR less than 30 mL/min: initiate infusion at 0.

Contraindications

  • 4 CONTRAINDICATIONS None. None ( 4 ).

Side Effects

  • 6 ADVERSE REACTIONS Most common adverse events include headache, flushing, palpitations/tachycardia, nausea, vomiting, dizziness, and hypotension (6.1). To report SUSPECTED ADVERSE REACTIONS, contact BTG International, Inc. at 1-877-377-3748 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Studies Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Interactions

  • No major interactions listed on the FDA label. Always consult a healthcare professional.