remifentanyl (Ultiva)

Introduction

Tradename: Ultiva. DEA-controlled substance: class 2

Indications

• analgesic component of monitored general anesthesia
• treatment of acute pain

Contraindications

(& cautions)

• NOT for epidural/intrathecal administration due to glycine component
• due to potency of drug, clear all IV lines which may contain drug prior to step-down care
• concurrent use of MAO inhibitors is contraindicated
• endotracheal intubation: inferior to neuromuscular blockers

Dosage

• general anesthesia:
  • induction: 0.5-1 ug/kg IV over 30-60 seconds
  • maintenance: 0.05-2.0 ug/kg/minute IV infusion

Pharmacokinetics

• rapid onset of action
• metabolized by blood & tissue esterase
• 95% metabolized to an inactive metabolite that is cleared by the kidney
• 1/2life is 3-10 minutes
• recovery is 5-10 mintues

elimination via plasma

1/2life = 3-10 minutes

Adverse effects

• rash
• headache
• shivering
• bradycardia
• hypotension
• nausea/vomiting
• respiratory depression (dose-related)
• drowsiness
• constipation
• muscle rigidity (dose & rate-related)

Drug interactions

• benzodiazepines, barbiturates, alcohol in combination increase adverse CNS effects
• MAO inhibitors in combination is contraindicated: fatal reactions have occurred
• naloxone is a direct opiate antagonist
• scorpion venom in combination increases toxic effects of the venom

Mechanism of action

• opiate agonist
• phenylpiperidine derivative
• 5-10 times as potent as fentanyl

More general terms

• opiate

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=60814
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=60815