Methoxyflurane

Administration

  • Type: Analgesic, inhaled
  • Dosage Forms: inhaler (3 mL liquid for inhalation)
  • Dosage Strengths: 3 mL per inhaler
  • Routes of Administration: Inhaled
  • Common Trade Names: Penthrox

Adult Dosing

  • 3 mL inhaled via Penthrox inhaler, self-administered
  • May use up to 2 inhalers (6 mL) per day
  • Maximum: 6 mL per day, 15 mL per week

Pediatric Dosing

  • Age ≥12 years: same as adult dosing
  • Not recommended for children <12 years

Special Populations

Pregnancy Rating

  • Contraindicated

Lactation risk

  • Unknown; avoid use

Renal Dosing

  • Adult: Contraindicated in significant renal impairment
  • Pediatric: N/A

Hepatic Dosing

  • Adult: Contraindicated in significant hepatic impairment
  • Pediatric: N/A

Contraindications

  • Allergy to class/drug
  • Allergy to fluorinated anesthetics
  • History of malignant hyperthermia
  • Significant renal or hepatic impairment
  • Cardiovascular instability
  • Altered level of consciousness
  • Respiratory depression

Adverse Reactions

Serious

  • Nephrotoxicity (dose-dependent; risk with repeated/prolonged use)
  • Hepatotoxicity
  • Malignant hyperthermia (rare)

Common

  • Dizziness, drowsiness
  • Headache
  • Euphoria
  • Cough

Pharmacology

  • Half-life: Highly variable (lipophilic, stored in adipose tissue)
  • Metabolism: Hepatic (CYP450); produces nephrotoxic metabolites (fluoride, oxalic acid)
  • Excretion: Renal (metabolites), pulmonary (unchanged drug)

Mechanism of Action

  • Fluorinated methyl ethyl ether; exact analgesic mechanism unclear
  • Acts as a CNS depressant providing analgesia at sub-anesthetic concentrations

Comments

  • Used widely in Australia, New Zealand, and parts of Europe for ED and prehospital analgesia
  • FDA-approved in the US in 2024 for short-term relief of moderate-to-severe acute pain in conscious adults
  • Self-administered via a handheld inhaler; onset within 6-10 breaths
  • Provides analgesia without loss of consciousness
  • Must not exceed dose limits due to nephrotoxicity risk
  • Previously withdrawn as a general anesthetic due to renal toxicity at high doses; low-dose analgesic use has a favorable safety profile

Indications by Condition

The following table is automatically generated from disease/condition pages across WikEM.


See Also

References

Authors: