Methohexital

Brand Names: Brevital

Drug Class: Barbiturate anesthetic, Ultra-short-acting barbiturate

Overview

Methohexital is an ultra-short-acting barbiturate anesthetic agent used primarily for induction of anesthesia and for short surgical procedures. It produces rapid onset of hypnosis (within 30-60 seconds) with a short duration of action (5-7 minutes). It is administered intravenously and has no analgesic properties.

Mechanism of Action

Methohexital acts primarily as a GABA-A receptor agonist, enhancing inhibitory neurotransmission in the central nervous system. It increases the duration of chloride channel opening at GABA receptors, leading to neuronal hyperpolarization and CNS depression.

Indications

  • Induction of general anesthesia
  • Maintenance of anesthesia for short surgical procedures
  • As an adjunct in balanced anesthesia techniques

Dosage

IV administration only. Induction: 50-120 mg (1-1.5 mg/kg) given over 30-60 seconds. Maintenance: 20-40 mg every 4-7 minutes as needed. Maximum single dose: 600 mg. Maximum 24-hour dose: 2 g.

Contraindications

  • Absolute hypersensitivity to barbiturates
  • Acute intermittent porphyria
  • Status asthmaticus
  • Severe cardiovascular instability

Side Effects

  • Respiratory depression
  • Hypotension
  • Injection site pain
  • Hiccups
  • Sneezing
  • Coughing
  • Muscle twitching
  • Nausea/vomiting
  • Headache
  • Emergence delirium

Interactions

  • Enhanced CNS depression with other CNS depressants (alcohol, opioids, benzodiazepines)
  • Reduced effectiveness of oral anticoagulants
  • Decreased metabolism of other drugs metabolized by CYP450 enzymes
  • Increased risk of hypotension with antihypertensive agents