indication

For use in the induction and maintenance of general anesthesia

pharmacology

Methoxyflurane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential.

mechanism of action

Methoxyflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Methoxyflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. It also appears to bind the D subunit of ATP synthase and NADH dehydogenase. Methoxyflurane also binds to the GABA receptor, the large conductance Ca²⁺ activated potassium channel, the glutamate receptor and the glycine receptor.

toxicity

LD₅₀=3600 mg/kg (Orally in rats). Symptoms of overexposure include eye irritation, CNS depression, analgesia, anesthesia, seizures, respiratory depression, and liver and kidney damage.

biotransformation

Hepatic.

drug interactions

Demeclocycline: The tetracycline, demeclocycline, may increase the renal toxicity of methoxyflurane.

Minocycline: The tetracycline, minocycline, may increase the renal toxicity of methoxyflurane.

Phenobarbital: The barbiturate, phenobarbital, increases the renal toxicity of methoxyflurane.

Primidone: The barbiturate, primidone, increases the renal toxicity of methoxyflurane.

Tetracycline: Tetracycline may increase the renal toxicity of methoxyflurane.