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Desflurane Pathway, Pharmacokinetics

PA166232762 Last updated March 2021 Caroline F. Thorn
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Desflurane Pathway, Pharmacokinetics pathway diagram
Desflurane Pathway, Pharmacokinetics — pathway diagram from PharmGKB / ClinPGx
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About this pathway

Background

Desflurane, enflurane, halothane, isoflurane, methoxyflurane, and sevoflurane are fluorinated inhaled anesthetics contraindicated in patients with variants in RYR1 and CACNA1S see CPIC guideline for volatile anesthetic agents and succinylcholine in the context of RYR1 or CACNA1S genotypes [Article:30499100]. These genes and variants are involved with the pharmacodynamics side effects of the drugs. Halothane, and to a lesser degree the other volatile anesthetics, have been associated with fatal hepatic necrosis [Article:18509326]. It is generally considered that the extent of metabolism correlates with the toxicity: halothane being the most extensively metabolized, then methoxyflurane > sevoflurane > enflurane > isoflurane > desflurane [Articles:8214760, 18509326].

Metabolism

Desflurane is minimally metabolized by CYP2E1 to trifluoroacetic acid (TFA). Fluoride ion formation from the in vitro metabolism of desflurane is considered minimal [Article:8214760]. Approximately 0.02–0.2% of desflurane is metabolized [Article:18509326]. Desflurane metabolism produces very low levels of TFA-protein conjugates and anti-TFA antibodies and incidences of immune hepatitis are very rare [Article:18509326].

Reactions & interactions (2)

  • Biochemical Reaction
    desflurane fluoride + trifluoroacetic acid
  • Catalysis
    CYP2E1 Biochemical Reaction

Edit history (1)

  • 2021-03-16 Create
Desflurane Pathway, Pharmacokinetics pathway diagram (enlarged)