Hepatotoxic metabolite
- Marks a metabolite whose clinical significance IS its liver injury, not any receptor it binds
- Marks a metabolite whose clinical significance IS its liver injury, not any receptor it binds
- 4-ene-valproate is formed by CYP-mediated desaturation of valproate and is implicated in valproate hepatotoxicity
- Its formation rises with enzyme-inducing co-medication, which is part of why polytherapy raises the risk
Drugs with this mechanism (5)
- Dantrolene — Blocks RyR1 calcium release in skeletal muscle; the antidote for malignant hyperthermia.
- 4-ene-VPA — Unsaturated valproate metabolite implicated in mitochondrial dysfunction and liver toxicity; not a separate therapeutic drug.
- Isoniazid — First-line tuberculosis drug; hepatotoxicity and pyridoxine-responsive neuropathy shape use.
- Terbinafine — Oral antifungal of choice for nail infections; a CYP2D6 inhibitor.
- Zileuton — 5-lipoxygenase inhibitor that blocks leukotriene synthesis rather than a leukotriene receptor.
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