Carbamazepine
Carbamazepine. Voltage-gated sodium-channel blocker — first-line for partial epilepsy + trigeminal neuralgia. Potent CYP3A4 + CYP2C9 + UGT auto-inducer (own ke rises…
Voltage-gated sodium-channel blocker — first-line for partial epilepsy + trigeminal neuralgia. Potent CYP3A4 + CYP2C9 + UGT auto-inducer (own ke rises 2-3× by week 4). HLA-B*1502 + Asian ancestry → SJS/TEN risk. Major DDI source.
PK REMOVED. THE RECORD ALREADY CONTRADICTED ITSELF: its mechanism string says the drug own elimination rate "rises 2-3x by week 4" while half_life_hr stored the treatment-naive 33 h, so the simulator over-predicted exposure two- to threefold for every patient actually taking it. Three independent disqualifiers, any one sufficient. AUTOINDUCTION, measured in the same subjects with deuterium-labelled drug: "After 17 to 32 days of treatment, the plasma clearance of CBZ-D4 was doubled", and "During multiple dosing, the half-life is decreased to 10-20 hours" from about 35 — no single elimination rate exists. AN ACTIVE METABOLITE: the 10,11-epoxide has "anticonvulsant activity comparable with that of the parent drug" and runs "between 5 and 81%" of parent concentration — no single analyte. AND A FORMULATION-DOMINATED BIOAVAILABILITY spanning about 25% for tablets to essentially complete for solution. The stored t-half 33 was itself verbatim and correctly attributed; that is the point. ka 0.3 was a back-derivation reproducing the same paper own 9.3 h peak. Its three interaction references are untouched.
Related compounds
- Warfarin — major
- Cyclosporine — major
- Simvastatin — major
- Midazolam — major
- Hormonal contraceptives — warn
- Ethinyl Estradiol — warn
Sources: PMID:14691614, PMID:8598183, PMID:2126946, PMID:3734137, PMID:346287, PMID:2344850