oxcarbazepine TRILEPTAL

Class: AED/​Mood Stabilizer
FDA Indications: Partial Seizures
Off-Label Use: Restless Leg Syndrome, Neuropathic Pain, Bipolar Disorder
Prescribing
Forms: 150, 300, 600mg tablet; 300 mg/5 mL po soln
Dose Range: 600-2400 mg/day
Starting: 300 mg bid; usual daily dose is 1200 mg/day in 2 divided doses; dosage ↑'s are made Q3 days in increments of 150 mg or 300 mg depending on weight and tolerability
Stopping: Taper. Abrupt discontinuation can elicit seizures and increase the risk of relapse in bipolar patients
Monitoring: Serum Na+ for 1st 3 mos b/c of possibility of hyponatremia

NAMI drug fact sheet

Precautions
Serious Side Effects: Hyponatremia (2.5%)
Side Effects: headache, ataxia, visual changes, tremor, nausea, fatigue, vomiting, nystagmus, diplopia, dizziness (20-49%), drowsiness (12-36%)
Pharmacodynamics
1° MOA: Binds to a site located within the open channel conformation of the VSSC α subunit, which decreases repetitive firing and spread of electrical activity
Pharmacokinetics
t½: 7-20° TMAX: 4.5°
Substrate of: AKR (oxcarbazepine→MHD), UGT (MHD→inactive metabolites→renal elimination)
Inhibits: 2C19; Induces: 3A4, UGT1A4
Active Metabolites: MHD
DDIs
  • - ↑'s levels of phenytoin
  • - ↓'s levels of lamotrigine & topiramate
  • - ↓'s levels of ethinylestradiol & levonorgestrel
Misc
  • - oxcarbazepine is a prodrug that is virtually entirely converted into MHD (by cytosolic AKR), which is responsible for the pharmacological effect of the drug
  • - unlike carbamazepine, MHD does not cause autoinduction of its own metabolism
  • - t½ of parent drug is 1-5°; t½ of MHD is 7-20°
  • - low potential for drug interactions
  • - compared to carbamazepine, less sedating, has less bone-marrow toxicity, and has fewer CYP3A4 interactions
Special Populations

Category C—Limited Human Data–Animal Data Suggest Risk: is embryo and fetal toxic and teratogenic in some animal species

Limited Human Data–Probably Compatible


No adjustments required


No dosage adjustment required in mild-moderate impairment, but should be initiated at ½ the usual starting dose in severe impairment (CrCl <30 mg/min)

No dose adjustment is needed for hepatically impaired subjects

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Last updated August 27 2018 18:45:06. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.