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felbamate (Felbatol)

Tradename: Felbatol. Indications: 1) monotherapy & adjunctive therapy in patients > 14 years of age with partial & secondary generalized seizures 2) adjunctive therapy in patients > 2 years of age with partial & generalized Lennox-Gastaut syndrome 3) reserve drug for patients with severe symptoms NOT responsive to other, less toxic agents 4) intractable seizures [4] Contraindications: - avoid in patients with liver failure [7] Dosage: 1) Start 400 mg PO TID, max 3.6 g/day 2) Pediatrics: Start 15 mg/kg/day, max 45 mg/kg/day 3) do NOT discontinue abruptly Tabs: 400 & 600 mg. Suspension: 600 mg/5 mL. Dosage adjustment in renal failure: - yes - supplemental dose after dialysis uncertain [7] Monitor: 1) complete blood count (CBC) baseline, weekly during therapy & for 4 weeks after discontinuation [6] 2) liver function tests (LFTs)baseline & weekly Adverse effects: 1) common (> 10%) - nausea, anxiety, headache, fatigue, dizziness, diarrhea, anorexia, weight loss, vomiting, constipation, cough 2) less common (1-10%) - drowsiness, insomnia, blurred or double vision, clumbsiness, weight gain, depression, behavioral changes, clouded sensorium, lethargy, muscle twitches, slurred speech, uncontrollable eye movements, acne, skin rash 3) uncommon (< 1%) - alopecia, bleeding gums, gingival hyperplasia 4) other (serious) a) aplastic anemia (marked increased incidence) b) hepatotoxicity Drug interactions: 1) felbamate increases levels of phenytoin, valproic acid 2) felbamate decreases carbamazepine level, but increases epoxide 3) phenytoin & carbamazepine decrease felbamate levels Mechanism of action: 1) potentiates GABA receptor-linked Cl- channels 2) inhibits spontaneous discharges from voltage-dependent Na+ channels 3) inhibits NMDA receptors 4) inhibits AMPA receptors [5]

Interactions

drug interactions drug adverse effects of anticonvulsants monitor with anticonvulsants

General

anticonvulsant

Properties

MISC-INFO: elimination route KIDNEY LIVER 1/2life 20-23 HOURS protein-binding 25% pregnancy-category C safety in lactation -

Database Correlations

PUBCHEM cid=3331

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Harrison's Principles of Internal Medicine, 13th ed. Companion Handbook. Isselbacher et al (eds), McGraw-Hill Inc. NY, 1995, pg 702
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Department of Veterans Affairs, VA National Formulary - restricted to neurology
  5. UpToDate 13.3 http://www.utdol.com
  6. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com
  7. Medical Knowledge Self Assessment Program (MKSAP) 17, American College of Physicians, Philadelphia 2015