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ethosuximide (Zarontin)

Tradename: Zarontin. Indications: 1) absence (petit mal) seizures 2) akinetic epilepsy Dosage: 1) 250 mg PO QD if 3-6 years of age 2) 500 mg PO QD > 6 years Tabs: 250 mg. Elixir: 250 mg/5 mL. Monitor: - liver function tests periodically [6] Adverse effects: 1) common (> 10%) - Stevens-Johnson syndrome, lupus-like syndrome, anorexia, ataxia, dizziness, drowsiness, hiccups, headache, nausea/vomiting, weight loss 2) less common (1-10%) - aggressiveness, depression, nightmares, weakness, fatigue 3) uncommon (< 1%) - agranulocytosis, leukopenia, aplastic anemia, thrombocytopenia, pancytopenia, paranoid psychosis, urticaria, exfoliative dermatitis 4) other: ataxia Drug interactions: 1) agents which may increase ethosuximide metabolism a) carbamazepine b) phenytoin c) primidone d) phenobarbital 2) valproic acid may increase or decrease ethosuximide levels 3) ethosuximide induces cyt P450 3A4 -> may diminish levels of drugs metabolized by cyt P450 3A4 4) isoniazid may inhibit hepatic metabolism of ethosuximide Test interactions: 1) may cause positive direct Coomb's test 2) may increase ANA titer 3) may increase serum AST Laboratory: 1) specimen: a) serum, plasma (heparin, EDTA) b) collect at trough concentration c) stable for several hours at room temperature d) stable for 1 year at -20 degrees C 2) methods: HPLC, GLC, EIA, FPIA 3) labs with Loincs - ethosuximide in body fluid - ethosuximide in serum/plasma

Interactions

drug interactions drug adverse effects of anticonvulsants monitor with anticonvulsants

General

anticonvulsant succinimide

Properties

COMPARTMENT: mitochondrial matrix MISC-INFO: elimination route LIVER KIDNEY 1/2life 24-72 HOURS 30-50 HOURS therapeutic-range 40-100 UG/ML toxic-range >150 UG/ML protein-binding <5% elimination by hemodialysis + pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

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 701
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
  5. Medical Knowledge Self Assessment Program (MKSAP) 15, American College of Physicians, Philadelphia 2009
  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