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Pronunciation |
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(eth
oh SUKS i
mide) |
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U.S. Brand
Names |
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Zarontin® |
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Generic
Available |
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Yes |
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Pharmacological Index |
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Anticonvulsant, Succinimide |
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Use |
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Management of absence (petit mal) seizures |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to ethosuximide |
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Warnings/Precautions |
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Use with caution in patients with hepatic or renal disease; abrupt withdrawal
of the drug may precipitate absence status; ethosuximide may increase
tonic-clonic seizures in patients with mixed seizure disorders; ethosuximide
must be used in combination with other anticonvulsants in patients with both
absence and tonic-clonic seizures |
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Adverse
Reactions |
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Central nervous system: Ataxia, drowsiness, sedation, dizziness, lethargy,
euphoria, headache, irritability, hyperactivity, fatigue, night terrors,
disturbance in sleep, inability to concentrate, aggressiveness, mental
depression, paranoid psychosis
Dermatologic: Stevens-Johnson syndrome, SLE, rash, hirsutism
Endocrine & metabolic: Increased libido
Gastrointestinal: Weight loss, gastric upset, cramps, epigastric pain,
diarrhea, nausea, vomiting, anorexia, abdominal pain
Genitourinary: Vaginal bleeding, microscopic hematuria
Hematologic: Leukopenia, agranulocytosis, pancytopenia, eosinophilia
Ocular: Myopia
Miscellaneous: Hiccups |
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Overdosage/Toxicology |
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Acute overdose can cause CNS depression, ataxia, stupor, coma, hypotension.
Chronic overdose can cause skin rash, confusion, ataxia, proteinuria, hepatic
dysfunction, and hematuria. Treatment is supportive. Hemoperfusion and
hemodialysis may be useful. |
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Drug
Interactions |
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CYP3A3/4 enzyme substrate; CYP3A3/4 enzyme inducer
Isoniazid may inhibit hepatic metabolism of ethosuximide with a resultant
increase in ethosuximide serum concentrations
Ethosuximide may elevate phenytoin levels
Valproate acid has been reported to both increase and decrease ethosuximide
levels |
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Mechanism of
Action |
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Increases the seizure threshold and suppresses paroxysmal spike-and-wave
pattern in absence seizures; depresses nerve transmission in the motor
cortex |
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Pharmacodynamics/Kinetics |
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Serum half-life:
Children: 30 hours
Adults: 50-60 hours
Time to peak serum concentration:
Capsule: Within 2-4 hours
Syrup: <2-4 hours |
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Usual Dosage |
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Oral:
Children >6 years and Adults: Initial: 250 mg twice daily; increase by 250
mg as needed every 4-7 days up to 1.5 g/day in 2 divided doses; usual
maintenance dose: 20-40 mg/kg/day in 2 divided doses |
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Dietary
Considerations |
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Increase dietary intake of folate; may be administered with food or milk;
alcohol: additive CNS depression has been reported with succimides; avoid or
limit alcohol |
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Administration |
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Take with food or milk to avoid GI upset |
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Mental Health: Effects
on Mental Status |
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May cause sedation, euphoria, insomnia, or hallucinations; may rarely cause
depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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Barbiturates and carbamazepine may decrease the clinical effects of
ethosuximide |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take exactly as directed (do not increase dose or frequency or discontinue
without consulting prescriber). While using this medication, do not use alcohol
and other prescription or OTC medications (especially pain medications,
sedatives, antihistamines, or hypnotics) without consulting prescriber. Maintain
adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid
intake). You may experience drowsiness, dizziness, or blurred vision (use
caution when driving or engaging in tasks requiring alertness until response to
drug is known); nausea, vomiting, loss of appetite, or dry mouth (small frequent
meals, frequent mouth care, chewing gum, or sucking lozenges may help);
constipation (increased exercise, fluids, or dietary fruit and fiber may help).
Wear identification of epileptic status and medications. Report CNS changes,
mentation changes, or changes in cognition; muscle cramping, weakness, tremors,
or changes in gait; persistent GI symptoms (cramping, constipation, vomiting,
anorexia); rash or skin irritations; unusual bruising or bleeding (mouth, urine,
stool); worsening of seizure activity, or loss of seizure control. Pregnancy
precautions: Inform prescriber if you are or intend to be
pregnant. |
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Nursing
Implications |
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Monitor CBC, platelets, liver enzymes, trough ethosuximide serum
concentration; observe patient for excess sedation; maintain serum levels;
monitor for bruising and bleeding |
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Dosage Forms |
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Capsule: 250 mg
Syrup (raspberry flavor): 250 mg/5 mL (473 mL) |
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References |
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Marbury TC, Lee CS, Perchalski RJ, et al,
"Hemodialysis Clearance of Ethosuximide in Patients With Chronic Renal Disease,"
Am J Hosp Pharm, 1981, 38(11):1757-60.
Marquardt ED, Ishisaka DY, Batra KK, et al,
"Removal of Ethosuximide and Phenobarbital by Peritoneal Dialysis in a Child,"
Clin Pharm, 1992, 11(12):1030-1.
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