Topiramate
(to-pir′a-mate)
Topamax
Classifications: ANTICONVULSANT; GAMMA-AMINOBUTYRATE (GABA) ENHANCER
Therapeutic: ANTICONVULSANT; ANTIEPILEPTIC
Pregnancy Category: D
AVAILABILITY
Tablet; extended release capsule; sprinkle
capsule
ACTION & THERAPEUTIC EFFECT
Sulfamate-substituted monosaccharide with a
broad spectrum of anticonvulsant activity. Exhibits sodium channel-blocking
action, as well as enhancing the ability of GABA to induce a flux of chloride
ions into the neurons, thus potentiating the activity of this inhibitory
neurotransmitter (GABA). Effectiveness indicated by
a decrease in seizure activity.
USES
Adjunctive therapy for partialonset seizures;
generalized tonicclonic seizures; migraine prophylaxis.
UNLABELED USES
Cluster headache, bulimia nervosa, neuropathic
pain, infantile spasms, bipolar disorder, obesity.
CONTRAINDICATIONS
Hypersensitivity to topiramate; suicidal
ideation; pregnancy (category D). Effect on labor and delivery is unknown.
CAUTIOUS USE
Moderate and severe renal impairment, hepatic
impairment; COPD; chronic acidosis;
history of suicidal thoughts or psychiatric
distubances; severe pulmonary disease; older adults; lactation; children
younger than 2 y. Extended
Release: Children younger than 6 y.
ROUTE & DOSAGE
Partial-Onset Seizures
Adult/Adolescent/Child
(over 10y): PO Immediate
release: Initiate with 25 mg b.i.d., increase by 25 mg/wk to efficacy PO Maintenance Dose 200–400 mg/day divided
b.i.d. (max: 1600 mg/ day) PO
Extended release: 50 mg daily
then increase by 50 mg/wk to reach
400 mg daily
Child (2–16 y): PO Initiate with 1–3 mg/kg at bedtime × 1 wk, then increase by 1–3 mg/kg/day in 2 divided
doses q1–2wk to a target range of 5–9 mg/kg/day
Generalized Tonic-Clonic Monotherapy
Adults/Adolescents/Children
(over 10 y): PO Immediate release: 50 mg/day in 2 daily divided
doses, taper up dose by 50 mg per
wk up to 400 mg/day
Child (2–10 y): POWeight
based dosing in package insert
Migraine Prophylaxis
Adult: PO Immediate release: Initiate with 25 mg b.i.d., increase by
25 mg/wk to 100 mg/day or max tolerated dose
Renal Impairment Dosage Adjustment
CrCl less than 70
mL/min: Decrease dose by 50%
ADMINISTRATION
Oral
- Make dosage increments of 50 mg at weekly
intervals to the recommended dose, usually 400 mg/day.
- Do not break tablets unless absolutely necessary
because of bitter taste.
- Store at 15°–30° C (59°–86° F) in a tightly
closed container. Protect from light and moisture.
ADVERSE EFFECTS (≥1%)
Body as a Whole: Fatigue, speech problems, weight loss; decreased sweating and hyperthermia in children; metabolic acidosis, upper respiratory infection. CNS: Somnolence, dizziness, ataxia, psychomotor slowing, confusion, nystagmus, paresthesia, memory difficulty, difficulty concentrating, nervousness, depression, anxiety, tremor. GI: Anorexia,
nausea. Special Senses: Angle closure glaucoma (rare).
INTERACTIONS
Drug: Increased CNS depression with alcohol and other CNS DEPRESSANTS; may increase phenytoin concentrations; may decrease ORAL CONTRACEPTIVE, valproate concentrations; may increase risk of kidney
stone formation with other CARBONIC ANHYDRASE INHIBITORS. Carbamazepine,
phenytoin, valproate may decrease topiramate concentrations. Use cautiously with metformin. Herbal: Ginkgo may decrease anticonvulsant effectiveness.
PHARMACOKINETICS
Absorption: Rapidly absorbed from GI tract;
80% bioavailability. Peak:
2 h. Distribution: 13–17% protein bound. Metabolism: Minimally metabolized in the
liver. Elimination: Primarily in urine. Half-Life: 21 h.
NURSING IMPLICATIONS
Assessment & Drug Effects
- Monitor mental status and report significant
cognitive impairment.
- Monitor lab tests: Periodic CBC with Hgb and
Hct.
Patient & Family Education
- Do not stop drug abruptly; discontinue gradually
to minimize seizures.
- To minimize risk of kidney stones, drink at
least 6–8 full glasses of water each day.
- Exercise caution with potentially hazardous
activities. Sedation is common, especially with concurrent use of alcohol or
other CNS depressants.
- Use or add barrier contraceptive if using
hormonal contraceptives.
- Be aware that psychomotor slowing and
speech/language problems may develop while on topiramate therapy.
- Report adverse effects that interfere with
activities of daily living.
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