eslicarbazepine acetate (Rx)

Brand and Other Names:Aptiom
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 200mg
  • 400mg
  • 600mg
  • 800mg
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Partial-Onset Seizures

Indicated for partial-onset seizures as monotherapy or adjunctive therapy

Initial

  • 400 mg PO qDay
  • For some patients, treatment may be initiated at 800 mg qDay if the need for additional seizure reduction outweighs an increased risk of adverse reactions during initiation

Titration and maintenance

  • Increase dose by weekly increments of 400-600 mg, based on clinical response and tolerability
  • Recommended maintenance dose is 800-1600 mg once daily
  • Monotherapy: Consider 800 mg/day maintenance dose in patients unable to tolerate 1200 mg/day
  • Adjunctive therapy: 1600 mg/day should be considered in patients who did not achieve a satisfactory response with 1200 mg/day

Dosage Modifications

Do not take adjunctively with oxcarbazepine

Coadministration with enzyme-inducing AEDs (eg, carbamazepine, phenytoin, phenobarbital, primidone): May need to increase eslicarbazepine dose

Renal impairment

  • Mild (CrCl ≥50 mL/min): No dosage adjustment necessary
  • Moderate-to-severe (CrCl <50 mL/min): Reduce the initial, titration, and maintenance doses by 50%; may adjust titration and maintenance doses according to clinical response

Hepatic impairment

  • Mild-to-moderate: No dosage adjustment required
  • Severe: Not recommended (not studied)

Dosing Considerations

When discontinuing eslicarbazepine acetate, gradually reduce dose and avoid abrupt discontinuation in order to minimize risk of increased seizure frequency and status epilepticus

Dosage Forms & Strengths

tablet

  • 200mg
  • 400mg
  • 600mg
  • 800mg
more...

Partial-Onset Seizures

Indicated for partial-onset seizures as monotherapy or adjunctive therapy

<4 years: Safety and efficacy not established

4-17 years

  • Recommended initial weight based dosage
    • 11-21 kg: 200 mg PO qDay initially; titration increment not to exceed 200 mg/day
    • 22-38 kg: 300 mg PO qDay; titration increment not to exceed 300 mg/day
    • >38kg: 400 mg PO qDay; titration increment not to exceed 400 mg/day
    • Dosage should be increased based on clinical response and tolerability, no more frequently than once per week
  • Maintenance dosage
    • 11-21 kg: Not to exceed 400-600 mg/day
    • 22-31 kg: Not to exceed 500-800 mg/day
    • 32-38 kg: Not to exceed 600-900 mg/day
    • >38kg: Not to exceed 800-1200 mg/day

Dosage Modifications

Do not take adjunctively with oxcarbazepine

Coadministration with enzyme-inducing AEDs (eg, carbamazepine, phenytoin, phenobarbital, primidone): May need to increase eslicarbazepine dose

Renal impairment

  • Mild (CrCl ≥50 mL/min): No dosage adjustment necessary
  • Moderate-to-severe (CrCl <50 mL/min): Reduce the initial, titration, and maintenance doses by 50%; may adjust titration and maintenance doses according to clinical response

Hepatic impairment

  • Mild-to-moderate: No dosage adjustment required
  • Severe: Not recommended (not studied)

Dosing Considerations

When discontinuing eslicarbazepine acetate, gradually reduce dose and avoid abrupt discontinuation in order to minimize risk of increased seizure frequency and status epilepticus

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Interactions

Interaction Checker

and eslicarbazepine acetate

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    Contraindicated

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            Adverse Effects

            >10%

            800 mg dose

            • Dizziness (20%)
            • Headache (13%)
            • Somnolence (11%)

            1200 mg dose

            • Dizziness (28%)
            • Somnolence (18%)
            • Nausea (16%)
            • Headache (15%)
            • Diplopia (11%)

            1-10%

            800 mg dose

            • Nausea (10%)
            • Diplopia (9%)
            • Blurred vision (6%)
            • Vomiting (6%)
            • Diarrhea (6%)
            • Fatigue (4%)
            • Ataxia (4%)
            • Balance disorder (3%)
            • Falls (3%)
            • Tremor (2%)
            • Hyponatremia (2%)
            • Asthenia (2%)
            • Gait disturbance (2%)
            • Peripheral edema (2%)
            • Urinary tract infections (2%)

            1200 mg dose

            • Fatigue (7%)
            • Ataxia (6%)
            • Blurred vision (5%)
            • Tremor (4%)
            • Asthenia (3%)
            • Balance disorder (3%)
            • Depression (3%)
            • Rash (3%)
            • Insomnia (2%)
            • Dysarthria (2%)
            • Memory disturbance (2%)
            • Nystagmus (2%)
            • Gait disturbances (2%)
            • Diarrhea and constipation (2%)
            • Abdominal pain (2%)

            Postmarketing Reports

            Hematologic and Lymphatic Systems: Leukopenia, agranulocytosis, thrombocytopenia, megaloblastic anemia, and pancytopenia

            Metabolism and Nutrition Disorders: Syndrome of inappropriate antidiuretic hormone secretion (SIADH)

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            Warnings

            Contraindications

            Hypersensitivity to eslicarbazepine or oxcarbazepine

            Cautions

            See FDA warning on potential suicidal behavior; monitor patients for notable changes in behavior that might be associated with suicidal thoughts or depression (notify health-care provider immediately if symptoms occur)

            Antiepileptic drugs (AEDs), including eslicarbazepine, increase the risk of suicidal thoughts or behavior in patients taking these drugs for any indication; monitor patients for notable changes in behavior that might be associated with suicidal thoughts or depression (notify health-care provider immediately if symptoms occur)

            Serious dermatologic reactions reported, including Stevens-Johnson syndrome (SJS); serious and sometimes fatal dermatologic reactions, including toxic epidermal necrolysis (TEN) and SJS, have been reported in patients using oxcarbazepine or carbamazepine which are chemically related

            Drug reaction with eosinophilia and systemic symptoms (DRESS) reported; DRESS may be fatal or life-threatening, and although not exclusively, presents with fever, rash, and/or lymphadenopathy, in association with other organ system involvement, such as hepatitis, nephritis, hematological abnormalities, myocarditis, or myositis sometimes resembling an acute viral infection

            Clinically significant hyponatremia (sodium <125 mEq/L); consider monitoring serum sodium and chloride levels during maintenance treatment, particularly in patients receiving other medications known to decrease serum sodium levels, and perform in patients exhibiting symptoms of hyponatremia develop (eg, nausea/vomiting, malaise, headache, lethargy, confusion, irritability, muscle weakness/spasms, obtundation, or increase in seizure frequency or severity)

            Anaphylactic reactions and angioedema: Monitor for breathing difficulties or swelling; discontinue if another cause cannot be established

            Hyponatremia: Monitor sodium levels in patients at risk or patients experiencing hyponatremia symptoms

            Neurological adverse reactions: Monitor for dizziness, disturbance in gait and coordination, somnolence, fatigue, cognitive dysfunction, and visual changes; caution when driving or operating machinery

            Discontinuing: Withdraw gradually to minimize risk of increased seizure frequency and status epilepticus

            Drug-induced liver injury: Discontinue with jaundice or evidence of significant liver injury

            Dose-dependent decreases in serum T3 and T4 (free and total) values reported

            Rare cases of pancytopenia, agranulocytosis, and leukopenia have been reported during postmarketing use of eslicarbazepine; consider discontinuation of treatment in patients who develop pancytopenia, agranulocytosis, or leukopenia

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            Pregnancy & Lactation

            Pregnancy

            Limited available data with eslicarbazepine acetate use in pregnant women are insufficient to inform a drug-associated risk of adverse developmental outcomes

            Encourage women who are taking eslicarbazepine acetate during pregnancy to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling 1-888-233-2334 or visiting http://www.aedpregnancyregistry.org

            Advise women of reproductive potential taking eslicarbazepine acetate who are using a contraceptive containing ethinylestradiol or levonorgestrel to use additional or alternative non-hormonal birth control

            Eslicarbazepine acetate was evaluated in rats and mice for potential adverse impact on fertility of the parental and first generation

            Lactation

            Eslicarbazepine is present in human milk; effects of eslicarbazepine acetate on the breastfed infant or on milk production are unknown

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Antiepileptic drug; eslicarbazepine acetate is a prodrug that is activated to eslicarbazepine (S-licarbazepine), the major active metabolite of oxcarbazepine

            Stabilizes neuronal membranes by blocking Na+ channels; this may inhibit repetitive firing and may decrease the propagation of synaptic impulses; may also increase potassium conductance and modulate the activity of high-voltage activated calcium channels

            Absorption

            Bioavailability: >90%

            Peak plasma concentration: 1-4 hr (as eslicarbazepine [major metabolite] of prodrug)

            Distribution

            Protein bound: <40%

            Vd: 61 L

            Metabolism

            Rapidly and extensively metabolized to its major active metabolite (eslicarbazepine) by hydrolytic first-pass metabolism

            Eslicarbazepine corresponds to 91% of systemic exposure

            Systemic exposure of minor active metabolites: (R)-licarbazepine 5%, oxcarbazepine 1%

            Systemic exposure of inactive glucuronide ~1%

            Moderate CYP2C19 inhibitor; no apparent autoinduction

            Elimination

            Half-life: 13-20 hr

            Excretion: >90% urine; two-thirds as unchanged form and one-third as glucuronide conjugate

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            Administration

            Instructions

            May take with or without food

            May swallow table whole or crush

            Discontinuation: Reduce dose gradually and avoid abrupt discontinuation to minimize risk of increased seizure frequency and status epilepticus

            Storage

            Store tablets at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F)

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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