perampanel (Rx)

Brand and Other Names:Fycompa
  • Print

Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet: Schedule III

  • 2mg
  • 4mg
  • 6mg
  • 8mg
  • 10mg
  • 12mg

oral suspension

  • 0.5mg/mL

Partial Onset Seizures

Initial

  • In absence of concomitant enzyme-inducing antiepileptic drugs (AEDs): 2 mg PO qHS initially; increase by 2 mg/day increments in at least weekly intervals based on clinical response and tolerability to 4-8 mg qHS

Maintenance

  • Dosage range: 8-12 mg/day
  • Response may occur with 4 mg/day; 12 mg/day resulted in greater seizure rate reductions and greater substantial increase in side effects

Tonic Clonic Seizures

Indicated as adjunctive therapy for primary generalized tonic-clonic seizures in patients with epilepsy

Initial

  • In absence of enzyme-inducing AEDs: 2 mg PO qHS initially; increase by 2 mg/day increments in at least weekly intervals based on clinical response and tolerability

Maintenance

  • 8 mg PO qHS
  • If 8 mg/day is well tolerated but further control is needed, may increase up to 12 mg/day

Dosage Modifications

Enzyme inducing antiepileptic drugs (AEDs)

  • Coadministration with enzyme inducing AEDs (eg, phenytoin, carbamazepine, oxcarbazepine, phenobarbital, primidone, topiramate): 4 mg PO qHS initially; increase by 2 mg/day increments in at least weekly intervals up to 8-12 mg/day
  • Maintenance dose has not been studied or established

Hepatic impairment

  • Mild-to-moderate: 2 mg PO qHS initially; increase by 2 mg/day increments no more frequently than q2weeks to target dose
  • Mild (maximum dose): Not to exceed 6 mg/day
  • Moderate (maximum dose): Not to exceed 4 mg/day
  • Severe: Not recommended

Renal impairment

  • Moderate: May be used with close monitoring and slower titration
  • Severe or hemodialysis: Not recommended

Dosing considerations

Psychiatric or behavioral adverse events (eg, aggression, hostility, irritability, anger) occurs reduce dosage; discontinue immediately if symptoms are severe or worsening

Dosage Forms & Strengths

tablet: Schedule III

  • 2mg
  • 4mg
  • 6mg
  • 8mg
  • 10mg
  • 12mg

oral suspension

  • 0.5mg/mL

Partial Onset Seizures

Indicated as monotherapy or adjunctive therapy for partial-onset seizures with or without secondarily generalized seizures in patients with epilepsy

<4 years: Safety and efficacy not established

≥4 years

  • Initial
    • In absence of enzyme-inducing AEDs: 2 mg PO qHS; increase by 2 mg/day increments in at least weekly intervals to 4-8 mg qHS based on clinical response and tolerability
  • Maintenance
    • Dosage range: 8-12 mg/day
    • Response may occur with 4mg/day; 12 mg/day resulted in greater seizure rate reductions and greater substantial increase in side effects

Tonic Clonic Seizures

Indicated as adjunctive therapy of primary generalized tonic-clonic seizures in patients with epilepsy

<12 years: Safety and efficacy not established

≥12 years

  • Initial
    • In absence of enzyme-inducing AEDs: 2 mg PO qHS initially; increase by 2 mg/day increments in at least weekly intervals based on clinical response and tolerability
  • Maintenance
    • 8 mg PO qHS
    • If 8 mg/day is well tolerated but further seizure control is needed, may increase up to 12 mg/day

Dosage Modifications

Coadministration with moderate or strong CYP3A4

  • Increase starting dose if coadministered with moderate or strong CYP3A4 inducers, including enzyme inducing AEDs (eg, phenytoin, carbamazepine, oxcarbazepine, phenobarbital, primidone, topiramate)
  • Increase initial dose to 4 mg PO qHS
  • Maintenance dose has not been established in clinical trials; highest dose studied when coadministered with enzyme-inducing AEDs was 12 mg qHS

Hepatic impairment

  • Mild-to-moderate: 2 mg PO qHS initially; increase by 2 mg/day increments no more frequently than q2weeks to target dose
  • Mild (maximum dose): Not to exceed 6 mg/day
  • Moderate (maximum dose): Not to exceed 4 mg/day
  • Severe: Not recommended

Renal impairment

  • Moderate: May be used with close monitoring and slower titration
  • Severe or hemodialysis: Not recommended

≥65 years: Increase dosage no more frequently than q2weeks to target dose

Next:

Adverse Effects

>10%

Dizziness (16-43%)

Somnolence (9-18%)

Headache (11-13%)

Fatigue (8-12%)

Irritability (4-12%)

1-10%

Falls (2-10%)

Nausea (6-8%)

Ataxia (1-8%)

Vertigo (3-5%)

Balance disorder (3-5%)

Back pain (2-5%)

Weight gain (4%)

Vomiting (2-4%)

Anxiety (3-4%)

Blurred vision (1-4%)

Dysarthria (1-4%)

Cough (1-4%)

Hypoaesthesia (3%)

Constipation (2-3%)

Arthralgia (2-3%)

Extremity pain (2-3%)

Aggression (1-3%)

Anger (1-3%)

Myalgia (1-3%)

Diplopia (1-3%)

Injuries due to falls (1-3%)

Hypersomnia (1-3%)

Hyponatremia (2%)

Contusions (2%)

Oropharyngeal pain (2%)

Asthenia (1-2%)

Confusional state (1-2%)

Euphoric mood (1-2%)

Altered mood (1-2%)

Abnormal coordination (1-2%)

Musculoskeletal pain (1-2%)

Peripheral edema (1-2%)

Memory impairment (1-2%)

Paraesthesia (1-2%)

Postmarketing Reports

Acute psychosis, hallucinations, delusions, paranoia, delirium, disorientation, drug reaction with eosinophilia and systemic symptoms (DRESS)/multiorgan hypersensitivity

Previous
Next:

Warnings

Black Box Warnings

Serious or life-threatening psychiatric and behavioral adverse reactions including aggression, hostility, irritability, anger, and homicidal ideation, and threats reported

May occur with and without prior psychiatric history, prior aggressive behavior, or concomitant use of medications associated with hostility and aggression

Advise patients and caregivers to contact a healthcare provider immediately if any of these reactions or changes in mood, behavior, or personality that are not typical for the patient are observed

Closely monitor patients particularly during the titration period and at higher doses

Reduce dose if psychiatric and behavioral reactions occur and discontinue if symptoms are severe or worsen

Contraindications

None

Cautions

Serious psychiatric and behavioral reactions (eg, hostility, aggression) may emerge and appear to be dose related

Antiepileptic drugs increase risk of suicidal thoughts or behavior; monitor for emergence or worsening of depression, suicidal thoughts or behavior, and unusual mood/behavior changes

Dizziness, vertigo, and gait disturbances reported; monitor

Somnolence and fatigue reported; caution patients against engaging in hazardous activities that require mental alertness

Increased risk of falls

Reports of drug reaction with eosinophilia and systemic symptoms (DRESS), also known as multiorgan hypersensitivity; presents with hypersensitivity reactions (eg, lymphadenopathy, fever, rash, and/or facial swelling) in association with other systemic organ involvement (eg, hepatitis, nephritis, hematological abnormalities, myocarditis, or myositis); monitor early manifestations of hypersensitivity; discontinue therapy if alternative etiology is not established

Moderate to strong CYP3A4 inducers (eg, carbamazepine, oxcarbazepine, phenytoin, phenobarbital, primidone, topiramate) may greatly increase clearance, resulting in reduced perampanel plasma concentrations (see Dosage Modifications)

Advise patients against engaging in hazardous activities requiring mental alertness, such as operating motor vehicles or dangerous machinery, until effect of therapy known; observe patients carefully observed for signs of central nervous system (CNS) depression, such as somnolence and sedation, when used with other drugs with sedative properties because of potential additive effects

Abrupt withdrawal should be avoided unless in response to adverse event; increased risk of seizure frequency

Previous
Next:

Pregnancy & Lactation

Pregnancy

There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to antiepileptic drugs (AEDs); encourage women to enroll in the North American Antiepileptic Drug (NAAED) Pregnancy Registry by calling 1-888-233-2334 or visiting http://www.aedpregnancyregistry.org

There are no adequate data on the developmental risk associated with use in pregnant women; in animal studies, perampanel induced developmental toxicity in pregnant rat and rabbit at clinically relevant doses

Contraception

  • Advise women who are using a levonorgestrel-containing contraceptive to use an additional non-hormonal form (eg, condoms) of contraception while in therapy and for a month after discontinuation

Lactation

Perampanel and/or its metabolites are present in rat milk, and are detected at concentrations higher than that in maternal plasma

The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed child from therapy or from the underlying maternal condition

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.

Previous
Next:

Pharmacology

Mechanism of Action

Noncompetitive antagonist of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptor on post-synaptic neurons; glutamate is a primary excitatory neurotransmitter in the CNS and is implicated in various neurological disorders caused by neuronal over excitation

The mechanism for its antiepileptic effects in humans is still unknown

Absorption

Rapid and complete absorption

Bioavailability: Oral suspension has comparable bioavailability to tablets under steady state; both formulations may be used interchangeably

Peak Plasma Time: 0.5-2.5 hr (fasting)

Food does not affect extent of absorption, but slows rate of absorption; Cmax decreased by 11-40% and Tmax delayed by 1-3 hr compared to fasted conditions

Distribution

Protein Bound: 95-96% (mainly albumin and alfa1-acid glycoprotein)

Blood to plasma ratio: 0.55-0.59

Metabolism

Extensively metabolized in liver via primary oxidation and sequential glucuronidation

In vitro studies indicated, oxidative metabolism mediated mainly by CYP3A4 and/or CYP3A5; lesser extent by CYP1A2 and CYP2B6

Elimination

Half-life: 105 hr

Renal clearance: 12 mL/min

Excretion: Feces (48%); urine (22%)

Previous
Next:

Administration

Oral Administration

May take tablet or oral suspension with or without food

Tablet and oral suspension may be used interchangeably on a mg-per-mg basis

Oral suspension

  • Shake well before measuring dose for each administrations
  • Use provided adapter and graduated oral dosing syringe to accurately administer the oral suspension; household teaspoons or tablespoons are not an adequate measuring device
  • The adapter, which is supplied in the product carton, should be inserted firmly into the neck of the bottle before use and remain in place for the duration of the usage of the bottle
  • The dosing syringe should be inserted into the adapter and the dose withdrawn from the inverted bottle
  • The cap should be replaced after each use; the cap fits properly when the adapter is in place
  • Discard any unused oral suspension remaing 90 days after first opening the bottle

Storage

Tablet

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

Oral suspension

  • Do not store above 86°F (30°C). Do not freeze. Use within 90 days after the first opening of the bottle.
Previous
Next:

Images

BRAND FORM. UNIT PRICE PILL IMAGE
Fycompa oral
-
0.5 mg/mL suspension
Fycompa oral
-
8 mg tablet
Fycompa oral
-
6 mg tablet
Fycompa oral
-
4 mg tablet
Fycompa oral
-
2 mg tablet

Copyright © 2010 First DataBank, Inc.

Previous
Next:

Patient Handout

Patient Education
perampanel oral

PERAMPANEL - ORAL

(per-AM-pa-nel)

COMMON BRAND NAME(S): Fycompa

WARNING: Perampanel may cause or worsen mental/mood disorders. Tell your doctor right away if you or your family/caregiver notice any unusual behavior changes (including aggression, attempts to hurt others, impulsive actions) or other mental/mood changes (including anxiety, irritability, hostile/angry feelings, paranoia, hallucinations, delusions, thoughts of harming others). Be especially watchful for these symptoms when you first start this medication or when the dose is changed. These symptoms may also occur even after stopping perampanel. Do not drink alcoholic beverages while taking perampanel because alcohol may make these symptoms worse.

USES: Perampanel is used to treat certain types of seizures (including focal and generalized tonic-clonic seizures). Perampanel belongs to a class of drugs known as anticonvulsants.

HOW TO USE: Read the Medication Guide and, if available, the Patient Information Leaflet provided by your pharmacist before you start taking perampanel and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth as directed by your doctor, usually once daily at bedtime.If you are using the liquid form of this medication, shake the bottle well before each dose. Carefully measure the dose using a special measuring device/spoon. Do not use a household spoon because you may not get the correct dose.The dosage is based on your medical condition, response to treatment, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).To reduce your risk of side effects, your doctor may direct you to start this medication at a low dose and gradually increase your dose. Follow your doctor's instructions carefully.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.Do not stop taking this medication without consulting your doctor. Some conditions may become worse when this drug is suddenly stopped. Your dose may need to be gradually decreased.Though it helps many people, this medication may sometimes cause addiction. This risk may be higher if you have a substance use disorder (such as overuse of or addiction to drugs/alcohol). Take this medication exactly as prescribed to lower the risk of addiction. Ask your doctor or pharmacist for more details.Tell your doctor if your condition does not improve or if it worsens.

SIDE EFFECTS: See also Warning Section.Dizziness, a feeling of spinning, unsteadiness, trouble walking, loss of balance, drowsiness, weakness, nausea, vomiting, headache, or weight gain may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: blurred/double vision, frequent falls.A small number of people who take anticonvulsants for any condition (such as seizures, bipolar disorder, pain) may experience depression, suicidal thoughts/attempts, or other mental/mood problems. Tell your doctor right away if you or your family/caregiver notice any unusual/sudden changes in your mood, thoughts, or behavior including signs of depression, suicidal thoughts/attempts, thoughts about harming yourself.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: fever, swollen lymph nodes, rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking perampanel, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver problems, kidney problems, mental/mood disorders, personal or family history of a substance use disorder (such as overuse of or addiction to drugs/alcohol), galactose intolerance (such as Lapp lactase deficiency or glucose-galactose malabsorption).This drug may make you dizzy or drowsy or blur your vision. Alcohol or marijuana (cannabis) can make you more dizzy or drowsy. Do not drive, use machinery, or do anything that needs alertness or clear vision until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis).Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older adults may be more sensitive to the side effects of this drug, especially falls, drowsiness, and weakness.During pregnancy, this medication should be used only when clearly needed. It may harm an unborn baby. However, since untreated seizures are a serious condition that can harm both a pregnant woman and her unborn baby, do not stop taking this medication unless directed by your doctor. If you are planning pregnancy, become pregnant, or think you may be pregnant, immediately discuss with your doctor the benefits and risks of using this medication during pregnancy.It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.A product that may interact with this drug is: orlistat.Other medications can affect the removal of perampanel from your body, which may affect how perampanel works. Examples include rifamycins (such as rifabutin), St. John's wort, among others.This medication may decrease the effectiveness of levonorgestrel-containing birth control. This could cause pregnancy. Discuss with your doctor or pharmacist if you should use reliable non-hormonal backup birth control methods (such as condoms, diaphragm with spermicide) while using perampanel and for a month after you stop using perampanel. Also tell your doctor if you have any new spotting or breakthrough bleeding, because these may be signs that your birth control is not working well.Tell your doctor or pharmacist if you are taking other products that cause drowsiness including alcohol, marijuana (cannabis), antihistamines (such as cetirizine, diphenhydramine), drugs for sleep or anxiety (such as alprazolam, diazepam, zolpidem), muscle relaxants, and opioid pain relievers (such as codeine).Check the labels on all your medicines (such as allergy or cough-and-cold products) because they may contain ingredients that cause drowsiness. Ask your pharmacist about using those products safely.

OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: mental/mood/behavior changes such as agitation, aggressive behavior.

NOTES: Do not share this medication with others. Sharing it is against the law.Medical tests (such as weight measurement, mental/mood screenings) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: If you miss a dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up. If you miss more than 1 dose, contact your doctor for more information.

STORAGE: Store the tablets at room temperature away from light and moisture. If you are taking the liquid, store it below 86 degrees F (30 degrees C), do not freeze, and discard any unused liquid 90 days after first opening the bottle. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).

Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

Previous
Next:

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.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
  • Manage and view all your plans together – even plans in different states.
  • 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.
Additional Offers
Email to Patient

From:

To:

The recipient will receive more details and instructions to access this offer.

By clicking send, you acknowledge that you have permission to email the recipient with this information.

Email Forms to Patient

From:

To:

The recipient will receive more details and instructions to access this offer.

By clicking send, you acknowledge that you have permission to email the recipient with this information.

Previous
Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.