Fycompa, pills 2mg, 7pcs

Composition

of 1 tab. perampanel 2 mg

Auxiliary substances:

lactose monohydrate – 78.5 mg,

low-substituted hyprolose-14 mg,

povidone-5 mg,

magnesium stearate-0.5 mg.

Composition of the film shell:

opadray orange – 5 mg (hypromellose 2910-56%, talc-28%, macrogol 8000-10%, titanium dioxide-4%, iron oxide yellow dye-1.8%, iron oxide red dye-0.2%).

Pharmacological action

Faykompa has an antiepileptic effect.

Indications

Faikompa is indicated as an adjunct to the treatment of partial seizures in patients with epilepsy aged 12 years and older with or without secondary generalized seizures.

Use during pregnancy and lactation

For women with preserved childbearing potential who do not use contraceptive methods, taking the drug Faykompa is recommended only if absolutely necessary.

Data on the use of perampanel in pregnant women are significantly limited (

Animal studies have shown that perampanel and/or its metabolites are excreted in breast milk. It is not known whether perampanel is excreted in human breast milk, so the risk to the child cannot be excluded.

Considering the benefits of both breast-feeding for the child and therapy for the woman, it is necessary to either stop breastfeeding, or refrain from taking / discontinue taking Faycompa during breastfeeding.

Impact on fertility

Animal studies have shown that high doses (30 mg/kg) of perampanel prolong and disrupt the regularity of the estrous cycle, but these changes did not affect fertility and early fetal development. No effect on male fertility was found. The effect of perampanel on human fertility has not been studied.

Contraindications

• hypersensitivity to perampanel or any of the excipients of the drug;
• galactose intolerance, lactase deficiency or glucose-galactose malabsorption;
• severe renal or hepatic insufficiency;
• patients on hemodialysis;
• pregnancy;
• lactation;
• children under 12 years of age (no data on efficacy and safety).

Side effects

Among 1,639 patients with partial seizures who received perampanel in all clinical trials,1,174 took the drug for 6 months and 703-for more than 12 months.

Adverse reactions leading to withdrawal of patients from controlled phase III trials were observed in 1.7,4.2, and 13.7% of patients treated with perampanel at doses of 4,8, and 12 mg/day, respectively, and in 1.4% of patients treated with placebo. The most common reasons for withdrawal from studies were dizziness and drowsiness (≥1% in the combined perampanel group and more than in the placebo group).

The following lists the adverse events observed with the use of perampanel, according to the systemic organ classes and frequency of their occurrence. To assess the frequency of adverse events, the following classification is used: very common (≥1/10); common (≥1/100,

Nutritional and metabolic disorders:  often-decreased appetite, increased appetite.

Mental disorders:  often — aggression, anger, anxiety, confusion.

Nervous system disorders:  very often — dizziness, drowsiness; often-ataxia, dysarthria, balance disorders, increased irritability.

Visual disturbances:  often — diplopia, blurred vision.

Hearing disorders and labyrinth disorders:  often-central vertigo.

Gastrointestinal disorders:  often — nausea.

Musculoskeletal and connective tissue disorders:  often — back pain.

General violations:  often-gait disorder, fatigue.

Laboratory and instrumental data:  often-an increase in body weight.

Injuries, intoxications, and manipulation complications:  often-falls.

Teens. Based on the data of clinical studies, we can expect that the frequency, nature and severity of adverse reactions in adolescents are the same as in adults.

Interaction

Faikompa is not a potent inducer or inhibitor of cytochrome P450 isoenzymes or the UGT isoenzyme involved in glucuronidation reactions.

Oral contraceptives

At a dose of 12 mg / day (but not 4 or 8 mg/day), perampanel reduced the Cmax and AUC of levonorgestrel by approximately 40%. Perampanel in a daily dose of 12 mg does not affect the AUC of ethinyl estradiol, but reduces its Cmax by 18%. Patients taking Faycompa should consider the possibility of reducing the effectiveness of contraceptives containing levonorgestrel, and use additional methods of contraception (intrauterine devices or condoms).

Interaction with other antiepileptic drugs (AEDs)

The potential interaction of Faicompa (with a single daily dose of up to 12 mg) and other AEDs was evaluated based on data from clinical studies and population pharmacokinetic analysis of combined data from three phase III studies. The effect of this interaction on the equilibrium concentrations of PEP is shown in the table:

Table of contents

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Some AEDs that are inducers of enzymes (carbamazepine, phenytoin, oxcarbazepine) increase the total clearance of perampanel and, accordingly, reduce its plasma concentrations.

In a study involving healthy volunteers, carbamazepine, a known potent enzyme inducer, reduced perampanel concentrations by 2/3 (3-fold).

A similar result was obtained in a population pharmacokinetic analysis in patients with partial seizures who received Faycompa at doses up to 12 mg / day in placebo-controlled clinical trials. Faicompa did not significantly affect the clearance of clonazepam, levetiracetam, phenobarbital, phenytoin, topiramate, zonisamide, carbamazepine, clobazam, lamotrigine, and valproic acid at the highest dose of perampanel (12 mg/day).

When perampanel was co-administered with oxcarbazepine, the clearance of the latter decreased by 26%. Oxcarbazepine is rapidly metabolized by cytosolic reductase to the active metabolite monohydroxycarbazepine. The effect of perampanel on the concentration of monohydroxycarbazepine is unknown.

The dose of perampanel is selected until the clinical effect is achieved, regardless of concomitant AEDs.

Effect of perampanel on CYP3A isoenzyme substrates

In healthy volunteers, the drug Faycompa (in a daily dose of 6 mg for 20 days) reduced the AUC of midazolam by 13%. A more significant reduction in exposure to midazolam (and other sensitive substrates of the CYP3A isoenzyme)cannot be excluded with higher doses of Faycompa.

Effect of cytochrome P 450 isoenzyme inducers on the pharmacokinetics of perampanel

It is expected that powerful inducers of cytochrome P450 isoenzymes, such as rifampicin and St. John’s wort, can also reduce the concentration of perampanel in plasma. Felbamate may also reduce the plasma concentration of perampanel.

Effect of cytochrome P 450 isoenzyme inhibitors on the pharmacokinetics of perampanel

In healthy volunteers, taking ketoconazole (400 mg daily for 10 days), which is an inhibitor of the CYP3A4 isoenzyme, increased the AUC of perampanel by 20% and prolonged its T1/2 by 15% (67.8 vs. 58.4 hours). When combining perampanel with another CYP3A4 inhibitor with a half-life longer than that of ketoconazole, or when taking the inhibitor for a longer period of time, an increase in the effect cannot be excluded. Potent inhibitors of other cytochrome P450 isoenzymes also have the potential to increase perampanel concentrations.

Interaction with levodopa

In healthy volunteers, taking Faikompa (4 mg daily for 19 days) had no effect on the AUC or Cmax of levodopa.

Interaction with alcohol

In a pharmacodynamic interaction study in healthy volunteers, the effect of perampanel on attentiveness and responsiveness, such as driving, was enhanced by alcohol intake. Repeated administration of perampanel at a daily dose of 12 mg also increased the severity of irritability, confusion and depression. This effect is also observed when taking the drug Faycompa in combination with other CNS depressants.

Use in adolescents

Drug interaction studies were conducted only in adults. In the population pharmacokinetic analysis of adolescents participating in phase III clinical trials, there were no significant differences from the general study population.

How to take it, course of administration and dosage

Inside, before going to bed, regardless of food intake.

Use in adults and adolescents. Perampanel is taken once a day.The tablet must be swallowed whole, washed down with 1 glass of water, you can not chew, crumble or break, because the tablet can not be carefully divided, because there is no risk on it.

It has been shown that the drug Faykompa in daily doses from 4 to 12 mg is effective in the treatment of partial epileptic seizures. Use of the drug Faykompa should begin with a dose of 2 mg / day. The dose can be increased depending on the clinical response and tolerability, in increments of 2 mg no more than once a week, up to 4-8 mg / day. Depending on the individual clinical response and tolerability of the drug at a dose of 8 mg/day, it is possible to further increase the dose of Faycomp to 12 mg / day, in increments of 2 mg no more than once a week. In patients receiving concomitant AEDs that do not reduce the elimination half-life of perampanel, the dose of perampanel should be selected at two-week intervals. In patients receiving concomitant AEDs that reduce the elimination half-life of perampanel, the dose of perampanel should be increased once a week.

Discontinuation of the drug is carried out gradually.

One-time medication skip: due to the fact that perampanel has a sufficiently long T1 / 2, the patient should wait and take the next planned dose in accordance with the agreed schedule of taking the drug.

If more than 1 dose is missed (the total duration without the drug is less than 5T1/2: 3 weeks — for patients not receiving PEP that changes the metabolism of perampanel, and 1 week — for patients receiving PEP that changes the metabolism of perampanel), you should consider resuming the drug at the last dose taken.

If the patient has stopped taking the drug for more than 5T1 / 2, follow the recommendations as at the initiation of treatment.

Use in children under 12 years of age. The safety and efficacy of perampanel in children under 12 years of age has not been established.

Use in elderly patients (≥65 years). In clinical trials of Faycompa, there were not enough patients with epilepsy older than 65 years to assess the differences with younger patients. Analysis of safety information in 905 elderly patients treated with perampanel revealed no age-related differences in the safety profile. These data confirm that no age-dependent dose adjustment of perampanel is required. In elderly patients, perampanel should be used with caution.

Use in patients with renal insufficiency. In patients with mild renal insufficiency, no dose adjustment of perampanel is required. The use of Faikompa in patients with moderate to severe renal insufficiency or patients undergoing hemodialysis is not recommended.

Use in patients with hepatic insufficiency. Dose increases in patients with mild to moderate hepatic insufficiency, as in other patients, are made depending on the clinical response and tolerability. Since T1 / 2 of perampanel is prolonged in mild to moderate hepatic insufficiency, the minimum time interval before each dose increase should be 2 weeks, and the maximum dose should not exceed 8 mg / day. Use in severe hepatic insufficiency is not recommended.

Overdose

Symptoms: clinical experience with perampanel overdose in humans is limited. In the report of a deliberate overdose that could have resulted in a dose of up to 264 mg, the patient showed a change in consciousness, agitation and aggressive behavior; recovery was without consequences.

Treatment: there is no specific antidote. General maintenance therapy is indicated, including monitoring of vital signs and clinical status of the patient. Given the long T1 / 2 of a perampanel, its effects may have a longer duration in time. Due to the low renal clearance of perampanel, special procedures such as forced diuresis, hemodialysis or hemoperfusion are ineffective.

Special instructions

Suicidal alertness

Suicidal thoughts and behaviors have been reported in patients taking PEP for various indications. A meta-analysis of randomized placebo-controlled studies of PEP also showed a small increase in the risk of suicidal thinking and behavior. The mechanism of increased risk is unknown, and at present it is impossible to exclude the possibility of an increase in this risk when using the drug Faykompa. As a result, patients should be monitored for signs of suicidal thinking and behavior, and appropriate treatment should be provided.

Patients or their caregivers should be informed about the need to seek medical attention if signs of suicidal thinking or behavior appear.

Nervous system disorders

Perampanel can cause dizziness and drowsiness and thus affect the ability to drive vehicles and use machinery.

Oral contraceptives

While taking the drug Faycompa at a dose of 12 mg/day, the effectiveness of progestogen-containing hormonal contraceptives may be reduced (see the section “Interaction with other drugs”). In these cases, it is necessary to provide for the use of additional non-hormonal methods of contraception.

End of therapy

It is recommended to complete therapy with Faycompa gradually in order to minimize the likelihood of an increase in the frequency of seizures. In extreme cases, abrupt discontinuation of the drug is possible, given its long elimination period and a relatively slow decrease in its plasma concentration after discontinuation.

Falls

There is a tendency to increase the number of falls, especially in elderly patients, the cause of which is unknown.

Aggression

Cases of aggressive and hostile behavior have been reported in patients receiving perampanel therapy. In clinical trials of perampanel, aggression, anger, and irritability were more common when administered at higher doses. Most of these adverse events were mild to moderate in severity and resolved either independently or with a reduced dose. However, thoughts of harming others, physical aggression, or threatening behavior were observed in some patients (

Developing an addiction

Caution should be exercised when prescribing Faycompa to patients with a history of drug dependence. Such patients should be monitored for timely detection of possible addiction to perampanel.

Concomitant therapy with AEDs inducing the CYP3A isoenzyme

The efficacy of perampanel in fixed doses was lower in those patients who received concomitant antiepileptic therapy with inducers of the CYP3A isoenzyme (carbamazepine, phenytoin, oxcarbazepine) than in patients who received AEDs that did not affect the activity of enzymes. A 50% response to 4,8, and 12 mg perampanel was achieved in 23,31.5, and 30% of patients treated with CYP3A-inducing PEPs, respectively, and in 33.3,46.5, and 50% of patients treated with PEPs that did not affect enzyme activity, respectively. The effect of perampanel therapy should be carefully monitored when replacing or adding concomitant AEDs. Depending on the individual clinical response to treatment and tolerability of the drug, the dose may be increased or decreased in 2 mg increments.

Concomitant therapy with other inducers or inhibitors of cytochrome P450 isoenzymes that are not PEP

The tolerability and effect of perampanel therapy should be carefully monitored when adding or withdrawing inducers or inhibitors of cytochrome P450 isoenzymes, as this may alter the plasma concentration of perampanel, and dose adjustment may be required.

Monotherapy

Within 28 days, seizures did not occur in 2-6.5% of patients taking perampanel in clinical trials (in the placebo group — in 0-1.7%). There are no data on the effect of discontinuation of concomitant anticonvulsant therapy.

Influence on the ability to drive vehicles and work with mechanisms. Faikompa has a moderate effect on the ability to drive vehicles and work with mechanisms. Perampanel can cause dizziness and drowsiness and thus affect the ability to drive vehicles and use machinery. Patients are advised not to drive vehicles, operate complex equipment, or engage in other potentially dangerous activities until it is determined whether the perampanel affects their ability to perform these activities.

Form of production

Orange film-coated tablets, round, biconvex, with the inscription “E 275” on one side and “2” on the other side.

Storage conditions

At a temperature not exceeding 30 °C

Shelf life

4 years

Active ingredient

Perampanel

Conditions of release from pharmacies

By prescription

Dosage form

Tablets