Fycompa 4mg Eisai medicine for additional epilepsy (2 blisters x 14 tablets)
Dosage form Box of 2 blisters x 14 tablets
Specifications Perampanel
Ingredient
| Composition information | Content |
| Perampanel | 4mg |
Uses
indications
Fymcopa 4mg drug is indicated in the following cases:
Group Pharmacological Therapy: anti -epileptic drugs.
Mechanism of action:
Perampanel is the first substance in the group (First-in-Class) selected, non-competitive antagonistic, ionotropic receptor A-Amino-3-hydroxy-5-methyl-4-IsoxazoleProproprife (AMPA) glutamate on the posterior neuron cell after synap. Glutamat is the main stimulant neurotransmitter in the central nervous system and is related to many neurological disorders caused by excessive stimulation of the neuron.
AMPA receptor activation by glutamat is thought to be responsible for most rapid transmission through synap in the brain.
In In vitro studies, Perampanel is not competing with AMPA to connect with the AMPA receptor, but the cohesion of Perampanel has been pushed out by non -competitive AMPA receptor counterparts, showing that Perampanel is an non -competitive AMPA receptor counterclose. In vitro, Perampanel inhibits the increase in intracellular calcium caused by AMPA (which is not caused by NMDA).
In Vivo, Perampanel significantly lasted the delay of seizures in a epilepsy model caused by AMPA.
The exact mechanism for Perampanel to promote anti -epileptic effects on humans still need to be completely clarified.
Pharmacological effect:
A pharmacokinetics analysis (about efficiency) has been conducted based on the data that combined with 3 tests on the effectiveness of the local start -up seizure. In addition, a pharmacokinetics analysis (about efficiency) has been conducted in an effective test for spastic spastic seizures - convulsions. In both analysis, the use of Perampanel is correlated with a decrease in the frequency of seizures.
Mental mental performance. Single and multi -dose of 8 mg and 12 mg reduces mental performance in healthy volunteers related to the dose. The impact of Perampanel on complex tasks such as driving ability is plus or united with the effect of reducing alcohol. Check the mental mental performance back to the original level within 2 weeks from the stop use of Perampanel.
Cognitive function. In a study in healthy volunteers to assess Perampanel's influence on alertness and memory by using a set of evaluation standards, no effect of Perampanel was found after the single and multi -doses of Perampanel up to 12 mg/day.
alertness and mood. The level of alertness decreases in the form of dosage related to healthy objects that are used for Perampanel doses 4-12 mg/day. The mood worsens only after the dose of 12 mg/day; Changes in lightweight mood and reflect the overall alert reduction. Use multi -dose Perampanel 12 mg/day also increases the effects of alcohol on vigilance and alertness and increases the level of anger, confusion and depression according to the evaluation of the 5 -point assessment of the mood stat state.
Heart physiological electrophysiology. Perampanel does not extend the adjustment range of QT (QTC) when used at daily dose of up to 12 mg/day and has no bureaucracy related to clinical or important important in QRS period.
Perampanel's pharmacokinetics
absorption
After drinking, Perampanel is easily absorbed without evidence that this substance has metabolized through the liver significantly. Food does not affect the level of absorption but slows down the absorption speed. When used with food, the peak concentration in plasma decreases and is 1 hour later than the drug when hungry.
Distribution
Data from In vitro studies show that Perampanel binds about 95% to plasma proteins. In vitro studies show that Perampanel is not a significant substrate or inhibitor of organic polypeptides (OATP) TB1 and B3, organic anions (OAT) 1, 2, 3 and 4, organic cation (oct) 1, 2, and 3, and 3, and P-Glycoprotein and anti-cancer proteins (BCRP).
Metabolism
Perampanel is strongly metabolized through the original oxidation and glucuronids. The initial oxidation metabolism through the intermediate of CYP3A is based on the results of In vitro studies using CYP enzymes of recombinant and human liver microsom. However, this transformation has not been completely explained and other roads cannot be excluded.
After using Perampanel with radioactive markers, only a small amount of Perampanel metabolites have been observed in plasma.
Elimination
After taking a dose of Perampanel with radioactive marks for 8 healthy elderly, 30% of the recovered radiation has been found in urine and 70% in feces. In urine and feces, this recovered radioactive amount mainly includes a mixture of oxidant metabolites and conjugated metabolites.
In a population dynamic analysis, it consists of gross data from 19 phase 1, t1/2 studies of Perampanel's average 105 hours. When used in combination with carbamazepin is a strong CYP3A, T1/2 induction drug on average 25 hours.
Before taking Fycompa 4mg Eisai medicine for additional epilepsy (2 blisters x 14 tablets)
How to use
Fymcopa 4mg drug used orally. Should drink Fycompa in the form of single dose before going to bed.
Can take the same or not with food (see pharmacokinetics). Should swallow the whole tablet with a glass of water. Do not chew, crush or divide the pill. It is impossible to divide the pills exactly because there is no lines. To ensure adequate dose, need to drink whole tablets without chewing or crushing.
Dosage
adults and adolescents aged 12 and older
Need to adjust Fycompa dose according to the response of each patient to optimize the balance between efficiency and tolerance.
Local sperm epilepsy
Perampanel at a dose of 4 mg/day to 12 mg/day has been shown to be effective for local boundary seizures.
Should start the starting dose of Fycompa 2 mg/day. It is possible to increase the dose based on clinical response and tolerance for each increase of 2 mg (per week or every 2 weeks, according to the considering the sale time described below) to the maintenance dose of 4 mg/day - 8 mg/day.
Depending on the clinical response and the ability to tolerate each individual at a dose of 8 mg/day, the dose may increase by increasing the amount of 2 mg/day to 12 mg/day. The patient is taking the drugs simultaneously without shortening the sale time of Perampanel (see the interaction) should be adjusted to the dose more often than the 2 -week distance. The patient is taking the drugs while shortening the sale time of Perampanel (see the interaction) should be adjusted to the dose more often than the 1 -week distance.
Sexicular seizures - First -level convulsions
Perampanel at a dose of up to 8 mg/day has been shown to be effective in spastic seizures - convulsions of the whole primary.
Should start the starting dose of Fycompa 2 mg/day. The dose can be increased based on clinical response and tolerant ability in each amount, an increase of 2 mg (per week or every 2 weeks, according to the considering the sale time described below to the maintenance dose of up to 8 mg/day.
Depending on the clinical response and the ability to tolerate each individual at a dose of 8 mg/day, the dose can be increased to 12 mg/day that can be effective in some patients (see the cautious part when used). The patient is taking the drugs simultaneously without shortening the sale time of Perampanel (see the interaction) should be titrated than the dosage more often than at a distance of 2 weeks.
Patients who are taking drugs and shorten the sale time of Perampanel (see the interaction) should be titrated than the dose more often than at a distance of 1 week.
When stopping using Fycompa, the dose should be slowly reduced (see the cautious part when used).
Other objects
Elderly (65 years or older)
Clinical studies on fycompa in epilepsy have not included enough subjects aged 65 and over to determine whether they have a different response than younger subjects.
Analysis of safety information on 905 elderly people treated with Perampanel (in double blind studies conducted on non -epileptic indications) shows no age difference in safety data. Combined with no age difference in the use of Perampanel, the results show that it is not necessary to adjust the dose in the elderly.
Perampanel should be used carefully in the elderly due to the ability to interact with drugs in patients who use a lot of drugs (see the cautious part when used).
kidney failure
Unsurting dose adjustment in mild renal impairment patients. It is not recommended to use in patients with average renal impairment or severe renal failure or patients who are being bloody.
Hepatic failure
Increasing dose in patients with mild and medium liver failure should be based on clinical response and tolerance. For patients with mild or medium liver failure, the dose may be started at a dose of 2 mg. The dose should be adjusted with 2 mg, not faster every 2 weeks based on tolerance and efficiency. Perampanel dose for patients with mild and moderate liver failure must not exceed 8 mg. Do not recommend use in severe liver failure.
Group of children's patients
The safety and effectiveness of Perampanel in children under 12 years of age has not been determined. There is no data.
Note: The above dose is for reference only. Specific dosage depends on the condition and level of progression of the disease. For a suitable dose, you need to consult a doctor or medical specialist.What do
do when using overdose? In an overdose report that may lead to a dose of up to 264 mg, a patient had events about mental changes, agitation, aggression and recovery without sequelae. There is currently no specific antidote to the effect of Perampanel.
Need to take care of general support for patients including monitoring survival signs and observing the patient's clinical status. Due to the long selling time of the drug, the effects caused by Perampanel can last. Due to low kidney clearance, special interventions such as mandatory diuretic, hemolysis or uncertainty blood transfusion.
What to do when forgetting a dose?
If you forget more than 1 dose, for a period of less than 5 semi -waste cycles (3 weeks for patients who do not use anti -epileptic drugs that cause perampanel metabolism, 1 week for patients using anti -epilepsy drugs that cause perampanel metabolism (see interaction part), should consider to start treating treatment from the last dose level.
If the patient has stopped using Perampanel for a continuous time of more than 5 semi -waste cycles, it is recommended to comply with the recommendations on the starting dose mentioned above.
Side Effects
When using Fymcopa 4mg, you may experience unwanted effects (ADR).
Common, ADR> 1/100
Mental disorders: aggression, anger, anxiety, a state of confusion. Central nervous system disorders: loss of air conditioning, speech disorder, balance disorders, easily stimulated. Uncommon, 1/1000 Instructions on how to handle ADR When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.
Warnings
Before using the drug you need to read the instructions carefully and refer to the information below.
Contraindicated
Fymcopa 4mg contraindications in the following cases:
Caution when using
suicide thoughts
suicide thoughts and suicidal behavior have been reported in patients treated with anti -epileptic drugs in some indications. A comprehensive analysis of random tests that are controlled to placebo on anti -epileptic drugs has also shown a slight increase in the risk of suicide thoughts and suicide behavior. The mechanism of this risk is not known and existing data does not exclude the possibility of increasing risk to Perampanel.
Therefore, it is necessary to monitor patients on signs of suicide thoughts, suicide behaviors and appropriate treatment. It is necessary to advise patients and patients to take care of the patient) to find medical advice if the signs of suicide or suicide are appeared.
Central nervous system disorders
Perampanel can cause dizziness and drowsiness, so it can affect the ability to drive or operate machinery (see the effect of the drug on the ability to drive and operate machinery).
Oral contraceptives
At 12 mg/day, Fycompa can reduce the effectiveness of hormone contraceptives containing progesterone; In this case, it is recommended to use additional methods of contraception without hormones when using Fycompa (see interactive section).
End of treatment
recommend that the stopping of the drug should be done slowly to minimize the possibility of an corresponding seizure (see the use, dose). However, due to the long -term semi -discharged time and plasma concentrations decreased slowly later, it is possible to stop Perampanel when it is really necessary.
falls
may increase the risk of falling, especially in the elderly, unknown reasons.
aggression
Acting and hostile behavior has been reported in patients treated with Perampanel. In patients treated with Perampanel in clinical trials, aggression, anger and discomfort that have been reported more often at higher doses. Most of the unwanted effects are reported to be mild or medium levels and patients recover or do the dose adjustments.
However, the thought of harming others, physical attacks or threats has been observed in some patients (
Patients and caregivers need advice to notify medical experts immediately if they notice the mood or behaviors that have a significant change. Perampanel dose should be reduced if symptoms occur and should be stopped immediately if the symptoms are severe.
Abuse of drugs
Be careful in patients with a history of drug abuse and need to monitor patients on Perampanel abuse symptoms.
Anti -epilepsy drug causes CYP 3A touch simultaneously
The response ratio after using more perampanel at a fixed dose is less when the patient is used anti -epileptic drugs that cause enzyme CYP3A (carbamazepin, phenytoin, oxcarbazepine) simultaneously when compared to the response rate in patients using non -enzyme anti -epileptic drugs at the same time.
Need to monitor the response of patients when they are converted from anti -epileptic drugs that do not cause enzyme induction used simultaneously to anti -epileptic drugs that cause enzyme induction and vice versa. Depending on the clinical response and tolerance of each individual, the dose may increase or decrease by 2 mg at a time (see the usage, dose).
Other drugs that cause induction or inhibition of Cytochrom P450 are simultaneously used (in addition to anti -epileptic drugs)
Patients should be closely monitored for the ability to tolerate and clinically respond when extra or eliminate induction or Cytochrom P450 inhibitors, because the perampanel concentration in plasma may decrease or increase; Perampanel dose may be adjusted.
Fycompa contains lactose, so patients with rare genetic problems are galactose intolerance, lactase deficiency or glucose-galactose absorption should not be taken.
The ability to drive and operate machinery
Fycompa has a moderate effect on the ability to drive and operate machinery, Perampanel can cause dizziness and drowsiness, so it can affect the ability to drive or operate machinery.
It is necessary to advise patients not to drive, operate complicated machines or participate in other dangerous activities until they know how Perampanel affects their ability to perform these jobs (see the cautious part when used and interactive).
Pregnancy
Women are likely to be pregnant and contraception in men and women
It is not recommended to use Fycompa in women who are likely to get pregnant without using contraception unless they are really necessary.
Pregnant women
The amount of data is limited (less than 300 pregnancy results) from the use of Perampanel in pregnant women. Animal studies do not show any teratogenic effect in rats and rabbits, but toxicity to the embryo has been observed in rats with toxic doses for mother animals. Do not recommend using fycompa during pregnancy.
Reproduction
In a study of fertility in rats, prolonged and uneven sexual cycle has been observed in high doses (30 mg/kg) on Cai mice; However, these changes do not affect fertility and early embryo development. There is no effect on the fertility of male rats. The influence of Perampanel on the fertility of people has not been determined.
The period of breastfeeding. It is not clear whether Perampanel will be excreted in breast milk. Can not rule out the risk for infants/young children. Must decide to stop breastfeeding or stop avoiding treatment with Fycompa, need to consider the benefits of breastfeeding for children and the benefits of the mother's treatment. Interactive drug
Fycompa is not considered a strong induction drug or a strong Cytochrom P450 or UGT enzyme (see pharmacokinetics).
Oral contraceptives
In healthy women using 12 mg Fycompa (not 4 mg/day or 8 mg/day) for 21 days simultaneously with a oral contraceptive pills, Fycompa has shown to reduce the level of levonorgestrel (CMAX values (the highest concentration in plasma) and AUC (area under the curve) average each type decreased by 40%).
Ethinylelestradiol is not affected by Fycompa 12 mg while CMAX fell 18%. Therefore, it is advisable to consider the ability to reduce the effectiveness of oral contraceptives containing progestatif for women who need to use Fycompa 12 mg/day and should use a reliable contraceptive additional method (uterine equipment (IUD), condoms) (see caution when used).
Interaction between Fycompa and other anti -epileptic drugs
The ability to interact between Fycompa (up to 12 mg once a day) and other anti-epileptic drugs (AED) have been assessed in clinical and evaluation studies in the pharmacokinetic analysis of 4-phase-3-phase-phase studies including patients with local-starting spaces and hard-working seizures. The influence of these interactions on the average concentration in a stable state is summarized in the following table.
Monohydroxycarbazepin metabolites are not evaluated
Some anti -epileptic drugs are known as enzyme -induced drugs (carbamazepin, phenytoin, oxcarbazepin) that shows Perampanel's clearance and thus reduces the concentration of perampanel in plasma.
Carbamazepin, a strongly known enzyme -induced drug, reduces two -thirds of Perampanel concentration in a study conducted on healthy objects.
A similar result was observed in a population pharmacokinetic analysis in patients with localized epilepsy using Perampanel up to 12 mg/day and patients with spasticity-Ce seizures of all primary primary use of Perampanel up to 8 mg/day in clinical trials that are controlled to placebo.
The total clearance of Fycompa increases when used with carbamazepin (2.75 times), phenytoin (1.7 times) and Oxcarbazepine (1.9 times) are the known drugs that cause drug metabolic enzyme (see pharmacokinetics part). This effect should be taken into account and treated when adding or withdrawing these anti -epileptic drugs from the patient's treatment regimen.
In a population dynamic analysis in patients with local start -up epilepsy using Fycompa up to 12 mg/day in clinical trials that are controlled to placebo, Fycompa does not affect clinical significance to the clearance of clonazepam, levetiracetam, phenobarbital, phenytoin, topiramat, zonisamid, carbazepin, carbazepin,, carbazepin,, carbazepin, carbazepin,, carbazepin, carbaziram Lamotrigin and Valproic acid at the highest perampanel dose have been evaluated (12 mg/day).
In a population pharmacokinetic analysis of epilepsy, Perampanel reduced the clearance of oxcarbazepi 26%. Oxcarbazepine is rapidly metabolized by cytosolic reductase enzyme into an active metabolic substance, monohydroxycarbazepine. The influence of Perampanel on Monohydroxycarbazepin concentration is not known.
Perampanel is used for clinical effects regardless of other anti -epileptic drugs (AED).
Effect of Perampanel on substrates of CYP3A
In healthy subjects, Fycompa (6 mg once a day for 20 days) has reduced the AUC of Midazolam 13%. Midazolam concentration is not eliminated (or other sensitive CYP3A4 substrates) with higher fycompa dose.
The effect of the drug causing Cytochrom P450 on the pharmacokinetics of Perampanel
Strong drugs Cytochrom P450, like Rifampicin and Hypericum, are expected to reduce Perampanel's concentration. Felbamat has been shown to reduce the concentration of some drugs and can also reduce Perampanel's concentration.
Effects of Cytochrom P450 inhibitors on Perampanel's pharmacokinetics
In healthy subjects, Ketoconazole (400 mg once a day for 10 days) is a CYP3A4 inhibitor that increased the AUC of Perampanel by 20% and extended the waste time of Perampanel 15% (67.8 hours compared to 58.4 hours). It is impossible to eliminate greater effects when Perampanel is combined with a CYP3A inhibitor with a longer selling time than ketoconazole or when the inhibitor is used during longer treatment. Strong inhibitors of other ISOforms of Cytochrom P450 may also be likely to increase Perampanel levels.
levodopa. In healthy subjects, Fycompa (4 mg once a day for 19 days) does not affect CMAX or AUC of Levodopa.
alcohol
A study of pharmacokinetic interaction in healthy objects has shown the effects of Perampanel on jobs related to alertness and vigilance as the ability to drive is a combination or co -effect with the effects of alcohol.
Use Perampanel 12 mg/day to increase the level of anger, confusion and depression as evaluated by using the data of the 5 -point evaluation of the mood state (see the pharmacological part). These effects can also be observed when Fycompa is used in combination with other antidepressants on the central nervous system (CNS).
Group of children's patients
Research on drug interaction is only done in adults. In an analysis of population dynamics in teenage patients in phase 3 clinical studies, there is no remarkable difference between this group of patients and the general group.
Storage
Store no more than 30 ° C.
Other drugs
- ARTHROSIN EC 500
- CARBOMER 0.2% EYE GEL
- Dynastat
- FUSIDIC ACID / BETAMETHASONE 20 MG / G + 1 MG / G CREAM
- TARGINACT 10MG / 5MG PROLONGED-RELEASE TABLETS
- XATRAL XL 10MG TABLETS
Disclaimer
Every effort has been made to ensure that the information provided by Drugslib.com is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Drugslib.com information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Drugslib.com does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Drugslib.com's drug information does not endorse drugs, diagnose patients or recommend therapy. Drugslib.com's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.
The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Drugslib.com does not assume any responsibility for any aspect of healthcare administered with the aid of information Drugslib.com provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.
Popular Keywords
- metformin obat apa
- alahan panjang
- glimepiride obat apa
- takikardia adalah
- erau ernie
- pradiabetes
- besar88
- atrofi adalah
- kutu anjing
- trakeostomi
- mayzent pi
- enbrel auto injector not working
- enbrel interactions
- lenvima life expectancy
- leqvio pi
- what is lenvima
- lenvima pi
- empagliflozin-linagliptin
- encourage foundation for enbrel
- qulipta drug interactions