How a New Medicine offer Lot of promise for Epilepsy
Before we read about this new medicine we will review more info about Epilepsy
What is Epilepsy?
Epilepsy is a neurological condition, which affects the nervous system. Epilepsy is also known as a seizure disorder. It is usually diagnosed after a person has had at least two seizures that were not caused by some known medical condition like alcohol withdrawal or extremely low blood sugar. Sometimes, according to the International League against Epilepsy, epilepsy can be diagnosed after one seizure, if a person has a condition that places them at high risk for having another.
New Information- How a New Medicine offer Lot of promise for Epilepsy
This new drug Fycompa arrival is exciting news. Mechanistically, this is the first of its kind drug. Perhaps combining this drug with an agent of a different mechanism of action may be beneficial but those studies have yet to be completed.
On October 22, 2012 the U.S. Federal Drug Administration (FDA) approved the drug Perampanel (Fycompa) for use in patients with partial onset seizures as adjunct therapy. Perampanel is a first in class, noncompetitive antagonist of a particular glutamate receptor known as AMPA, which are found on postsynaptic neurons. Glutamate is a primary neurotransmitter involved in excitation in the central nervous system and is implicated in a number of conditions, particularly epilepsy. Although, the precise way by which Perampanel exerts its effects in humans is not fully understood but it is believed to be through this mechanism.
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Epilepsy is also known as a seizure disorder. It is usually diagnosed after a person has had at least two seizures that were not caused by some known medical condition like alcohol withdrawal or extremely low blood sugar.
Fycompa’s effectiveness was proven through three trials in which it was utilized as add-on treatment for partial onset seizures given on a once a day basis. These trials were randomized, double blind, placebo-controlled, multi-centered in adult and adolescent patients. Two studies compared doses of Fycompa at 8 and 12 mg. per day with placebo,
and the third study compared doses of 2, 4, and 8 mg. of Perampanel against placebo. The pooled responder rate was 29% for 4 mg. a day; 35% for 8 mg. a day; and 35% for 12 mg. per day. No benefit was observed at the dose of 12 mg. as compared to the dose of 8 mg. in an overall population. A clinically meaningful reduction in seizure frequency was observed as early as the second week of dosing when patients reached a daily dose of 4 mg. Pediatric population studies are currently underway and the results from trials in that population is not available, nor is it approved for use in the younger aged patients. There have been three pivotal, double blind, placebo-controlled studies for adolescents between the age of 12 and 18. The results in these adolescents are similar to those seen in the adult population.
Pharmacology
The pharmacology of Perampanel has been studied in healthy adult subjects with partial onset seizures, as well as in other neurological and medical conditions. Perampanel is easily absorbed after oral administration with no evidence of first pass metabolism. When taken with food peak concentrations delayed by two hours. The drug is extensively metabolized via primary oxidation and sequential glucuronidation in the liver. Primary metabolism is mediated by CYP3A and this means that there are some aspects of drug interactions that one will need to consider. The drug has linear pharmacokinetics and there is a linear relationship between dose and concentration over the dose range of 2-12 mg. per day.
The drug does have some known adverse effects associated with this drug. The most common ones are anxiety, confusion, imbalance, double vision, dizziness, gastrointestinal distress or nausea, imbalance – some of which may lead to falls on some occasions, and increased weight. The effects of Perampanel on tasks involving alertness and vigilance, such as driving, were additive to the effects of alcohol itself. Multiple doses of Perampanel increased levels of anger, confusion, and depression, particularly when taken with alcohol. Fycompa may lead to euphoria and other similar feelings in some patients. Thus, the drug will be a scheduled in the United States. Final labeling and information is not yet available.
Drug Interactions
Because this drug is metabolized through the liver there are specific drug interactions that need to be considered. Fycompa may decrease the effectiveness of progesterone-containing hormone contraceptives. It is also known to decrease levonorgestrel by almost 40%; ethynylestradiol is decreased by 18%. Therefore, considerations for contraception need to be considered. Fycompa itself may have decreased levels when taken with carbamazepine, oxcarbazepine, and topiramate. However, Fycompa may decrease the levels of carbamazepine, clobazam, lamotrigine, valproic acid, but increase the level of oxcarbazepine. Carbamazepine is a known enzyme inducer and it reduces Perampanel levels by almost two-thirds. Therefore, dosing needs to be adjusted when taken with carbamazepine, phenytoin or oxcarbazepine. Perampanel decreases the clearance of oxcarbazepine. It does decrease midazolam levels by 13%. Drugs such as rifampin may decrease Perampanel concentrations. Felbamate may also reduce Perampanel concentration as well. Ketoconazole increases Perampanel by 20% and prolongs its half life by 15%. Fycompa has no impact on Levodopa.
Pregnancy, Fertility, and Lactation
There is limited data with regards to pregnancy experience with Fycompa. Studies in animals do not indicate any teratogenic effects but this is something that needs to be proven with more studies as more individuals use the drug. With regards to breastfeeding, studies in lactating rats have shown excretion of Perampanel and/or its metabolites in milk. It is not known whether Perampanel is excreted in human milk, however. It is important to understand those impacts when making a decision. With regards to fertility, there is no impact on male fertility and the effect of Perampanel in human fertility has not been established.
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