Few animal studies have proved that gabapentin has a potential to activate a serotonin receptor (5HT3) at the spinal level and also attenuate the function of microglial cells[6]. In some parts of the brain such as periaqueductal grey (PAG) and anterior cingulated cortex, gabapentin has been shown to elevate the level of GABA, a major inhibitory neurotransmitter, which might serve as an explanation of its’ efficacy in partial management of seizure[14]. Although gabapentin is approved to be used as an add-on treatment of focal epilepsies in 6 years and older patients and as monotherapy in patients older than 12 years of age, it seems to show no efficacy when used in a management of generalized tonic-clonic seizures, generalized absence …show more content…
Due to an effect of gabapentin at the level of hypothalamus to regulate the temperature, it can also be used as an effective non-hormonal therapy for hot flashes, a bothersome problem of menopause. It is shown to be more efficacy if used in patients with hot flashes that associated with sleep interference [17]. Study shows that a bioavailability of gabapentin is low and it is dose-dependent. The bioavailability of 300 mg is around 60% and decreasing to less than 30% if the dosage is 1600 mg 3 times a day [4; 11]. It has low protein binding property and it is eliminated unchanged in the urine, which means it will not change into toxic metabolite or intermediate that can be harmful to the body. Gabapentin has a short half life of 5 to 9 hours, but with renal impairment, it will increase[4]. A dose adjustment is required in patient who has creatinine clearance of 60 ml/min and in the elderly because of reduced renal function that has been thought to be decreased around 1% per year after the age of 40[4; 16]. A number needed to treat (NNT) of gabapentin is 6.3 and its number needed to harm (NNH) is 25.6, therefore it is considered a safe drug [6]. The ceiling effect has been reported to be 100 mg/kg in one study and 30-300 mg/kg in another study following oral administration [13]. The pharmacokinetic of absorption of gabapentin is not linear unlike other newer anti-seizure medications. The explanation for this event is because gabapentin absorption depends on
Treatment for epilepsy is often focused on controlling the seizures with the least amount of medication as possible. Antiepileptic drugs (AEDs) are the class used to accomplish this. Some of the AEDs that are used most often are Clonazepam, Diazepam, Divalproex, Gabapentin, and Phenytoin. The most common side effects of these medications include nausea, vomiting, sedation, fatigue, and lethargy. (Kwan,1; Benbadis, 3-5; Huethers,637)
The gabapentinoids, gabapentin and pregabalin are increasingly prescribed for a variety of conditions by medical practitioners from family physicians, neurologists, rheumatologists, orthopaedic surgeons, and others. The indications may vary according to the countries these medications are marketed in. Some of the indications include neuropathic pain, fibromyalgia, generalised anxiety disorder, epilepsy and so on.1
Gamma-Aminobutyric acid commonly referred to as GABA, and glutamate make up around 80 percent of the neurotransmitters found in brain. GABA dampens the activity in the brain while
In certain high risk individuals, medication may be initiated after the first seizure.10 Nonpharmacological treatment that can be initiated include a special diet or removal of the stimulus that could be causing the seizure, if it is known. If an individual is experiencing a seizure, the most important thing to remember is to remain calm. Seizures do not often warrant a 911 call if the person experiences them regularly, but they should be timed for their duration. If they last longer than three minutes, emergency personnel should be notified immediately. If the individual is standing, try to prevent them from falling and move any furniture out of the way. If they are already on the ground, try to position them on their side so any vomit or saliva can leak out.10 There are currently several drugs FDA approved to treat seizures which are each unique to their respective category.11 Seizure prophylaxis is crucial to patients that experience them to enhance their quality of life. Some common drugs used to treat seizures include Carbamazepine, Oxcarbazepine, Levetiracetam, Valproic Acid, Topiramate, Lamotrigine, Lacosamide, and the newest addition that recently acquired FDA approval is Brivaracetam, which is a chemical analogue of
Anticonvulsants main domains consist of treating seizures and bipolar disorder. Many researchers believe that anticonvulsants increase concentration of the neurotransmitter GABBA. Valproate, Carbamazepine, Lamotrigine, and Gabapentin are the main anticonvulsants used to treat the disorder.
With the increase of antidepressants being prescribed in the UK, in 2012, it reached over a half a million prescriptions. Some indications have shown with the increase of antidepressants is a rise in epilepsy/seizures, only a small number of researches have been done on people for “long-term” use. In the UK 1 in 100 people are diagnosed with epilepsy, the disorder is severe
Choosing an appropriate antiepileptic drug is the key to successful medical management of epilepsy in children. The choice of antiepileptic drug depends on several factors, of which the most important is accurate seizure classification. The other factors used to choose an appropriate antiepileptic drug include the side effect profile of the drug, The available age- and patient-appropriate preparations of the drug, Whether therapeutic levels are needed quickly or not (depending on the frequency and severity of the patient’s seizures), and the patient’s comorbidities.
There are many current drugs and therapies for seizure illnesses. One example of these drugs is, carbamazepine (epitol). Epitol, according to webmd.com, works in the sense of
In this study we found that the majority of epileptic children either using valporate mono therapy (57.7%) or valporate with other drug (7%). while carbamazepine was used in (25.4%) as monotherapy or with other drug in (2.8%). More than 50% of the doses were ranged between 10 to 28 mg/kg which is a moderate dose with (60.6%) of the patient's duration ranged between 1 year and 5 year.
On a fundamental level, seizures can be viewed as resulting from an imbalance between excitatory and inhibitory processes in the brain. Proposed mechanisms for the generation and spread of seizure activity within the brain include abnormalities in the membrane properties of neurons, changes in the ionic micro environment surrounding the neuron, decreased inhibitory neurotransmission which is primarily by gamma-amino butyric acid (GABA), or enhanced excitatory neurotransmission which is primarily mediated by the acidic amino acid,
Perampanel (Fycompa®) is a new antiepileptic drug used as a secondary therapy in adolescents and adults who suffer from partial-onset seizures. Perampanel was identified via a focused discovery program at Eisai Research Laboratories in London and Ibaraki Prefecture, Japan (Satlin, Kramer & Laurenza, 2013). It is a selective, non-competitive antagonist drug and is the first in this new class of antiepileptic drug known as a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptor antagonist on post-synaptic neurons; thereby selectively preventing the transmission of seizures by blocking the effects of glutamate(Perucca, French and Bialer, 2007). Glutamate affects how electrical activity is spread in the brain and it is believed perampanel helps to reduce seizures by blocking this electrical spread to the brain (Plosker, 2012). This is a
GABA is an inhibitory neurotransmitter critical in regulating anxiety and reducing stress. It does this by preventing overstimulation in the brain, and subduing excitatory neurotransmitters, which can cause anxiety when the brain is overstimulated. Hence, GABA deficiency results in overstimulation in the brain, and consequently, anxiety. Furthermore, those who experience anxiety due to GABA deficiency, often develop anxiety disorder/s (Neurotransmitters, Depression and Anxiety, 2008). Additionally, as GABA induces relaxation, analgesia, and sleep, “dysfunction of the GABA system is implicated in the pathophysiology of several neuropsychiatric disorders, including anxiety” (Neurotransmitters, Depression and Anxiety, 2008). GABA is synthesised by the amino acid glutamate decarboxylase (glutamine); thus, glutamine deficiency will result in GABA deficiency (Graham, n.d.). Whilst glutamine deficiency can be caused by diets lacking protein (Henderson, n.d.), it also results from Epilepsy (Glutamate decarboxylase deficiency, n.d.), which scientists believe have genetics aspects (Fisher and Saul, n.d.). Statistics suggest that in every 100 children born to parents with Epilepsy, between 2 and 5 will inherit Epilepsy (Epilepsy and inheritance, 2012). In cases where the cause of Epilepsy is unidentified, professionals believe that it can be attributed to an inherited low seizure threshold that makes individuals more susceptible to seizures (Epilepsy and inheritance, 2012). Additionally, children with an extensive history of, or mothers with Epilepsy in their genealogy, are more susceptible to the disorder, as shown in Figure
Gabapentin became a routine drug therapy for me because of manic disorder. I had panic attacks too. When I consulted the doctor, he made the necessary investigations and explained me that the best way to stay mentally calm and healthy is to take Gabapentin. I started taking 2700 mg per day in three divided doses. It helped me in getting rid of the panic attacks. I could even sleep properly because of this medicine. Gabapentin is responsible for increasing the gamma amino butyric acid levels in the brain indirectly. It does not bind to plasma proteins and therefore remains unchanged. It does not undergo any metabolism and is removed as it is, from the body in the form of urine. You can take this medicine with or without food as food does not affect its absorption. Gabapentin is available for purchase from online pharmacy stores for antiepileptic treatment. It is legal to buy Gabapentin online even without prescription.
More possible drugs treatments that are used include Gabapentin and Pregabalin. These two are thought to be effective in variety of neuropathic pain problems. They act by binding to voltage gated calcium channels. However, the side effects of this drug are somnolence and dizziness, which can be minimized by using gradual dose titration. Intravenous Lidocaine also has been reported that it brings good results in neuropathic pain. Mexiletine, an oral analogue of intravenous Lidocaine has been shown in a small study that is results in pain relief in phantom limb
Carbamazepine, an anticonvulsant structurally similar to tricyclic antidepressants, is used to treat partial seizures, tonic-clonic seizures, pain of neurologic origin such as trigeminal neuralgia, and psychiatric disorders including manic-depressive illness and aggression due to dementia. The response to carbamazepine is variable and may be due to its variable transport, especially across the blood-brain-barrier. The transporter that may confer drug resistance is