Anticonvulsants and Seizure Treatment
The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures.
| Epileptic Disorder: Medications and Descriptions | 14th May 2009, 12:30 | |
| Primidone (Mysoline) Primidone, which is a deoxybarbiturate, is a useful agent in the treatment of grand mal and psychomotor epilepsy. It is generally given in combination with diphenylhydantoin in order to achieve better results in the treatment of grand mal epilepsy and myoclonic seizures. Dosage: The average daily oral dose of primidone is 0.5 to 2 g. Adverse Effects: The most common complaint is a feeling of lethargy, drowsiness, and dizziness. Sometimes the drug may cause visual disturbances. Precautions The drug should be stopped immediately if there is any sign of an allergic reaction. It should not be administered to a patient who has any previous history of mental illness or has an unstable personality . Lamotrigine (Lamitor 25 mg, 50 mg) A broad spectrum anti-epileptic effective in refractory cases. Its adverse effects are dizziness, unsteadiness, double vision and skin rash. Gabapentin (Neurontin) It is an add-on drug for the treatment of resistant partial seizures. It can be used as first line drug for diabetic neuropathic pain and post-theraupetic neuralgia. It is also useful in manic depressive illness and prevention of migraine. Its unwanted effects are mild sedation and unsteadiness. Topiramate It is used as an add-on drug for the treatment of refractory grand mal and partial seizures. Adverse effects are poor concentration, unsteadiness, sedation, weight loss and occasional formation of kidney stones. Psychitric symptoms may also appear. Tiagabine, Vigabatrin and Levetiracetum are some of the other drugs. Drugs Used in Petit mal (Minor) Epilepsy Ethosuximide (Zarontin) This drug is a succinimide, which is preferred in the treatment of patients suffering from petit mal (absence seizures) epilepsy. Ethosuximide has gained more popularity because of its less toxic than other drugs. It is also used in combination with diphenylhydantoin or primidone (described earlier in this chapter) to control unmasked grand mal convulsions which occur in the majority of patients suffering from petit mal epilepsy. Dosage: The average daily oral dose of ethosuximide is 0.5 to 1.5 g. Adverse Effects: In many patients it causes nausea, vomiting, and abdominal distress. Some patients may experience drowsiness, dizziness, or headache, but these usually decrease on continued use. In some cases of unstable personalities, these agents may cause aggressiveness, agitation, anxiety, restlessness, or euphoria (a false sense of well-being). A few cases of depression of the bone marrow due to an allergic reaction have also been reported. Precautions It should not be taken on an empty stomach. Patients with an unstable personality should be carefully observed for development of abnormal behaviour. The drug should be stopped immediately if symptoms like anxiety or agitation appear. The drug should be stopped as soon as any symptoms of allergy such as skin rash, or agitation appear. Total and differential white blood cell count should be done periodically. |
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| Neurontin (Gabapentin) for Chronic Back Pain | 30th April 2009, 13:40 | |
| For chronic back pain, Neurontin (Gabapentin) will work for most people. Neurontin is really excreted by the body primarily through the kidneys and not by the liver like most other things. It has also been used for therapy in the treatment of partial seizures in pediatric patients from the ages of 3 to 12. In the 1990's, the sale of Neurontin was approved as treatment for epileptic seizures. The FDA has approved this to treat epilepsy only when used with another drug for shingles pain. The recommended dosage is 3 times a day. Gabapentin is indicated for the management of postherpetic neuralgia in adults. This medicine does not interact with other seizure medicines, so it can be used as an add on. It has not been approved to treat severe RLS (restless leg syndrome). Neurontin is expensive and one of the best selling drug in the world used for the treatment of chronic back pain. The average cost is $400/month for 3200mg/day. The effects are good even though it is an expensive drug to treat pain. However, if you constantly need the medication and want to save money you can buy generic Neurontin instead of the brand one. Generic versions are usuallu 30 - 40% cheaper. Neurontin is the first oral medication approved by the FDA and found in breast milk. It was prescribed for epilepsy. The medicine has also been approved for a few off label uses. One of the biggest selling points is that it has few side effects. Neurontin does not produce any active or inactive metabolites and is not metabolized by the body. It can be taken with or without food orally. Neurontin is good for the nerve damage from chronic back pain and should not be used as pain management. Pfizer is the manufacturer and this is its best selling drug. It is popular too. It is one of the 50 most prescribed medicines in the United States in 2003. Neurontin is well tolerated, has relatively mild side effects and also opasses through the body unmetabolized. Therefore, is often one of the first drugs prescribed. |
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| Second-generation AEDs | 30th April 2009, 12:59 | |
| Since 1993 there have been a number of new medications approved for the treatment of epilepsy. These new medications have provided new options that were not previously available to treat epilepsy. Many patients that have not had their seizures controlled with the older medications have found that the new medications have provided them seizure control. Felbamate was approved by the FDA in early 1994 and was the first new drug for epilepsy to be approved in 15 years. Although there was great initial enthusiasm for this agent, in less than a year post-marketing surveillance revealed an unacceptably high rate of drug-related aplastic anemia. Lamotrigine was approved in late 1994. It is thought to act by blockade of sodium channels; useful in partial seizures and possibly also in primary generalized seizures. Gabapentin is approved for use as an add-on medication for treatment of partial seizures. Mechanism is uncertain; toxicity is low and does not induce or inhibit metabolism of other anticonvulsants. Topiramate approved in 1997; unknown mechanism, possibly acts on voltage-gated Na+ channels. Tiagabin - an inhibitor of GABA reuptake, approved in 1997 as add-on for treatment of partial seizures. Levetiracetam analog of piracetam, mechanism uncertain, approved as add-on for refractory partial seizures. Vigabatrin - an inhibitor of GABA transaminase, the degradative enzyme for GABA; approved as an add-on agent in refractory epilepsy Zonisamide, a sulfonamide derivative approved for partial seizures; acts on Na+ channels. Pregabalin - this drug is approved for use in adults as adjunct therapy for partial onset seizures. Lyrica, which is also used to treat diabetic peripheral neuropathy and postherpetic neuralgia, can be taken 2 or 3 times a day. All these medications belong to the second generation of AEDs. It is generally considered that these AEDs are better tolerated and safer than first-generation AEDs as they have less severe side effects. |
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| Classes of Anticonvulsants | 29th April 2009, 13:40 | |
| Anticonvulsants are broken up into different classes based upon chemical structure, how they work in the brain or how your liver deals with them. In the US market we have the following valproates: Depakote (divalproex sodium) Depakene (valproic acid), and the rarely used (but much more popular overseas) Depacon (valproate sodium or sodium valproate). It should be noted that valproic acid is not the generic for Depakote. These three meds are very closely related chemically, and are often lumped together as the same med. But they aren't really. Next up are the Enzyme Inducing Anti-Epileptic Drugs, or EIAEDs. A family of meds that produce similar effects on the liver, and wildly different results in the brain. They are grouped together though because of important drug-drug interactions with other meds, including other anticonvulsants, antidepressants, antipsychotics, and other medications. The drugs in this family include: Dilantin (phenytoin) Luminal (phenobarbital) Tegretol / Carbatrol (carbamazepine) Trileptal (oxcarbazepine) Only the last two work in similar ways in the brain and chemically related and a patient can easily swithch between Tegretol and Trileptal without too much trouble. Dilantin is also classed as a Hydantoin, along with Cerebyx. Then there are the GABA analogues. These meds are basically fake GABA, a neurotransmitter critical to treating epilepsy, bipolar disorder, anxiety disorder and a variety of other issues. Gabitril isn't really a GABA analogue, but it gets classified as such because all it does is potent GABA reuptake inhibition and absolutely nothing else. No voltage channel modification, no messing with glutamate or kainate. Neurontin (gabapentin) Gabitril (tiagabine) Technically the benzodiazepines are also anticonvulsants, and while they have their place in treating both epilepsy and bipolar disorder, they have a section of their own. A couple meds we may or may not cover are the Succinimides - Celontin and Zarontin. These are kind of last resort meds for absence and partial seizures. As they are new it is rather difficult to find information about them. That leaves all the other anticonvulsants: Felbatol (felbamate) Lyrica (pregablin) Keppra (levetiracetam) Lamictal (lamotrigine) Mysoline (primodone) (withdrawn from most markets, good luck finding it) Topamax (topiramate) Zonegran (zonisamide) |
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| AEDs and their side-effects | 29th April 2009, 12:45 | |
| In December 2008, the U.S. Food and Drug Administration (FDA) announced that medications used to treat epilepsy must carry label warnings indicating that they may increase the risk for suicidal thoughts and behavior (suicidality). In recent studies, approximately one in 500 patients taking these drugs experienced this higher risk. According to the FDA, patients who have epilepsy should read the patient information inserts provided with anticonvulsant medications carefully, should be monitored for changes in behavior, and should speak with a qualified physician about their epilepsy treatment. Each anticonvulsant may have slightly different side effects. Common side effects of frequently prescribed AEDs such as Stavzor, Depakote, Neurontin and the big one Topamax (topamirate) may include: dizziness, drowsiness, fatigue, nausea, and tremor. All side effects can be generally divided into two groups: normal side effect and long-term effects. As for the first group, besides the conditions mentioned above, the possible side effects may include feeling dopey all of the time, having nightmares and having an increase in appetite. Many people also lose interest in sex. Your blood pressure may go down when on these, so guys your body may not be able to pump enough blood to Mr. Happy in order to get or maintain an erection. Some people also lose their hair or get thinning hair. What concerns long-term side effects they are a bit more serious. For some people, the loss of interest in sex winds up being a long-term side effect instead of a short-term side effect. For others, baldness or thinning hair as well as feeling sleepy all of the time. Perhaps the most common long-term side effect is weight gain. You feel sleepy and your appetite increases, so weight gain is kind of inevitable. You need to be sure you are eating sensibly when on thiese kinds of medications. But you may not be that hungry, because some anti-convulsants like depakote give chronic heartburn. With some meds like depakote, one may need to take tests to be sure that the liver is functioning properly because the medicine could make your liver very cranky. |
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| Anticonvulsants: General Overview | 28th April 2009, 07:22 | |
| The anticonvulsants are a diverse group of pharmaceuticals used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder, since many seem to act as mood stabilizers. The goal of an anticonvulsant is to suppress the rapid and excessive firing of neurons that start a seizure. Failing this, a good anticonvulsant would prevent the spread of the seizure within the brain and offer protection against possible excitotoxic effects that may result in brain damage. There are several possible mechanisms of action: some of them block Sodium (Na+) channels and Calcium (Ca2+) channels, while some block AMPA receptors or NMDA receptors. Some anticonvulsants inhibit the metabolism of GABA or increase its release. Anticonvulsants most commonly used are barbiturates and benzodiazepines. Instead of using only one drug, people often take two or more anticonvulsant medications to prevent seizures; possible interaction may cause several health problems. Anticonvulsant drugs include medicines such as phenobarbitol, carbamazepine (Tegretol), phenytoin (Dilantin), and valproic acid (Depakote, Depakene). The drugs are available only with a physician's prescription and come in tablet, capsule, liquid, and "sprinkle" forms. The recommended dosage depends on the type of anti-convulsant, its strength, and the type of seizures for which it is being taken. Phenobarbital is an anticonvulsant drug that has been used since 1912 and it is still one of the better drugs for this purpose. Phenobarbital is used to treat infants (ages 01 year) with any type of seizure disorder, and other children with generalized, partial, or febrile seizures. It is also used for treatment of status epilepticus (seizures lasting longer than 15 minutes). The barbiturates, such as mephobarbital, and metharbital, are also sometimes used as anticonvulsants. Of the family of barbiturate drugs, these are the only three that are satisfactory for use over a long period of time. They act directly on the central nervous system and can produce effects such as drowsiness, hypnosis, deep coma, or death, depending upon the dose taken. Because they are habit forming drugs, the barbiturates probably are the least desirable to use as anticonvulsant drugs. Valproic acid compounds are also antiepileptic drugs, though their mechanism of action is unknown. One of their major side effects is liver toxicity, appearing most often in young patients and in those who are taking more than one anticonvulsant drug. Another class of anticonvulsant drugs, the succinimides, suppress the brain wave pattern leading to seizures and stabilizes the cortex against them. These are useful drugs in the treatment of petit mal epilepsy, and like phenytoin, must be withdrawn slowly. Neurontin is another anticonvulsant medication belonging to the antiepileptic drug class. Another name for this drug is Gabapentin. It is a medication used as add-on therapy with other antiepileptic medications to treat partial seizures common among adults over 12 years old with epilepsy. Sources: 1. Anticonvulsants - www.science.jrank.org 2. http://en.wikipedia.org/wiki/Anticonvulsant |
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