Portal:Anticonvulsants
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Introduction
Anticonvulsants (also commonly known as antiepileptic drugs or as antiseizure drugs) are a diverse group of pharmacological agents used in the treatment of epileptic seizures. Anticonvulsants are also increasingly being used in the treatment of bipolar disorder and borderline personality disorder, since many seem to act as mood stabilizers, and for the treatment of neuropathic pain. Anticonvulsants suppress the excessive rapid firing of neurons during seizures. Anticonvulsants also prevent the spread of the seizure within the brain.
Conventional antiepileptic drugs may block sodium channels or enhance γ-aminobutyric acid (GABA) function. Several antiepileptic drugs have multiple or uncertain mechanisms of action. Next to the voltage-gated sodium channels and components of the GABA system, their targets include GABAA receptors, the GAT-1 GABA transporter, and GABA transaminase. Additional targets include voltage-gated calcium channels, SV2A, and α2δ. By blocking sodium or calcium channels, antiepileptic drugs reduce the release of excitatory glutamate, whose release is considered to be elevated in epilepsy, but also that of GABA. This is probably a side effect or even the actual mechanism of action for some antiepileptic drugs, since GABA can itself, directly or indirectly, act proconvulsively. Another potential target of antiepileptic drugs is the peroxisome proliferator-activated receptor alpha. The drug class was the 5th-best-selling in the US in 2007.
Selected general articles
Paramethadione (brand name Paradione) is an anticonvulsant in the oxazolidinedione class developed by the Illinois-based pharmaceutical company Abbott Laboratories (known as AbbVie since January 1, 2013 ), and approved by the Food and Drug Administration in 1949 for the treatment of absence seizures, also called partial seizures.
In 1960, the yearly cost for 900 mg/day paramethadione was approximately $66, which would translate to $462 yearly in 2007 (with CPI inflation) if paramethadione was still sold. Read more...
Levetiracetam, marketed under the trade names Keppra among others, is a medication used to treat epilepsy. It is used for partial onset, myoclonic, or tonic-clonic seizures. It is the S-enantiomer of etiracetam.
Levetiracetam is available by mouth in two forms: immediate release and extended release. It is also available by injection. An immediate release tablet has been available as a generic in the United States since November 2008, and in the UK since 2011. The United States patent for the extended release tablet will expire on September 17, 2028. It was initially patented by UCB Pharma. Read more...
Pentobarbital (INN, AAN, BAN, USAN) or pentobarbitone (former AAN and BAN) is a short-acting barbiturate. Pentobarbital can occur as a free acid, but is usually formulated as the sodium salt, pentobarbital sodium. The free acid is only slightly soluble in water and in ethanol.
One brand name for this drug is Nembutal, coined by John S. Lundy, who started using it in 1930, from the structural formula of the sodium salt—Na (sodium) + ethyl + methyl + butyl + al (common suffix for barbiturates). Nembutal is trademarked and manufactured by the Danish pharmaceutical company Lundbeck (now produced by Akorn pharmaceuticals) and is the only injectable form of pentobarbital approved for sale in the United States. Read more...
Midazolam, marketed under the trade name Versed, among others, is a medication used for anesthesia, procedural sedation, trouble sleeping, and severe agitation. It works by inducing sleepiness, decreasing anxiety, and causing a loss of ability to create new memories. It is also useful for the treatment of seizures. Midazolam can be given by mouth, intravenously, or injection into a muscle, by spraying into the nose, or through the cheek. When given intravenously, it typically begins working within five minutes; when injected into a muscle, it can take fifteen minutes to begin working. Effects last for between one and six hours.
Side effects can include a decrease in efforts to breathe, low blood pressure, and sleepiness. Tolerance to its effects and withdrawal syndrome may occur following long-term use. Paradoxical effects, such as increased activity, can occur especially in children and older people. There is evidence of risk when used during pregnancy but no evidence of harm with a single dose during breastfeeding. It belongs to the benzodiazepine class of drugs and works by increasing the activity of the GABA neurotransmitter in the brain. Read more...
Phenobarbital, also known as phenobarbitone or phenobarb, is a medication recommended by the World Health Organization for the treatment of certain types of epilepsy in developing countries. In the developed world it is commonly used to treat seizures in young children, while other medications are generally used in older children and adults. It may be used intravenously, injected into a muscle, or taken by mouth. The injectable form may be used to treat status epilepticus. Phenobarbital is occasionally used to treat trouble sleeping, anxiety, and drug withdrawal and to help with surgery. It usually begins working within five minutes when used intravenously and half an hour when administered orally. Its effects last for between four hours and two days.
Side effects include a decreased level of consciousness along with a decreased effort to breathe. There is concern about both abuse and withdrawal following long-term use. It may also increase the risk of suicide. It is pregnancy category B or D (depending on how it is taken) in the United States and category D in Australia, meaning that it may cause harm when taken by pregnant women. If used during breastfeeding it may result in drowsiness in the baby. A lower dose is recommended in those with poor liver or kidney function, as well as elderly people. Phenobarbital is a barbiturate that works by increasing the activity of the inhibitory neurotransmitter GABA. Read more...
Temazepam (brand names Restoril and Normison, among others) is an intermediate-acting 3-hydroxy hypnotic of the benzodiazepine class of psychoactive drugs. It is the 3-hydroxy analogue of diazepam, and one of diazepam's primary active metabolites. In the US, temazepam is approved for the short-term treatment of insomnia. In addition, temazepam has anxiolytic (antianxiety), anticonvulsant, and skeletal muscle relaxant properties.
Temazepam was patented in 1965 and went on sale in the United States in 1981. Read more...
Oxcarbazepine is an anticonvulsant medication primarily used in the treatment of epilepsy. It may also be used as add-on therapy for bipolar disorder in people that have failed or are unable to tolerate other treatments.
Common side effects include nausea, vomiting, dizziness, drowsiness, headache, double vision and trouble with walking. Although not common, anaphylaxis may occur. Due to its structural similarities to carbamazepine there is approximately a 25–30% chance of cross-reactivity between the two medications. Read more...
Topiramate (brand name Topamax) is a broad-spectrum anticonvulsant (antiepilepsy) drug. In late 2012, topiramate was approved by the United States Food and Drug Administration (FDA) in combination with phentermine for weight loss. The drug had previously been used off-label for this purpose. Topiramate was originally produced by Ortho-McNeil Neurologics and Noramco, Inc., both divisions of the Johnson & Johnson Corporation. This medication was discovered in 1979 by Bruce E. Maryanoff and Joseph F. Gardocki during their research work at McNeil Pharmaceuticals.
The commercial usage of Topiramate began in 1996. Mylan Pharmaceuticals was granted final approval by the FDA for the sale of generic topiramate in the United States and the generic version was made available in September 2006. The last patent for topiramate in the U.S. was for use in children and expired on February 28, 2009. Read more...
Perampanel (sold under the trade name Fycompa) is an antiepileptic drug developed by Eisai Co. that is used in addition to other drugs to treat partial seizures and generalized tonic-clonic seizures for people older than 12 years. It was first approved in 2012 and as of 2016 its optimal role in the treatment of epilepsy relative to other drugs was not clear. It was the first antiepileptic drug in the class of selective non-competitive antagonist of AMPA receptors.
The drug label has a black box warning that the drug cause may cause serious psychiatric and behavioral changes; it may cause homicidal or suicidal thoughts. Other side effects have included dizziness, somnolence, vertigo, aggression, anger, loss of coordination, blurred vision, irritability, and slurred speech. Perampanel reduced the effectiveness of levonorgestrel oral contraceptives by about 40%. Women who may get pregnant should not take it as studies in animals show it may harm a fetus. Perampanel is liable to be abused; very high doses produced euphoria responses similar to ketamine. It is designated as a Schedule III controlled substance by the Drug Enforcement Administration. Read more...
Zonisamide is a medication used to treat the symptoms of epilepsy and Parkinson's disease. Chemically it is a sulfonamide. It serves as an anticonvulsant used primarily as an adjunctive therapy in adults with Parkinson's disease, partial-onset seizures; infantile spasm, mixed seizure types of Lennox–Gastaut syndrome, myoclonic and generalized tonic clonic seizure. Despite this it is also sometimes used as a monotherapy for partial-onset seizures. Read more...
Lorazepam, sold under the brand name Ativan among others, is a benzodiazepine medication. It is used to treat anxiety disorders, trouble sleeping, active seizures including status epilepticus, alcohol withdrawal, and chemotherapy-induced nausea and vomiting. It is also used during surgery to interfere with memory formation and to sedate those who are being mechanically ventilated. While it can be used for severe agitation, midazolam is usually preferred. It is also used, along with other treatments, for acute coronary syndrome due to cocaine use. It can be given by mouth or as an injection into a muscle or vein. When given by injection onset of effects is between one and thirty minutes and effects last for up to a day.
Common side effects include weakness, sleepiness, low blood pressure, and a decreased effort to breathe. When given intravenously the person should be closely monitored. Among those who are depressed there may be an increased risk of suicide. With long-term use, larger doses may be required for the same effect. Physical dependence and psychological dependence may also occur. If stopped suddenly after long-term use, benzodiazepine withdrawal syndrome may occur. Older people more often develop adverse effects. In this age group lorazepam is associated with falls and hip fractures. Due to these concerns, lorazepam use is generally only recommended for up to two to four weeks. Read more...
Pregabalin, marketed under the brand name Lyrica among others, is a medication used to treat epilepsy, neuropathic pain, fibromyalgia, and generalized anxiety disorder. Its use for epilepsy is as an add-on therapy for partial seizures with or without secondary generalization in adults. Some off-label uses of pregabalin include restless leg syndrome, prevention of migraines, anxiety disorders, and alcohol withdrawal. When used before surgery it does not appear to affect pain after surgery but may decrease the use of opioids.
Common side effects include: sleepiness, confusion, trouble with memory, poor motor coordination, dry mouth, problem with vision, and weight gain. Potentially serious side effects include angioedema, drug misuse, and an increased suicide risk. When pregabalin is taken at high doses over a long period of time, addiction may occur, but if taken at usual doses the risk of addiction is low. Pregabalin is a gabapentinoid and acts by inhibiting certain calcium channels. Read more...
Cannabidiol (CBD) is a naturally occurring cannabinoid constituent of cannabis. It was discovered in 1940 and initially thought not to be pharmaceutically active. It is one of at least 113 cannabinoids identified in hemp plants, accounting for up to 40% of the plant's extract.
Cannabidiol can be taken into the body in multiple different ways, including by inhalation of cannabis smoke or vapor, as an aerosol spray into the cheek, and by mouth. It may be supplied as an oil containing only CBD as the active ingredient (no added THC or terpenes), a full-plant CBD-dominant hemp extract oil, capsules, dried cannabis, or as a prescription liquid solution. Read more...
Primidone (INN, BAN, USP) is an anticonvulsant of the barbiturate class. It is a structural analog of phenobarbital and related to barbiturate-derivative anticonvulsants. The active metabolites, phenobarbital, p-hydroxyphenobarbital, and phenylethylmalonamide, are also anticonvulsants. Primidone was once a mainstay anticonvulsant in the treatment of partial and generalized seizures and was the treatment of choice for secondarily generalized seizures originating in the temporal lobes, especially when combined with phenytoin, but by the early 1980s, carbamazepine had surpassed it in popularity due to the latter's lower incidence of sedation. As time passed and more and more anticonvulsants came on the market, primidone was pushed further and further away from its former place of prominence, and major Western pharmaceutical corporations became less and less interested in manufacturing and selling it. It has largely fallen into disuse in the developed world as more and more anticonvulsants entered the market, and it has been withdrawn from various markets around the world. Read more...
Topiramate (brand name Topamax) is a broad-spectrum anticonvulsant (antiepilepsy) drug. In late 2012, topiramate was approved by the United States Food and Drug Administration (FDA) in combination with phentermine for weight loss. The drug had previously been used off-label for this purpose. Topiramate was originally produced by Ortho-McNeil Neurologics and Noramco, Inc., both divisions of the Johnson & Johnson Corporation. This medication was discovered in 1979 by Bruce E. Maryanoff and Joseph F. Gardocki during their research work at McNeil Pharmaceuticals.
The commercial usage of Topiramate began in 1996. Mylan Pharmaceuticals was granted final approval by the FDA for the sale of generic topiramate in the United States and the generic version was made available in September 2006. The last patent for topiramate in the U.S. was for use in children and expired on February 28, 2009. Read more...
Clorazepate, sold under the brand names Tranxene among others, is a benzodiazepine medication. It possesses anxiolytic, anticonvulsant, sedative, hypnotic, and skeletal muscle relaxant properties. Clorazepate is an unusually long-lasting benzodiazepine and serves as a majoritive prodrug for the equally long-lasting desmethyldiazepam, which is rapidly produced as an active metabolite. Desmethyldiazepam is responsible for most of the therapeutic effects of clorazepate. Read more...
Retigabine or ezogabine is an anticonvulsant used as an adjunctive treatment for partial epilepsies in treatment-experienced adult patients. The drug was developed by Valeant Pharmaceuticals and GlaxoSmithKline. It was approved by the European Medicines Agency under the trade name Trobalt on March 28, 2011, and by the United States Food and Drug Administration (FDA), under the trade name Potiga, on June 10, 2011. Production has been discontinued in June 2017.
Retigabine works primarily as a potassium channel opener—that is, by activating a certain family of voltage-gated potassium channels in the brain. This mechanism of action is unique among antiepileptic drugs, and may hold promise for the treatment of other neurologic conditions, including tinnitus, migraine and neuropathic pain. The company is withdrawing retigabine from clinical use in 2017. Read more...
Ethoxzolamide (alternatively known as ethoxyzolamide) is a sulfonamide medication that functions as a carbonic anhydrase inhibitor. It is used in the treatment of glaucoma and duodenal ulcers, and as a diuretic. It may also be used in the treatment of some forms of epilepsy. Read more...
Diazepam, first marketed as Valium, is a medicine of the benzodiazepine family that typically produces a calming effect. It is commonly used to treat a range of conditions including anxiety, alcohol withdrawal syndrome, benzodiazepine withdrawal syndrome, muscle spasms, seizures, trouble sleeping, and restless legs syndrome. It may also be used to cause memory loss during certain medical procedures. It can be taken by mouth, inserted into the rectum, injected into muscle, or injected into a vein. When given into a vein, effects begin in one to five minutes and last up to an hour. By mouth, effects may take 40 minutes to begin.
Common side effects include sleepiness and trouble with coordination. Serious side effects are rare. They include suicide, decreased breathing, and an increased risk of seizures if used too frequently in those with epilepsy. Occasionally excitement or agitation may occur. Long term use can result in tolerance, dependence, and withdrawal symptoms on dose reduction. Abrupt stopping after long-term use can be potentially dangerous. After stopping, cognitive problems may persist for six months or longer. It is not recommended during pregnancy or breastfeeding. Its mechanism of action is by increasing the effect of the neurotransmitter gamma-aminobutyric acid (GABA). Read more...
Zonisamide is a medication used to treat the symptoms of epilepsy and Parkinson's disease. Chemically it is a sulfonamide. It serves as an anticonvulsant used primarily as an adjunctive therapy in adults with Parkinson's disease, partial-onset seizures; infantile spasm, mixed seizure types of Lennox–Gastaut syndrome, myoclonic and generalized tonic clonic seizure. Despite this it is also sometimes used as a monotherapy for partial-onset seizures. Read more...
Lamotrigine, sold as the brand name Lamictal among others, is an anticonvulsant medication used to treat epilepsy and bipolar disorder. For epilepsy, this includes focal seizures, tonic-clonic seizures, and seizures in Lennox-Gastaut syndrome. In bipolar disorder, it is used to treat acute episodes of depression, rapid cycling in bipolar type II, and prevent recurrence in bipolar type I.
Common side effects include sleepiness, headache, vomiting, trouble with coordination, and rash. Serious side effects include lack of red blood cells, increased risk of suicide, Stevens-Johnson syndrome, and allergic reactions. There are concerns that use during pregnancy or breastfeeding may result in harm. Lamotrigine is a phenyltriazine, making it chemically different from other anticonvulsants. How it works is not exactly clear. It appears to increase the action of gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter in the central nervous system and decrease voltage-sensitive sodium channels. Read more...
Brivaracetam (trade name Briviact), a chemical analog of levetiracetam, is a racetam derivative with anticonvulsant (antiepileptic) properties. It is marketed by the pharmaceutical company UCB. In India it is co-promoted and distributed by Dr. Reddy's Laboratories. Read more...
Eslicarbazepine acetate (trade names Aptiom in North America, Zebinix in Europe, Exalief in Russia, Eslicarba in Egypt ), abbreviated as ESL, is an anticonvulsant medication approved for use in Europe and the United States as monotherapy or adjunctive therapy (additional therapy) for partial-onset seizures epilepsy.
Similarly to oxcarbazepine, ESL behaves as a prodrug to (S)-(+)-licarbazepine. As such, their mechanisms of action are identical. Read more...
Hydantoin, or glycolylurea, is a heterocyclic organic compound with the formula CH2C(O)NHC(O)NH. It is a colorless solid that arises from the reaction of glycolic acid and urea. It is an oxidized derivative of imidazolidine. In a more general sense, hydantoins can refer to a groups and a class of compounds with the same ring structure as the parent. For example, phenytoin (mentioned below) has two phenyl groups substituted onto the number 5 carbon in a hydantoin molecule. Read more...
Paraldehyde is the cyclic trimer of acetaldehyde molecules. Formally, it is a derivative of 1,3,5-trioxane. The corresponding tetramer is metaldehyde. A colourless liquid, it is sparingly soluble in water and highly soluble in ethanol. Paraldehyde slowly oxidizes in air, turning brown and producing an odour of acetic acid. It quickly reacts with most plastics and rubber.
Paraldehyde was first observed in 1835 by the German chemist Justus Liebig; its empirical formula was determined in 1838 by Liebig's student Hermann Fehling. Paraldehyde was first synthesized in 1848 by the German chemist Valentin Hermann Weidenbusch (1821–1893), another student of Liebig; he obtained paraldehyde by treating acetaldehyde with acid (either sulfuric or nitric acid). It has uses in industry and medicine. Read more...
Three-dimensional representations of several fatty acids. Saturated fatty acids have perfectly straight chain structure. Unsaturated ones are typically bent, unless they have a trans configuration.
In chemistry, particularly in biochemistry, a fatty acid is a carboxylic acid with a long aliphatic chain, which is either saturated or unsaturated. Most naturally occurring fatty acids have an unbranched chain of an even number of carbon atoms, from 4 to 28. Fatty acids are usually not found per se in organisms, but instead as three main classes of esters: triglycerides, phospholipids, and cholesterol esters. In any of these forms, fatty acids are both important dietary sources of fuel for animals and they are important structural components for cells. Read more...
Vigabatrin, brand name Sabril, is an antiepileptic drug that inhibits the breakdown of γ-aminobutyric acid (GABA) by acting as a suicide inhibitor of the enzyme GABA transaminase (GABA-T). It is also known as γ-vinyl-GABA, and is a structural analogue of GABA, but does not bind to GABA receptors. Read more...
Nitrazepam (brand names Alodorm and Mogadon, among others) is a hypnotic drug of the benzodiazepine class used for short-term relief from severe, disabling anxiety and insomnia. It also has sedative (calming) properties, as well as amnestic (inducing forgetfulness), anticonvulsant, and skeletal muscle relaxant effects. Read more...
Phenytoin (PHT), sold under the brand name Dilantin among others, is an anti-seizure medication. It is useful for the prevention of tonic-clonic seizures and partial seizures, but not absence seizures. The intravenous form is used for status epilepticus that does not improve with benzodiazepines. It may also be used for certain heart arrhythmias or neuropathic pain. It can be taken intravenously or by mouth. The intravenous form generally begins working within 30 minutes and is effective for 24 hours. Blood levels can be measured to determine the proper dose.
Common side effects include nausea, stomach pain, loss of appetite, poor coordination, increased hair growth, and enlargement of the gums. Potentially serious side effects include sleepiness, self harm, liver problems, bone marrow suppression, low blood pressure, and toxic epidermal necrolysis. There is evidence that use during pregnancy results in abnormalities in the baby. It appears to be safe to use when breastfeeding. Alcohol may interfere with the medication's effects. Read more...
Clonazepam, sold under the brand name Klonopin among others, is a medication used to prevent and treat seizures, panic disorder, and for the movement disorder known as akathisia. It is a tranquilizer of the benzodiazepine class. It is taken by mouth. It begins having an effect within an hour and lasts between 6 and 12 hours.
Common side effects include sleepiness, poor coordination, and agitation. Long-term use may result in tolerance, dependence, and withdrawal symptoms if stopped abruptly. Dependence occurs in one-third of people who take clonazepam for longer than four weeks. It may increase risk of suicide in people who are depressed. If used during pregnancy it may result in harm to the baby. Clonazepam binds to GABAA receptors and increases the effect of the chief inhibitory neurotransmitter gamma-aminobutyric acid (GABA). Read more...
Stiripentol (marketed as Diacomit by Laboratoires Biocodex) is an anticonvulsant drug used in the treatment of epilepsy. It is approved for the treatment of Dravet syndrome, an epilepsy syndrome. It is unrelated to other anticonvulsants and belongs to the group of aromatic allylic alcohols. Read more...
Topiramate (brand name Topamax) is a broad-spectrum anticonvulsant (antiepilepsy) drug. In late 2012, topiramate was approved by the United States Food and Drug Administration (FDA) in combination with phentermine for weight loss. The drug had previously been used off-label for this purpose. Topiramate was originally produced by Ortho-McNeil Neurologics and Noramco, Inc., both divisions of the Johnson & Johnson Corporation. This medication was discovered in 1979 by Bruce E. Maryanoff and Joseph F. Gardocki during their research work at McNeil Pharmaceuticals.
The commercial usage of Topiramate began in 1996. Mylan Pharmaceuticals was granted final approval by the FDA for the sale of generic topiramate in the United States and the generic version was made available in September 2006. The last patent for topiramate in the U.S. was for use in children and expired on February 28, 2009. Read more...
Methylphenobarbital (INN), also known as mephobarbital (USAN, JAN) and mephobarbitone (BAN), marketed under brand names such as Mebaral, Mephyltaletten, Phemiton, and Prominal, is a drug which is a barbiturate derivative and is used primarily as an anticonvulsant, but also as a sedative and anxiolytic. It is the N-methylated analogue of phenobarbital and has similar indications, therapeutic value, and tolerability. Read more...
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