Dictionary:
an·ti·con·vul·sant (ăn'tē-kən-vŭl'sənt, ăn'tī-)
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5min Related Video:
anticonvulsant |
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Neurological Disorder:
Anticonvulsants |
Definition
Anticonvulsants are a class of drugs indicated for the treatment of various types of seizures associated with seizure disorders such as epilepsy, a neurological dysfunction in which excessive surges of electrical energy are emitted in the brain, and other disorders.
Some anticonvulsants are indicated for other medical uses. Some hydantoins, such as phenytoin, are also used as skeletal muscle relaxants and antineuralgics in the treatment of neurogenic pain. Some anticonvulsants and antiepileptic drugs (AEDs) are used in psychiatry for the treatment of bipolar disorders (manic-depression).
Purpose
Although there is no cure for the disorder, anticonvulsants are often effective in controlling the seizures associated with epilepsy. The precise mechanisms by which many anticonvulsants work are unknown, and different sub-classes of anticonvulsants are thought to exert their therapeutic effects in diverse ways. Some anticonvulsants are thought to generally depress central nervous system (CNS) function. Others, such as GABA inhibitors, are thought to target specific neurochemical processes, suppress excess neuron function, and regulate electrochemical signals in the brain.
Description
There are several sub-classes and types of anticonvulsants. They are marketed in the United States under a variety of brand names.
A physician prescribes anticonvulsant medication, or a combination of anticonvulsant medications, according to seizure type and pattern in individual patients. Some anti-convulsant medications are not appropriate for pediatric patients under 16 years of age.
Recommended dosage
Anticonvulsants are available in oral suspension (syrup), injectable, capsule, tablet, and sprinkle forms, depending on the type of medication. Not all anticonvulsants will be available in all forms. Anticonvulsants are prescribed by physicians in varying daily dosages, depending on the age, weight, and other health concerns of the individual patient, as well as the severity and frequency of their seizures.
It is important to follow the prescribing physicians directions carefully as each individual anticonvulsant medication has its own recommended daily dosages and dose schedule. Some anticonvulsants are taken in a single daily dose; others are taken in divided, multiple daily doses. A double dose of any anticonvulsant medication should not be taken. If a dose is missed, it should be taken as soon as possible. However, if it is within four hours of the next scheduled dose, the missed dose should be skipped. Taking an anticonvulsant at regular intervals and at the same time each day enables consistent levels of the medication to be maintained in the bloodstream, and results in more effective seizure control.
In general, initiating any course of treatment which includes anticonvulsants requires a gradual dose-increasing regimen. Adults and children typically take a smaller daily dose for the first two weeks. Daily dosages of anti-convulsant medication may then be slowly titrated, or increased over time until adequate seizure control is achieved using the lowest dose possible.
When ending a course of treatment of anticonvulsant, physicians typically taper the patient's daily dose over a period of several weeks. Suddenly stopping treatment including anticonvulsants may cause seizures to return or occur with greater frequency. Patients taking anticonvulsants drugs for the treatment of pain or bipolar disorders may experience also have seizures, even if they have never had them before, if they suddenly stop taking the medication.
Precautions
Each anticonvulsant medication may have its own precautions, counter-indications, and side-effects. However, many are common to all anticonvulsant medications.
Consult the prescribing physician before taking any anticonvulsant with non-perscription medications. Patients should avoid alcohol and CNS depressants (medications that make one drowsy or tired, such as antihistimines, sleep medications, and some pain medications) while taking anticonvulants. Anticonvulsants can exacerbate the side effects of alcohol and other medications. Alcohol may also increase the risk or frequency of seizures.
Anticonvulsants may not be suitable for persons with a history of stroke, anemia, thyroid, liver, depressed kidney function, diabetes mellitus, severe gastro-intestional disorders, porphyria, lupus, some forms of mental illness, high blood presure, angina (chest pain), irregular heartbeats, and other heart problems.
Before beginning treatment with anticonvulsants, patients should notify their physician if they consume a large amount of alcohol, have a history of drug use, are nursing, pregnant, or plan to become pregnant.
Physicians generally advise the use of effective birth control while taking many anticonvulsant medications. Patients taking anticonvulsants should be aware that many anticonvulsants may increase the risk of birth defects. Furthermore, many anticonvulsant medications are secreted in breast milk. Patients who become pregnant while taking any anticonvulsant should contact their physician immediately to discuss the risks and benefits of continuing treatment during pregnancy and while nursing.
Some anticonvulsants may be prescribed for children. However, children may experience increased side effects. Research indicates that some children who take high doses of some anticonvulsants (such as hydantoins) for an extended period of time may experience mild learning difficulties or not perform as well in school.
Side effects
In some patients, anticonvulsants may produce usually mild side effects. Headache, nausea, and unusual tiredness and weakness are the most frequently reported side effects of anticonvulsants. Other general side effects of anticonvulsants that do not usually require medical attention include:
Many of these side effects disappear or occur less frequently during treatment as the body adjusts to the medication. However, if any symptoms persist or become too uncomfortable, the perscribing physician should be consulted.
Other, uncommon side effects of anticonvulsants can be serious or may indicate an allergic reaction. A patient taking any anticonvulsant who experiencs one or more of the following symptoms should contact the prescribing physician immediately:
Interactions
Anticonvulsants may have negative interactions with some antacids, anticoagulants, antihistimines, antidepressants, antibiotics, pain killers (including lidocaine) and monoamine oxidase inhibitors (MAOIs). Other medications such as amiodarone, diazoxide, phenybutazone, sulfonamides (sulfa drugs), corticosteroids, sucralfate, rifampin, and warfarin may also adversely react with anti-convulsants.
Some anticonvulsants should not be used in combination with other anticonvulsants. (For example, phenytoin (a hydantoin) when used with valproic acid, another anticonvulsant, may increase the seizure frequency). However, several anticonvulsant medications are indicated to be used in conjunction with or suppliment other anti-convulsants. If advised and carefully monitored by a physician, a course of treatment including multiple seizure prevention medications can be effective and safe.
Most anticonvulsants decrease the effectiveness of contraceptives that contain estrogens or progestins, including oral contraceptives (birth control pills), progesterone implants (Norplant), and progesterone injections (Depo-Provera).
Resources
BOOKS
Masters, Roger D., Michael T. McGuire. The Neurotransmitter Revolution. Southern Illinois University Press, 1994.
Mondimore, Francis Mark. Bipolar Disorder: A Guide for Patients and Families. Baltimore: The Johns Hopkins University Press, 1999.
Weaver, Donald F. Epilepsy and Seizures: Everything You Need to Know. Firefly Books, 2001.
Wyllie, Elaine. The Treatment of Epilepsy: Principles and Practice. New York: Lippincott, Williams & Wilkins, 2001.
PERIODICALS
Feely, Morgan. "Drug treatment of epilepsy." BMJ 318 (9 January 1999): 106–109.
"Risk of birth defects with anticonvulsants evaluated." Psychopharmacology Update 12, no. 5 (May 2001): 3.
OTHER
"Seizure Medicines." Epilepsy.com.http://www.epilepsy.com/epilepsy/seizure_medicines.html (May 1, 2004).
ORGANIZATIONS
Epilepsy Foundation. 4351 Garden City Drive, Landover, MD 20785-7223. (800) 332-1000. http://www.epilepsyfoundation.org.
American Epilepsy Society. 342 North Main Street, West Hartford, CT 06117-2507. http://www.aesnet.org.
Adrienne Wilmoth Lerner
Dental Dictionary:
anticonvulsive |
Relieving or preventing convulsion.
Veterinary Dictionary:
anticonvulsant |
1. inhibiting convulsions. Any drug that depresses the central nervous system may be used for its anticonvulsant effect. This includes narcotics and sedatives. They have the undesirable effect of depressing all CNS functions.
2. a specific motor depressant, such as anticonvulsant or antiepileptic, which depresses specifically the motor centers and suppresses spontaneous motor activity; examples are phenobarbital, phenytoin, primidone and diazepam.
Wikipedia:
Anticonvulsant |
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. Because of this, anticonvulsants also have proven effective in treating many kinds of dysfunctional anxiety. Failing this, an effective anticonvulsant would prevent the spread of the seizure within the brain and offer protection against possible excitotoxic effects that may result in brain damage. However, anticonvulsants themselves have been linked to lowered IQ in children.[1] Anticonvulsants are often called antiepileptic drugs (abbreviated "AEDs") or antiseizure drugs (abbreviated "ASDs").
The major molecular targets of marketed anticonvulsant drugs are 1) voltage-gated sodium channels; 2) components of the GABA system, including GABAA receptors, the GAT-1 GABA transporter, and GABA transaminase; and 3) voltage-gated calcium channels.[2]
Some anticonvulsants have shown antiepileptogenic effects in animal models of epilepsy. That is, they either prevent the expected development of epilepsy or can halt or reverse the progression of epilepsy. However, no drug has been shown to prevent epileptogenesis (the development of epilepsy after an injury such as a head injury) in human trials.[3]
The usual method of achieving approval for a drug is to show it is effective when compared against placebo, or that it is more effective than an existing drug. In monotherapy (where only one drug is taken) it is considered unethical by most to conduct a trial with placebo on a new drug of uncertain efficacy. This is because untreated epilepsy leaves the patient at significant risk of death. Therefore, almost all new epilepsy drugs are initially approved only as adjunctive (add-on) therapies. Patients whose epilepsy is currently uncontrolled by their medication (i.e., it is refractory to treatment) are selected to see if supplementing the medication with the new drug leads to an improvement in seizure control. Any reduction in the frequency of seizures is compared against a placebo.[3]
Once there is confidence that a drug is likely to be effective in monotherapy, trials are conducted where the drug is compared to an existing standard. For partial-onset seizures, this is typically carbamazepine. Despite the launch of over ten drugs since 1990, no new drug has been shown to be more effective than the older set, which includes carbamazepine, valproate and phenytoin. The lack of superiority over existing treatment, combined with lacking placebo-controlled trials, means that few modern drugs have earned FDA approval as initial monotherapy. In contrast, Europe only requires equivalence to existing treatments, and has approved many more. Despite their lack of FDA approval, the American Academy of Neurology and the American Epilepsy Society still recommend a number of these new drugs as initial monotherapy.[3]
In the following list, the dates in parentheses are the earliest approved use of the drug.
Main article: Aldehydes
Main article: Barbiturates
Barbiturates are drugs that act as central nervous system (CNS) depressants, and by virtue of this they produce a wide spectrum of effects, from mild sedation to anesthesia. The following are classified as anticonvulsants:
Phenobarbital was the main anticonvulsant from 1912 till the development of phenytoin in 1938. Today, phenobarbital is rarely used to treat epilepsy in new patients since there are other effective drugs that are less sedating. Phenobarbital sodium injection can be used to stop acute convulsions or status epilepticus, but a benzodiazepine such as lorazepam, diazepam or midazolam is usually tried first. Other barbiturates only have an anticonvulsant effect at anaesthetic doses.
Main article: Benzodiazepines
The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsive, amnestic and muscle relaxant properties. Benzodiazepines act as a central nervous system depressant. The relative strength of each of these properties in any given benzodiazepine varies greatly and influences the indications for which it is prescribed. Long-term use can be problematic due to the development of tolerance to the anticonvulsant effects and dependency.[4][5][6][7] Of the many drugs in this class, only a few are used to treat epilepsy:
The following benzodiazepines are used to treat status epilepticus:
Nitrazepam, temazepam, and especially nimetazepam are powerful anticonvulsant agents, however their use is rare due to an increased incidence of side effects and strong sedative and motor-impairing properties.
Main article: Bromides
Main article: Carbamates
Main article: Carboxamides
The following are carboxamides:
Main article: Fatty acids
The following are fatty-acids:
Vigabatrin and progabide are also analogs of GABA.
Main article: Hydantoins
The following are hydantoins:
Main article: Oxazolidinediones
The following are oxazolidinediones:
Main article: Propionates
Main article: Pyrimidinediones
Main article: Pyrrolidines
Main article: Succinimides
The following are succinimides:
Main article: Sulfonamides
Main article: Triazines
Main article: Ureas
Main article: Amides
The ketogenic diet is a strict medically supervised diet that has an anticonvulsant effect. It is typically used in children with refractory epilepsy.
The vagus nerve stimulator (VNS) is a device that sends electric impulses to the left vagus nerve in the neck via a lead implanted under the skin. It was FDA approved in 1997 as an adjunctive therapy for partial-onset epilepsy.
The following table lists anticonvulsant drugs together with the date their marketing was approved in the US, UK and France. Data for the UK and France are incomplete. In recent years, the European Medicines Agency has approved drugs throughout the European Union. Some of the drugs are no longer marketed.
| Drug | Brand | US | UK | France |
|---|---|---|---|---|
| acetazolamide | Diamox | 27 July 1953[8] | 1988[9] | |
| carbamazepine | Tegretol | 15 July 1974[10][11] | 1965[9] | 1963[12] |
| clobazam | Frisium | 1979[9] | ||
| clonazepam | Klonopin/Rivotril | 4 June 1975[13] | 1974[9] | |
| diazepam | Valium | 15 November 1963[14] | ||
| divalproex sodium | Depakote | 10 March 1983[15] | ||
| ethosuximide | Zarontin | 2 November 1960[16] | 1955[9] | 1962[12] |
| ethotoin | Peganone | 22 April 1957[17] | ||
| felbamate | Felbatol | 29 July 1993[18] | ||
| fosphenytoin | Cerebyx | 5 August 1996[19] | ||
| gabapentin | Neurontin | 30 December 1993[20] | May 1993[9][12] | October 1994[12] |
| lamotrigine | Lamictal | 27 December 1994[21] | October 1991[9][12] | May 1995[12] |
| levetiracetam | Keppra | 30 November 1999[22] | 29 September 2000[9][23] | 29 September 2000[23] |
| mephenytoin | Mesantoin | 23 October 1946[24] | ||
| metharbital | Gemonil | 1952[25][26] | ||
| methsuximide | Celontin | 8 February 1957[27] | ||
| methazolamide | Neptazane | 26 January 1959[28] | ||
| oxcarbazepine | Trileptal | 14 January 2000[29] | 2000[9] | |
| phenobarbital | 1912[9] | 1920[12] | ||
| phenytoin | Dilantin/Epanutin | 1938[12][30] | 1938[9] | 1941[12] |
| phensuximide | Milontin | 1953[31][32] | ||
| pregabalin | Lyrica | 30 December 2004[33] | 6 July 2004[9][34] | 6 July 2004[34] |
| primidone | Mysoline | 8 March 1954[35] | 1952[9] | 1953[12] |
| sodium valproate | Epilim | December 1977[12] | June 1967[12] | |
| stiripentol | Diacomit | 5 December 2001[36] | 5 December 2001[36] | |
| tiagabine | Gabitril | 30 September 1997[37] | 1998[9] | November 1997[12] |
| topiramate | Topamax | 24 December 1996[38] | 1995[9] | |
| trimethadione | Tridione | 25 January 1946[39] | ||
| valproic acid | Depakene/Convulex | 28 February 1978[40] | 1993[9] | |
| vigabatrin | Sabril | 21 August 2009[41] | 1989[9] | |
| zonisamide | Zonegran | 27 March 2000[42] | 10 March 2005[9][43] | 10 March 2005[43] |
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This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)
| paramethadione | |
| phenacemide | |
| valproic acid |
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