 | Anticonvulsant: Encyclopedia - Anticonvulsant
Anticonvulsant
The anticonvulsants, sometimes also called antiepileptics, belong to a diverse group of pharmaceuticals used in prevention of the occurrence of epileptic seizures. 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 excitotoxic effects that can result in brain damage. An excellent anticonvulsant would have few serious side-effects. However, no such drug exists.
Many anticonvulsants block Sodium (Na+) channels, Calcium (Ca2+) channels, AMPA receptors or NMDA receptors. Some anticonvulsants inhibit the metabolism of GABA or increase its release.
In the following list, the dates in parenthesis are the earliest approved use of the drug.
Anticonvulsant - Aldehydes
Main article: Aldehydes
- Paraldehyde (1882). One of the earliest anticonvulsants. Still used to treat status epilepticus, particularly where there are no resuscitation facilities.
Anticonvulsant - Aromatic Allylic Alcohols
- Stiripentol (2001 - limited availability). Indicated for the treatment of severe myoclonic epilepsy in infancy (SMEI).
Anticonvulsant - Barbiturates
Main article: Barbiturates
Barbiturates are drugs that acts 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 (1912). See also the related drug primidone.
- Methylphenobarbital (1935). Known as mephobarbital in the US. No longer marketed in the UK
- Metharbital (1952). No longer marketed in the UK or US.
- Barbexaclone (1982). Only available in some European countries.
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.
Anticonvulsant - Benzodiazepines
Main article: Benzodiazepines
The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsive, amnestic and muscle relaxant properties. 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 and dependency. Of the many drugs in this class, only a few are used to treat epilepsy:
- Clobazam (1979). Notably used on a short-term basis around menstruation in women with catamenial epilepsy.
- Clonazepam (1974).
- Clorazepate (1972).
The following benzodiazepines are used to treat status epilepticus:
- Diazepam (1963). Can be given rectally by trained care-givers.
- Midazolam (N/A). Increasingly being used as an alternative to diazepam. This water-soluble drug is squirted into the side of the mouth but not swallowed. It is rapidly absorbed by the buccal mucosa.
- Lorazepam (1972). Given by injection in hospital.
Anticonvulsant - Bromides
Main article: Bromides
- Potassium bromide (1857). The earliest effective treatment for epilepsy. There would not be a better drug for epilepsy till phenobarbital in 1912. It is still used as an anticonvulsant for dogs and cats.
Anticonvulsant - Carbamates
Main article: Carbamates
- Felbamate (1993). This effective anticonvulsant has had its usage severely restricted due to rare but life-threatening side effects.
Anticonvulsant - Carboxamides
Main article: Carboxamides
The following are carboxamides:
- Carbamazepine (1965). A popular anticonvulsant that is available in generic formulations.
- Oxcarbazepine (1990). A derivative of carbamazepine that has similar efficacy but is better tolerated.
Anticonvulsant - Fatty Acids
Main article: Fatty acids
The following are fatty-acids:
- The valproates — valproic acid, sodium valproate, and divalproex sodium (1978).
- Vigabatrin (1989).
- Progabide
- Tiagabine (1997).
Vigabatrin and progabide are also analogs of GABA.
Anticonvulsant - Fructose Derivatives
Main article: Fructose
Anticonvulsant - GABA Analogs
- Gabapentin (1993).
- Pregabalin (2004).
Anticonvulsant - Hydantoins
Main article: Hydantoins
As hydantoins have a slow onset of action, they are not recommended for acute control of epilepsy.
The following are hydantoins:
- Ethotoin (1957).
- Phenytoin (1938).
- Mephenytoin
- Fosphenytoin (1996).
Anticonvulsant - Oxazolidinediones
Main article: Oxazolidinediones
The following are oxazolidinediones:
- Paramethadione
- Trimethadione (1946).
- Ethadione
Anticonvulsant - Propionates
Main article: Propionates
Anticonvulsant - Pyrimidinediones
Main article: Pyrimidinediones
Anticonvulsant - Pyrrolidines
Main article: Pyrrolidines
- Brivaracetam
- Levetiracetam (1999).
- Seletracetam
Anticonvulsant - Succinimides
Main article: Succinimides
The following are succinimides:
- Ethosuximide (1955).
- Phensuximide
- Mesuximide
Anticonvulsant - Sulfonamides
Main article: Sulfonamides
- Acetazolamide (1953).
- Sultiame
- Methazolamide
- Zonisamide (2000).
Anticonvulsant - Triazines
Main article: Triazines
Anticonvulsant - Ureas
Main article: Ureas
Anticonvulsant - Valproylamides Amide Derivatives of Valproate
Main article: Amides
Other related archivesAMPA receptors, Acetazolamide, Aldehydes, Amides, Barbexaclone, Barbiturates, Beclamide, Benzodiazepines, Bromides, Calcium (Ca2+) channels, Carbamates, Carbamazepine, Carboxamides, Clobazam, Clonazepam, Clorazepate, Diazepam, Ethosuximide, Ethotoin, Fatty acids, Felbamate, Fosphenytoin, Fructose, GABA, Gabapentin, Hydantoins, Lamotrigine, Levetiracetam, Lorazepam, Metharbital, Methylphenobarbital, Midazolam, NMDA receptors, Oxazolidinediones, Oxcarbazepine, Paraldehyde, Phenobarbital, Phenytoin, Potassium bromide, Pregabalin, Primidone, Progabide, Propionates, Pyrimidinediones, Pyrrolidines, Sodium (Na+) channels, Stiripentol, Succinimides, Sulfonamides, Tiagabine, Topiramate, Triazines, Ureas, Valnoctamide, Valpromide, Vigabatrin, Zonisamide, amnestic, anesthesia, anxiolytic, brain damage, buccal mucosa, classified, dependency, depressants, divalproex sodium, drugs, epilepsy, epileptic, excitotoxic, hydantoins, hypnotic, muscle relaxant, myoclonic, neurons, pharmaceuticals, primidone, sedation, seizures, side-effects, sodium valproate, status epilepticus, tolerance, valproates, valproic acid
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