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Anticonvulsant Historical Information
Drugs
In the following list, the dates in parentheses are the earliest approved use of the drug.
Aldehydes
Main article: Aldehydes
* Paraldehyde (1882). One of the earliest anticonvulsants. Still used to treat status epilepticus, particularly where there are no resuscitation facilities.
Aromatic allylic alcohols
* Stiripentol (2001 - limited availability). Indicated for the treatment of severe myoclonic epilepsy in infancy (SMEI).
Barbiturates
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 (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.
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.
Bromides
Main article: Bromides
* Potassium bromide (1857). The earliest effective treatment for epilepsy. There would not be a better drug for epilepsy until phenobarbital in 1912. It is still used as an anticonvulsant for dogs and cats.
Carbamates
Main article: Carbamates
* Felbamate (1993). This effective anticonvulsant has had its usage severely restricted due to rare but life-threatening side effects.
Carboxamides
Main article: Carboxamides
The following are carboxamides:
* Carbamazepine (1963). A popular anticonvulsant that is available in generic formulations.
* Oxcarbazepine (1990). A derivative of carbamazepine that has similar efficacy but is better tolerated.
Fatty acids
Main article: Fatty acids
The following are fatty-acids:
* The valproates — valproic acid, sodium valproate, and divalproex sodium (1967).
* Vigabatrin (1989).
* Progabide
* Tiagabine (1996).
Vigabatrin and progabide are also analogs of GABA.
Fructose derivatives
Main article: Fructose
* Topiramate (1995).
Gaba analogs
* Gabapentin (1993).
* Pregabalin (2004).
Hydantoins
Main article: Hydantoins
The following are hydantoins:
* Ethotoin (1957).
* Phenytoin (1938 ).
* Mephenytoin
* Fosphenytoin (1996).
Oxazolidinediones
Main article: Oxazolidinediones
The following are oxazolidinediones:
* Paramethadione
* Trimethadione (1946).
* Ethadione
Propionates
Main article: Propionates
* Beclamide
Pyrimidinediones
Main article: Pyrimidinediones
* Primidone (1952).
Pyrrolidines
Main article: Pyrrolidines
* Brivaracetam
* Levetiracetam (1999).
* Seletracetam
Succinimides
Main article: Succinimides
The following are succinimides:
* Ethosuximide (1955).
* Phensuximide
* Mesuximide
Sulfonamides
Main article: Sulfonamides
* Acetazolamide (1953).
* Sulthiame
* Methazolamide
* Zonisamide (2000).
Triazines
Main article: Triazines
* Lamotrigine (1990).
Ureas
Main article: Ureas
* Pheneturide
* Phenacemide
Valproylamides (amide derivatives of valproate)
Main article: Amides
* Valpromide
* Valnoctamide
Diet
The ketogenic diet is a strict medically supervised diet that has an anticonvulsant effect. It is typically used in children with refractory epilepsy.
Devices
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.
Marketing approval history
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 is incomplete. In recent years, the European Medicines Agency has approved drugs throughout the European Union.
Some of the drugs are no longer marketed.
Generic.....................Brand
acetazolamide............Diamox
carbamazepine...........Tegretol
clobazam...................Frisium
clonazepam................Klonopin/Rivotril
diazepam...................Valium
divalproex sodium........Depakote
ethosuximide..............Zarontin
ethotoin....................Peganone
felbamate..................Felbatol
fosphenytoin..............Cerebyx
gabapentin.................Neurontin
lamotrigine..................Lamictal
levetiracetam..............Keppra
mephenytoin...............Mesantoin
metharbital.................Gemonil
methsuximide..............Celontin
methazolamide............Neptazane
oxcarbazepine.............Trileptal
phenobarbital
phenytoin...................Dilantin/Epanutin
phensuximide..............Milontin
pregabalin..................Lyrica
primidone...................Mysoline
sodium valproate.........Epilim
stiripentol..................Diacomit
tiagabine...................Gabitril
topiramate.................Topamax
trimethadione.............Tridione
valproic acid...............Depakene/Convulex
vigabatrin...................Sabril
zonisamide.................Zonegran
Drugs
In the following list, the dates in parentheses are the earliest approved use of the drug.
Aldehydes
Main article: Aldehydes
* Paraldehyde (1882). One of the earliest anticonvulsants. Still used to treat status epilepticus, particularly where there are no resuscitation facilities.
Aromatic allylic alcohols
* Stiripentol (2001 - limited availability). Indicated for the treatment of severe myoclonic epilepsy in infancy (SMEI).
Barbiturates
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 (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.
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.
Bromides
Main article: Bromides
* Potassium bromide (1857). The earliest effective treatment for epilepsy. There would not be a better drug for epilepsy until phenobarbital in 1912. It is still used as an anticonvulsant for dogs and cats.
Carbamates
Main article: Carbamates
* Felbamate (1993). This effective anticonvulsant has had its usage severely restricted due to rare but life-threatening side effects.
Carboxamides
Main article: Carboxamides
The following are carboxamides:
* Carbamazepine (1963). A popular anticonvulsant that is available in generic formulations.
* Oxcarbazepine (1990). A derivative of carbamazepine that has similar efficacy but is better tolerated.
Fatty acids
Main article: Fatty acids
The following are fatty-acids:
* The valproates — valproic acid, sodium valproate, and divalproex sodium (1967).
* Vigabatrin (1989).
* Progabide
* Tiagabine (1996).
Vigabatrin and progabide are also analogs of GABA.
Fructose derivatives
Main article: Fructose
* Topiramate (1995).
Gaba analogs
* Gabapentin (1993).
* Pregabalin (2004).
Hydantoins
Main article: Hydantoins
The following are hydantoins:
* Ethotoin (1957).
* Phenytoin (1938 ).
* Mephenytoin
* Fosphenytoin (1996).
Oxazolidinediones
Main article: Oxazolidinediones
The following are oxazolidinediones:
* Paramethadione
* Trimethadione (1946).
* Ethadione
Propionates
Main article: Propionates
* Beclamide
Pyrimidinediones
Main article: Pyrimidinediones
* Primidone (1952).
Pyrrolidines
Main article: Pyrrolidines
* Brivaracetam
* Levetiracetam (1999).
* Seletracetam
Succinimides
Main article: Succinimides
The following are succinimides:
* Ethosuximide (1955).
* Phensuximide
* Mesuximide
Sulfonamides
Main article: Sulfonamides
* Acetazolamide (1953).
* Sulthiame
* Methazolamide
* Zonisamide (2000).
Triazines
Main article: Triazines
* Lamotrigine (1990).
Ureas
Main article: Ureas
* Pheneturide
* Phenacemide
Valproylamides (amide derivatives of valproate)
Main article: Amides
* Valpromide
* Valnoctamide
Diet
The ketogenic diet is a strict medically supervised diet that has an anticonvulsant effect. It is typically used in children with refractory epilepsy.
Devices
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.
Marketing approval history
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 is incomplete. In recent years, the European Medicines Agency has approved drugs throughout the European Union.
Some of the drugs are no longer marketed.
Generic.....................Brand
acetazolamide............Diamox
carbamazepine...........Tegretol
clobazam...................Frisium
clonazepam................Klonopin/Rivotril
diazepam...................Valium
divalproex sodium........Depakote
ethosuximide..............Zarontin
ethotoin....................Peganone
felbamate..................Felbatol
fosphenytoin..............Cerebyx
gabapentin.................Neurontin
lamotrigine..................Lamictal
levetiracetam..............Keppra
mephenytoin...............Mesantoin
metharbital.................Gemonil
methsuximide..............Celontin
methazolamide............Neptazane
oxcarbazepine.............Trileptal
phenobarbital
phenytoin...................Dilantin/Epanutin
phensuximide..............Milontin
pregabalin..................Lyrica
primidone...................Mysoline
sodium valproate.........Epilim
stiripentol..................Diacomit
tiagabine...................Gabitril
topiramate.................Topamax
trimethadione.............Tridione
valproic acid...............Depakene/Convulex
vigabatrin...................Sabril
zonisamide.................Zonegran
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