Anticonvulsants

Carbamazepine

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 possible excitotoxic effects that may 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 parentheses are the earliest approved use of the drug.

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

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:

Benzodiazepines

The benzodiazepines are a class of drugs with hypnotic, anxiolytic, anticonvulsive, amnestic and muscle relaxant properties.

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

• Felbamate (1993). This effective anticonvulsant has had its usage severely restricted due to rare but life-threatening side effects.

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.

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.

Fructose derivatives

• Topiramate (1995).

Gaba analogs

• Gabapentin (1993).
  Pregabalin (2004).

Hydantoins

The following are hydantoins:

• Ethotoin (1957).
  Phenytoin (1938).
  Mephenytoin
  Fosphenytoin (1996).

Oxazolidinediones

The following are oxazolidinediones:

• Paramethadione
  Trimethadione (1946).
  Ethadione

Propionates

• Beclamide

Pyrimidinediones

• Primidone (1952).

Pyrrolidines

• Brivaracetam
  Levetiracetam (1999).
  Seletracetam

Succinimides

The following are succinimides:

• Ethosuximide (1955).
  Phensuximide
  Mesuximide

Sulfonamides

• Acetazolamide (1953).
  Sulthiame
  Methazolamide
  Zonisamide (1990).

Triazines

• Lamotrigine (1991).

Ureas

• Pheneturide
  Phenacemide

Valproylamides (amide derivatives of valproate)

• Valpromide
  Valnoctamide

References

• Drug Reference for FDA Approved Epilepsy Drugs
• UK Anti-Epileptic Drugs List

Links

• eMedicine: Antiepileptic Drugs: an overview
• NINDS: Anticonvulsant Screening Program
• Use of Anticonvulsants in Pharmacotherapy of Bronchial Asthma
• MDNG: Anticonvulsants and Bone Health

This guide is licensed under the GNU Free Documentation License. It uses material from the Wikipedia.