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Home » GATE Study Material » Pharmaceutical Science » Medicinal Chemistry » Anticonvulsant


Anticonvulsant


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Anticonvulsant

Drugs

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 rugs that act as central nervous system (CNS) epressants, and by virtue of this they produce a wide spectrum of effects, from mild edation to nesthesia. The following are classified as anticonvulsants:

  • Phenobarbital (1912). See also the related drug rimidone.
  • 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

The benzodiazepines are a class of rugs with ypnotic, nxiolytic, 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 and ependency. 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.

Nitrazepam, emazepam, 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.

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 (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

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

 
  • 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

Main article: Pyrimidinediones

  • Primidone (1952).

Pyrrolidines

  • Brivaracetam
  • Levetiracetam (1999).
  • Seletracetam

Succinimides

The following are succinimides:

  • Ethosuximide (1955).
  • Phensuximide
  • Mesuximide

Sulfonamides

  • Acetazolamide (1953).
  • Sulthiame
  • Methazolamide
  • Zonisamide (2000).

Triazines

  • Lamotrigine (1990).

Ureas

  • Pheneturide
  • Phenacemide

Valproylamides (amide derivatives of valproate)

  • Valpromide
  • Valnoctamide
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