Antiepileptic drugs (also anticonvulsants , from lat. Convulsio - convulsion) are pharmaceutical anticonvulsant drugs used to treat epilepsy , relieve muscle cramps of various origins (with epilepsy, eclampsia , intoxication, tetanus ).
Antiepileptic drugs are also used to treat bipolar disorders (manic-depressive psychosis), as some of the drugs in this group are normotimics and have the ability to stabilize mood .
Many tranquilizers - benzodiazepine derivatives ( diazepam , nitrazepam , clonazepam ) have an anticonvulsant effect. Moreover, clonazepam in many pharmaceutical classifications is designated primarily as an anticonvulsant.
Content
History
Classification
A common principle for antiepileptic drugs is to reduce the frequency of response of neurons. Modern drugs of this group exhibit selective inhibition of the activity of pathologically active neurons. This action is usually achieved mainly in three ways:
- increased activity of inhibitory neurons, for example, stimulating the activity of GABA receptors
- inhibition of neuronal excitatory receptors, for example, reducing the activity of NMDA receptors .
- a direct effect on the conduction of an electrical impulse, for example, by regulating the ion channels of neurons .
Pharmacological Mechanism
- Phenytoin , lamotrigine and phenobarbital inhibit the release of glutamate from the ends of exciting neurons, thereby preventing the activation of neurons in the epileptic focus.
- Valproic acid and some other antiepileptic drugs, according to modern concepts, are antagonists of NMDA receptors in neurons and interfere with the interaction of glutamate with NMDA receptors.
- Benzodiazepines and phenobarbital interact with the GABA-A receptor complex. The resulting allosteric changes in the GABA-A receptor contribute to an increase in its sensitivity to GABA and even greater entry of chlorine ions into the neuron, which as a result counteracts the development of depolarization .
- Thiagabin is a GABA reuptake blocker from the synaptic cleft. The stabilization of this inhibitory mediator in the synaptic cleft is accompanied by the potentiation of its interaction with GABA-A, receptors of neurons of the epileptic focus and an increase in the inhibitory effect on their excitability.
- Vigabatrin (an inhibitor of GABA-transaminase ) - blocks the catabolism of GABA and increases its content in the ends of inhibitory nerve cells.
- Gabapentin has the ability to enhance the formation of GABA. The mechanism of its antiepileptic action is also due to the ability to directly open channels for potassium ions.
- Carbamazepine , valproate and phenytoin alter the inactivation of voltage-gated sodium and calcium channels, thereby limiting the distribution of electrical potential.
- Ethosuximide blocks T-type calcium channels .
Common side effects
Due to the fact that almost all antiepileptic drugs have an inhibitory effect on the central nervous system , the following side effects often develop: drowsiness, asthenia , dizziness , ataxia , memory loss, and weakening of cognitive functions .
See also
- Methindione
Links
- Ermakov A.Yu., Boldyreva S.R., Litvinovich E.F. Modern antiepileptic drugs in the treatment of symptomatic partial epilepsy in children // Medical Council. - No. 1 . Archived on October 28, 2014.
- Boldyreva S.R., Ermakov A.Yu. Side effects of antiepileptic drugs // Medical Council. - 2008. - No. 9-10 . (inaccessible link)