Drug Groups

approved; investigational

Description

Levetiracetam is an anticonvulsant medication used to treat epilepsy. Levetiracetam may selectively prevent hypersynchronization of epileptiform burst firing and propagation of seizure activity. Levetiracetam binds to the synaptic vesicle protein SV2A, which is thought to be involved in the regulation of vesicle exocytosis. Although the molecular significance of levetiracetam binding to synaptic vesicle protein SV2A is not understood, levetiracetam and related analogs showed a rank order of affinity for SV2A which correlated with the potency of their antiseizure activity in audiogenic seizure-prone mice.

Indication

Used as adjunctive therapy in the treatment of partial onset seizures in adults and children 4 years of age and older with epilepsy.

Toxicity

Side effects include aggression, agitation, coma, drowsiness, reduced consciousness, slowed breathing

Affected Organisms

Biotransformation

The major metabolic pathway of levetiracetam (24% of dose) is an enzymatic hydrolysis of the acetamide group. No CYP450 metabolism detected.

Absorption

Rapidly and almost completely absorbed after oral administration (99%). Peak plasma concentrations occurring in about an hour following oral administration in fasted subjects.

Half Life

6-8 hours

Protein Binding

Very low (<10%)

Elimination

Sixty-six percent (66%) of the dose is renally excreted unchanged. The metabolites have no known pharmacological activity and are renally excreted. The mechanism of excretion is glomerular filtration with subsequent partial tubular reabsorption.

Clearance

* 0.96 mL/min/kg

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