Drug/Small Molecule:
levetiracetam

2D structure

Overview

Generic Names: Levetiracetam [INN]; Levetiracetamum [INN-Latin]; Levitiracetam; levetiracetam
Trade Names: Keppra
PharmGKB Accession Id: PA450206

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. (source: Drug Bank)

Indication

Used as adjunctive therapy in the treatment of partial onset seizures in adults and children 4 years of age and older with epilepsy. (source: Drug Bank)

ATC Therapeutic Category

  • N03AX:Other antiepileptics

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

The precise mechanism(s) by which levetiracetam exerts its antiepileptic effect is unknown. The antiepileptic activity of levetiracetam was assessed in a number of animal models of epileptic seizures. Levetiracetam did not inhibit single seizures induced by maximal stimulation with electrical current or different chemoconvulsants and showed only minimal activity in submaximal stimulation and in threshold tests. Protection was observed, however, against secondarily generalized activity from focal seizures induced by pilocarpine and kainic acid, two chemoconvulsants that induce seizures that mimic some features of human complex partial seizures with secondary generalization. Levetiracetam also displayed inhibitory properties in the kindling model in rats, another model of human complex partial seizures, both during kindling development and in the fully kindled state. The predictive value of these animal models for specific types of human epilepsy is uncertain. (source: Drug Bank)

Food Interactions

Take without regard to meals. Food does not affect bioavailabilty. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

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

Protein Binding

Very low (<10%) (source: Drug Bank)

Absorption

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

Toxicity

Side effects include aggression, agitation, coma, drowsiness, reduced consciousness, slowed breathing (source: Drug Bank)

Isomeric SMILES Code:

CC[C@@H](C(=O)N)N1CCCC1=O (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs2032582 at chr7:86998554 in ABCB1
    This variant maybe associated with drug resistance in chinese epilepsy patients. Sample size: 464 chinese epilepsy patients (270 drug responsive, 194 drug resistant).
    Variant Name:
    ABCB1: 2677T/A>G
    Related Drugs:
    carbamazepine, clobazam, clonazepam, gabapentin, lamotrigine, levetiracetam, phenobarbital, phenytoin, topiramate, valproic acid, vigabatrin
    Related Diseases:
    Epilepsy
    Evidence:
    PMID:19450124
  2. rs3789243 at chr7:87058822 in ABCB1
    This variant maybe associated with drug resistance in chinese epilepsy patients. Sample size: 464 chinese epilepsy patients (270 drug responsive, 194 drug resistant).
    Related Drugs:
    carbamazepine, clobazam, clonazepam, gabapentin, lamotrigine, levetiracetam, phenobarbital, phenytoin, topiramate, valproic acid, vigabatrin
    Related Diseases:
    Epilepsy
    Evidence:
    PMID:19450124
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  •   
  • PK
  • FA
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
SV2A
  •   
  • PD
  •   
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
CACNA1G Uncurated Annotation (source: Drug Bank)
CA1 Uncurated Annotation (source: Drug Bank)
SCN1A Uncurated Annotation (source: Drug Bank)
SV2A Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
carbamazepine Uncurated Annotation This association may increases the risks of carbamazepine toxicity (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Epilepsy
  •   
  • PD
  • PK
  • FA
  • GN
Publications, Variants

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01202
KEGG Compound ID:
C07841
KEGG Drug ID:
D00709
PubChem Compound ID:
441341
PubChem Substance ID:
10043

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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