Levetiracetam

Products

Levetiracetam is commercially available as film-coated tablets, an oral solution, and an infusion concentrate (Keppra, generics). It has been approved in many countries since 2000 (United States: 1999). Starting in 2011, generics and new dosage forms entered the market (minipacks). Brivaracetam (Briviact) was developed by UCB as its successor.

Structure and properties

Levetiracetam (C8H14N2O2, Mr = 170.2 g/mol) is a pyrrolidinone derivative (oxo-pyrrolidine) and exists as a pure -enantiomer of etiracetam (lev-etiracetam). It is a white crystalline powder with a faint odor and a bitter taste that is very soluble in water. Levetiracetam is structurally related to the nootropic piracetam (Nootropil, also UCB).

Effects

Levetiracetam (ATC N03AX14) has antiepileptic and anticonvulsant properties. The effects are attributed to binding to synaptic vesicle protein 2A (SV2A). SV2A is a membrane protein found in synaptic vesicles and plays an important role in the release of neurotransmitters from the vesicles into the synaptic space. Binding of levetiracetam to SV2A reduces the release of neurotransmitters. Furthermore, it also has an effect on calcium levels in neurons. Levetiracetam is very well absorbed and has a half-life of approximately 7 hours.

Indications

For the treatment of patients with epilepsy:

  • For the treatment of partial seizures with or without secondary generalization in patients with epilepsy.
  • For adjunctive treatment of myoclonic seizures in patients with juvenile myoclonic epilepsy.
  • For adjunctive treatment of primary generalized tonic-clonic seizures in patients with idiopathic generalized epilepsy.

Dosage

According to the drug label. The tablets are usually taken twice daily (morning and evening), regardless of meals. Discontinuation should be gradual.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Unlike previous antiepileptic drugs, levetiracetam has a low potential for drug-drug interactions. It does not interact with CYP or UGT isozymes. Levetiracetam is biotransformed by enzymatic hydrolysis of the acetamide group. Elimination occurs primarily through the urine.

Adverse effects

The most common possible adverse effects include fatigue, drowsiness, and weakness. Therefore, caution is advised when driving.