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Figure 1. Levetiracetam.
(Figure omitted. See article PDF.)
Figure 2. Expected percentage reduction in seizure frequency as a function of the daily dose of levetiracetam in (A) adults and (B) children, expressed as percentiles. The solid line represents the median or 50th percentile. (A) Reprinted from [72] with permission from Elsevier; (B) UCB, data on file.
(Figure omitted. See article PDF.)
Figure 3. Geometric mean levetiracetam plasma concentration profiles after single doses of levetiracetam IR tablets (750 mg and 3 ×500 mg), 10% SOL (750 mg), iv. infusion (1500 mg) and XR tablets (2 ×750 mg and 3 ×500 mg). IR: Immediate release; iv. Intravenous; SOL: Oral solution; XR: Extended release. Adapted from [37,77,81].
(Figure omitted. See article PDF.)
Epilepsy is one of the most common neurological disorders and is estimated to affect at least 50 million people worldwide [1]. It represents a substantial global burden, affecting health, wellbeing and economic status. Treatment with traditional antiepileptic drugs (AEDs) is often associated with side effects and failure to control seizures adequately. Over the past 20 years, treatment options have increased with the introduction of many new AEDs with the potential for improved efficacy and fewer side effects. Despite the availability of these second-generation drugs, a substantial proportion of patients do not achieve acceptable seizure control [2,3] and may experience intolerable adverse events [4,5].
The selection of an appropriate AED for an individual patient depends on many different factors, including seizure type, underlying syndrome, age, concomitant medication, available formulations and patient preference, as well as comorbid diseases. The tolerability profile of an AED may be a determining factor in drug selection [4]. It is also important to consider the pharmacokinetic properties of an AED to predict the ease of use [6-8].
Levetiracetam, an AED with a novel mechanism of action, has been available for almost a decade for the treatment of epilepsy. This article will focus on some of the recent advances in our understanding of the clinical and pharmacokinetic profile of levetiracetam. also highlighted are the availability of data from studies in special patient populations, population pharmacokinetics and exposure-response modeling, and formulation development.
Introduction to levetiracetam
Chemical structure
Levetiracetam is the S -enantiomer of a-ethyl-2-oxo-1-pyrrolidine acetamide (Figure 1). It is a white to off-white powder...