Pharmacokinetics of levetiracetam XR 500mg tablets

Rouits, Elisabeth; Burton, Ingrid; Guénolé, Evelyne; Troenaru, Mona-Mihaela; Stockis, Armel; Sargentini‐Maier, Maria Laura

doi:10.1016/j.eplepsyres.2009.02.001

Cited by 31 publications

(32 citation statements)

References 21 publications

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“…Therefore, this study demonstrates that extended release levetiracetam2 displays an extended pharmacologic profile in the dog compared to IV formulations. Food did not negatively impact or prohibit absorption; it only slowed the disposition of extended release levetiracetam in dogs, a finding consistent with pharmacokinetics in humans 17. Food did increase the time to reach maximum concentrations, but at the estimated accumulation, this difference would not be clinically relevant.…”

Section: Discussionsupporting

confidence: 58%

“…Furthermore, drug concentrations will fluctuate >75% during a dosing interval,1 which may contribute to poor seizure control. An extended release levetiracetam product approved for use in humans has lengthened the dosing interval from 12 to 24 hours in human epileptic patients 17, 18, 19, 20. However, previous studies have indicated that dosing regimens for slow or extended release products approved for use in humans cannot accurately be extrapolated to dogs 21.…”

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confidence: 99%

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Disposition of Extended Release Levetiracetam in Normal Healthy Dogs After Single Oral Dosing

Boothe

2015

Veterinary Internal Medicne

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BackgroundLevetiracetam is an anticonvulsant used for control of canine epilepsy. An extended release preparation should improve dosing convenience.ObjectivesTo determine the disposition of extended release levetiracetam in normal dogs after single dosing.AnimalsPharmacokinetic study: 16 healthy, adult dogs.MethodsUsing a partially randomized crossover study, levetiracetam (30 mg/kg) was administered intravenously (IV) and orally (PO) as extended release preparation with or without food. Blood was collected for 24 hours (IV) or 36 hours (PO). Serum levetiracetam was quantitated by immunoassay and data were subjected to noncompartmental analysis.ResultsPharmacokinetic parameters for fasted versus fed animals, respectively, were (mean ± SEM): C max = 26.6 ± 2.38 and 30.7 ± 2.88 μ/mL, T max = 204.3 ± 18.9 and 393.8 ± 36.6 minutes, t 1/2 = 4.95 ± 0.55 and 4.48 ± 0.48 hours, MRT = 9.8 ± 0.72 and 10 ± 0.64 hours, MAT = 4.7 ± 0.38 and 5.6 ± 0.67 hours, and F = 1.04 ± 0.04 and 1.26 ± 0.07%. Significant differences were limited to T max (longer) and F (greater) in fed compared to fasted animals. Serum levetiracetam concentration remained above 5 μ/mL for approximately 20 hours in both fasted and fed animals.Conclusions and Clinical ImportanceExtended release levetiracetam (30 mg/kg q12h), with or without food, should maintain concentrations above the recommended minimum human therapeutic concentration.

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Section: Discussionsupporting

confidence: 58%

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confidence: 99%

Disposition of Extended Release Levetiracetam in Normal Healthy Dogs After Single Oral Dosing

Boothe

2015

Veterinary Internal Medicne

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“…[20][21][22] New antiepileptic drugs are usually first launched and marked as conventional dosage forms or IR formulation. IR formulation of antiepileptic drugs with short half-lives, in fact, necessitate frequent administration to maintain drug concentrations over the dosing interval and produce wide fluctuations in drug concentrations throughout the day.…”

Section: Resultsmentioning

confidence: 99%

Preparation of Lacosamide Sustained-release Tablets and Their Pharmacokinetics in Beagles and Mini-pigs

Ahn¹,

Kim²,

Nam³

et al. 2014

Bulletin of the Korean Chemical Society

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The aim of the present study was to improve dosing of lacosamide, a functionalized amino acid used as an antiepileptic agent, from twice daily to once daily for the convenience of patients. A sustained-release lacosamide tablet was developed and dissolution testing was employed to determine in vitro release behavior using water or buffer solutions at pH 1.2, 4.0, or 6.8. Lacosamide was released for 12 h from the sustainedrelease (SR) tablet, as compared to complete release within 1 h from an immediate-release Vimpat ® tablet. Each formulation (100 mg) was orally administered to six beagle dogs and six mini-pigs under fasted conditions, and pharmacokinetic parameters such as the area under the concentration time curve (AUC t ), the maximum plasma concentration (C max ), and the time at which this occurred (T max ) were calculated. These results showed similar values for AUC t , C max , and T max following oral administration of immediate-release (Vimpat ® ) and SR lacosamide tablets.

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“…Эпитерра лонг отличается от исходной формы ЛЕВ более поздним Tmax, соответственно, эта форма должна обладать потенци-ально меньшей частотой и выраженностью НЯ (рис. 3, 4) [25]. Это свойство ЛЕВ ДВ будет способствовать более ши-рокому его применению, особенно у детей, страдающих эпилепсией, женщин детородного возраста и пожилых па-циентов.…”

Section: р е з у л ь т а т ы и с с л е д о в а н и й п р и м е н е н unclassified

Clinical results of and prospects for the use of controlled-release antiepileptic drugs: a new once-daily levetiracetam formulation

Власов

2017

RJTAO

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Внедрение в клиническую практику современных противоэпилептических препаратов (ПЭП) существенно расширяет возможности и повышает эффективность лекар-ственной терапии эпилепсии благодаря их особой, порой уникальной фармакокинетике и фармакодинамике. Боль-шинство ПЭП последнего поколения синтезированы целе-направленно, часто обладают заранее прогнозируемыми свойствами. Вместе с тем дополнительные возможности фармакотерпии эпилепсии появляются при применении новых форм препаратов, уже длительно существующих на фармацевтическом рынке. Рядом положительных свойств обладают формы ПЭП с контролируемым высвобождением активного вещества, которые получили широкое распро-странение в последние 20-25 лет, и врачи, и пациенты счи-тают их более предпочтительными для длительной терапии [1, 2-6]. Наличие разнообразных лекарственных форм Власов П.Н. Nevrologiya, neiropsikhiatriya, psikhosomatika = Neurology, neuropsychiatry, psychosomatics. 2017;9(3):98-104.

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Pharmacokinetics of levetiracetam XR 500mg tablets

Cited by 31 publications

References 21 publications

Disposition of Extended Release Levetiracetam in Normal Healthy Dogs After Single Oral Dosing

Disposition of Extended Release Levetiracetam in Normal Healthy Dogs After Single Oral Dosing

Preparation of Lacosamide Sustained-release Tablets and Their Pharmacokinetics in Beagles and Mini-pigs

Clinical results of and prospects for the use of controlled-release antiepileptic drugs: a new once-daily levetiracetam formulation

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