Pharmacokinetics of Single Oral Dose Extended‐Release Levetiracetam in Healthy Cats
نویسندگان
چکیده
BACKGROUND Repeated PO dosing of anti-epileptic drugs may contribute to poor compliance in treated cats. Intermediate-release levetiracetam has been used safely in cats, but must be given q8h to maintain serum concentrations in the therapeutic interval for humans (5-45 μg/mL). Approved extended-release levetiracetam (XRL) for human use may require less frequent dosing, but the large dosing unit has limited its use in cats. HYPOTHESES In healthy cats, serum levetiracetam concentration will remain above 5 μg/mL for at least 24 hours after administration of a single dose of XRL PO and will be well tolerated. ANIMALS 7 healthy cats. METHODS Extended-release levetiracetam (500 mg) was administered PO. Blood was collected and neurologic examination findings recorded at scheduled times over 30 hours. Serum levetiracetam concentration was quantitated by an immunoassay validated in cats. Data were subjected to noncompartmental analysis. Descriptive statistics were reported. RESULTS The median dosage of 86.2 mg/kg, (range, 80-94.3) achieved a mean maximum concentration (Cmax ) of 89.8 ± 25.8 μg/mL at 4.9 ±1.57 hours. Serum levetiracetam was >5 μg/mL in all cats by 90 minutes. Mean concentrations were 43.7 ± 18.4 and 4.9 ± 3.4 μg/mL at 12 and 24 hours, respectively. The half-life was 4.1 ± 1.0 hours. The drug was well tolerated. CONCLUSIONS AND CLINICAL IMPORTANCE A single 500 mg PO dose of XRL safely maintained serum levetiracetam concentration ≥5 μg/mL in healthy cats for at least 21 hours. Clinical efficacy studies in epileptic cats receiving XRL are indicated; however, monitoring should be implemented for individual cats.
منابع مشابه
Pharmacokinetics and Bioavailability Comparison of two oral Tablet Formulations of Escitalopram 20 mg: A Single-Dose, Open-Label, Two-Period Crossover Study in Healthy Indian Adult Subjects
This study was done to assess bioequivalence between test and reference formulations of escitalopram oxalate 20 mg in healthy Indian male subjects. This single-dose, randomized, open-label, 2-period crossover study was carried out in 12 Healthy Indian Male volunteers aged 18 to 55 years under fasting conditions with a wash out of 14 days. The subjects were randomly assigned to receive the test...
متن کاملDisposition of Extended Release Levetiracetam in Normal Healthy Dogs After Single Oral Dosing
BACKGROUND Levetiracetam is an anticonvulsant used for control of canine epilepsy. An extended release preparation should improve dosing convenience. OBJECTIVES To determine the disposition of extended release levetiracetam in normal dogs after single dosing. ANIMALS Pharmacokinetic study: 16 healthy, adult dogs. METHODS Using a partially randomized crossover study, levetiracetam (30 mg/k...
متن کاملPreparation and release study of Levetiracetam 500 mg extended release tablet by using combination of hydrophilic and hydrophobic polymers.
Abstract Levetiracetam as an Anti-epileptic drug with exclusive mechanism of action is accepted by the USA Food and Drug Administration as an adjunctive therapy in treating epilepsy in young adults. The purpose of this project is the design and formulation of prolonged release of levetiracetam using two types of retarding agent such as Hydroxyl Propyl Methylcellulose (HPMC K4...
متن کاملDisposition of levetiracetam in healthy adult horses.
Nine horses received 20 mg/kg of intravenous (LEVIV ); 30 mg/kg of intragastric, crushed immediate release (LEVCIR ); and 30 mg/kg of intragastric, crushed extended release (LEVCER ) levetiracetam, in a three-way randomized crossover design. Crushed tablets were dissolved in water and administered by nasogastric tube. Serum samples were collected over 48 hr, and levetiracetam concentrations wer...
متن کاملPharmacokinetics of Dalfampridine Extended Release 7.5-mg Tablets in Healthy Subjects and Individuals With Mild and Moderate Renal Impairment: An Open-Label Study
Dalfampridine extended release tablets (D-ER; prolonged-release fampridine in Europe) are available to improve walking in patients with multiple sclerosis (MS). D-ER is mainly renally eliminated; the approved 10-mg twice daily dose is contraindicated in the United States in patients with moderate or severe renal impairment. This study evaluated single-dose and steady-state pharmacokinetics of a...
متن کامل