Pharmacokinetic Evaluation of Sustained Release Formulations of Antiepileptic Drugs

Bialer, Meir

doi:10.2165/00003088-199222010-00002

Cited by 30 publications

(17 citation statements)

References 31 publications

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“…This might be improved simply with new drug formulations that enable once‐daily dosing regimens, as has been shown for antiretroviral medications in human immunodeficiency virus (HIV) . In addition to improved adherence, controlled‐release formulations of antiepileptic drugs (AEDs) may prevent or minimize potential intermittent declines in serum concentrations that may be associated with seizure breakthroughs …”

mentioning

confidence: 99%

“…8 In addition to improved adherence, controlledrelease formulations of antiepileptic drugs (AEDs) may prevent or minimize potential intermittent declines in serum concentrations that may be associated with seizure breakthroughs. 9 Pregabalin (PGB) is currently approved as an immediaterelease (IR) capsule in >100 countries, with country-specific indications for adjunctive therapy of partial-onset seizures with or without secondary generalization in adults. The approved dose range in epilepsy is 150-600 mg/day, administered twice daily (BID) or three-times daily (TID).…”

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confidence: 99%

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Adjunctive use of controlled‐release pregabalin in adults with treatment‐resistant partial seizures: A double‐blind, randomized, placebo‐controlled trial

French¹,

Brandt

Friedman³

et al. 2014

Epilepsia

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SUMMARYObjectives: To assess the efficacy and tolerability of add-on pregabalin controlledrelease formulation (PGB-CR) (doses of 165 or 330 mg/day) in patients with partialonset seizures (POS). Methods: This was a randomized, double-blind (DB), parallel-group study of PGB-CR once-daily as adjunctive treatment in adults with treatment-resistant partial seizures. After an 8-week baseline period, eligible patients were randomized (1:1:1) to placebo, PGB-CR 165 mg, or PGB-CR 330 mg for 14 weeks, including a 2-week dose escalation. Primary endpoint was the log e -transformed 28-day seizure rate for all POS with observable component during the full 14-week double-blind treatment phase. Secondary endpoints included the 50% responder rate and percent change from baseline in 28-day POS rate. Results: Three hundred twenty-three patients were randomized and received treatment; placebo (n = 110), PGB-CR 330 mg (n = 100), PGB-CR 165 mg (n = 113); and 287 (88.9%) completed the trial. The primary efficacy analysis result, expressed as percent reduction from placebo, was 13.1% and 1.0% for PGB-CR 330 mg and PGB-CR 165 mg, respectively, and was not statistically significant (p = 0.091, 0.908). The proportion of 50% responders was similar for placebo (35.8%) and 165 mg PGB-CR (37.8%) and nominally higher for 330 mg PGB-CR (45.9%, p = 0.125 compared to placebo). The LS mean estimates of the percent change from baseline for placebo (À5.7%) was nominally smaller than 165 mg PGB-CR (À15.0%, p = 0.540) and 330 mg PGB-CR (À31.5%, p = 0.079); however, the median percent changes from baseline were not as well differentiated (placebo, À35.4%; 165 mg PGB-CR, À38.0%; 330 mg PGB-CR À43.4%). Rates of adverse events (AEs) were low for placebo and study drug; the most frequent reported AEs were dizziness, somnolence, and fatigue, consistent with the immediate-release formulation. Significance: Results from this trial did not demonstrate that PGB-CR is effective in reducing seizure frequency below that of placebo. Both doses of PGB-CR were shown to be safe and well-tolerated.

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confidence: 99%

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confidence: 99%

Adjunctive use of controlled‐release pregabalin in adults with treatment‐resistant partial seizures: A double‐blind, randomized, placebo‐controlled trial

French¹,

Brandt

Friedman³

et al. 2014

Epilepsia

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“…Keywords: antiepileptic drugs, extended-release, modified-release, suffix designations BAC KGRO UND Immediate-release (IR) oral formulations of antiepileptic drugs (AEDs) with short elimination half-lives require frequent administration to maintain the desired therapeutic concentration over the dosing interval and commonly result in large fluctuations in plasma AED concentrations (1)(2)(3).…”

Section: Resultsmentioning

confidence: 99%

What do the suffixes - XR, ER, Chrono, Chronosphere - really mean as it pertains to modified-release antiepileptic drugs?

Reed¹,

Meinhold²,

Dutta³

et al. 2010

Journal of Clinical Pharmacy and Therapeutics

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Summary Background: Epilepsy is a disease requiring chronic therapy with antiepileptic drugs (AEDs). Many conventional AEDs currently available have either too rapid an absorption or elimination, requiring the patient to take multiple doses per day, which may adversely impact adherence or cause peak‐related side‐effects. Consequently, some AEDs with immediate‐release characteristics have been modified to prolong absorption and/or reduce peak serum concentration, enabling dosage regimen simplification. Modified‐release (MR) AED formulations have been labelled with various suffixes or names (‘XR, ER, ‐Chrono, ‐Chronosphere’), but such labelling may not adequately distinguish those MR AEDs with the most prolonged absorption or unique formulation characteristics. Such suffixes lack precise definition. Objective: We identified the formulation characteristics of currently available MR AEDs, attempting to distinguish them by suffix designation. Design/methods: Nine MR AED formulations, representing six different AEDs, were characterized, utilizing information from FDA‐approved inserts (2001 +) and published literature. Results: The formulation characteristics of commercially available MR AEDs are quite variable and do not appear to correlate with their brand name suffix. Conclusions: When all MR AEDs are compared, suffix designations do not provide distinguishable information about formulation characteristics. Clarification of MR AED suffix terminology may be warranted.

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“…It is more certain that they minimize concentration-related adverse effects. 3,4 From a patient compliance perspective, it is unknown whether once-daily administration of AEDs is "better" than twice-daily administration. Levy et al demonstrated that switching dosing schedules from multiple doses per day to once daily by the use of ER drug formulations did not generally improve therapeutic coverage.…”

Section: Defining An Optimal Dosing Regimen For Medication Compliancementioning

confidence: 99%

“…2 Some postulate that the ER drug formulations could minimize the undesirable events and increase patient compliance by maintaining flat plasma drug concentrations. 3,4 However, available data suggest that less frequent dosing intervals do not necessarily translate to increased compliance, indicating that side effects and inconvenience alone cannot explain non-adherence.…”

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confidence: 99%

Overactive Bladder Disease: The Urge for Better Therapies

Thomas

Culley²

2008

JMCP

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Pharmacokinetic Evaluation of Sustained Release Formulations of Antiepileptic Drugs

Cited by 30 publications

References 31 publications

Adjunctive use of controlled‐release pregabalin in adults with treatment‐resistant partial seizures: A double‐blind, randomized, placebo‐controlled trial

Adjunctive use of controlled‐release pregabalin in adults with treatment‐resistant partial seizures: A double‐blind, randomized, placebo‐controlled trial

What do the suffixes - XR, ER, Chrono, Chronosphere - really mean as it pertains to modified-release antiepileptic drugs?

Overactive Bladder Disease: The Urge for Better Therapies

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