Effect of repeated administration of eslicarbazepine acetate on the pharmacokinetics of simvastatin in healthy subjects

Falcão, Amı́lcar; Pinto, Roberto; Nunes, Teresa; Soares-da-Silva, Patrı́cio

doi:10.1016/j.eplepsyres.2013.04.009

Cited by 28 publications

(10 citation statements)

References 20 publications

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“…Eslicarbazepine acetate reduces the levels of mean systemic exposure by 54% for simvastatin and 36–39% for rosuvastatin, thus it is advisable to monitor response to therapy (e.g., cholesterol levels) and increase the dose of these drugs if necessary (Fig. 6 ) [ 32 , 34 ]. Eslicarbazepine acetate has also been shown to decrease (S)-warfarin levels by 23%, but it has no influence over (R)-warfarin pharmacokinetics or coagulation [ 35 ].…”

Section: Interactionsmentioning

confidence: 99%

Eslicarbazepine Acetate: A New Improvement on a Classic Drug Family for the Treatment of Partial-Onset Seizures

Galiana¹,

Gauthier²,

Mattson³

2017

Drugs R D

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Eslicarbazepine acetate is a new anti-epileptic drug belonging to the dibenzazepine carboxamide family that is currently approved as adjunctive therapy and monotherapy for partial-onset (focal) seizures. The drug enhances slow inactivation of voltage-gated sodium channels and subsequently reduces the activity of rapidly firing neurons. Eslicarbazepine acetate has few, but some, drug–drug interactions. It is a weak enzyme inducer and it inhibits cytochrome P450 2C19, but it affects a smaller assortment of enzymes than carbamazepine. Clinical studies using eslicarbazepine acetate as adjunctive treatment or monotherapy have demonstrated its efficacy in patients with refractory or newly diagnosed focal seizures. The drug is generally well tolerated, and the most common side effects include dizziness, headache, and diplopia. One of the greatest strengths of eslicarbazepine acetate is its ability to be administered only once per day. Eslicarbazepine acetate has many advantages over older anti-epileptic drugs, and it should be strongly considered when treating patients with partial-onset epilepsy.

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Section: Interactionsmentioning

confidence: 99%

Eslicarbazepine Acetate: A New Improvement on a Classic Drug Family for the Treatment of Partial-Onset Seizures

Galiana¹,

Gauthier²,

Mattson³

2017

Drugs R D

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“…70 Eslicarbazepine acetate is mainly a pro-drug of S-MHD. 69 Eslicarbazepine does not self-induce its own metabolism, but appears to be a clinically relevant inducer of CYP3A4, demonstrated by increasing the clearance of simvastatin by approximately 2 71 and of the ethinyl estradiol and levonorgestrel present in oral contraceptives in a dose-dependent manner. 72 Eslicarbazepine may also be a weak UGT inducer, slightly increasing (<20%) the clearance of several AEDs including carbamazepine, lamotrigine and topiramate.…”

Section: Eslicarbazepinementioning

confidence: 99%

The effects of antiepileptic inducers in neuropsychopharmacology, a neglected issue. Part I: A summary of the current state for clinicians

León

2015

Revista de Psiquiatría y Salud Mental (English Edition)

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Right click to open a feedback form in a new tab to let us know how this document benefits you.This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/ 1 The effects of antiepileptic inducers in neuropsychopharmacology, a neglected issue. Part I: A summary of the current state for clinicians. AbstractThe literature on inducers in epilepsy and bipolar disorder is seriously contaminated by false negative findings. This is part I of a comprehensive review on antiepileptic drug (AED) inducers using both mechanistic pharmacological and evidence-based medicine to provide practical recommendations to neurologists and psychiatrists concerning how to control for them. Carbamazepine, phenobarbital and phenytoin, are clinically relevant AED inducers; correction factors were calculated for studied induced drugs. These correction factors are rough simplifications for orienting clinicians, since there is great variability in the population regarding inductive effects. As new information is published, the correction factors may need to be modified. Some of the correction factors are so high that the drugs (e.g., bupropion, quetiapine or lurasidone) should not co-prescribed with potent inducers. Clobazam, eslicarbazepine, felbamate, lamotrigine, oxcarbazepine, rufinamide, topiramate, vigabatrin and valproic acid are grouped as mild inducers which may (i) be inducers only in high doses; (ii) frequently combine with inhibitory properties; and (iii) take months to reach maximum effects or de-induction, definitively longer than the potent inducers. Potent inducers, definitively, and mild inducers, possibly, have relevant effects in the endogenous metabolism of (i) sexual hormones, (ii) vitamin D, (iii) thyroid hormones, (iv) lipid metabolism and (v) folic acid.Footnote: Table 1 and 3 were included in second part of this article but they are included here to facilitate reading.

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“…However, the AUC of main (inactive) metabolite, GS-331007, was found to increase by 5.5-fold in severe RI and 13.8-and 21.7-fold in ESRD 1 hour before and after dialysis, respectively. On the basis of these results, no dose adjustment is needed for patients with mild or moderate renal (Falcão et al, 2013;FDA, 2013c) Maximum changes in the victim AUC are presented. a 2013 NMEs are underlined.…”

Section: Hepatic and Renal Impairment Studiesmentioning

confidence: 99%

Drug Disposition and Drug-Drug Interaction Data in 2013 FDA New Drug Applications: A Systematic Review

Ritchie

Mulgaonkar

et al. 2014

Drug Metabolism and Disposition

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The aim of the present work was to perform a systematic review of drug metabolism, transport, pharmacokinetics, and DDI data available in the NDAs approved by the FDA in 2013, using the University of Washington Drug Interaction Database, and to highlight significant findings. Among 27 NMEs approved, 22 (81%) were well characterized with regard to drug metabolism, transport, or organ impairment, in accordance with the FDA drug interaction guidance (2012) and were fully analyzed in this review. In vitro, a majority of the NMEs were found to be substrates or inhibitors/inducers of at least one drug metabolizing enzyme or transporter. However, in vivo, only half (n = 11) showed clinically relevant drug interactions, with most related to the NMEs as victim drugs and CYP3A being the most affected enzyme. As perpetrators, the overall effects for NMEs were much less pronounced, compared with when they served as victims. In addition, the pharmacokinetic evaluation in patients with hepatic or renal impairment provided useful information for further understanding of the drugs' disposition.

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Effect of repeated administration of eslicarbazepine acetate on the pharmacokinetics of simvastatin in healthy subjects

Cited by 28 publications

References 20 publications

Eslicarbazepine Acetate: A New Improvement on a Classic Drug Family for the Treatment of Partial-Onset Seizures

Eslicarbazepine Acetate: A New Improvement on a Classic Drug Family for the Treatment of Partial-Onset Seizures

The effects of antiepileptic inducers in neuropsychopharmacology, a neglected issue. Part I: A summary of the current state for clinicians

Drug Disposition and Drug-Drug Interaction Data in 2013 FDA New Drug Applications: A Systematic Review

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