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Drug Evaluations

Pharmacokinetic and pharmacodynamic profile of pregabalin and its role in the treatment of epilepsy

Pages 105-115 | Published online: 04 Dec 2012

Bibliography

  • ILAE/IBE/WHO Global Campaign Against Epilepsy, 2003. Annual Report 2003. Epilepsy Out of the Shadows. ILAE/IBE/WHO Global Campaign Against Epilepsy
  • Arain AM, Abou-Khalil BW. Management of new-onset epilepsy in the elderly. Nat Rev Neurol 2009;5:363-71
  • Ridsdale L, Charlton J, Ashworth M, Epilepsy mortality and risk factors for death in epilepsy: a population-based study. Br J Gen Pract 2011;61(586):e271-8
  • Faught E, Richman J, Martin R, Incidence and prevalence of epilepsy among older U.S. Medicare beneficiaries. Neurology 2012;78:448-53
  • Kwan P, Brodie MJ. Early identification of refractory epilepsy. N Engl J Med 2000;342:314-19
  • Mohanraj R, Brodie MJ. Diagnosing refractory epilepsy: response to sequential treatment schedules. Eur J Neurol 2006;13:277-82
  • Schiller Y, Najjar Y. Quantifying the response to antiepileptic drugs: effect of past treatment history. Neurology 2008;70:54-65
  • Bryans JS, Wustrow DJ. 3-Substituted GABA analogs with central nervous system activity: a review. Med Res Rev 1999;19:149-77
  • Piechan JL, Donevan SD, Taylor CP, Pregabalin, a novel anticonvulsant, analgesic, and anxiolytic drug, exhibits class-specific alpha2—delta-1 and alpha2—delta-2 calcium channel subunit binding. Soc Neurosci Abstr 2004;111:Program No. 115
  • Silverman RB, Andruszkiewicz R, Nanavati SM, 3-Alkyl-4-aminobutyric acids: the first class of anticonvulsant agents that activates L-glutamic acid decarboxylase. J Med Chem 1991;34:2295-8
  • Errante LD, Petroff OAC. Acute effects of gabapentin and pregabalin on rat forebrain cellular GABA, glutamate, and glutamine concentrations. Seizure 2003;12:300-6
  • Whitworth TL, Quick MW. Upregulation of gammaaminobutyric acid transporter expression: role of alkylated gamma-aminobutyric acid derivatives. Biochem Soc Transact 2001;29:736-41
  • Su TZ, Feng MR, Weber ML. Mediation of highly concentrative uptake of pregabalin by L-type amino acid transport in Chinese hamster ovary and Caco-2 cells. J Pharmacol Exp Ther 2005;313:1-10
  • Bockbrader HN, Wesche D, Miller R, A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin. Clin Pharmacokinet 2010;49:661-9
  • Brodie MJ, Wilson EA, Wesche DL, Pregabalin drug interactions studies: lack of effect on the pharmacokinetis of carbamazepine, phenyoin, lamotrigine and valproate in patients with partial epilepsy. Epilepsia 2005;46:1407-13
  • Taylor CP, Angelotti T, Fauman E. Pharmacology and mechanism of action of pregabalin: the calcium channel 2-subunit as a target for antiepileptic drug discovery. Epil Res 2007;73:137-50
  • Arikkath J, Campbell KP. Auxiliary subunits: essential components of the voltage-gated calcium channel complex. Curr Opin Neurobiol 2003;13:298-307
  • Davies A, Hendrich J, Van-Minh AT, Functional biology of the alpha(2)delta subunits of voltage-gated calcium channels. Trends Pharmacol Sci 2007;28:220-8
  • Bauer A, Tran-Van-Minh A, Kadurin I, Dolphin AC. A new look at calcium channel 2 subunits. Curr Opin Neurobiol 2010;20:563-71
  • Fink K, Meder W, Dooley DJ, Gothert M. Inhibition of neuronal Ca(2+) influx by gabapentin and subsequent reduction of neurotransmitter release from rat neocortical slices. Br J Pharmacol 2000;130:900-6
  • Fink K, Dooley DJ, Meder WP, Inhibition of neuronal Ca-2+ influx by gabapentin and pregabalin in the human neocortex. Neuropharmacology 2002;42:229-36
  • van Hooft JA, Dougherty JJ, Endeman D, Gabapentin inhibits presynaptic Ca(2+) influx and synaptic transmission in rat hippocampus and neocortex. Eur J Pharmacol 2002;449:221-8
  • McClelland D, Evans RM, Barkworth L, A study comparing the actions of gabapentin and pregabalin on the electrophysiological properties of cultured DRG neurones from neonatal rats. BMC Pharmacol 2004;4:14-24
  • Taylor CP, Vartanian MG. Profile of the anticonvulsant activity of CI-1008 (pregabalin) in animal models. Epilepsia 1997;38(Suppl 8):8
  • Williamson J, Lothman CTE, Bertran E. Comparison of S(+)-3 Isobutyl GABA and gabapentin against kindled hippocampal seizures. Epilepsia 1997;38(Suppl 8):29
  • Delahoy P, Thompson S, Marschner IC. Pregabalin versus gabapentin in partial epilepsy: a meta-analysis of dose-response relationships. BMC Neurol 2010;10:104
  • Stephen LJ, Parker P, Kelly K, Adjunctive pregabalin for uncontrolled partial-onset seizures: findings from a prospective audit. Acta Neurol Scand 2011;124:142-5
  • Ben-Menachem E. Pregabalin pharmacology and its relevance to clinical practice. Epilepsia 2004;45(Suppl 6):13-18
  • Taylor CP, Vartanian MG, Yuen P, Potent and stereospecific anticonvulsant activity of 3-isobutyl GABA relates to in vitro binding at a novel site labelled by tritiated gabapentin. Epilepsy Res 1993;14:11-15
  • Vartanian MG, Radulovic LL, Kinsora JJ, Activity profile of pregabalin in rodent models of epilepsy and ataxia. Epilepsy Res 2006;68:189-205
  • Lang N, Sueske E, Hasan A, Pregabalin exerts oppositional effects on different inhibitory circuits in human motor cortex: a double-blind, placebo-controlled transcranial magnetic stimulation study. Epilepsia 2006;47:813-19
  • Lee JW, Dworetzky B. Rational polytherapy with antiepileptic drugs. Pharmaceuticals 2010;3:2362-79
  • Luszczki JJ, Jaskolska A, Dworzanski W, Zolkowska D. 7-Nitroindazole, but not NG-nitro-L-arginine, enhances the anticonvulsant activity of pregabalin in the mouse maximal electroshock-induced seizure model. Pharmacol Rep 2011;63:169-75
  • French JA, Kugler AR, Robbins JL, Dose-response trial of pregabalin adjunctive therapy in patients with partial seizures. Neurology 2003;60:1631-7
  • Arroyo S, Anhut H, Kugler AR, Pregabalin add-on treatment: a randomized, double-blind, placebo-controlled, dose-response study in adults with partial seizures. Epilepsia 2004;45:20-7
  • Beydoun A, Uthman BM, Kugler AR, Pregabalin 1008-009 Study Group. Safety and efficacy of two pregabalin regimens for add-on treatment of partial epilepsy. Neurology 2005;64:475-80
  • Elger CE, Brodie MJ, Anhut H, Pregabalin add-on treatment in patients with partial seizures: a novel evaluation of flexible-dose and fixed-dose treatment in a double-blind, placebo-controlled study. Epilepsia 2005;46:1926-36
  • Lee BI, Yi S, Hong SB, Pregabalin add-on therapy using a flexible, optimized dose schedule in refractory partial epilepsies: a double-blind, randomized, placebo-controlled, multicenter trial. Epilepsia 2009;50:464-74
  • Baulac M, Leon T, O'Brien TJ, A comparison of pregabalin, lamotrigine, and placebo as adjunctive therapy in patients with refractory partial-onset seizures. Epilepsy Res 2010;91:10-19
  • Lozsadi D, Hemming K, Marson AG. Pregabalin add-on for drug-resistant partial epilepsy. Cochrane Database Syst Rev 2008(1):CD005612
  • Tomson T, Almsas M, Giordano S, Cabrerac J. The impact of background antiepileptic drugs on the efficacy and safety of pregabalin in treating partial-onset seizures: a post hoc analysis of combined clinical trials. Epil Res 2011;96:64-73
  • French JA, Kanner AM, Bautista J, Efficacy and tolerability of the new antiepileptic drugs I: treatment of new onset epilepsy: report of the Therapeutics and Technology Assessment Subcommittee and Quality Standards Subcommittee of the American Academy of Neurology and the American Epilepsy Society. Neurology 2004;62:1252-60
  • Fakhoury T, French J, Kwan P, Pregabalin Monotherapy in Patients with Partial Onset Seizures: a Randomized, Double-Blind, Historical-Controlled Trial. Poster, presented at the AES; 2012
  • Available from: http://clinicaltrials.gov/ct2/show/NCT00280059
  • Marson AG, Al-Kharusi AM, Alwaidh M, On behalf of the SANAD Study group. The SANAD study of effectiveness of carbamazepine, gabapentin, lamotrigine, oxcarbazepine, or topiramate for treatment of partial epilepsy: an unblinded randomised controlled trial. Lancet 2007;369:1000-15
  • Kwan P, Brodie MJ, Kälviäinen R, Efficacy and safety of pregabalin versus lamotrigine in patients with newly diagnosed partial seizures: a phase 3, double-blind, randomised, parallel-group trial. Lancet Neurol 2011;10:881-90
  • Uthman BM, Bazil CW, Beydoun A, Long-term add-on pregabalin treatment in patients with partial-onset epilepsy: pooled analysis of open-label clinical trials. Epilepsia 2010;51:968-78
  • Ryvlin P, Kalviainen R, Von Raisonc R, Pregabalin in partial seizures: a pragmatic 21-week, open-label study (PREPS). Eur J Neurol 2010;726-32
  • Rivera-Castanoa L, Leal-Cantub R, Abreuc P, A 21-week open-label clinical trial of pregabalin as adjunctive therapy in partial seizures at multiple centers in Mexico (PREPS Mexico). Epil Res 2012;100:74-9
  • Brodie MJ. Pregabalin as adjunctive therapy for partial seizures. Epilepsia 2004;45(Suppl 6):19-27
  • Yuen AW, Singh R, Bell GS, The long-term retention of pregabalin in a large cohort of patients with epilepsy at a tertiary referral centre. Epilepsy Res 2009;87:120-3
  • Wensel TM, Powe KW, Cates ME. Pregabalin for the treatment of generalized anxiety disorder. Ann Pharmacother 2012;46:424-9
  • Piedad J, Rickards H, Besag FM, Cavanna AE. Beneficial and adverse psychotropic effects of antiepileptic drugs in patients with epilepsy: a summary of prevalence, underlying mechanisms and data limitations. CNS Drugs 2012;26:319-35
  • Salinsky M, Storzbach D, Munoz S. Cognitive effects of pregabalin in healthy volunteers: a double-blind, placebo-controlled trial. Neurology 2010;74:755-61
  • Ciesielski AS, Samson S, Steinhoff BJ. Neuropsychological and psychiatric impact of add-on titration of pregabalin versus levetiracetam: a comparative short-term study. Epilepsy Behav 2006;9:424-31
  • Bazil CW, Dave J, Cole J, Pregabalin increases slow-wave sleep and may improve attention in patients with partial epilepsy and insomnia. Epilepsy Behav 2012;23:422-5
  • Huppertz HJ, Feuerstein TJ, Schulze-Bonhage A. Myoclonus in epilepsy patients with anticonvulsive add-on therapy with pregabalin. Epilepsia 2001;42:790-2
  • Yoo L, Matalon D, Hoffman RS, Goldfarb DS. Treatment of pregabalin toxicity by hemodialysis in a patient with kidney failure. Am J Kidney Dis 54:1127-30
  • Criswell KA, Cook JC, Wojcinski Z, Mode of action associated with development of hemangiosarcoma in mice given pregabalin and assessment of human relevance. Toxicol Sci 2012;128:57-71
  • Cramer JA, Mattson RH, Prevey ML, How often is medication taken as prescribed? A novel assessment technique. JAMA 1989;261:3273-7
  • Cramer JA, Glassman M, Rienzi BA. The relationship between poor medication compliance and seizures. Epilepsy Behav 2002;3:338-42
  • Pellock JM, Smith MC, Cloay JC, Extended-release formulations: simplifying strategies in the management of antiepileptic drug therapy. Epilepsy Behav 2004;5:301-7
  • Ramsay RE, Perucca E, Robbins J, Rapid onset of seizure suppression with pregabalin adjunctive treatment in patients with partial seizures. Epilepsia 2009;50:1891-8
  • Swisher CB, Doreswamy M, Gingrich KJ, Phenytoin, levetiracetam, and pregabalin in the acute management of refractory status epilepticus in patients with brain tumors. Neurocrit Care 2012;16:109-13
  • Available from: http://clinicaltrials.gov/ct2/show/NCT01262677
  • Relling MV, Pui CH, Sandlund JT, Adverse effect of anticonvulsants on efficacy of chemotherapy for acute lymphoblastic leukaemia. Lancet 2000;356:285-90
  • Available from: http://clinicaltrials.gov/ct2/show/NCT00629889
  • Johannessen SI, Tomson T. Pharmacokinetic variability of newer antiepileptic drugs: when is monitoring needed? Clin Pharmacokinet 2006;45:1061-75
  • May TW, Rambeck B, Neb R, Jürgens U. Serum concentrations of Pregabalin in patients with epilepsy: the influence of dose, age, and comedication. Ther Drug Monit 2007;29:789-94
  • Patsalos PN. Pharmacokinetic profile of levetiracetam: toward ideal characteristics. Pharmacol Ther 2000;85:77-85
  • Pande AC, Crockatt JG, Feltner DE, Pregabalin in generalized anxiety disorder: a placebo-controlled trial. Am J Psychiatry 2003;160:533-40
  • Hellwig S, Mamalis P, Feige B, Psychiatric comorbidity in patients with pharmacoresistant focal epilepsy and psychiatric outcome after epilepsy surgery. Epilepsy Behav 2012;23:272-9
  • Available from: http://clinicaltrials.gov/ct2/show/NCT00537238
  • Kugler AR, Robbins JL, Strand JC, Pregabalin overview: a novel CNS-active compound with anticonvulsant activity. Poster presented at the Annual Meeting of the American Epilepsy Society; 6 – 11 December 2002; Washington, Seattle
  • Bockbrader HN, Radulovic LL, Posvar EL, Clinical pharmacokinetics of pregabalin in healthy volunteers. J Clin Pharmacol 2010;50:941-50
  • French JA, Abou-Khalil BW, Leroy RF, RESTORE 1/Study 301 Investigators. Randomized, double-blind, placebo-controlled trial of ezogabine (retigabine) in partial epilepsy. Neurology 2011;76:1555-63
  • Betts T, Waegemans T, Crawford P. A multicentre, double-blind, randomized, parallel group study to evaluate the tolerability and efficacy of two oral doses of levetiracetam, 2000 mg daily and 4000 mg daily, without titration in patients with refractory epilepsy. Seizure 2000;9:80-7
  • Cereghino JJ, Biton V, Abou-Khalil B, Levetiracetam for partial seizures: results of a double-blind, randomized clinical trial. Neurology 2000;55:236-42
  • Faught E, Ayala R, Montouris GG, Leppik IE; Zonisamide 922 Trial Group. Randomized controlled trial of zonisamide for the treatment of refractory partial-onset seizures. Neurology 2001;57:1774-9
  • Sackellares JC, Ramsay RE, Wilder BJ, Randomized, controlled clinical trial of zonisamide as adjunctive treatment for refractory partial seizures. Epilepsia 2004;45:610-17
  • Brodie MJ, Duncan R, Vespignani H, Dose-dependent safety and efficacy of zonisamide: a randomized, double-blind, placebo-controlled study in patients with refractory partial seizures. Epilepsia 2005;46:31-41
  • Ben-Menachem E, Biton V, Jatuzis D, Efficacy and safety of oral lacosamide as adjunctive therapy in adults with partial-onset seizures. Epilepsia 2007;48:1308-17
  • Chung S, Sperling MR, Biton V, SP754 Study Group. Lacosamide as adjunctive therapy for partial-onset seizures: a randomized controlled trial. Epilepsia 2010;51:958-67
  • Porter RJ, Partiot A, Sachdeo R, 205 Study Group. Randomized, multicenter, dose-ranging trial of retigabine for partial-onset seizures. Neurology 2007;68:1197-204

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