常用抗癫痫药物的临床应用及药理特点
摘要
癫痫是神经系统常见疾病,在我国患病率较高,现如今口服药物是治疗癫痫的主要手段,经过不断研发,越来越多的抗癫痫药物应用于临床。本文旨在总结临床常用抗癫痫药物的临床应用及药理特点,对指导临床合理用药提供参考和借鉴。
引文
[1]Shahabeddin SS,Javad J,Norouzi JA,et al.Descriptive epidemiology prevalence,incidence,sociodemographic factors,socioeconomic domains and quality of life of epilepsy:an update and systematic review[J].Archives of Medical Science,2018,14(4):717-724.
[2]李世绰,洪震,吴逊,等.临床诊疗指南癫痫分册[M].北京:人民卫生出版社,2015:11.
[3]Kane JC,Elafros MA,Murray SM,et al.A scoping review of health-related stigma outcomes for high-burden diseases in low-and middle-income countries[J].BMC Medicine,2019,17(1):1-40.
[4]Bhandare AM,Kapoor K,Powell KL,et al.Inhibition of microglial activation with minocycline at the intrathecal level attenuates sympathoexcitatory and proarrhythmogenic changes in rats with chronic temporal lobe epilepsy[J]Neuroscience,2017,350:23-38.
[5]Maguire MJ,Jackson CF,Marson AG,et al.Treatments for the prevention of sudden unexpected death in epilepsy(SUDEP)[J].Cochrane Database Syst Rev,2016,82(7):425-460.
[6]Perucca E.An introduction to antiepileptic drugs[J].Epilepsia,2010,46(s4):31-37.
[7]Zhengmao L,Fenzan W,Xie Z,et al.Valproate attenuates endoplasmic reticulum stress-induced apoptosis in SH-SY5Y cells via the AKT/GSK3βsignaling pathway[J].International Journal of Molecular Sciences,2017,18(2):315-331.
[8]Johnson JJ,Pajarillo E,Karki P,et al.Valproic acid attenuates manganeseinduced reduction in expression of GLT-1 and GLAST with concomitant changes in murine dopaminergic neurotoxicity[J].Neurotoxicology,2018,67:112-120.
[9]Maxime Doré,Juan AES,Frenette AJ,et al.Clinical importance of monitoring unbound valproic acid concentration in patients with hypoalbuminemia[J].Ph armacotherapy,2017,37(8):900-907.
[10]Wang C,Wang P,Yang LP,et al.Association of CYP2C9,CYP2A6ACSM2A,and CPT1A gene polymorphisms with adverse effects of valproic acid in Chinese patients with epilepsy[J].Epilepsy Research,2017,132:64-69.
[11]吴冬燕,朱国行.抗癫痫药物的分类、作用机制与不良反应[J].上海医药,2015,36(9):3-7.
[12]Voinescu PE,Pennell PB.Management of epilepsy during pregnancy[J]Expert Review of Neurotherapeutics,2015,10(2):161-176.
[13]Veroniki AA,Rios P,Cogo E,et al.Comparative safety of antiepileptic drugs for neurological development in children exposed during pregnancy and breast feeding a systematic review and network meta-analysis[J].BMJ Open,2017,7(7):1-11.
[14]P e r u c c a E.A n i n t r o d u c t i o n t o a n t i e p i l e p t i c d r u g s[J]Epilepsia,2010,46(4):31-37.
[15]Zhang H,Zhang W,Li Y,et al.Correlations between UGT2B7 2 gene polymorphisms and plasma concentrations of carbamazepine and valproic acid in epilepsy patients[J].Brain Dev,2018,40(2):100-106.
[16]Hartley R,Forsythe WI,Mclain B,et al.Daily variations in steady-state plasma concentrations of carbamazepine and its metabolites in epileptic children[J].Clinical Pharmacokinetics,1991,20(3):237-246.
[17]Djordjevic N,Jankovic SM,Milovanovic JR.Pharmacokinetics and Pharmacogenetics of Carbamazepine in Children[J].Eur J Drug Metab Pharmacokinet,2017,42(5):729-744.
[18]Balestrini S,Sisodiya SM.Pharmacogenomics in epilepsy[J].Neuroscience Letters,2018,667:27-39.
[19]周福永,蔡志琴,王枳人.卡马西平致重症型皮肤损伤1例[J].医药导报,2018,37(12):41-42.
[20]李六水,刘宪军.临床常用传统抗癫痫药物及其药理作用特点[J].北京联合大学学报(自然科学版),2017,31(3):66-69.
[21]Pacifici GM.Clinical pharmacology of phenobarbital in neonates:effects metabolism and pharmacokinetics[J].Current Rheumatology Reviews2016,12(1):48-54.
[22]El-Dib M,Soul JS.The use of phenobarbital and other anti-seizure drugs in newborns[J].Seminars in Fetal and Neonatal Medicine,2017,22(5):321-327.
[23]Moffett BS,Weingarten MM,Marianne G,et al.Phenobarbita population pharmacokinetics across the pediatric age spectrum[J].Epileps ia,2018,59(7):1327-1333.
[24]Kousar S,Wafai ZA,Wani MA,et al.Clinical relevance of genetic polymorphism in the CYP2C9 gene to pharmacodynamics and pharmacokinetics of phenytoin in epileptic patients:Validatory pharmacogenomic approach to pharmacovigilance[J].International Journa of Clinical Pharmacology&Therapeutics,2015,53(7):392-401.
[25]Uribe-San-Martín R,Ciampi E,Uslar W,et al.Risk factors of early adverse drug reactions with phenytoin:A prospective inpatient cohort[J].Epilepsy&Behavior,2017,76:139-144.
[26]Hedderick EF,Morris CM,Singer HS.Double-blind,crossover study of clonidine and levetiracetam in Tourette syndrome[J].Pediatric Neurology,2009,40(6):420-425.
[27]朱锦莉.丙戊酸钠合用氯硝西泮治疗难治性癫痫的临床疗效分析[J]中国医药指南,2016,14(22):133-134.
[28]Nozawa H,Minakata K,Yamagishi I,et al.MALDI-TOF mass spectrometric determination of eight benzodiazepines with two of their metabolites in blood[J].Legal Medicine,2015,17(3):150-156.
[29]Kobayashi T,Hirai H,Iino M,et al.Inhibitory effects of the antiepileptic drug ethosuximide on G protein-activated inwardly rectifying K+channels[J]Neuropharmacology,2009,56(2):499-506.
[30]任夏洋,赵志刚.抗癫痫药的药物基因组学研究进展[J].中国临床药理学杂志,2010,26(5):386-389.
[31]范磊,陈海燕.乙琥胺与拉莫三嗪治疗儿童失神性癫痫的疗效比较[J]中国现代药物应用,2013,7(13):161-162.
[32]Kanner AM,Ashman E,Gloss D,et al.Practice guideline update summary Efficacy and tolerability of the new antiepileptic drugs II:Treatment-resistant epilepsy[J].Epilepsy Currents,2018,18(4):269-278.
[33]Dr Gérard Flesch.Overview of the clinical pharmacokinetics of oxcarbazepine[J].Clinical Drug Investigation,2004,24(4):185-203.
[34]Du Y,Lin J,Shen J,et al.Adverse drug reactions associated with six commonly used antiepileptic drugs in southern China from 2003 to 2015[J]BMC Pharmacology and Toxicology,2019,20(1):2-8.
[35]Glauser TA.Expanding first-line therapy options for children with partia seizures[J].Neurology,2000,55(3):30-37.
[36]Eadie MJ.Treating epilepsy in pregnant women[J].Expert Opinion on Pharmacotherapy,2014,15(6):841-850.
[37]Muradi AB,Doaa Z,Mohammed J.Lennox-Gastaut syndrome management update[J].Neurosciences,2015,20(3):207-212.
[38]Kim HR,Kim GH,Eun SH,et al.Therapeutic outcomes and prognostic factors in childhood absence epilepsy[J].Journal of Clinica Neurology,2016,12(2):1-6.
[39]Brigo F,Igwe SC.Ethosuximide,sodium valproate or lamotrigine for absence seizures in children and adolescents[J].Cochrane Database Syst Rev,2017,14(2):1-38.
[40]LasońW,Chlebicka M,Rejdak K.Research advances in basic mechanisms of seizures and antiepileptic drug action[J].Pharmacologica Reports,2013,65(4):787-801.
[41]Hadjiloizou SM,Bourgeois BF.Antiepileptic drug treatment in children[J]Expert Rev Neurother,2007,7(2):179-193.
[42]Tomson T,Battino D,Bonizzoni E,et al.Dose-dependent risk of malformations with antiepileptic drugs:an analysis of data from the EURAPepilepsy and pregnancy registry[J].Lancet Neurol,2011,10(7):609-617.
[43]Thomas SV,Jose M,Divakaran S,et al.Malformation risk of antiepileptic drug exposure during pregnancy in women with epilepsy:Results from a pregnancy registry in South India[J].Epilepsia,2017,58(2):274-281.
[44]Spritzer SD,Bravo TP,Drazkowski JF.Topiramate for treatment in patients with migraine and epilepsy[J].Headache:The Journal of Head and Face Pain,2016,56(6):1081-1085.
[45]Jankovic J,Jimenez-Shahed J,Brown LW.A randomised,double-blind,placebocontrolled study of topiramate in the treatment of Tourette syndrome[J].Journa of Neurology,Neurosurgery&Psychiatry,2010,81(1):70-73.
[46]Motaghinejad M,Motevalian M,Fatima S,et al.Topiramate via NMDAAMPA/kainate,GABAA and Alpha2 receptors and by modulation of CREB/BDNF and Akt/GSK3 signaling pathway exerts neuroprotective effects against methylphenidate-induced neurotoxicity in rats[J].Journal of Neural Transmission,2017,124(11):1369-1387.
[47]Lyseng-Williamson KA,Yang LP.Spotlight on topiramate in epilepsy[J]CNS Drugs,2008,22(2):171-174.
[48]Huh HJ,Joo EY,Hong SB,et al.Factors influencing serum topiramate concentrations in routine therapeutic drug monitoring in Korean adult patients with epilepsy[J].Therapeutic Drug Monitoring,2013,35(2):177-182.
[49]Hernández-Díaz S,Smith CR,Shen A,et al.Comparative safety of antiepileptic drugs during pregnancy[J].Neurology,2012,78(21):1692-1699.
[50]Klitgaard H,Matagne A,Nicolas JM,et al.Brivaracetam:Rationale for discovery and preclinical profile of a selective SV2A ligand for epilepsy treatment[J].Epilepsia,2016,57(4):538-548.
[51]Wang M,Wang M,Zhang Q,et al.Pharmacokinetics and safety of levetiracetam extended-release tablets and relative bioavailability compared with immediate-release tablets in healthy chinese subjects[J].European Journal of Drug Metabolism&Pharmacokinetics,2018,43(4):405-413.
[52]Guray K,Selda KG,Omer K,et al.Fetal safety of levetiracetam use during pregnancy[J].Acta Neurologica Belgica,2018,118(3):503-508..
[53]Chincholkar M.Analgesic mechanisms of gabapentinoids and effects in experimental pain models:a narrative review[J].British Journal of Anaesthesia,2018,120(6):1315-1334.
[54]带状疱疹后神经痛诊疗共识编写专家组.带状疱疹后神经痛诊疗中国专家共识[J].中国疼痛医学杂志,2016,22(3):161-167.
[55]Suto T,Severino AL,Eisenach JC,et al.Gabapentin increases extracellular glutamatergic level in the locus coeruleus via astroglial glutamate transporterdependent mechanisms[J].Neuropharmacology,2014,81:95-100.
[56]Ahmed GF,Bathena SP,Brundage RC,et al.Pharmacokinetics and saturable absorption of gabapentin in nursing home elderly patients[J].The AAPSJournal,2017,19(2):551-556.
[57]夏伟,唐颖莹,邢爱耘.孕期新型抗癫痫药物的合理应用和研究进展[J]中华妇幼临床医学杂志(电子版),2016,12(1):108-113.
[58]Lotarski S,Hain H,Peterson J,et al.Anticonvulsant activity of pregabalin in the maximal electroshock-induced seizure assay inα2δ1(R217A)andα2δ2(R279A)mouse mutants[J].Epilepsy Research,2014,108(5):833-842.
[59]Bockbrader HN,Radulovic LL,Posvar EL,et al.Clinical pharmacokinetics of pregabalin in healthy volunteers[J].The Journal of Clinical Pharmacology2010,50(8):941-950.
[60]Otsuki T,Higuchi T,Yamazaki T,et al.Efficacy and safety of pregabalin for the treatment of neuropathic pain in patients undergoing hemodialysis[J].Clin Drug Investig,2017,37(1):95-102.
[61]Toth C.Drug safety evaluation of pregabalin[J].Expert Opinion on Drug Safety,2012,11(3):487-502.
[2]李世绰,洪震,吴逊,等.临床诊疗指南癫痫分册[M].北京:人民卫生出版社,2015:11.
[3]Kane JC,Elafros MA,Murray SM,et al.A scoping review of health-related stigma outcomes for high-burden diseases in low-and middle-income countries[J].BMC Medicine,2019,17(1):1-40.
[4]Bhandare AM,Kapoor K,Powell KL,et al.Inhibition of microglial activation with minocycline at the intrathecal level attenuates sympathoexcitatory and proarrhythmogenic changes in rats with chronic temporal lobe epilepsy[J]Neuroscience,2017,350:23-38.
[5]Maguire MJ,Jackson CF,Marson AG,et al.Treatments for the prevention of sudden unexpected death in epilepsy(SUDEP)[J].Cochrane Database Syst Rev,2016,82(7):425-460.
[6]Perucca E.An introduction to antiepileptic drugs[J].Epilepsia,2010,46(s4):31-37.
[7]Zhengmao L,Fenzan W,Xie Z,et al.Valproate attenuates endoplasmic reticulum stress-induced apoptosis in SH-SY5Y cells via the AKT/GSK3βsignaling pathway[J].International Journal of Molecular Sciences,2017,18(2):315-331.
[8]Johnson JJ,Pajarillo E,Karki P,et al.Valproic acid attenuates manganeseinduced reduction in expression of GLT-1 and GLAST with concomitant changes in murine dopaminergic neurotoxicity[J].Neurotoxicology,2018,67:112-120.
[9]Maxime Doré,Juan AES,Frenette AJ,et al.Clinical importance of monitoring unbound valproic acid concentration in patients with hypoalbuminemia[J].Ph armacotherapy,2017,37(8):900-907.
[10]Wang C,Wang P,Yang LP,et al.Association of CYP2C9,CYP2A6ACSM2A,and CPT1A gene polymorphisms with adverse effects of valproic acid in Chinese patients with epilepsy[J].Epilepsy Research,2017,132:64-69.
[11]吴冬燕,朱国行.抗癫痫药物的分类、作用机制与不良反应[J].上海医药,2015,36(9):3-7.
[12]Voinescu PE,Pennell PB.Management of epilepsy during pregnancy[J]Expert Review of Neurotherapeutics,2015,10(2):161-176.
[13]Veroniki AA,Rios P,Cogo E,et al.Comparative safety of antiepileptic drugs for neurological development in children exposed during pregnancy and breast feeding a systematic review and network meta-analysis[J].BMJ Open,2017,7(7):1-11.
[14]P e r u c c a E.A n i n t r o d u c t i o n t o a n t i e p i l e p t i c d r u g s[J]Epilepsia,2010,46(4):31-37.
[15]Zhang H,Zhang W,Li Y,et al.Correlations between UGT2B7 2 gene polymorphisms and plasma concentrations of carbamazepine and valproic acid in epilepsy patients[J].Brain Dev,2018,40(2):100-106.
[16]Hartley R,Forsythe WI,Mclain B,et al.Daily variations in steady-state plasma concentrations of carbamazepine and its metabolites in epileptic children[J].Clinical Pharmacokinetics,1991,20(3):237-246.
[17]Djordjevic N,Jankovic SM,Milovanovic JR.Pharmacokinetics and Pharmacogenetics of Carbamazepine in Children[J].Eur J Drug Metab Pharmacokinet,2017,42(5):729-744.
[18]Balestrini S,Sisodiya SM.Pharmacogenomics in epilepsy[J].Neuroscience Letters,2018,667:27-39.
[19]周福永,蔡志琴,王枳人.卡马西平致重症型皮肤损伤1例[J].医药导报,2018,37(12):41-42.
[20]李六水,刘宪军.临床常用传统抗癫痫药物及其药理作用特点[J].北京联合大学学报(自然科学版),2017,31(3):66-69.
[21]Pacifici GM.Clinical pharmacology of phenobarbital in neonates:effects metabolism and pharmacokinetics[J].Current Rheumatology Reviews2016,12(1):48-54.
[22]El-Dib M,Soul JS.The use of phenobarbital and other anti-seizure drugs in newborns[J].Seminars in Fetal and Neonatal Medicine,2017,22(5):321-327.
[23]Moffett BS,Weingarten MM,Marianne G,et al.Phenobarbita population pharmacokinetics across the pediatric age spectrum[J].Epileps ia,2018,59(7):1327-1333.
[24]Kousar S,Wafai ZA,Wani MA,et al.Clinical relevance of genetic polymorphism in the CYP2C9 gene to pharmacodynamics and pharmacokinetics of phenytoin in epileptic patients:Validatory pharmacogenomic approach to pharmacovigilance[J].International Journa of Clinical Pharmacology&Therapeutics,2015,53(7):392-401.
[25]Uribe-San-Martín R,Ciampi E,Uslar W,et al.Risk factors of early adverse drug reactions with phenytoin:A prospective inpatient cohort[J].Epilepsy&Behavior,2017,76:139-144.
[26]Hedderick EF,Morris CM,Singer HS.Double-blind,crossover study of clonidine and levetiracetam in Tourette syndrome[J].Pediatric Neurology,2009,40(6):420-425.
[27]朱锦莉.丙戊酸钠合用氯硝西泮治疗难治性癫痫的临床疗效分析[J]中国医药指南,2016,14(22):133-134.
[28]Nozawa H,Minakata K,Yamagishi I,et al.MALDI-TOF mass spectrometric determination of eight benzodiazepines with two of their metabolites in blood[J].Legal Medicine,2015,17(3):150-156.
[29]Kobayashi T,Hirai H,Iino M,et al.Inhibitory effects of the antiepileptic drug ethosuximide on G protein-activated inwardly rectifying K+channels[J]Neuropharmacology,2009,56(2):499-506.
[30]任夏洋,赵志刚.抗癫痫药的药物基因组学研究进展[J].中国临床药理学杂志,2010,26(5):386-389.
[31]范磊,陈海燕.乙琥胺与拉莫三嗪治疗儿童失神性癫痫的疗效比较[J]中国现代药物应用,2013,7(13):161-162.
[32]Kanner AM,Ashman E,Gloss D,et al.Practice guideline update summary Efficacy and tolerability of the new antiepileptic drugs II:Treatment-resistant epilepsy[J].Epilepsy Currents,2018,18(4):269-278.
[33]Dr Gérard Flesch.Overview of the clinical pharmacokinetics of oxcarbazepine[J].Clinical Drug Investigation,2004,24(4):185-203.
[34]Du Y,Lin J,Shen J,et al.Adverse drug reactions associated with six commonly used antiepileptic drugs in southern China from 2003 to 2015[J]BMC Pharmacology and Toxicology,2019,20(1):2-8.
[35]Glauser TA.Expanding first-line therapy options for children with partia seizures[J].Neurology,2000,55(3):30-37.
[36]Eadie MJ.Treating epilepsy in pregnant women[J].Expert Opinion on Pharmacotherapy,2014,15(6):841-850.
[37]Muradi AB,Doaa Z,Mohammed J.Lennox-Gastaut syndrome management update[J].Neurosciences,2015,20(3):207-212.
[38]Kim HR,Kim GH,Eun SH,et al.Therapeutic outcomes and prognostic factors in childhood absence epilepsy[J].Journal of Clinica Neurology,2016,12(2):1-6.
[39]Brigo F,Igwe SC.Ethosuximide,sodium valproate or lamotrigine for absence seizures in children and adolescents[J].Cochrane Database Syst Rev,2017,14(2):1-38.
[40]LasońW,Chlebicka M,Rejdak K.Research advances in basic mechanisms of seizures and antiepileptic drug action[J].Pharmacologica Reports,2013,65(4):787-801.
[41]Hadjiloizou SM,Bourgeois BF.Antiepileptic drug treatment in children[J]Expert Rev Neurother,2007,7(2):179-193.
[42]Tomson T,Battino D,Bonizzoni E,et al.Dose-dependent risk of malformations with antiepileptic drugs:an analysis of data from the EURAPepilepsy and pregnancy registry[J].Lancet Neurol,2011,10(7):609-617.
[43]Thomas SV,Jose M,Divakaran S,et al.Malformation risk of antiepileptic drug exposure during pregnancy in women with epilepsy:Results from a pregnancy registry in South India[J].Epilepsia,2017,58(2):274-281.
[44]Spritzer SD,Bravo TP,Drazkowski JF.Topiramate for treatment in patients with migraine and epilepsy[J].Headache:The Journal of Head and Face Pain,2016,56(6):1081-1085.
[45]Jankovic J,Jimenez-Shahed J,Brown LW.A randomised,double-blind,placebocontrolled study of topiramate in the treatment of Tourette syndrome[J].Journa of Neurology,Neurosurgery&Psychiatry,2010,81(1):70-73.
[46]Motaghinejad M,Motevalian M,Fatima S,et al.Topiramate via NMDAAMPA/kainate,GABAA and Alpha2 receptors and by modulation of CREB/BDNF and Akt/GSK3 signaling pathway exerts neuroprotective effects against methylphenidate-induced neurotoxicity in rats[J].Journal of Neural Transmission,2017,124(11):1369-1387.
[47]Lyseng-Williamson KA,Yang LP.Spotlight on topiramate in epilepsy[J]CNS Drugs,2008,22(2):171-174.
[48]Huh HJ,Joo EY,Hong SB,et al.Factors influencing serum topiramate concentrations in routine therapeutic drug monitoring in Korean adult patients with epilepsy[J].Therapeutic Drug Monitoring,2013,35(2):177-182.
[49]Hernández-Díaz S,Smith CR,Shen A,et al.Comparative safety of antiepileptic drugs during pregnancy[J].Neurology,2012,78(21):1692-1699.
[50]Klitgaard H,Matagne A,Nicolas JM,et al.Brivaracetam:Rationale for discovery and preclinical profile of a selective SV2A ligand for epilepsy treatment[J].Epilepsia,2016,57(4):538-548.
[51]Wang M,Wang M,Zhang Q,et al.Pharmacokinetics and safety of levetiracetam extended-release tablets and relative bioavailability compared with immediate-release tablets in healthy chinese subjects[J].European Journal of Drug Metabolism&Pharmacokinetics,2018,43(4):405-413.
[52]Guray K,Selda KG,Omer K,et al.Fetal safety of levetiracetam use during pregnancy[J].Acta Neurologica Belgica,2018,118(3):503-508..
[53]Chincholkar M.Analgesic mechanisms of gabapentinoids and effects in experimental pain models:a narrative review[J].British Journal of Anaesthesia,2018,120(6):1315-1334.
[54]带状疱疹后神经痛诊疗共识编写专家组.带状疱疹后神经痛诊疗中国专家共识[J].中国疼痛医学杂志,2016,22(3):161-167.
[55]Suto T,Severino AL,Eisenach JC,et al.Gabapentin increases extracellular glutamatergic level in the locus coeruleus via astroglial glutamate transporterdependent mechanisms[J].Neuropharmacology,2014,81:95-100.
[56]Ahmed GF,Bathena SP,Brundage RC,et al.Pharmacokinetics and saturable absorption of gabapentin in nursing home elderly patients[J].The AAPSJournal,2017,19(2):551-556.
[57]夏伟,唐颖莹,邢爱耘.孕期新型抗癫痫药物的合理应用和研究进展[J]中华妇幼临床医学杂志(电子版),2016,12(1):108-113.
[58]Lotarski S,Hain H,Peterson J,et al.Anticonvulsant activity of pregabalin in the maximal electroshock-induced seizure assay inα2δ1(R217A)andα2δ2(R279A)mouse mutants[J].Epilepsy Research,2014,108(5):833-842.
[59]Bockbrader HN,Radulovic LL,Posvar EL,et al.Clinical pharmacokinetics of pregabalin in healthy volunteers[J].The Journal of Clinical Pharmacology2010,50(8):941-950.
[60]Otsuki T,Higuchi T,Yamazaki T,et al.Efficacy and safety of pregabalin for the treatment of neuropathic pain in patients undergoing hemodialysis[J].Clin Drug Investig,2017,37(1):95-102.
[61]Toth C.Drug safety evaluation of pregabalin[J].Expert Opinion on Drug Safety,2012,11(3):487-502.