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维基百科

阿坎酸

阿坎酸(英語:Acamprosate)以Campral及Alglutol(戒酒妥)等品牌銷售,是一種與治療酒精使用疾患(酗酒)諮詢合併使用的藥物。[1][2]

阿坎酸
臨床資料
读音/əˈkæmprst/
商品名英语Drug nomenclatureCampral、Alglutol,及其他
其他名稱N-乙酰基高牛磺酸(N-Acetyl homotaurine), 阿坎酸鈣 (JAN JP), 阿坎酸鈣 (USAN US)
懷孕分級
给药途径口服給藥[1]
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度11%[1]
血漿蛋白結合率可忽略不計[1]
药物代谢[1]
生物半衰期20 - 33小時[1]
排泄途徑[1]
识别信息
  • 3-乙酰氨基丙烷-1-磺酸(3-Acetamidopropane-1-sulfonic acid)
CAS号77337-76-9  Y
PubChem CID
  • 155434
IUPHAR/BPS
  • 7106
DrugBank
  • DB00659 Y
ChemSpider
  • 136929 Y
UNII
  • N4K14YGM3J
KEGG
  • D07058 Y
ChEBI
  • CHEBI:51042 Y
ChEMBL
  • ChEMBL1201293 N
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
  • DTXSID3044259
ECHA InfoCard100.071.495
化学信息
化学式C5H11NO4S
摩尔质量181.21 g·mol−1
3D模型(JSmol英语JSmol
  • 交互式图像
  • [Ca+2].O=C(NCCCS(=O)(=O)[O-])C.[O-]S(=O)(=O)CCCNC(=O)C
  • InChI=1S/2C5H11NO4S.Ca/c2*1-5(7)6-3-2-4-11(8,9)10;/h2*2-4H2,1H3,(H,6,7)(H,8,9,10);/q;;+2/p-2 Y
  • Key:BUVGWDNTAWHSKI-UHFFFAOYSA-L Y

阿坎酸被認為可穩定大腦的神經傳遞英语Neurotransmission,這些訊號傳遞會因酒精戒斷而受干擾。[3]對大多數患者而言,單獨使用阿坎酸並非有效的治療方法。[4]研究發現將阿坎酸與社會心理支持結合時效果會最佳,因為該藥物有助於減少飲酒數量,也有達到完全戒酒的效果。[2][5][6]

服用此藥物的嚴重副作用有過敏反應心律不整以及低血壓或是高血壓,而較不嚴重的副作用有頭痛失眠勃起功能障礙[7]最常見的副作用是腹瀉[8]目前尚不清楚個體於懷孕期間使用是否對胎兒有安全的問題。[9][10]

此藥物被列入世界衛生組織基本藥物標準清單之中。[11]

醫療用途 编辑

有酒精使用障礙的患者在接受諮詢,並同時服用阿坎酸時會非常有用。[2]在三到十二個月的治療期間,完全不喝酒的人數和患者不喝酒的天數會增加。[2]它在維持戒酒方面似乎與納曲酮英语naltrexone一樣有效,[12]然而納曲酮在減少酒精渴望和酗酒方面效果稍好,[13]同時在歐洲以外,而治療服務不太健全的地區,使用阿坎酸的效果往往會較差。[14]

用藥禁忌 编辑

阿坎酸主要經由臟排除。對於腎功能中度受損的患者(肌酸酐清除率在30毫升/分鐘和50毫升/分鐘之間),建議將使用劑量降低。[1][15]對藥物中阿坎酸鈣或其任何成分有強烈過敏反應的人也應禁止使用。[15]

不良影響 编辑

此藥物在美國銷售的標籤上會列有服用會與自殺行為、重性憂鬱疾患腎衰竭增加有關聯的警告。[1]

臨床試驗中,對停止服用者導致的不良反應有腹瀉、噁心憂鬱焦慮[1]

潛在的副作用包括頭痛、腹痛、背痛、肌肉痛關節痛胸痛感染、類流感症狀、發冷、心悸、高血壓、昏厥嘔吐、胃部不適、便秘食慾增加、體重增加、水腫嗜睡、性慾減退、勃起功能障礙、健忘思考障礙、視力異常、味覺異常、顫抖流鼻涕咳嗽、呼吸困難、喉嚨痛、支氣管炎和皮[1]

藥理學 编辑

 
阿坎酸鈣分子結構

藥效學 编辑

阿坎酸的藥效學很複雜且尚未被完全了解,[16][17][18]然而它被認為可作為NMDA受體拮抗劑和[[GABAA受體]]的正變構調節劑英语allosteric modulator[17][18]

此藥物與大多數其他藥物不同,其對這些受體產生的活性是間接性的。[19]抑制GABAB系統被認為會間接導致GABAA受體增強。[19]對NMDA受體的影響具有劑量依賴性,藥物似乎在低濃度下可增強受體活性,而在較高濃度時會有抑制作用,可抵消患者在發生酒精戒斷情況下NMDA受體過度激活狀態。[20]

該藥物還可增加服用者的牛磺酸內源性產量。[20]

乙醇苯二氮平類藥物透過與GABAA受體結合,將具有抑制神經傳導作用的GABA功能增強,而對中樞神經系統發揮作用(即此藥物充當這些受體的正變構調節劑)。[17][4]對有酒精使用疾患的患者,發生耐受性的主要機制之一是GABAA受體下調(即這些受體對GABA變得不太敏感)。[4]而當個體停止飲酒後,正常的GABA生產就會導致戒斷症狀出現,[4]而導致神經元過度興奮。阿坎酸的作用機制之一是透過正變構受體調節,增強GABAA受體的GABA訊號傳導。[17][18]據稱此藥物能以一種新穎的方式打開氯離子通道,而不需要GABA作為輔助因子,因此比苯二氮平類藥物更不易產生依賴性。阿坎酸已成功用於控制因鼓膜張肌痙攣而導致的耳鳴聽覺過敏、耳痛和飲酒期間的內耳壓力。[21]

此外,酒精也會抑制NMDA受體的活性。[22][23]長期飲酒會導致這些受體過度生產(上調)。突然戒酒後會導致這些大量生產的NMDA受體比正常情況更為活躍,而產生震顫性譫妄興奮性毒性英语excitotoxicity而導致神經元死亡的情況。[24]戒酒會導致麩胺酸等興奮性神經傳導物質釋放激增,而過度激活NMDA受體。[25]阿坎酸可減少麩氨酸的激增。[26]該藥物還表現出可保護實驗室培養大鼠細胞免受乙醇戒斷引起的興奮性毒性,[27]以及受乙醇戒斷加上麩氨酸暴露的影響。[28]

此藥物也透過讓睡眠週期第3階段快速動眼期正常化來重建標準睡眠結構,而被認為是其藥理活性的一重要作用。[20]

藥物動力學 编辑

阿坎酸不會被人體代謝。[18]口服阿坎酸的絕對生物利用度約為11%,[18]飲食時服用阿坎酸,其生物利用度會被降低。[29]服用的阿坎酸會以原形經由腎臟排泄。[18]

阿坎酸受人體的吸收和消除非常緩慢,達到最大血藥濃度需6小時,達到生物半衰期需時超過30小時。[19]

歷史 编辑

阿坎酸由默克集團子公司Lipha所開發。[30]於1989年獲准在歐洲用於治療酒精依賴[31]

藥業公司Forest Laboratories英语Forest Laboratories於2001年10月取得藥物在美國的銷售權。[30][32]

該藥物於2004年7月獲得美國食品藥物管理局(FDA)核准用於醫療用途。[33]

阿坎酸的首個通用名藥物於2013年在美國上市。[34]

截至2015年,名為Confluence Pharmaceuticals的藥業公司在開發阿坎酸作為X染色體易裂症的治療法。此藥物在2013年被FDA授予孤兒藥地位,並於2014年也被歐洲藥品管理局(EMA)授予孤兒藥地位。[35]

社會與文化 编辑

"阿坎酸"是此藥物的國際非專有藥名(INN)和英國核准藥名英语British Approved Name(BAN)。 "阿坎酸鈣"是美國通用名英语United States Adopted Name(USAN)和日本接受名英语Japan Accepted Name(JAN)。它在技術上也稱為N-乙酰基高牛磺酸(N-acetylhomotaurine )或乙醯高牛磺酸(acetylhomotaurinate)。

此藥物以Campral[1]及Alglutol等品牌銷售。

研究 编辑

此藥物除能明顯幫助患者戒酒之外,一些證據顯示其具有神經保護作用(即它可保護神經元,免受酒精戒斷以及可能的其他神經毒性原因,而造成的損傷和死亡)。[26][36]

參見 编辑

  1. ^ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 Campral label (PDF). FDA. January 2012 [2017-11-27].  For label updates see FDA index page for NDA 021431
  2. ^ 2.0 2.1 2.2 2.3 Plosker GL. Acamprosate: A Review of Its Use in Alcohol Dependence. Drugs. July 2015, 75 (11): 1255–1268. PMID 26084940. S2CID 19119078. doi:10.1007/s40265-015-0423-9. 
  3. ^ Williams SH. . American Family Physician. November 2005, 72 (9): 1775–1780 [2006-11-29]. PMID 16300039. (原始内容存档于2007-09-29). 
  4. ^ 4.0 4.1 4.2 4.3 Malenka RC, Nestler EJ, Hyman SE, Holtzman DM. Chapter 16: Reinforcement and Addictive Disorders. Molecular Neuropharmacology: A Foundation for Clinical Neuroscience 3rd. New York: McGraw-Hill Medical. 2015. ISBN 9780071827706. It has been hypothesized that long-term ethanol exposure alters the expression or activity of specific GABAA receptor subunits in discrete brain regions. Regardless of the underlying mechanism, ethanol-induced decreases in GABAA receptor sensitivity are believed to contribute to ethanol tolerance, and also may mediate some aspects of physical dependence on ethanol. ... Detoxification from ethanol typically involves the administration of benzodiazepines such as chlordiazepoxide, which exhibit cross-dependence with ethanol at GABAA receptors (Chapters 5 and 15). A dose that will prevent the physical symptoms associated with withdrawal from ethanol, including tachycardia, hypertension, tremor, agitation, and seizures, is given and is slowly tapered. Benzodiazepines are used because they are less reinforcing than ethanol among alcoholics. Moreover, the tapered use of a benzodiazepine with a long half-life makes the emergence of withdrawal symptoms less likely than direct withdrawal from ethanol. ... Unfortunately, acamprosate is not adequately effective for most alcoholics. 
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  15. ^ 15.0 15.1 Saivin S, Hulot T, Chabac S, Potgieter A, Durbin P, Houin G. Clinical pharmacokinetics of acamprosate. Clinical Pharmacokinetics. November 1998, 35 (5): 331–345. PMID 9839087. S2CID 34047050. doi:10.2165/00003088-199835050-00001. 
  16. ^ Acamprosate: Biological activity. IUPHAR/BPS Guide to Pharmacology. International Union of Basic and Clinical Pharmacology. [2017-11-26]. Due to the complex nature of this drug's MMOA, and a paucity of well defined target affinity data, we do not map to a primary drug target in this instance. 
  17. ^ 17.0 17.1 17.2 17.3 Acamprosate: Summary. IUPHAR/BPS Guide to Pharmacology. International Union of Basic and Clinical Pharmacology. [2017-11-26]. Acamprosate is a NMDA glutamate receptor antagonist and a positive allosteric modulator of GABAA receptors.
    Marketed formulations contain acamprosate calcium
     
  18. ^ 18.0 18.1 18.2 18.3 18.4 18.5 Acamprosate. DrugBank. University of Alberta. 2017-11-19 [2017-11-26]. Acamprosate is thought to stabilize the chemical balance in the brain that would otherwise be disrupted by alcoholism, possibly by blocking glutaminergic N-methyl-D-aspartate receptors, while gamma-aminobutyric acid type A receptors are activated. ... The mechanism of action of acamprosate in the maintenance of alcohol abstinence is not completely understood. Chronic alcohol exposure is hypothesized to alter the normal balance between neuronal excitation and inhibition. in vitro and in vivo studies in animals have provided evidence to suggest acamprosate may interact with glutamate and GABA neurotransmitter systems centrally, and has led to the hypothesis that acamprosate restores this balance. It seems to inhibit NMDA receptors while activating GABA receptors. 
  19. ^ 19.0 19.1 19.2 Kalk NJ, Lingford-Hughes AR. The clinical pharmacology of acamprosate. British Journal of Clinical Pharmacology. February 2014, 77 (2): 315–323. PMC 4014018 . PMID 23278595. doi:10.1111/bcp.12070.  温哥华格式错误 (帮助)
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  27. ^ Mayer S, Harris BR, Gibson DA, Blanchard JA, Prendergast MA, Holley RC, Littleton J. Acamprosate, MK-801, and ifenprodil inhibit neurotoxicity and calcium entry induced by ethanol withdrawal in organotypic slice cultures from neonatal rat hippocampus. Alcoholism: Clinical and Experimental Research. October 2002, 26 (10): 1468–1478. PMID 12394279. doi:10.1097/00000374-200210000-00003. 
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  36. ^ Mann K, Kiefer F, Spanagel R, Littleton J. Acamprosate: recent findings and future research directions. Alcoholism: Clinical and Experimental Research. July 2008, 32 (7): 1105–1110. PMID 18540918. doi:10.1111/j.1530-0277.2008.00690.x. 

阿坎酸, 维基百科中的醫學内容仅供参考, 並不能視作專業意見, 如需獲取醫療幫助或意見, 请咨询专业人士, 詳見醫學聲明, 英語, acamprosate, 以campral及alglutol, 戒酒妥, 等品牌銷售, 是一種與治療酒精使用疾患, 酗酒, 諮詢合併使用的藥物, 臨床資料读音, 商品名, 英语, drug, nomenclature, campral, alglutol, 及其他其他名稱n, 乙酰基高牛磺酸, acetyl, homotaurine, usan, 懷孕分級b2, 给药途径口服給藥, a. 维基百科中的醫學内容仅供参考 並不能視作專業意見 如需獲取醫療幫助或意見 请咨询专业人士 詳見醫學聲明 阿坎酸 英語 Acamprosate 以Campral及Alglutol 戒酒妥 等品牌銷售 是一種與治療酒精使用疾患 酗酒 諮詢合併使用的藥物 1 2 阿坎酸臨床資料读音 e ˈ k ae m p r oʊ s eɪ t 商品名 英语 Drug nomenclature Campral Alglutol 及其他其他名稱N 乙酰基高牛磺酸 N Acetyl homotaurine 阿坎酸鈣 JAN JP 阿坎酸鈣 USAN US 懷孕分級B2 AU 给药途径口服給藥 1 ATC碼N07BB03 WHO 法律規範狀態法律規範澳 限医生处方 S4 英 处方药 only POM 美 处方药 only 藥物動力學數據生物利用度11 1 血漿蛋白結合率可忽略不計 1 药物代谢無 1 生物半衰期20 33小時 1 排泄途徑腎臟 1 识别信息IUPAC命名法 3 乙酰氨基丙烷 1 磺酸 3 Acetamidopropane 1 sulfonic acid CAS号77337 76 9 YPubChem CID155434IUPHAR BPS7106DrugBankDB00659 YChemSpider136929 YUNIIN4K14YGM3JKEGGD07058 YChEBICHEBI 51042 YChEMBLChEMBL1201293 NCompTox Dashboard 英语 CompTox Chemicals Dashboard EPA DTXSID3044259ECHA InfoCard100 071 495化学信息化学式C 5H 11N O 4S摩尔质量181 21 g mol 13D模型 JSmol 英语 JSmol 交互式图像SMILES Ca 2 O C NCCCS O O O C O S O O CCCNC O CInChI InChI 1S 2C5H11NO4S Ca c2 1 5 7 6 3 2 4 11 8 9 10 h2 2 4H2 1H3 H 6 7 H 8 9 10 q 2 p 2 YKey BUVGWDNTAWHSKI UHFFFAOYSA L Y阿坎酸被認為可穩定大腦的神經傳遞 英语 Neurotransmission 這些訊號傳遞會因酒精戒斷而受干擾 3 對大多數患者而言 單獨使用阿坎酸並非有效的治療方法 4 研究發現將阿坎酸與社會心理支持結合時效果會最佳 因為該藥物有助於減少飲酒數量 也有達到完全戒酒的效果 2 5 6 服用此藥物的嚴重副作用有過敏反應 心律不整以及低血壓或是高血壓 而較不嚴重的副作用有頭痛 失眠和勃起功能障礙 7 最常見的副作用是腹瀉 8 目前尚不清楚個體於懷孕期間使用是否對胎兒有安全的問題 9 10 此藥物被列入世界衛生組織基本藥物標準清單之中 11 目录 1 醫療用途 2 用藥禁忌 3 不良影響 4 藥理學 4 1 藥效學 4 2 藥物動力學 5 歷史 6 社會與文化 7 研究 8 參見醫療用途 编辑有酒精使用障礙的患者在接受諮詢 並同時服用阿坎酸時會非常有用 2 在三到十二個月的治療期間 完全不喝酒的人數和患者不喝酒的天數會增加 2 它在維持戒酒方面似乎與納曲酮 英语 naltrexone 一樣有效 12 然而納曲酮在減少酒精渴望 和酗酒方面效果稍好 13 同時在歐洲以外 而治療服務不太健全的地區 使用阿坎酸的效果往往會較差 14 用藥禁忌 编辑阿坎酸主要經由腎臟排除 對於腎功能中度受損的患者 肌酸酐清除率在30毫升 分鐘和50毫升 分鐘之間 建議將使用劑量降低 1 15 對藥物中阿坎酸鈣或其任何成分有強烈過敏反應的人也應禁止使用 15 不良影響 编辑此藥物在美國銷售的標籤上會列有服用會與自殺行為 重性憂鬱疾患和腎衰竭增加有關聯的警告 1 在臨床試驗中 對停止服用者導致的不良反應有腹瀉 噁心 憂鬱和焦慮 1 潛在的副作用包括頭痛 腹痛 背痛 肌肉痛 關節痛 胸痛 感染 類流感症狀 發冷 心悸 高血壓 昏厥 嘔吐 胃部不適 便秘 食慾增加 體重增加 水腫 嗜睡 性慾減退 勃起功能障礙 健忘 思考障礙 視力異常 味覺異常 顫抖 流鼻涕 咳嗽 呼吸困難 喉嚨痛 支氣管炎和皮疹 1 藥理學 编辑 nbsp 阿坎酸鈣分子結構藥效學 编辑 阿坎酸的藥效學很複雜且尚未被完全了解 16 17 18 然而它被認為可作為NMDA受體拮抗劑和 GABAA受體 的正變構調節劑 英语 allosteric modulator 17 18 此藥物與大多數其他藥物不同 其對這些受體產生的活性是間接性的 19 抑制GABAB系統被認為會間接導致GABAA受體增強 19 對NMDA受體的影響具有劑量依賴性 藥物似乎在低濃度下可增強受體活性 而在較高濃度時會有抑制作用 可抵消患者在發生酒精戒斷情況下NMDA受體過度激活狀態 20 該藥物還可增加服用者的牛磺酸內源性產量 20 乙醇和苯二氮平類藥物透過與GABAA受體結合 將具有抑制神經傳導作用的GABA功能增強 而對中樞神經系統發揮作用 即此藥物充當這些受體的正變構調節劑 17 4 對有酒精使用疾患的患者 發生耐受性的主要機制之一是GABAA受體下調 即這些受體對GABA變得不太敏感 4 而當個體停止飲酒後 正常的GABA生產就會導致戒斷症狀出現 4 而導致神經元過度興奮 阿坎酸的作用機制之一是透過正變構受體調節 增強GABAA受體的GABA訊號傳導 17 18 據稱此藥物能以一種新穎的方式打開氯離子通道 而不需要GABA作為輔助因子 因此比苯二氮平類藥物更不易產生依賴性 阿坎酸已成功用於控制因鼓膜張肌痙攣而導致的耳鳴 聽覺過敏 耳痛和飲酒期間的內耳壓力 21 此外 酒精也會抑制NMDA受體的活性 22 23 長期飲酒會導致這些受體過度生產 上調 突然戒酒後會導致這些大量生產的NMDA受體比正常情況更為活躍 而產生震顫性譫妄和興奮性毒性 英语 excitotoxicity 而導致神經元死亡的情況 24 戒酒會導致麩胺酸等興奮性神經傳導物質釋放激增 而過度激活NMDA受體 25 阿坎酸可減少麩氨酸的激增 26 該藥物還表現出可保護實驗室培養大鼠 細胞免受乙醇戒斷引起的興奮性毒性 27 以及受乙醇戒斷加上麩氨酸暴露的影響 28 此藥物也透過讓睡眠週期第3階段快速動眼期正常化來重建標準睡眠結構 而被認為是其藥理活性的一重要作用 20 藥物動力學 编辑 阿坎酸不會被人體代謝 18 口服阿坎酸的絕對生物利用度約為11 18 飲食時服用阿坎酸 其生物利用度會被降低 29 服用的阿坎酸會以原形經由腎臟排泄 18 阿坎酸受人體的吸收和消除非常緩慢 達到最大血藥濃度需6小時 達到生物半衰期需時超過30小時 19 歷史 编辑阿坎酸由默克集團子公司Lipha所開發 30 於1989年獲准在歐洲用於治療酒精依賴 31 藥業公司Forest Laboratories 英语 Forest Laboratories 於2001年10月取得藥物在美國的銷售權 30 32 該藥物於2004年7月獲得美國食品藥物管理局 FDA 核准用於醫療用途 33 阿坎酸的首個通用名藥物於2013年在美國上市 34 截至2015年 名為Confluence Pharmaceuticals的藥業公司在開發阿坎酸作為X染色體易裂症的治療法 此藥物在2013年被FDA授予孤兒藥地位 並於2014年也被歐洲藥品管理局 EMA 授予孤兒藥地位 35 社會與文化 编辑 阿坎酸 是此藥物的國際非專有藥名 INN 和英國核准藥名 英语 British Approved Name BAN 阿坎酸鈣 是美國通用名 英语 United States Adopted Name USAN 和日本接受名 英语 Japan Accepted Name JAN 它在技術上也稱為N 乙酰基高牛磺酸 N acetylhomotaurine 或乙醯高牛磺酸 acetylhomotaurinate 此藥物以Campral 1 及Alglutol等品牌銷售 研究 编辑此藥物除能明顯幫助患者戒酒之外 一些證據顯示其具有神經保護作用 即它可保護神經元 免受酒精戒斷以及可能的其他神經毒性原因 而造成的損傷和死亡 26 36 參見 编辑 1 00 1 01 1 02 1 03 1 04 1 05 1 06 1 07 1 08 1 09 1 10 1 11 Campral label PDF FDA January 2012 2017 11 27 For label updates see FDA index page for NDA 021431 2 0 2 1 2 2 2 3 Plosker GL Acamprosate A Review of Its Use in Alcohol Dependence Drugs July 2015 75 11 1255 1268 PMID 26084940 S2CID 19119078 doi 10 1007 s40265 015 0423 9 Williams SH Medications for treating alcohol dependence American Family Physician November 2005 72 9 1775 1780 2006 11 29 PMID 16300039 原始内容存档于2007 09 29 4 0 4 1 4 2 4 3 Malenka RC Nestler EJ Hyman SE Holtzman DM Chapter 16 Reinforcement and Addictive Disorders Molecular Neuropharmacology A Foundation for Clinical Neuroscience 3rd New York McGraw Hill Medical 2015 ISBN 9780071827706 It has been hypothesized that long term ethanol exposure alters the expression or activity of specific GABAA receptor subunits in discrete brain regions Regardless of the underlying mechanism ethanol induced decreases in GABAA receptor sensitivity are believed to contribute to ethanol tolerance and also may mediate some aspects of physical dependence on ethanol Detoxification from ethanol typically involves the administration of benzodiazepines such as chlordiazepoxide which exhibit cross dependence with ethanol at GABAA receptors Chapters 5 and 15 A dose that will prevent the physical symptoms associated with withdrawal from ethanol including tachycardia hypertension tremor agitation and seizures is given and is slowly tapered Benzodiazepines are used because they are less reinforcing than ethanol among alcoholics Moreover the tapered use of a benzodiazepine with a long half life makes the emergence of withdrawal symptoms less likely than direct withdrawal from ethanol Unfortunately acamprosate is not adequately effective for most alcoholics Mason BJ Treatment of alcohol dependent outpatients with acamprosate a clinical review The Journal of Clinical Psychiatry 2001 62 Suppl 20 42 48 PMID 11584875 Nutt DJ Rehm J Doing it by numbers a simple approach to reducing the harms of alcohol Journal of Psychopharmacology January 2014 28 1 3 7 PMID 24399337 S2CID 36860967 doi 10 1177 0269881113512038 Acamprosate drugs com 2005 03 25 2007 01 08 原始内容存档于2006 12 22 Wilde MI Wagstaff AJ Acamprosate A review of its pharmacology and clinical potential in the management of alcohol dependence after detoxification Drugs June 1997 53 6 1038 1053 PMID 9179530 S2CID 195691152 doi 10 2165 00003495 199753060 00008 Acamprosate Campral Use During Pregnancy Drugs com 英语 Haber P Lintzeris N Proude E Lopatko O Guidelines for the Treatment of Alcohol Problems PDF Australian Government Department of Health and Ageing 2023 02 20 World Health Organization The selection and use of essential medicines 2023 web annex A World Health Organization model list of essential medicines 23rd list 2023 Geneva World Health Organization 2023 hdl 10665 371090 nbsp WHO MHP HPS EML 2023 02 Kranzler HR Soyka M Diagnosis and Pharmacotherapy of Alcohol Use Disorder A Review JAMA August 2018 320 8 815 824 PMC 7391072 nbsp PMID 30167705 doi 10 1001 jama 2018 11406 Maisel NC Blodgett JC Wilbourne PL Humphreys K Finney JW Meta analysis of naltrexone and acamprosate for treating alcohol use disorders when are these medications most helpful Addiction February 2013 108 2 275 293 PMC 3970823 nbsp PMID 23075288 doi 10 1111 j 1360 0443 2012 04054 x Donoghue K Elzerbi C Saunders R Whittington C Pilling S Drummond C The efficacy of acamprosate and naltrexone in the treatment of alcohol dependence Europe versus the rest of the world a meta analysis Addiction June 2015 110 6 920 930 PMID 25664494 doi 10 1111 add 12875 15 0 15 1 Saivin S Hulot T Chabac S Potgieter A Durbin P Houin G Clinical pharmacokinetics of acamprosate Clinical Pharmacokinetics November 1998 35 5 331 345 PMID 9839087 S2CID 34047050 doi 10 2165 00003088 199835050 00001 Acamprosate Biological activity IUPHAR BPS Guide to Pharmacology International Union of Basic and Clinical Pharmacology 2017 11 26 Due to the complex nature of this drug s MMOA and a paucity of well defined target affinity data we do not map to a primary drug target in this instance 17 0 17 1 17 2 17 3 Acamprosate Summary IUPHAR BPS Guide to Pharmacology International Union of Basic and Clinical Pharmacology 2017 11 26 Acamprosate is a NMDA glutamate receptor antagonist and a positive allosteric modulator of GABAA receptors Marketed formulations contain acamprosate calcium 18 0 18 1 18 2 18 3 18 4 18 5 Acamprosate DrugBank University of Alberta 2017 11 19 2017 11 26 Acamprosate is thought to stabilize the chemical balance in the brain that would otherwise be disrupted by alcoholism possibly by blocking glutaminergic N methyl D aspartate receptors while gamma aminobutyric acid type A receptors are activated The mechanism of action of acamprosate in the maintenance of alcohol abstinence is not completely understood Chronic alcohol exposure is hypothesized to alter the normal balance between neuronal excitation and inhibition in vitro and in vivo studies in animals have provided evidence to suggest acamprosate may interact with glutamate and GABA neurotransmitter systems centrally and has led to the hypothesis that acamprosate restores this balance It seems to inhibit NMDA receptors while activating GABA receptors 19 0 19 1 19 2 Kalk NJ Lingford Hughes AR The clinical pharmacology of acamprosate British Journal of Clinical Pharmacology February 2014 77 2 315 323 PMC 4014018 nbsp PMID 23278595 doi 10 1111 bcp 12070 温哥华格式错误 帮助 20 0 20 1 20 2 Mason BJ Heyser CJ Acamprosate a prototypic neuromodulator in the treatment of alcohol dependence CNS amp Neurological Disorders Drug Targets March 2010 9 1 23 32 PMC 2853976 nbsp PMID 20201812 doi 10 2174 187152710790966641 Azevedo Andreia A Figueiredo Ricardo R Tinnitus treatment with acamprosate double blind study Brazilian Journal of Otorhinolaryngology Sep Oct 2005 71 5 2024 02 04 请检查 date 中的日期值 帮助 Malenka RC Nestler EJ Hyman SE Chapter 15 Reinforcement and Addictive Disorders Sydor A Brown RY 编 Molecular Neuropharmacology A Foundation for Clinical Neuroscience 2nd New York McGraw Hill Medical 2009 372 ISBN 9780071481274 Moykkynen T Korpi ER Acute effects of ethanol on glutamate receptors Basic amp Clinical Pharmacology amp Toxicology July 2012 111 1 4 13 PMID 22429661 doi 10 1111 j 1742 7843 2012 00879 x nbsp Tsai G Coyle JT The role of glutamatergic neurotransmission in the pathophysiology of alcoholism Annual Review of Medicine 1998 49 173 184 PMID 9509257 doi 10 1146 annurev med 49 1 173 Tsai GE Ragan P Chang R Chen S Linnoila VM Coyle JT Increased glutamatergic neurotransmission and oxidative stress after alcohol withdrawal The American Journal of Psychiatry June 1998 155 6 726 732 PMID 9619143 26 0 26 1 De Witte P Littleton J Parot P Koob G Neuroprotective and abstinence promoting effects of acamprosate elucidating the mechanism of action CNS Drugs 2005 19 6 517 537 PMID 15963001 S2CID 11563216 doi 10 2165 00023210 200519060 00004 Mayer S Harris BR Gibson DA Blanchard JA Prendergast MA Holley RC Littleton J Acamprosate MK 801 and ifenprodil inhibit neurotoxicity and calcium entry induced by ethanol withdrawal in organotypic slice cultures from neonatal rat hippocampus Alcoholism Clinical and Experimental Research October 2002 26 10 1468 1478 PMID 12394279 doi 10 1097 00000374 200210000 00003 al Qatari M Khan S Harris B Littleton J Acamprosate is neuroprotective against glutamate induced excitotoxicity when enhanced by ethanol withdrawal in neocortical cultures of fetal rat brain Alcoholism Clinical and Experimental Research September 2001 25 9 1276 1283 PMID 11584146 doi 10 1111 j 1530 0277 2001 tb02348 x Trevor AJ The Alcohols Katzung BG 编 Basic amp Clinical Pharmacology 14th New York 2017 ISBN 9781259641152 OCLC 1015240036 30 0 30 1 Berfield S A CEO and His Son Bloomberg Businessweek 2002 05 27 Yahn Stephanie L Watterson Lucas R Safety and Efficacy of Acamprosate for the Treatment of Alcohol Dependence Substance Abuse Research and Treatment 2013 01 31 7 2013 2023 4 02 04 doi 10 4137 SART S9345 请检查 access date 中的日期值 帮助 Press release Forest Laboratories Announces Agreement For Alcohol Addiction Treatment Forest Labs via Evaluate Group 2001 10 23 FDA Approves New Drug for Treatment of Alcoholism FDA Talk Paper Food and Drug Administration 2004 07 29 2009 08 15 原始内容存档于2008 01 17 Acamprosate generics DrugPatentWatch 2017 11 27 原始内容存档于2017 12 01 英语 Acamprosate Confluence Pharmaceuticals AdisInsight Springer Nature Switzerland AG 2017 11 27 英语 Mann K Kiefer F Spanagel R Littleton J Acamprosate recent findings and future research directions Alcoholism Clinical and Experimental Research July 2008 32 7 1105 1110 PMID 18540918 doi 10 1111 j 1530 0277 2008 00690 x 取自 https zh wikipedia org w index php title 阿坎酸 amp oldid 81466123, 维基百科,wiki,书籍,书籍,图书馆,

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