普瑞巴林：修订间差异

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{{Drugbox
| image = Structure_of_pregabalin.svg

<!-- 化学数据 -->
| C = 8 | H = 17 | N = 1 | O = 2

<!-- 识别信息 -->
| IUPAC_name = (3<i>S</i>)S)-3-(氨基甲基)-5-甲基己酸
| CAS_number = 148553-50-8
| PubChem = 5486971
}}

'''普瑞巴林'''（'''Pregabalin'''），是一种治疗[[癫痫]]、[[神经痛]]、[[纤维肌痛]]、[[广泛性焦虑症]]<ref>{{cite journal|last1=Frampton|first1=JE|title=Pregabalin: a review of its use in adults with generalized anxiety disorder.|journal=CNS Drugs|date=September 2014|volume=28|issue=9|pages=835–54|pmid=25149863|doi=10.1007/s40263-014-0192-0}}</ref><ref name=AHFS2015>{{cite web|title=Pregabalin|url=http://www.drugs.com/monograph/pregabalin.html|publisher=The American Society of Health-System Pharmacists|accessdate=2015-10-23|archive-date=2020-08-09|archive-url=https://web.archive.org/web/20200809174922/https://www.drugs.com/monograph/pregabalin.html|dead-url=no}}</ref>的药物。
'''普瑞巴林'''（'''Pregabalin'''），是一种治疗[[癫痫]]、[[神经痛]]、[[纤维肌痛]]、[[广泛性焦虑症]]<ref>{{cite journal|last1=Frampton|first1=JE|title=Pregabalin: a review of its use in adults with generalized anxiety disorder.|journal=CNS Drugs|date=September 2014|volume=28|issue=9|pages=835–54|pmid=25149863|doi=10.1007/s40263-014-0192-0}}</ref><ref name=AHFS2015>{{cite web|title=Pregabalin|url=http://www.drugs.com/monograph/pregabalin.html|publisher=The American Society of Health-System Pharmacists|accessdate=2015-10-23|archive-date=2020-08-09|archive-url=https://web.archive.org/web/20200809174922/https://www.drugs.com/monograph/pregabalin.html|dead-url=no}}</ref>的药物。


== 药理学 ==
== 药理学 ==
普瑞巴林是[[神经递质]][[γ-氨基丁酸]]的衍生物，<ref name="pmid10189176">{{cite journal | vauthors = Bryans JS, Wustrow DJ | title = 3-substituted GABA analogs with central nervous system activity: a review | url = https://archive.org/details/sim_medicinal-research-reviews_1999-03_19_2/page/149 | journal = Medicinal Research Reviews | volume = 19 | issue = 2 | pages = 149–177 | date = March 1999 | pmid = 10189176 | doi = 10.1002/(SICI)1098-1128(199903)19:2<149::AID-MED3>3.0.CO;2-B | s2cid = 38496241 }}</ref> 也是一种强效的[[加巴喷丁]]类物质，但它并不与任何γ-氨基丁酸受体结合，而是通过抑制[[钙通道]]发挥作用。<ref name="Cal2016">{{cite journal | vauthors = Calandre EP, Rico-Villademoros F, Slim M | title = Alpha<sub>2</sub>delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use | journal = Expert Review of Neurotherapeutics | volume = 16 | issue = 11 | pages = 1263–1277 | date = November 2016 | pmid = 27345098 | doi = 10.1080/14737175.2016.1202764 | s2cid = 33200190 }}</ref><ref name="Uch2010">{{cite journal | vauthors = Uchitel OD, Di Guilmi MN, Urbano FJ, Gonzalez-Inchauspe C | title = Acute modulation of calcium currents and synaptic transmission by gabapentinoids | journal = Channels | volume = 4 | issue = 6 | pages = 490–496 | year = 2010 | pmid = 21150315 | doi = 10.4161/chan.4.6.12864 | title-link = doi | doi-access = free }}</ref>它是某些[[电压依赖性钙通道]]（VDCCs）的辅助[[CACNA2D|α<sub>2</sub>δ]]亚基位点的[[配體_(生物化學)|配体]]，从而作为含α<sub>2</sub>δ亚基的电压依赖性钙通道的抑制剂。<ref name="Cal2016" />
普瑞巴林是[[神经递质]][[γ-氨基丁酸]]（GABA）的衍生物，<ref name="pmid10189176">{{cite journal | vauthors = Bryans JS, Wustrow DJ | title = 3-substituted GABA analogs with central nervous system activity: a review | url = https://archive.org/details/sim_medicinal-research-reviews_1999-03_19_2/page/149 | journal = Medicinal Research Reviews | volume = 19 | issue = 2 | pages = 149–177 | date = March 1999 | pmid = 10189176 | doi = 10.1002/(SICI)1098-1128(199903)19:2<149::AID-MED3>3.0.CO;2-B | s2cid = 38496241 }}</ref> 也是一种强效的[[加巴喷丁]]类物质。虽然它是[[GABA]]的衍生物，但它并不与任何GABA受体结合，而是通过抑制[[钙通道]]发挥作用。<ref name="Cal2016">{{cite journal | vauthors = Calandre EP, Rico-Villademoros F, Slim M | title = Alpha<sub>2</sub>delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use | journal = Expert Review of Neurotherapeutics | volume = 16 | issue = 11 | pages = 1263–1277 | date = November 2016 | pmid = 27345098 | doi = 10.1080/14737175.2016.1202764 | s2cid = 33200190 }}</ref><ref name="Uch2010">{{cite journal | vauthors = Uchitel OD, Di Guilmi MN, Urbano FJ, Gonzalez-Inchauspe C | title = Acute modulation of calcium currents and synaptic transmission by gabapentinoids | journal = Channels | volume = 4 | issue = 6 | pages = 490–496 | year = 2010 | pmid = 21150315 | doi = 10.4161/chan.4.6.12864 | title-link = doi | doi-access = free }}</ref> 它是某些[[电压依赖性钙通道]]（VDCCs）的辅助[[CACNA2D|α<sub>2</sub>δ]]亚基位点的[[配体_(生物化学)|配体]]，从而作为含α<sub>2</sub>δ亚基的电压依赖性钙通道的抑制剂。<ref name="Cal2016" />
<ref name="pmid16376147">{{cite journal | vauthors = Sills GJ | title = The mechanisms of action of gabapentin and pregabalin | journal = Current Opinion in Pharmacology | volume = 6 | issue = 1 | pages = 108–113 | date = February 2006 | pmid = 16376147 | doi = 10.1016/j.coph.2005.11.003 }}</ref>它与[[CACNA2D1|α<sub>2</sub>δ1]]以及[[CACNA2D2|α<sub>2</sub>δ2]]这两个亚基结合，并在这两个位点上表现出了相似的[[亲和力]]，因此普瑞巴林缺乏α<sub>2</sub>δ亚基的选择性，<ref name="Cal2016" />但具有电压依赖性钙通道的α<sub>2</sub>δ亚基选择性。<ref name="pmid16376147" />
<ref name="pmid16376147">{{cite journal | vauthors = Sills GJ | title = The mechanisms of action of gabapentin and pregabalin | journal = Current Opinion in Pharmacology | volume = 6 | issue = 1 | pages = 108–113 | date = February 2006 | pmid = 16376147 | doi = 10.1016/j.coph.2005.11.003 }}</ref>它与[[CACNA2D1|α<sub>2</sub>δ1]]以及[[CACNA2D2|α<sub>2</sub>δ2]]这两个亚基结合，并在这两个位点上表现出了相似的[[亲和力]]，因此普瑞巴林缺乏α<sub>2</sub>δ亚基的选择性，<ref name="Cal2016" />但具有电压依赖性钙通道的α<sub>2</sub>δ亚基选择性。<ref name="pmid16376147" />
<ref name="BenzonRathmell2013">{{Cite book | vauthors = Benzon HM, Rathmell JP, Wu CL, Turk DC, Argoff CE, Hurley RW |url=https://books.google.com/books?id=kfcDAQAAQBAJ&pg=PA1006 |title=Practical Management of Pain |date=September 11, 2013 |publisher=Elsevier Health Sciences |isbn=978-0-323-17080-2 |page=1006}}</ref> 虽然普瑞巴林不与任何γ-氨基丁酸受体结合，也不会转换为γ-氨基丁酸或其他γ-氨基丁酸受体激动剂，也不直接调节γ-氨基丁酸的[[转运]]或代谢，<ref name="Uch2010" /><ref name="pmid16376147" />但它会增加[[L-谷氨酸脱羧酶]]（GAD）在大脑中的[[基因表达|表达]]，<ref>{{Cite book|veditors=Lin GQ, You QD, Cheng JF|url=https://books.google.com/books?id=Zgx13oMZaYUC&pg=PA88|title=Chiral Drugs: Chemistry and Biological Action|date=August 8, 2011|publisher=John Wiley & Sons|isbn=9781118075630|page=88|via=Google Books|access-date=August 17, 2016|archive-date=April 25, 2022|archive-url=https://web.archive.org/web/20220425105353/https://books.google.com/books?id=Zgx13oMZaYUC&pg=PA88|url-status=live}}</ref><ref>{{cite journal | vauthors = Li Z, Taylor CP, Weber M, Piechan J, Prior F, Bian F, Cui M, Hoffman D, Donevan S | display-authors = 6 | title = Pregabalin is a potent and selective ligand for α(2)δ-1 and α(2)δ-2 calcium channel subunits | journal = European Journal of Pharmacology | volume = 667 | issue = 1–3 | pages = 80–90 | date = September 2011 | pmid = 21651903 | doi = 10.1016/j.ejphar.2011.05.054 | url = https://scholar.google.com/scholar?hl=en&as_sdt=0%2C5&q=Pregabalin+is+a+potent+and+selective+ligand+for+alpha%282%29delta-1+and+alpha%282%29delta-2+calcium+channel+subunits&btnG= | access-date = October 20, 2020 | url-status = live | archive-url = https://web.archive.org/web/20201021030744/https://scholar.google.com/scholar?hl=en&as_sdt=0,5&q=Pregabalin+is+a+potent+and+selective+ligand+for+alpha(2)delta-1+and+alpha(2)delta-2+calcium+channel+subunits&btnG= | archive-date = October 21, 2020 }}</ref>
<ref name="BenzonRathmell2013">{{Cite book | vauthors = Benzon HM, Rathmell JP, Wu CL, Turk DC, Argoff CE, Hurley RW |url=https://books.google.com/books?id=kfcDAQAAQBAJ&pg=PA1006 |title=Practical Management of Pain |date=September 11, 2013 |publisher=Elsevier Health Sciences |isbn=978-0-323-17080-2 |page=1006}}</ref> 虽然普瑞巴林不直接充当GABA的功能，也不调节GABA的[[转运]]或代谢，<ref name="Uch2010" /><ref name="pmid16376147" />但它会增加[[L-谷氨酸脱羧酶]]（GAD）在大脑中的[[基因表达|表达]]，<ref>{{Cite book|veditors=Lin GQ, You QD, Cheng JF|url=https://books.google.com/books?id=Zgx13oMZaYUC&pg=PA88|title=Chiral Drugs: Chemistry and Biological Action|date=August 8, 2011|publisher=John Wiley & Sons|isbn=9781118075630|page=88|via=Google Books|access-date=August 17, 2016|archive-date=April 25, 2022|archive-url=https://web.archive.org/web/20220425105353/https://books.google.com/books?id=Zgx13oMZaYUC&pg=PA88|url-status=live}}</ref><ref>{{cite journal | vauthors = Li Z, Taylor CP, Weber M, Piechan J, Prior F, Bian F, Cui M, Hoffman D, Donevan S | display-authors = 6 | title = Pregabalin is a potent and selective ligand for α(2)δ-1 and α(2)δ-2 calcium channel subunits | journal = European Journal of Pharmacology | volume = 667 | issue = 1–3 | pages = 80–90 | date = September 2011 | pmid = 21651903 | doi = 10.1016/j.ejphar.2011.05.054 | url = https://scholar.google.com/scholar?hl=en&as_sdt=0%2C5&q=Pregabalin+is+a+potent+and+selective+ligand+for+alpha%282%29delta-1+and+alpha%282%29delta-2+calcium+channel+subunits&btnG= | access-date = October 20, 2020 | url-status = live | archive-url = https://web.archive.org/web/20201021030744/https://scholar.google.com/scholar?hl=en&as_sdt=0,5&q=Pregabalin+is+a+potent+and+selective+ligand+for+alpha(2)delta-1+and+alpha(2)delta-2+calcium+channel+subunits&btnG= | archive-date = October 21, 2020 }}</ref>
<ref>{{Cite book | vauthors = Sze PY |chapter=L-Glutamate Decarboxylase |title=GABA—Biochemistry and CNS Functions |year=1979 |isbn=978-1-4899-5201-1 |series=Advances in Experimental Medicine and Biology |volume=123 |pages=59–78 |doi=10.1007/978-1-4899-5199-1_4 |pmid=390996}}</ref> 而此酶是用于合成γ-氨基丁酸的酶，因此可能由于大脑内γ氨基丁酸水平升高造成一些γ-氨基丁酸能的作用。但目前没有证据可以说明普瑞巴林的作用是除了抑制含α<sub>2</sub>δ亚基的电压依赖性钙通道介导的。<ref name="pmid16376147" />
<ref>{{Cite book | vauthors = Sze PY |chapter=L-Glutamate Decarboxylase |title=GABA—Biochemistry and CNS Functions |year=1979 |isbn=978-1-4899-5201-1 |series=Advances in Experimental Medicine and Biology |volume=123 |pages=59–78 |doi=10.1007/978-1-4899-5199-1_4 |pmid=390996}}</ref>因此可能导致部分GABA水平升高。但目前没有证据可以说明普瑞巴林的作用是除了抑制含α<sub>2</sub>δ亚基的电压依赖性钙通道介导的。<ref name="pmid16376147" />
<ref name="pmid23642658">{{cite journal | vauthors = Stahl SM, Porreca F, Taylor CP, Cheung R, Thorpe AJ, Clair A | title = The diverse therapeutic actions of pregabalin: is a single mechanism responsible for several pharmacological activities? | journal = Trends in Pharmacological Sciences | volume = 34 | issue = 6 | pages = 332–339 | date = June 2013 | pmid = 23642658 | doi = 10.1016/j.tips.2013.04.001 }}</ref> 因此，普瑞巴林对其的抑制作用似乎是它[[抗惊厥]]、[[镇痛]]和[[抗焦虑]]效果的原因。<ref name="pmid16376147" /><ref name="pmid23642658" />
<ref name="pmid23642658">{{cite journal | vauthors = Stahl SM, Porreca F, Taylor CP, Cheung R, Thorpe AJ, Clair A | title = The diverse therapeutic actions of pregabalin: is a single mechanism responsible for several pharmacological activities? | journal = Trends in Pharmacological Sciences | volume = 34 | issue = 6 | pages = 332–339 | date = June 2013 | pmid = 23642658 | doi = 10.1016/j.tips.2013.04.001 }}</ref> 因此，普瑞巴林对其的抑制作用似乎是它[[抗惊厥]]、[[镇痛]]和[[抗焦虑]]效果的原因。<ref name="pmid16376147" /><ref name="pmid23642658" />


2024年10月14日 (一) 08:30的最新版本

普瑞巴林
化学数据
化学式C8H17NO2
摩尔质量159.23 g·mol−1
识别信息
IUPAC名称(3S)S)-3-(氨基甲基)-5-甲基己酸
CAS号
PubChem CID

普瑞巴林（Pregabalin），是一种治疗癫痫、神经痛、纤维肌痛、广泛性焦虑症[1][2]的药物。

药理学

普瑞巴林是神经递质γ-氨基丁酸（GABA）的衍生物，[3] 也是一种强效的加巴喷丁类物质。虽然它是GABA的衍生物，但它并不与任何GABA受体结合，而是通过抑制钙通道发挥作用。[4][5] 它是某些电压依赖性钙通道（VDCCs）的辅助α2δ亚基位点的配体，从而作为含α2δ亚基的电压依赖性钙通道的抑制剂。[4] [6]它与α2δ1以及α2δ2这两个亚基结合，并在这两个位点上表现出了相似的亲和力，因此普瑞巴林缺乏α2δ亚基的选择性，[4]但具有电压依赖性钙通道的α2δ亚基选择性。[6] [7] 虽然普瑞巴林不直接充当GABA的功能，也不调节GABA的转运或代谢，[5][6]但它会增加L-谷氨酸脱羧酶（GAD）在大脑中的表达，[8][9] [10]因此可能导致部分GABA水平升高。但目前没有证据可以说明普瑞巴林的作用是除了抑制含α2δ亚基的电压依赖性钙通道介导的。[6] [11] 因此，普瑞巴林对其的抑制作用似乎是它抗惊厥、镇痛和抗焦虑效果的原因。[6][11]


在一项研究中发现，普瑞巴林对含α2δ亚基的电压依赖性钙通具有比加巴喷丁高6倍的亲和力，[12][13]而在另一项研究中发现，普瑞巴林和加巴喷丁对人类重组α2δ1亚基具有差不多的亲和力（Ki分别为32 nM和40 nM）。[14]在任何情况下，普瑞巴林作为镇痛药的效力是加巴喷丁的2~4倍，[3][15]在动物身上作为抗惊厥药时的效力似乎是加巴喷丁的3~10倍。[3][15]

滥用

普瑞巴林因其中枢抑制的特性时常被滥用，通常会使用至少一次300mg或更高的剂量。普瑞巴林在过量时可能具有成瘾性和戒断反应。

參考文献

  1. ↑ Frampton, JE (September 2014). "Pregabalin: a review of its use in adults with generalized anxiety disorder". CNS Drugs. 28 (9): 835–54. doi:10.1007/s40263-014-0192-0. PMID 25149863.
  2. ↑ "Pregabalin". The American Society of Health-System Pharmacists. Archived from the original on 2020-08-09. Retrieved 2015-10-23. {{cite web}}: Unknown parameter |dead-url= ignored (|url-status= suggested) (help)
  3. ↑ 3.0 3.1 3.2 Bryans JS, Wustrow DJ (March 1999). "3-substituted GABA analogs with central nervous system activity: a review". Medicinal Research Reviews. 19 (2): 149–177. doi:10.1002/(SICI)1098-1128(199903)19:2<149::AID-MED3>3.0.CO;2-B. PMID 10189176. S2CID 38496241.
  4. ↑ 4.0 4.1 4.2 Calandre EP, Rico-Villademoros F, Slim M (November 2016). "Alpha2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use". Expert Review of Neurotherapeutics. 16 (11): 1263–1277. doi:10.1080/14737175.2016.1202764. PMID 27345098. S2CID 33200190.
  5. ↑ 5.0 5.1 Uchitel OD, Di Guilmi MN, Urbano FJ, Gonzalez-Inchauspe C (2010). "Acute modulation of calcium currents and synaptic transmission by gabapentinoids". Channels. 4 (6): 490–496. doi:10.4161/chan.4.6.12864. PMID 21150315.
  6. ↑ 6.0 6.1 6.2 6.3 6.4 Sills GJ (February 2006). "The mechanisms of action of gabapentin and pregabalin". Current Opinion in Pharmacology. 6 (1): 108–113. doi:10.1016/j.coph.2005.11.003. PMID 16376147.
  7. ↑ Benzon HM, Rathmell JP, Wu CL, Turk DC, Argoff CE, Hurley RW (September 11, 2013). Practical Management of Pain. Elsevier Health Sciences. p. 1006. ISBN 978-0-323-17080-2.
  8. ↑ Lin GQ, You QD, Cheng JF, eds. (August 8, 2011). Chiral Drugs: Chemistry and Biological Action. John Wiley & Sons. p. 88. ISBN 9781118075630. Archived from the original on April 25, 2022. Retrieved August 17, 2016 – via Google Books.
  9. ↑ Li Z, Taylor CP, Weber M, Piechan J, Prior F, Bian F, et al. (September 2011). "Pregabalin is a potent and selective ligand for α(2)δ-1 and α(2)δ-2 calcium channel subunits". European Journal of Pharmacology. 667 (1–3): 80–90. doi:10.1016/j.ejphar.2011.05.054. PMID 21651903. Archived from the original on October 21, 2020. Retrieved October 20, 2020.
  10. ↑ Sze PY (1979). "L-Glutamate Decarboxylase". GABA—Biochemistry and CNS Functions. Advances in Experimental Medicine and Biology. Vol. 123. pp. 59–78. doi:10.1007/978-1-4899-5199-1_4. ISBN 978-1-4899-5201-1. PMID 390996.
  11. ↑ 11.0 11.1 Stahl SM, Porreca F, Taylor CP, Cheung R, Thorpe AJ, Clair A (June 2013). "The diverse therapeutic actions of pregabalin: is a single mechanism responsible for several pharmacological activities?". Trends in Pharmacological Sciences. 34 (6): 332–339. doi:10.1016/j.tips.2013.04.001. PMID 23642658.
  12. ↑ Baidya DK, Agarwal A, Khanna P, Arora MK (July 2011). "Pregabalin in acute and chronic pain". Journal of Anaesthesiology Clinical Pharmacology. 27 (3): 307–314. doi:10.4103/0970-9185.83672. PMC 3161452. PMID 21897498.
  13. ↑ McMahon SB (2013). Wall and Melzack's textbook of pain (6th ed.). Philadelphia, PA: Elsevier/Saunders. p. 515. ISBN 9780702040597.
  14. ↑ Taylor CP, Angelotti T, Fauman E (February 2007). "Pharmacology and mechanism of action of pregabalin: the calcium channel alpha2-delta (alpha2-delta) subunit as a target for antiepileptic drug discovery". Epilepsy Research. 73 (2): 137–150. doi:10.1016/j.eplepsyres.2006.09.008. PMID 17126531. S2CID 54254671. Archived from the original on October 23, 2020. Retrieved October 19, 2020.
  15. ↑ 15.0 15.1 Lauria-Horner BA, Pohl RB (April 2003). "Pregabalin: a new anxiolytic". Expert Opinion on Investigational Drugs. 12 (4): 663–672. doi:10.1517/13543784.12.4.663. PMID 12665421. S2CID 36137322.
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