The Korean Journal of Pain

  • 제34권1호
  • /
  • Pages.4-18
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  • 2021
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  • 2005-9159(pISSN)
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  • 2093-0569(eISSN)
대한통증학회 (The Korean Pain Society)
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Mirogabalin: could it be the next generation gabapentin or pregabalin?

  • Kim, Jae-Yeon (Department of Anesthesia and Pain Medicine, Pusan National University School of Medicine) ;
  • Abdi, Salahadin (Department of Pain Medicine, The University of Texas MD Anderson Cancer Center) ;
  • Huh, Billy (Department of Pain Medicine, The University of Texas MD Anderson Cancer Center) ;
  • Kim, Kyung-Hoon (Department of Anesthesia and Pain Medicine, Pusan National University School of Medicine)
  • 투고 : 2020.11.30
  • 심사 : 2020.12.22
  • 발행 : 2021.01.01
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초록

Except for carbamazepine for trigeminal neuralgia, gabapentinoid anticonvulsants have been the standard for the treatment of neuropathic pain. Pregabalin, which followed gabapentin, was developed with the benefit of rapid peak blood concentration and better bioavailability. Mirogabalin besylate (DS-5565, Tarlige®) shows greater sustained analgesia due to a high affinity to, and slow dissociation from, the α2δ-1 subunits in the dorsal root ganglion (DRG). Additionally, it produces a lower level of central nervous system-specific adverse drug reactions (ADRs), due to a low affinity to, and rapid dissociation from, the α2δ-2 subunits in the cerebellum. Maximum plasma concentration is achieved in less than 1 hour, compared to 1 hour for pregabalin and 3 hours for gabapentin. The plasma protein binding is relatively low, at less than 25%. As with all gabapentinoids, it is also largely excreted via the kidneys in an unchanged form, and so the administration dose should also be adjusted according to renal function. The equianalgesic daily dose for 30 mg of mirogabalin is 600 mg of pregabalin and over 1,200 mg of gabapentin. The initial adult dose starts at 5 mg, given orally twice a day, and is gradually increased by 5 mg at an interval of at least a week, to 15 mg. In conclusion, mirogabalin is anticipated to be a novel, safe gabapentinoid anticonvulsant with a greater therapeutic effect for neuropathic pain in the DRG and lower ADRs in the cerebellum.

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과제정보

This study was supported by a 2-year research grant from Pusan National University (2019-2021).

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피인용 문헌

  1. Mirogabalin-A Novel Selective Ligand for the α2δ Calcium Channel Subunit vol.14, pp.2, 2021, https://doi.org/10.3390/ph14020112