Safety, tolerability, and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain—a topical review

Abstract Gabapentin and pregabalin, known as gabapentinoids, have been used effectively as a monotherapy or in combination with other agents for managing chronic neuropathic pain due to various etiologies. These drugs act via α2δ-1 and α2δ-2 subunits of voltage-gated calcium channels (VGCCs) non-sel...

Full description

Bibliographic Details
Main Authors: Abhijit Nair, Subodh Kamtikar, Suresh Seelam
Format: Article
Language:English
Published: SpringerOpen 2021-10-01
Series:Ain Shams Journal of Anesthesiology
Subjects:
Online Access:https://doi.org/10.1186/s42077-021-00183-1
_version_ 1819148647379501056
author Abhijit Nair
Subodh Kamtikar
Suresh Seelam
author_facet Abhijit Nair
Subodh Kamtikar
Suresh Seelam
author_sort Abhijit Nair
collection DOAJ
description Abstract Gabapentin and pregabalin, known as gabapentinoids, have been used effectively as a monotherapy or in combination with other agents for managing chronic neuropathic pain due to various etiologies. These drugs act via α2δ-1 and α2δ-2 subunits of voltage-gated calcium channels (VGCCs) non-selectively. Due to its non-selective action, a certain group of patients reports central nervous system adverse effects like dizziness, drowsiness, somnolence, and cerebellar ataxia. Mirogabalin besylate is an orally administered next-generation gabapentinoid approved for use in diabetic neuropathy and post-herpetic neuralgia. It binds selectively and with greater affinity to the α2δ-1 and α2δ-2 subunits of human VGCCs and thus has lesser central nervous system adverse events making it more tolerable. We reviewed all articles in various categories, published in reputed databases since 2014 where mirogabalin was used to treat chronic neuropathic pain. Case series and open-label studies have demonstrated the safety and efficacy of mirogabalin in cancer pain and lumbar spine disease. Pharmacokinetic/pharmacodynamic studies have cautioned using full dose in patients with renal/hepatic impairment and along with drugs that could lead to adverse effects like sedatives and opioids. Dose up to 30 mg/day when administered as a twice-daily divided dose has been tolerated quite well with adequate pain relief in diabetic neuropathy and post-herpetic neuralgia. Mirogabalin appears to be a safe gabapentinoid in diabetic neuropathy and post-herpetic neuralgia. Further studies need to be conducted to explore the role of mirogabalin in cancer pain, postoperative pain, and neuropathic pain due to various other etiologies.
first_indexed 2024-12-22T13:49:02Z
format Article
id doaj.art-d53389fc90834c318ea9cc0c48a408d4
institution Directory Open Access Journal
issn 2090-925X
language English
last_indexed 2024-12-22T13:49:02Z
publishDate 2021-10-01
publisher SpringerOpen
record_format Article
series Ain Shams Journal of Anesthesiology
spelling doaj.art-d53389fc90834c318ea9cc0c48a408d42022-12-21T18:23:43ZengSpringerOpenAin Shams Journal of Anesthesiology2090-925X2021-10-011311710.1186/s42077-021-00183-1Safety, tolerability, and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain—a topical reviewAbhijit Nair0Subodh Kamtikar1Suresh Seelam2Department of Anaesthesiology, Ibra Hospital, North Sharqiya Governorate, Ministry of Health-OmanDepartment of Anesthesiology, Bidar Institute of Medical SciencesDepartment of Anesthesiology, Royal HospitalAbstract Gabapentin and pregabalin, known as gabapentinoids, have been used effectively as a monotherapy or in combination with other agents for managing chronic neuropathic pain due to various etiologies. These drugs act via α2δ-1 and α2δ-2 subunits of voltage-gated calcium channels (VGCCs) non-selectively. Due to its non-selective action, a certain group of patients reports central nervous system adverse effects like dizziness, drowsiness, somnolence, and cerebellar ataxia. Mirogabalin besylate is an orally administered next-generation gabapentinoid approved for use in diabetic neuropathy and post-herpetic neuralgia. It binds selectively and with greater affinity to the α2δ-1 and α2δ-2 subunits of human VGCCs and thus has lesser central nervous system adverse events making it more tolerable. We reviewed all articles in various categories, published in reputed databases since 2014 where mirogabalin was used to treat chronic neuropathic pain. Case series and open-label studies have demonstrated the safety and efficacy of mirogabalin in cancer pain and lumbar spine disease. Pharmacokinetic/pharmacodynamic studies have cautioned using full dose in patients with renal/hepatic impairment and along with drugs that could lead to adverse effects like sedatives and opioids. Dose up to 30 mg/day when administered as a twice-daily divided dose has been tolerated quite well with adequate pain relief in diabetic neuropathy and post-herpetic neuralgia. Mirogabalin appears to be a safe gabapentinoid in diabetic neuropathy and post-herpetic neuralgia. Further studies need to be conducted to explore the role of mirogabalin in cancer pain, postoperative pain, and neuropathic pain due to various other etiologies.https://doi.org/10.1186/s42077-021-00183-1MirogabalinNeuropathic painDiabetic neuropathyPost-herpetic neuralgiaChronic pain
spellingShingle Abhijit Nair
Subodh Kamtikar
Suresh Seelam
Safety, tolerability, and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain—a topical review
Ain Shams Journal of Anesthesiology
Mirogabalin
Neuropathic pain
Diabetic neuropathy
Post-herpetic neuralgia
Chronic pain
title Safety, tolerability, and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain—a topical review
title_full Safety, tolerability, and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain—a topical review
title_fullStr Safety, tolerability, and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain—a topical review
title_full_unstemmed Safety, tolerability, and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain—a topical review
title_short Safety, tolerability, and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain—a topical review
title_sort safety tolerability and efficacy of a selective gabapentinoid mirogabalin in neuropathic pain a topical review
topic Mirogabalin
Neuropathic pain
Diabetic neuropathy
Post-herpetic neuralgia
Chronic pain
url https://doi.org/10.1186/s42077-021-00183-1
work_keys_str_mv AT abhijitnair safetytolerabilityandefficacyofaselectivegabapentinoidmirogabalininneuropathicpainatopicalreview
AT subodhkamtikar safetytolerabilityandefficacyofaselectivegabapentinoidmirogabalininneuropathicpainatopicalreview
AT sureshseelam safetytolerabilityandefficacyofaselectivegabapentinoidmirogabalininneuropathicpainatopicalreview