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

Abstract

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.

Keywords

• Mirogabalin
• Neuropathic pain
• Diabetic neuropathy
• Post-herpetic neuralgia
• Chronic pain