The therapeutic potential of Na⁺ and Ca²⁺ channel blockers in pain management

Abstract

Chronic pain affects a large percentage of the population, representing a socio–economic burden. Current treatments are characterised by suboptimal efficacy and/or side effects that limit their use. Among several approaches to treating chronic pain, voltage-sensitive Ca²⁺ and Na⁺ channels are promising targets. This review evaluates the preclinical evidence that supports the involvement of these targets, with specific attention to those subtypes that appear more strictly correlated with pain generation and sustainment, as well as those compounds that modulate the activity of Ca²⁺ and/or Na⁺ channels that are currently in clinical development for chronic pain conditions.

• cancer pain
• Cav2.2
• central pain
• chronic pain
• clinical trials
• inflammatory pain
• low back pain
• Nav1.3
• Nav1.8
• Nav1.9
• neuropathic pain
• N-type Ca2+ channels
• osteoarthritis
• peripheral diabetic neuropathy
• postherpetic neuralgia
• spinal cord injury
• tetrodotoxin-resistant channels
• tetrodotoxin-sensitive channels
• voltage-gated Ca2+ channels
• voltage-gated Na+ channels