MET Institute of Pharmacy, Bhujbal Knowledge City, Reclamation, Bandra West, Mumbai, Maharashtra 400050, India.
SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Mithibai College Campus, Vaikunthlal Mehta Rd, Vile Parle West, Mumbai, Maharashtra 400056, India.
Curr Drug Targets. 2022;23(14):1290-1303. doi: 10.2174/1389450123666220819141827.
Inflammation is the body's mechanism to trigger the immune system, thereby preventing bacteria and viruses from manifesting their toxic effect. Inflammation plays a vital role in regulating inflammatory mediator levels to initiate the wound healing process depending on the nature of the stimuli. This process occurs due to chemical release from white blood cells by elevating blood flow to the site of action, leading to redness and increased body temperature. Currently, there are numerous Non-steroidal anti-inflammatory drugs (NSAIDs) available, but these drugs are reported with adverse effects such as gastric bleeding, progressive kidney damage, and increased risk of heart attacks when prolonged use. For such instances, alternative options need to be adopted. The introduction of voltage-gated ion channel blockers can be a substantial alternative to mask the side effects of these currently available drugs. Chronic inflammatory disorders such as rheumatoid and osteoarthritis, cancer and migraine, etc., can cause dreadful pain, which is often debilitating for the patient. The underlying mechanism for both acute and chronic inflammation involves various complex receptors, different types of cells, receptors, and proteins. The working of voltage-gated sodium and calcium channels is closely linked to both inflammatory and neuropathic pain. Certain drugs such as carbamazepine and gabapentin, which are ion channel blockers, have greater pharmacotherapeutic activity for sodium and calcium channel blockers for the treatment of chronic inflammatory pain states. This review intends to provide brief information on the mechanism of action, latest clinical trials, and applications of these blockers in treating inflammatory conditions.
炎症是身体触发免疫系统的机制，从而防止细菌和病毒表现出其毒性作用。炎症在调节炎症介质水平方面起着至关重要的作用，根据刺激的性质启动伤口愈合过程。这个过程是由于白细胞通过增加流向作用部位的血液释放化学物质而发生的，导致发红和体温升高。目前有许多非甾体抗炎药 (NSAIDs) 可用，但这些药物据报道有不良反应，如胃出血、进行性肾损伤和长期使用时心脏病发作的风险增加。在这种情况下，需要采用替代方案。电压门控离子通道阻滞剂的引入可以作为一种替代方案，以掩盖这些现有药物的副作用。慢性炎症性疾病，如类风湿性关节炎和骨关节炎、癌症和偏头痛等，会引起可怕的疼痛，这对患者来说常常是致残的。急性和慢性炎症的潜在机制涉及各种复杂的受体、不同类型的细胞、受体和蛋白质。电压门控钠和钙通道的工作与炎症和神经性疼痛密切相关。某些药物，如卡马西平和加巴喷丁，作为离子通道阻滞剂，对治疗慢性炎症性疼痛状态的钠和钙通道阻滞剂具有更大的药物治疗活性。本综述旨在提供这些阻滞剂在治疗炎症性疾病中的作用机制、最新临床试验和应用的简要信息。
