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Dr. Alexandra LaStella, PharmD, RPh
alexandra.lastella14@gmail.com
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Dr. Andrea Saenz, PharmD, RPh
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Dr. Katherine Gabriel, PharmD, RPh​
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Lastella A, Saenz A, Gabriel K. The case for lidocaine 7.5% in the management of localized pain: a biopharmaceutical review. J Scrip Pharm. Published online January 31, 2025. doi: 10.70390/Z7Q4NWJ1
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The Case for Transdermal Lidocaine 7.5% in the Management of Localized Pain: A Biopharmaceutical Review
Abstract
Transdermal anesthesia is a cornerstone of pain management, offering localized analgesia with minimal systemic effects. Lidocaine, a widely utilized local anesthetic, achieves pain relief primarily through sodium channel blockade, with emerging evidence highlighting additional mechanisms such as modulation of inflammatory mediators and nociceptive signaling. This review of the literature investigates Lidocaine 7.5% Cream as a potentially superior option compared to 4-5% lidocaine formulations and EMLA cream (lidocaine 2.5% and prilocaine 2.5%). With its higher concentration, Lidocaine 7.5% Cream may provide deeper, longer-lasting anesthesia while mitigating risks such as prilocaine-induced methemoglobinemia and delayed onset associated with EMLA Cream. Through the integration of published pharmacokinetic, pharmacodynamic, and clinical trial data we evaluate the suitability of lidocaine 7.5% (w/w) in the management of localized musculoskeletal and neuropathic pain. Our findings suggest lidocaine 7.5% cream offers improved efficacy and tolerability vs FDA approved alternatives; however, additional PK/PD studies and clinical trials must be conducted to further optimize dose and formula.