Benzydamine HCl is a topical non-steroidal anti-inflammatory drug with anti-inflammatory, analgesic, antipyretic, and local anesthetic activities[1-2]. Benzydamine HCl alleviates inflammatory responses by inhibiting prostaglandin synthesis, stabilizing cell membranes, and suppressing the production of pro-inflammatory cytokines. Benzydamine HCl is used in studies related to oropharyngeal inflammation, postoperative pain, and radiotherapy-induced oral mucositis[3-4].
In vitro, Benzydamine HCl (6–50μM) was co-treated with LPS for 24h in human peripheral blood mononuclear cells (PBMCs) or for 6–24h in mouse peritoneal macrophages. Benzydamine HCl significantly inhibited TNF-α production and mildly suppressed IL-1β production[5]. Benzydamine HCl (1.0mg/mL) was incubated with Pseudomonas aeruginosa (PA) for 24h. Benzydamine HCl significantly inhibited the proliferation of PA[6].
In vivo, Benzydamine HCl (10mg/kg; administered twice on day 0 and day 2) was locally injected into the calvaria of C57BL/6 mice in an LPS-induced inflammatory bone destruction model, or administered intraperitoneally (six times per week for three weeks) in an ovariectomy (OVX)-induced postmenopausal osteoporosis model in C57BL/6 mice. Benzydamine HCl significantly reduced inflammation-induced calvarial bone destruction and osteoclast number, and reversed OVX-induced decreases in bone mineral density, bone volume, and other bone loss parameters[7]. Benzydamine HCl (10 or 20mg/kg; single injection) was subcutaneously injected either concurrently with or after (30min or 4h) LPS administration in an endotoxemia model in female Balb/c mice. Benzydamine HCl significantly increased the median lethal dose of LPS and, when given 30min or 4h after LPS injection, significantly decreased LPS-induced mortality in mice[8].
References:
[1] Zhang Y, Yang L, Gan Y, et al. Benzydamine attenuates microglia-mediated neuroinflammation and ischemic brain injury by targeting cathepsin s. Int Immunopharmacol. 2025 Jan 27;146:113824.
[2] Modéer T, Yucel-Lindberg T. Benzydamine reduces prostaglandin production in human gingival fibroblasts challenged with interleukin-1 beta or tumor necrosis factor alpha. Acta Odontol Scand. 1999 Feb;57(1):40-5.
[3] Zhou Y, He X, Jiang Y, et al. Repurposed benzydamine targeting CDK2 suppresses the growth of esophageal squamous cell carcinoma. Front Med. 2023 Apr;17(2):290-303.
[4] Yamazaki-Nishioka M, Shimizu M, Suemizu H, et al. Human plasma metabolic profiles of benzydamine, a flavin-containing monooxygenase probe substrate, simulated with pharmacokinetic data from control and humanized-liver mice. Xenobiotica. 2018 Feb;48(2):117-123.
[5] Sironi M, Pozzi P, Polentarutti N, et al. Inhibition of inflammatory cytokine production and protection against endotoxin toxicity by benzydamine. Cytokine. 1996 Sep;8(9):710-6.
[6] Fanaki NH, el-Nakeeb MA. Antimicrobial activity of benzydamine, a non-steroid anti-inflammatory agent. J Chemother. 1992 Dec;4(6):347-52.
[7] Son HS, Lee J, Lee HI, et al. Benzydamine inhibits osteoclast differentiation and bone resorption via down-regulation of interleukin-1 β expression. Acta Pharm Sin B. 2020 Mar;10(3):462-474.
[8] Guglielmotti A, Aquilini L, Rosignoli MT, et al. Benzydamine protection in a mouse model of endotoxemia. Inflamm Res. 1997 Sep;46(9):332-5.
Benzydamine HCl是一种局部非甾体抗炎药，具有抗炎、镇痛、解热和局部麻醉活性[1-2]。Benzydamine HCl可通过抑制前列腺素合成、稳定细胞膜并抑制促炎细胞因子产生来减轻炎症反应。Benzydamine HCl可用于口腔咽喉炎症、术后疼痛以及放疗引起的口腔黏膜炎的相关研究[3-4]。
在体外，Benzydamine HCl（6-50μM）与LPS共同处理人外周血单个核细胞（PBMC）24小时，或处理小鼠腹腔巨噬细胞6-24小时。Benzydamine HCl显著抑制TNF-α的产生，对IL-1β的产生有轻度抑制[5]。Benzydamine HCl（1.0mg/mL）孵育Pseudomonas aeruginosa（PA）24小时。Benzydamine HCl显著抑制PA的增殖[6]。
在体内，Benzydamine HCl（10mg/kg；在第0天和第2天共两次注射）通过颅骨局部注射于LPS诱导的炎症性骨破坏模型中的C57BL/6小鼠，或通过腹腔注射（每周六次；持续三周）于卵巢切除（OVX）诱导的绝经后骨质疏松模型中的C57BL/6小鼠。Benzydamine HCl显著减少了炎症引起的颅骨骨破坏和破骨细胞数量，并逆转了卵巢切除引起的骨密度下降、骨体积减少等骨质流失现象[7]。Benzydamine HCl（10或20mg/kg；单次注射）通过皮下注射，在LPS注射的同时或之后（30分钟或4小时）用于处理内毒素血症模型中的雌性Balb/c小鼠。Benzydamine HCl能显著提高LPS的半数致死剂量，并在LPS注射后30分钟或4小时给药，显著降低LPS诱导的小鼠死亡率[8]。