Bifonazole (Bay H-4502) acts to destabilize the fungal cytochrome p450 51 enzyme (also known as Lanosterol 14-alpha-demethylase). It works by inhibiting the production of a substance called ergosterol, which is an essential component of fungal cell membranes. This is vital in the cell membrane structure of the fungus. Its inhibition leads to cell lysis. The disruption in production of ergosterol disrupts the cell membrane and causes holes to appear. The cell membranes of fungi are vital for their survival. They keep unwanted substances from entering the cells and stop the contents of the cells from leaking out.

Bifonazole 是一种广谱抗真菌剂，能够抑制单加氧酶活性，并在2B4dH(H226Y)（一种以4-(4-氯苯基)咪唑（CPI）存在下结晶的改造酶）中诱导II型结合谱。[1] Bifonazole （40 mM）可以释放对1 mM丝裂霉素敏感的储存Ca2+，且自身可诱导电容耦联的Ca2+进入，同时减少1 mM丝裂霉素诱导的电容耦联Ca2+进入。[2] Bifonazole 作为钙调蛋白拮抗剂，在B16黑色素瘤细胞中极为有效地降低糖酵解和ATP水平，其作用机制涉及异构体调节和糖酵解酶从细胞骨架的脱离。[3] Bifonazole 阻断由2 μm和4μm花生四烯酸诱导的PGE2形成，效果明显优于6或10μm激动剂条件下。在MC3T3-E1和UMR-106细胞中，Bifonazole 对氨甲环酸或不同浓度花生四烯酸的刺激表现出相同的特性。[4]

Bifonazole显示出过氧化物酶增生剂的特性，表现为肝脏增大（肝脏与体重比例的增加）。Bifonazole还能诱导P402B1/2B2、P4503A和P4501A1的表达，但并不诱导P4502E1。[5]