Fluomizin Mechanism of Action

Pharmacotherapeutic Group: Gynaecological anti-infective and antiseptic. ATC Code: G01AC05.
Pharmacology: Pharmacodynamics: Fluomizin contains dequalinium chloride, a quaternary ammonium compound with a broad antimicrobial spectrum against different gram-positive and gram-negative bacteria, fungi and protozoa (Trichomonas vaginalis).
The in vitro activity of dequalinium chloride against the following vaginally-important microorganisms was established and expressed as minimum inhibition concentration (MIC).
Gram-Positive Bacteria MIC (mg/L): Group B streptococci 2-8; Staphylococcus aureus 0.2-10; Group A streptococci 0.25-20; Listeria sp 4-32; Peptostreptococci 1-32; Group D streptococci 0.2-64.
Fungi MIC (mg/L): Candida tropicalis 0.2-50; Candida albicans 0.2-200; Candida glabrata 0.2-256; Candida krusei 128.
Gram-Negative Bacteria MIC (mg/L): Fusobacteria 32-64; Gardnerella vaginalis 2-256; Echerichia coli 1-400; Serratia sp 3.1-400; Klebsiella sp 3.1-400; Pseudomonas sp 5-400; Bacteroides sp/Prevotella sp 64-512; Proteus sp 20->1024.
Protozoa MIC (mg/L): Trichomonas vaginalis 28.8-400.
After dissolution of a Fluomizin vaginal tablet (dequalinium chloride 10 mg) in an estimated 2.5-5 mL of vaginal fluid, the dequalinium chloride concentration in the vaginal fluid is 4000 to 2000 mg/L, which is higher as the MIC₉₀ of all tested pathogenic microrganisms.
Development of resistance of microorganisms to dequalinium chloride has not been reported.
As for other surface-active compounds, the primary mode of action of dequalinium chloride is the enhancement of cell permeability and the subsequent loss of enzymatic activity which causes cell death.
Dequalinium chloride in vaginal tablets exerts its action locally within the vagina. Marked relief of discharge and inflammation generally occurs within 24-72 hrs.
The efficacy of Fluomizin in the treatment of vaginal infections of various origin have been shown by an active controlled, double-blind clinical study.
Pharmacokinetics: Preclinical data from rabbits indicate that dequalinium chloride is absorbed only to a very small amount after vaginal application.
Distribution is observed into the liver, kidney and lung. Dequalinium chloride appears to be metabolised to the 2,2'-dicarboxylic acid derivate and excreted in the non-conjugated form via faeces.
In view of the negligible vaginal absorption, there are no available human pharmacokinetic data for dequalinium chloride.
Toxicology: Preclinical Safety Data: Considering the minimal vaginal absorption of dequalinium chloride, no acute or chronic toxicity is to be expected.
No reproduction toxicity studies have been conducted with Fluomizin. However, developmental toxicity studies with quarternary ammonium compounds did not reveal evidence of embryofoetal toxicity.
Local Tolerance: A study in rabbits showed the good vaginal tolerance of Fluomizin.