Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2017 Publisher: Kora Corporation Ltd t/a Kora Healthcare, Swords Business Park, Swords, Co. Dublin, Ireland
Pharmacotherapeutic group: Gynaecological anti-infective and antiseptic, Quinoline derivatives
ATC code: G01AC05
Dequalinum chloride is an anti-infective and antiseptic agent belonging to the class of quaternary ammonium compounds.
Dequalinium chloride is a surface-active substance. The primary mechanism of action is an increase in bacterial cell permeability and the subsequent loss of enzyme activity, finally resulting in cell death.
Dequalinium chloride exhibits a rapid bactericidal activity.
Dequalinium chloride in vaginal tablets exerts its action locally within the vagina.
No major PK/PD determinant of efficacy has been established for Fluomizin. As the bactericidal effect of dequalinium chloride occurs within 30 to 60 minutes, the maximum local concentration within the first hour after application is considered crucial for the efficacy.
The mechanisms resulting in the inherent resistance of some pathogens are not known. No mechanisms of acquired resistance have been observed thus far.
No Breakpoints for dequalinium chloride are available by any recommending body and no relationship between minimal inhibitory concentrations and the clinical efficacy has been established. Thus, the information on susceptibility in the table below is descriptive and is based on the concentrations achievable in the vagina (see section 5.2) and respective MIC data of the pathogens. The prevalence of acquired resistance may vary geographically and with time for selected species and local information on resistance is desirable, particularly when treating severe infections. As necessary, expert advice should be sought when the local prevalence of resistance is such that the utility of the agent in at least some types of infection is questionable.
Aerobic Gram-positive bacteria:
Enterococcus faecalis
Lactobacillus spp.
Staphylococcus aureus
Streptococcus agalactiae (Group B streptococci)
Streptococcus pyogenes (Group A streptococci)
Aerobic Gram-negative bacteria:
Enterobacter spp.
Escherichia coli
Klebsiella spp.
Pseudomonas spp.
Serratia spp.
Anaerobic bacteria:
Atopobium vaginae
Bacteroides spp.
Fusobacteria
Gardnerella vaginalis
Prevotella spp.
Peptostreptococci
Poryphyromonas spp
None known.
Gram-negative bacteria:
Proteus sp.
Chlamydia trachomatis
Other micro-organisms:
Trichomonas vaginalis
After dissolution of a Fluomizin vaginal tablet (10 mg dequalinium chloride) in an estimated 2.5 to 5 ml of vaginal fluid, the dequalinium chloride concentration in the vaginal fluid is 2000-4000 mg/l.
Preclinical data indicate that dequalinium chloride is absorbed only to a very small amount after vaginal application.
Therefore, systemic exposure to Fluomizin is negligible and no further pharmacokinetic data are available.
Systemic toxic effects of Fluomizin are unlikely on the basis of the negligible systemic exposure of dequalinium chloride administered intravaginally.
In vivo and in vitro studies with dequalinium chloride did not yield any indication of a potential to cause mutagenicity.
No reproduction toxicity studies have been conducted with dequalinium chloride.
A study in rabbits showed the good vaginal tolerance of Fluomizin.
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