Dequalinium

Chemical formula: C₃₀H₄₀N₄²⁺  Molecular mass: 456.665 g/mol  PubChem compound: 2993

Mechanism of action

Dequalinum is an anti-infective and antiseptic agent belonging to the class of quaternary ammonium compounds.

Dequalinium 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 exhibits a rapid bactericidal activity.

Dequalinium in vaginal tablets exerts its action locally within the vagina.

Pharmacodynamic properties

Pharmacokinetic/pharmacodynamics relationship

No major PK/PD determinant of efficacy has been established for dequalinium. As the bactericidal effect of dequalinium occurs within 30 to 60 minutes, the maximum local concentration within the first hour after application is considered crucial for the efficacy.

Mechanism(s) of resistance

The mechanisms resulting in the inherent resistance of some pathogens are not known. No mechanisms of acquired resistance have been observed thus far.

Pharmacokinetic properties

After dissolution of a dequalinium vaginal tablet (10 mg dequalinium chloride) in an estimated 2.5 to 5 ml of vaginal fluid, the dequalinium concentration in the vaginal fluid is 2000-4000 mg/l.

Preclinical data indicate that dequalinium is absorbed only to a very small amount after vaginal application.

Therefore, systemic exposure to dequalinium is negligible and no further pharmacokinetic data are available.

Preclinical safety data

Systemic toxic effects of dequalinium are unlikely on the basis of the negligible systemic exposure of dequalinium administered intravaginally.

In vivo and in vitro studies with dequalinium did not yield any indication of a potential to cause mutagenicity.

No reproduction toxicity studies have been conducted with dequalinium.

A study in rabbits showed the good vaginal tolerance of dequalinium.

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