Tonsillol

Tonsillol 10 mg vaginal tablets are indicated for the treatment of Bacterial vaginosis

Consideration should be given to official guidance on the appropriate use of antibacterial agents.

Posology

One vaginal tablet daily for six days.

The vaginal tablets should be inserted deeply into the vagina in the evenings before retiring. This is best performed in a reclining position with the legs slightly bent.

The treatment should be interrupted during menstruation and resumed afterwards.

Although relief of discharge and inflammation generally occurs within 24 to 72 hours, the treatment should be continued even when there is no subjective discomfort (itching, discharge, smell) anymore. A treatment less than six days could result in a relapse.

Tonsillol contains excipients which do not dissolve completely, such that remains of the tablet are occasionally found in the underwear. This is of no importance for the efficacy of Tonsillol.

In rare cases of a very dry vagina, it is possible that the vaginal tablet does not dissolve and is discharged by the vagina as intact tablet. As consequence, the treatment is not optimal. For prevention, the vaginal tablet can be moistened with a drop of water before insertion into a very dry vagina.

Patients should use a sanitary towel or panty liner. There is no change in colour of the underwear.

Women more than 55 years and elderly

There is a lack of data on the efficacy and safety of dequalinium chloride in women above 55 years of age.

Paediatric population

There is a lack of data on the efficacy and safety of dequalinium chloride in children below 18.

Method of administration

For vaginal use

Ulceration of the vaginal epithelium and the vaginal portion of the cervix.

Young girls who have not yet had their first menstruation, and thus did not reach sexual maturity must not use Tonsillol.

To minimize exposure of the newborn to dequalinium chloride, vaginal tablets should not be used within 12 hours before birth.

There are no efficacy and safety data available on the re-treatment of patients who did not respond to or relapsed immediately after initial therapy with Tonsillol. Patients should be advised to consult their physician if the symptoms persist at the end of the treatment or in case of recurrence.

Using a higher daily dose or increasing the recommended treatment duration might increase the risk of vaginal ulcerations.

No efficacy and safety data on the treatment of bacterial vaginosis in women aged less than 18 years or more than 55 years are available.

No studies on the effects on the ability to drive and use machines have been performed.

In clinical trials, the following undesirable effects possibly or probably related to dequalinum chloride have been reported.

Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.

No case of overdose has been reported. However, use of a higher daily dose might result in vaginal ulcerations. In case of overdose with adverse events, a vaginal lavage can be performed.

Pharmacotherapeutic group: Gynaecological anti-infective and antiseptic, Quinoline derivatives

ATC code: G01A C05

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

Mechanism of Action

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.

Pharmacokinetic/pharmacodynamics relationship

No major PK/PD determinant of efficacy has been established for Tonsillol. 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.

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.

Breakpoints

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 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.

After dissolution of a Tonsillol 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 Tonsillol is negligible and no further pharmacokinetic data are available.

Systemic toxic effects of Tonsillol 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 Tonsillol.

Tonsillol is incompatible with soaps and other anionic surfactants.

No special requirements.