Fluomizin

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT FLUOMIZIN (FLUOMIZIN®)

Composition:

Active substance: decqualinium chloride;

1 vaginal tablet contains 10 mg of decqualinium chloride;

Excipients: lactose monohydrate; microcrystalline cellulose; magnesium stearate.

Pharmaceutical form. Vaginal tablets.

Main physicochemical properties: white or almost white, oval, biconvex tablets.

Pharmacotherapeutic group.

Antimicrobial and antiseptic agents used in gynecology.

ATC Code G01AC05.

Pharmacological properties.

Pharmacodynamics.

Fluomizin contains dequalinium chloride – a quaternary ammonium compound with a broad antimicrobial spectrum of activity against various gram-positive and gram-negative bacteria, fungi, and protozoa (Trichomonas vaginalis).

Mechanism of action

Dequalinium chloride is a surface-active substance. The primary mechanism of action of dequalinium chloride involves increasing the permeability of the bacterial cell membrane, leading to subsequent loss of enzyme activity and resulting in cell death.

Dequalinium chloride exhibits rapid bactericidal and fungicidal activity.

Dequalinium chloride in vaginal tablets exerts its effect locally within the vagina. A noticeable reduction in discharge and inflammation usually occurs within 24–72 hours.

Pharmacokinetic/pharmacodynamic relationship

No limiting influence of pharmacokinetics/pharmacodynamics on the efficacy of Fluomizin has been established. Since the bactericidal effect of dequalinium chloride occurs within 30–60 minutes, the key factor for efficacy is achieving maximum local concentration during the first hour after administration.

Mechanisms of resistance

Mechanisms leading to primary resistance of pathogenic microorganisms have not been identified. There have been no reports of acquired microbial resistance to dequalinium chloride.

Breakpoints for susceptibility

Breakpoints have not been defined, and no correlation has been established between minimum inhibitory concentrations (MICs) and clinical efficacy.

Therefore, the information on microbial susceptibility provided below is based on concentrations achieved in the vagina (see section "Pharmacokinetics") and corresponding MIC data for pathogenic microorganisms.

Antimicrobial spectrum of activity

Typically sensitive species

Aerobic gram-positive bacteria

Enterococcus faecalis,

Listeria 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,

Porphyromonas spp.

Fungi

Candida albicans,

Candida tropicalis,

Candida glabrata,

Candida krusei

Organisms with inherent resistance

Gram-negative bacteria

Proteus sp.,

Chlamydia trachomatis

Pharmacokinetics.

After dissolution of a Fluomizin vaginal tablet (10 mg dequalinium chloride) in 2.5–5 mL of vaginal fluid, the concentration of dequalinium chloride in vaginal fluid ranges from 4000–2000 mg/L, which exceeds the MIC₉₀ values for all tested pathogenic microorganisms.

Preclinical study results indicate that only a small amount of dequalinium chloride is absorbed following vaginal administration.

Due to negligible vaginal absorption, there are no data available on the pharmacokinetics of dequalinium chloride in humans.

Clinical characteristics.

Indications.

• Vaginal infections of bacterial and fungal origin.
• Bacterial vaginosis.
• Candidiasis.

Contraindications.

• Hypersensitivity to the active substance or to any of the excipients.
• Epithelial ulcers of the vagina and vaginal portion of the cervix.
• Not to be used in young girls who have not yet experienced menarche and who have not reached sexual maturity.

Interaction with other medicinal products and other forms of interaction.

Soap and other surfactants may reduce the antimicrobial activity of dequalinium chloride. Therefore, during treatment, the intravaginal use of soap, spermicidal agents, and douching is not recommended. Fluomizin does not affect the functionality of latex condoms. There are no data regarding interactions with non-latex condoms and other intravaginal devices such as diaphragms.

Therefore, during treatment and for at least 12 hours after treatment, the use of non-latex condoms and other intravaginal devices is not recommended.

Special precautions for use

Fluomizin contains excipients that do not dissolve completely. Residues of the tablet may sometimes be found on underwear. This does not affect the efficacy of Fluomizin.

In some cases, when vaginal dryness is present, there is a possibility that the vaginal tablet does not dissolve and is expelled from the vagina intact. As a result, such treatment may not be effective. To prevent this, the tablet may be moistened with a small amount of water before insertion into a dry vagina.

Patients should use sanitary pads or daily liners. The medicinal product does not change the color of underwear. Patients should be advised to change their underwear and towels daily and to wash them at a temperature of at least 80 °C.

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

There are no data on the efficacy and safety of repeated treatment in patients who did not respond or experienced a recurrence of the disease immediately after initial treatment with the drug. Patients should be advised to consult their physician if symptoms persist at the end of treatment or if the disease recurs.

Exceeding the recommended daily dose or duration of treatment increases the risk of vaginal epithelial ulceration.

There are no data on the efficacy and safety of bacterial vaginosis treatment in women under 18 years of age or over 55 years of age.

Use during pregnancy or breastfeeding

Pregnancy

Fluomizin may be used during pregnancy or breastfeeding. However, caution should be exercised when prescribing Fluomizin to pregnant women during the first trimester of pregnancy. Data obtained from clinical studies with dequalinium chloride and from studies with the medicinal product Fluomizin indicate no adverse effects of dequalinium chloride on pregnancy or on the health of the fetus/newborn child.

Post-marketing surveillance data from approximately 1.1 million pregnant women exposed to the drug indicate no adverse effects of dequalinium chloride on the course of pregnancy or on the health of the fetus/newborn child.

There are no data on the passage of dequalinium chloride into breast milk.

Considering the lack of systemic absorption and the short treatment duration of only 6 days, adverse effects on the fetus or newborn are unlikely.

Reproductive toxicity studies in animals were not conducted due to the expected low degree of absorption of dequalinium chloride after vaginal administration.

Fluomizin should be used during pregnancy if clinically necessary.

Breastfeeding

Since systemic absorption of Fluomizin is negligible, harmful effects on the newborn/infant are unlikely.

Fluomizin may be used during lactation if clinically necessary.

Fertility

Studies on the effects on fertility in animals have not been conducted.

Ability to affect reaction speed when driving vehicles or operating machinery

Studies on the ability to affect reaction speed when driving vehicles or operating machinery have not been conducted.

Method of Administration and Dosage

It is recommended to use 1 vaginal tablet daily for 6 days. Insert the vaginal tablet deep into the vagina in the evening before going to bed. It is best to do this while lying on your back, with knees slightly bent.

During menstruation, treatment should be discontinued and resumed after menstruation ends.

Although reduction of discharge and inflammation usually occurs within 24–72 hours, treatment must be continued even if discomfort symptoms (such as itching, discharge, odor) have already subsided. Treatment lasting less than 6 days may lead to recurrence. The full course of treatment is 6 days.

Children

Not recommended for use in children.

Overdose

No cases of overdose have been reported. However, exceeding the daily dose may lead to the formation of vaginal epithelial ulcers.

Adverse Reactions

The following adverse reactions, which are likely related to dequalinium chloride, were reported during clinical studies.

The list of adverse reactions is presented by organ systems and frequency: common (≥ 1/100 to < 1/10), uncommon (≥ 1/1000 to < 1/100), frequency not known – these adverse reactions were reported during the post-marketing period.

Genital organs and breast.

Common: vaginal discharge, vulvovaginal pruritus, burning sensation in the vulvovaginal area.

Uncommon: vaginal bleeding, vaginal pain.

Frequency not known: vaginal epithelial ulcers and maceration, uterine bleeding, erythema, vaginal dryness.

Infections and parasitic diseases.

Common: vaginal candidiasis.

Uncommon: bacterial vaginosis, fungal skin infection, vulvitis, vulvovaginitis.

Frequency not known: cystitis.

Nervous system disorders.

Uncommon: headache.

Gastrointestinal disorders.

Uncommon: nausea.

General disorders and administration site conditions.

Frequency not known: allergic reactions with symptoms such as urticaria, erythema, exanthema, edema, rash or pruritus, fever.

Shelf life.

3 years

Storage conditions.

Store at temperatures not exceeding 30 °C. Keep in the original packaging. Store out of reach of children.

Packaging.

6 tablets in a blister, 1 blister in a cardboard box. 2 tablets in a blister, 1 blister in a cardboard box.

Prescription status.

Over-the-counter.

Manufacturer.

Medinova AG / Medinova AG.

Manufacturer's address and place of business.

Eggbühlstrasse 28, 8050 Zurich, Switzerland / Eggbuhlstrasse 28, 8050 Zurich, Switzerland.