Efisol

Uses

Efisol chloride, the active ingredient in Fluomizin, belongs to the family of anti-infective and antiseptic drugs. Efisol chloride is active against the bacteria which cause bacterial vaginosis. Fluomizin is used for the treatment of bacterial vaginosis. It is inserted into the vagina for treatment at the site of infection.

Efisol is also used to associated treatment for these conditions: Breath odour, Gingivitis, Infection, Inflammation of Mouth, Oral Candidiasis, Pharyngitis, Stomatitis, Tonsillitis, Mouth infection, Throat infections, Throat inflammation, Tongue inflammation, Ulceration of the mouth, Oropharyngeal antisepsis

How Efisol works

Efisol has a multiple mode of action. It disrupts the cell permeability of the bacteria by absorbing onto the bacterial cell surface and diffusing across the membrane. It also binds to the cytoplasmic membrane with subsequent formation of complexes and protein precipitation and lyses the membrane in adequate concentrations, perturbing osmotic exchange. Loss of normal enzymatic activity is achieved through several different processes. Denaturation of proteins results in inhibition of bacterial cell metabolism. Disruption of bacterial energy production is mediated through inhibition of glucose metabolism and inhibition of mitochondrial ATP synthesis via inhibition of bacterial F1-ATPase. Protein synthesis is also terminated at the level of ribosomes. Bacterial nucleic acids are also affected through direct binding of the drug to DNA in vitro, and precipitation of cytoplasmic material with nucleic acids being the most sensitive . The cationic form of dequalinium accumulates in the mitochondria and promotes anticancer activity in human leukemia cells. It mediates a cytotoxic effect by altering redox balance in cells and downregulating Raf/MEK/ERK1/2 and PI3K/Akt signaling pathways in these cells which leads to cell death by apoptosis and/or necrosis . Efisol inhibits mycothiol ligase activity in Mycobacterium tuberculosis strains .

Dosage

Efisol dosage

• Adult: The recommended dose is 1 vaginal tablet daily for 6 days.
• Children and adolescents: There is insufficient experience of the use of Fluomizin in children and adolescents under 18 years of age.
• Women above 55 years and elderly: There is insufficient experience of the use of Fluomizin in women above 55 years.

• Use every evening before bed.
• Wash your hands before opening the blister pack.
• Lie down in a reclining position with the legs slightly bent. Insert one vaginal tablet deeply into the vagina.
• You should stop the treatment during the heavy bleeding period of your menstruation and resume afterwards.
• Do not stop treatment early, even if you no longer have any discomfort (e.g. itching, discharge, smell). A treatment of less than 6 days may result in your symptoms returning.
• Efisol contains ingredients which do not dissolve completely, and the remains of the tablet are occasionally found in the underwear. This won’t affect the effectiveness of the treatment. The tablet will not stain your underwear but for your own comfort you can use a sanitary towel or panty liner.
• If your vagina is dry, the vaginal tablet might not dissolve and be discharged as an intact tablet. As a consequence, the treatment is not optimal. In this case the vaginal tablet can be moistened with a drop of water before insertion.

Side Effects

Sometimes the symptoms of vaginal infections (such as itching, burning and discharge) can get worse at the beginning of the treatment, before they start to get better. You should continue with the treatment, but if the complaints persist see your doctor for advice as soon as possible. Common side effects are Vaginal discharge; vaginal itching or vaginal burning; Vaginal yeast infection (thrush).

Toxicity

The oral LD50 value of dequalinium chloride for mouse is 300mg/kg. Lethal dose (LD50) of a single intraperitoneal administration in a murine model system is 18.3 mg/kg. The majority of the adverse reactions of vaginal dequalinium tablets in clinical studies (about 90 %) were local reactions, particularly vaginal discharge, vulvovaginal pruritus, and a vaginal burning sensation. Dequalinuim is not reported to possess embryo-foetal toxicity at clinically relevant doses.

Precaution

• Intravaginal use of soaps, spermicides and vaginal douches (vaginal washes) is not recommended during treatment with Fluomizin.
• As with all vaginal infections, unprotected sexual intercourse during treatment with Fluomizin is not recommended.
• Fluomizin does not reduce the effectiveness of latex condoms.
• This product may reduce the effectiveness of non-latex condoms or diaphragms. Consequently, you should use alternative methods of contraception for at least 12 hours following the treatment.
• Do not use Fluomizin within 12 hours before birth to minimize exposure of the newborn to dequalinium chloride. Please inform your doctor otherwise.
• You should stop the treatment during the heavy bleeding period of your menstruation and resume afterwards.
• You should talk to your doctor if the symptoms persist at the end of the treatment or in case the symptoms return.

Food Interaction

Elimination Route

The degree of absorption is minimal in case of topical or vaginal administration thus systemic exposure is negligible. <0.1 % is absorbed systemically after oral administration.

Pregnancy & Breastfeeding use

If you are pregnant, think you may be pregnant or plan to have a baby ask your doctor or pharmacist for advice before using Efisol. Tell your doctor or pharmacist if you are breast-feeding or if you plan to breast-feed. Based on previous experience and since Efisol acts locally, no harmful effects on pregnancy and/or the unborn and breast fed infant are expected. Efisol should only be used during pregnancy and during breast-feeding if medically needed. Ask your doctor or pharmacist for advice before taking any medicine.

Contraindication

Do not use Efisol Chloride:

• if you are allergic to the active substance dequalinium chloride or any of the other ingredients of this medicine.
• if you have ulcers on your vagina or cervix.
• if you have not yet had your first period.

Acute Overdose

• Using a higher daily dose or increasing the recommended duration might increase the risk of vaginal ulcerations. If you have accidentally used too many vaginal tablets, tell your doctor.
• Do not use a double dose to make up for a forgotten tablet.
• A treatment of less than 6 days may result in a relapse. Therefore, do not stop treatment early, even when you have no discomfort (e.g. itching, discharge, smell) anymore.

Storage Condition

Keep this medicine out of the sight and reach of children. Do not use this medicine after the expiry date which is stated on the carton and the blister. The expiry date refers to the last day of that month.

Innovators Monograph

You find simplified version here Efisol