Ketodine

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT KETODIN (KETODIN)

Composition:

Active substance: ketoconazole;

1 suppository contains ketoconazole 400 mg;

Excipients: polyethylene glycol 400, polyethylene glycol 4000, butylated hydroxyanisole (E 320).

Pharmaceutical form. Vaginal suppositories.

Main physicochemical properties: suppositories from white to almost white, torpedo-shaped.

Pharmacotherapeutic group. Antimicrobial and antiseptic agents used in gynecology. Imidazole derivatives.

ATC code G01AF11.

Pharmacological Properties.

Pharmacodynamics.

Ketoconazole is a synthetic derivative of imidazoldioxolane. It exerts pronounced fungicidal and fungistatic activity against dermatophytes (Trichophyton spp., Epidermophyton floccosum, Microsporum spp.), yeast fungi (Candida spp., Pityrosporum spp., Torulopsis spp., Cryptococcus spp., Rhodotorula spp.), dimorphic and higher fungi (zygomycetes). Aspergillus spp., Sporothrix schenckii, some Dermatiaceae, Mucor spp., and other phcomycetes (except Entomophthorales) are less sensitive to ketoconazole. Ketoconazole is also active against Gram-positive cocci (Staphylococcus spp., Streptococcus spp.). Its mechanism of action involves inhibition of ergosterol biosynthesis and alteration of the fungal membrane lipid composition, leading to fungal lysis. Keton is also active against pathogens resistant to antifungal antibiotics (nystatin, levorin) as well as to clotrimazole. Development of secondary resistance during ketoconazole treatment has not been observed to date.

Pharmacokinetics.

After intravaginal administration, only a negligible amount (< 1%) of ketoconazole enters the systemic circulation. The maximum plasma concentration in women following intravaginal administration of 400 mg ketoconazole ranges between 0–10.7 ng/mL, which is considered trace and does not produce systemic effects.

Clinical characteristics.

Indications.

Acute and chronic recurrent vulvovaginal candidiasis; prevention of fungal infections of the vagina in conditions of decreased body resistance and during treatment with agents that disrupt normal vaginal microflora.

Contraindications.

Hypersensitivity to ketoconazole or other components of the drug.

Interaction with other medicinal products and other forms of interaction.

When ketoconazole is used concomitantly with rifampicin and isoniazid, the plasma concentration of ketoconazole decreases. When used concomitantly with cyclosporine, oral anticoagulants, and methylprednisolone, ketoconazole may increase plasma concentrations of these agents. The clinical significance of these interactions during treatment with ketoconazole in the form of vaginal suppositories is unknown.

Special precautions for use

In isolated cases, local allergic reactions in the sexual partner are possible. To reduce the risk of disease recurrence, simultaneous treatment of the sexual partner is recommended. Contact with latex products (contraceptive diaphragms, condoms) should be avoided due to reduced reliability of mechanical contraception; therefore, pregnancy or transmission of sexually transmitted infections may still occur. Sexual abstinence is advised during treatment.

Ketodin is recommended to be used at night, as the drug exerts an osmotic and draining effect, which is accompanied by increased vaginal discharge. It is recommended to use sanitary pads during the treatment period with Ketodin at night.

If hypersensitivity reactions develop, the drug should be discontinued.

Use during pregnancy or breastfeeding

Although systemic absorption of ketoconazole following intravaginal administration is extremely low or negligible, adequate controlled clinical studies on the safety of Ketodin use during pregnancy are lacking. Ketodin should not be used during the first trimester of pregnancy. During the second and third trimesters, as well as during breastfeeding, the drug should be used only if the expected benefit to the mother outweighs the potential risk to the fetus or infant.

Ability to influence reaction rate while driving or operating machinery

Does not affect.

Dosage and Administration.

Remove the suppository from the strip and insert deeply into the vagina while lying on the back with knees bent and drawn up to the chest, or in a kneeling position. Suppositories should not be cut into parts, as such alteration of the storage conditions may lead to an uneven distribution of the active substance. Administer 1 suppository once daily before bedtime for 3–5 days. If necessary, repeat the treatment course until clinical and laboratory recovery. For chronic candidiasis, use 1 suppository daily for 10 days.

Children.

There is no experience with the use of ketoconazole in the form of vaginal suppositories in children.

Overdose.

In case of local overdose, hyperemia, burning, itching, and irritation of the vaginal mucosa may occur. In such cases, irrigation with water is recommended.

Side effects.

Side effects occur rarely and quickly resolve after discontinuation of the drug.

Skin and mucous membranes: pruritus, rash, burning, hyperemia, irritation of the vaginal mucosa, skin rash, urticaria, possible reactions at the site of administration.

Gastrointestinal tract: rarely – nausea, abdominal pain.

Nervous system: rarely – dizziness.

Hypersensitivity reactions: rarely – urticaria, anaphylactic and anaphylactoid reactions, angioedema.

Shelf life.

3 years.

Do not use the medication after the expiry date stated on the packaging.

Storage conditions.

Store at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging.

5 suppositories per strip, 2 strips per cardboard box.

Supply category.

Over-the-counter (without prescription).

Manufacturer.

Ukrainian-Spanish joint venture "Sperco Ukraine".

Manufacturer's address and place of business.

21027, Ukraine, Vinnytsia, 600-richchia St., 25.

Tel.: + 38 (0432) 52-30-36. E-mail: [email protected]

www.sperco.com.ua