Santequin®

INSTRUCTIONS for medical use of the medicinal product SANTekvin® (Santekvin®)

Composition:

Active substance: econazole nitrate;

1 suppository contains econazole nitrate 150 mg;

Excipients: polyethylene glycol 400, polyethylene glycol 1500, hard fat, cetyl alcohol, titanium dioxide (E 171), silicon dioxide colloidal anhydrous.

Medicinal form. Vaginal suppositories.

Main physicochemical properties: white, globular-shaped suppositories.

Pharmacotherapeutic group. Antimicrobial and antiseptic agents used in gynecology. ATC code G01AF05.

Pharmacological properties.

Pharmacodynamics.

The drug is a triazole fungicide. It exhibits antifungal activity against dermatophytes, yeasts, and molds. It is active against some Gram-positive and Gram-negative bacteria. The action of econazole nitrate involves damaging fungal cell membranes by increasing the permeability of fungal cells and damaging intracellular membranes in the cytoplasm. The site of action is likely the acyl residues of unsaturated fatty acids of membrane phospholipids.

Pharmacokinetics.

After vaginal administration, econazole nitrate is absorbed to a negligible extent. Maximum concentrations of econazole and/or its metabolites were observed within 1–2 days after administration and amounted to 65 ng/mL. The amount of econazole absorbed into the systemic circulation is approximately 5%.

Econazole and/or its metabolites in the systemic circulation are predominantly bound to serum proteins (> 98%).

Econazole is mainly metabolized via oxidation, deamination, and/or O-dealkylation. Less than 1% of the administered dose is excreted in feces and urine.

Clinical characteristics.

Indications.

Vulvovaginal fungal infections caused by pathogens sensitive to econazole.

Contraindications.

Hypersensitivity to econazole nitrate or to any of the excipients of the product.

Interaction with other medicinal products and other forms of interaction.

Concomitant use of diaphragms or condoms with Santekvin® should be avoided. Such interaction reduces the efficacy of the medicinal product and weakens the strength of barrier contraceptives.

Santekvin® should not be combined with other gynecological medicinal products for intravaginal or topical use based on mineral oil, vegetable oil, or vaseline.

No adequate studies have been conducted. Since econazole is chemically similar to imidazole derivatives, there is a potential for competitive interaction between econazole nitrate and substances metabolized by CYP3A/2C9 enzymes. However, due to the low systemic absorption of the drug, clinically significant interactions are unlikely.

If the patient is taking oral anticoagulants such as warfarin or acenocoumarol, caution should be exercised and blood coagulation parameters should be monitored. Dose adjustment of oral anticoagulants may be necessary during and after treatment with Santekvin®.

Special precautions for use.

Santequin® is intended for vaginal use only – it should not be administered orally.

Place the suppositories in a cool place 30 minutes before use. The suppositories contain hard fat, which may damage rubber contraceptives such as diaphragms or latex condoms and reduce their effectiveness. Therefore, concurrent use of these contraceptive methods should be avoided.

If symptoms of irritation or hypersensitivity occur, treatment should be discontinued. Patients who are hypersensitive to imidazole derivatives may also exhibit hypersensitivity to econazole nitrate.

Cetyl alcohol may cause local skin reactions (contact dermatitis).

Santequin® should not be used concomitantly with other medicinal products intended for the treatment of gynecological conditions administered orally or externally.

Patients using spermicidal contraceptives should consult their physician, as local vaginal treatment may inactivate the effect of spermicidal contraceptives.

The product does not stain underwear.

The efficacy and safety of use in women aged 65 years and older have not been established.

Use during pregnancy or breastfeeding.

Econazole nitrate did not show teratogenic effects in animal studies; however, at high doses, it was fetotoxic. The significance of this effect in humans is unknown.

The drug may be systemically absorbed from the vagina; therefore, it should not be used during the first trimester of pregnancy unless the physician determines that treatment with this drug is essential for the patient's health. During the second and third trimesters of pregnancy, the drug may be used if the potential benefit to the mother outweighs the possible risk to the fetus.

It is unknown whether econazole nitrate passes into breast milk; therefore, during breastfeeding, the drug should be used with caution, taking into account the benefit-risk ratio.

Ability to influence reaction rate while driving or operating machinery.

Santequin® does not affect the ability to drive or operate machinery.

Method of Administration and Dosage

Before using the suppository, it is necessary to:

• tear off one suppository along the perforation line of the blister pack in the primary packaging;
• then pull the edges of the film apart in opposite directions to remove the suppository from its primary packaging.

Treatment course – 3 days, 1 suppository administered once daily into the posterior vaginal fornix before bedtime, preferably while lying on the back. In case of recurrence or if culture analysis one week after treatment shows a positive result, a repeated course of treatment should be conducted.

Children. Safety and efficacy of the drug in children have not been established; therefore, it is not recommended for use in this patient population.

Overdose.

Adverse reactions that may occur in case of overdose are expected to be similar to the general profile of adverse reactions.

If the drug is accidentally ingested orally, nausea, vomiting, and diarrhea may occur. In such cases, symptomatic therapy should be administered as necessary.

In case of contact with eyes, immediately rinse with water or physiological saline. If irritation symptoms persist, seek medical advice.

Side effects.

Immune system disorders: hypersensitivity.

Skin and subcutaneous tissue disorders: itching, burning sensation, urticaria, contact dermatitis, skin desquamation, rash, erythema. Cases of generalized allergic reactions including angioneurotic edema have been reported.

Reproductive system and breast disorders: burning sensation in the vagina.

General disorders and administration site conditions: very rarely – localized reactions at the application site such as erythema, rash, contact dermatitis, skin desquamation, burning sensation and itching, pain, irritation, swelling.

Shelf life.

3 years.

Storage conditions.

Keep in the original packaging, protected from light, at a temperature not exceeding 25 °C. Keep out of reach of children.

Packaging.

3 suppositories in a blister; 1 blister per carton.

Prescription status.

Prescription only.

Manufacturer.

Private Joint-Stock Company "Lekhim-Kharkiv".

Manufacturer's address.

36 Severina Pototskogo Street, Kharkiv, Kharkiv Region, 61115, Ukraine.