DARSTIN

INSTRUCTIONS for medical use of the medicinal product DARSTIN (DARSTIN)

Composition:

Active substance: progesterone;

1 g of gel contains 10 mg of progesterone;

Excipients: carbomer, triethanolamine, ethanol 96%, purified water.

Pharmaceutical form. Gel.

Main physicochemical characteristics: semitransparent, colorless gel.

Pharmacotherapeutic group. Sex hormones and drugs used in disorders of the reproductive system. Progestogens. Derivatives of 4-pregnene. Progesterone.

ATC code G03D A04.

Pharmacological properties.

Pharmacodynamics.

The active ingredient of the Darstin preparation is synthetic progesterone, dispersed in a special solvent for transdermal application. The antiestrogenic action of progesterone corrects the local imbalance between estrogens and progesterone.

Progesterone acts directly on the mammary gland, where it accumulates. Darstin prevents local effects of progesterone deficiency at the vascular and cellular levels within the mammary gland. At these levels, progesterone:

• prevents estrogen-induced increase in capillary permeability;
• suppresses growth and differentiation of mammary ducts and acini;
• blocks the epithelial mitotic cycle provoked by estrogens.

Pharmacokinetics.

Absorption

The extent of absorption is approximately 10% of the administered dose.

Biotransformation

Approximately 80% of absorbed progesterone is metabolized within the mammary gland, whereas only 20% reaches the systemic circulation.

Elimination

Maximum elimination of the metabolized substance occurs within 48 hours.

Clinical characteristics.

Indications.

Benign breast diseases:

• essential mastodynia;
• mastodynia associated with benign breast disease (complex treatment of benign mastopathy against the background of progesterone deficiency).

Darstine is not indicated for use in men.

Contraindications.

Hypersensitivity to the active substance or to any of the excipients of the drug.

Nodular forms of fibrocystic mastopathy.

Tumors (tumor-like formations) of the breast of unclear etiology.

Breast cancer or genital organs (as monotherapy).

Interaction with other medicinal products and other forms of interaction.

During clinical studies, no clinically significant interactions were observed.

The effect of the drug may be enhanced when using combined hormonal contraceptives.

According to currently available information, no interactions with other drugs have been observed.

Special precautions for use.

Since the drug is an aqueous-alcoholic solution, it must not be applied directly to mucous membranes.

Frequent use may cause skin irritation and skin dryness.

In case of impaired skin barrier function, there is a risk of progesterone entering the systemic circulation. Therefore, use of the drug in such cases is not recommended.

Use with caution in the following conditions: hepatic insufficiency, renal insufficiency, bronchial asthma, epilepsy, migraine, depression, hyperlipoproteinemia, ectopic pregnancy, abortion, tendency to thrombosis, acute forms of phlebitis or thromboembolic disorders, vaginal bleeding of unknown etiology, porphyria, arterial hypertension, diabetes mellitus.

Use during pregnancy or breastfeeding.

There is insufficient experience with the use of the drug during pregnancy. However, no negative effects of progesterone on the fetus have been reported.

Progesterone may be partially excreted into breast milk. However, no adverse effects on the infant have been reported. Therefore, it is recommended to avoid using this drug during breastfeeding.

Ability to influence reaction rate while driving or operating machinery.

Data regarding the possible effect of the drug on the ability to drive vehicles or operate machinery are not available.

Dosage and Administration

Dosage

Apply 5 g of gel to the skin of the breasts (one spatula for each breast) daily, including during menstruation.

The duration of treatment depends on the indication and is determined individually by the physician.

Administration

For topical application (transdermal use).

Holding the end of the spatula in one hand and the tube in the other, squeeze out the gel along the entire length of the spatula. This amount corresponds to the correct dose for one breast (2.5 g).

Repeat the procedure for the other breast.

Children

The drug is not used in pediatric practice.

Overdose

No cases of overdose have been reported.

Adverse reactions.

Isolated cases of hypersensitivity or non-specific skin irritation have been reported.

In some cases, menstruation may start one to two days earlier, without any changes in the usual monthly volume of discharge. Weak secretory LH-mimetic activity has been observed, which does not share characteristics with the effects of systemic administration of an equivalent dose of progesterone.

When the recommended method of application is followed, systemic absorption of progesterone is unlikely. However, if the skin barrier function is impaired, there is a risk of developing systemic adverse reactions, including menstrual cycle disturbances, amenorrhea, breakthrough bleeding, headache.

Very rare: breast tenderness, hot flushes, metrorrhagia, decreased libido, hypersensitivity reactions including erythema at the site of gel application, swelling of lips and neck, fever, headache, nausea.

Reporting suspected adverse reactions

Reporting suspected adverse reactions after authorization of the medicinal product is important. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report any suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 3 years.

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

Use within 1 month after first opening of the tube.

Storage conditions.

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Packaging.

80 g of gel in an aluminum tube with an internal lacquer coating, closed with a polyethylene cap.

One tube with a dosing spatula in a cardboard box.

Prescription status.

Prescription only.

Manufacturer.

SEID S.A. / SEID S.A.

Manufacturer's address and location of operations.

Ctra. de Sabadell a Granollers, Km. 15, Llica de Vall, Barcelona, 08185, Spain /
Ctra. de Sabadell a Granollers, Km. 15, Llica de Vall, Barcelona, 08185, Spain.