Decapeptyl Depot (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Ferring, GmbH (Germany)

Contact Information

Ferring Pharmaceuticals B.V. (Netherlands)

ATC Code

L02AE04 (Triptorelin)

Active Substance

Triptorelin (Rec.INN registered by WHO)

Dosage Form

Decapeptyl Depot

Lyophilizate for preparation of suspension for intramuscular and subcutaneous administration of prolonged action 3.75 mg: syringes in a set with solvent

Dosage Form, Packaging, and Composition

Lyophilisate for preparation of suspension for intramuscular and subcutaneous administration of prolonged action in the form of a powder or porous mass of white or light yellow color; the supplied solvent is a colorless or light yellow liquid with a characteristic odor of polysorbate 80.

Excipients: copolymer of lactic and glycolic acids, propylene glycol caprylocaprate.

Solvent: polysorbate 80, dextran 70, sodium chloride, sodium dihydrogen phosphate dihydrate, sodium hydroxide, water for injections.

Disposable syringes with a volume of 2.25 ml (1) in a set with solvent (disposable syringes 1 ml 1 pc.), connecting elements (1 pc.) and injection needles (1 pc.) – cardboard packs.

Clinical-Pharmacological Group

Gonadotropin-releasing hormone analogue – depot form

Pharmacotherapeutic Group

Antineoplastic agent, gonadotropin-releasing hormone analog

Pharmacological Action

The active substance of Decapeptyl Depot – Triptorelin – is a synthetic analogue of gonadotropin-releasing hormone (GnRH). The replacement of the 6th amino acid residue in the molecule of natural GnRH results in a stronger affinity for GnRH receptors and a longer half-life than the natural molecule.

The initial effect of Decapeptyl Depot administration is the stimulation of the secretion of FSH and LH by the pituitary gland. After prolonged stimulation (constant concentration of triptorelin in the blood), the pituitary gland becomes insensitive to the action of GnRH. As a result, the level of gonadotropins in the blood decreases, leading to a decrease in the level of sex hormones to post-castration or menopausal levels. The described effects are reversible.

Pharmacokinetics

Pharmacokinetic tests were performed on female patients with a confirmed diagnosis of endometriosis or uterine fibroids, patients with prostate carcinoma, and healthy male volunteers.

Absorption

In the first hours after intramuscular administration of Decapeptyl Depot, the C_max of triptorelin in blood plasma is recorded, which decreases significantly within 24 hours. On the 4th day after intramuscular injection, the concentration of triptorelin in the blood reaches a second maximum, after which the concentration decreases in a bi-exponential manner to undetectable values over 44 days.

After subcutaneous administration, the increase in the concentration of the active substance occurs more slowly compared to intramuscular administration. The decrease in the concentration of triptorelin in the blood occurs more slowly, the duration of the decrease in concentration to undetectable values is 65 days.

Repeated injections of Decapeptyl Depot at 28-day intervals do not lead to an increase in its concentration in the blood. With intramuscular and subcutaneous administration, the concentration of triptorelin in the blood on the eve of the next injection decreased to 85 pg/ml and 100 pg/ml, respectively.

In men, the constant biological availability of the active component triptorelin from the depot is 38.3% in the first 13 days. Further, the release of the drug becomes linear with an average daily value of 0.92% of the administered dose.

In women, after 27 days of the study, an average of 35.7% of the initially administered dose is determined, with 25.5% of the dose released in the first 13 days, followed by linear release, on average, of 0.73% of the administered dose daily.

Elimination

The half-life of triptorelin in plasma is 18.7 minutes, while for natural gonadotropin-releasing hormone this figure is 7.7 minutes. The clearance of triptorelin (503 ml/min) is 3 times slower than that of the natural releasing hormone (1766 ml/min) and consists of two components – rapid and slow elimination. Less than 4% of triptorelin is excreted unchanged in the urine.

Indications

In women

• Endometriosis;
• Uterine fibroids;
• Treatment of infertility using assisted reproductive technologies (IVF).

In men

• Hormone-dependent carcinoma of the prostate.

ICD codes

Dosage Regimen

Decapeptyl Depot is administered subcutaneously (into the subcutaneous tissue of the abdomen) or intramuscularly once every 4 weeks. The injection site should be alternated.

For uterine fibroids and endometriosis, the drug is administered once every 4 weeks, treatment begins in the first 5 days of the menstrual cycle, the duration of treatment is from 3 to 6 months.

For assisted reproductive technologies (IVF) – once on days 2-3 or 22 of the menstrual cycle.

For hormone-dependent prostate carcinoma – once every 4 weeks, long-term.

Rules for drug administration

1. Remove the Decapeptyl Depot package from the refrigerator.
2. Remove the cap from the syringe with the lyophilisate.
3. Open the package with the connector without removing it.
4. Screw the syringe with the lyophilisate onto the connector and remove it from the package.
5. Screw the syringe with the solvent onto the free end of the connector and ensure that the syringes are tightly connected to the connector.
6. Transfer the solvent into the syringe with the lyophilisate and then transfer the mixture back. Transfer at least 10 times. The mixture should be carefully transferred between the two syringes until a homogeneous milky suspension is formed. The first 2-3 transfers should not be performed until the liquid is completely moved from one syringe to the other.

Adverse Reactions

From the reproductive system: side effects are due to a decrease in the level of sex hormones (testosterone and estrogens) in the blood, which can lead to symptoms such as mood lability, depression, decreased libido, frequent headaches, sleep disturbance, weight gain, hot flashes, increased sweating, nausea, decreased appetite, myalgia, arthralgia, bone demineralization (with long-term use) in men and women; in women – vaginal dryness, uterine bleeding; in men – decreased potency, gynecomastia, testicular size reduction.

Laboratory parameters rarely – in men and women, increased activity of liver transaminases (LDH, GGTP, ALT, AST), increased cholesterol content in blood plasma may be noted.

Allergic reactions: itching, skin redness, fever, anaphylaxis.

Local reactions: pain at the injection site.

All described side effects are usually moderate in severity and disappear after the end of the course of treatment.

Contraindications

• Hormone-independent prostate carcinoma;
• Pregnancy;
• Lactation period (breastfeeding);
• Childhood;
• Hypersensitivity to triptorelin or other components of the drug.

With caution, Decapeptyl Depot should be prescribed when performing an assisted reproductive technology program (IVF) to patients with polycystic ovary syndrome, especially in cases where the number of follicles determined by ultrasound is more than 10, as well as to patients with clinical manifestations of osteoporosis or a high risk of its development.

Use in Pregnancy and Lactation

The use of Decapeptyl Depot during pregnancy is contraindicated.

Breastfeeding should be discontinued during treatment.

Pediatric Use

Contraindication: childhood.

Special Precautions

When used in men

During the treatment of hormone-dependent prostate cancer in the presence of metastases in the spine and/or urinary disorders, the start of treatment may be accompanied by a temporary exacerbation of the symptoms of the underlying disease: difficulty urinating, bone pain, symptoms of spinal cord compression, muscle tension, leg swelling. If these symptoms appear, you should consult a doctor. Antiandrogen drugs can be used as additional therapy to alleviate the initial exacerbation of the symptoms of the underlying disease.

When used in women

Before treatment, an examination should be performed to exclude a possible pregnancy at the time of starting therapy.

Uterine fibroids and endometriosis

Treatment of uterine fibroids should be carried out under ultrasound control, since a rapid decrease in the size of the uterus can, in some cases, lead to the development of uterine bleeding. During treatment, amenorrhea occurs; 7-12 weeks after the last injection, ovarian function is restored. If regular menstruation persists during treatment, you should consult a doctor.

It seems appropriate to combine therapy with Decapeptyl Depot with subsequent surgical treatment. Prescribing the drug leads to a significant reduction in the size of the myomatous uterus, which facilitates the surgical technique, and in some cases allows for organ-preserving surgical intervention using laparoscopic techniques to preserve reproductive function, which is especially important in young patients.

Throughout the entire course of treatment until the onset of menstruation after its completion, only non-hormonal methods of contraception should be used. The use of estrogen-containing drugs is not recommended.

Due to the possible effect on bone density, the duration of treatment for women with endometriosis or uterine fibroids should not exceed 6 months.

Infertility, assisted reproductive technologies (IVF)

Decapeptyl Depot is prescribed to stabilize the level of endogenous sex hormones with the subsequent administration of exogenous gonadotropins to stimulate follicle growth. The use of Decapeptyl Depot avoids premature spontaneous luteinization of stimulated follicles, which increases the effectiveness of the IVF program as a whole. Since the use of Decapeptyl Depot can lead to ovarian hyperstimulation, regular clinical monitoring, including ultrasound monitoring, is necessary. Cases of multiple pregnancy after treatment with Decapeptyl Depot have been described.

Overdose

No cases of overdose of Decapeptyl Depot have been reported.

Drug Interactions

Drug interactions of Decapeptyl Depot with other drugs have not been described.

Storage Conditions

The drug should be stored in a dry place, out of the reach of children, at a temperature of 2°C (35.6°F) to 8°C (46.4°F).

Shelf Life

Shelf life – 3 years. Do not use after the expiration date.

For the prepared suspension, the shelf life is 3 minutes.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.