Decapeptil depot, 3.75mg

Pharmacodynamics

The active ingredient of Decapeptil Depot is triptorelin, a synthetic analog of gonadotropin-releasing hormone (GnRH). The result of replacing the 6th amino acid residue in the natural GnRH molecule is a more pronounced affinity for GnRH receptors and a longer half-life than that of the natural molecule.

The initial effect of administration of Decapeptil Depot is stimulation of pituitary FSH and LH secretion. After prolonged stimulation (constant concentration of tryptorelin in the blood) the pituitary gland becomes insensitive to the action of GnRH. As a result, the gonadotropin level in blood decreases, which leads to a decrease in the level of sex hormones to the post-castral or menopausal level. The effects described are reversible.

Pharmacokinetics

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

Absorption

In the first hours after intravenous administration of Decaleptil Depot, the C_max of triptorelin in plasma is recorded, decreasing markedly within 24 hours. On the 4th day after the intravenous injection, the concentration of tryptorelin in blood reaches a second maximum, followed by a biexpansential decrease in concentration to indeterminate values for 44 days.

The increase in the concentration of the active ingredient is slower after a p / n injection compared to a v / m injection. Decrease of the concentration of tryptorelin in blood is slower, the duration of decrease of concentration to undetermined values is 65 days.

Repeat injections of Decapeptil Depot at 28-day intervals do not increase its blood concentration. When injected v/m and p/c, the concentration of tryptorelin in the blood on the eve of the next injection decreased to 85 pg/ml and 100 pg/ml, respectively.

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

In women, after 27 days of 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, averaging 0.73% of the administered dose daily.

Elevation

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

Indications

For women:

endometriosis;
uterine fibroids;
infertility treatment using assisted reproductive technologies (IVF).

For men:

hormone-dependent prostate carcinoma.

Pharmacological effect

Pharmacodynamics

The active ingredient of Decapeptyl Depot is triptorelin, a synthetic analogue of gonadotropin-releasing hormone (GnRH). The result of replacing the 6th amino acid residue in the natural GnRH molecule is a more pronounced affinity for GnRH receptors and a longer half-life than the natural molecule.

The initial effect of administering the drug Decapeptyl Depot is the stimulation of the pituitary gland’s secretion of FSH and LH. 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, which leads 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 patients with a confirmed diagnosis of endometriosis or uterine fibroids, patients with prostate carcinoma and healthy male volunteers.

Suction

In the first hours after the intramuscular injection of the drug Dekaleptil depot, the Cmax of triptorelin in the blood plasma is recorded, which decreases noticeably within 24 hours. On the 4th day after the intramuscular injection, the concentration of triptorelin in the blood reaches the second maximum, after which the concentration decreases in a bi-exponential order to undetermined 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 triptorelin concentration in the blood occurs more slowly, the duration of the decrease in concentration to undetermined values ​​is 65 days.

Repeated injections of the drug Decapeptyl depot, with an interval of 28 days, do not lead to an increase in its concentration in the blood. With IM and SC administrations, 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 bioavailability of the active component triptorelin from the depot is 38.3% in the first 13 days. Thereafter, drug release 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 was detected, with 25.5% of the dose released in the first 13 days, followed by a linear release of an average of 0.73% of the administered dose daily.

Removal

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 natural releasing hormone (1766 ml/min) and consists of two components – fast and slow clearance. Less than 4% of triptorelin is excreted unchanged in the urine.

Special instructions

When used in men

During the treatment of hormone-dependent prostate cancer in the presence of metastases in the spine and/or urination disorders, the beginning 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, a feeling of tension in the muscles, swelling of the legs. If these symptoms occur, you should consult a doctor. Antiandrogen drugs can be used as additional therapy to alleviate the initial exacerbation of symptoms of the underlying disease.

When used in women

Before treatment, it is necessary to conduct a study to exclude possible pregnancy at the time of initiation of therapy.

Uterine fibroids and endometriosis

Treatment of uterine fibroids should be carried out under ultrasound guidance, 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 continues during treatment, you should consult a doctor.

It seems appropriate to combine therapy with Decapeptyl depot followed by surgical treatment. The administration of 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-sparing surgery using laparoscopic techniques to preserve reproductive function, which is especially important in young patients.

During 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 medications 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, followed by the administration of exogenous gonadotropins to stimulate follicular growth. The use of the drug Decapeptil Depot allows you to avoid premature spontaneous luteinization of stimulated follicles, which increases the effectiveness of the IVF program as a whole. Due to the fact that the use of Decapeptyl Depot can lead to ovarian hyperstimulation, regular clinical monitoring, including ultrasound monitoring, is necessary. Cases of multiple pregnancies after treatment with Decapeptyl depot have been described.

Active ingredient

Triptorelin

Composition

1 syringe contains:

Active substances:

triptorelin acetate 4.12 mg, which corresponds to the content of triptorelin 3.75 mg.

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 injection.

Contraindications

Hormone-independent prostate carcinoma;
pregnancy;
lactation period (breastfeeding);
childhood;
hypersensitivity to triptorelin or other components of the drug.

With caution: the drug Decapeptyl Depot should be prescribed during an assisted reproductive technology (IVF) program 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.

Side Effects

From the reproductive system: side effects are caused by a decrease in the level of sex hormones (testosterone and estrogens) in the blood, which can lead to the appearance in men and women of such symptoms as mood lability, depression, weakened libido, frequent headaches, sleep disturbances, weight gain, hot flashes, increased sweating, nausea, loss of appetite, myalgia, arthralgia, bone demineralization (with prolonged reception); in women – dryness of the vaginal mucosa, uterine bleeding; in men – decreased potency, gynecomastia, decreased testicular size.

Laboratory indicators: rarely – in men and women there may be increased activity of liver transaminases (LDH, GGTP, ALT, AST), an increase in cholesterol levels in the blood plasma.

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

Local reactions: pain at the injection site. All described side effects, as a rule, are of moderate severity and disappear after completion of the course of treatment.

Interaction

Drug interactions between Decapeptyl Depot and other medications have not been described.

Overdose

No cases of overdose of Decapeptyl Depot have been reported.

Storage conditions

Store in a dry place, out of reach of children, at a temperature of 2° to 8°C.

Shelf life

3 years.

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

Manufacturer

Ferring GmbH, Germany