Decapeptil Depot - instructions for use, doses, side effects, contraindications

active substance: tryptorelin acetate 4.12 mg (corresponding to 3.75 mg of triptorelin); auxiliary substances: lactic and glycolic acid copolymer, propylene glycol caprilocaprate

Solvent

Polysorbate 80, dextran 70, sodium chloride, sodium dihydrogen phosphate dihydrate, sodium hydroxide, water for injection

Description:

The contents of the syringe with the active substance is a lyophilized powder or a porous mass of white or light yellow color

The contents of the syringe with the solvent is a colorless or pale yellow liquid with a characteristic smell of polysorbate 80.

Pharmacotherapeutic group:Antitumor agent - gonadotropin-releasing hormone analog

ATX: & nbsp

L.02.A.E.04 Triptorelin

Pharmacodynamics:The active substance of the drug Decapeptal Depot - tryptorelin, which is a synthetic analogue of gonadotropin-releasing a hormone. The replacement of the 6th amino acid residue in the natural releasing molecule resulted in a more pronounced affinity for the GnRH receptors and a longer half-life than the natural molecule.

The initial effect of the drug Decapeptil Depot is stimulation of the pituitary gland by follicle-stimulating hormone and luteinizing hormone. After prolonged stimulation (constant concentration of triptorelin in the blood), the pituitary gland becomes insensitive to the action of GnRH, which leads to a decrease in the level of gonadotropins in the blood, followed by a decrease in the level of sex hormones in the blood to the post-cystic or menopausal level. The effects described are reversible.

Studies in animals have not revealed a teratogenic or mutagenic effect.

Pharmacokinetics:

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

In the first hours after intramuscular administration of the drug Decapeptil Depot, the maximum concentration of triptorelin in the blood plasma is recorded. Then, the concentration of tryptorelin decreases markedly within 24 hours. On the 4th day after the injection, the concentration of tryptorelin in the blood reaches the second maximum, after which the concentration decreases in the bi-exponential order to undetectable values for 44 days.

After subcutaneous administration, the decrease in the concentration of tryptorelin in the blood is slower, the duration of the decrease in concentration to undetectable values is 65 days ..

Repeated, with an interval of 28 days, injections of the drug Decapeptil Depot, do not lead to an increase in its concentration in the blood. With intramuscular and subcutaneous injections, the content of tryptorelin in the blood on the eve of the next injection was reduced to 85 pg / ml and 100 pg / ml, respectively.

In men, the constant bioavailability of the active ingredient - 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 initial dose is administered, with 25.5% of the dose being released in the first 13 days, followed by a linear release, on average, 0.73% of the administered dose daily.

The half-life of triptorelin in plasma is 18.7 min, while for natural gonadotropin-releasing hormone this figure is 7.7 min. Triptorelin's clearance (503 ml / min) is 3 times slower than the natural releasing hormone (1766 ml / min) and consists of two components - fast and slow elimination.

Less than 4% of triptorelin in unchanged form is excreted in the urine.

Indications:

Among women:

- endometriosis, confirmed by laparoscopy

- fibroids of the uterus (before surgery, to reduce bleeding and pain)

- Infertility treatment with the use of assisted reproductive techniques (in vitro fertilization)

In men:

- hormone-dependent carcinoma of the prostate

Children:

premature puberty of the central genesis

Contraindications:

- hypersensitivity to triptorelin, any other components of the drug and the solvent

- pregnancy

- Breastfeeding period

- adolescence (boys over 13, girls over 12)

- hormone-independent carcinoma prostate cancer.

Carefully:

Caution should be given to the preparation of Decapeptil Depot when performing an assisted reproductive technology (IVF) program for patients with polycystic ovaries, especially when the number of ultrasound detected follicles is more than 10, as well as patients with clinical manifestations of osteoporosis or a high risk of its development.

Pregnancy and lactation:

The drug is contraindicated for use in pregnancy, at the time of treatment should stop breastfeeding.

Dosing and Administration:

The drug Decapeptil Depot is administered subcutaneously (in the abdomen, thighs or buttocks) or deep intramuscularly once in 4 weeks. Place the drug should be changed.

Fibromyoma of the uterus and endometriosis:

for 3.75 mg of the drug once in 4 weeks, treatment is started in the first 5 days of the menstrual cycle, the duration of treatment is 3 to 6 months.

Auxiliary reproductive technologies (extracorporeal fertilization):

3.75 mg of the drug 1 time on the 2nd or 3rd or 22nd days of the menstrual cycle.

Hormone-dependent carcinoma of the prostate glands:

3.75 mg of the drug every 4 weeks, for a long time.

Premature sexual maturation of the central genesis:

in the first month of therapy once in the 1st, 14th and 28th day. Then 1 time in 3-4 weeks. The dose is selected individually, taking into account the body weight:

Body mass	The dose of Decapeptal Depot
<20 kg	1.875 mg (1/2 dose)
20 - 30 kg	2.5 mg (2/3 of the dose)
> 30 kg	3.75 mg (1 dose)

Treatment continues until the age of 13 years in boys and 12 years in girls.

Preparation of the solution:

- get the package of the drug Decapeptil Depot from the refrigerator;

- remove the cap from the syringe with lyophilizate;

- open the packing of the adapter, without removing him;

- screw the syringe with the lyophilizate onto the adapter and remove it from the package;

- Screw the syringe with the solvent onto the free edge of the adapter. The syringe must be firmly connected to the adapter.

Overtake solvent syringe with lyophilizate and then distill the mixture in the opposite direction (at least 10 times).

The mixture should be carefully distilled between the two syringes until a homogeneous milk-like suspension is formed.Do not perform the first 2-3 distillations until the fluid is completely transferred from one syringe to the other.

Side effects:

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 symptoms such as mood lability, depression, weakening of libido, frequent headaches, sleep disorders, weight gain, "hot flashes" , increased sweating, nausea, decreased appetite, myalgia, arthralgia, bone demineralization (with prolonged admission); in women: dryness of the vaginal mucosa, uterine bleeding; in men: a decrease in potency, gynecomastia, a decrease in the size of the testicles.

Rarely laboratory (in men and women) there may be increased activity of "liver" transaminases (LDH, GGTP, ALT, ACT) and cholesterol in the blood plasma.

Also, there may be reactions of hypersensitivity (itching, redness of the skin, fever, anaphylaxis), there may be complaints of pain at the injection site.

All described side effects tend to have a moderate degree of severity and disappear after the course of treatment.

Overdose:

Cases of overdose are not described.

Interaction:

Not described.

Special instructions:

When used in men

In the treatment of hormone-dependent prostate cancer in the presence of metastases in the spine and / or urination disorders, the onset of treatment may be accompanied by a temporary exacerbation of the symptoms of the underlying disease: difficulty urination, bone pain, spinal cord compression symptoms, tension in the muscles, swelling of the legs. In case of these symptoms, you should see a doctor. As an additional therapy, antiandrogen preparations can be used to relieve the initial exacerbation of the symptoms of the underlying disease.

When used in women

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

Uterine fibroids and endometriosis

Treatment of uterine fibroids should be carried out under the supervision of ultrasound (ultrasound), because 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 to 12 weeks after the last injection, the function of the ovaries is restored.In the event that the treatment persists regular menstruation should consult a doctor.

It seems advisable to combine therapy with Decapeptal Depot with subsequent surgical treatment. Appointment of the drug leads to a significant decrease in the size of the myomatous uterus, which facilitates the technique of surgery, and in some cases allows performing an organ-saving surgical procedure with laparoscopic technique to preserve reproductive function, which is especially important in young patients.

Throughout the course of treatment until the appearance of menstruation after its termination, only non-hormonal methods of contraception should be used. The use of estrogen-containing medications is not recommended.

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

Infertility, assisted reproductive technologies (in vitro fertilization)

Decapeptil Depot is appointed with the goal of stabilizing the level of endogenous sex hormones with the subsequent appointment of exogenous gonadotropins to stimulate the growth of follicles.The use of the drug Decapeptil depot avoids the 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 Decapeptil Depot can lead to ovarian hyperstimulation, regular clinical monitoring, including monitoring of ultrasound, is necessary. Multiple pregnancies after treatment with Decapeptal Depot are described.

Form release / dosage:

Lyophilizate for the preparation of suspensionfor intramuscular and subcutaneous injectionth administration of prolonged3.75 mg.

Packaging:

For 3.75 mg of active substance per onea single syringe with a volume of 2.25 ml.

1 ml of solvent in a single-use syringe. 1 syringe with active substanceand 1 syringe with a solvent together with the connecting element and 2 needles for injection in a contour cellpackaging in a cardboard package withstructure on the application inside.

Storage conditions:

At a temperature of 2 to 8 ° C in a dry place inaccessible to children.

Shelf life:

3 years. Do not use after the expiration date.

For the prepared suspension - 3 minutes.

Terms of leave from pharmacies:On prescription

Registration number:P N008612

Date of registration:22.10.2008 / 19.08.2016

Expiration Date:Unlimited

The owner of the registration certificate: Ferring GmbH Ferring GmbH Germany

Manufacturer: & nbsp

FERRING, GmbH Germany

Representation: & nbspFERRING PHARMACEUTICALS LLCFERRING PHARMACEUTICALS LLCRussia

Information update date: & nbsp20.03.2017

Illustrated instructions

Instructions

Decapeptil Depot (Decapeptyl depot)