Dekapeptil DEPOT

Active material: Triptorelin
When ATH: L02AE04
CCF: An analogue of gonadotropin-releasing hormone – depot
ICD-10 codes (testimony): C61, D25, N80, N97, Z31.1
When CSF: 15.07.04.01
Manufacturer: FERRING GmbH (Germany)

Pharmaceutical form, composition and packaging

Valium for drug suspensions / m and p / to the introduction of prolonged action as a powder or porous mass of white or light-yellow; enclosed solvent – colorless or light yellow liquid with a characteristic odor of polysorbate 80.

Excipients: a copolymer of lactic and glycolic acids, propylene kaprilokaprat.

Solvent: polysorbate 80, dextran 70, sodium chloride, sodium dihydrogen phosphate dihydrate, Sodium hydroxide, water d / and.

Syringe volume 2.25 ml (1) together with the solvent (disposable syringes 1 ml 1 PC.), The connecting element (1 PC.) and needles etc. and / (1 PC.) – packs cardboard.

Pharmacological action

The active ingredient of the drug depot Dekapeptil – triptorelin – synthetic analog of gonadotropin-releasing hormone (GnRG). The result of the replacement of the 6th amino acid residue of natural GnRH molecule is more pronounced affinity for the GnRH receptor and longer, than that of the native molecule, half life.

The initial effect of administration Dekapeptil depot is to stimulate the secretion of pituitary FSH and LH. After a prolonged stimulation (triptorelin constant concentration in the blood) pituitary becomes insensitive to the action of GnRH. This reduces the level of gonadotropin in the blood, resulting in lower levels of sex hormones to menopausal levels or postcastration. These effects are reversible.

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.

Absorption

In the first hours after the / m injection depot Dekaleptil registered C_max triptorelin plasma, markedly reduced during 24 no. On the 4th day after the / m injection of triptorelin concentration in the blood reaches the second peak, after which the concentration decreases in order to biekspanentsialnom nulls for 44 days.

After n / k administration increased concentration of active ingredient is slower compared to the / m. Lowering the concentration of triptorelin in the blood is slower, duration to reduce the concentration of nulls 65 days.

Repeated, at intervals of 28 days, Dekapeptil depot injections, do not lead to an increase in its concentration in the blood. When the / m and s / to a concentration of triptorelin in the blood on the eve of injection was reduced to 85 pg / ml 100 pg / ml, respectively.

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

In women through 27 day study, average determined 35.7% from the originally administered dose, wherein 25.5% the dose is released in the first 13 days, followed by linear release, average, by 0.73% of the administered dose daily.

Deduction

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

Testimony

Women

- Endometriosis;

- Uterine fibroids;

- Treatment of infertility using assisted reproductive technologies (IVF).

Men

- Hormone-dependent prostate carcinoma.

Dosage regimen

The drug is administered depot Dekapeptil n / a (in n / a fat belly) or / m 1 once every 4 of the week. Injection site should be changed.

At uterine fibroids and endometriosis the drug is administered 1 once every 4 of the week, Treatment starts on the first 5 days of the menstrual cycle, the duration of treatment 3 to 6 Months.

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

At hormone-dependent prostate carcinoma – 1 once every 4 of the week, protractedly.

Rules of administration

1. Take the packaging of the drug depot from the refrigerator Dekapeptil.

2. Remove the cap from the syringe with a lyophilisate.

3. Open the package with an adapter, without removing it.

4. Screw the syringe with a lyophilisate on the adapter and remove it from the package.

5. Screw the syringe with the solvent in the free edge of the adapter and to ensure a tight fit syringes with an adapter.

6. The distilled solvent in a syringe with lyophilized and then surpass the mixture in the opposite direction. Distill at least 10 time. The mixture should be gently distill between the two syringes until a homogeneous milky suspension. Do not perform the first 2-3 playout to the total displacement of fluid from one syringe to another.

Side effect

On the part of the reproductive system: side effects caused by a decrease in the level of sex hormones (testosterone and estrogen) in blood, which can lead to the appearance of men and women symptoms such as mood lability, depression, the weakening of the libido, frequent headaches, sleep disturbance, weight gain, tides, increased sweating, nausea, decreased appetite, mialgii, artralgii, bone demineralization (Propafenone); female – dryness of the vaginal mucosa, uterine bleeding; males – reduced potency, gynecomastia, reducing the size of the testicles.

Laboratory findings: rarely – men and women may experience elevated liver transaminases (LDH, GGT, GOLD, ACT), plasma cholesterol.

Allergic reactions: itch, erythema, fever, anaphylaxis.

Local reactions: pain at the site of administration.

All of the side effects tend to have moderate severity and disappear after treatment.

Contraindications

- Prostate cancer gormononezavisimaâ;

- Pregnancy;

- Lactation (breast-feeding);

- Children's age;

- Hypersensitivity to triptorelin or other ingredients.

FROM caution should be prescribed Dekapeptil depot when the program of assisted reproductive technologies (IVF) patients with polycystic ovaries particularly in cases, when the number of follicles, determined using ultrasound, better 10, and patients with clinical manifestations of osteoporosis or a high risk of developing.

Pregnancy and lactation

Use of the drug Dekapeptil depot during pregnancy is contraindicated.

During treatment should stop breastfeeding.

Cautions

When using male

In the treatment of hormone-dependent prostate cancer in the presence of metastases in the spine and / or urinary disorders treatment can be accompanied by a temporary exacerbation of the symptoms of the underlying disease: difficulty urinating, ostealgias, Symptoms of spinal cord compression, feeling of tension in the muscles, swelling of the feet. In case of these symptoms should see a doctor. As an additional therapy can be used anti-androgen drugs to facilitate an initial exacerbation of symptoms of the underlying disease.

When applied in women

Before treatment is necessary to conduct a study in order to avoid a possible pregnancy at the time of initiation of therapy.

Uterine fibroids and endometriosis

Treatment of uterine fibroids should be under the control of US, because the rapid reduction in the size of the uterus can, in some cases, can lead to uterine bleeding. During treatment, there is amenorrhea, after 7-12 weeks after the last injection, ovarian function is restored. When, If during treatment with regular menstruation Reserved, should see a doctor.

It seems appropriate combination therapy Dekapeptilom depot followed by surgery. The appointment of the drug leads to a significant reduction in the size of uterine myoma, which facilitates the operation technique, and in some cases it allows you to perform organ-surgery using laparoscopic techniques for the preservation of reproductive function, which is especially important in young patients.

During the course of treatment until the appearance of menstruation after it should be used only hormonal methods of contraception. Using estrogensoderjath drugs is not recommended.

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

Infertility, assisted reproductive technologies (IVF)

Dekapeptil depot assigned in order to stabilize the level of endogenous sex hormones, followed by administration of exogenous gonadotropins to stimulate the growth of follicles. Use of the drug depot Dekapeptil avoids premature spontaneous luteal stimulated follicles, which increases the efficiency of the IVF program as a whole. Because, that the use of the drug depot Dekapeptil may cause ovarian hyperstimulation, requires regular clinical monitoring, including monitoring of ultrasound. Described multiple pregnancies after treatment Dekapeptilom depot.

Overdose

No cases of overdose were reported Dekapeptil depot.

Drug Interactions

Drug interaction Dekapeptil drug depot with other medicines are not described.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored in a dry, inaccessible to children at 2 ° to 8 ° C. Shelf life – 3 year. Do not use after the expiry date.

To the suspension was shelf life – 3 minutes.