Composition, form of production and packaging
Lyophilizate for the preparation of a suspension for w / m and / or the introduction of prolonged action in the form of a powder or a porous mass of white or light yellow color; the applied solvent is a colorless or pale yellow liquid with a characteristic odor of polysorbate 80.
Triptorelin acetate 4.12 mg,
which corresponds to the content of triptorelin 3.75 mg
Excipients: copolymer of lactic and glycolic acids, propylene glycol caprylcaprate.
Solvent: polysorbate 80, dextran 70, sodium chloride, sodium dihydrogen phosphate dihydrate, sodium hydroxide, water d / u.
Syringes disposable in volume 2.25 ml (1) complete with a solvent (disposable syringes 1 ml 1 piece), connecting elements (1 pc.) And needles d / and (1 pc.) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2010.
The active substance of the drug Decapeptil Depot - tryptorelin - a synthetic analogue of gonadotropin-releasing hormone (GnRH). The result of the replacement of the 6th amino acid residue in the natural GnRH molecule is 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 secretion of FSH and LH. After prolonged stimulation (constant concentration of triptorelin in the blood), the pituitary 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-cystic or menopausal levels. The effects described are reversible.
Pharmacokinetic tests were performed on patients with a confirmed diagnosis of endometriosis or uterine fibroids, patients with prostatic carcinoma and healthy male volunteers.
In the first hours after intravenous administration of Decaleptyl Depot, Cmax of Triptorelin in the blood plasma is registered, markedly decreasing within 24 hours. On the 4th day after the intravenous injection the concentration of Triptorelin in the blood reaches the second maximum, after which the concentration decreases in bi-exponential order to undetermined values вЂ‹вЂ‹for 44 days.
After SC administration, an increase in the concentration of the active substance is slower in comparison with the IM injection. Lowering the concentration of triptorelin in the blood is slower, the duration of the decrease in concentration to undetermined values вЂ‹вЂ‹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 the / m and / / injections, 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 of 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, of 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.
- myoma of the uterus;
- Infertility treatment with the use of assisted reproductive technologies (IVF).
- hormone-dependent carcinoma of the prostate.
The drug Dekapeptil depot injected p / k (in n / to the cellular tissue of the stomach) or in / m 1 time in 4 weeks. Place the drug should be changed.
With uterine myoma and endometriosis, the drug is administered once in 4 weeks, treatment is started in the first 5 days of the menstrual cycle, and the duration of treatment is 3 to 6 months.
With assisted reproductive technologies (IVF) - once for 2-3 or 22 days of the menstrual cycle.
With hormone-dependent carcinoma of the prostate gland - 1 every 4 weeks, for a long time.
Rules of drug administration
1. Remove the Decapeptil Depot from the refrigerator.
2. Remove the cap from the syringe with the lyophilizate.
3. Open the package from the adapter without removing it.
4. Screw the syringe with lyophilizate onto the adapter and remove it from the package.
5. Screw the syringe with the solvent onto the free edge of the adapter and check the tightness of the connection of the syringes with the adapter.
6. Transfer the solvent to the syringe with the lyophilizate and then disperse the mixture in the opposite direction. Disturb 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.
On the part of the reproductive system: side effects due to 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 libido, frequent headaches, sleep disorders, weight gain , hot flashes, excessive sweating, nausea, decreased appetite, myalgia, arthralgia, demineralization of bones (with prolonged admission); women - dryness of the mucous membrane of the vagina, uterine bleeding; in men - a decrease in potency, gynecomastia, a decrease in the size of the testes.
Laboratory indicators: rarely - in men and women, there may be an increased activity of hepatic transaminases (LDH, GGTP, ALT, ACT), an increase in the cholesterol content 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, have a moderate degree of severity and disappear after the course of treatment.
- hormone-independent prostate carcinoma;
- the period of lactation (breastfeeding);
- hypersensitivity to triptorelin or other components of the drug.
Caution should be given to the preparation of Decapeptil Depot when performing an assisted reproductive technology (IVF) program for patients with polycystic ovary, especially when the number of ultrasound detected follicles is more than 10, as well as to patients with clinical manifestations of osteoporosis or a high risk of its development.
PREGNANCY AND LACTATION
The use of the drug Decapeptil Depot during pregnancy is contraindicated.
During treatment should stop breastfeeding.
APPLICATION FOR CHILDREN
Contraindication: children's age.
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 urinating, 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 initiation of therapy.
Uterine fibroids and endometriosis
Treatment of uterine fibroids should be performed under the supervision of 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 regular menstruation persists against the background of treatment, you should consult your 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 drugs 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 (IVF)
Decapeptil Depot is appointed to stabilize the level of endogenous sex hormones with the subsequent administration 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. The cases of multiple pregnancies after treatment with Decapeptal Depot are described.
No cases of an overdose of Decapeptil Depot were reported.
Drug interaction of the drug Decapeptil Depot with other medications is not described.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry place inaccessible to children at a temperature of 2 В° to 8 В° C. Shelf life - 3 years. Do not use after the expiration date.
For the prepared suspension, the expiration date is 3 minutes.