antitumor agent – gonadotropin-releasing hormone analog.
The pharmacological action of
antitumor agents. It has antigonadotropnym action
Active substance depot preparation Dekapeptil – Testosterone sustanon, which is a synthetic analog of gonadotropin-releasing hormone. Changing the second amino acid residue in the molecule, releasing natural resulted in a greater affinity for the GnRH receptor and more prolonged than the native molecule, its half-life.
The initial effect of administration is a depot Dekapeptil pituitary secretion of follicle stimulating hormone and luteinizing hormone. After prolonged stimulation (constant concentration Testosterone sustanon blood) pituitary becomes insensitive to the action of GnRH, resulting in reduced gonadotropin levels in the blood with the consequent reduction in the level of hormones in the blood to postcastration or menopausal levels.
These effects are reversible.
Animal studies revealed no teratogenic or mutagenic effect. Pharmacokinetics pharmacokinetic tests were performed on a patient 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 injection depot Dekapeptil recorded the highest level of Testosterone sustanon concentration in blood plasma. Then Testosterone sustanon concentration decreases markedly within 24 hours. On the 4th day after injection Testosterone sustanon concentration in the blood reaches the second peak, followed by concentration decreases in a biexponential manner to undetectable levels within 44 days. Following subcutaneous administration, lowering blood Testosterone sustanon concentration is slower duration lower concentrations to undetectable levels of 65 days. The repeated at intervals of 28 days, the drug depot injection Dekapeptil not lead to an increase in its concentration in the blood. Intramuscular and subcutaneous administrations Testosterone sustanon blood eve of injection was reduced to a level of 85 pg / ml and 100 pg / ml – respectively. In men, the constant bioavailability of the active ingredient – of Testosterone sustanon depot is 38.3% in the first 13 days. Next, release the drug becomes linear with an average daily value -. 0.92% of the administered dose in women after 27 days of the study, an average of 35.7% is determined by initially administered dose, with 25.5% of the dose is released in the first 13 days followed by a linear evolution, on average, 0.73% of the administered daily dose. the half-life in plasma Testosterone sustanon – 18.7 min, and for natural gonadotropin-releasing hormone, the figure of 7.7 minutes. Testosterone sustanon clearance (503 mL / min) 3 times slower than that of the natural hormone releasing (1766 ml / min) and consists of two components -. Fast and slow clearance than 4% Testosterone sustanon unaltered excreted in urine.
Indications for use:
– uterine fibroids
– treatment of infertility using assisted reproductive technologies (IVF) In men: – hormone-dependent prostate carcinoma.
– Hypersensitivity to Testosterone sustanon, other ingredients of the drug and solvent
– Children’s age
– hormone-cell carcinoma of the prostate
should be prescribed the drug depot Dekapeptil when the program of assisted reproductive technologies (IVF) patients with polycystic ovaries particularly in cases where the number of follicles, as determined by ultrasound, more than 10, as well as patients with clinical manifestations of osteoporosis or at high risk for its development.
Pregnancy and lactation
The drug is contraindicated in pregnancy, breast-feeding should be discontinued during treatment.
Dosing and Administration
The drug depot Dekapeptil injected subcutaneously (into the subcutaneous tissue of the abdomen) or intramuscularly 1 every 4 weeks. Injection site should be changed. Uterine fibroids and endometriosis: 1 every 4 weeks, treatment is initiated in the first 5 days of the menstrual cycle, duration of treatment 3 to 6 months. Assisted reproductive technologies (IVF): once at 2-3 or 22 days . menstrual Hormone-dependent carcinoma of the prostate: 1 every 4 weeks, for a long time. it is necessary to observe the following instructions: – control the packaging of the drug Dekapeptil depot from the refrigerator; – remove the cap from the syringe with a lyophilisate; – open the package with the adapter without removing it; – screw syringe with a lyophilisate on the adapter and remove it from its packaging; – screw the syringe with the solvent on the free edge of the adapter and make sure the connection density syringes with an adapter
The mixture should be gently distill between the two syringes until a homogeneous milky suspension. Should not be performed before the driving of the first 3/2 of the total displacement of fluid from one syringe to another.
Side effects are due to a decrease in the level of sex hormones (testosterone and estrogen) in the blood, which can lead to the appearance of men and women symptoms such as: mood lability, depression, weakening of libido, frequent headaches, sleep disorders, weight gain, ” tides “, increased sweating, nausea, decreased appetite, myalgia, arthralgia, bone demineralization (chronic administration); women: dryness of the vaginal mucosa, uterine bleeding; men:. decreased potency, gynecomastia, decrease testicular size
Rarely laboratory (men and women) may experience increased activity of “liver” transaminases (LDH, GGT, ALT, the ACT) and cholesterol in the blood plasma.
may also be observed hypersensitivity reactions ( itching, redness, fever, anaphylaxis), possible complaints of pain in the injection site.
All these side effects tend to have moderate severity and disappear after treatment.
Cases of overdose have not been described.
Interactions with other medicinal products
are not described.
Cautions In applying the men in the treatment of hormone dependent prostate cancer in the presence of metastases in the spine and / or urination disorders initiation of treatment may be associated with temporary worsening of the symptoms of the underlying disease: difficulty urinating, pain in bones, symptoms of spinal cord compression, a sense of tension in the muscles, swelling of the legs. In the case of the appearance of these symptoms should seek medical advice. 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 exclude the possibility of pregnancy at the time of initiation of therapy.
Uterine fibroids and endometriosis
treatment of uterine fibroids should be under the control of US (ultrasound) as a rapid decrease in size of the uterus can, in some cases, can lead to uterine bleeding. During treatment occurs amenorrhea, after 7-12 weeks after the last injection of ovarian function is restored. If during treatment with regular menstruation should persist, seek medical advice.
It seems appropriate combination therapy Dekapeptilom depot followed by surgery. Appointment of the drug leads to a significant reduction of myoma size of the uterus, which facilitates equipment operation, and in some cases 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 applied only to non-hormonal methods of contraception. The use of estrogen-containing medicinal products is not recommended.
Because of the possible effects on bone density, duration of the treatment of women with endometriosis or uterine fibroids should not exceed 6 months.
Infertility, assisted reproductive technologies (IVF)
Dekapeptil depot is appointed in order to stabilize the level of endogenous sex hormones, followed by administration of exogenous gonadotropins to stimulate follicle growth. Application Dekapeptil depot formulation avoids premature spontaneous luteal stimulated follicles, which increases the efficiency of the IVF program as a whole. Due to the fact that the use of the drug depot Dekapeptil may cause ovarian hyperstimulation, requires regular clinical monitoring, including ultrasound monitoring.
Described multiple pregnancies after treatment Dekapeptilom depot.
The lyophilisate for suspension for intramuscular and subcutaneous administration of 3.75 mg of depot.
According 3.75 mg of the active substance in a disposable syringe 2.25 ml volume 1 ml of solvent in a disposable syringe.
By syringe 1 with the drug and the syringe 1 with solvent with the connecting element and the needle for injection in blisters in a cardboard package with instructions for use.