Dekapeptil of depot

General characteristics. Structure:

Active agent: a triptorelina acetate of 4.12 mg that corresponds to the maintenance of a triptorelin of 3.75 mg

Excipients: copolymer of milk and glycolic acids, propylene glycol каприлокапрат.

Solvent: polysorbate 80, a dextran 70, sodium chloride, dihydrophosphate sodium a dihydrate, sodium hydroxide, water for and.

Pharmacological properties:

Active ingredient of drug Dekapeptil of depot - трипторелин - a synthetic analog a gonadotrophin-rileasing of hormone (GNRG). In a molecule of natural GNRG more expressed affinity to receptors of GNRG and longer, than at a natural molecule, half-life is result of replacement of the 6th amino-acid rest.
Initial effect of administration of drug Dekapeptil of depot is secretion stimulation a hypophysis of FSG and LG. After long stimulation (constant concentration of a triptorelin in blood) the hypophysis becomes insensitive to action of GNRG. As a result the level of gonadotrophins in blood decreases that leads to decrease in level of sex hormones to postkastratsionny or menopauzny level. The described effects are reversible.

Pharmacokinetics. Pharmacokinetic tests were carried out on patients with the confirmed diagnosis of endometriosis or a hysteromyoma, patients with a carcinoma of a prostate and healthy male volunteers.

Absorption. During the first hours after administration of drug in oil Dekaleptil of depot is registered Cmax of a triptorelin in a blood plasma considerably decreasing during 24 h. For the 4th day after an injection in oil concentration of a triptorelin in blood reaches the second maximum after which concentration decreases in a biekspanentsialny order to uncertain values for 44 days.
After п / to introduction increase in concentration of active ingredient happens more slowly in comparison with introduction in oil. Decrease in concentration of a triptorelin in blood happens more slowly, duration of decrease in concentration to uncertain values makes 65 days.
Repeated, at an interval of 28 days, a drug injection Dekapeptil depots, do not lead to increase in its concentration in blood. At in oil and п / to introductions concentration of a triptorelin in blood on the eve of the next injection decreased to 85 pg/ml and 100 pg/ml respectively.

At men constant biological availability of active component of a triptorelin makes 38.3% in the first 13 days of depot. Further release of drug becomes linear with average daily value of 0.92% of the entered dose.

Women in 27 days have researches, 35.7% of originally entered dose on average are defined, at the same time 25.5% of a dose are released in the first 13 days with the subsequent linear allocation, on average, on 0.73% of the entered dose daily.

Removal. Half-life of a triptorelin in plasma - 18.7 min., at the same time for natural a hormone gonadotrophin-rileasing this indicator makes 7.7 min. The clearance of a triptorelin (503 ml/min.) by 3 times more slowly, than at natural a hormone rileasing (1766 ml/min.) also consists of two components - bystry and slow removal. Less than 4% of a triptorelin in not changed look are removed with urine.

Indications to use:

For women
— endometriosis;
— hysteromyoma;
— treatment of infertility using auxiliary reproductive technologies (including EKO and PE/transfer of an embryo/).

For men

— a symptomatic treatment of the progressing hormonedependent carcinoma of a prostate.

Route of administration and doses:

Dekapeptil depots administer the drug п / to (in п / to stomach cellulose) or 1 time in oil in 4 weeks. The injection site of drug should be changed.

At a hysteromyoma and endometriosis the drug is administered 1 time in 4 weeks, treatment is begun in the first 5 days of a menstrual cycle, duration of treatment from 3 to 6 months.

At auxiliary reproductive technologies (EKO) - once for the 2-3 or 22 days of a menstrual cycle.

At a hormonedependent carcinoma of a prostate - 1 time in 4 weeks, it is long.

Rules of administration of drug
1. To get drug packaging Dekapeptil of depot from the refrigerator.
2. To remove a cap from the syringe with lyophilisate.
3. To open packaging from an adapter, without taking it.
4. To screw the syringe with lyophilisate on an adapter and to take it from packaging.
5. To screw the syringe with solvent on free edge of an adapter and to be convinced of density of connection of syringes with an adapter.
6. To overtake solvent in the syringe with lyophilisate and then to overtake mix in the opposite direction. To overtake not less than 10 times. Mix should be overtaken carefully between two syringes before formation of homogeneous molokoobrazny suspension. It is not necessary to carry out the first 2-3 stages before full movement of liquid from one syringe in another.

Features of use:

At use for men

In the course of treatment of a hormonedependent prostate cancer in the presence of metastasises in a backbone and/or disturbances of an urination the initiation of treatment can be followed by a temporary aggravation of symptoms of a basic disease: difficulty of an urination, ostealgia, symptoms of a prelum of a spinal cord, feeling of tension in muscles, puffiness of legs. In case of these symptoms it is necessary to see a doctor. As additional therapy drugs of anti-androgens for the purpose of simplification of an initial aggravation of symptoms of a basic disease can be used.

At use for women

Before treatment it is necessary to conduct a research for the purpose of an exception of possible pregnancy at the time of the beginning of therapy.

Hysteromyoma and endometriosis

Treatment of a hysteromyoma should be carried out under ultrasonography control as bystry reduction of the sizes of a uterus can, in certain cases, can lead to development of uterine bleeding. During treatment there is an amenorrhea, 7-12 weeks later after the last injection function of ovaries is recovered. If against the background of treatment regular periods remain, it is necessary to see a doctor.

The therapy combination Dekapeptily depot with the subsequent surgical treatment is advisable. Purpose of drug leads to considerable reduction of the sizes of a myomatous uterus that facilitates technology of operation, and also in some cases allows to execute organosberegayushchy surgical intervention by means of the laparoscopic equipment for preservation of reproductive function that is especially important at young patients.

During all course of treatment up to emergence of periods after its termination it is necessary to apply only non-hormonal methods of contraception. Use of estrogensoderzhashchy medicines is not recommended.

Because of possible influence on density of a bone tissue, duration of treatment of women with endometriosis or a hysteromyoma should not exceed 6 months.

Infertility, auxiliary reproductive technologies (EKO)

Dekapeptil of depot is appointed for the purpose of stabilization of level of endogenous sex hormones with the subsequent purpose of exogenous gonadotrophins for the purpose of stimulation of growth of follicles. Drug use Dekapeptil of depot allows to avoid a premature spontaneous luteinization of stimulated follicles that increases efficiency of the EKO program in general. Because drug use Dekapeptil can lead depot to hyper stimulation of ovaries, regular clinical control, including ultrasonography monitoring is necessary. Cases of polycarpous pregnancy after treatment Dekapeptily depot are described.

Side effects:

From a reproductive system: side effects are caused by decrease in level of sex hormones (testosterone and estrogen) in blood that can lead to emergence in men and women of such symptoms as lability of mood, a depression, easing a libido, frequent headaches, a sleep disorder, increase in body weight, inflows, the increased perspiration, nausea, a loss of appetite, mialgiya, arthralgias, demineralization of bones (at long reception); women have a dryness of a mucous membrane of a vagina, uterine bleedings; men have a decrease in a potentiality, a gynecomastia, reduction of the sizes of testicles.

Laboratory indicators: seldom - at men and women a superactivity of hepatic transaminases (LDG, GGTP, ALT, ACT), increase in content of cholesterol in a blood plasma can be noted.

Allergic reactions: itch, erubescence, fever, anaphylaxis.

Local reactions: pain in a drug injection site.

All described side effects, as a rule, have moderate degree of manifestation and disappear after the termination of a course of treatment.

Interaction with other medicines:

Medicinal interaction of drug Dekapeptil by depot with other medicines is not described.

Contraindications:

— gormononezavisimy carcinoma of a prostate;
— pregnancy;
— period of a lactation (breastfeeding);
— children's age;
— hypersensitivity to a triptorelin or other components of drug.

With care patients should appoint drug Dekapeptil depot at implementation of the program of auxiliary reproductive technologies (EKO) with a polycystosis of ovaries, especially in cases when number of the follicles defined by ultrasonography more than 10, and also to patients with clinical displays of osteoporosis or high risk of its development.

Use of drug DEKAPEPTIL of DEPOT at pregnancy and feeding by a breast
Drug use Dekapeptil is contraindicated to depot at pregnancy.
During treatment it is necessary to stop breastfeeding.

Use for children
Contraindication: children's age.

Overdose:

Dekapeptil the depot was not reported about drug overdose cases.

Storage conditions:

Drug should be stored in the place, dry, unavailable to children, at a temperature from 2 °C to 8 °C.

Issue conditions:

According to the recipe

Packaging:

Lyophilisate for пригот. сусп. for in oil and п / to introduction пролонгир. actions of 3.75 mg: syringes in set. with solvent.