Decapeptil Depot

Antitumor medication Decapeptyl Depot - Decapeptil Depot - antigonadotropic agent, agonist hormone-releasing gonadotropin. The active ingredient of the medication is tryptorelin.

Decapeptil depot is released and used strictly according to the doctor's prescription.

[1], [2], [3], [4]

Indications of the decapeptal Depot

For female patients, a medication can be prescribed for:

• endometrioid sprouting;
• fibromyoma, leiomyoma of the uterus;
• as one of the components of the IVF protocol for problems with conception of the child.

 To male patients:

• for the treatment of hormone-dependent prostate cancer.

[5], [6]

Release form

Dekapeptil depot is available in a lyophilized form provided for the manufacture of a solution for / m or n / k injections. It is characterized by prolonged (longer) exposure.

 The active ingredient of the medication is tryptorelin acetate 0.00412 g (equivalent to 3.75 mg of triptorelin).

 Additional components: copolymers of hydroxypropionic (ethylidene-milk) and hydroxyacetic acids, caprylocaprate-propylene glycol.

 The solution for dilution of the lyophilized mass is represented by: Tween-80, Dextran 70, sodium chloride, sodium dihydrophosphate, sodium hydroxide, caustic soda, sterile water d / a.

 In the package there are 2 filled syringes, one of which contains a lyophilized mass of light shade, and the second - a solvent, gently yellowish or neutral shade.

[7], [8], [9], [10]

Pharmacodynamics

The active ingredient of triptorelin is a synthesized agonist hormone-releasing gonadotropin. Substitution of the sixth monomer link in the natural releasing factor molecule revealed a more pronounced affinity for gonadorelin receptors and longer half-life than the natural microparticle.

 The initial and one of the main effects of decapeptil injection is the secretory activation of the pituitary gland that secretes FSH and LH. With prolonged stimulation with the establishment of a stable amount of triptorelin in the bloodstream, the pituitary gland loses sensitivity to gonadorelin, which causes a decrease in the concentration of gonadotrophic and sex hormones to post-infection or menopause.

 This condition is absolutely reversible, hormonal activity and secretion are renewed after the end of the period of action of the drug. 

[11], [12], [13], [14]

Pharmacokinetics

The pharmacokinetic properties of decapeptil depot were studied both in healthy individuals and in patients with the corresponding diseases: endometriosis, fibromyoma, prostate cancer.

 A few hours after the injection, a peak amount of the active ingredient in the blood stream is fixed. Further, the level is significantly reduced throughout the day. On the fourth day after the injection, the level of tryptorelin sets a repeated maximum, then gradually lowering to the minimum difficult to determine values within 44 days.

 With SC injections, the decrease in the level of the active component is slower, the period of lowering the level to hard-to-determine parameters increases to 65 days. Repeat injection of Decapeptil Depot with a periodicity of 28 days does not cause an increase in the level of active substance in the bloodstream.

 In male patients, stable bioavailability of the active substance is estimated at 38.3% during the initial 13 days. After this, a constant linear rate of release of the active ingredient is established - 0.92% of the amount of the substance introduced.

 In female patients, after a 27-day observation period, 35.7% of the initially administered amount of the drug was found, with 25.5% of the total released in the initial 13 days with further continuous release, approximately 0.73% per day of the total of the administered amount of the drug.

 The half-life of the active ingredient is 18.7 minutes (in a natural gonadorelin this duration is 7.7 minutes).

 The rate of plasma clearance is 503 ml per minute (the natural gonadorelin clearance is three times faster - 1766 ml per minute).

 Up to 4% of the active ingredient of the drug in unchanged form is excreted by the kidneys. 

[15], [16], [17], [18], [19]

Dosing and administration

Medpreparat is introduced p / k (in the abdomen) or in / m. Conduct 1 injection in 28 days.

•  In fibromiomas and endometrioid sprouting injections are done once in 28 days, starting the course at the beginning of menstruation (from 1 to 5 days). The course of therapy - from 3 months to six months.
•  With IVF, the drug is administered once from the second to the third, or on day 22 of the monthly cycle.
•  With a hormone-dependent cancer tumor of the prostate, Decapeptil Depot is used in the amount of one injection in 28 days. The course of therapy is long, determined by the doctor individually.
• How to properly use Decapeptil Depot?
• We open the package with medication;
• with clean hands, remove the protective cap from the syringe with lyophilized mass;
• open the package from the transitional element (you do not need to remove it);
• we fasten the transitional element to a syringe with a freeze-dried mass and remove it from the package;
• screw the syringe with the dissolving liquid to the opposite edge of the transition element, we check the reliability of the connection;
• pressing the piston from the side of the dissolving liquid, we move it into the syringe with the lyophilizate, then the action is repeated in the opposite direction;
• the mixing of the mass is continued until a homogeneous mixture is formed, which should be injected. 

[23], [24]

Use of the decapeptal Depot during pregnancy

Decapeptil depot is not strictly shown to pregnant and lactating women. Before appointing Decapeptil Depot, the doctor should be convinced of the absence of pregnancy in the patient. 

Contraindications

 Contraindications to the use of decapeptal depot are:

• hypersensitivity of the organism to the ingredients of the drug;
• period of gestation and breastfeeding;
• hormone-independent prostate cancer.

 Medication is not used in pediatric practice.

 With polycystic adnexa, the appointment of the drug requires great care, as well as with osteoporosis. 

Side effects of the decapeptal Depot

Side effects are explained by a decrease in the concentration of sex hormones in the bloodstream, which triggers the development of the following undesirable effects in patients:

• psychoemotional instability;
• depressive state;
• lowering of sexual desire;
• migraine-like pain;
• insomnia;
• fluctuations in weight;
• periodic sensations of heat;
• increased sweating;
• dyspeptic phenomena;
• musculo-articular pain;
• dryness of the genitals, pain during intercourse;
• deterioration of potency in male patients.

 Occasionally, activation of liver transaminases can be observed.

 Due to the fact that in some cases there is an atypical reaction in the injection zone of the drug (swelling, hyperemia, pruritus), it is not recommended to inject each time in the same place.

 These side effects are completely eliminated after the medication is withdrawn.

[20], [21], [22]

Overdose

Facts that reliably confirm the possibility of drug overdose have not been described.

[25]

Interactions with other drugs

 There is no information on the positive or negative interaction of Decapeptil Depot with other medicinal medications.

[26],

Storage conditions

Dekapeptil depots are stored exclusively in the refrigerator with a temperature of + 2 ° C to + 8 ° C, in the compartments not accessible to children. The prepared suspension must be used immediately.

[27]

Shelf life

Shelf life of the medication is up to 3 years.