Decapeptil depot, 3.75mg

Pharmacodynamics

The active ingredient of Decapeptil Depot is triptorelin, a synthetic analog of gonadotropin-releasing hormone (GnRH). The result of replacing the 6th amino acid residue in the natural GnRH molecule is a more pronounced affinity for GnRH receptors and a longer half-life than that of the natural molecule.

The initial effect of administration of Decapeptil Depot is stimulation of pituitary FSH and LH secretion. After prolonged stimulation (constant concentration of tryptorelin in the blood) the pituitary gland becomes insensitive to the action of GnRH. As a result, the gonadotropin level in blood decreases, which leads to a decrease in the level of sex hormones to the post-castral or menopausal level. The effects described are reversible.

Pharmacokinetics

Pharmacokinetic tests were performed on patients with a confirmed diagnosis of endometriosis or uterine myoma, patients with prostatic carcinoma, and healthy male volunteers.

Absorption

In the first hours after intravenous administration of Decaleptil Depot, the C_max of triptorelin in plasma is recorded, decreasing markedly within 24 hours. On the 4th day after the intravenous injection, the concentration of tryptorelin in blood reaches a second maximum, followed by a biexpansential decrease in concentration to indeterminate values for 44 days.

The increase in the concentration of the active ingredient is slower after a p / n injection compared to a v / m injection. Decrease of the concentration of tryptorelin in blood is slower, the duration of decrease of concentration to undetermined values is 65 days.

Repeat injections of Decapeptil Depot at 28-day intervals do not increase its blood concentration. When injected v/m and p/c, the concentration of tryptorelin 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 tryptorelin from the depot is 38.3% in the first 13 days. Thereafter, release of the drug becomes linear with an average daily value of 0.92% of the administered dose.

In women, after 27 days of study, an average of 35.7% of the initially administered dose is determined, with 25.5% of the dose released in the first 13 days followed by linear release, averaging 0.73% of the administered dose daily.

Elevation

The plasma half-life of tryptorelin is 18.7 minutes, while for natural gonadotropin-releasing hormone this figure is 7.7 minutes. The clearance of tryptorelin (503 mL/min) is 3 times slower than that of natural releasing hormone (1766 mL/min) and consists of two components, fast and slow elimination. Less than 4% of triptorelin unchanged is excreted in the urine.

Indications

In women:

In men:

Active ingredient

Composition

1 syringe contains:

Active ingredients:

tryptorelin acetate 4.12 mg, which corresponds to the triptorelin content of 3.75 mg.

Excipients:

Lactic and glycolic acid copolymer,

Propylene glycol caprylocaprate.

Solvent:

Polysorbate 80, dextran 70, sodium chloride, sodium dihydrophosphate dihydrate, sodium hydroxide, water d/i.

How to take, the dosage

The drug Decapeptil Depot is administered p/k (into the p/k abdominal cage) or intramuscularly once every 4 weeks. The site of administration should be changed.

In case of uterine myoma and endometriosis the drug is administered once every 4 weeks, treatment begins in the first 5 days of the menstrual cycle, the duration of treatment is 3 to 6 months.

In assisted reproductive technologies (IVF), the drug is administered once on days 2 to 3 or 22 of the menstrual cycle.

In case of hormone-dependent carcinoma of the prostate – once every 4 weeks, long-term.

Principles for administration

Interaction

Special Instructions

In the treatment of hormone-dependent prostate cancer with spinal metastases and/or urinary disorders, initiation of treatment may be accompanied by a temporary worsening of symptoms of the underlying disease: difficulty in urination, bone pain, symptoms of spinal cord compression, muscle tension, leg swelling. If these symptoms occur, you should consult a doctor. As additional therapy, anti-androgens may be used to alleviate the initial exacerbation of symptoms of the underlying disease.

When used in women

Pre-treatment must be investigated to rule out possible pregnancy at the time of initiation of therapy.

Myoma of the uterus and endometriosis

Treatment of uterine myoma should be monitored with ultrasound because rapid reduction in uterine size may, in some cases, lead to uterine bleeding. Amenorrhea occurs during treatment, 7-12 weeks after the last injection the ovarian function is restored. If regular menstruation persists against the background of treatment, you should consult a doctor.

The combination of therapy with Decapeptyl depot followed by surgical treatment seems reasonable. Administration of the drug leads to a significant reduction in the size of the myomatous uterus, which facilitates the technique of surgery, and in some cases allows performing organ-preserving surgical intervention using laparascopic techniques to preserve reproductive function, which is especially important in young patients.

For the duration of treatment, only non-hormonal methods of contraception should be used until menstruation occurs after treatment ends. The use of oestrogen-containing medications is not recommended.

Contraindications

With caution: Decapeptil Depo should be used in patients with polycystic ovarian syndrome (IVF), especially if the number of follicles determined by ultrasound is greater than 10, and in patients with clinical signs of or a high risk of osteoporosis.

Side effects

The sexual system: side effects are due to decreased levels of sex hormones (testosterone and estrogen) in the blood, which can lead to symptoms in men and women such as mood lability, depression, decreased libido, frequent headaches, sleep disorders, weight gain, hot flashes, increased sweating, nausea, reduced appetite, myalgia, arthralgia, bone demineralization (with long-term use); In women – vaginal mucous membrane dryness, uterine bleeding; in men – decreased potency, gynecomastia, reduced testicular size.

Laboratory measures: rarely – in men and women increased liver transaminase activity (LDH, GGTP, ALT, ACT), increased plasma cholesterol may be observed.

Allergic reactions: itching, skin redness, fever, anaphylaxis.

Local reactions: pain at the site of administration of the drug. All of the side effects described are usually moderate in severity and disappear after the end of treatment.

Overdose