Dekapeptil

Antineoplastic hormone Decapeptil belongs to the pharmacological group of analogues (agonists) of the hormone gonadoliberin (gonadotropin-releasing hormone or GnRH). 

Other trade names: Triptorelin, Decapeptil Depot, Diferelin. Analogues: Goserelin (Zoladex), Buserelin (Buserelin-long), Leiprorelin (Lupron Depot, Leuprolide, Lekrin Depot). 

[1],

Indications of the decapeptal

The main indications for the use of Decapeptol as an antitumor agent include hormone-dependent disseminated prostatic carcinoma in men, and can also be prescribed for endometriosis, uterine fibromatosis, and benign neoplasia of myometrium (myomas) in women.

The drug is used in the treatment of hypogonadotropic amenorrhea (ie, due to a decrease in the functions of the ovaries).

Decapeptil has found application in reproductive medicine - for the treatment of endocrine infertility in women and preparation (stimulation of the ovaries) for in vitro fertilization (IVF).

[2]

Release form

Decapeptil is available in the form of a solution for injection - in sterile syringes with a volume of 1 ml (each packed in a contour cell).

[3], [4], [5], [6]

Pharmacodynamics

Pharmacodynamics of the drug Decapeptil is due to the action of a synthetic analogue of the endogenous hormone of the hypothalamus gonadoliberin (gonadotropin-releasing hormone or GnRH) -triptorelin (D-tryptophan-6-gonadorelin acetate).

The effect of decapeptal is two-stage. First, stimulation of the anterior lobe of the pituitary gland occurs with an increase in the release of gonadotropic hormones, luteinizing (LH) and follicle stimulating (FSH), which leads to a temporary increase in the level of estradiol in women, and in men, through the activation of interstitial cells of testosterone, to an increase in testosterone synthesis.

But in the second stage, the action of this drug on the pituitary gland completely blocks the sensitivity of its receptors to gonadoliberin and the secretion of LH and FSH decreases with a gradual cessation of their production. Accordingly, the content of female and male sex hormones is sharply reduced: women develop artificial menopause, men stop spermatogenesis. Both processes are reversible after the discontinuation of the use of Decapeptil.

The reduction factor of sex hormones and their effect on the growth of cancer cells is used in oncology for the treatment of prostate cancer in men, as well as in drug therapy associated with increased proliferation of cells of benign uterine formations in women. 

Dekapeptil in IVF is used because of its effect on ovulation, because suppression of LH synthesis prevents too early release of the ovary from the ovary (premature ovulation). Suppression of spontaneous emissions of luteinizing hormone contributes to better folliculogenesis and an increased likelihood of pregnancy.

[7], [8], [9], [10], [11]

Pharmacokinetics

The bioavailability of tryptorelin after subcutaneous injection of Decapeptal is 70%; the drug quickly enters the blood, but does not bind to plasma proteins. The maximum concentration in the blood is noted 30-40 minutes after the administration.

The half-life period ranges from 3.5 to 6.5 hours.

Triptorelin cleavage occurs in the liver, but the biochemical mechanism of this 

Dosing and administration

Decapeptil is administered by subcutaneous injection. In the treatment of prostate cancer, the first seven days daily injected into the skin of the abdominal wall dose - 0.5 mg (once). Then the dose is reduced to 0.1 mg - once a day.

The method of administration and dose in the treatment of endometriosis, fibromatosis of the uterus and myoma in women is similar.

For long-term use, doctors recommend the drug Triptorelin - Decapeptyl Depot (containing 3.75 mg of active substance), which is injected once every four weeks (the injection should be done in the first five days of the menstrual cycle).

Dekapeptil with IVF in a short protocol is introduced on the first day of the menstrual cycle -

0.1 mg (once a day) for 10 days.

To stimulate ovulation, Decaepptil in IVF in a long protocol is introduced in the middle of the luteal phase (that is, on the 21-23th day of the menstrual cycle) - once a day (at the same time), subcutaneously in the anterior abdominal wall; the dose is determined by the doctor for each patient individually - according to the results of blood tests to the level of hormones. The following injections can be done on their own, the nurse should instruct the patient how to stab Decapeptil in the stomach. The drug is administered within 12-22 days: the duration is also determined by the doctor in the process of ultrasound monitoring of the ovaries every three days - to accurately determine the time of administration of chorionic gonadotropin preparations and subsequent puncture of the ovaries (to obtain a mature egg). Normally, the monthly after Decapeptal should be absent, since the drug blocks the production of luteotropin by the pituitary gland, which leads to an amino acid.

Dekapeptil in cryoprotocol is used in a lower dosage, and before embryo embryo is frozen (cryopreservation in liquid nitrogen).

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

Use of the decapeptal during pregnancy

Decapeptil is not used during pregnancy and during lactation.

Contraindications

Decapeptil is contraindicated in cases of hypersensitivity to the drug and other synthetic analogues of gonadoliberin, during pregnancy and lactation, with pituitary adenoma, severe forms of allergy, osteoporosis, polycystic ovary and patients under 18 years of age.

[12],

Side effects of the decapeptal

The most likely side effects of Decapeptol are:

• nausea and worsening of appetite;
• itching and flushing of the skin:
• hyperhidrosis, night sweats, tides of blood to the face and chest;
• increased blood pressure;
• dizziness, fainting and headaches;
• shortness of breath and heart rhythm disturbances;
• numbness of limbs (paresthesia);
• abdominal, muscular and joint pain;
• decreased visual acuity;
• increased levels of glucose and cholesterol in the blood;
• frequent mood changes, depressed state, sleep disorders, decreased sexual desire (decreased potency in men);
• dryness of the vaginal mucosa, dyspareunia, uterine bleeding, painful menstruation, the appearance of ovarian cysts in women;
• decrease testicles and hair, increase mammary glands in men;
• decreased bone density.

[13], [14], [15]

Overdose

Overdose of Decapeptal may lead to an increase in side effects; in such cases it is necessary to interrupt treatment.

Interactions with other drugs

The interaction of decapeptil with other drugs has not been investigated, therefore, they should not be excluded. In any case, combine this antitumor hormone and antibiotics, antihistamines, neuroleptics, etc. Not recommended.

In addition, Decapeptil and alcohol may aggravate such side effects of the drug as dizziness and increased blood pressure.

[20]

Storage conditions

The drug should be stored in a dark place at t + 2-10 ° C (it can not be frozen).

Shelf life

36 months.