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Pharmacological properties

Triptorelin is a synthetic decapeptide, an analogue of natural gonadotropin-rg (releasing hormone). The data of the studies showed that after a short initial period of stimulation of the pituitary gonadotropic function, prolonged use of triptorelin has an inhibitory effect on the secretion of gonadotropin with further inhibition of both female and male steroidogenesis.

Further studies suggest a different mechanism of action: a direct effect on gonads by reducing the sensitivity of peripheral receptors to the effects of the factor responsible for the release of gonadotropin.

When using the drug, an initial increase in the level of LH and FSH in the blood and, accordingly, the level of testosterone in men and estradiol in women is possible. With prolonged treatment, the levels of LH and FSH decrease to an indicator corresponding to the state after surgical castration for 20 days after the first injection, which remains at this level throughout the entire period of drug use.

Pharmacokinetics

Diferelin 0.1 mg

After sc administration of 0.1 mg, Diferelin is rapidly absorbed; time to reach Cmax drug in blood plasma - 0.63 ± 0.26 h; WITHmax drug in plasma - 1.85 ± 0.23 ng / ml. T½ biological - 7.6 ± 1.6 hours after 3-4 hours of the distribution phase. The total plasma clearance is 161 ± 28 ml / min. The conditional volume of distribution is 1562 ± 158 ml / kg.

Diferelin 3.75 mg

It is a drug for prolonged release due to the microspherical structure of the deposition of tryptorelin, which provides a clinically effective concentration for 28 days.

Men

After the intramuscular administration of a prolonged form of the drug, the initial stage of drug release occurs with a further usual release (Cmax - 0.32 ± 0.12 ng / ml), during which the average release rate of tryptorelin is 46.6 ± 7.1 mg / day. Bioavailability after 1 month - 53%.

Women

After a / m injection, the maximum level of tryptorelin in the blood is noted between 2-6 hours after injection, Cmax - 11 ng / ml. There is no data on the cumulation of the drug after 6 months of use. WITHmin in the blood ranges between 0.1-0.2 ng / ml. The bioavailability of the drug is a sustained release form of about 50%.

Diferelin 11.25 mg

After i / m administration of a dose of Diferelin 11.25 mg Cmax plasma tryptorelin is detected approximately 3 hours later. After the phase of the concentration decrease, which occurs during the 1st month, until the 90th day, the level of circulating tryptorelin remains constant (about 0.03-0.06 ng / ml).

Indications

Diferelin 0.1 mg

Female infertility. Ovulation stimulation in combination with gonadotropins for the purpose of in vitro fertilization and embryo transplantation (I.V.F.E.T.).

Diferelin 3.75 mg

  • Prostate cancer and its complications, in which inhibition of testosterone secretion is indicated;
  • endometriosis genital and extragenital: stages I – IV;
  • endometrioid cysts;
  • endometrial hyperplastic processes;
  • female infertility; complex treatment in combination with gonadotropins, for artificial reproduction of ovulation conditions, with the aim of in vitro fertilization and further transplantation of the embryo;
  • premature puberty in children (onset of the disease in girls under 8 years old and in boys under 10 years old);
  • breast cancer when hormone therapy is indicated;
  • uterine fibroids.

Diferelin 11.25 mg

  • Prostate adenocarcinoma with metastases;
  • mammary cancer;
  • genital and extragenital endometriosis;
  • premature puberty in children.

Application

Diferelin 0.1 mg

Used in combination with gonadotropins.

Subcutaneous injection 1 time per day, starting from the 2nd day of the menstrual cycle (simultaneously with the beginning of ovarian stimulation) until the day preceding the planned induction of ovulation, that is, the average period of use is 10-12 days for each attempt.

Diferelin 3.75 mg

Prostate cancer and its complications: 1 v / m injection of Diferelin 3.75 mg of prolonged action every 4 weeks. The duration of the drug is corrected by the doctor individually for each patient.

Endometriosis, endometrioid cysts, endometrial hyperplastic processes: 1 v / m injection of Diferelin 3.75 mg every 4 weeks. Treatment must begin in the first 5 days of the menstrual cycle. The duration of treatment depends on the initial degree of endometriosis and the positive dynamics of clinical manifestations during treatment. The course of treatment is not more than 6 months. It is not recommended to start the second course of treatment with triptorelin or another analog of gonadotropin-RG.

Female infertility: the usual therapeutic regimen is based on the use of 1 i / m injection on the 2nd day of the cycle. The concomitant use of gonadotropins should begin after pituitary desensitization is achieved (plasma estrogen level does not exceed 50 pkg / ml), usually on the 15th day after injection of Diferelin.

Uterine fibroids: treatment begins in the first 5 days of the menstrual cycle. Introduction Diferelin spend every 4 weeks. The duration of the course of treatment is 3 months for patients preparing for surgery, and up to 6 months for patients who are not indicated for surgical treatment.

Breast cancer: 1 i / m injection of Diferelin 3.75 mg prolonged action every 4 weeks. The duration of the drug is corrected by the doctor individually for each patient.

Premature puberty: 1 v / m injection at the rate of 50 mcg / kg body weight every 4 weeks.

Diferelin 11.25 mg

Prostate adenocarcinoma with metastases: 1 v / m injection of Diferelin 11.25 mg of prolonged action every 3 months. The duration of the drug is corrected by the doctor individually for each patient.

Endometriosis: 1 v / m injection of 11.25 mg every 3 months. Treatment must begin in the first 5 days of the menstrual cycle. The period of treatment depends on the initial degree of endometriosis and the presence of positive clinical dynamics during treatment. The course of treatment is not more than 6 months.

Breast cancer: 1 v / m injection of Diferelin 11.25 mg of prolonged action every 3 months. The duration of the drug is corrected by the doctor individually for each patient.

Premature puberty: 1 i / m injection of the drug 11.25 mg Diferelin every 3 months.

ATTENTION! It is important that the injection of the drug with prolonged action be performed in accordance with all instructions. Each unsuccessful injection, after which the volume of the drug remains in the syringe more than prescribed by the instruction, should be recorded.

Contraindications

Hypersensitivity to the components of the drug; During pregnancy and breastfeeding.

Side effects

Clinical trial data

Most of the adverse reactions reported during clinical trials are associated with the pharmacological properties of the active substance and are the result of hypogonadotropic hypogonadism or, rarely, the primary pituitary-gonadal stimulation caused by the drug.

General tolerance in adults. Hot flashes and sweating, which usually does not require discontinuation of therapy.

General tolerance in men. At the beginning of treatment, with an increase in testosterone in the blood plasma, an increase in the severity of symptoms from the urinary tract (dysuria and hematuria), increased pain in the bones of metastatic origin, exacerbation of symptoms associated with compression of metastases in the spinal cord (back pain, weakness, upper paresthesia) limbs). These symptoms disappear after 1-2 weeks.

During the treatment period, the most frequently observed adverse reactions (decreased libido and impotence) are associated with a decrease in testosterone in blood plasma, which is the pharmacological effect of the active substance of the drug. A decrease in testicular volume may also occur as a result of a decrease in plasma testosterone levels.

Gynecomastia is occasionally possible.

General tolerance in women.At the beginning of treatment, symptoms associated with endometriosis (pelvic pain, dysmenorrhea) may intensify during an initial and unsteady increase in plasma estradiol levels, which, as a rule, disappear within 1-2 weeks.

Genital hemorrhages (menorrhagia, metrorrhagia, or spotting) can occur 1 month after the first injection.

In the treatment of infertility, a combination with gonadotropins can lead to ovarian hyperstimulation; at the same time, ovarian hypertrophy, pain in the pelvic and / or abdominal region are noted).

During treatment, sleep disturbance, headache, mood changes, vaginal dryness and dyspareunia, decreased libido associated with pituitary-ovarian blockade may occur. Cases of chest pain, muscle cramps, joint pain, weight gain, nausea, pain or discomfort in the abdomen, asthenia have been reported.

General tolerance in children. Allergic reactions, headaches, and hot flashes have been reported. Initial ovarian stimulation can cause minor spotting of the vagina in girls. Occasionally, short-term pain, redness, local inflammation at the injection site are noted.

Post-Marketing Surveillance Data

Adults Very rarely, the following adverse reactions have been identified, which are classified by organs and systems:

body as a whole: fever, weakness, peripheral edema.

Metabolic and nutritional disorders: anorexia.

Mental disorders: depression, personality changes.

CNS and peripheral nervous system: dizziness, paresthesia in men.

Organ of vision: blurred or impaired vision.

Cardiovascular system: increased blood pressure, tachycardia.

Respiratory system: dyspnea.

Gastrointestinal tract: diarrhea, vomiting, constipation.

Skin: pruritus, urticaria, skin rash, Quincke edema, alopecia.

Musculoskeletal system: arthralgia, myalgia, muscle weakness, bone pain, the risk of osteoporosis.

Reproductive system: in women after discontinuation of treatment, menstrual irregularities can be noted: amenorrhea, menorrhagia or metrorrhagia.

Children. Additionally, the following separate reactions in children were reported: allergic reactions such as urticaria, skin rash, Quinckes edema, weight gain, hypertension, visual impairment, discomfort, gastrointestinal pain and vomiting, nosebleeds, weakness, myalgia, emotional lability, nervousness.

special instructions

Diferelin 0.1 mg

It should be borne in mind that in some patients, especially with polycystic ovary syndrome, the use of Diferelin 0.1 mg in combination with gonadotropins can cause an increase in the number of mature follicles.

The reaction of the ovaries to the administration of Diferelin together with gonadotropins in equal doses can be individual in each patient, and even in the same patient in different cycles.

Warning regarding use. Before starting treatment, make sure that the patient is not pregnant.

Ovarian induction should be carried out under strict medical supervision with regular biological and clinical monitoring: rapid determination of estrogen in plasma and ultrasound. If the ovarian reaction is excessive, it is recommended to stop the gonadotropin stimulation cycle.

Diferelin 3.75 mg

In adults, prolonged use of gonadotropin-RH analogues can lead to bone demineralization and is a risk factor for osteoporosis.

Patients receiving the drug may need a correction of antihypertensive therapy. Before starting treatment with the drug, the absence of pregnancy should be confirmed.

Men. Prostate cancer: in some cases, an increase in the severity of clinical symptoms (e.g. bone pain) is possible. However, this effect is noted in a few patients; it, as a rule, is temporary.Such patients require medical supervision, especially with obstruction of the urinary tract and metastases in the spinal cord.

Due to the same reasons, it is also necessary to control patients with initial manifestations of medullary compression at the beginning of treatment.

During this period, a temporary increase in plasma phosphatase levels is possible.

Periodic monitoring of blood testosterone levels is required (1 ng / ml).

Women. Female infertility: the drug is used with caution in patients with polycystic ovary syndrome when conducting an ovulation stimulation scheme. This is due to the fact that few patients may increase the number of induced follicles. In different patients, the reaction of the ovaries to the administration of the same dose of tryptorelin-gonadotropin can vary, and in some cases, from one cycle to another in the same patient. It is necessary to carefully monitor the level of cycle stimulation during in vitro fertilization in order to identify patients at risk of developing ovarian hyperstimulation syndrome, since the degree and frequency of the syndrome may depend on the dosage regimen of gonadotropin. If ovarian hyperstimulation is suspected, it is recommended to cancel gonadotropin injections.

Endometriosis and uterine myoma: the use of the drug Diferelin 3.75 mg causes persistent hypogonadotropic amenorrhea. The appearance of metrorrhagia after the end of the 1st month of treatment is an abnormal phenomenon and requires monitoring of the level of estradiol in the blood (50 pg / ml).

After cessation of treatment, ovarian function is restored and ovulation occurs on average on the 58th day after the last injection of the drug. The first menstruation occurs on the 70th day after the last injection. Thus, contraceptives can be prescribed on the 15th day after discontinuation of the drug, that is, 1.5 months after the last injection.

Breast cancer: in patients with breast cancer, treatment with Diferelin 3.75 mg may be effective, while other drugs did not have a clinical effect or are less effective; if the drug is used as the drug of first choice, it does not reduce the effectiveness of another treatment if necessary.

Diferelin 11.25 mg

Mixing the powder with the solvent must be carried out immediately before injection by shaking the bottle in smooth movements to obtain a homogeneous suspension of a milky color. The suspension should not be mixed with other drugs.

Prostate adenocarcinoma: periodic monitoring of blood testosterone levels (1 ng / ml) is required.

Endometriosis: before starting treatment with the drug, the absence of pregnancy should be confirmed.

The use of the drug Diferelin 11.25 mg causes persistent hypogonadotropic amenorrhea. The appearance of metrorrhagia at the end of the 1st month of treatment is an abnormal phenomenon and requires monitoring of the level of estradiol in the blood (50 pg / ml).

After cessation of treatment, ovarian function is restored and ovulation occurs on average on the 134th day after the last injection of the drug. Thus, contraceptives can be prescribed on the 15th day after discontinuation of the drug, that is, 3.5 months after the last injection.

Use during pregnancy and lactation. The use of the drug during pregnancy and lactation is contraindicated.

Children. At the beginning of treatment, minor spotting of the vagina may occur. 1/3 girls (after the first injection, which indicates the need for additional therapy with medroxyprogesterone acetate (40 mg / day) or cyproterone acetate (40 mg / day), or cyproterone acetate (100 mg / day) during the 1st week of treatment.

The ability to influence the reaction rate when driving vehicles or while working with other mechanisms. Not identified.However, dizziness or visual impairment, which may be a manifestation of a likely side effect or underlying disease, may affect the ability to perform work that requires increased attention.

Interactions

No clinically significant cases of interaction with other drugs have been reported.

The possibility of the combined use of other drugs is decided by the doctor.

Do not use simultaneously with drugs that increase the level of prolactin, since they reduce the level of luteinizing pituitary RH receptors.

Overdose

With an overdose, side effects of the drug are possible.

The treatment is symptomatic.

Storage conditions

At temperatures up to 25 ° C.