Dyferelin, lyophilizate 3.75mg+syringe+2 needles

Composition

1 bottle contains:

Active ingredient:

triptorelin acetate, in terms of triptorelin 3.75 mg*

* – taking into account the characteristics of the dosage form, the preparation contains an excess of the Active ingredient to ensure the introduction of an effective dose.

Auxiliary substances:

copolymer of D, L-lactic and glycolic acids – about 160 mg (the amount depends on the level of encapsulation),

mannitol-85 mg,

carmellose sodium-30 mg,

polysorbate 80-2 mg.

Solvent:

mannitol-16 mg,

d/i water – up to 2000 mg

Pharmacological action

Pharmacodynamics

Synthetic decapeptide, an analog of natural GnRH. Diferelin®, after a short initial period of stimulation of pituitary gonadotropic function, has an inhibitory effect on gonadotropin secretion, followed by suppression of testicular and ovarian function.

Continuous use of the drug Diferelin® inhibits the secretion of estrogen by the ovaries before menopause, and also reduces the secretion of testosterone, whose concentrations can reach levels that are observed after surgical castration.

Pharmacokinetics

Suction and distribution

After intravenous use of the suspension, the initial phase of rapid release of the Active ingredient occurs, followed by a permanent release phase. The Cmax of triptorelin in blood plasma is 0.32±0.12 ng / ml, and the average amount of continuously released triptorelin is 46.6±7.1 mcg / day.

The bioavailability of the drug when administered once a month is 53%.

Indications

Prostate cancer; genital and extragenital endometriosis; premature puberty; female infertility (in vitro fertilization program); uterine fibromyoma (before surgery).

Use during pregnancy and lactation

Diferelin® is contraindicated for use during pregnancy and lactation (breastfeeding).

Contraindications

• Pregnancy;
• lactation (breastfeeding);
• hypersensitivity to triptorelin, other components of the drug and other GnRH analogues.

With caution: the drug should be prescribed for osteoporosis.

Side effects

Allergic reactions: urticaria, rash, pruritus; very rarely – angioedema. On the part of the reproductive system: in men-decreased potency; in women-headache, depression, sweating and changes in libido, dryness of the vaginal mucosa, dyspareunia and changes in the size of the mammary glands.

When used in combination with gonadotropins, cases of ovarian hyperstimulation syndrome have been reported. When treating premature puberty, girls may experience spotting from the vagina. Prolonged use of the drug may cause hypogonadotropic amenorrhea.

From the musculoskeletal system: with prolonged use-demineralization of bones, which is a risk of developing osteoporosis. At the beginning of treatment for prostate cancer, patients may experience a temporary increase in pain in the bones affected by metastases (treatment is symptomatic). There are isolated cases of ureteral obstruction and the appearance of symptoms associated with compression by spinal cord metastases (they pass after 1-2 weeks). Also, during this period, there may be a temporary increase in the activity of acid phosphatase in blood plasma.

From the digestive system: in isolated cases-nausea, vomiting.

From the central nervous system: in isolated cases-increased emotional lability, visual impairment.

From the cardiovascular system: in isolated cases – arterial hypertension, hot flashes.

Local reactions: in isolated cases – pain at the injection site.

Other: in isolated cases – an increase in body weight, an increase in body temperature.

Interaction

The drug interaction of Diferelin® is not described.

How to take, course of use and dosage

The drug is administered only intravenously.

In prostate cancer, Diferelin® is administered at a dose of 3.75 mg (1 injection) every 4 weeks, for a long time.

With premature puberty, the drug is prescribed to patients with a body weight of more than 20 kg of 3.75 mg every 28 days, to patients with a body weight of less than 20 kg – 1.875 mg every 28 days.

In endometriosis, the drug is administered at a dose of 3.75 mg 1 time in 4 weeks. The injection is performed in the first 5 days of the menstrual cycle. Duration of treatment-no more than 6 months.

In case of female infertility, the drug is prescribed at a dose of 3.75 mg (1 injection) on the 2nd day of the cycle. The association with gonadotropins should be monitored after pituitary desensitization (plasma estrogen concentrations of less than 50 pg / ml are usually determined 15 days after Diferelin injection).

For uterine fibromyoma, the drug should be administered in the first 5 days of the menstrual cycle. The drug is prescribed for 3.75 mg every 4 weeks. The duration of the course of treatment is 3 months for patients preparing for surgery.

Rules for suspension preparation and use

The suspension for intravenous use is prepared by dissolving the lyophilizate in the supplied solvent immediately before use. Mix the contents of the bottle with caution until a homogeneous suspension is obtained.

Cases of incomplete injection resulting in the loss of more suspension than is normally left in the injection syringe should be reported to the attending physician.

Introduction should be carried out in strict accordance with the instructions.

The patient should be in a supine position. Disinfect the buttock skin.

Overdose

To date, no cases of Diferelin overdose have been reported.

Special instructions

At the beginning of treatment, clinical symptoms may increase, and therefore Diferelin® should be prescribed with caution to patients with prostate cancer who are at risk of developing ureteral obstruction or spinal cord compression. These patients should be carefully monitored during the first month of therapy.

Before starting Diferelin therapy, it is necessary to confirm the absence of pregnancy.

The drug is used with caution in patients with polycystic ovarian syndrome during ovulation stimulation schemes. This is due to the fact that a small number of patients may increase the number of induced follicles.

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 severity and frequency of manifestations of the syndrome may depend on the gonadotropin dosage regimen. If necessary, the use of human chorionic gonadotropin should be discontinued.

Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention

There is no information available.

Form of production

Lyophilizate for the preparation of a suspension for intravenous use of prolonged action.

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Triptorelin

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Purpose

For adults as directed by your doctor

Indications

Cancer, Infertility Treatment