Dipherelin lyophilisate d / prig.sp.v / m 3.75mg, No. 1

• Prostate cancer;

• premature puberty;

• genital and extragenital endometriosis;

• fibroids of the uterus (before surgery);

• female infertility (in the in vitro fertilization program).

The drug is administered only intramuscularly.

For prostate cancer, DipherelinЃ 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 weighing more than 20 kg, 3.75 mg every 28 days, to patients weighing less than 20 kg - 1.875 mg every 28 days.

In endometriosis, the drug is administered at a dose of 3.75 mg once every 4 weeks. The injection is carried out in the first 5 days of the menstrual cycle. The duration of treatment is no more than 6 months.

For female infertility, the drug is prescribed at a dose of 3.75 mg (1 injection) on the 2nd day of the cycle. The connection with gonadotropins should be monitored after desensitization of the pituitary gland (the concentration of estrogens in the blood plasma is less than 50 pg / ml is usually determined 15 days after the injection of the DipherelinЃ drug).

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

Rules for the preparation and administration of the suspension

A suspension for intramuscular administration is prepared by dissolving the lyophilisate in the supplied solvent immediately before administration. Stir the contents of the vial with caution until a homogeneous suspension is obtained.

Cases of incomplete injection, leading to the loss of more suspension than usually remains in the injection syringe, must be reported to the attending physician.

The introduction should be carried out in strict accordance with the instructions.

The patient should be in the supine position. Disinfect the skin of the buttocks.

1. Break the neck of the ampoule (dot on the front side at the top).

2. Draw solvent into a syringe with a needle.

3. Remove the protective plastic cap from the top of the bottle.

4. Transfer the solvent to the lyophilisate vial.

5. Pull the needle so that it remains in the vial, but does not touch the suspension.

6. Without turning the bottle, gently shake the contents until a homogeneous suspension is obtained.

7. Check the absence of agglomerates before drawing the suspension into the syringe (if there are no agglomerates, shake until completely homogeneous).

8. Without turning the bottle over, draw the entire suspension into the syringe.

9. Remove the suspension needle and firmly attach the other needle to the tip of the syringe. Only hold on to the colored tip.

10. Remove air from the syringe.

11. Immediately inject into the gluteus muscle.

12. Dispose of needles in sharps containers.

Lyophilisate for preparation of a suspension for intramuscular administration of prolonged action of white or white with a creamy shade, dispersing in the supplied solvent to form a suspension of white or white with a creamy shade.

1 fl.

triptorelin acetate, calculated as triptorelin 3.75 mg *

* - taking into account the characteristics of the dosage form, the preparation contains an excess of the active substance to ensure the introduction of an effective dose.

Excipients: copolymer of D, L-lactic and glycolic acids - about 160 mg (the amount depends on the level of encapsulation), mannitol - 85 mg, sodium carmellose - 30 mg, polysorbate 80 - 2 mg.

• Pregnancy;

• lactation period (breastfeeding);

• hypersensitivity to triptorelin, other components of the drug and other GnRH analogues.

  The drug should be prescribed with caution in osteoporosis.

pharmachologic effect

Synthetic decapeptide, analog of natural GnRH. DipherelinЃ, after a short initial period of stimulation of the gonadotropic function of the pituitary gland, has an inhibitory effect on the secretion of gonadotropin, followed by suppression of the function of the testicles and ovaries.

The constant use of the drug DipherelinЃ inhibits the secretion of estrogen by the ovaries until menopause, and also reduces the secretion of testosterone, the concentration of which can reach the levels that are observed after surgical castration.

Pharmacokinetics

Absorption and distribution

After the i / m administration of the suspension, an initial phase of rapid release of the active substance occurs, followed by a phase of constant release. In this case, the Cmax of triptorelin in blood plasma is 0.32 ± 0.12 ng / ml, and the average amount of constantly released triptorelin is 46.6 ± 7.1 ?g / day.

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

Side effect

Allergic reactions: urticaria, rash, itching; very rarely - Quincke's edema.

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

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 bleeding from the vagina. Long-term use of the drug can cause hypogonadotropic amenorrhea.

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

From the side of the cardiovascular system: in isolated cases - arterial hypertension, sensation of hot flashes.

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

Others: in isolated cases - an increase in body weight, an increase in body temperature.

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

Application during pregnancy and lactation

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

special instructions

At the beginning of treatment, clinical symptoms may increase, and therefore, DipherelinЃ should be prescribed with caution to patients with prostate cancer who are at risk of developing ureteral obstruction or spinal cord compression. Careful medical supervision of these patients is necessary during the first month of therapy.

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

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

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 introduction of human chorionic gonadotropin should be discontinued.

Influence on the ability to drive vehicles and mechanisms

No information available.