Diferelin - instructions for use, doses, side effects, contraindications

Mannitol 16.0 mg; water for injection up to 2000.0 mg.
* Taking into account the characteristics of the dosage form, the preparation contains an excess of the active component to ensure the introduction of an effective dose.

** The amount depends on the level of encapsulation.

Description:white or white lyophilizate with a creamy shade of color, dispersible in the applied solvent to form a white or white suspension with a creamy shade of color

Pharmacotherapeutic group:antitumor agent - gonadotropin-releasing hormone analogue

ATX: & nbsp

L.02.A.E.04 Triptorelin

Pharmacodynamics:

Triptorelin is a synthetic decapeptide, an analog of natural gonadotropin-releasing hormone (releasing gonadotropin).

After a short initial period of stimulation of the gonadotropic function of the pituitary gland tryptorelin suppresses the secretion of gonadotropins and, accordingly, the function of the testicles and ovaries. Continuous use of the drug inhibits the secretion of estrogen by the ovaries to the state of menopause, and also reduces the secretion of testosterone, the concentration of which can reach the values that are observed after surgical castration.

Pharmacokinetics:

After intramuscular administration of the prolonged form of the drug, the initial stage of rapid release of the drug begins, followed by a phase of constant release of tryptorelin (the maximum concentration is 0.32 ± 0.12 ng / ml). The average amount of constantly released tryptorelin is 46.6 ± 7.1 μg / day.

Bioavailability of the drug is about 53% for 1 month.

Indications:

- prostate cancer;

- premature puberty;

- genital and extragenital endometriosis;

- fibroids of the uterus (before surgical intervention);

- female infertility (in the program of in vitro fertilization).

Contraindications:

Hypersensitivity to Dipherylin® or other gonadotropin analogues-hormone releasing, pregnancy and the period of breastfeeding.

Carefully:

With caution - with osteoporosis.

Pregnancy and lactation:

The drug is contraindicated for use during pregnancy and during breastfeeding.

Dosing and Administration:

The drug is administered only intramuscularly.

Prostate cancer:

Diferelin® is administered at a dose of 3.75 mg every 4 weeks, long-term.

Premature puberty:

- 3.75 mg every 28 days (children weighing more than 20 kg),

- 1,875 mg every 28 days (children weighing less than 20 kg).

Endometriosis:

The drug should be administered in the first 5 days of the menstrual cycle - at a dose of 3.75 mg every 4 weeks. The duration of therapy is no more than 6 months.

Female infertility:

Dipherelin® should be administered on the second day of the cycle at a dose of 3.75 mg. Linkage with gonadotropins should be monitored after desensitisation of the pituitary gland (estrogen concentration in the blood plasma less than 50 pg / ml is usually determined 15 days after the injection of Dipherylin®).

Fibromyoma of the uterus:

The drug should be administered in the first 5 days of the menstrual cycle. Dipherylin® should be administered every 4 weeks at a dose of 3.75 mg.

Duration of treatment: 3 months (for patients preparing for surgery).

Rules for the preparation of suspension

Dissolution of the lyophilizate in the attached solvent must be conducted immediately before the introduction. Mix the contents of the vial with caution until a uniform suspension is obtained.

About incomplete injection, leading to a loss of more suspension than usually remains in the injection syringe, it is necessary to inform the attending physician.

The introduction should be carried out in strict accordance with the instruction. The patient should be lying down. Disinfect the skin of the buttocks.

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

2. Collect all of the solvent in the syringe with needle.

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

4. Transfer the solvent to a vial of lyophilizate.

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

6.Do not turn over the vial, gently shake the contents until a uniform suspension is obtained.

7.Check the absence of agglomerates before dialing the suspension into the syringe (in the case of the presence of agglomerates, shake until complete homogeneity).

8. Do not flip the vial, put the entire suspension into the syringe.

9. Remove the needle used to prepare the suspension and tightly attach the other needle to the tip of the syringe. Hold on only for the colored tip.

10. Remove air from the syringe.

11. Immediately inject the injection into the gluteus muscle.

12.Utilize needles in containers, intended for sharp objects.

Side effects:

Allergic reactions, such as urticaria, rash, itching and very rarely swelling of Quincke. Several cases of nausea, vomiting, weight gain, arterial hypertension, increased emotional lability, visual impairment, pain at the injection site and increased body temperature, sensation of "hot flashes" are described.

Long-term use of gonadotropin-releasing hormone analogues can lead to demineralization of bones and is a possible risk factor for the development of osteoporosis.

In men, a decrease in potency. At the beginning of treatment, patients with prostate cancer may experience temporary pain in the bones affected by metastases (symptomatic treatment).There are isolated cases of obstruction of the ureters and symptoms associated with compression by metastases of the spinal cord (after 1-2 weeks). Also during this period there may be a temporary increase in the activity of acid phosphatase in the blood plasma.

Women - headache, depression, sweating and changes in libido, dryness of the vaginal mucosa, dyspareunia and changes in the size of the mammary glands.

When Diperelin® was used in combination with gonadotropins, there were reports of cases of ovarian hyperstimulation syndrome.

In the treatment of premature puberty, girls can have spotting from the vagina.

Prolonged use of the drug may cause hypogonadotropic amenorrhea. After discontinuation of treatment, the function of the ovaries is restored and ovulation occurs on average 58 days after the last injection of the drug. The first menstruation occurs on the 70th day after the last injection of Dipherylin®. This should be taken into account in contraceptive planning.

Overdose:

Cases of drug overdose are not known.

Interaction:

Not described.

Special instructions:

- At the beginning of treatment, there may be an increase in clinical symptoms, which should be followed with caution in appointing Diferelin® patients with prostate cancer, at risk of developing obstruction of the ureters or compression of the spinal cord. Careful observation of these patients during the first month of therapy is necessary.

- Before starting therapy with Differelin®, it is necessary to confirm the absence of pregnancy.

- Use with caution in patients with polycystic ovary syndrome in 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 stimulation of the cycle for in vitro fertilization to identify patients at risk of developing ovarian hyperstimulation syndrome, because the severity and frequency of the syndrome may depend on the dosage regimen of gonadotropin. If necessary, the introduction of human chorionic gonadotropin should be discontinued.

Effect on the ability to drive transp. cf. and fur:

No information.

Form release / dosage:

Lyophilizate for the preparation of a suspension for intramuscular injection prolonged action of 3.75 mg.

Packaging:

For 3.75 mg of triptorelin per vial of slightly darkened glass, ukuporenny rubber stopper under aluminum with a needle hole in the center and closed with protective plastic cover the control of the first autopsy. 2 ml of solvent in an ampoule of colorless glass. One empty sterile disposable polypropylene syringe with capacity 3 ml, two subcutaneous disposable needles measuring 0.90 x 40 mm with yellow tips in a blister pack of PVC and laminated paper. One bottle with the drug, one ampoule with solvent, one blister pack with a syringe and two needles placed in a pack of cardboard along with the instructions for application.

Storage conditions:

At a temperature not higher than 25 ° C in a place inaccessible to children.

Shelf life:

2 years.

Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011452 / 01

Date of registration:13.08.2010

The owner of the registration certificate:IPSEN PHARMA IPSEN PHARMA France

Manufacturer: & nbsp

IPSEN PHARMA BIOTECH France

Representation: & nbspIPSEN PHARMA IPSEN PHARMA France

Information update date: & nbsp18.10.2015

Illustrated instructions

Instructions

Diferelin® (Diphereline®)