Diferelin

Active material: Triptorelin
When ATH: L02AE04
CCF: An analogue of gonadotropin-releasing hormone – depot
ICD-10 codes (testimony): C61, N80
When CSF: 15.07.04.01
Manufacturer: BEAUFOUR IPSEN PHARMA (France)

Pharmaceutical form, composition and packaging

Lyophilisate for suspension for the / m of prolonged action white or slightly yellowish, dispersible attached solvent to form a slurry of white or slightly yellowish.

* – allowing for the formulation of the dosage form in excess of active substance incorporated for administration of effective doses.

Excipients: copolymer D,L-lactic and glycolic acids, mannitol, carmellose sodium, polysorbate 80.

Solvent: mannitol, water d / and (2 ml).

Slightly darkened glass vials (1) together with the solvent (amp. 1 PC.), disposable polypropylene syringe, needles etc. and / (2 PC.) – packs cardboard.

Pharmacological action

Synthetic decapeptide, natural GnRH analogue. After a short initial period gonadotropic stimulation of pituitary function triptorelin exerts an inhibitory effect on the secretion of gonadotropins followed by suppression of testicular and ovarian.

In the initial period of application Diferelin^® temporarily increases the concentration of luteinizing hormone (LG) and FSH (FSH) in blood, accordingly increases the concentration of testosterone in men and in women estradiol. Long-term treatment reduces the concentration of LH and FSH, which reduces the performance of testosterone (to levels, the relevant state after testikulektomii) and a decrease in performance of estradiol (to levels, relevant state postovarioektomii) – about to 20 day after the first injection and then remains unchanged throughout the treatment period.

Prolonged treatment with triptorelin suppresses the secretion of estradiol in women and, thus, prevents the development of endometrial ectopia.

Pharmacokinetics

Absorption and distribution

When i / m administration Diferelin^® dose 11.25 mg C_max triptorelin plasma (men and women) determined approximately 3 hours after injection. After the phase of reducing the concentration, continued during the first month, to 90 day circulating triptorelin concentration remains constant (about 0.04 to 0.05 ng / ml in the treatment of endometriosis and about 0.1 ng / ml in the treatment of prostate cancer).

Testimony

- Prostate cancer with metastases;

- Genital and extragenital endometriosis (I-IV stages).

Dosage regimen

At prostate cancer Diferelin^® injected i / m in a dose of 11.25 mg every 3 of the month.

At эndometrioze introducing drug / m dose 11.25 mg every 3 of the month. Treatment should begin during the first 5 days of the menstrual cycle. The duration of treatment depends on the severity of endometriosis and observable clinical (functional and anatomical changes) during therapy. Usually, treatment is carried out for 3-6 Months. Not recommended repeated treatment triptorelin or other GnRH analogues.

Rules suspension

A suspension for a / m administration is prepared with the supplied solvent just prior to administration. Stir the contents of the vial should be with caution until a homogeneous suspension.

Cases of incomplete implementation of injection, leading to the loss of a large number of suspensions, than usually remains in the syringe for injection, you must tell your doctor.

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

Side effect

Men

Early treatment: dizuricheskie violation (difficulty urinating, incomplete bladder emptying, soreness), ostealgias (associated with metastatic and metastatic spinal cord compression, which may be exacerbated due to the temporary increase in testosterone plasma levels at the start of treatment). These symptoms pass through 1-2 of the week. Also during this period may be a temporary increase in liver enzymes in blood plasma.

During treatment: “hot” tides, decreased libido, gynecomastia, impotence (due to the reduction of the testosterone concentration in blood plasma).

Women

Early treatment: symptoms, associated with endometriosis (pelvic pain, dysmenorrhoea), which can be amplified in an initial transient increase in the concentration of estradiol in blood plasma and disappear through 1-2 of the week. Through 1 month after the first injection may metrorrhagia.

During treatment: vaginal dryness, “hot” tides, decreased libido, breast enlargement, dyspareunia (due to pituitary-ovarian blockade); rarely – headache, arthralgia, myalgia.

Men and women

Allergic reactions: hives, rash, itch; in a few cases – angioedema.

From the central and peripheral nervous system: mood disorder, irritability, depression, feeling tired, sleep disorders, paresthesia, blurred vision.

From the digestive system: nausea, vomiting.

Cardio-vascular system: arterial hypertension.

On the part of the musculoskeletal system: prolonged use – bone demineralization, that is the risk of osteoporosis.

Other: weight gain, panhydrosis, fever.

Local reactions: pain at the injection site.

Contraindications

- Hormone-prostate cancer, state after prior surgical testikulektomii;

- Pregnancy;

- Lactation (breast-feeding);

- Hypersensitivity to triptorelin, components of the drug or other GnRH analogues.

FROM caution should be prescribed for osteoporosis, as well as women with polycystic ovary syndrome.

Pregnancy and lactation

Diferelin^® contraindicated during pregnancy and lactation (breast-feeding).

Before treatment Diferelin^® Pregnancy must be excluded.

Because there are no data on the allocation of triptorelin in breast milk and its possible effect on the breastfed baby, should not treat Diferelin^® during breastfeeding.

According to available data, not show any teratogenic effects at experimental studies Animal. In rare cases, the use of GnRH analogues (carelessly) any defects in fetal development and fetotoxicity were found.

Cautions

Before treatment endometriosis Pregnancy must be excluded. During the first month of therapy should be used hormonal contraceptives.

V / m injection of the drug leads to permanent hypogonadotropic amenorrhea.

Treatment should not be recommended for more than 6 Months. We do not recommend a second course of therapy triptorelin or other GnRH analogues.

The emergence of metrorrhagia in the course of treatment, except for the first month, not the norm, in connection with what is necessary to determine the concentration of estradiol in blood plasma. By reducing the concentration of estradiol less 50 pg / ml, there may be other organic lesions.

Ovarian function is restored after completion of therapy. The first menstruation occurs on average over 134 days after the last injection. Therefore, contraceptive measures should begin to apply through 15 days after cessation of treatment, that is, 3.5 month after the last injection.

When treating prostate cancer most pronounced beneficial effect seen in patients in the absence of other previously conducted hormone therapy.

Early treatment can be observed the emergence and strengthening of clinical symptoms (in particular, bone pain, dizuricheskih events), wearing transitory nature. This involves careful monitoring of these patients during the first few weeks of therapy (Testosterone levels in the blood plasma does not exceed 1 ng / ml).

Treatment Diferelin^® should be carried out in strict accordance with the instructions for use. Any change in the amount of input / m slurry should be recorded.

Overdose

So far, cases of drug overdose Diferelin^® unknown.

Drug Interactions

Drug Interactions drug Diferelin^® not disclosed.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 2 year.