Diferelin is an analogue of gonadotropin-releasing hormone - depot form.
Release form and composition
Release Diferelin in the form of a lyophilisate for the preparation of suspensions for intramuscular administration. One vial of the drug contains 3.75 mg of the active substance - triptorelin, as well as the following auxiliary components: carmellose sodium, polysorbate 80, copolymer D, L-lactic and glycolic acids, mannitol.
In vials of 2 ml, complete with a solvent (mannitol 16 mg and water for injection - 2000 mg), a disposable polypropylene syringe and two needles for injection.
Indications for use
According to the instructions, Diferelin is indicated for use in:
- Malignant tumor of the prostate gland;
- In the preoperative period in order to remove uterine fibroids;
- Premature puberty;
- Genital and extragenital endometriosis;
- Female infertility (the use of the drug is included in the program of in vitro fertilization).
According to the instructions, Diferelin is contraindicated for use:
- During pregnancy and breastfeeding;
- With increased sensitivity to the active component of the drug or excipients.
The drug is prescribed with caution in osteoporosis.
Dosing and Administration
The drug is administered intramuscularly.
The dosage of Diferelin for prostate cancer is 3.75 mg (1 injection) once every four weeks. The drug is used for a long time.
For premature puberty in patients whose body weight exceeds 20 kg, 3.75 mg of triptorelin is administered every 28 days. With a weight of less than 20 kg, the dosage is 1,875 mg once every 28 days.
In endometriosis, an injection is made at a dose of 3.75 mg in the first five days of the menstrual cycle (once every 28 days). The duration of therapy is no more than six months.
With uterine fibroids, an injection is given in the first five days of the menstrual cycle at a dose of 3.75 mg every four weeks. The duration of therapy is three months for patients in the preoperative period.
In case of female infertility, the use of Diferelin is 1 injection (3.75 mg) on the second day of the cycle. After 15 days, the plasma estrogen concentration is determined.
The suspension of Diferelin is prepared as follows: dissolve the lyophilisate in the attached solvent immediately before administration. The contents of the vial should be gently mixed until a homogeneous consistency is obtained.
During the injection, the patient should be in a horizontal position, face down. The skin of the buttocks before the injection should be disinfected.
The use of Diferelin can cause the following adverse reactions in a patient:
- Allergies: skin rash, itching, hives, in rare cases - angioedema;
- Musculoskeletal system: demineralization of bones (with long-term use), which causes the likelihood of osteoporosis. At the beginning of drug therapy, patients with prostate cancer may experience pronounced pain in the bones affected by metastases. This side effect requires symptomatic treatment. Symptoms caused by compression of spinal cord metastases were noted, which usually disappear within 1-2 weeks. Also observed cases of obstruction of the ureters and increased activity of acid phosphatase in the blood plasma;
- The reproductive system: in women - depression, headache, dryness of the vaginal mucosa, changes in libido, change in the size of the mammary glands, dyspareunia. With long-term use of Diferelin, hypogonadotropic amenorrhea may occur. When treating premature puberty in girls, bloody discharge from the vagina was observed. In combination with gonadotropic drugs, the development of ovarian hyperstimulation syndrome has been reported. In men, potency may decrease;
- Cardiovascular system: hot flashes, high blood pressure;
- Digestive system: nausea, vomiting;
- Central nervous system: impaired vision, increased emotional lability;
- Local reactions: pain at the injection site;
- Other reactions Diferelin: increased body temperature, weight gain.
At the initial stage of therapy with Diferelin, intensification of the clinical manifestations of the disease is not excluded. Therefore, in patients with prostate cancer who are at risk for compression of the spinal cord or development of obstruction of the ureters, the drug should be prescribed with caution. During the first month of therapy, it is necessary to exercise medical control over such patients.
Women before using Diferelin should ensure that there is no pregnancy.
With caution, the drug is used in patients with polycystic ovarian syndrome when conducting ovulation stimulation schemes, since some of them had an increase in the number of induced follicles.
In vitro fertilization requires careful monitoring of the stimulation cycle. This is necessary in order to promptly identify patients with the risk of ovarian hyperstimulation syndrome, since the dosage regimen of gonadotropin may affect the severity and frequency of its manifestations. If necessary, the use of Diferelin should be discontinued.
During therapy with Diferelin, it is possible to safely manage potentially dangerous mechanisms that require increased concentration of attention.
The structural analogue of the drug Diferelin is Decapeptil Depot.
Terms and conditions of storage
According to the instructions, Diferelin stored in a cool (up to 25 degrees Celsius), dark, dry and out of reach of children. The shelf life of the lyophilisate is 2 years.