Composition, form of production and packaging
Liofilizate for the preparation of a solution for s / c introduction of almost white, dispersed in the applied solvent to form a transparent solution, practically free of particles; the solvent is a clear, colorless solution.
1 f.
tryptorelin acetate, in terms of triptorelin 100 Ојg
Excipients: mannitol - 10 mg.
Solvent: sodium chloride - 9 mg, water d / and - up to 1000 mg.
Vials of colorless glass (7) complete with a solvent (amp 1 ml 7 pcs.) - packings of cellular contour (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Synthetic decapeptide, an analog of natural GnRH. Animal studies and clinical studies have shown that after an initial period of stimulation, long-term use of the preparation of Diferelin В® suppresses the secretion of gonadotropin with subsequent inhibition of ovarian function.
Continuous use of the drug Diferelin В® suppresses the secretion of gonadotropin (FSH and LH). Suppression of intermediate endogenous peaks of LH allows to increase the quality of folliculogenesis, at the same time the number of ripening follicles increases, and as a result - the probability of pregnancy per cycle increases.
PHARMACOKINETICS
In healthy volunteers
Suction
After sc administration at a dose of 100 Ојg, tryptorelin is rapidly absorbed. C max in blood plasma is achieved through 0.63 В± 0.26 h and is 1.85 В± 0.23 ng / ml.
Distribution
The distribution phase ends after 3-4 hours, V d is 1562 В± 158 ml / kg.
Excretion
T 1/2 is 7.6 В± 1.6 hours. The total plasma clearance is 161 В± 28 ml / min.
INDICATIONS
- female infertility. Carrying out ovarian stimulation together with gonadotropins (hMG, hCG, FSH) in programs of in vitro fertilization and embryo transfer, as well as other assisted reproductive technologies.
DOSING MODE
Short course of treatment
Dipherelin В® is administered SC at a dose of 100 Ојg / day daily, starting from the 2nd day of the cycle (simultaneously starting ovarian stimulation), and complete the treatment 1 day before the planned introduction of human chorionic gonadotropin. The course of treatment is 10-12 days.
Long course of treatment
Diferelin В® is administered sc in a dose of 100 mcg / day daily, starting from the 2nd day of the cycle. When the pituitary is desensitized (E 2 less than 50 pg / ml, that is, approximately on the 15th day after the start of treatment), ovarian stimulation with gonadotropins starts and continues injections of Dipherylin in a dose of 100 mcg / day, finishing them 1 day before planned introduction of human chorionic gonadotropin. The duration of treatment is determined by the doctor individually.
Rules for the preparation of solution
The applied solvent is introduced into the vial with lyophilizate and shaken until completely dissolved. Used needles should be placed in a container designed for sharp objects.
SIDE EFFECT
At the beginning of treatment
From the side of the reproductive system: when combined with gonadotropins, it is possible to hyperstimulate the ovaries (there is an increase in the size of the ovaries, abdominal pain).
In the process of treatment
On the part of the reproductive system: most often - sudden hot flashes, dryness of the vagina, decreased libido and dyspareunia associated with pituitary-ovarian blockade.
From the digestive system: nausea, vomiting, increased activity of hepatic transaminases.
From the side of the central nervous system and peripheral nervous system: emotional lability, visual impairment, headache.
From the musculoskeletal system: muscle and joint pain. Prolonged use of GnRH analogues can lead to bone demineralization, a risk of osteoporosis (this side effect was not observed with the short-term use of the drug Diferelin В® 0.1 mg).
From the cardiovascular system: increased blood pressure.
Allergic reactions: urticaria, skin rash, itching; rarely - angioedema.
Local reactions: pain at the injection site.
Other: weight gain.
CONTRAINDICATIONS
- Pregnancy;
- lactation period;
- Hypersensitivity to GnRH, other GnRH analogues, to the preparation of Diferelin В® and its components.
PREGNANCY AND LACTATION
Currently, GnRH analogues are used in combination with gonadotropins to stimulate ovulation and pregnancy.
Pregnancy is a contraindication for the use of the drug. However, practice has shown that after ovulation, stimulated in the previous cycle, in some cases, pregnancy comes without stimulation, and a further course of ovulation stimulation continued.
Two qualitatively performed experimental studies on animals showed no teratogenic effects of Dipherylin.
Thus, the use of the drug is not expected to develop congenital anomalies in humans.
Results of clinical trials involving a small number of pregnant women who received an analogue of GnRH showed no developmental or fetotoxic malformations.Nevertheless, further study of the effects of the drug on pregnancy is necessary.
SPECIAL INSTRUCTIONS
Before starting treatment, pregnancy should be excluded.
The response of the ovaries to the SC administration of Dipherylin in combination with gonadotropins can significantly increase in predisposing patients, particularly in the case of polycystic ovary.
The response of ovaries to the administration of the drug in combination with gonadotropins in patients may differ, in addition, the reaction may be different in the same patients for different cycles.
Stimulation of ovulation should be performed under the supervision of a physician and conducting regular analysis with the help of biological and clinical methods: an increase in the content of estrogens in the plasma and ultrasound echography. If the response of the ovaries is excessive, it is recommended to interrupt the stimulation cycle and stop gonadotropin injections.
Impact on the ability to drive vehicles and manage mechanisms
Since the drug in rare cases can cause visual impairment, in this case during treatment with the drug Diferelin В® is not recommended to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
OVERDOSE
Cases of overdose with Diperelin В® are not known.
DRUG INTERACTION
Drug interaction is not described.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of the reach of children at a temperature of no higher than 25 В° C. Shelf life - 2 years.
