Diferelin

General characteristics. Structure:

Active agent: a triptorelina acetate, in terms of трипторелин 100 mkg

Excipients: Mannitolum - 10 mg.

Solvent: sodium chloride - 9 mg, water for and - to 1000 mg.

Pharmacological properties:

Synthetic decapeptide, analog of natural GNRG. Researches on animals and clinical trials showed that after an initial stage of stimulation, prolonged use of the drug Diferelin® suppresses secretion of a gonadotrophin with the subsequent oppression of function of ovaries.
Constant use of the drug Diferelin® suppresses secretion of a gonadotrophin (FSG and LG). Suppression of intermediate endogenous peaks of LG allows to increase quality of a folliculogenesis, at the same time the quantity of the ripening follicles increases, and as a result - the probability of pregnancy for a cycle increases.

Pharmacokinetics. At healthy volunteers. Absorption. After п / to introduction in a dose of 100 mkg трипторелин it is quickly absorbed. Cmax in a blood plasma is reached in 0.63±0.26 h and makes 1.85±0.23 ng/ml.

Distribution. The phase of distribution comes to an end in 3-4 h, Vd makes 1562±158 ml/kg.

Removal. T1/2 makes 7.6±1.6 h. The general plasma clearance - 161±28 ml/min.

Indications to use:

— female infertility. Carrying out stimulation of ovaries together with gonadotrophins (chMG, chHG, FSG) in programs of extracorporal fertilization and transfer of an embryo, and also other auxiliary reproductive technologies.

Route of administration and doses:

Short course of treatment
Диферелин® enter п / to in a dose of 100 mkg/days daily, since 2nd day of a cycle (at the same time beginning stimulation of ovaries), and finish treatment in 1 day prior to the planned introduction of a human chorionic gonadotrophin. The course of treatment makes 10-12 days.

Long course of treatment
Диферелин® enter п / to in a dose of 100 mkg/days daily, since 2nd day of a cycle. At desensitization of a hypophysis (E2 less than 50 pg/ml, i.e. approximately for the 15th day after an initiation of treatment) begin stimulation of ovaries with gonadotrophins and continue п / to Diferelin's injection in a dose of 100 mkg/days, finishing them in 1 day prior to the planned introduction of a human chorionic gonadotrophin. Duration of treatment is defined by the doctor individually.

Rules of preparation of solution
The enclosed solvent is entered into a bottle with lyophilisate and shaken up before full dissolution. The used needles should be placed in the container intended for sharp objects.

Features of use:

Before an initiation of treatment it is necessary to exclude pregnancy.

Response of ovaries on п / to Diferelin's introduction in combination with gonadotrophins can increase considerably at predisposed patients, in particular, in case of a polycystosis of ovaries.

Response of ovaries to administration of drug in combination with gonadotrophins at patients can differ, besides, the same patients can have various reaction at different cycles.

Stimulation of an ovulation should be carried out under observation of the doctor and carrying out the regular analysis by means of biological and clinical methods: increase in content of estrogen in plasma and carrying out an ultrasonic ekhografiya. If response of ovaries is excessive, then it is recommended to interrupt a cycle of stimulation and to stop gonadotrophin injections.

Influence on ability to driving of motor transport and to control of mechanisms

As drug in rare instances can cause a vision disorder, in this case during treatment the drug Diferelin® is not recommended to be managed vehicles and to be engaged in other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

In an initiation of treatment
From reproductive system: at a combination to gonadotrophins hyper stimulation of ovaries is possible (increase in the sizes of ovaries, abdominal pains is noted).

In the course of treatment
From reproductive system: most often - the sudden inflows, dryness of a vagina, decrease in a libido and a dispareuniya connected with gipofizo-ovarian blockade.

From the alimentary system: nausea, vomiting, increase in activity of hepatic transaminases.

From TsNS and peripheral nervous system: emotional lability, vision disorder, headache.

From a musculoskeletal system: muscular and joint pains. Long use of analogs of GNRG can lead to demineralization of bones, risk of development of osteoporosis (this side effect was not observed at short-term use of the drug Диферелин® 0.1 of mg).

From cardiovascular system: increase in the ABP.

Allergic reactions: urticaria, skin rash, itch; seldom - a Quincke's edema.

Local reactions: pain in a drug injection site.

Others: increase in body weight.

Interaction with other medicines:

Medicinal interaction is not described.

Contraindications:

— pregnancy;
— lactation period;
— hypersensitivity to GNRG, other analogs of GNRG, to the drug Diferelin® and its components.

Use of the drug DIFERELIN® for п / to introduction at pregnancy and feeding by a breast
Now analogs of GNRG are used in a combination with gonadotrophins for stimulation of an ovulation and pregnancy.

Pregnancy is a contraindication for drug use. However practice showed that after an ovulation, stimulated in the previous cycle, in certain cases pregnancy occurred without stimulation, and the further course of stimulation of an ovulation proceeded.
In two qualitatively executed pilot studies on animals teratogenic effects of Diferelin are not revealed.

Thus, at use of drug development of congenital anomalies in the person is not expected.

Results of the conducted clinical trials with participation of a small amount of pregnant women who received GNRG analog showed absence of malformations of a fruit or fetotoksichnost. Nevertheless, further studying of effects of impact of drug on pregnancy is necessary.

Overdose:

Overdose cases are not known for the drug Diferelin®.

Storage conditions:

Drug should be stored in the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Bottles of colourless glass (7) complete with solvent (amp. 1 ml 7 pieces) - planimetric strip packagings (1) - packs cardboard.