Diferelin

General characteristics. Structure:

Active agent: a triptorelina acetate, in terms of трипторелин 3.75 mg *
* - taking into account features of a dosage form in drug excess of active agent for ensuring introduction of an effective dose is put.

Excipients: copolymer D, L-milk and glycolic acids - about 160 mg (the quantity depends on capsulation level), Mannitolum - 85 mg, a karmelloza of sodium - 30 mg, polysorbate of 80 - 2 mg.

Solvent: Mannitolum - 16 mg, water for and - to 2000 mg.

Pharmacological properties:

Synthetic decapeptide, analog of natural GNRG. Диферелин®, after a short initial stage of stimulation of gonadotropic function of a hypophysis, has an inhibiting effect on secretion of a gonadotrophin with the subsequent suppression of function of testicles and ovaries.
Constant use of the drug Diferelin® inhibits secretion of estrogen ovaries to a condition of a menopause, and also reduces secretion of testosterone which concentration can reach indicators which are observed after surgical castration.

Pharmacokinetics. Absorption and distribution. After administration of suspension in oil there comes the initial phase of bystry release of active agent with the subsequent phase of continuous release. At this Cmax of a triptorelin in a blood plasma makes 0.32±0.12 ng/ml, and the average quantity of constantly released triptorelin makes 46.6±7.1 mkg/days.

Bioavailability of drug at introduction makes 53% once a month.

Indications to use:

— prostate cancer;
— premature puberty;
— genital and extragenital endometriosis;
— a uterus fibromyoma (before an operative measure);
— female infertility (in the program of extracorporal fertilization).

Route of administration and doses:

The drug is administered only by in oil.

At a prostate cancer of Diferelin® each 4 weeks enter in a dose 3.75 mg (1 injection), it is long.

At premature puberty drug is appointed to patients with body weight by more than 20 kg on 3.75 mg each 28 days, to patients with body weight less than 20 kg - on 1.875 mg each 28 days.

At endometriosis the drug is administered in a dose 3.75 mg of 1 times in 4 weeks. The injection is carried out in the first 5 days of a menstrual cycle. Treatment duration - no more than 6 months.

At female infertility drug appoint in a dose 3.75 mg (1 injection) to the 2nd day of a cycle. Communication with gonadotrophins should be controlled after desensitization of a hypophysis (concentration of estrogen in a blood plasma less than 50 »¬ú/ml usually is defined in 15 days after a drug Diferelin® injection).

At a uterus fibromyoma the drug should be administered in the first 5 days of a menstrual cycle. Drug is appointed on 3.75 mg by each 4 weeks. Duration of a course of treatment makes 3 months for the patients preparing for operation.

Rules of preparation and administration of suspension

Suspension for introduction in oil is prepared by dissolution of lyophilisate in the enclosed solvent just before introduction. It is necessary to mix bottle contents with care before receiving homogeneous suspension.

About the cases of implementation of an incomplete injection leading to loss of bigger amount of suspension than usually remains in the syringe for an injection, it is necessary to tell the attending physician.

Introduction has to be carried out in strict accordance with the instruction.

The patient has to be in a prone position. Disinfect buttock skin.

1. Break an ampoule neck (a point on the face from above).
2. Gather solvent in the syringe with a needle.
3. Remove a protective plastic cover from an upper part of a bottle.
4. Transfer solvent to a bottle with lyophilisate.
5. Pull a needle so that it remained in a bottle, but did not concern suspension.
6. Without overturning a bottle, accurately shake up contents before receiving homogeneous suspension.
7. Check lack of agglomerates before you gather suspension in the syringe (in case of lack of agglomerates, shake up to total homogeneity).
8. Without overturning a bottle, gather all suspension in the syringe.
9. Remove the needle used for suspension preparation and densely attach other needle on a syringe tip. You hold only a color tip.
10. Remove air from the syringe.
11. Immediately make an injection in a gluteus.
12. Utilize needles in the containers intended for sharp objects.

Features of use:

In an initiation of treatment strengthening of clinical symptoms in this connection it is necessary to appoint with care Diferelin® the patient with cancer of a prostate subject to risk of development of impassability of ureters or prelums of a spinal cord is possible. Careful medical observation of these patients within the first month of therapy is necessary.

Prior to therapy by Diferelin it is necessary to confirm lack of pregnancy.

With care use drug at patients with a syndrome of a polycystosis of ovaries when carrying out schemes of stimulation of an ovulation. It is connected with the fact that at a small amount of patients the quantity of the induced follicles can increase.

It is necessary to monitorirovat carefully the level of stimulation of a cycle at extracorporal fertilization to reveal patients with risk of development of a syndrome of hyper stimulation of ovaries as expressiveness and frequency of manifestations of a syndrome can depend on the mode of dosing of a gonadotrophin. If necessary introduction of a chorionic gonadotrophin of the person should be stopped.

Influence on ability to driving of motor transport and to control of mechanisms
Data are absent.

Side effects:

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

From a musculoskeletal system: at prolonged use - demineralization of bones that is risk of development of osteoporosis. In an initiation of treatment at a prostate cancer patients can experience temporary strengthening of the ostealgias struck with metastasises (a symptomatic treatment). Separate cases of impassability of ureters and emergence of the symptoms connected with a compression metastasises of a spinal cord are noted (pass through 1-2 weeks). Also during this period temporary increase in activity of acid phosphatase in a blood plasma can be observed.

From a reproductive system: men have a decrease in a potentiality; women have a headache, a depression, perspiration and change of a libido, dryness of a mucous membrane of a vagina, a dispareuniya and change of the size of mammary glands. At use in a combination with gonadotrophins it was reported about cases of development of a syndrome of hyper stimulation of ovaries. At treatment of premature puberty at girls bloody allocations from a vagina can be observed. Prolonged use of drug can cause a hypogonadotropic amenorrhea.

From the alimentary system: in isolated cases - nausea, vomiting.

From cardiovascular system: in isolated cases - arterial hypertension, feeling of inflows.

From TsNS: in isolated cases - the increased emotional lability, a vision disorder.

Others: in isolated cases - increase in body weight, fervescence.

Local reactions: in isolated cases - pain in the place of an injection.

Interaction with other medicines:

Medicinal interaction of the drug Diferelin® is not described.

Contraindications:

— pregnancy;
— period of a lactation (breastfeeding);
— hypersensitivity to a triptorelin, other components of drug and other analogs of GNRG.

With care it is necessary to appoint drug at osteoporosis.

Use of the drug ДИФЕРЕЛИН® 3.75 of mg at pregnancy and feeding by a breast
Диферелин® it is contraindicated to use at pregnancy and in the period of a lactation (breastfeeding).

Overdose:

So far about cases of overdose of the drug Diferelin® it was not reported.

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 slightly tinted glass (1) complete with solvent (amp. 2 ml 1 pieces), the one-time polypropylene syringe, needles for and (2 pieces) - packs cardboard.