Alterpur

General characteristics. Structure:

Active ingredient: 75 ME or 150 ME urofollitropins (FGS).

Excipients: lactoses monohydrate of 10 mg.

Solvent: sodium chloride (depyrogenized for and) 9 mg, water for and (to 1 ml).

Pharmacological properties:

Pharmacodynamics. The high cleaning follicle-stimulating hormone (FSG) received from urine of women in a postmenopause with insignificant impurity of the luteinizing hormone (LH). The maintenance of LG in an end product is minimized through a procedure of cleaning with a hromatografichesky method with antibodies to a chorionic gonadotrophin of the person.

Stimulates growth and maturing of follicles, causing increase in concentration of estrogen and proliferation of an endometria. Practically does not possess luteinizing action.

FSG interacts with specific receptors on a surface of small granulosa cells of ovaries and Sertoli's cells in testicles: these receptors are tied with adenylatecyclase by means of guaninnukleotidny regulatory protein (protein Gs).

Pharmacokinetics. Vsasyvani. After a single p / to and introductions in oil in a dose 225 ME time of achievement of Cmax of drug in plasma makes 20.5 and 17.4 h, respectively. However after repeated use (150 ME daily within 7 days) Tmax makes about 10 h at both ways of introduction.

At a repeated p / to and introduction in oil bioavailability of FSG leaves 81.8% and 77.7% respectively.

At a single p / to and introduction in oil Cmax in plasma makes 6.0±1.7 MME/ml and 8.8 ± 4.5 MME/ml, respectively. At a repeated p / to and introduction in oil Cmax makes 14.8±2.9 MME/ml and 11.5±2.9 MME/ml, respectively.

AUC at a single p / to and introduction in oil makes 379±111 мМЕ×ч/мл and 331±179 мМЕ×ч/мл, respectively. At a repeated p / to and introduction in oil AUC makes 234.7±77.0 мМЕ×ч/мл and 192.1±52.3 мМЕ×ч/мл, respectively.

Removal. Average T1/2 FSG for a single p / to and introductions in oil makes 31.8 and 37 h, respectively. However, after repeated use of T1/2 makes 20.6 and 15.2 h for п / to and introductions in oil, respectively.

Indications to use:

— anovulation at a syndrome of polycystic ovaries at women (only at inefficiency of clomifene);

— controlled hyper stimulation of ovaries for the purpose of induction of growth of multiple follicles when carrying out auxiliary reproductive technologies, such as fertilization of in vitro, intra fallopian transfer of a gamete, intra fallopian transfer of zygotes (only at inefficiency of clomifene).

Route of administration and doses:

Treatment by drug Alterpur should be carried out only under control of the doctor having the corresponding specialization and experience of treatment of infertility.

The drug is administered in oil or п / to. Solution for injections is prepared just before introduction (to 5 bottles of urofollitropin it can be dissolved in 1 ml of solvent).

During the first 7 days of a cycle at the menstruating women daily enter on 75-150 ME/days. Maturing of follicles is usually reached during a medical cycle - 7-12 days. Adequacy of the response to treatment is estimated according to daily analyses of concentration of estrogen, direct visualization of size of follicles by means of ultrasonography and to clinical data.

If adequate stimulation is not reached, the dose can be gradually increased. After performing treatment and in the presence of the adequate, but not excessive answer of ovaries according to clinical and biochemical trials, in 24-48 h after the last injection to the patient enter once human chorionic gonadotrophin of the person (chHG) in a dose 5000-10000 ME ovulations, in oil for the purpose of induction. The next day is optimum for conception.

In the presence of an ovulation and lack of approach of pregnancy the course can be repeated during 2 cycles. In the absence of the adequate response to therapy within 4 weeks from its beginning drug should be cancelled.

For stimulation of a superovulation when carrying out auxiliary reproductive technologies treatment is begun about 2-3 days of a menstrual cycle - daily on 150-225 ME/days. In the course of stimulation the dose can be changed depending on reaction of ovaries, at the same time the daily dose should not exceed 450 ME. Treatment is continued before adequate maturing of follicles. In 24-48 h after the last injection enter chHG of 5000-10 000 ME in oil for the purpose of induction of an ovulation.

At stimulation of an ovulation with use of agonists of GNRG administration of urofollitropin is begun in 2 weeks after the beginning of use of an agonist on 225 ME/days within 7 days (administration of drug continue before achievement of the adequate size of a follicle), from 8 in the afternoon the dose can be adjusted (depending on reaction of ovaries).

Features of use:

Use at pregnancy and feeding by a breast. Drug is contraindicated at pregnancy and during feeding by a breast.

Use for children. It is contraindicated at children's age.

Special instructions. Emergence of polycarpous pregnancy is probable. Emergence of ectopic pregnancy is possible, especially at diseases of uterine tubes in the anamnesis. Frequency early and misbirths at the pregnancy which occurred after treatment by urofollitropin, above than at healthy patients, but is comparable with that at infertility of other etiology.

Before an initiation of treatment carry out treatment of a hypothyroidism, insufficiency of bark of adrenal glands, giperprolaktinemiya, tumors of a hypophysis and a hypothalamus, the analysis of sperm of the sexual partner.

At increase in ovaries gynecologic inspection is performed carefully, in order to avoid a rupture of cysts of ovaries, it is recommended to avoid the sexual relations.

The Syndrome of Hyper Stimulation of Ovaries (SHSO) arises for 7-10 day after an ovulation, stimulated introduction of chHG more often. It is characterized by sharp increase in permeability of vessels that can lead to bystry accumulation of liquid in an abdominal cavity, a thorax and a pericardium. Precursory symptoms of development of SGYa are severe pelvic pain, nausea, vomiting, increase in body weight. At SGYa the following symptoms can be observed: an abdominal pain, abdominal distention, gastrointestinal symptoms, including nausea, vomiting and diarrhea, significant increase in ovaries, increase in body weight, an asthma and an oliguria. Also the signs following clinical can be observed: hypovolemia, pachemia, disturbance of electrolytic balance, ascites, hemoperitoneum, pleural exudate, hydrothorax, acute respiratory distress syndrome, tromboembolic episodes. The probability of development of SGYa during implementation of the "superovulation" (created when carrying out auxiliary reproductive technologies) can be reduced if contents of all follicles before an ovulation are aspirated. At emergence of signs of SGYa administration of drug should be stopped.

Development of tromboembolic episodes is probable. The intravascular fibrinferments and embolisms which are in venous and arterial vessels can lead to reduction of inflow of blood to vitals and extremities. Venous thrombophlebitis, a pulmonary embolism, the lung heart attack, a stroke and thrombosis of arteries leading to loss of an extremity can be a complication of it.

Influence on ability to driving of motor transport and to control of mechanisms. During use of drug it is necessary to refrain from potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions since drug can cause dizziness and other side effects which can influence the specified abilities.

Side effects:

Adverse side reactions classified as follows: very frequent (> 1/10); frequent (from ≥1/100 to ≤1/10); infrequent (from ≥1/1000 to ≤1/100); rare (from ≥1/10 000 to ≤ 1/1000); very rare (<1/10 000).

For drug the following undesirable side reactions were noted:

From endocrine system: infrequently - a hyperthyroidism.

From a nervous system: often - a headache; infrequently - a lethargy, dizziness, a depression.

From respiratory system: infrequently - short wind, nasal bleeding.

From the alimentary system: often - a lock, abdominal distention; infrequently - nausea, an abdominal pain, dyspepsia.

Dermatological reactions: infrequently - an erythema, an itch.

From an urinary system: infrequently - cystitis.

From a reproductive system: often - a syndrome of hyper stimulation of ovaries; infrequently - increase in mammary glands, morbidity of mammary glands, inflows.

From an organism in general: often - pain; infrequently - fatigue.

From laboratory indicators: infrequently - increase in duration of bleedings.

Local reactions: infrequently - pain, reddening, a hematoma.

In rare instances there is an arterial thromboembolism connected with treatment human менотропином / a chorionic gonadotrophin.

Frequency of abortions at gonadotropic therapy is comparable with that at women with other disturbances of fertility. The small risk of an extrauterine pregnancy and polycarpous pregnancy is recorded.

Besides, the following side reactions can be observed: atelectases of lungs, a respiratory distress syndrome, not cardiogenic fluid lungs, vomiting, diarrhea, increase in ovaries, cysts of ovaries, pains in a stomach bottom, increase in permeability of walls of vessels, a hemoperitoneum, a pachemia, nasal bleeding, chromosomal disturbances (a trisomy in 13 and 18 couples of chromosomes), an acute anaphylaxis, a hypovolemia, water and electrolytic disturbances, ascites, a hydrothorax, an alopecia, an arthralgia, a mialgiya, rushes of blood to face skin.

Interaction with other medicines:

Alterpur it is not necessary to mix with other medicines.

Contraindications:

— high concentration of FSG at primary ovarian insufficiency;

— dekompensirovanny pathology of a thyroid gland and adrenal glands;

— organic lesions of TsNS, for example, hypophysis tumors;

— the infertility which is not connected with dysfunction of ovaries;

— the persistent increase in ovaries, a cyst of ovaries (which are not caused by a syndrome of a polycystosis of ovaries);

— anomalies of development of generative organs, hysteromyoma (incompatible with pregnancy);

— metrorrhagia and other bleedings of an unspecified etiology;

— ovarian cancer, uterus and/or mammary gland;

— primary insufficiency of ovaries;

— pregnancy;

— lactation period;

— children's age;

— hypersensitivity to drug.

With care it is necessary to appoint drug with risk factors of a thromboembolism, such as individual or family predisposition, heavy degree of obesity (body weight index> of 30 kg/sq.m) or at a thrombophilia since in this case there is an increased risk of a venous or arterial thromboembolism in process or after treatment by gonadotrophins. In this case the advantage of treatment has to surpass by gonadotrophins risk from their use.

Overdose:

Symptoms: a syndrome of hyper stimulation of ovaries (increase in ovaries, pains in a stomach bottom, nausea, vomiting, diarrhea, increase in body weight, an oliguria, ascites, a hydrothorax, a hemoperitoneum, haemo concentration, an asthma), polycarpous pregnancy, tromboembolic episodes.

Treatment consists of 3 stages: the first stage is directed to decrease in concentration of hormone in blood and preventions of development of tromboembolic episodes (pneumonia, an acute renal failure), it consists in in introduction of small amounts of albumine (with constant control of concentration of electrolytes in blood and a hematocrit). The second stage begins after stabilization of a condition of the patient and has to lead to decrease in content of liquid in organism cavities for what in/in enter small amounts of hypertonic salt solution of sodium of chloride and albumine. The third stage aims to warn edematization of lungs, the organism connected with massive intake of liquid from cavities in a vascular bed, and includes use of diuretics (at constant control of a hematocrit and concentration of electrolytes in plasma).

Storage conditions:

Drug should be stored in protected from light, the place, unavailable to children, at a temperature not above 25 °C. A lyophilisate period of validity - 2 years, solvent - 5 years. The period of validity of a set is established on a component with the smallest period of validity.

Issue conditions:

According to the recipe

Packaging:

75 ME - bottles glass (1) complete with solvent (amp. 1 pieces) - packs cardboard. 75 ME - bottles glass (1) complete with solvent (amp. 1 pieces) - packs cardboard (10) - packs the cardboard general.

150 ME - bottles glass (1) complete with solvent (amp. 1 pieces) - packs cardboard. 150 ME - bottles glass (1) complete with solvent (amp. 1 pieces) - packs cardboard (10) - packs the cardboard general.