Instruction for use: Traktocil

ATX Code G03GA05 Foliotropin alfa

Pharmacological group

Generic activity suppressing agent - blocker of oxytocin receptors [Hormones of the hypothalamus, pituitary gland, gonadotropins and their antagonists]

Nosological classification (ICD-10)

O60 Premature birth

Pregnancy prematurity, The birth premature, Preterm labor pains, Premature contractions prehospital, Immobilization of the uterus before the cesarean section, Immobilization of the uterus, Acute tocolysis, Threatening premature labor, Premature discharge of water, Preventing premature births, The threat of premature birth

Composition

Concentrate for solution for infusion 7.5 mg / ml 1 fl.

active substance:

Atosibane acetate (in terms of atosiban) 7.5 mg

Auxiliary substances: mannitol - 50 mg; Hydrochloric acid - up to pH 4.5; Water for injection - up to 1 ml

Description of dosage form

Clear colorless solution.

pharmachologic effect

Blocking oxytocin receptors.

Pharmacodynamics

The active component of Traktocil is atosiban, a synthetic peptide that is a competitive antagonist of human oxytocin at the receptor level.

Atosiban, binding to the receptors of oxytocin, reduces the frequency of uterine contractions and tone of the myometrium, leading to suppression of uterine contractility. Also, atosiban binds to vasopressin receptors, inhibiting the effect of vasopressin, but does not affect the CCC.

In the case of premature birth in women, atosiban in recommended doses suppresses uterine contractions and provides the uterus with functional rest. Relaxation of the uterus begins immediately after the administration of atosiban, within 10 min the contractile activity of the myometrium is significantly reduced, maintaining stable functional uterine rest (<4 reductions / h) for 12 hours.

Pharmacokinetics

Pharmacokinetic parameters (Vd, Cl, T1 / 2).

Distribution. After intravenous infusion (300 μg / min for 6-12 hours), Cmax of atosiban in plasma is achieved within 1 hour after the onset of infusion (on average (442 ± 73) ng / ml, in the range from 298 to 533 ng / ml ). Binding to plasma proteins is 46-48%. Atosiban penetrates the placental barrier. After the administration of Traktocil at a rate of 300 μg / min, the ratio of the concentration of atosiban in the fetus and the concentration of atosiban in the mother is 0.12. The average value of Vd is (18.3 ± 6.8) l.

Metabolism. In the blood plasma and urine, 2 metabolites were identified. The ratio of the concentration of the main metabolite M1 and the concentration of atosiban in blood plasma was 1.4 and 2.8 for the second hour of infusion and after its termination, respectively. Metabolite M1 has pharmacological activity on par with atosiban and penetrates into breast milk.

Inhibition of cytochrome P450 isoforms by atosiban is unlikely.

Excretion. After stopping the infusion, the concentration of the drug in the plasma rapidly decreases with the values of the initial (Ta) and final (Tp) T1 / 2 (0.21 ± 0.01) and (1.7 ± 0.3) h, respectively. The average clearance value of the preparation is (41.8 ± 8.2) l / h.

Atosiban is detected in urine in very small amounts, its concentration in the urine is 50 times lower than the concentration of M1. The amount of atosiban, excreted with feces, was not determined.

Indications

Traktocil is used for the threat of premature birth in pregnant women in the following cases:

Regular uterine contractions lasting at least 30 seconds and a frequency of more than 4 within 30 minutes;

The opening of the cervix from 1 to 3 cm (0-3 cm for nulliparous women);

Age over 18 years;

Gestational age from 24 to 33 full weeks;

Normal heart rate in the fetus.

Contraindications

The gestation period is less than 24 or more than 33 full weeks;

Premature rupture of membranes during pregnancy for more than 30 weeks;

Intrauterine growth retardation;

Abnormal heart rate in fetus;

Uterine bleeding, requiring immediate delivery;

Eclampsia and severe preeclampsia requiring immediate delivery;

Intrauterine fetal death;

Suspicion of intra-uterine infection;

Placenta previa;

Placental abruption;

Any conditions of the mother and fetus, in which the retention of pregnancy is a danger;

breast-feeding;

Hypersensitivity to atosiban or to one of the components of the drug.

With caution: in case of suspicion of premature rupture of the membranes, the use of Tractocil for the prolongation of labor should be compared with the potential risk of developing chorioamnionitis. Caution should be applied to Tractocil in case of multiple pregnancy, as well as at the gestational age of 24-27 weeks (due to lack of sufficient clinical experience).

pregnancy and lactation

Traktocil should be used only in the case of diagnosed premature birth for a period of 24 to 33 full weeks of pregnancy.

Traktocil is contraindicated in breastfeeding.

Side effects

From the gastrointestinal tract: very often (> 1/10) - nausea, less often - vomiting.

From the side of metabolism: often (> 1/100, <1/10) - hyperglycemia.

From the side of the central nervous system: often (> 1/100, <1/10) - headache, dizziness; Rarely (> 1/1000, <1/100) - insomnia.

On the part of the CCC: often (> 1/100, <1/10) - tachycardia, arterial hypotension, hot flashes.

From the skin: rarely (> 1/1000, <1/100) - itching, skin rash.

Local reactions: rarely (> 1/1000, <1/100) - hyperthermia at the injection site.

From the side of the reproductive organs: very rarely (> 1/10000, <1/1000) - uterine bleeding / atony of the uterus.

If any of the side effects listed in the manual are aggravated, or any other side effects not indicated in the instructions develop, you should inform your doctor.

Interaction

Interaction with other drugs

Tractocyl does not affect the pharmacokinetics of drugs metabolized with the participation of cytochrome P450.

With the combined use of the drug Traktocil and betametazone, no clinically significant interactions were observed.

Labetalol does not affect the pharmacokinetics of the drug Traktocil.

The interaction of the drug Traktocil with antibiotics is unlikely.

The combined use of the drug Traktocil with ergot alkaloids is impractical in connection with the opposite pharmacological action and indications for use.

Dosing and Administration

Traktocil is administered IV immediately after the diagnosis of premature birth in 3 stages:

1) at the beginning, within 1 minute, I fl. 0.9 ml of the drug without dilution (initial dose - 6.75 mg);

2) Immediately thereafter, infusion of the drug at a dose of 300 μg / min (injection rate 24 ml / h, dose of atosiban - 18 mg / h) is performed within 3 hours;

3) After this, a long (up to 45 h) infusion of Tractocil at a dose of 100 mcg / min (rate of administration - 8 ml / h, dose of atosiban - 6 mg / h) is then carried out.

The total duration of treatment should not exceed 48 hours. The maximum dose of the drug Traktocil for the entire course should not exceed 330 mg.

If there is a need for repeated use of the drug Traktocil, also should begin with the 1 st stage, followed by infusion of the drug (stages 2 nd and 3 rd).

Repeated use can begin at any time after the first use of the drug, it can be repeated up to 3 cycles.

If the contractile activity of the uterus does not decrease after 3 cycles of therapy with Traktocil, consideration should be given to using another drug.

Instructions for the preparation of a solution for infusion (stage 2 and 3)

Concentrate is diluted in one of the following solutions:

- 0.9% solution of sodium chloride;

- Ringer's acetate solution;

- 5% glucose solution.

From a vial containing 100 ml of one of the above dilution solutions, 10 ml are drained. Then, 10 ml (2 fl.) Of Traktocil is injected into the vial to give a concentration of 75 mg / 100 ml.

Shelf life of the prepared solution for infusions is 24 hours. Do not use if insoluble particles are visible in solution or the solution has changed color.

Overdose

There are several cases of overdose. Specific symptoms and signs are absent. The specific antidote is unknown.

Treatment is symptomatic and maintenance therapy.

special instructions

In the absence of a decrease in contractile activity of the uterus during the introduction of the drug Traktocil, uterine contractions should be monitored, as well as monitoring the fetal heart rate. Other drugs should also be considered.

Experience with atosiban in patients with impaired liver and kidney function is absent.

Atosiban is not used in cases of abnormal attachment of the placenta. As an antagonist of oxytocin, atosiban can theoretically contribute to uterine relaxation and provoke postpartum uterine bleeding, therefore, a continuous assessment of the degree of blood loss after labor is necessary.

Influence on ability to drive a car and mechanisms requiring increased attention. Not applicable, given indications for use.

Form of issue

Concentrate for solution for infusion, 7.5 mg / ml. For 0.9 ml of the drug in a colorless bottle with a capacity of 2 ml of glass type I, sealed with a gray bromobutyl plug and a hermetically sealed flip-off cap.

For 5 ml of the drug in a colorless vial with a capacity of 5 ml of Type I glass, sealed with a gray bromobutyl plug and a hermetically sealed "flip-off" cap. On 1 ôë. Placed in a plastic bag and a cardboard box

Terms of leave from pharmacies

On prescription.

storage Conditions

At a temperature of 2-8 ° C (do not freeze).

Keep out of the reach of children.

Shelf life

4 years.

Do not use after the expiry date printed on the package.