Tractocile, vial 7.5mg/ml, 5ml

Composition

Composition per 1 ml: Active ingredient: atosiban acetate in terms of atosiban 7.5 mg; excipients: Mannitol 50 mg, hydrochloric acid up to pH 4.5, water for injection up to 1 ml

Pharmacological action

Pharmacodynamicaactive component of Tractocile is atosiban, a synthetic peptide that is a competitive antagonist of human oxytocin at the receptor level. Atosiban, by binding to oxytocin receptors, reduces the frequency of uterine contractions and the tone of the myometrium, leading to suppression of uterine contractility. Atosiban also binds to vasopressin receptors, inhibiting the effect of vasopressin, but it does not affect the cardiovascular system. In the case of preterm labor in a woman, atosiban in the recommended doses suppresses uterine contractions and provides the uterus with functional rest. Relaxation of the uterus begins immediately after the introduction of atosiban, within 10 minutes the contractile activity of the myometrium is significantly reduced, maintaining a stable functional rest of the uterus (/h) within 12 hours. Pharmacokineticpharmacokinetic parameters (Vd, Cl, T1 / 2). Distribution. After intravenous infusion (300 mcg / min for 6-12 hours), Cmax of atosiban in plasma is reached within 1 hour after the start of the 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 use of the drug Tractocile at a rate of 300 mcg / min, the ratio of the concentration of atosiban in the fetus and the concentration of atosiban in the mother’s body is 0.12. The average value of Vd is (18.3 ± 6.8) L. Metabolism. Two metabolites were identified in the blood plasma and urine. The ratio of the concentration of the main metabolite M1 and the concentration of atosiban in blood plasma was 1.4 and 2.8 at the second hour of infusion and after its termination, respectively. The M1 metabolite has pharmacological activity on a par with atosiban and penetrates into breast milk. Inhibition of cytochrome P450 isoforms by atosiban is unlikely. Output. After stopping the infusion, the drug concentration in plasma decreases rapidly with the values of the initial (Ta) and final (Tp) T1/2 (0.21±0.01) and (1.7±0.3) hours, respectively. The average clearance of the drug is (41.8±8.2) l/h. Atosiban is detected in the urine in very small amounts, its concentration in the urine is 50 times lower than the concentration of M1. The amount of atosiban excreted in the faeces was not determined.

Indications

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

• regular contractions of the uterus lasting at least 30 seconds and a frequency of more than 4 within 30 minutes;
• opening of the cervix from 1 to 3 cm (0-3 cm for nulliparous women);
• age over 18 years;
• gestation period from 24 to 33 full weeks;
• normal fetal heart rate.

Use during pregnancy and lactation

Tractocile should be used only in the case of diagnosed preterm labor for a period of 24 to 33 full weeks of pregnancy. Tractocile is contraindicated in breast-feeding.

Contraindications

• The gestation of less than 24 or more than 33 weeks;
• premature rupture of membranes during pregnancy, a period of more than 30 weeks;
• fetal growth retardation;
• abnormal fetal heart rate;
• uterine bleeding, requiring immediate delivery;
• eclampsia and severe preeclampsia requiring immediate delivery;
• intrauterine fetal death;
• the suspicion of intra uterine infection;
• placenta previa;
• abruption;
• any state of the mother and fetus, in which continuation of the pregnancy poses a risk;
• breastfeeding;
• hypersensitivity to atosiban or to one of the components of the drug.

Caution: if premature rupture of membranes is suspected, the use of Tractocile for prolonging labor should be compared with the potential risk of chorioamnionitis. Caution should be exercised when using Tractocile during multiple pregnancies, as well as during pregnancy of 24-27 weeks (due to lack of sufficient clinical experience).

Side effects

From the gastrointestinal tract: very often (>1/10) — nausea, less often-vomiting. From the side of metabolism: often (>1/100, >From the central nervous system: often (>1/100, ><1/10) – headache, dizziness; rarely (>1/1000, <1/10 — – headache, dizziness; rarely (>From the CVS: often (>1/100, >Skin disorders: rare (>1/1000, >Local reactions: rare (>1/1000, >From the reproductive organs: very rare (>1/10000, >If any of the side effects listed in the instructions get worse, or any other side effects that are not listed in the instructions develop, you should inform your doctor.

Interaction

Interaction with other Lactocil does not affect the pharmacokinetics of drugs metabolized with the participation of cytochrome P 450. No clinically significant interactions were observed when Tractocile and betamethasone were co-administered. Labetalol does not affect the pharmacokinetics of Traktocil. The interaction of Traktocil with antibiotics is unlikely. The combined use of Traktocil with ergot alkaloids is impractical due to the opposite pharmacological effect and indications for use.

How to take, course of use and dosage

Tractocile is administered intravenously immediately after the diagnosis of preterm birth in 3 stages: 1) at the beginning, within 1 min,0.9 ml of the drug is administered I fl. without dilution (the initial dose is 6.75 mg);2) immediately after that, the drug is infused at a dose of 300 mcg/min (the rate of use is 24 ml/h, the dose of atosiban is 18 mg/h);3) after that, a prolonged (up to 45 hours) infusion of the drug Tractocile at a dose of 100 mcg/min (the rate of use is 8 ml/h, the dose of atosiban is 6 mg/h) is performed. h). The total duration of treatment should not exceed 48 hours. The maximum dose of Traktocil for the entire course should not exceed 330 mg. If there is a need for repeated use of the drug Tractocile, you should also start with the 1st stage, followed by infusion of the drug (stages 2 and 3). Repeated use can be started at any time after the first application of the drug, it can be repeated up to 3 cycles. If uterine contractile activity does not decrease after 3 cycles of therapy with Tractocile, the use of another drug should be considered. Instructions for preparing the infusion solution (stage 2 and 3)The concentrate is diluted in one of the following solutions: – 0.9% sodium chloride solution; – Ringer acetate solution;- 5% glucose solution.

Overdose

There are several known cases of overdose. There are no specific symptoms or signs. The specific antidote is unknown. Treatment consists of symptomatic and supportive therapy.

Special instructions

If there is no decrease in uterine contractility during the use of Traktocil, uterine contractions should be monitored, as well as fetal heart rate. You should also consider using other medications. There is no experience of using atosiban in patients with impaired liver and kidney function. Atosiban is not used in cases of abnormal placental attachment. As an oxytocin antagonist, atosiban can theoretically promote uterine relaxation and provoke postpartum uterine bleeding, so the degree of blood loss after childbirth should be constantly evaluated. Influence on the ability to drive a car and mechanisms that require increased attention. Not applicable, given the indications for use.

Form of production

Concentrate for preparation of infusion solution,7.5 mg / ml.

Storage conditions

The drug should be stored out of the reach of children in its original packaging at a temperature of 2-8°C. After opening the concentrate bottle, dilution should be performed immediately. The diluted solution for intravenous infusion should be used within 24 hours after preparation.

Shelf

life is 4 years.

Active ingredient

Atosiban

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

Pregnant women by doctor’s prescription