Traktocil 7.5 mg/mL 5 mL

Pharmacodynamics

The active component is a drug Traktotsil atosiban, a synthetic peptide, which is a competitive antagonist at human oxytocin receptor level.

Atosiban, oxytocin binding to receptors reduces the frequency of uterine contractions and tone of the myometrium, leading to inhibition of uterine contractility. Also atosiban vasopressin binds to receptors, inhibiting the effect of vasopressin, but it has no effect on the cardiovascular system.

In the case of preterm birth in women atosiban at the recommended doses, inhibits contractions of the uterus and uterine function provides peace. uterine relaxation begins immediately after the administration of atosiban, for 10 min contractility of myometrial activity is significantly reduced while maintaining a stable functional uterine rest (< 4 cuts / h) for 12 h
.

Pharmacokinetics

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

Distribution.

After the on / in infusion (300 mcg / min for 6-12 hr) Cmax atosiban plasma achieved within 1 hour after the start of infusion (mean (442 ± 73) ng / mL, ranging from 298 to 533 ng / ml ). Binding to plasma proteins is 46-48%. Atosiban crosses the placental barrier. After administration Traktotsil at 300 mcg / min atosiban concentration ratio in the body of the fetus and atosiban concentration in the mother equal to 0.12. The average value Vd – (18,3 ± 6,8) l
.

Metabolism.

In plasma and urine metabolites identified 2. The ratio of the concentration of the main metabolite M1 and atosiban concentration in plasma was 1.4 and 2.8 for the second hour of infusion and after termination, respectively. The metabolite M1 has pharmacological activity on a par with atosiban and passes into breast milk.
Inhibition of cytochrome P450 isoforms atosiban unlikely.

Withdrawal.

After stopping the infusion of the drug concentration in plasma rapidly decreases from the initial value (Ta) and final (Tp) T1 / 2 (0,21 ± 0,01) and (1,7 ± 0,3) h, respectively. The mean value of drug clearance – (41,8 ± 8,2) l / h
.
Atosiban is determined in urine in very small quantities, its concentration in the urine in the 50-fold lower concentration of M1. Number of atosiban excreted in the faeces, was not determined.

Active substance:
Atosiban

Manufacturer

Ferring GmbH, Germany

Prescribing

Pregnant on prescription

Composition

Composition per 1 ml:

active substance:

atosiban acetate based on atosiban 7.5 mg;

Excipients:

mannitol 50 mg,

hydrochloric acid up to pH 4,5,

Water for injections to 1 mL.

Indications

Traktotsil used in threatened preterm labor in pregnant women in the following cases:

• regular uterine contractions of at least 30 and with a frequency greater than 4 over 30 min;
• cervix from 1 to 3 cm (0-3 cm for nulliparous women);
• the age of 18 years;
• gestational age from 24 to 33 completed weeks;
• a normal heart rate of the fetus.

Contraindications

• Gestational age less than 24 or over 33 completed weeks;
• premature rupture of membranes in pregnancies of more than 30 weeks;
• intrauterine growth retardation;
• abnormal heart rate of the fetus;
• uterine bleeding that requires immediate delivery;
• eclampsia and severe pre-eclampsia requiring immediate delivery;
• intrauterine fetal death;
• suspicion of infection in the mother;
• placenta previa;
• placental abruption;
• any maternal and fetal condition in which the continuation of the pregnancy is dangerous;
• breastfeeding;
• hypersensitivity to atosiban or any of the product components.

Caution: in case of suspicion of premature rupture of membranes Traktotsil use of the drug to prolong the delivery must be weighed against the potential risk of chorioamnionitis. Traktotsil used with caution in multiple pregnancy, and in gestational age 24-27 weeks (due to lack of sufficient clinical experience).

Side effects

On the part of the digestive tract: very common (> 1/10) – nausea, rarely – vomiting
.

Metabolism: often (> 1/100, < 1/10) – hyperglycemia
.

CNS: often (> 1/100, < 1/10) – headache, dizziness; rarely (> 1/1000, < 1/100) – insomnia
.

From the CCC: often (> 1/100, < 1/10) – tachycardia, hypotension, flushing
.

Skin: rare (> 1/1000, < 1/100) – itching, skin rash
.

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

On the part of the reproductive organs: very rare (> 1/10000, < 1/1000) – uterine bleeding / uterine atony
.

If any of these instructions side effects are compounded, or develop any other side effects not mentioned in the instructions, you should inform your doctor.

How to accept, acceptance rate and dosage

Traktotsil entered in / in immediately after diagnosis of preterm delivery in 3 stages:
1) at the beginning, during 1 min I fl is introduced. 0.9 ml of the product without dilution (starting dose – 6.75 mg);
2) immediately thereafter held for 3 hours infusion preparation in a dose of 300 mcg / min (injection rate – 24 ml / h, atosiban dose – 18 mg / hr);
3) thereafter held prolonged (45 h) infusion preparation Traktotsil a dose of 100 mcg / min (the rate of introduction – 8 ml / h, the dose atosiban – 6 mg / h)
.

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

If there is a need to re-use of the drug Traktotsil should also start with the 1st stage, behind which will follow the introduction of the infusion of the drug (steps 2nd and 3rd).
Repeated use can begin at any time after the first use of the drug, it can be repeated up to 3 cycles.
If after 3 cycles of therapy with Traktotsil uterine activity is not reduced, it is necessary to consider the application of another drug.

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

The concentrate is diluted in one of the following solutions:
– 0.9% sodium chloride solution;
– Ringer’s acetate solution;
– 5% glucose solution
.

Storage conditions

The drug should be stored in reach of children in the original package at temperature 2-8 ° C. After opening the vial with the concentrate dilution should be carried out immediately. Single solution for in / infusion should be used within 24 hours after preparation.

Active substance

Atosiban

Interaction

Interaction with other drugs

Traktotsil not affect the pharmacokinetics of drugs metabolized by the cytochrome P450.
In a joint application of the drug Traktotsil betamethasone and there were no clinically significant interactions.

Labetalol has no effect on the pharmacokinetics of the drug Traktotsil.

Interaction Traktotsil medication with antibiotics is unlikely.

The combined use of the drug Traktotsil with ergot alkaloids inexpedient in connection with the opposite pharmacological effect and indications for use.

Special conditions

In the absence of reducing uterine activity during administration of the drug should Traktotsil monitoring uterine contractions, as well as to monitor the fetal heart rate. You should also consider the use of other drugs.

Experience of atosiban in patients with impaired liver function and kidney offline.

Atosiban does not apply in cases of abnormal attachment of the placenta. As an antagonist of oxytocin, atosiban may theoretically facilitate uterine relaxation and trigger postpartum uterine bleeding, so you should continually assess the degree of blood loss after childbirth.

Effects on ability to drive and use mechanisms that require attention. Not applicable, given the indications for use.

Pregnancy and lactation

Traktotsil should be used only in case of diagnosed preterm labor for a period from 24 to 33 completed weeks of pregnancy.
Traktotsil contraindicated during breastfeeding.

Overdose

There are several known cases of overdose. Specific symptoms and signs are absent. A specific antidote is not known.

Treatment is symptomatic and supportive therapy.

Weight	0.026 kg
Expiration date	4 years.
Dosage form	Infusion solution