Traktocil, 7.5 mg/ml 5 ml

The active ingredient of Tractocil is atoziban, a synthetic peptide that is a competitive antagonist of human oxytocin at the receptor level.

Atoziban, binding to oxytocin receptors, reduces the frequency of uterine contractions and myometrial tone, leading to suppression of uterine contractility. Atoziban also binds to vasopressin receptors, inhibiting the effect of vasopressin, but has no effect on cardiovascular system.

In cases of premature labor in women atoziban inhibits uterine contractions and provides uterine functional rest in recommended doses. Uterine relaxation begins immediately after administering atoziban and myometrium contractile activity is significantly reduced within 10 minutes, maintaining stable functional peace of the uterus (<4 contractions/h) for 12 hours.

Pharmacokinetics

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

Distribution.

After intravenous infusion (300 mcg/min for 6-12 h), the Cmax of atoziban in plasma is reached within 1 h after the start of infusion (average (442±73) ng/mL, range 298 to 533 ng/mL). Binding to plasma proteins is 46-48%. Atoziban penetrates through the placental barrier. After administration of Tractocil at a rate of 300 µg/min, the ratio of atoziban concentration in the fetus to that of atoziban in the mother is 0.12. The mean Vd value is (18.3 ± 6.8) l.

Metabolism.

Two metabolites have been identified in plasma and urine. The ratio of the concentration of the main metabolite M1 to the plasma concentration of atoziban was 1.4 and 2.8 at the second hour of infusion and after discontinuation of the infusion, respectively. M1 metabolite has pharmacological activity on a par with atoziban and penetrates into breast milk.
Inhibition of cytochrome P450 isoforms by atoziban is unlikely.

Excretion.

After discontinuation of infusion, plasma drug concentration decreases rapidly with initial (Ta) and final (Tp) T1/2 values of (0.21±0.01) and (1.7±0.3) h, respectively. The mean drug clearance is (41.8±8.2) l/h.
Atoziban is determined in the urine in very small amounts, its concentration in the urine being 50 times lower than that of M1. The amount of atoziban excreted with feces was not determined.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

Overdose

Pregnancy use