Clinical and pharmacological group: & nbsp
Tokolitiki
Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):VED
АТХ:G.02.C.X Other drugs for use in gynecology
G.02.C.X.01 Atosiban
Pharmacodynamics:Atosiban is a synthetic peptide that is antagonist of human oxytocin at the receptor level. Competitively blocks oxytocin receptors of the uterus, in connection with which reduces the frequency of uterine contractions and tone of the myometrium. The contractile activity of the myometrium is inhibited 10 minutes after the administration of the drug. The drug provides stability of functional resting of the uterus within 12 hours - less than 4 cuts per hour.
Pharmacokinetics:The maximum concentration in the blood plasma is reached after 1 hour. Relationship with plasma proteins 46-48%. Penetrates through the placenta.
Half-life is 20-30 minutes.
Metabolized in plasma with the formation of 2 metabolites, one of which M1 (the main metabolite) is pharmacologically active on a par with atosiban. M1 is found in breast milk.
Elimination with urine in the form of metabolites.
Indications:Used for tocolysis in case of threat of premature birth in the period of pregnancy from 24 to 33 weeks.
XV.O60-O75.O60 Premature birth
Contraindications:The gestation period is below 24 and above 33 weeks.
Obstetric situations requiring immediate delivery: placental abruption, eclampsia, fetal hypoxia, dead fetus, etc.
Individual intolerance.
Carefully:It is used with caution in the premature escape of amniotic fluid - the risk of developing chorioamnionitis.
Pregnancy and lactation:Pregnancy and lactation: recommendations for Food and Drug Administration (US Food and Drug Administration) - Category B. It is used during pregnancy. It enters the breast milk, is not used for lactation.
Dosing and Administration:The scheme of three-stage intravenous administration is applied:
1. Within 1 minute, the initial dose of 6.75 mg is administered.
2. Infusion for 3 minutes 300 μg per minute at a rate of 24 ml per hour - a dose of 18 mg per hour.
3. Prolonged infusion of the drug (up to 48 hours) at a dose of 100 mcg per minute at a rate of 8 ml per hour (dose - 6 mg per hour).
If necessary, the course of tocolysis is repeated at any time, but in accordance with the instruction for phased introduction, starting with the bolus dose. It is allowed to repeat 3 cycles. In the case of low efficiency after 3 cycles, discontinue the introduction of atosiban, replacing it with another drug.
The highest daily dose: 330 g.
The highest single dose: 6.75 mg.
Side effects:Central and peripheral nervous system: insomnia.
Cardiovascular system: tachycardia, arterial hypotension.
The digestive system: nausea and vomiting - are possible at the very beginning of treatment, after the administration of the bolus dose.
Reproductive system: atony of the uterus.
Allergic reactions.
Overdose:Increased manifestation of side effects. It is necessary to reduce the rate of infusion or stop the administration of the drug.
Interaction:Antagonist of ergot preparations.
With simultaneous use with labetalol labetalol maximum concentration is reduced by 36% and the half-life is increased by 45 minutes. The pharmacokinetics of the atosiban remain unchanged.
Special instructions:In case of premature rupture of membranes on the further tocolysis is solved in accordance with the obstetric situation. If a positive decision is made on the prolonging pregnancy prevention of chorioamnionitis and antibiotic therapy administered surfactants for fetal lung maturation.
With the development of labor after tocolysis, it is necessary to prevent postpartum hemorrhage.