Active substanceAtosibanAtosiban
Similar drugsTo uncover
  • Atosiban
    concentrate d / infusion 
  • Tractocyl
    concentrate d / infusion 
    Ferring AB     Sweden
  • Dosage form: & nbspconcentrate for solution for infusion
    Composition:

    Composition per 1ml:

    active substance: atosibane acetate in terms of atosiban 7.5 mg;

    Excipients: mannitol 50 mg, hydrochloric acid to pH 4.5, water for injection up to 1 ml.

    Description:A clear, colorless solution.
    Pharmacotherapeutic group:a suppressant agent - an inhibitor of oxytocin receptors.
    ATX: & nbsp

    G.02.C.X   Other drugs for use in gynecology

    G.02.C.X.01   Atosiban

    Pharmacodynamics:

    Active component of the drug Traktotsil 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 with this does not affect the cardiovascular system.

    In the case of premature birth in women atosiban in the recommended doses suppresses uterine contractions and provides the uterus functional peace.

    Relaxation of the uterus begins immediately after the administration of atosiban, within 10 minutes the contractile activity of the myometrium is significantly reduced, maintaining a stable functional uterine rest (<4 cuts per hour) for 12 hours.
    Pharmacokinetics:

    Pharmacokinetic parameters (volume of distribution, clearance and half-life) do not depend on the dose.

    - distribution: after intravenous infusion (300 μg / mi for 6 to 12 hours) the maximum concentration of atosiban Cmin plasma is reached within 1 hour after the start of infusion (on average 442 ± 73 ng / ml, in the range from 298 to 533 ng / ml). Binding to proteins, plasma is 46 - 48%. Atosiban penetrates the placental barrier. After the administration of Tractocil 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 the volume distribution is 18.3 ± 6.8 liters.

    - Metabolism: 2 metabolites were identified in 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.

    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 () and final () the half-life of 0.21 ± 0.01 and 1.7 ± 0.3 hours, respectively. The average clearance of the drug is 41.8 ± 8.2 liters / hour.

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

    Traktotsil is used in case of 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;

    - 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;

    - The normal heart rate of 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 intrauterine infection;

    Placenta previa;

    Placental abruption;

    Any condition of the mother and fetus, in which the preservation of pregnancy

    represents a danger;

    Breast-feeding;

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

    Carefully:

    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.

    With caution use Traktotsil in multiple pregnancies, as well as at the gestation period of 24 to 27 weeks (due to lack of sufficient clinical experience).

    Pregnancy and lactation:

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

    Traktotsil is contraindicated in breastfeeding.
    Dosing and Administration:

    Traktotsil is administered intravenously immediately after the diagnosis of "premature birth" in three stages:

    - First, for 1 minute, 1 vial of 0.9 ml of the drug is administered without dilution (initial dose of 6.75 mg),

    - 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 carried out for 3 hours;

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

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

    If there is a need for repeated use of the drug Traktotsil, also should begin with the 1 stage, followed by the infusion introduction of the drug (steps 2 and 3). 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 preparing a solution for infusion (stages 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 bottles) of Tractocil are 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 the solution or the solution has changed color.

    Side effects:

    Very often (> 1/10)

    Disorders from the gastrointestinal tract: nausea, rarely vomiting.

    Often (> 1/100, <1/100)

    Metabolic disorders: hyperglycemia.

    Disorders from the central nervous system: headache, dizziness.

    Disorders from the cardiovascular system: tachycardia, arterial hypotension; "Tides".

    Rarely (> 1/1000, <1/100)

    Disorders from the central nervous system: insomnia.

    From the skin: itching, skin rash.

    Local reactions: hyperthermia at the injection site.

    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 if you notice any other side effects not listed in the instructions, tell your doctor.

    Overdose:

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

    Treatment consists in symptomatic and maintenance therapy.

    Interaction:

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

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

    Labetalol does not affect the pharmacokinetics of the drug Traktotsil.

    The interaction of the drug Traktotsil with antibiotics is unlikely.

    Joint use of the drug Traktotsil with ergot alkaloids is inappropriate in connection with the opposite pharmacological action and indications for use.

    Special instructions:

    In the absence of a decrease in the contractile activity of the uterus during the administration of the drug Traktocil, uterine contractions should be monitored, and behind heart rate of the fetus. 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 oxytocin antagonist, atosiban can theoretically contribute to relaxation uterus and provoke postpartum uterine bleeding, therefore, it is necessary to constantly assess the degree of blood loss after childbirth.

    Effect on the ability to drive transp. cf. and fur:

    Not applicable, given indications for use.

    Form release / dosage:

    Concentrate for the preparation of a solution for infusions 7.5 mg / ml.

    Packaging:

    For 0.9 ml of the drug in a colorless vial with a capacity of 2 ml of glass type I, sealed with a bromobutyl cork of gray color and hermetically sealed with a "flip-off" cap.

    For 5 ml of the preparation in a colorless vial with a capacity of 5 ml of glass type I, sealed with a bromobutyl cork of gray color and hermetically sealed with a "flip-off" cap.

    For 1 bottle in plastic packaging in a cardboard box along with instructions for use.
    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 expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001692
    Date of registration:03.05.2012
    The owner of the registration certificate:Ferring ABFerring AB Sweden
    Manufacturer: & nbsp
    Representation: & nbspFERRING PHARMACEUTICALS BV FERRING PHARMACEUTICALS BV Netherlands
    Information update date: & nbsp03.12.2012
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