Tractocile [Atosiban]
1431 Items
2019-09-19
- done All payments are SSL encrypted
- done Full Refund if you haven't received your order
- done International shipping to the USA, UK and Europe
Clinical Pharmacology
Tractoxil - a synthetic peptide, a competitive antagonist of human oxytocin at the receptor level. By binding to oxytocin receptors, it reduces the incidence of uterine contractions and myometrial tone, leading to inhibition of uterine contractility.Tractoxil also binds to vasopressin receptors, thus inhibiting the effect of vasopressin.
In case of preterm birth,Tractoxil in recommended doses inhibits uterine contractions and provides functional rest to the uterus. Uterine relaxation begins almost immediately after the injection. Within 10 minutes, the contractile activity of the myometrium is significantly reduced, maintaining a stable functional rest of the uterus (less than 4 contractions per hour) for 12.
Pharmacokinetics.
Distribution
In healthy non-pregnant women who received atociban in the form of infusions from 10 to 300 mcg / min for 12 hours, persistent plasma concentrations increased in proportion to the dose. Clearance of the drug, Vdand t1/2 do not depend on the dose.
In women receiving Atobacan in the form of intravenous infusions of 300 mcg / min for 6–12 h during preterm labor, a steady plasma concentration was reached within 1 h after the start of the infusion, on average, 442 ± 73 ng / ml, in the range of 298– 533 ng / ml.
Medium Vd- 18.3 ± 6.8 l. A binding to plasma protein in pregnant women ranges from 46 to 48%. Atociban penetrates the placenta.
Metabolism and excretion
Two metabolites have been identified in human blood plasma and urine. The ratio of the concentrations of the main metabolite M1 (des- (ornithine, glycine-NH2) - [Mpa, D-tyrosine (Et)2, threonine-oxytocin) and plasma atomic concentration were 1.4 and 2.8 during the second hour of infusion and after its cessation, respectively. It is not known whether the metabolite accumulates M1 in the tissues. Atosiban is determined in urine in very small quantities, its concentration in urine is 50 times less than the concentration of metabolite M1. Metabolite M1 is a pharmacologically active metabolite regarding inhibition of oxytocin-induced uterine contractions in vitro. Metabolite M1 penetrates into breast milk.
After cessation of infusion, the concentration of the drug in the blood plasma rapidly decreased. T1/2 α-phase - 0.21 ± 0.01 h, T1/2 β-phases - 1.7 ± 0.3 h. The average clearance of the drug - 41.8 ± 8.2 l / h.
Indications
With the threat of preterm birth.
For inhibition of labor in spontaneous preterm labor in the following cases:
- regular uterine contractions with a duration of at least 30 seconds and a frequency of more than 4 times within 30 minutes;
- dilation of the cervix from 1 to 3 cm for giving birth, from 0 to 3 cm for those who have not given birth;
- women over 18;
- gestation period from 24 to 33 full weeks;
- normal fetal heart rate.
Composition
Excipients:mannitol (E421), hydrochloric acid 1M, water d / i.
No customer reviews for the moment.
Dosage and Administration
TherapyTractocyl should be prescribed and administered by a qualified doctor with experience in preterm labor.
The drug is administered IV 3 consecutive stages:
- First, a bolus injection for the initial dose of 6.75 mg.
- Immediately after this, a continuous infusion of the concentrate is carried out to prepare an infusion solution at a high dose of 300 mcg / min (load infusion) for 3 hours.
- After that, a long-term (up to 45 h) infusion of the concentrate is carried out at a low dose of 100 mcg / min.
The duration of treatment should not exceed 48 hours.
The total dose of the drug for the entire course of therapy should not exceed 330 mg. IV the one-stage administration of the drug should be carried out immediately after diagnosis. After the bolus dose is administered, the infusion should begin.
If the contractile activity of the uterus persists during therapyTractocylshould consider the treatment of another drug.
Data on the need for a special selection of doses in patients with hepatic and renal insufficiency are not available.
The table shows the method of dosing the drug for bolus and subsequent infusion.
| Stage | Mode | Injection / Infusion Rate | Dose of atosiban |
| 1 | 0.9 ml i / v bolus | within 1 min | 6.75 mg |
| 2 | 3-hour IV loading infusion | 24 ml / h | 18 mg / h |
| 3 | next continuous infusion | 8 ml / h | 6 mg / h |
If necessary, reapplyTracts, it must again be started with a bolus injection followed by an infusion in the usual manner.
Repeated treatment can begin at any time after the first course, you can spend up to 3 repeated courses.
Adverse reactions
In clinical studies, possible adverse reactions on the part of the mother's body were described and no specific adverse reactions of atosiban in newborns were identified. The side effects observed in newborns were not significant.
In women, the following adverse reactions were observed.
From the digestive system: nausea, vomiting.
From the side of the central nervous system: headache, dizziness, insomnia.
On the part of the endocrine system: hyperglycemia.
Since the cardiovascular system: tachycardia, hypotension, rush of blood.
From the reproductive system: uterine bleeding, uterine atony.
Other: reactions at the injection site, itching, rash.
Contraindications
- gestation period is less than 24 weeks or more than 33 full weeks;
- premature rupture of membranes during pregnancy for more than 30 weeks;
- intrauterine growth retardation, accompanied by a violation of fetal heart rhythm;
- prenatal uterine bleeding, which requires emergency delivery;
- fetal death;
- suspected intrauterine infection;
- placenta previa;
- premature detachment of a normally located placenta;
- eclampsia and severe pre-eclampsia, which requires emergency delivery;
- hypersensitivity to the active substance or other components of the drug in history.
Drug interactions
Given the lack of studies on drug compatibility,Tractoxil do not mix with any other drug. This makes it possible to carry out continuous independent control of the rate of infusion.
In vitro studies have shown that atosibanne is a substrate of the cytochrome P450 system and does not inhibit the utilization of drugs by the enzymes of this system, therefore it is unlikely that atosiban is involved in drug interactions mediated by cytochrome P450.
With the combined use of atosiban and betamethasone, there were no clinically significant interactions.
When combined use of atosiban and labetalol Cmaxlabetalol decreased by 36%, and the maximum T1/2lengthened by 45 min, although the nature of the bioavailability of labetalol did not change. Labetalol did not affect the pharmacokinetics of atosiban.
Other studies of drug interactions with antibiotics, ergot alkaloids, antihypertensive drugs, with the exception of labetalol, have not been conducted.
Pregnancy and Lactation
Tractoxil should be used only for preterm birth from 24 to 33 full weeks of pregnancy.
Studies have shown the absence of the embryo-and phototoxic effect of atosiban.
In clinical trials of atosiban, no effect on lactation was detected. It is proved that a small amount of the drug penetrates into breast milk.
Special instructions
In the case whenTractoxil used in patients in whom it is impossible to exclude premature rupture of the membranes, the advantage of the prolongation of labor should be compared with the potential risk of developing chorioamnionitis.
Application ExperienceTracts in patients with impaired liver and kidney absent.
Overdosage
Several cases of overdose have been described that have passed without specific symptoms and signs.
Treatment:symptomatic, specific therapy is required.
- Active ingredient: Atosiban
Studies and clinical trials of Atosiban (Click to expand)
- Quantitative determination of oxytocin receptor antagonist atosiban in rat plasma by liquid chromatography–tandem mass spectrometry
- Development and clinical experience with the new evidence-based tocolytic atosiban
- Clinical practice evaluation of atosiban in preterm labour management in six European countries
- Effectiveness and safety of the oxytocin antagonist atosiban versus beta-adrenergic agonists in the treatment of preterm labour
- The oxytocin/vasopressin receptor antagonist atosiban delays the gastric emptying of a semisolid meal compared to saline in human
- Design of Oxytocin Antagonists, which are more Selective than Atosiban
- Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban
- Molecular Dynamics of Complexes of Atosiban with Neurohypophyseal Receptors in the Fully Hydrated Phospholipid Bilayer
- Tocolysis with atosiban: experience in the management of premature labor before 24
- Elevated cardiac oxidative stress in newborn rats from mothers treated with atosiban
- Effectiveness and safety of the oxytocin antagonist atosiban versus beta-adrenergic agonists in the treatment of preterm labour
- Atosiban for the primary prevention of preterm labour
- The in vitro effect of dual combinations of ritodrine, nicardipine and atosiban on contractility of pregnant rat myometrium
- Effectiveness of nifedipine versus atosiban for tocolysis in preterm labour: a meta-analysis with an indirect comparison of randomised trials
- A prospective randomised trial of atosiban versus hexoprenaline for acute tocolysis and intrauterine resuscitation
- Pharmacokinetic interaction studies of atosiban with labetalol or betamethasone in healthy female volunteers
- Multicentre, parallel group, randomised, single-blind study of the safety and efficacy of atosiban versus ritodrine in the treatment of acute preterm labour in Korean women
- Clinical practice evaluation of atosiban in preterm labour management in six European countries
- Authors response to: Evaluation of the effects of atosiban on breast feeding
- The use of atosiban and ritodrine in external cephalic version
- OP19.01: Atosiban, magnesium sulfate and ritodrine therapy for preterm labor: effects on uterine, fetal umbilical and middle cerebral artery Doppler parameters in the first 24 hours
- Atosiban treatment for uterine hyperactivity during active labor
- PP-22. Effectiveness and safety of the oxytocin antagonist atosiban in the treatment of preterm labour
- Oxytocin Stimulated Release of PGF2α and its Inhibition by Indomethacin and Atosiban During Culture of Equine Endometrial Explants
8 other products in the same category:
arrow_upward