Atosiban
Tractocile, Antocin, Atosiban SUN (generic), RWJ 22164, ORF 22164
1What it is
Atosiban is an oxytocin-receptor blocker — a tocolytic, meaning a drug given to pause labour. It was designed in the 1980s by substituting four positions of oxytocin so the molecule still docks on the receptor but no longer activates it. Ferring developed it as Tractocile; the EMA approved it in January 2000 to delay imminent preterm birth between 24 and 33 completed weeks of pregnancy. The US FDA declined approval in 1998 after an advisory committee was unconvinced by efficacy data and troubled by an imbalance in infant deaths in the placebo-controlled trial, and the company did not resubmit.
Its appeal is tolerability. Older tocolytics (beta-agonists such as ritodrine and terbutaline) cause maternal tachycardia, pulmonary oedema and metabolic effects; atosiban acts on the uterus with few systemic effects. The question the literature has never settled is whether delaying labour by 48 hours — the time needed for antenatal steroids and transfer to a neonatal unit — improves babies' outcomes, with any tocolytic.
2How it's thought to work
Oxytocin and vasopressin acting on uterine receptors release calcium from stores and drive myometrial contraction. Atosiban competes for those receptors (affinity for V1a is actually higher than for the oxytocin receptor, which may matter because vasopressin contributes to preterm contractions). Reduced calcium signalling lowers contraction frequency and amplitude. It does not treat the underlying cause of preterm labour (infection, inflammation, cervical insufficiency), which is one reason effects on prolongation are modest.
3What the research shows
Versus placebo
Versus beta-agonists
Systematic reviews
Threatened preterm birth at 30–34 weeks (APOSTEL 8)
IVF embryo transfer
4Reported side effects and interactions
Literature-reported
nausea (most common, ~12%), headache, dizziness, hot flushes, vomiting, tachycardia, hypotension, hyperglycaemia, injection-site reactions; rarely uterine haemorrhage or atony after birth (theoretical from receptor blockade), pulmonary oedema (mostly with concurrent beta-agonists or multiple pregnancy), allergic reactions. In the placebo-controlled trial there was a numerical excess of fetal/infant deaths at very early gestations, not confirmed elsewhere. Contraindicated before 24 weeks or after 33 completed weeks, with ruptured membranes after 30 weeks, fetal distress, antepartum haemorrhage, eclampsia or intrauterine infection.Community-reported
essentially none documented.Theoretical. antagonism of oxytocin receptors could in principle blunt postpartum uterine contraction if delivery follows rapidly.
Interactions. no cytochrome interactions; labetalol and betamethasone studied without clinically relevant interaction; limited data with other tocolytics (combination generally avoided).
Markers researchers commonly monitor
From the label and obstetric practice:
| Marker | Why it's watched |
|---|---|
| Uterine contraction frequency (tocodynamometry) and cervical change | the direct treatment response. |
| Fetal heart rate monitoring | standard throughout tocolysis. |
| Maternal pulse, blood pressure, fluid balance, respiratory assessment | pulmonary oedema risk, mainly in multiple pregnancy or with corticosteroids. |
| Blood glucose | hyperglycaemia is reported, relevant alongside antenatal steroids and in diabetic women. |
| Signs of infection (temperature, CRP, white cell count) | chorioamnionitis is a contraindication and a common underlying cause. |
Free for everyone. Safety information is never behind a paywall.
5Reconstitution and handling
Supplied as a 6.75 mg/0.9 mL solution for the bolus and 37.5 mg/5 mL concentrate for dilution into a 100 mL infusion bag. Prepared and run by hospital staff via infusion pump according to the three-step label regimen. The calculator is not applicable.
6Commonly studied alongside
Nifedipine and beta-agonists (comparator tocolytics), antenatal corticosteroids and magnesium sulphate (co-therapies the 48-hour delay is meant to enable), oxytocin (#48) and carbetocin (#216, the agonist counterpart), retosiban and barusiban (later oxytocin antagonists whose development was discontinued).
Informational cross-links. Not stack recommendations.
7Regulatory status by region
| Region | Status (checked —) |
|---|---|
| United States | Not FDA-approved (application not approved 1998); not marketed |
| European Union | EMA centrally authorised (Tractocile, January 2000); generics authorised since 2013 |
| United Kingdom | MHRA-licensed (Tractocile and generics); hospital use |
| Australia | TGA-registered (Tractocile) |
| South Africa | SAHPRA-registered † |
| Sport (WADA) | Not prohibited |
8Open questions
- Does any tocolytic improve neonatal outcomes, or only prolong pregnancy by hours to days?
- The unexplained infant-death imbalance at very early gestations in the placebo trial.
- Whether maintenance (prolonged) tocolysis after the acute episode has any value — current evidence says no.
9References
- 1Romero R et al. (2000). An oxytocin receptor antagonist (atosiban) in the treatment of preterm labor: a randomized, double-blind, placebo-controlled trial with tocolytic rescue. Am J Obstet Gynecol. PubMed · DOI
- 2Worldwide Atosiban versus Beta-agonists Study Group (2001). Effectiveness and safety of the oxytocin antagonist atosiban versus beta-adrenergic agonists in the treatment of preterm labour. BJOG. PubMed
- 3Flenady V et al. (2014). Oxytocin receptor antagonists for inhibiting preterm labour. Cochrane Database Syst Rev. PubMed · DOI
- 4van Vliet EOG et al. (2016). Nifedipine versus atosiban for threatened preterm birth (APOSTEL III): a multicentre, randomised controlled trial. Lancet. DOI
- 5Ng EHY et al. (2014). A randomized double blind comparison of atosiban in patients undergoing IVF treatment. Hum Reprod. PubMed · DOI
- 6European Medicines Agency. Tractocile EPAR — scientific discussion and current Summary of Product Characteristics. PubMed
References are being resolved to PubMed/DOI identifiers; links search PubMed for the citation until then.
† Being confirmed by our reviewers against current sources.
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Self-reported side effects Phase 2
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