Barusiban

Summary

Barusiban is a selective oxytocin receptor antagonist developed as a tocolytic agent for the management of preterm labor. It demonstrates high selectivity for the oxytocin receptor over vasopressin receptors, potentially offering an improved side-effect profile compared to atosiban. Clinical trials have investigated its use in inhibiting preterm uterine contractions.

Mechanism of Action

Selective competitive antagonist of the oxytocin receptor, blocking oxytocin-induced uterine contractions (tocolytic effect) without significant vasopressin receptor activity.

Routes of Administration

Goals & Uses

• Inhibition of preterm laborObstetric / TocolysisModerate
• Improved tocolytic tolerability vs atosibanSafety / PharmacologyLow
• Reduction of uterine contractionsObstetricsModerate

Contraindications

• Hypersensitivity to barusiban or related peptidesAllergyHigh
• Severe fetal distressObstetricHigh
• Intrauterine infection / chorioamnionitisObstetricHigh
• Placenta previa with active bleedingObstetricHigh

Adverse Effects

• Cardiovascular effects (tachycardia, hypotension)CardiovascularRare
• Injection site reactionsLocalCommon
• HeadacheNeurologicUncommonPain in the head or upper neck
• NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit

Drug Interactions

• OxytocinModerate
• Ergot alkaloids (e.g., ergometrine)Moderate

Population Constraints

• Multiple gestationObstetricRelative
• Gestational age < 24 weeks or > 34 weeksObstetricRelative
• Hepatic or renal impairmentOrgan ImpairmentRelative

Regulatory Status

• European UnionInvestigationalNot EMA-approved; clinical development conducted in European centers.
• United StatesInvestigationalNot FDA-approved; investigated in clinical trials for preterm labor tocolysis.
• United KingdomInvestigationalNot MHRA-approved; research use only.

Not approved by FDA, EMA, or other major regulatory agencies. Investigated in Phase II/III clinical trials for preterm labor but has not received marketing authorization.

Evidence & Sources

No sources recorded yet.