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approvedHormone Regulation

Carbetocin

Also known as: Pabal, Duratocin, 1-Deamino-1-monocarba-oxytocin, Long-Acting Oxytocin

Carbetocin is a synthetic long-acting analog of oxytocin with a single amino acid modification (replacement of the disulfide bridge with a thioether linkage) that confers resistance to enzymatic degradation while retaining full agonist activity at oxytocin receptors. Approved in over 30 countries (including the EU and Canada, but not the US) for the prevention of postpartum hemorrhage (PPH) following cesarean delivery, carbetocin offers a major practical advantage over oxytocin: a single IV or IM injection replaces multi-hour oxytocin infusions. The landmark WHO CHAMPION trial (2018) demonstrated non-inferiority to oxytocin for PPH prevention, including in tropical settings where carbetocin is heat-stable.

3 cited references·5 researched benefits

Quick Answer

Carbetocin is a long-acting synthetic oxytocin analog approved in 30+ countries for preventing postpartum hemorrhage after cesarean delivery. A single injection provides sustained uterine contraction for 1-2 hours, replacing the need for prolonged oxytocin infusions. The WHO CHAMPION trial confirmed non-inferiority to oxytocin. Its heat-stable formulation is particularly valuable in low-resource tropical settings where oxytocin requires refrigeration.

Key Facts

Mechanism
Carbetocin is a full agonist at the oxytocin receptor (OXTR) on uterine myometrial cells. Receptor activation triggers Gq-mediated phospholipase C signaling, generating IP3 and DAG, which mobilize intracellular calcium stores and activate protein kinase C. The resulting sustained increase in intracellular calcium drives rhythmic and tonic uterine contractions that compress myometrial blood vessels (the "living ligature" mechanism), preventing postpartum hemorrhage. The thioether bridge replacing the disulfide bond in native oxytocin makes carbetocin resistant to aminopeptidase and disulfidase degradation, extending the duration of action to approximately 1-2 hours compared to oxytocin's 3-5 minute half-life. Carbetocin also retains oxytocin's effect on mammary myoepithelial cells, supporting lactation.
Research Status
approved
Half-Life
~40 minutes (approximately 10× longer than oxytocin)
Molecular Formula
C₄₃H₆₇N₁₁O₁₂S
Primary Use
Hormone Regulation
Table of Contents

Benefits

  • Prevents postpartum hemorrhage after cesarean delivery — non-inferior to oxytocin infusion in the WHO CHAMPION trial (n=29,645)strong
  • Single-dose convenience — one IM or IV injection replaces multi-hour oxytocin infusion, reducing nursing workload and medication errorsstrong
  • Heat-stable formulation — does not require cold chain storage, critical for use in tropical and low-resource settings where oxytocin degradesstrong
  • Sustained uterotonic effect lasting 1-2 hours — provides more consistent uterine contraction than intermittent oxytocin bolusesstrong
  • Being researched for autism spectrum disorder and social cognition — intranasal carbetocin may provide longer-lasting pro-social effects than oxytocin due to extended half-lifepreliminary

Dosage Protocols

RouteDosage RangeFrequencyNotes
Intravenous injection (PPH prevention, cesarean)100 mcgSingle dose given slowly over 1 minute after delivery of infantStandard WHO/international dose for cesarean PPH prevention. Given immediately after umbilical cord clamping. No additional uterotonics needed in most cases.
Intramuscular injection (PPH prevention, vaginal delivery)100 mcgSingle dose after delivery of the placentaWHO CHAMPION trial used IM route. The heat-stable formulation is stored at room temperature (up to 30°C for 36 months), making it ideal for settings without reliable refrigeration.
Intranasal (research — social cognition)24-48 IUSingle dose in research settingsInvestigational use for autism and social behavior research. Extended half-life compared to oxytocin may produce more sustained effects on social cognition. Not approved for this indication.

Medical disclaimer

Dosage information is provided for educational reference only. Always follow your prescriber's instructions and consult a qualified healthcare provider before starting any peptide protocol.

Side Effects

  • Nausea and vomiting — the most commonly reported side effects, occurring in 5-15% of patientscommon
  • Abdominal pain and cramping — due to uterotonic activity, usually mild and self-limitingcommon
  • Headache — reported in 3-8% of patients in clinical trialscommon
  • Flushing and sensation of warmth — transient vasodilation reported in approximately 5% of patientscommon
  • Hypotension — may cause a transient drop in blood pressure, particularly with rapid IV injection; monitor hemodynamically unstable patientsrare

Frequently Asked Questions

Why is carbetocin not approved in the United States?
Carbetocin is approved in over 30 countries including Canada, EU member states, and many developing nations, but has not received FDA approval in the United States. This is primarily a regulatory and commercial decision: the manufacturer has not completed the FDA-specific clinical trials and application process required for US approval. In US hospitals, oxytocin (Pitocin) infusions remain the standard for PPH prevention and are well-established in clinical practice. The convenience advantage of carbetocin is less significant in well-resourced hospitals where nursing staff can monitor multi-hour oxytocin infusions. However, global advocacy continues for broader access, particularly given the heat-stability advantage.
How does carbetocin compare to oxytocin for preventing postpartum hemorrhage?
The WHO CHAMPION trial (2018, n=29,645) demonstrated that a single IM dose of heat-stable carbetocin was non-inferior to oxytocin for preventing blood loss >=500 mL and use of additional uterotonics after vaginal delivery. Both drugs had similar safety profiles. Carbetocin's advantages are primarily logistical: a single injection versus multi-hour infusion, no need for refrigeration, and reduced medication errors. Oxytocin is substantially cheaper and has decades more clinical experience. In resource-limited tropical settings, carbetocin's heat stability is a potentially life-saving advantage, as oxytocin degrades significantly when stored above 30°C.
What makes carbetocin heat-stable compared to oxytocin?
Oxytocin contains a disulfide bridge between cysteine residues that is susceptible to thermal degradation, oxidation, and hydrolysis — losing 14-24% of potency when stored at 30°C for 12 months. Carbetocin replaces this disulfide bridge with a thioether linkage and also deaminates the N-terminal cysteine. These modifications make the molecule resistant to thermal degradation while retaining full oxytocin receptor agonist activity. The heat-stable carbetocin formulation maintains >90% potency after 36 months at 30°C and 75% relative humidity, eliminating the cold-chain requirement that is a major barrier to reliable uterotonic availability in tropical countries.

References

  1. 1
    Heat-stable carbetocin versus oxytocin to prevent hemorrhage after vaginal birth (CHAMPION trial)(2018)PubMed ↗
  2. 2
    Carbetocin versus oxytocin for the prevention of postpartum hemorrhage: a systematic review and meta-analysis(2019)PubMed ↗
  3. 3
    Carbetocin: a review of its use in the prevention of postpartum hemorrhage(2009)PubMed ↗

Latest Research

Last updated: 2026-02-19