Drug intelligence / Profile preview

oxytocin + methylergonovine + carboprost

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Peptides
Administration
Intravenous, Intramuscular, Intramyometrial
01

Overview

This is a combination of three uterotonic agents—oxytocin, methylergonovine, and carboprost—used in the management of postpartum hemorrhage (PPH) due to uterine atony. - **Oxytocin** is a peptide hormone that stimulates uterine smooth muscle contraction by acting as an agonist at the oxytocin receptor. It is considered the first-line agent for restoring uterine tone and preventing or treating PPH. - **Methylergonovine** is an ergot alkaloid that acts primarily as an agonist at serotonin and alpha-adrenergic receptors on uterine smooth muscle, causing sustained contractions. It serves as a second-line agent when oxytocin alone is insufficient but carries risks such as hypertension and vasoconstriction. - **Carboprost** is a synthetic prostaglandin F2α analog that induces myometrial contractions via prostaglandin F receptor activation; it also serves as a second-line agent for refractory cases but may cause bronchospasm or gastrointestinal side effects. The combination may be used sequentially or together in severe cases of PPH unresponsive to monotherapy, with each drug targeting different pathways to maximize efficacy in restoring uterine tone[1][3][5].

02

Targets

HTR2A (Serotonin receptor 5-HT2A)DRD (Dopamine receptors)Oxytocin receptorPTGFR (Prostaglandin F2 alpha receptor)ADRA1A (α1A)ADRA1 (Alpha-1 adrenergic receptor family)

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