DT-Web

DB01282 - Carbetocin


Identification
Name Carbetocin
Accession Number DB01282
Type small molecule
Description Carbetocin is a drug used to control postpartum hemorrhage, bleeding after giving birth. It is an analogue of oxytocin, and its action is similar to that of oxytocin -- it causes contraction of the uterus.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 988.161
Groups approved
Monoisotopic Weight 987.484787417
Pharmacology
Indication Used to control postpartum hemorrhage and bleeding after giving birth.
Mechanism of action Carbetocin binds to oxytocin receptors present on the smooth musculature of the uterus, resulting in rhythmic contractions of the uterus, increased frequency of existing contractions, and increased uterine tone. The oxytocin receptor content of the uterus is very low in the non-pregnant state, and increases during pregnancy, reaching a peak at the time of delivery.
Absorption Bioavailability is 80% following intramuscular injection.
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Dinoprostone Dinoprostone may enhance the therapeutic effect of carbetocin. Avoid concomitant use of carbetocin with dinoprostone. The oxytocic activity of carbetocin (oxytocin analogue) may be augmented by agents used to promote cervical ripening (eg, dinoprostone, misoprostol). Dinoprostone (vaginal insert) prescribing information recommends waiting at least 30 minute following its removal before initiating treatment with oxytocic agents. A similar approach might be anticipated with misoprostol use.
Misoprostol Misoprostol may enhance the therapeutic effect of Carbetocin. Avoid the concomitant use of carbetocin and misoprostol. The oxytocic activity of carbetocin (oxytocin analogue) may be augmented by agents used to promote cervical ripening (eg, dinoprostone, misoprostol). Dinoprostone (vaginal insert) prescribing information recommends waiting at least 30 minute following its removal before initiating treatment with oxytocic agents. A similar approach might be anticipated with misoprostol use.
Food Interactions Not Available

Targets


Oxytocin receptor
Name Oxytocin receptor
Gene Name OXTR
Pharmacological action yes
Actions agonist
References
  • Engstrom T, Barth T, Melin P, Vilhardt H: Oxytocin receptor binding and uterotonic activity of carbetocin and its metabolites following enzymatic degradation. Eur J Pharmacol. 1998 Aug 21;355(2-3):203-10. - Pubmed
  • Gimpl G, Postina R, Fahrenholz F, Reinheimer T: Binding domains of the oxytocin receptor for the selective oxytocin receptor antagonist barusiban in comparison to the agonists oxytocin and carbetocin. Eur J Pharmacol. 2005 Mar 7;510(1-2):9-16. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 1.3333

Predictions


Id Partner name Gene Name Score
826 Oxytocin-neurophysin 1 OXT 0.3265
3873 Prolyl endopeptidase PREP 0.1748
6928 Prolyl endopeptidase Not Available 0.1748
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