Carbetocin
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| Clinical data | |
|---|---|
| Trade names | Duratocin, Pabal, Lonactene, others |
| Other names | (2-O-Methyltyrosine)deamino-1-carbaoxytocin; Deamino-2-O-methyltyrosine-1-carbaoxytocin; 1-Butanoic acid-2-(O-methy-L-tyrosine)-1-carbaoxytocin; 1-butyric acid-2-[3-(4-methoxyphenyl)-L-alanine]oxytocin |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
| Routes of administration | Intravenous, intramuscular |
| ATC code | |
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | 80% (IM) |
| Elimination half-life | 85–100 minutes[1] |
| Identifiers | |
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Carbetocin, sold under the brand names Pabal among others, is a medication used to prevent
Side effects differ little from that of no treatment or
Carbetocin was first described in 1974.[5] It was approved for medical use in Canada and the United Kingdom in 1997.[3] It is on the World Health Organization's List of Essential Medicines.[6] It is not available in the United States or Japan.[7][3]
Medical uses
Carbetocin has been approved for use immediately following an elective
Safety of carbetocin following vaginal births and emergency Cesarean sections has not been established, though studies have suggested efficacy following vaginal births to that following Cesarean sections. Some studies have shown that a 10-70 ug dose following vaginal delivery caused contractions and no adverse side effects.[10] Carbetocin has also been shown to increase uterine involution (the return of the uterus to its contracted state after the birth of the baby) in humans, horses and cows.[11][12]
Comparison with other medication
In 2018, heat-stable carbetocin, a formulation that does not require strict refrigeration, was found to be as good as oxytocin for reduction of postpartum hemorrhage after vaginal delivery.[13] It is hoped that this will make oxytocic hemorrhage control more widely available and less expensive,[13] which will be particularly useful in regions of developing countries where the cold chain (in drug transport and storage) is unreliable because of power outages or equipment problems.[14][15]
Due to carbetocin's considerably longer half-life, its effects are longer lasting than other oxytocin homologs such as oxytocin or barusiban.[16] A single carbetocin dose compared to a placebo or an eight-hour intravenous drip of oxytocin in a randomized blind study, necessitated less additional oxytocin therapy following a Cesarean section. Oxytocin receptor antagonists, such as barusiban or atosiban have the opposite effect of depressing oxytocin receptor activity and can be used to stop premature labor and uterine contractions.[16]
Adverse effects
Ten to forty percent of people will experience nausea, vomiting, abdominal pain, itching skin, increased body temperature, trembling and weakness. One to five percent of peoples may experience back and chest pain, dizziness, anemia, chills and sweating, metallic taste, tachycardia and respiratory distress.[17][18][19]
Contraindications for the use of carbetocin include inappropriate timing during labor and delivery (such as before parturition or to induce labor) or allergic reactions to carbetocin or other oxytocin homologues.
Interactions
Due to oxytocin's close sequence
Pharmacology
Mechanism of action
Carbetocin works as an
Carbetocin functions as an agonist at peripheral
During pregnancy, the synthesis of oxytocin receptors in the uterus greatly increases, reaching a peak during labor and delivery. Consequently, the administration of carbetocin or another oxytocin analog during or immediately following birth will have increased uterotonic and contractile effect. The application of carbetocin does not affect a non-pregnant uterus with lower oxytocin receptor expression.[9] Carbetocin also functions to thicken the blood, further preventing post-partum hemorrhage.[18] Carbetocin should not be used to induce or augment labor since it could cause cardiac or respiratory distress to mother or infant.[8][9]
Pharmacokinetics
Carbetocin is to be used in the hospital by prescription only. It can be administered intravenously or intramuscularly. In both cases, the recommended dose for an average adult female is 100 ug. Contractile effects of the uterus are apparent within two minutes and can be observed for approximately one hour,
Endogenous and synthetic oxytocin has a half-life of approximately 3.5 minutes.[9][22] Carbetocin, in comparison, has a much longer half-life ranging from 85 to 100 minutes.[9][22] The bioavailable dose is around 80%.[10] The elimination half-life following intravenous administration is around 40 minutes, though the elimination mechanism is not entirely known.[17] Studies have shown that elimination is only minimally renal (0.7%), but may occur at least partially through enzymatic degradation of peptides, primarily on the C-terminal end.[22] Both elimination and volume of distribution are not dose dependent.[17]
Society and culture
Legal status
Carbetocin has been approved for use under the following three brand names in 23 countries: Duratocin (Argentina, Australia, Bahrain, Canada, China, Hong Kong, Italy, Malaysia, Singapore, New Zealand), Lonactene (Mexico), and Pabal (Austria, Belgium, Switzerland, Germany, Estonia, France, UK, Hungary, Lithuania, Luxembourg, Finland). Duratocin has also been approved for veterinary use in Poland, Germany, Italy, Belgium, Luxembourg, France and the Netherlands.[18]
Brand names
Duratocin, Pabal, Lonactene, Depotocin, Comoton, and Decomoton.[citation needed]
References
- ISBN 978-2-88919-407-0.
- ^ ISBN 978-0-85711-338-2.
- ^ a b c d e f g "Proposal for Inclusion of Carbetocin in the Who List of Essential Medicines" (PDF). WHO. Retrieved 25 October 2019.
- ISBN 978-94-011-4439-1.
- ISBN 978-1-4757-2085-3.
- hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- ^ "Carbetocin Drug Information, Professional". Drugs.com. Archived from the original on 28 November 2020. Retrieved 12 November 2019.
- ^ S2CID 205616218.
- ^ S2CID 41172212.
- ^ PMID 8355953.
- PMID 15993938.
- PMID 19165935.
- ^ S2CID 205103322.
- PMID 29700898.
- ^ Mundasad S (28 June 2018). "Revamped drug could save lives of many new mothers: WHO". BBC News. Retrieved 28 June 2018.
- ^ PMID 15740719.
- ^ a b c d e f g "Product Information - Duratocin". healthlinks.net. Archived from the original on 15 November 2011. Retrieved 5 June 2012.
- ^ a b c "Carbetocin". drugs.com. Archived from the original on 3 March 2016. Retrieved 5 June 2012.
- ^ a b "Duratocin - Detailed Prescribing Information (Membership Required)". MIMS Malaysia. Archived from the original on 17 January 2014. Retrieved 5 June 2012.
- ^ "Therapeutic Areas - Reproductive Health". Ferring Pharmaceuticals. Archived from the original on 25 May 2012. Retrieved 5 June 2012.
- ^ S2CID 13265083.
- ^ PMID 9760035.
- S2CID 54559394.
