Carbetocin Acetate

Sequence: Butyryl-Tyr(Me)-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2 (Sulfide bond between Butyryl-4-yl and Cys)
CAS: 37025-55-1
Appearance: White powder
EINECS: 253-312-6
M.F.: C45H69N11O12S
M.W.: 988.17
Specific Optical Rotation D(c=1,1%HAc): -38.0~-42.0°
Water Content(Karl Fischer): ≤5.0%
Acetate Content(by HPLC): ≤12.0%
Amino Acid Composition: ±10% of theoretical
Purity (by HPLC): ≥98.0%
Single Impurity(by HPLC): ≤1.0%
Peptide Content(by N%): ≥80%
Assay(By Anhydrous, Acetic Acid-free ): 97.0~103.0%
Bacterial Endotoxins: ≤5EU/mg
Usage:An obstetric drug used to control postpartum hemorrhaging.

Description :
Carbetocin (INN, BAN) (brand names Duratocin, Pabal, Lonactene, Depotocin, Comoton, Decomoton), or 1-butanoic acid-2-(O-methy-L-tyrosine)-1-carbaoxytocin, is an oxytocic used in obstetrics to control postpartum hemorrhage and bleeding after giving birth, particularly following Cesarean section. It is an eight amino acid long analogue of oxytocin (a nonapeptide )and, in accordance, has a similar action. Carbetocin primarily agonizes peripherally expressed oxytocin receptors.

The most common causes of postpartum hemorrhage are lack of tone in the uterus from overstretching or the use of an anesthetic. Carbetocin has been approved for use immediately following an elective Cesarean section when a local or spinal anesthesia has been administered.Since the uterus cannot contract on its own following incision during a Cesarean section, exogenous administration of oxytocin or an analog is necessary to restore uterine tone and prevent hemorrhage. 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.

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. Carbetocin has also been shown to stimulate milk letdown through its action on the oxytocin receptors on the myoepithelial cells and there was not a significant amount of carbetocin in breastmilk.

Pharmacokinetics Carbetocin is to be used in the hospital by prescription only. It can be administered intravenously or intramuscularly, resulting in different pharmacokinetic action.

Medicine Use :
Carbetocin works as an oxytocic, antihemorrhagic and uterotonic drug in the peripheral nervous system. The most common causes of postpartum hemorrhage are lack of tone in the uterus from overstretching or the use of an anesthetic.
Carbetocin has been approved for use immediately following an elective Cesarean section when a local or spinal anesthesia has been administered.[8] Since the uterus cannot contract on its own following incision during a Cesarean section, exogenous administration of oxytocin or an analog is necessary to restore uterine tone and prevent hemorrhage.
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.

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. Carbetocin has also been shown to stimulate milk letdown through its action on the oxytocin receptors on the myoepithelial cells and there was not a significant amount of carbetocin in breastmilk.[10]
Each dose of Duratocin contains 100 micrograms of carbetocin, 9 mg sodium chloride and ascetic acid. pH is 3.8 and peptide content is greater than 85 percent.
 

Application:

Carbetocin is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth, particularly following Cesarean section.It is an eight amino long oxytocin analogue (oxytocin is a nonapeptide) and its action is similar to that of oxytocin. Carbetocin primarily agonizes peripherally expressed oxytocin receptors.

Carbetocin is for selective epidural or spinal anesthesia after caesarean section to prevent uterine contraction fatigue and postpartum hemorrhage.

Carbetocin Acetate or 1-butanoic acid-2-(O-methy-L-tyrosine)-1-carbaoxytocin, is an oxytocic used in obstetrics to control postpartum hemorrhage and bleeding after giving birth, particularly following Cesarean section.

Carbetocin Acetate Function:

Carbetocin is an oxytocic used in obstetrics to control postpartum hemorrhage and bleeding after giving birth, particularly following Cesarean section. It is an eight amino acid long analogue of oxytocin (a nonapeptide) and, in accordance, has a similar action. Carbetocin primarily agonizes peripherally expressed oxytocin receptors.

Specifications:

Single Impurity (HPLC): 0.5%max
Amino Acid Composition: ± 10% of theoretical
Peptide Content (N%): ≥ 80.0%
Water Content (Karl Fischer): ≤ 8.0%
Acetate Content (HPIC): ≤ 10.0%
Specific Rotation (20/D): -55.0~-65.0° (c=11%HAc)
MS (ESI): Consistent
Mass Balance: 95.0~105.0%