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Carbetocin,Carbétocine,Carbetocina карбетоцин,Ацетат карбетоцина,Acétate de carbétocine Acetato de carbetocina,
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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
EINECS: 253-312-6
M.F.: C45H69N11O12S
M.W.: 988.17
Appearance: White powder
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
Applications:
1.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. 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.
2.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.
3.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.
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.
1.Carbetocin is to be used in the hospital by prescription only. It can be administered intravenously or intramuscularly, resulting in different pharmacokinetic action. In both cases, the recommended dose for an average adult female is 100 ug, administered slowly over a minute. Contractile effects of the uterus are apparent within two minutes and can be observed for approximately one hour,though maximum binding occurs about 30 minutes after intramuscular injection. Administration is performed immediately following parturition to minimize risk of postpartum hemorrhage by inducing uterine contractions, increasing muscle tone and thickening the blood. Administration can be performed only once; further administration would prove risky. If further uterine stimulation is needed, treatment with other forms of oxytocic uterotonic drugs should be used.
2.Endogenous and synthetic oxytocin has a half-life of approximately 3.5 minutes.Carbetocin, in comparison, has a much longer half-life ranging from 85-100 minutes.The bioavailable dose is around 80%. The elimination half-life following intravenous administration is around 40 minutes, though the elimination mechanism is not entirely known. 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.Both elimination and volume of distribution are not dose dependent.
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