Oxytocin Acetate


Oxytocin Acetate  is measured on mg


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Oxytocin is a hormone that helps relax and reduce blood pressure and cortisol levels. Oxytocin increases pain thresholds, has anti anxiety effects, and stimulates various types of positive social interaction. In addition, oxytocin promotes growth and healing. The nonapeptide oxytocin, originally known to stimulate labor and milk ejection, appears to play an important role stress and pain. Oxytocin can induce anti-stress-like effects such as reduction of blood pressure and cortisol levels. It increases pain thresholds, exerts an anxiolytic-like effect and stimulates various types of positive social interaction. In addition, it promotes growth and healing. Repeated exposure to oxytocin causes long-lasting effects by influencing the activity of other transmitter systems, a pattern which makes oxytocin potentially clinically relevant. Oxytocin can be released by various types of non-noxious sensory stimulation, for example by touch and warmth. Ingestion of food triggers oxytocin release by activation of vagal afferents. Most likely, oxytocin can also be released by stimulation of other senses such as olfaction, as well as by certain types of sound and light. In addition, purely psychological mechanisms may trigger the release of oxytocin. This means that positive interaction involving touch and psychological support may be health-promoting. The social interaction of daily life, as well as a positive environment, continuously activate this system. In addition, various types of psychotherapy involving transfer of support, warmth and empathy are likely to induce similar effects, which thus contribute to the positive effects of these kinds of therapies.

Methods of Manufacturing

Obtained from the posterior lobe of the pituitary of healthy hogs or cattle.
Biomedical Effects and Toxicity
[Pharmacological Action]
– Drugs that stimulate contraction of the myometrium. They are used to induce LABOR, OBSTETRIC at term, to prevent or control postpartum or postabortion hemorrhage, and to assess fetal status in high risk pregnancies. They may also be used alone or with other drugs to induce abortions (ABORTIFACIENTS). Oxytocics used clinically include the neurohypophyseal hormone OXYTOCIN and certain prostaglandins and ergot alkaloids. (From AMA Drug Evaluations, 1994, p1157)

[Therapeutic Uses]
Oxytocin is indicated for the medical rather than the elective induction of labor. Available data and information are inadequate to define the benefits-to-risks considerations in the use of the drug product for elective induction. Elective induction of labor is defined as the initiation of labor for convenience in an individual with a term pregnancy who is free of medical indications.
Oxytocin is indicated for the initiation or improvement of uterine contractions, where this is desirable and considered suitable for reasons of fetal or maternal concern, in order to achieve early vaginal delivery. It is indicated for induction of labor in patients with a medical indication for the initiation of labor, such as Rh problems, maternal diabetes, preeclampsia at or near term, when delivery is in the best interests of mother and fetus or when membranes are prematurely ruptured and delivery is indicated…
Oxytocin is indicated for stimulation or reinforcement of labor, as in selected cases of uterine inertia…
Oxytocin is indicated as adjunctive therapy in the management of incomplete or inevitable abortion. In the first trimester, curettage is generally considered primary therapy. In second trimester abortion, oxytocin infusion will often be successful in emptying the uterus. Other means of therapy, however, may be required in such cases.
Oxytocin is indicated to produce uterine contractions during the third stage of labor and to control postpartum bleeding or hemorrhage.
Oxytocin infusion has been used with success to evaluate the adequacy of fetal respiratory capabilities in high-risk pregnancies of greater than 31 weeks gestation. By inducing uterine contractions, oxytocin transiently impedes uterine blood flow. If placental reserve is low, a late deceleration in fetal heart rate may occur following oxytocin administration, indicating chronic hypoxia (positive response). If fetal heart rate is unchanged (negative response) by the oxytocin challenge, adequate placental support is probably available. The test should be repeated in 1 week to reassess fetal response. A positive response indicates that there may be fetal distress and may be an indication for termination of pregnancy, especially if a lecithin-sphingomyelin ratio of greater than 1.5 can be demonstrated.
Oxytocin infusion has been used following prostaglandin or hypertonic abortifacients to shorten the induction-to-abortion time when these abortifacients are being used to induce second trimester abortions, to induce abortion when a patient has failed to respond to the abortifacient, or to induce abortion after membranes have ruptured. Oxytocin also has been used as an adjunct in cases of incomplete abortion when the placenta fails to abort spontaneously within 1 hour after abortion of the fetus; however, some clinicians maintain that oxytocin may hinder rather than assist in expulsion of the placenta. Because concurrent use of oxytocin with abortifacients may produce uterine contractions of such intensity that uterine rupture or cervical laceration may be more likely to occur, oxytocin usually should not be administered until the oxytocic effect of the abortifacient has subsided, and patients should be carefully monitored. Oxytocin, however, is routinely used in conjunction with hypertonic urea- and dinoprostone-induced abortions.
MEDICATION (Vet): Because of the specific action of oxytocin upon the uterine musculature, it is recommended as an aid in the management of the following conditions: To precipitate labor; To accelerate normal parturition; Postpartum evacuation of uterine debris; Postoperative contraction of the uterus following a cesarean section and control of uterine hemorrhage. Oxytocin will contract the smooth muscle cells of the mammary gland to induce milk let-down if the udder is in a proper physiological state. For use in inducing rhythmic contractions of the smooth musculature of the uterus and/or milk letdown.
MEDICATION (Vet): Stimulates milk letdown, uterine contraction.
/EXPERIMENTALTHERAPY:/ This is a case report on male anorgasmia that was successfully treated with oxytocin. Oxytocin is increased during arousal and peaks during orgasm. More recently, a study on humans published in Nature has shown its value in social bonding, increasing trust, and enhancing the sense of well-being. To test the effectiveness of administering oxytocin in a case of treatment-resistant anorgasmia. The patient underwent a biopsychosocial evaluation by a psychiatrist trained in sexual medicine and sex therapy for male orgasmic disorder, acquired type. Medical conditions, effect of substances, and psychological issues were ruled out. The patient was properly consented to using oxytocin as an off-label trial. Oxytocin was administered using a nasal spray intracoitally because of its ultra-short half-life. Oxytocin was effective in restoring ejaculation. A case of treatment-resistant male anorgasmia was successfully treated with intracoital administration of intranasal oxytocin. [Ishak WW et al; J Sex Med 5 (4): 1022-4 (2008). Available from, as of February 11, 2010:]
[Biomedical Effects and Toxicity]
Oxytocin is destroyed by chymotrypsin in the GI tract. Uterine response occurs almost immediately and subsides within 1 hour following iv administration of oxytocin. Following im injection of the drug, uterine response occurs within 3-5 minutes and persists for 2-3 hours. Following intranasal application of 10-20 units of oxytocin (nasal preparations are no longer commercially available in the US), contractions of myoepithelial tissue surrounding the alveoli of the breasts begin within a few minutes and continue for 20 minutes; iv oxytocin produces the same effect with a dose of 100-200 milliunits.
Like vasopressin, oxytocin is distributed throughout the extracellular fluid. Small amounts of oxytocin probably reach the fetal circulation.
It is not known whether this drug is excreted in human milk.
Its rapid removal from plasma is accomplished largely by the kidney and the liver. Only small amounts oxytocin are excreted in the urine unchanged.
A very small portion of the oxytocin extracted by the kidney reaches the urine in active form, bound like ADH, to larger nondialyzable molecules.
Its rapid removal from plasma is accomplished largely by kidney and liver. Lactating mammary gland also inactivates significant portion of circulating hormone.
Samples of human milk obtained from lactating women in the early postpartum period were assayed for oxytocin concentrations by specific RIA, following extraction procedures with Florisil. Mean oxytocin concentrations in human milk at postpartum day 1 to 5 were 4.5 +/- 1.1, 4.7 +/- 1.1, 4.0 +/- 1.3, 3.2 +/- 0.4, 3.3 +/- 0.6 microunits/mL (+/- SE), respectively. Oxytocin levels in milk were significantly increased by nursing (3.1 +/- 0.6, 5.3 +/- 1.0 microunits/mL, respectively). 3H-oxytocin in human milk was stable even after incubation at 37 degrees C for 2 hours. The dilution curve for milk was parallel to the curve for the standard oxytocin. The chromatographic fraction of immunoreactive oxytocin was identical to that of 3H-oxytocin. 3H-oxytocin was administered to lactating rats. Radioactivity in the neonatal gastric contents and plasma were 12.8% and 4.4% of the counts in the maternal plasma. It was made clear that oxytocin is stable in milk and that oxytocin in maternal blood can be transferred to mik and then to neonates. [Takeda S et al; Endocrinol Jpn 33 (6): 821-6 (1986). Available from, as of March 24, 2010:] PubMed Abstract


Oxytocin in a nine amino acid peptide that is synthesized in hypothalamic neurons and transported down axons of the posterior pituitary for secretion into blood. Oxytocin is also secreted within the brain and from a few other tissues, including the ovaries and testes. Oxytocin differs from antidiuretic hormone in two of the nine amino acids. Both hormones are packaged into granules and secreted along with carrier proteins called neurophysins.
Oxytocin, derived from the Greek words oxus, meaning sharp, and tokos, meaning childbirth, is a peptide hormone consisting of nine amino acids (Mitchell et al, 1998, Engstrom, 2002). The amino acids are: NH2 – Gly – Leu – Pro – Cys – Asn – Gln – Ile – Tyr – Cys, with a disulfide linkage between the two Cys residues (Messer, 2000). This hormone, to date, is the most potent stimulant of uterine contractions in mammals, and is administered in the clinical setting to induce labor (Serradeil-Le Gal et al, 2004). Oxytocin is produced in the paraventricular and supraoptical nuclei of the hypothalamus, and stored in the posterior pituitary gland (Engstrom, 2002). Cervical distension within the uterus causes an action potential to travel to the hypothalamus, signaling the production and release of oxytocin (Blanks et al, 2003). During pregnancy, the quantity of oxytocin produced by the hypothalamus increases by roughly 50% (Russell et al, 1998, Blanks et al, 2003). Once in circulation, it travels through the blood to its target site. Oxytocin has a half-life of 5-15 minutes in circulation, after which it is degraded in the liver by oxytocinase (Engstrom, 2002). In addition, oxytocin is synthesized locally within the epithelium of the uterus (endometrium) (Blanks et al, 2003). Local and hypothalamic oxytocin leads to myometrial contractions, which ultimately leads to the expulsion of the young (parturition) (Russell et al, 1998, Blanks et al, 2003).


Chemical and Physical Properties


[CAS number]50-56-6

3-Isoleucine-8-leucine vasopressin
Atonin O
Intertocine S
Nobitocin S
Piton S
Synpitan forte
Synthetic oxytocin
Vasopressin, 3-L-isoleucine-8-L-leucine-
Oxytocin Acetate
Oxytocin Acetate USP30
[Molecular Formula] C43H66N12O12S2 (Products with the same molecular formula)
[Molecular Weight] 1007.19
[Canonical SMILES]


[Appearance]lyophilized powder
[Density]1.27 g/cm3
[Melting Point]192-194 °C
[Boiling Point]1533.3 °C at760mmHg
[Flash Point]881.1 °C
[Solubilities]Soluble in water, butanol
In water, 1.2X10+4 mg/L at 25 deg C (est)
[Color/Form]White powder
[Spectral properties]
[Computed Properties]
Molecular Weight:1007.18734 [g/mol]
Molecular Formula:C43H66N12O12S2
H-Bond Donor:12
H-Bond Acceptor:15
Rotatable Bond Count:17
Tautomer Count:1001
Exact Mass:1006.436457
MonoIsotopic Mass:1006.436457
Topological Polar Surface Area:450
Heavy Atom Count:69
Formal Charge:0
Isotope Atom Count:0
Defined Atom Stereocenter Count:0
Undefined Atom Stereocenter Count:9
Defined Bond Stereocenter Count:0
Undefined Bond Stereocenter Count:0
Covalently-Bonded Unit Count:1



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