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25 API Suppliers, 14 USDMF, 6 CEP/COS, 2 JDMF, 1 EU WC, 19 NDC API, 5 VMF, 13 Listed Suppliers

25 API Suppliers
14 USDMF
6 CEP/COS
2 JDMF
1 EU WC
19 NDC API
5 VMF
13 Listed Suppliers

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29 Drugs in Development

29 Drugs in Development

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72 FDF Dossiers, 19 FDA Orange Book, 18 Europe, 4 Canada, 6 South Africa, 25 Listed Dossiers

72 FDF Dossiers
19 FDA Orange Book
18 Europe
4 Canada
6 South Africa
25 Listed Dossiers

DRUG PRODUCT COMPOSITIONS

INJECTABLE;INJECTION - 100USP UNITS/10ML (10USP UNITS/ML), INJECTABLE;INJECTION - 10USP UNITS/ML (10USP UNITS/ML), INJECTABLE;INJECTION - 300USP UNITS/30ML (10USP UNITS/ML), INJECTABLE;INJECTION - 100USP UNITS/10ML (10USP UNITS/ML), INJECTABLE;INJECTION - 10USP UNITS/ML (10USP UNITS/ML), INJECTABLE;INJECTION - 500USP UNITS/50ML (10USP UNITS/ML)

drugProductComposition
INJECTABLE;INJECTION - 100USP UNITS/10ML (10USP UNITS/ML)
INJECTABLE;INJECTION - 10USP UNITS/ML (10USP UNITS/ML)
INJECTABLE;INJECTION - 300USP UNITS/30ML (10USP UNITS/ML)
INJECTABLE;INJECTION - 100USP UNITS/10ML (10USP UNITS/ML)
INJECTABLE;INJECTION - 10USP UNITS/ML (10USP UNITS/ML)
INJECTABLE;INJECTION - 500USP UNITS/50ML (10USP UNITS/ML)

RELATED EXCIPIENT COMPANIES

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1 Faran Shimi Pharmaceutical
2 Nanjing Well Pharmaceutical
3 Actylis
2 BASF
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2 Pluviaendo
5 Roquette
2 Seppic
1 Valens Pharmachem

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12 Parenteral
6 Solubilizers
5 Topical
5 Fillers, Diluents & Binders
2 Surfactant & Foaming Agents
2 Emulsifying Agents
2 Thickeners and Stabilizers
2 Film Formers & Plasticizers
1 Controlled & Modified Release
1 Co-Processed Excipients
1 Taste Masking

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14 APIs, 13 FDF Dossiers

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2 EDQM , 2 USP , 3 JP , 7 Others

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2 USP
3 JP
7 Others

Aspen Oxytocin

Synopsis

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USDMF

CEP/COS

JDMF

EU WC

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NDC API

VMF

Listed Suppliers

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$ 105,736

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FDF Dossiers

FDA Orange Book

Europe

Canada

Australia

South Africa

Listed Dossiers

29DRUGS IN DEVELOPMENT

DRUG PRODUCT COMPOSITIONS

REF. STANDARDS OR IMPURITIES

EDQM

USP

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Chemistry

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Also known as: 50-56-6, Pitocin, Endopituitrina, Ocytocin, Syntocinon, Orasthin

Molecular Formula

C₄₃H₆₆N₁₂O₁₂S₂

Molecular Weight

1007.2 g/mol

InChI Key

XNOPRXBHLZRZKH-DSZYJQQASA-N

A nonapeptide hormone released from the neurohypophysis (PITUITARY GLAND, POSTERIOR). It differs from VASOPRESSIN by two amino acids at residues 3 and 8. Oxytocin acts on SMOOTH MUSCLE CELLS, such as causing UTERINE CONTRACTIONS and MILK EJECTION.

1 2D Structure

Oxytocin

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide

2.1.2 InChI

InChI=1S/C43H66N12O12S2/c1-5-22(4)35-42(66)49-26(12-13-32(45)57)38(62)51-29(17-33(46)58)39(63)53-30(20-69-68-19-25(44)36(60)50-28(40(64)54-35)16-23-8-10-24(56)11-9-23)43(67)55-14-6-7-31(55)41(65)52-27(15-21(2)3)37(61)48-18-34(47)59/h8-11,21-22,25-31,35,56H,5-7,12-20,44H2,1-4H3,(H2,45,57)(H2,46,58)(H2,47,59)(H,48,61)(H,49,66)(H,50,60)(H,51,62)(H,52,65)(H,53,63)(H,54,64)/t22-,25-,26-,27-,28-,29-,30-,31-,35-/m0/s1

2.1.3 InChI Key

XNOPRXBHLZRZKH-DSZYJQQASA-N

2.1.4 Canonical SMILES

CCC(C)C1C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)N1)CC2=CC=C(C=C2)O)N)C(=O)N3CCCC3C(=O)NC(CC(C)C)C(=O)NCC(=O)N)CC(=O)N)CCC(=O)N

2.1.5 Isomeric SMILES

CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N1)CC2=CC=C(C=C2)O)N)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N)CC(=O)N)CCC(=O)N

2.2 Synonyms

2.2.1 MeSH Synonyms

1. Ocytocin

2. Pitocin

3. Syntocinon

2.2.2 Depositor-Supplied Synonyms

1. 50-56-6

2. Pitocin

3. Endopituitrina

4. Ocytocin

5. Syntocinon

6. Orasthin

7. Oxytocinum

8. Oxitocina

9. Oxytocine

10. (1-hemicystine)oxytocin

11. Piton S

12. Alpha-hypophamine

13. 3-isoleucine-8-leucine Vasopressin

14. Oxytocic Hormone

15. Chebi:7872

16. Chembl395429

17. (2s)-1-[(4r,7s,10s,13s,16s,19r)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2s)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-n-[(2s)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide

18. Oxystin

19. Partocon

20. Synthetic Oxytocin

21. Oxt

22. Ocytocinum

23. Ossitocina

24. Syntocinone

25. Oxetakain

26. Oxoject

27. Oxtocin

28. Presoxin

29. Synpitan

30. Syntocin

31. Utedrin

32. Uteracon

33. Di-sipidin

34. Nobitocin S

35. Atonin O

36. Oxytocin (syntocinon)

37. [3h]oxytocin

38. Oxetakain [czech]

39. 1-({(4r,7s,10s,13s,16s,19r)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-16-(4-hydroxybenzyl)-13-[(1s)-1-methylpropyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosan-4-yl}carbonyl)-l-prolyl-l-leucylglycinamide

40. L-cysteinyl-l-tyrosyl-l-isoleucyl-l-glutaminyl-l-asparaginyl-l-cysteinyl-l-prolyl-l-leucylglycinamide Cyclic(1-6)-disulfide

41. Ossitocina [dcit]

42. Oxytocin 5 Usp Units In Dextrose 5%

43. Oxytocin 10 Usp Units In Dextrose 5%

44. Oxytocin 20 Usp Units In Dextrose 5%

45. Oxytocine [inn-french]

46. Oxytocinum [inn-latin]

47. Oxitocina [inn-spanish]

48. Posterior Pituitary Extract

49. Unii-1jqs135eyn

50. A-hypophamine

51. Intertocine S

52. [3h]ot (human, Mouse, Rat)

53. Hsdb 2182

54. Oxytocin [usp:inn:ban:jan]

55. Syntocinon (tn)

56. Oxytocin (tn)

57. Oxytocin,(s)

58. (2s)-1-[(4r,7s,10s,13s,16s,19r)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2s)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-n-[(2s)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide

59. Einecs 200-048-4

60. Pitocin (tn)

61. Mfcd00076731

62. Brn 3586108

63. Vasopressin, 3-l-isoleucine-8-l-leucine-

64. 1jqs135eyn

65. Schembl29048

66. Oxytocin (jp17/usp/inn)

67. Gtpl2174

68. Gtpl2176

69. Dtxsid8048361

70. Bcbcmap01_000094

71. Tnx1900

72. Tta-121

73. Amy25364

74. Cys-tyr-ile-gln-asn-cys-pro-leu-gly-nh2, Cyclic 1-6 Disulfide

75. Tnx-1900

76. Bdbm50205990

77. Ti-001

78. Akos015994657

79. Hs-2021

80. Ncgc00167132-01

81. Ac-28730

82. L-cysteinyl-l-tyrosyl-l-isoleucyl-l-glutaminyl-l-asparaginyl-l-cysteinyl-l-prolyl-l-leucylglycinamide Cyclic (1-6)-disulfide

83. C00746

84. D00089

85. 076o731

86. A828179

87. Q169960

88. Sr-01000945111

89. Sr-01000945111-1

90. W-105951

91. Oxytocin, European Pharmacopoeia (ep) Reference Standard

92. Oxytocin, United States Pharmacopeia (usp) Reference Standard

93. Oxytocin-(leucine-5,5,5-d3, Glycine-2,2-d2) Trifluoroacetate Salt

94. Oxytocin, Lyophilized Powder, ~15 Iu/mg Solid (prepared From Synthetic Oxytocin)

95. 1-[19-amino-7-(2-amino-2-oxo-ethyl)-10-(3-amino-3-oxo-propyl)-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-13-sec-butyl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-n-[1-[(2-amino-1-methyl-2-oxo-ethyl)carbamoyl]-3-methyl-butyl]pyrrolidine

96. L-cysteinyl-l-tyrosyl-l-isoleucyl-l-glutaminyl-l-asparaginyl-l-cysteinyl-l-prolyl-l-leucylglycinamide Cyclic (1-->6)-disulfide

97. Otx

2.3 Create Date

2005-06-24

3 Chemical and Physical Properties

Molecular Formula	C₄₃H₆₆N₁₂O₁₂S₂
Molecular Weight	1007.2 g/mol
XLogP3	-2.6
Hydrogen Bond Donor Count	12
Hydrogen Bond Acceptor Count	15
Rotatable Bond Count	17
Exact Mass	1006.43645793 g/mol
Monoisotopic Mass	1006.43645793 g/mol
Topological Polar Surface Area	450 Å²
Heavy Atom Count	69
Formal Charge	0
Complexity	1870
Isotope Atom Count	0
Defined Atom Stereocenter Count	9
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Information

1 of 4
Drug Name	Oxytocin
PubMed Health	Oxytocin
Drug Classes	Diagnostic Agent, Fetal Heart Rate Distress, Endocrine-Metabolic Agent, Uterine Stimulant
Drug Label	Pitocin (oxytocin injection, USP) is a sterile, clear, colorless aqueous solution of synthetic oxytocin, for intravenous infusion or intramuscular injection. Pitocin is a nonapeptide found in pituitary extracts from mammals. It is standardized to con...
Active Ingredient	Oxytocin
Dosage Form	Injectable
Route	Injection
Strength	300usp units/30ml (10usp units/ml); 10usp units/ml (10usp units/ml); 100usp units/10ml (10usp units/ml)
Market Status	Prescription
Company	Hikma Farmaceutica; Fresenius Kabi Usa; Hikma Maple

2 of 4
Drug Name	Pitocin
PubMed Health	Oxytocin
Drug Classes	Diagnostic Agent, Fetal Heart Rate Distress, Endocrine-Metabolic Agent, Uterine Stimulant
Drug Label	Pitocin (oxytocin injection, USP) is a sterile, clear, colorless aqueous solution of synthetic oxytocin, for intravenous infusion or intramuscular injection. Pitocin is a nonapeptide found in pituitary extracts from mammals. It is standardized to con...
Active Ingredient	Oxytocin
Dosage Form	Injectable
Route	Injection
Strength	10usp units/ml (10usp units/ml); 100usp units/10ml (10usp units/ml); 500usp units/50ml (10usp units/ml)
Market Status	Prescription
Company	Par Sterile Products

3 of 4
Drug Name	Oxytocin
PubMed Health	Oxytocin
Drug Classes	Diagnostic Agent, Fetal Heart Rate Distress, Endocrine-Metabolic Agent, Uterine Stimulant
Drug Label	Pitocin (oxytocin injection, USP) is a sterile, clear, colorless aqueous solution of synthetic oxytocin, for intravenous infusion or intramuscular injection. Pitocin is a nonapeptide found in pituitary extracts from mammals. It is standardized to con...
Active Ingredient	Oxytocin
Dosage Form	Injectable
Route	Injection
Strength	300usp units/30ml (10usp units/ml); 10usp units/ml (10usp units/ml); 100usp units/10ml (10usp units/ml)
Market Status	Prescription
Company	Hikma Farmaceutica; Fresenius Kabi Usa; Hikma Maple

4 of 4
Drug Name	Pitocin
PubMed Health	Oxytocin
Drug Classes	Diagnostic Agent, Fetal Heart Rate Distress, Endocrine-Metabolic Agent, Uterine Stimulant
Drug Label	Pitocin (oxytocin injection, USP) is a sterile, clear, colorless aqueous solution of synthetic oxytocin, for intravenous infusion or intramuscular injection. Pitocin is a nonapeptide found in pituitary extracts from mammals. It is standardized to con...
Active Ingredient	Oxytocin
Dosage Form	Injectable
Route	Injection
Strength	10usp units/ml (10usp units/ml); 100usp units/10ml (10usp units/ml); 500usp units/50ml (10usp units/ml)
Market Status	Prescription
Company	Par Sterile Products

4.2 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. /Included in US product label/

US Natl Inst Health; DailyMed. Current Medication Information for Oxytocin injection (June 2009). Available from, as of February 10, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=10243

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... /Included in US product label/

US Natl Inst Health; DailyMed. Current Medication Information for Oxytocin injection (June 2009). Available from, as of February 10, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=10243

Oxytocin is indicated for stimulation or reinforcement of labor, as in selected cases of uterine inertia... /Included in US product label/

US Natl Inst Health; DailyMed. Current Medication Information for Oxytocin injection (June 2009). Available from, as of February 10, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=10243

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. /Included in US product label/

US Natl Inst Health; DailyMed. Current Medication Information for Oxytocin injection (June 2009). Available from, as of February 10, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=10243

For more Therapeutic Uses (Complete) data for Oxytocin (11 total), please visit the HSDB record page.

4.3 Drug Warning

When oxytocin is administered in excessive dosage, with abortifacients or to sensitive patients, hyperstimulation of the uterus, with strong (hypertonic) and/or prolonged (tetanic) contractions, or a resting uterine tone of 15-20 mm H2O between contractions may occur, possibly resulting in uterine rupture, cervical and vaginal lacerations, postpartum hemorrhage, abruptio placentae, impaired uterine blood flow, amniotic fluid embolism, and fetal trauma including intracranial hemorrhage.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3348

Increased uterine motility may cause adverse fetal effects, including sinus bradycardia, tachycardia, premature ventricular complexes and other arrhythmias, permanent CNS or brain damage, and death secondary to asphyxia. Excessive maternal dosage or administration of the drug to sensitive women also can cause uteroplacental hypoperfusion and variable deceleration of fetal heart rate, fetal hypoxia, perinatal hepatic necrosis, and fetal hypercapnia. Rare incidents of pelvic hematoma have been reported, but these were probably also related to the high incidence of operative vaginal deliveries in primiparas, the fragility of engorged pelvic veins (especially if varicosed), and faulty episiotomy repair.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3348

When large amounts of oxytocin are administered, severe decreases in maternal systolic and diastolic blood pressure, increases in heart rate, systemic venous return and cardiac output, and arrhythmia may occur; these effects may be particularly hazardous to patients with valvular heart disease and those receiving spinal and epidural anesthesia.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3348

Postpartum bleeding may be increased by administration of oxytocin; this effect may be related to reports of oxytocin-induced thrombocytopenia, afibrinogenemia, and hypoprothrombinemia. By carefully controlling delivery, the incidence of postpartum bleeding may be minimized.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3348

For more Drug Warnings (Complete) data for Oxytocin (22 total), please visit the HSDB record page.

4.4 Drug Indication

Administration of exogenous oxytocin is indicated in the antepartum period to initiate or improve uterine contractions for vaginal delivery in situations where there is fetal or maternal concern. For example, It may be used to induce labor in cases of Rh sensitization, maternal diabetes, preeclampsia at or near term, and when delivery is indicated due to prematurely ruptured membranes. Importantly, oxytocin is not approved or indicated for elective induction of labor. Oxytocin may be used to reinforce labor in select cases of uterine inertia and as adjunctive therapy in the management of incomplete or inevitable abortion. In the postpartum period, oxytocin may be used to induced contractions in the 3rd stage of labor and to control postpartum bleeding or hemorrhage.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Oxytocin is a nonapeptide, pleiotropic hormone that exerts important physiological effects. It is most well known to stimulate parturition and lactation, but also has important physiological influences on metabolic and cardiovascular functions, sexual and maternal behaviour, pair bonding, social cognition, and fear conditioning. It is worth noting that oxytocin receptors are not limited to the reproductive system but can be found in many peripheral tissues and in central nervous system structures including the brain stem and amygdala.

5.2 MeSH Pharmacological Classification

Oxytocics

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) (See all compounds classified as Oxytocics.)

5.3 FDA Pharmacological Classification

5.3.1 Pharmacological Classes

Oxytocic [EPC]; Oxytocin [CS]; Increased Uterine Smooth Muscle Contraction or Tone [PE]

5.4 ATC Code

H - Systemic hormonal preparations, excl. sex hormones and insulins

H01 - Pituitary and hypothalamic hormones and analogues

H01B - Posterior pituitary lobe hormones

H01BB - Oxytocin and analogues

H01BB02 - Oxytocin

5.5 Absorption, Distribution and Excretion

Absorption

Oxytocin is administered parenterally and is fully bioavailable. It takes approximately 40 minutes for oxytocin to reach steady-state concentrations in the plasma after parenteral administration.

Route of Elimination

The enzyme oxytocinase is largely responsible for the metabolism and regulation of oxytocin levels in pregnancy; only a small percentage of the neurohormone is excreted in the urine unchanged.

Clearance

In a study that observed 10 women who were given oxytocin to induce labor, the mean metabolic clearance rate was 7.87 mL/min.

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.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3349

Like vasopressin, oxytocin is distributed throughout the extracellular fluid. Small amounts of oxytocin probably reach the fetal circulation.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3349

It is not known whether this drug is excreted in human milk.

US Natl Inst Health; DailyMed. Current Medication Information for Oxytocin injection (June 2009). Available from, as of February 10, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=10243

Its rapid removal from plasma is accomplished largely by the kidney and the liver. Only small amounts oxytocin are excreted in the urine unchanged.

US Natl Inst Health; DailyMed. Current Medication Information for Oxytocin injection (June 2009). Available from, as of February 10, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=10243

For more Absorption, Distribution and Excretion (Complete) data for Oxytocin (7 total), please visit the HSDB record page.

5.6 Metabolism/Metabolites

Oxytocin is rapidly removed from the plasma by the liver and kidney. The enzyme oxytocinase is largely responsible for the metabolism and regulation of oxytocin levels in pregnancy and only a small percentage of the neurohormone is excreted in the urine unchanged. Oxytocinase activity increases throughout pregnancy and peaks in the plasma, placenta and uterus near term. The placenta is a key source of oxytocinase during gestation and produces increasing amounts of the enzyme in response to increasing levels of oxytocin produced by the mother. Oxytocinase activity is also expressed in mammary glands, heart, kidney, and the small intestine. Lower levels of activity can be found in the brain, spleen, liver, skeletal muscle, testes, and colon. The level of oxytocin degradation is negligible in non-pregnant women, men, and cord blood.

Oxytocinase, a circulating enzyme produced early in pregnancy, is also capable of inactivating the polypeptide.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3349

During pregnancy ... "oxytocinase" ... is capable of inactivating oxytocin by cleavage of the 1-cysteine to 2-tyrosine peptide bond.

Gilman, A. G., L. S. Goodman, and A. Gilman. (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 6th ed. New York: Macmillan Publishing Co., Inc. 1980., p. 938

5.7 Biological Half-Life

The plasma half-life of oxytocin ranges from 1-6 minutes. The half-life is decreased in late pregnancy and during lactation.

Oxytocin has a plasma half-life of about 3 to 5 minutes.

US Natl Inst Health; DailyMed. Current Medication Information for Oxytocin injection (June 2009). Available from, as of February 10, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=10243

5.8 Mechanism of Action

Oxytocin plays a vital role in labour and delivery. The hormone is produced in the hypothalamus and is secreted from the paraventricular nucleus to the posterior pituitary where it is stored. It is then released in pulses during childbirth to induce uterine contractions. The concentration of oxytocin receptors on the myometrium increases significantly during pregnancy and reaches a peak in early labor. Activation of oxytocin receptors on the myometrium triggers a downstream cascade that leads to increased intracellular calcium in uterine myofibrils which strengthens and increases the frequency of uterine contractions. In humans, most hormones are regulated by negative feedback; however, oxytocin is one of the few that is regulated by positive feedback. The head of the fetus pushing on the cervix signals the release of oxytocin from the posterior pituitary of the mother. Oxytocin then travels to the uterus where it stimulates uterine contractions. The elicited uterine contractions will then stimulate the release of increasing amounts of oxytocin. This positive feedback loop will continue until parturition. Since exogenously administered and endogenously secreted oxytocin result in the same effects on the female reproductive system, synthetic oxytocin may be used in specific instances during the antepartum and postpartum period to induce or improve uterine contractions.

The pharmacologic and clinical properties of oxytocin are identical with those of naturally occurring oxytocin principle of the posterior lobe of pituitary. Oxytocin exerts a selective action on the smooth musculature of the uterus, particularly toward the end of pregnancy, during labor, and immediately following delivery. Oxytocin stimulates rhythmic contractions of the uterus, increases the frequency of existing contractions, and raises the tone of the uterine musculature.

US Natl Inst Health; DailyMed. Current Medication Information for Oxytocin injection (June 2009). Available from, as of February 10, 2010: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=10243

Oxytocin indirectly stimulates contraction of uterine smooth muscle by increasing the sodium permeability of uterine myofibrils. High estrogen concentrations lower the threshold for uterine response to oxytocin. Uterine response to oxytocin increases with the duration of pregnancy and is greater in patients who are in labor than those not in labor; only very large doses elicit contractions in early pregnancy. Contractions produced in the term uterus by oxytocin are similar to those occurring during spontaneous labor. In the term uterus, oxytocin increases the amplitude and frequency of uterine contractions which in turn tend to decrease cervical activity producing dilation and effacement of the cervix and to transiently impede uterine blood flow.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3348

Oxytocin contracts myoepithelial cells surrounding the alveoli of the breasts, forcing milk from the alveoli into the larger ducts and thus facilitating milk ejection. The drug possesses no galactopoietic properties.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3348

Oxytocin produces vasodilation of vascular smooth muscle, increasing renal, coronary, and cerebral blood flow. Blood pressure is usually unchanged, but following iv administration of very large doses or undiluted solutions, blood pressure may decrease transiently, and tachycardia and an increase in cardiac output may be reflexly induced. Any initial fall in blood pressure is usually followed by a small but sustained increase in blood pressure. In contrast to vasopressin, oxytocin has minimal antidiuretic effects; however, water intoxication may occur when oxytocin is administered with an excessive volume of electrolyte-free iv fluids and/or at too rapid a rate.

American Society of Health System Pharmacists; AHFS Drug Information 2009. Bethesda, MD. (2009), p. 3349

For more Mechanism of Action (Complete) data for Oxytocin (15 total), please visit the HSDB record page.

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