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Description
Curator's Comment:: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/24141993 http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/018261s031lbl.pdf

More than a century ago, Sir Henry Dale demonstrated that a component of the pituitary causes contractions of the mammalian uterus, hence his coining the term “oxytocic,” derived from the Greek for “quick birth,” for its activity. The discovery that a component of the pituitary causes milk secretion followed within a few years. By 1930, oxytocin was separated from vasopressin into pitocin and pitressin, respectively, at Parke Davis and made available for research. That a single peptide was responsible for these uterine and mammary actions was definitively confirmed upon the sequencing and synthesis of the peptide, 9 amino acids in length. Vincent du Vigneaud was awarded a Nobel Prize for this work. 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 vaginal delivery. Oxytocin is indicated to produce uterine contractions during the third stage of labor and to control postpartum bleeding or hemorrhage. Uterine motility depends on the formation of the contractile protein actomyosin under the influence of the Ca2+- dependent phosphorylating enzyme myosin light-chain kinase. Oxytocin promotes contractions by increasing the intracellular Ca2+. Oxytocin has specific receptors in the myometrium and the receptor concentration increases greatly during pregnancy, reaching a maximum in early labor at term. The Oxytocin receptor is a typical class I G protein-coupled receptor that is primarily coupled via G(q) proteins to phospholipase C-beta. The high-affinity receptor state requires both Mg(2+) and cholesterol, which probably function as allosteric modulators. The agonist-binding region of the receptor has been characterized by mutagenesis and molecular modeling and is different from the antagonist binding site. The function and physiological regulation of the Oxytocin system is strongly steroid dependent.

Originator

Curator's Comment:: references retrieved from | https://www.ncbi.nlm.nih.gov/pubmed/24141993

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.76 nM [Kd]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
PITOCIN

Approved Use

Pitocin® (Oxytocin Injection, USP) Synthetic is indicated Antepartum and Postpartum. Antepartum: Pitocin 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 vaginal delivery. It is indicated for (1) 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; (2) stimulation or reinforcement of labor, as in selected cases of uterine inertia; (3) 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. Postpartum: Pitocin is indicated to produce uterine contractions during the third stage of labor and to control postpartum bleeding or hemorrhage.

Launch Date

3.78604814E11
Primary
PITOCIN

Approved Use

Pitocin® (Oxytocin Injection, USP) Synthetic is indicated Antepartum and Postpartum. Antepartum: Pitocin 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 vaginal delivery. It is indicated for (1) 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; (2) stimulation or reinforcement of labor, as in selected cases of uterine inertia; (3) 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. Postpartum: Pitocin is indicated to produce uterine contractions during the third stage of labor and to control postpartum bleeding or hemorrhage.

Launch Date

3.78604814E11
PubMed

PubMed

TitleDatePubMed
Oxytocin attenuates the cocaine-induced exploratory hyperactivity in mice.
1990 Nov-Dec
Effect of excitatory amino acid receptor antagonists on apomorphine-, oxytocin- and ACTH-induced penile erection and yawning in male rats.
1992 Sep 10
Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women.
1999 Oct
EP 91073 prevents EP 80661-induced penile erection: new evidence for the existence of specific EP peptide receptors mediating penile erection.
2001 Aug
[Which tocolytics should be used in 2001?].
2001 Feb
[Ogilvie syndrome after Cesarean section].
2001 May 28
A randomised trial of oral versus vaginal administration of misoprostol for the purpose of mid-trimester termination of pregnancy.
2001 Nov
[Missed diagnosis of postpartum hemorrhage].
2001 Oct
Catecholamines are not linked to myometrial phospholipase C and uterine contraction in late pregnant and parturient mouse.
2001 Oct 1
Osteogenesis imperfecta in pregnancy: two case reports and review of literature.
2001 Sep
A randomised controlled trial of intramuscular syntometrine and intravenous oxytocin in the management of the third stage of labour.
2002 Feb
Accidental administration of oxytocin to a premature infant.
2002 Feb
Risk factors at caesarean section and failure of subsequent trial of labour.
2002 Jan 10
Induction of labor with prostaglandin E2 vaginal tablets in parous and grandmultiparous patients with previous cesarean section.
2002 Jul
Myocardial ischaemia complicating an elective Caesarean section.
2003 Aug
Syntocinon and 'epidurals' in labour--which comes first?
2003 Dec
[Clozapine and pregnancy].
2003 Mar-Apr
A randomised controlled trial of admission electronic fetal monitoring in normal labour.
2003 Sep
Intrapartum pain management at the Royal Hospital for Women.
2004 Aug
[Comparison of the uterine reflex activity during artificial insemination and mating in the ewe].
2004 Dec
[Anesthesiologists at the initial stage of postpartum hemorrhage].
2004 Dec
The impact of delivery suite guidelines on intrapartum care in 'standard primigravida'.
2004 Jul 15
[Recombinant activated factor VII as a life-saving therapy for severe postpartum haemorrhage unresponsive to conservative traditional management].
2004 Nov
Labor induction with dinoprostone or oxytocine and postpartum disseminated intravascular coagulation: a hospital-based case-control study.
2004 Nov
CA: Nurse errs in giving pitocin to stop labor: father's suit for emotional distress fails.
2004 Oct
QT interval prolongation after oxytocin bolus during surgical induced abortion.
2004 Oct
Induction of labour for women with a previous Caesarean birth: a systematic review of the literature.
2004 Oct
[Pharmacodynamical study on Danqi capsule].
2005 Dec
[Is it already time to legalize the usage of Cytotec (Misoprostol) in the obstetrics' practice?].
2007
Avoiding manual removal of placenta: evaluation of intra-umbilical injection of uterotonics using the Pipingas technique for management of adherent placenta.
2007
Predicting a failed induction.
2007 Oct
Post partum haemorrhage secondary to uterine atony, complicated by platelet storage pool disease and partial placenta diffusa: a case report.
2008 Dec 13
The views of obstetricians in the south-west of England on the use of prostaglandins and syntocinon in VBAC.
2008 Feb
The hemodynamics of oxytocin and other vasoactive agents during neuraxial anesthesia for cesarean delivery: findings in six cases.
2008 Jul
[Clinical and experimental study on effect of cuichan zhusheng decoction on the structure and tension of pregnant cervix uteri].
2008 Jun
Prenatal organochlorine exposure and measures of behavior in infancy using the Neonatal Behavioral Assessment Scale (NBAS).
2008 May
Signs of myocardial ischaemia after injection of oxytocin: a randomized double-blind comparison of oxytocin and methylergometrine during Caesarean section.
2008 May
Intraumbilical veinous injection oxytocin in the active management of third stage of labour.
2008 Sep
A randomized controlled trial of misoprostol and sulprostone to end pregnancy after fetal death.
2009
[Frequency of uterine rupture at delivery and accompanying risks for the mother and the newborn].
2009 Aug
Study protocol. ECSSIT - Elective Caesarean Section Syntocinon Infusion Trial. A multi-centre randomised controlled trial of oxytocin (Syntocinon) 5 IU bolus and placebo infusion versus oxytocin 5 IU bolus and 40 IU infusion for the control of blood loss at elective caesarean section.
2009 Aug 24
The effect of ovarian steroids on oxytocin-stimulated secretion and synthesis of prostaglandins in bovine myometrial cells.
2009 Dec
Using snowball sampling method with nurses to understand medication administration errors.
2009 Feb
A randomised controlled trial comparing the efficacy of intramuscular syntometrine and intravenous syntocinon, in preventing postpartum haemorrhage.
2009 Jul
Anaesthesiological considerations on tocolytic and uterotonic therapy in obstetrics.
2009 Jul
[Effectiveness of non-pharmacological strategies in relieving labor pain].
2009 Jun
Trends in postpartum hemorrhage in high resource countries: a review and recommendations from the International Postpartum Hemorrhage Collaborative Group.
2009 Nov 27
Involvement of the transcription factor STAT1 in the regulation of porcine ovarian granulosa cell functions treated and not treated with ghrelin.
2009 Sep
The role of cervical Electrical Impedance Spectroscopy in the prediction of the course and outcome of induced labour.
2009 Sep 2
Patents

Sample Use Guides

The dosage of (Oxytocin Injection, USP) Synthetic is determined by the uterine response and must therefore be individualized and initiated at a very low level. The following dosage information is based upon various regimens and indications in general use. A. Induction or Stimulation of Labor Intravenous infusion (drip method) is the only acceptable method of parenteral administration of Pitocin for the induction or stimulation of labor. Accurate control of the rate of infusion is essential and is best accomplished by an infusion pump. It is convenient to piggyback the Pitocin infusion on a physiologic electrolyte solution, permitting the Pitocin infusion to be stopped abruptly without interrupting the electrolyte infusion. This is done in the following way. 1. Preparation a. The standard solution for infusion of Pitocin is prepared by adding the contents of one 1-mL vial containing 10 units of oxytocin to 1000 mL of 0.9% aqueous sodium chloride or Ringer's lactate. The combined solution containing 10 milliunits (mU) of oxytocin/mL is rotated in the infusion bottle for thorough mixing. b. Establish the infusion with a separate bottle of physiologic electrolyte solution not containing Pitocin. c. Attach (piggyback) the Pitocin-containing bottle with the infusion pump to the infusion line as close to the infusion site as possible. 2. Administration The initial dose should be 0.5–1 mU/min (equal to 3–6 mL of the dilute oxytocin solution per hour). At 30–60 minute intervals the dose should be gradually increased in increments of 1–2 mU/min until the desired contraction pattern has been established. Once the desired frequency of contractions has been reached and labor has progressed to 5–6 cm dilation, the dose may be reduced by similar increments. Studies of the concentrations of oxytocin in the maternal plasma during Pitocin infusion have shown that infusion rates up to 6 mU/min give the same oxytocin levels that are found in spontaneous labor. At term, higher infusion rates should be given with great care, and rates exceeding 9–10 mU/min are rarely required. Before term, when the sensitivity of the uterus is lower because of a lower concentration of oxytocin receptors, a higher infusion rate may be required. 3. Monitoring a. Electronically monitor the uterine activity and the fetal heart rate throughout the infusion of Pitocin. Attention should be given to tonus, amplitude and frequency of contractions, and to the fetal heart rate in relation to uterine contractions. If uterine contractions become too powerful, the infusion can be abruptly stopped, and oxytocic stimulation of the uterine musculature will soon wane (see PRECAUTIONS section). b. Discontinue the infusion of Pitocin immediately in the event of uterine hyperactivity and/or fetal distress. Administer oxygen to the mother, who preferably should be put in a lateral position. The condition of mother and fetus should immediately be evaluated by the responsible physician and appropriate steps taken. B. Control of Postpartum Uterine Bleeding 1. Intravenous infusion (drip method). If the patient has an intravenous infusion running, 10 to 40 units of oxytocin may be added to the bottle, depending on the amount of electrolyte or dextrose solution remaining (maximum 40 units to 1000 mL). Adjust the infusion rate to sustain uterine contraction and control uterine atony. 2. Intramuscular administration. (One mL) Ten (10) units of Pitocin can be given after the delivery of the placenta. C. Treatment of Incomplete, Inevitable, or Elective Abortion Intravenous infusion of 10 units of Pitocin added to 500 mL of a physiologic saline solution or 5% dextrose-in-water solution may help the uterus contract after a suction or sharp curettage for an incomplete, inevitable, or elective abortion. Subsequent to intra-amniotic injection of hypertonic saline, prostaglandins, urea, etc., for midtrimester elective abortion, the injection-to-abortion time may be shortened by infusion of Pitocin at the rate of 10 to 20 milliunits (20 to 40 drops) per minute. The total dose should not exceed 30 units in a 12-hour period due to the risk of water intoxication.
Route of Administration: Other
Using the BV-2 microglial cell line and primary mouse microglia, it was found that oxytocin (0.1, 1, and 10 μM) pre-treatment significantly inhibited LPS-induced microglial activation and reduced subsequent release of pro-inflammatory factors.
Name Type Language
OXYTOCIN
EP   GREEN BOOK   HSDB   INN   MART.   MI   ORANGE BOOK   USP   USP-RS   VANDF   WHO-DD   WHO-IP  
INN  
Official Name English
SYNTOCINON
Brand Name English
OXYTOCIN [USP MONOGRAPH]
Common Name English
OXYTOCIN [WHO-DD]
Common Name English
GLYCINAMIDE, L-CYSTEINYL-L-TYROSYL-L-ISOLEUCYL-L-GLUTAMINYL-L-ASPARAGINYL-L-CYSTEINYL-L-PROLYL-L-LEUCYL-, CYCLIC (1->6)-DISULFIDE
Common Name English
PITOCIN
Brand Name English
OXYTOCIN [USP-RS]
Common Name English
UTERACON
Common Name English
OXYTOCIN [VANDF]
Common Name English
OXYTOCIN [USP]
Common Name English
OXYTOCIN [WHO-IP]
Common Name English
ALPHA-HYPOPHAMINE [WHO-IP]
Common Name English
TTA-121
Code English
OXYTOCINUM [WHO-IP LATIN]
Common Name English
OXYTOCIN [INN]
Common Name English
OXYTOCIN [ORANGE BOOK]
Common Name English
OXYTOCIN [JAN]
Common Name English
OXYTOCIN [HSDB]
Common Name English
OXYTOCIN [MART.]
Common Name English
ENDOPITUITRINA
Common Name English
OXYTOCIN [MI]
Common Name English
OXYTOCIN [GREEN BOOK]
Common Name English
INTERTOCINE S
Common Name English
Classification Tree Code System Code
NDF-RT N0000006473
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NDF-RT N0000009705
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WHO-VATC QG02AC90
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FDA ORPHAN DRUG 453614
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CFR 21 CFR 522.1680
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WHO-ESSENTIAL MEDICINES LIST 22.1
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NDF-RT N0000009705
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NDF-RT N0000006473
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WHO-ATC G02AC01
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WHO-VATC QH01BB02
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NDF-RT N0000009705
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WHO-VATC QG02AC01
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LOINC 2718-5
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EU-Orphan Drug EU/3/14/1302
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FDA ORPHAN DRUG 582717
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NDF-RT N0000175828
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WHO-ATC H01BB02
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LOINC 35415-9
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Code System Code Type Description
CAS
50-56-6
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PRIMARY
ECHA (EC/EINECS)
200-048-4
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PRIMARY
EPA CompTox
50-56-6
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PRIMARY
PUBCHEM
439302
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PRIMARY
FDA UNII
1JQS135EYN
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PRIMARY
INN
1480
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PRIMARY
DRUG CENTRAL
2042
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PRIMARY
WIKIPEDIA
OXYTOCIN
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PRIMARY
NCI_THESAURUS
C724
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PRIMARY
MERCK INDEX
M8348
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PRIMARY Merck Index
USP_CATALOG
1491300
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PRIMARY USP-RS
HSDB
2182
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PRIMARY
ChEMBL
CHEMBL395429
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PRIMARY
RXCUI
7824
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PRIMARY RxNorm
LACTMED
Oxytocin
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PRIMARY
MESH
D010121
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PRIMARY
DRUG BANK
DB00107
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PRIMARY
WHO INTERNATIONAL PHARMACOPEIA
OXYTOCIN
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PRIMARY Description: White or almost white powder. Solubility: Very soluble in water. It dissolves in dilute solutions of acetic acid and of ethanol. Category: Uterine-stimulating (Oxytocic). Storage: Oxytocin should be kept in an airtight container, protected from light, at a temperature of 2 ?C to 8 ?C or if sterile, in asterile, airtight, tamper-evident container. Labelling: The label states:- where applicable, that the substance is free from bacterial endotoxins,- where applicable, that the substance is sterile.Additional information: Oxytocin is hygroscopic. Definition: Oxytocin is a synthetic cyclic nonapeptide having the structure of the hormone produced by the posterior lobe of thepituitary gland that stimulates contraction of the uterus and milk ejection in receptive mammals. It is available in the freeze-dried form as an acetate. Oxytocin contains not less than 93.0% and not more than 103.0% of the peptide C43H66N12O12S2, calculated with reference tothe anhydrous, acetic acid-free substance.By convention, for the purpose of labelling oxytocin preparations, 1 mg of oxytocin peptide (C43H66N12O12S2) is equivalent to 600 IU of biological activity.
EVMPD
SUB09580MIG
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PRIMARY
IUPHAR
2174
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PRIMARY