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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
Apomorphine- and oxytocin-induced penile erection and yawning in male rats: effect of pertussis toxin.
1992 Feb
Syntocinon and 'epidurals' in labour--which comes first?
2003 Dec
Vaginal birth after Caesarean section: a survey of practice in Australia and New Zealand.
2003 Jun
[Effect of steroid hormones and oxytocin on NO and H2O2 production in the endometrium].
2004 Jan-Feb
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
Cephalic version by moxibustion for breech presentation.
2005 Apr 18
[Pharmacodynamical study on Danqi capsule].
2005 Dec
Randomized controlled trial of vaginal misoprostol versus vaginal misoprostol and isosorbide dinitrate for termination of pregnancy at 13-29 weeks.
2005 Dec
[Effects of epidural ropivacaine labor analgesia on duration of labor and mode of delivery].
2005 Jun
Ruptured uterus in a primigravida: a case report.
2005 Mar
Maternal complications with vaginal birth after cesarean delivery: a multicenter study.
2005 Nov
Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist.
2005 Nov
Does the maxim "once a Caesarean, always a Caesarean" still hold true?
2005 Sep
A randomised trial of carbetocin versus syntometrine in the management of the third stage of labour.
2006 Dec
Distribution of MT1 melatonin receptor immunoreactivity in the human hypothalamus and pituitary gland: colocalization of MT1 with vasopressin, oxytocin, and corticotropin-releasing hormone.
2006 Dec 20
Therapeutic termination of second trimester pregnancies with low dose misoprostol.
2006 Jul
IMOP: randomised placebo controlled trial of outpatient cervical ripening with isosorbide mononitrate (IMN) prior to induction of labour - clinical trial with analyses of efficacy, cost effectiveness and acceptability.
2006 Jul 25
Using clinical audit to improve the quality of obstetric care at the Tibetan Delek Hospital in North India: a longitudinal study.
2006 Jun 7
[Delivery of a macrosomic infant: factors predictive of failed labor].
2006 May
Porcine reproductive and respiratory syndrome virus (PRRSV) infection spreads by cell-to-cell transfer in cultured MARC-145 cells, is dependent on an intact cytoskeleton, and is suppressed by drug-targeting of cell permissiveness to virus infection.
2006 Nov 2
[Effect of the calcitonine gene-related peptide on the myometrium contractile activity].
2006 Sep
[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
Experiences of non-progressive and augmented labour among nulliparous women: a qualitative interview study in a Grounded Theory approach.
2007 Jul 28
[Effect of acupuncture on Cx43 knock-out mice dysmenorrhea response].
2008 Dec
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
National survey of obstetricians in Wales regarding induction of labour in women with a previous caesarean section.
2008 Jan
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
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
Effects of oxytocin on methamphetamine-induced conditioned place preference and the possible role of glutamatergic neurotransmission in the medial prefrontal cortex of mice in reinstatement.
2009 Apr
[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
Pulseless electrical activity during caesarean delivery under spinal anaesthesia: a case report of severe anaphylactic reaction to Syntocinon.
2009 Jan
A randomised controlled trial comparing the efficacy of intramuscular syntometrine and intravenous syntocinon, in preventing postpartum haemorrhage.
2009 Jul
"Oxytocin hand": extravasation and vascular compromise after obstetrical pitocin.
2009 Jul
Anaesthesiological considerations on tocolytic and uterotonic therapy in obstetrics.
2009 Jul
[Effectiveness of non-pharmacological strategies in relieving labor pain].
2009 Jun
External aortic compression device: the first aid for postpartum hemorrhage control.
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
Oxytocin decreases methamphetamine self-administration, methamphetamine hyperactivity, and relapse to methamphetamine-seeking behaviour in rats.
2010 Jan
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.
Substance Class Protein
Created
by admin
on Sat Jun 26 15:20:12 UTC 2021
Edited
by admin
on Sat Jun 26 15:20:12 UTC 2021
Protein Sub Type
Sequence Type COMPLETE
Record UNII
1573L6WJ8U
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
OXYTOCIN CITRATE
WHO-DD  
Common Name English
PITOCIN CITRATE
Brand Name English
PITOCIN-BUCCAL
Brand Name English
OXYTOCIN, 2-HYDROXY-1,2,3-PROPANETRICARBOXYLATE (1:1) (SALT)
Common Name English
BUCCAL
Brand Name English
OXYTOCIN, 2-HYDROXY-1,2,3-PROPANETRICARBOXYLATE (SALT)
Common Name English
OXYTOCIN, CITRATE
Common Name English
OXYTOCIN CITRATE [WHO-DD]
Common Name English
Code System Code Type Description
ECHA (EC/EINECS)
277-888-3
Created by admin on Sat Jun 26 15:20:12 UTC 2021 , Edited by admin on Sat Jun 26 15:20:12 UTC 2021
PRIMARY
FDA UNII
1573L6WJ8U
Created by admin on Sat Jun 26 15:20:12 UTC 2021 , Edited by admin on Sat Jun 26 15:20:12 UTC 2021
PRIMARY
PUBCHEM
72941595
Created by admin on Sat Jun 26 15:20:12 UTC 2021 , Edited by admin on Sat Jun 26 15:20:12 UTC 2021
PRIMARY
CAS
7563-62-4
Created by admin on Sat Jun 26 15:20:12 UTC 2021 , Edited by admin on Sat Jun 26 15:20:12 UTC 2021
NON-SPECIFIC STOICHIOMETRY
EVMPD
SUB23136
Created by admin on Sat Jun 26 15:20:12 UTC 2021 , Edited by admin on Sat Jun 26 15:20:12 UTC 2021
PRIMARY
CAS
74499-03-9
Created by admin on Sat Jun 26 15:20:12 UTC 2021 , Edited by admin on Sat Jun 26 15:20:12 UTC 2021
PRIMARY
From To
1_1 1_6
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:SEQUENCE(CALCULATED) CHEMICAL
Molecular Formula CHEMICAL