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Oxytocin - DrugBank
Oxytocin - DrugBank
IDENTIFICATION
Name Oxytocin
Type Biotech
Description Synthetic 9 residue cyclic peptide. The hormone is prepared synthetically to avoid possible
contamination with vasopressin (ADH) and other small polypeptides with biologic activity.
Protein structure
Synonyms Oxitocina
Oxytocin
MARKETING MARKETING
NAME ↑↓ DOSAGE ↑↓ STRENGTH ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓
ADDITIONA
MARKETING MARKETING
Oxytocin
NAME ↑↓ Injection
DOSAGE ↑↓ 10 ↑↓
[USP'U]/1mL
STRENGTH ↑↓
Intramuscular;
ROUTE Hikma
LABELLER ↑↓ 1980-04-29
START ↑↓ ↑↓
Not applicable
END ↑↓ ↑↓
Intravenous Pharmaceuticals
USA Inc. Drugs
Oxytocin Injection, 30 Intravenous Cantrell Drug 2016-03-18 Not applicable
solution [USP'U]/1000mL Company
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MARKETING MARKETING
NAME ↑↓ INGREDIENTS DOSAGE ↑↓ ROUTE ↑↓ LABELLER ↑↓ START ↑↓ END ↑↓ ↑↓ ↑↓
Showing 1 to 2 of 2 entries ‹ 1 ›
Oxytocin Oxytocin (30 Injection, Intravenous Cantrell Drug 2011-10-20 Not applicable
[USP'U]/500mL) solution Company Drugs
Oxytocin Oxytocin (10 Injection, Intravenous Cantrell Drug 2012-07-30 Not applicable
[USP'U]/1000mL) solution Company
Oxytocin Oxytocin (20 Injection, Intravenous Cantrell Drug 2016-03-18 Not applicable
[USP'U]/500mL) solution Company
Oxytocin Oxytocin (30 Injection, Intravenous Cantrell Drug 2016-03-18 Not applicable
[USP'U]/1000mL) solution Company
Showing 1 to 10 of 13 entries ‹ 1 2 ›
Categories Amino Acids, Peptides, and Oxytocin and Analogues Pituitary Hormones, Posterior
Proteins
Oxytocin, analogs & derivatives Posterior Pituitary Lobe Hormones
Genito Urinary System and Sex
Oxytocin, antagonists & inhibitors Potential QTc-Prolonging Agents
Hormones
Peptide Hormones QTc Prolonging Agents
Hormones
Peptides Reproductive Control Agents
Hormones, Hormone Substitutes,
and Hormone Antagonists Pituitary and Hypothalamic Systemic Hormonal Preparations,
Hormones and Analogues Excl. Sex Hormones and Insulins
Increased Uterine Smooth Muscle
Contraction or Tone Pituitary Hormones Uterotonic agents
UNII 1JQS135EYN
PHARMACOLOGY
Indication Used for labor induction, augmentation of labor, postpartum abbreviation of third stage of labor,
postpartum control of uterine bleeding, termination of pregnancy and for the evaluation of fetal
respiratory capability. Oxytocin cannot be used for elective induction of labor, there must be a
clear medical requirement.
Postpartum Bleeding
Reinforcement of labor
Pharmacodynamics Indirectly stimulates contraction of uterine smooth muscle by increasing the sodium permeability
of uterine myofibrils. Increases contraction amplitude and frequency, which tends to decrease
cervical activity, produce dilation and effacement of the cervix, and transiently impede uterine
blood flow; contractions produced by oxytocin at term are similar to those occurring during
spontaneous labor. High estrogen concentrations lower the threshold for uterine response to
oxytocin. Uterine response increases with the duration of pregnancy and is greater in labor than
DrugsContracts
when not in labor; only very large doses elicit contractions in early pregnancy.
myoepithelial cells surrounding the alveoli of the breasts, forcing milk from the alveoli into the
larger ducts and facilitating milk ejection. Minimal antidiuretic activity relative to vasopressin;
water intoxication possible at high doses and/or excessive electrolyte-free fluid.
Mechanism of action 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+, which in turn activates myosin's light
chain kinase.. Oxytocin has specific receptors in the muscle lining of the uterus and the receptor
concentration increases greatly during pregnancy, reaching a maximum in early labor at term.
Comprehensive structured data on known drug Structured data covering drug Structured data representing warnings from the
adverse effects with statistical prevalence. contraindications. Each contraindication black box section of drug labels. These warnings
MedDRA and ICD10 ids are provided for adverse describes a scenario in which the drug is not to cover important and dangerous risks,
effect conditions and symptoms. be used. Includes restrictions on co- contraindications, or adverse effects.
administration, contraindicated populations,
LEARN MORE and more. LEARN MORE
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Volume of Distributes throughout the extracellular fluid and crosses the placenta. It is probable that it also
distribution distributes into milk in small amounts.
Metabolism
Oxytocin is rapidly metabolized in the liver and also in the plasma by oxytocinases. It is also
metabolized to a smaller degree by the mammary glands.
Half life 1-6 min, this is decreased in late pregnancy and during lactation.
Toxicity Oxytocin can produce a severe water intoxication due to its antidiuretic effect. Prolonged IV
infusions of more 40milliunits/min are usually the cause. Severe water intoxication with
convulsions, coma, and death can occur. Some neonatal seizures have also been reported.
Consider potential for water intoxication, particularly when administered by IV infusion and
patient is receiving oral fluids. Uterine effects: High doses or hypersensitivity to oxytocin may
cause uterine hypertonicity, spasm, tetanic contraction, or rupture of the uterus. There have also
been reported allergic and anaphylactic reactions to oxytocin but they were rarely fatal.
INTERACTIONS
Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are
experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does
not necessarily mean no interactions exist.
INVESTIGATIONAL EXPERIMENTAL
DRUG ↑↓ INTERACTION ↑↓
Abexinostat The risk or severity of QTc prolongation can be increased when Oxytocin is combined with
Abexinostat.
Acebutolol The risk or severity of QTc prolongation can be increased when Oxytocin is combined with
Acebutolol.
Aceprometazine The risk or severity of QTc prolongation can be increased when Oxytocin is combined with
Aceprometazine.
Acrivastine The risk or severity of QTc prolongation can be increased when Oxytocin is combined with
Acrivastine.
Adenosine The risk or severity of QTc prolongation can be increased when Oxytocin is combined with
Adenosine.
Ajmaline The risk or severity of QTc prolongation can be increased when Oxytocin is combined with
Ajmaline.
Alfuzosin The risk or severity of QTc prolongation can be increased when Oxytocin is combined with
Alfuzosin.
Alimemazine The risk or severity of QTc prolongation can be increased when Oxytocin is combined with
Alimemazine.
Amantadine The risk or severity of QTc prolongation can be increased when Oxytocin is combined with
Amantadine.
REFERENCES
Synthesis Reference Kerstin Uvnas-Moberg, Thomas Lundeberg, "Use of substances having oxytocin activity for
preparation of medicaments for wound healing." U.S. Patent US6262021, issued August, 1988.
US6262021
General References
1. Kosfeld M, Heinrichs M, Zak PJ, Fischbacher U, Fehr E: Oxytocin increases trust in humans. Nature. 2005 Jun 2;435(7042):673-6.
[PubMed:15931222]
2. Takayanagi Y, Yoshida M, Bielsky IF, Ross HE, Kawamata M, Onaka T, Yanagisawa T, Kimura T, Matzuk MM, Young LJ, Nishimori
K: Pervasive social deficits, but normal parturition, in oxytocin receptor-deficient mice. Proc Natl Acad Sci U S A. 2005 Nov
1;102(44):16096-101. Epub 2005 Oct 25. [PubMed:16249339]
3. Carmichael MS, Humbert R, Dixen J, Palmisano G, Greenleaf W, Davidson JM: Plasma oxytocin increases in the human sexual
response. J Clin Endocrinol Metab. 1987 Jan;64(1):27-31. [PubMed:3782434]
4. Paquin J, Danalache BA, Jankowski M, McCann SM, Gutkowska J: Oxytocin induces differentiation of P19 embryonic stem
cells to cardiomyocytes. Proc Natl Acad Sci U S A. 2002 Jul 9;99(14):9550-5. Epub 2002 Jul 1. [PubMed:12093924]
5. Jankowski M, Danalache B, Wang D, Bhat P, Hajjar F, Marcinkiewicz M, Paquin J, McCann SM, Gutkowska J: Oxytocin in cardiac
ontogeny. Proc Natl Acad Sci U S A. 2004 Aug 31;101(35):13074-9. Epub 2004 Aug 17. [PubMed:15316117]
External Links KEGG Drug D00089
RxNav 7824
ChEMBL CHEMBL395429
PharmGKB PA450760
Wikipedia Oxytocin
H01BB02 — Oxytocin
H01BB — Oxytocin and analogues
H01B — POSTERIOR PITUITARY LOBE HORMONES
H01 — PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
H — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
CLINICAL TRIALS
PHARMACOECONOMICS
Manufacturers App pharmaceuticals llc Baxter healthcare corp Teva parenteral medicines
anesthesia critical care inc
anesthesia critical care inc
Packagers APP Pharmaceuticals BAM Biotech Baxter International Inc. Bimeda Inc.
Cardinal Health Gland Pharma Ltd. MWI Veterinary Supply Co. Pharmedium
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DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PROPERTIES
State Liquid
TAXONOMY Drugs
TARGETS
Kind Protein
Organism Humans
Actions Agonist
General Function Vasopressin receptor activity
Specific Function Receptor for oxytocin. The activity of this receptor is mediated by G
proteins which activate a phosphatidylinositol-calcium second messenger
system.
Uniprot ID P30559
References
1. Spyranti Z, Fragiadaki M, Magafa V, Borovickova L, Spyroulias GA, Cordopatis P, Slaninova J: In position 7 L- and D-Tic-substituted oxytocin and
deamino oxytocin: NMR study and conformational insights. Amino Acids. 2010 Jul;39(2):539-48. doi: 10.1007/s00726-009-0470-1. Epub 2010 Jan
27. [PubMed:20108008]
2. Frantz MC, Rodrigo J, Boudier L, Durroux T, Mouillac B, Hibert M: Subtlety of the structure-affinity and structure-efficacy relationships around a
nonpeptide oxytocin receptor agonist. J Med Chem. 2010 Feb 25;53(4):1546-62. doi: 10.1021/jm901084f. [PubMed:20104850]
3. Gimpl G, Reitz J, Brauer S, Trossen C: Oxytocin receptors: ligand binding, signalling and cholesterol dependence. Prog Brain Res. 2008;170:193-
204. doi: 10.1016/S0079-6123(08)00417-2. [PubMed:18655883]
4. Ahn TG, Han SJ, Cho YS, An TH, Pak SC, Flouret G: In vivo activity of the potent oxytocin antagonist on uterine activity in the rat. In Vivo. 2004
Nov-Dec;18(6):763-6. [PubMed:15646817]
5. Furman DJ, Chen MC, Gotlib IH: Variant in oxytocin receptor gene is associated with amygdala volume. Psychoneuroendocrinology. 2011
Jul;36(6):891-7. doi: 10.1016/j.psyneuen.2010.12.004. Epub 2011 Jan 3. [PubMed:21208749]
2. Oxytocin-neurophysin 1 Details
Drugs
Kind Protein
Organism Humans
Actions Binder
Uniprot ID P01178
References
1. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
[PubMed:17016423]
2. Land H, Grez M, Ruppert S, Schmale H, Rehbein M, Richter D, Schutz G: Deduced amino acid sequence from the bovine oxytocin-neurophysin I
precursor cDNA. Nature. 1983 Mar 24-30;302(5906):342-4. [PubMed:6687626]
3. Rao VV, Loffler C, Battey J, Hansmann I: The human gene for oxytocin-neurophysin I (OXT) is physically mapped to chromosome 20p13 by in situ
hybridization. Cytogenet Cell Genet. 1992;61(4):271-3. [PubMed:1486803]
ENZYMES
Kind Protein
Organism Humans
Actions Substrate
Specific Function Cleaves peptide bonds on the C-terminal side of prolyl residues within
peptides that are up to approximately 30 amino acids long.
Uniprot ID P48147
References
1. Irazusta J, Silveira PF, Gil J, Varona A, Casis L: Effects of hydrosaline treatments on prolyl endopeptidase activity in rat tissues. Regul Pept. 2001
Sep 15;101(1-3):141-7. [PubMed:11495689]
2. Bausback HH, Ward PE: Vascular, post proline cleaving enzyme: metabolism of vasoactive peptides. Adv Exp Med Biol. 1986;198 Pt A:397-404.
[PubMed:3544718]
3. Yoshimoto T, Nishimura T, Kita T, Tsuru D: Post-proline cleaving enzyme (prolyl endopeptidase) from bovine brain. J Biochem. 1983
Oct;94(4):1179-90. [PubMed:6361010]
Drug created on June 13, 2005 07:24 / Updated on July 03, 2020 08:33
Drugs