Oxytocin 10mg

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Description

Oxytocin for sale

Labor is synonymous to the body’s natural phenomenon of childbirth. Labor begins with steady uterine contractions, which continue through the delivery of the baby.

There is no definitive time when labor would begin. While it is different for every woman, there are some physical changes which occur either a few hours or a couple weeks before the labor begins. These include increased need to urinate (which mainly occurs due to the baby settling lower into the pelvis), vaginal discharge and finally, the beginning of uterine contractions.

Uterine contractions can be extremely intense, some say these are as intense as menstrual cramps (1).

A commonly used peptide during the labor process is Oxytocin.

Oxytocin is a potent facilitator peptide as it not only helps facilitate childbirth, but also helps after childbirth, mainly in breastfeeding. Oxytocin plays a vital role in female reproduction (2).

What is Oxytocin

Oxytocin is derived from a Greek word where ‘oxus’ means ‘swift’ and ‘tokos’ means ‘childbirth’.

The peptide is a naturally occurring cyclic peptide hormone composed of nine amino acids. It mainly acts as a neurotransmitter in the brain and is secreted by the pituitary gland (3).

The synthetic form of the peptide, called Recombinant Oxytocin, is also a cyclic nonapeptide that is exactly analogous to the naturally occurring peptide (4).

When Was Oxytocin Discovered?

The uterine contracting properties of Oxytocin were first discovered in 1906 by a British pharmacologist (5), and the milk ejecting properties were later discovered in 1910 – 1911 by other scientists (6).

First isolation of Oxytocin was carried out in 1920, followed by its structure discovery in the 1950s and thereafter several research studies have been conducted to fully explore the peptide abilities and characteristics.

What Is The Working Mechanism?

As mentioned above, Oxytocin is a naturally occurring peptide hormone.

Created by the hypothalamus, Oxytocin is then secreted and stored in the posterior pituitary gland, which is then secreted in the body on hormonal stimulation (7).

Unlike other hormones, Oxytocin works by a positive feedback mechanism. This means that the initial secretion of the hormone peptide leads to further release of the peptide in higher concentrations and with higher intensity (7).

Both synthetic and natural forms of Oxytocin work through the same mechanism causing similar responses in the female reproductive system.

Uterine Contractions

Once entered into the system, Oxytocin binds with the G-protein coupled receptors found in the uterus membrane that leads to increased levels of intracellular calcium. This calcium secretion then causes uterine contractions. Once the uterine contractions begin, it stimulates further release of Oxytocin leading to higher frequency and intensity of the contractions, via positive feedback mechanism (7).

Breastfeeding Abilities

Oxytocin causes the contraction of myoepithelial cells found in the alveolar ducts of the female breasts. These contractions then stimulate milk ejection from these alveolar ducts into the larger sinuses, thereby leading to milk expulsion. The positive feedback mechanism also works here, and initial milk expulsion stimulates more peptide release and continuous milk release (7).

What Are The Advantages of Oxytocin?

As stated earlier, the two main advantages of Oxytocin are how it facilitates the female reproductive system through (a) uterine contractions during labor, and (b) breastfeeding after delivery.

The other advantages of the peptide are:

  • Antidiuretic effects
  • Vasodilatory effects
  • Increased cerebral, coronary, and renal blood flow

Scientific Research Studies on Oxytocin

Labor Induction

It is known that Oxytocin induces uterine contractions leading to labor. The main aim of this study (8) was to determine the rate of cesarean delivery in women after discontinuing Oxytocin administration once active labor starts (5 cm cervical dilation) compared to women where Oxytocin is administered until the maintenance level as determined in clinical trial study protocol.

A randomized clinical trial was conducted in 252 female participants aged between 18 to 50 years.

The participants were divided into two groups with 127 volunteers (group A) continuously administered with Oxytocin per study protocol even after the participants reach active labor, and 125 volunteers (group B) administered with Oxytocin and then discontinued after active labor induction.

After a 24-72 hour study period, there were 32 cesarean deliveries in group A with 10 infants admitted to NICU whereas there were 24 caesarean deliveries in group B with 9 infants admitted to NICU. No adverse events were reported.

This study demonstrates that Oxytocin has a positive effect in women to induce labor and can be given as a determined dose in this study (dose not specified in the online data).

Breastfeeding

The main goal of this study (9) was to evaluate the effects of Oxytocin on breastfeeding after childbirth.

A retrospective study (9) was conducted where 100 women who were treated with Oxytocin during labor were compared with 100 other women not exposed to Oxytocin. As a part of this study, duration of breastfeeding was examined through a phone call interview.

After analysis, it was demonstrated that the Oxytocin administered women showed impaired breastfeeding for the first hour.

Also, for the first three months after delivery, women from both groups (27% women treated with Oxytocin, and 14% of non-treated women) were not able to breastfeed. Post three months, the breastfeeding was significant in the peptide treated women.

The reason identified for impaired breastfeeding during the first three months was the high pregestational body mass index.

This study demonstrates that further studies are yet to be completed, but the evaluation strongly suggests that medical practitioners should assist obese women to maximize lactation outcomes.

Vasodilation

Vasodilation is the dilation of blood vessels, which is a mechanism to increase blood flow to areas of the body. The main purpose of this study (10) was to evaluate the effects of Oxytocin on cardiac function and tone in the heart muscles.

Fifty-one pregnant women were enrolled in this study who were divided into two groups, one being treated with 8.3 microg Oxytocin and other with a placebo during the first trimester. Heart rate and blood pressure were recorded before and after administration.

The results demonstrated that Oxytocin had vasodilatory effects on the small and outlying arteries and elevated that left ventricular ejection time, thereby suggesting the vasodilatory effects of Oxytocin.

Psychiatric Disorders

Autism

The main aim of this study (11) was to evaluate if Oxytocin has any effect on patients suffering from autism. Autism is a psychiatric disorder related to poor brain development impacting how people socialize and communicate with others.

59 males, aged 6 to 11 years, were examined in this study. Out of the 59 volunteers, 29 were autistic, whereas the rest were healthy candidates. The plasma levels of oxytocin were measured in this study, and it was seen that autistic candidates had significantly lower levels of peptide hormone (~0.64 pg/mL) compared to the healthy candidates (~1.16 pg/mL). Once the levels of Oxytocin were elevated, the VABS score (analytic behavior score) of autistic candidates improved.

These results show that Oxytocin has a positive effect on the social behavior abilities of the autistic patients and can potentially be used in psychiatric treatment.

Schizophrenia

The main aim of this study (11) was to evaluate if Oxytocin has any effect on patients suffering from schizophrenia. Schizophrenia is a chronic neurological disorder characterized with hallucinations, impaired speech, and lack of motivation.

When plasma levels of Oxytocin were measured between 12 schizophrenic patients and 12 healthy candidates, the levels were significantly higher in schizophrenic patients compared to the rest (11,12).

In another study (13), there were 43 volunteers out of whom 28 were schizophrenic patients and 15 were healthy candidates. The schizophrenic candidates were treated with Haldol, a neurological medication used to treat mood disorders. However, even after treatment, the schizophrenic patients showed elevated Oxytocin levels (10 to 13 pg/mL) compared to healthy candidates (7 pg/mL).

This demonstrated that any imbalance in Oxytocin levels can potentially induce Schizophrenia and hence, these levels need to be maintained at equilibrate levels.

Obsessive Compulsive Disorder (OCD)

Reports (14) have shown that a 55-year-old patient suffering from obsessive compulsive disorder (OCD) demonstrated a significant improvement after 4 weeks of intranasal Oxytocin treatment.

However, in addition to this improvement, there were also increased cases of memory disturbances. Besides, the patient also showed reduced sodium levels in blood plasma and decreased osmolality.

Hence, a clear understanding is yet to be established and additional studies are to be conducted to clearly show if the peptide helps treat OCD patients.

Are There Any Adverse Effects of Oxytocin?

The common side effects of Oxytocin administration are (7):

  • Irritation and redness at the site of injection
  • Nausea
  • Vomiting
  • Stomach ache
  • Appetite loss
  • Increased contractions
  • Breathing difficulties
  • Abnormal bleeding (15)

Serious adverse effects of the peptide include (7):

  • Irregular rhythm of the heart
  • Seizures
  • Hallucinations, delusions
  • Elevated blood pressure
  • Blurred vision

Contraindications

There can be certain contradictions towards Oxytocin that are primarily due to hypersensitivity towards the peptide itself or towards the content of its synthetic version.

Besides, the following conditions can lead to contradictions to administering the peptide (7):

  • When fetal position is abnormal
  • Cervical cancer
  • Herpes
  • Women with pelvises not large enough to handle normal delivery
  • Women with a uterus that is extremely active and/or tonic
  • High blood pressure (15)
  • Placenta previa (condition where placenta is blocking the uterine neck)(15)
  • Uterus surgery / cervical surgery (15)

Can Improper Oxytocin Dosage Lead to Toxicity?

It is very critical to monitor the fluid levels of the patients after Oxytocin administration (7).

Improper dosing of Oxytocin may cause severe toxic reactions in the patients such as arrhythmia and ischemia, and high doses can also lead to spasms and uterine rupture (7).

In 2012, a retrospective study (16) was conducted where the hemoglobin levels of the women treated with Oxytocin during labor were examined. Women treated with higher Oxytocin dose led to an extremely high blood loss compared to women either treated with moderate Oxytocin levels or not treated with the peptide. This demonstrates that improper dosing of the peptide hormone can lead to severe adverse effects.

Recommended Administration

US FDA Approval Status

Oxytocin is approved by the US FDA to be used in antepartum (to induce uterine contractions and labor) and postpartum (to control post-delivery hemorrhage) stages (7).

However, it should be noted that the product is not yet FDA approved for treating psychiatric disorders in humans (13).

Recommended Route of Administration

Oxytocin is primarily administered via intravenous route of administration using drip method in complicated labor situations. It can also be administered intramuscularly during excessive bleeding after childbirth (7).

Recommended Dosage for Oxytocin

To induce labor, the recommended dosage is 0.5 to 2 milliunits/min via intravenous route, with 1 to 2 milliunits increment every 15 to 40 minutes. This can continue until a consistent contraction pattern is established (7).

To control excessive postpartum bleeding, the recommended dose is 10 units via intramuscular route after placental delivery (only administered once)(7). For therapeutic (continued) dosing, it can be administered at the dose of 60 to 200 milliunits/min via intravenous route.

Summary

Oxytocin is a nonapeptide, which is a facilitating hormone peptide, primarily due to its facilitating capabilities to the female reproductive system.

Available in both endogenous (natural) and exogenous (synthetic) form, Oxytocin primarily works via a positive feedback mechanism.

The primary benefits of the peptide are that it stimulates uterine muscle contraction (used to induce labor) and increases milk ejection (used to induce lactation). Besides, it also possesses vasodilatory effects and may play a vital role in monitoring psychiatric disorders.

The dosing of the Oxytocin is extremely critical. While overall the peptide is well tolerated by the body, any overdose or improper dosing of the product can cause severe side effects including postpartum hemorrhage.

Since its discovery over 100 years ago, Oxytocin has been rigorously studied and is now FDA approved for labor induction and postpartum use (11). However, further studies of the peptide are still underway, especially to explore its role in potentially treating human psychiatric disorders.

References:

1. Signs of Labor. https://www.webmd.com/baby/labor-signs#1

2. Magon, N., & Kalra, S. (2011). The orgasmic history of oxytocin: Love, lust, and labor. Indian journal of endocrinology and metabolism, 15 Suppl 3(Suppl3), S156–S161. https://doi.org/10.4103/2230-8210.84851

3. National Center for Biotechnology Information. “PubChem Compound Summary for CID 439302, Oxytocin” PubChem, https://pubchem.ncbi.nlm.nih.gov/compound/Oxytocin

4. Recombinant Oxytocin (Code C724). https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C724

5. Dale, H H. “On some physiological actions of ergot.” The Journal of physiology vol. 34,3 (1906): 163-206. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1465771/

6. The action of animal extracts on milk secretion. https://royalsocietypublishing.org/doi/10.1098/rspb.1911.0042

7. Osilla EV, Sharma S. Oxytocin. [Updated 2021 Jul 27]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2021 Jan. https://www.ncbi.nlm.nih.gov/books/NBK507848/

8. Induction of Labor with Oxytocin: When Should Oxytocin be held? https://clinicaltrials.gov/ct2/show/results/NCT00957593

9. Gomes M, Trocado V, Carlos-Alves M, Arteiro D, Pinheiro P. Intrapartum synthetic oxytocin and breastfeeding: a retrospective cohort study. J Obstet Gynaecol. 2018 Aug;38(6):745-749. Epub 2018 Mar 9. https://pubmed.ncbi.nlm.nih.gov/29523035/

10. Rabow, S., Hjorth, U., Schönbeck, S. et al. Effects of oxytocin and anaesthesia on vascular tone in pregnant women: a randomised double-blind placebo-controlled study using non-invasive pulse wave analysis. BMC Pregnancy Childbirth 18, 453 (2018). https://bmcpregnancychildbirth.biomedcentral.com/articles/10.1186

11. Cochran, D. M., Fallon, D., Hill, M., & Frazier, J. A. (2013). The role of oxytocin in psychiatric disorders: a review of biological and therapeutic research findings. Harvard review of psychiatry, 21(5), 219–247. https://doi.org/10.1097/HRP.0b013e3182a75b7d

12. Hollander E, Bartz J, Chaplin W, Phillips A, Sumner J, Soorya L, Anagnostou E, Wasserman S. Oxytocin increases retention of social cognition in autism. Biol Psychiatry. 2007 Feb 15;61(4):498-503. https://pubmed.ncbi.nlm.nih.gov/16904652/

13. Guastella AJ, Einfeld SL, Gray KM, Rinehart NJ, Tonge BJ, Lambert TJ, Hickie IB. Intranasal oxytocin improves emotion recognition for youth with autism spectrum disorders. Biol Psychiatry. 2010 Apr 1;67(7):692-4. https://pubmed.ncbi.nlm.nih.gov/19897177/

14. Ansseau M, Legros JJ, Mormont C, Cerfontaine JL, Papart P, Geenen V, Adam F, Franck G. Intranasal oxytocin in obsessive-compulsive disorder. Psychoneuroendocrinology. 1987;12(3):231-6. https://pubmed.ncbi.nlm.nih.gov/3615752/

15. Oxytocin Injection. https://medlineplus.gov/druginfo/meds/a682685.html

16. Pursche T, Diedrich K, Banz-Jansen C. Blood loss after caesarean section: depending on the management of oxytocin application? Arch Gynecol Obstet. 2012 Sep;286(3):633-6. https://pubmed.ncbi.nlm.nih.gov/22569708/


 

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