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Prescriber’s Guide

Oxytocin Nasal Spray

WHAT IS THIS MEDICATION?

Oxytocin is a peptide hormone produced in the hypothalamus and it is best known for its role in labor and lactation.

Intranasal oxytocin has been clinically studied for the treatment of women suffering from sexual dysfunction.13-15

HOW IS THIS MEDICATION SUPPLIED?

Oxytocin is commonly compounded via multiple administration routes including sublingual tablets and intranasal spray.

Common dosage forms requested include the following:

  • Oxytocin 50IU Sublingual Tablet
  • Oxytocin 8IU, 16IU Intranasal Spray

All Oxytocin formulations must be refrigerated.

HOW DOES THIS MEDICATION WORK IN THE HUMAN BODY?

Oxytocin is a key neuromodulator involved in the synchronization of body and brain in the coordination of a wide spectrum of physiological and psychological affects which may promote sexual satisfaction.

Attachment and Pair bonding
An increase of endorphin levels during sexual activity in humans is presumed to contribute to attachment and bonding between partners, similar to that of a mother and newborn.1 Furthermore, the release of endogenous oxytocin from the brain during intimate touching or sexual activity with a partner has been suggested to play a vital role in sexual monogamy in men and women.2 Endogenous oxytocin also arouses feelings of pleasure, peace and security when in the company of a partner.3

Anxiety, Fear & Stress
The release of endogenous oxytocin decreases fearfulness and works as an anxiolytic agent, diminishing the level of anxiety through inhibiting fear responses in the amygdala, which contains substantial numbers of oxytocin receptors. 4,5,6

The amygdala is also the part of the brain that modulates trust. In fact, intranasal administration of synthetic oxytocin has been shown to improve attachment related behaviors such as eye gazing, interpersonal trust, compassion, and positive communiation.7,8

Sexual Arousal and Lubrication
The release of endogenous oxytocin from the pituitary gland into the bloodstream is triggered by sexual stimuli such as hugging, touching, and genital and nipple stimulation in both genders, and its plasma level is correlated with levels of arousal, lubrication, and reaching a peak during orgasm.9

New Relationships and Dyspareunia
A rise in endogenous oxytocin results in an increase of plasma endorphins, natural pain killers that can diminish pain in women who suffer dyspareunia, due to anxiety or lack of trust in their partner during the first stages of their relationship.10

Orgasm
In 2017, a study was performed to monitor oxytocin levels in anorgasmic and orgasmic women. It was reported that orgasmic women had a higher level of endogenous oxytocin that peaked during orgasm, whereas the anorgasmic women had no change.11

Orgasmic women experience increases of oxytocin up to five times its normal level during sexual climax, possibly due to smooth muscle contraction of the reproductive system. Medical literature confirms that women with higher levels of oxytocin experience more intense and more frequent orgasms.12

WHAT CLINICAL STUDIES HAVE BEEN PERFORMED ON THIS MEDICATION?

In 2014, Behnia evaluated 29 heterosexual couples (n=58) with acute effects of 24IU of intranasally administered oxytocin. Oxytocin was found to increase intensity of orgasm and contentment after sexual intercourse. Women reported feeling more relaxed and subgroups indicated better abilities to share sexual desires or to empathize with their partners.13

In a randomized, prospective, double-blind, placebo controlled, crossover trial, Muin et al studied oxytocin in pre- and postmenopausal women (41-65 years old) with sexual dysfunction over a 22-week period. Patients were instructed to inhale 32 IU of oxytocin intranasally up to 50 minutes before intercourse. Female Sexual Function Index scores (FSFI) increased by 26%, Sexual Quality of Life (SQOL-F) scores increased 144%, Sexual Interest and Desire (SIDI-F) scores, increased by 29%, and Female Sexual Distress (FSDS) scores decreased by 36%. The authors concluded that long term intranasal oxytocin improves (1) Sexual Function, (2) Symptoms of Depression, and (3) Sexual Satisfaction.14

HOW DOES THIS MEDICATION MOVE THROUGH THE HUMAN BODY?

Administration of oxytocin nasal spray resulted in an increase in oxytocin plasma levels from 20.8 ± 5.9 pg/mL at baseline to 41.1 ± 19.9 pg/mL after 15 minutes (P=.02) and 35.1 ± 16.4 pg/mL after 30 minutes (P=.07).

After placebo administration, oxytocin plasma levels remained unaltered from baseline levels of 20.0 ± 3.2 pg/mL to 20.0 ± 5.2 pg/mL after 15 minutes and 20.7 ± 5.6 pg/mL after 30 minutes (repeated measures ANOVA, P<.001, between groups)

Oxytocinase, a glycoprotein aminopeptidase that is capable of degrading oxytocin, is produced during pregnancy and is present in the plasma. There is little or no degradation of oxytocin in nonpregnant women and men.

Oxytocin is rapidly removed from plasma by the liver and kidneys, with only small amounts being excreted unchanged in the urine.

WHAT IS THIS MEDICATION USED FOR?

Oxytocin has been studied in pre- and postmenopausal women with female sexual dysfunction.13,14,15

WHAT IS THE DOSAGE FOR THIS MEDICATION?

Oxytocin has been clinically studied for intranasal use at doses ranging from 24-32IU daily.

Many physicians also prescribe oxytocin 50IU SL tabs to be used daily and 1 hour prior to sexual activity.

MAXIMUM DOSAGE

No specific maximum dosage limit recommendations are available. Dosage regimens of oxytocin depend upon the patient’s age, sex, weight, and condition being treated, product chosen, and the prescribing clinician’s judgment. Therefore, doses may vary widely and must be carefully individualized.

WHEN SHOULD THIS MEDICATION NOT BE PRESCRIBED?

The common exclusion criteria in oxytocin studies are pregnancy, breastfeeding, severe medical/psychiatric illnesses, known allergies to ingredients of medication, excessive smoking or drinking, and other medication intake with associated reduction of sexual function.

Oxytocin may possess antidiuretic effects, and prolonged use can increase the possibility of an antidiuretic effect.

WHAT SIDE EFFECTS CAN BE CAUSED BY THIS MEDICATION?

Based on the study by Muin et al, the following adverse reactions occurred: runny nose and burning sensation in the nose (10%), headache (10%), epistaxis (3%), nausea (3%), dizziness (3%).15

Oxytocin causes dilation of vascular smooth muscle, thus increasing renal, coronary, and cerebral blood flow. Blood pressure usually remains unaffected. Oxytocin does process antidiuretic effects, but they are minimal.

IS THIS MEDICATION SAFE DURING BREASTFEEDING AND CAN I USE IT FOR KIDS?
Pregnancy and Lactation

Oxytocin presents a potential occupational hazard to men and women actively trying to conceive and women who are pregnant or may become pregnant, and are breast feeding, due to presence of the drug in breast milk. Endogenous oxytocin is involved in the process of lactation and therefore, oxytocin has been used in mothers having difficulty with engorgement and breast feeding. Because several small studies have failed to show a beneficial effect, oxytocin is not used for this indication. Oxytocin is excreted in breast milk, but is not expected to have adverse effects in the infant.

Geriatric Use

Oxytocin has been studied for sexual dysfunction in premenopausal and postmenopausal women and couples identified as 65 years of age or older.

Renal and Hepatic Impairment

Specific guidelines for dosage adjustments in renal and hepatic impairments are not available; it appears that no dosage adjustments are needed.

REFERENCES
  1. Esch T, Stefano GB. The Neurobiology of Love. Neuro Endocrinol Lett. 2005 Jun;26(3):175-92. PMID: 15990719.
  2. Levin, R. and Meston, C. (2006), Nipple/Breast Stimulation and Sexual Arousal in Young Men and Women. The Journal of Sexual Medicine, 3: 450-454.
  3. Marjan Khajehei, Elmira Behroozpour Endorphins, oxytocin, sexuality and romantic relationships: An understudied area. World J Obstet Gynecol. Oct 22, 2018; 7(2): 17-23
  1. Esch T, Stefano GB. The Neurobiology of Love. Neuro Endocrinol Lett. 2005 Jun;26(3):175-92. PMID: 15990719.
  2. Levin, R. and Meston, C. (2006), Nipple/Breast Stimulation and Sexual Arousal in Young Men and Women. The Journal of Sexual Medicine, 3: 450-454.
  3. Marjan Khajehei, Elmira Behroozpour Endorphins, oxytocin, sexuality and romantic relationships: An understudied area. World J Obstet Gynecol. Oct 22, 2018; 7(2): 17-23
  4. Jones C, Barrera I, Brothers S, Ring R, Wahlestedt C. Oxytocin and social functioning. Dialogues Clin Neurosci. 2017;19(2):193-201. doi:10.31887/DCNS.2017.19.2/cjones
  5. Hoge EA., Pollack MH., Kaufman RE., Zak PJ., Simon NM. Oxytocin levels in social anxiety disorder. CNS Neurosci Ther. 2008;14(3):165–170.
  6. Marazziti D., Baroni S., Catena M., et al A relationship between social anxiety and oxytocin. Eur Psychiatry. 2007;22:S281–S282.
  7. Guastella AJ, Mitchell PB, Dadds MR. Oxytocin increases gaze to the eye region of human faces. Biol Psychiatry. 2008;63:3-5.
  8. Ditzen B, Schaer M, Gabriel B, Bodenmann G, Ehlert U, Heinrichs M. Intranasal oxytocin increases positive communication and reduces cortisol levels during couple conflict. Biol Psychiatry. 2009;65:728-731.
  9. Meston CM, Levin RJ, Sipski ML, Hull EM, Heiman JR. Women's orgasm. Annu Rev Sex Res. 2004;15:173-257. PMID: 16913280.
  10. Rosenbaum TY. Musculoskeletal pain and sexual function in women. J Sex Med. 2010 Feb;7(2 Pt 1):645-53. doi: 10.1111/j.1743-6109.2009.01490.x. Epub 2009 Sep 14. PMID: 19751383.
  11. Caruso S, Mauro D, Scalia G, Palermo CI, Rapisarda AMC, Cianci A. Oxytocin plasma levels in orgasmic and anorgasmic women. Gynecol Endocrinol. 2018 Jan;34(1):69-72. doi: 10.1080/09513590.2017.1336219. Epub 2017 Jun 11. PMID: 28604123.
  12. 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. doi: 10.1210/jcem-64-1-27. PMID: 3782434.
  13. Anderson-Hunt M, Dennerstein L. Increased female sexual response after oxytocin. BMJ. 1994;309:929.
  14. Behnia B, Heinrichs M, Bergmann W, et al. Differential effects of intranasal oxytocin on sexual experiences and partner interactions in couples. Horm Behav. 2014;65(3):308-318.
  15. Muin DA, Wolzt M, Marculescu R, et al. Effect of long-term intranasal oxytocin on sexual dysfunction in premenopausal and postmenopausal women: a randomized trial. Fertil Steril. 2015;104(3):715-23.e4.
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