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Drug Monograph

Oxytocin Intranasal Spray

DESCRIPTION

Oxytocin is a hormone produced by the hypothalamus that may promote feelings of intimacy.

HOW SUPPLIED

Oxytocin is compounded, and available via multiple administration routes: sublingual tablet, intranasal spray, or oral capsule.

Oxytocin 50IU Sublingual Tablet

Oxytocin 50IU Capsule

Oxytocin 8IU, 16IU Intranasal Spray

CLINICAL PHARMACOLOGY

Oxytocin is a key neuromodulator involved in the synchronization of body and brain in the coordination of a wide spectrum of behavior, physiological, and psychological responses. This is supported by evidence that brain regions such as the amygdala and nucleus accumbens that are associated with socio-affective and reward are particularly sensitive to oxytocin. Hence, oxytocin may be an important factor in improving the multifaceted problem of sexual dysfunction.

Oxytocin is released in response to a variety of stimuli, including skin-to-skin contact, foreplay, and sex. At normal levels, oxytocin encourages a mild desire for contact with your partner. Being touched, however, can lead to a rise in oxytocin levels. This rise in oxytocin levels causes a cascade of reactions within the body, including the release of endorphins and testosterone, which results in both biological and psychological arousal. Eventually nerves in erogenous zones become sensitized, with continued contact causing even more oxytocin to be released. Arousal continues its upward climb from there. Furthermore, oxytocin causes vasodilation and increase blood flow to the genitals.

Oxytocin increases five times its normal level during sexual climax, possibly due to smooth muscle contraction of the reproductive system. Medical literature confirms that the higher the levels of oxytocin, the more intense and the more frequent the orgasm. Also, oxytocin lowers serum cortisol, which is often called the “stress” hormone, therefore, it can improve mood.

PHARMACOKINETICS

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.

CLINICAL STUDIES

There are oxytocin receptors in the brain of both sexes, as well as in the uterus of a pregnant woman. One of the key effects of oxytocin is to block fear, anxiety, and panic input into the amygdala. The amygdala is the almond-shaped group of nuclei within the brain and is part of the limbic system, which modulates emotion, behavior, long-term memory, and olfaction. The amygdala is also the part of the brain that modulates trust. Researchers have confirmed a strong link between oxytocin and sociability.

In 2014, Behnia reported that women experienced an increased intensity of orgasm and contentment after sexual intercourse after being administered intranasal oxytocin. 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.1

Muin et al studied oxytocin in pre- and postmenopausal women (41-65 years old) with sexual dysfunction. For each treatment arm, patients were instructed to inhale 32 IU of oxytocin intranasally up to 50 minutes before intercourse. It was shown that oxytocin improved their sexual function index score from baseline. Overall, scores in Female Sexual Distress Scale (FSDS) improve in pre and post-menopausal women with long term treatment with intranasal oxytocin.

INDICATIONS

Oxytocin has been studied in pre- and postmenopausal women with hypoactive sexual desire, arousal and orgasmic disorder.2

Although not studied, literature regarding oxytocin indicates that it may be useful in women to improve the inability to become aroused relating to anxiety or inadequate stimulation as well as those with inhibited sexual desire from stress and fatigue.

DOSAGE, ADMINISTRATION, and STORAGE
Form Route Storage Dosing
Intranasal Spray Intranasal 2-8oC 32 IU IN daily and 1 hour prior to sex
Capsule Oral 2-8oC 50 IU cap PO daily
Sublingual Tablet Sublingual 2-8oC 50 IU 1-2 tabs SL daily
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.

CONTRAINDICATIONS and PRECAUTIONS

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.

ADVERSE REACTIONS

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

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.

USE IN SPECIFIC POPULATIONS
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 and shown improvement in 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. 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.
  2. 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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