by Sebastian Denison, RPh, FAARM (candidate), PCCA Clinical Compounding Pharmacist

Many think of February as a month devoted to romance—specifically, Valentine’s Day. But February is also recognized as heart health month, which perfectly aligns with gifts from the heart. The last time I wrote about the relationship between heart health and romance was back in 2016. Since then, a few things changed, including new ideas for compounding.

Although my wife remains impressed by my romantic gestures, I believe a good night’s sleep is by far the best heart health and Valentine’s Day gift possible. A good night’s sleep is imperative for the removal of waste products from the central nervous system (CNS), providing repair of muscle and connective tissues and ensuring healthy brain function.

Many patients with sleep disturbances are commonly prescribed sleep aids, but those medicines may cause side-effects such as neurotransmitter imbalances, cognitive impairment and dependence.

Alternative Sleep Aids

Melatonin, perhaps the most overlooked option, is one way to avoid the side-effects of traditional drugs. Starting patients at 3 mg of melatonin at bedtime and titrating up for adequate sleep induction and duration can help patients obtain beneficial sleep.¹ Melatonin production is influenced by a number of factors, including light exposure from electronic devices (think electronic tablets and smart phones) near bedtime. If your patients complain about waking up in the middle of the night and are unable to fall back to sleep, consider recommending a sustained-release melatonin supplement.

Combining melatonin with theanine is a great compounding option for patients experiencing sleep disruptions. Research shows 100-200 mg of theanine at bedtime helps decrease alpha waves, allowing patients to slow their racing thoughts and fall asleep. Theanine regulates the production of most neurotransmitters and serotonin. Patients will fall asleep faster and may notice an overall improved mood.²

You may also consider advising patients to take 600 mg of magnesium glycinate at bedtime. Studies indicate magnesium helps improve sleep, as well as offers powerful anti-inflammatory properties that regulate calcium. In fact, many patients who are magnesium deficient also suffer from heart palpitations; these patients would benefit from including magnesium glycinate as a dietary supplement.³

I also recommend PCCA Formula #13535 to member pharmacies whose patients use naltrexone hydrochloride (NHL) to combat sleep disorders, as it combines three of my favorite anti-inflammatory molecules while helping to ensure a good night’s rest!⁴

Remember to check the Wellness Works catalog for nutritional supplements that offer the best balance for your patients. If you are in need of a specific formulation currently not available, reach out to Wellness Works Manager Stephanie Allen (sallen@wellnessworks.com) for a customized option designed by you for your patients!

Additional Benefits of Good Sleep

Sleep also benefits other aspects of a patient’s life, including heart function and brain fog. It also improves libido!

Treatments for low libido are available in numerous forms. For example, one case study showed a dose of 20 IU of oxytocin daily improved male sexual arousal. The study also indicates a higher dose, with a prn used 15-20 minutes prior to sexual activity, offers improved responses.⁵ If you look further into the relationship between oxytocin and libido, you can recognize it’s equally important for men and women — as evidenced in clinical practices.⁶ Although not recommended for oral administration (oxytocin is degraded in the gut), other administration routes are available; for example, delivered as a nasal spray or as a sublingual troche (see PCCA Formula #12238).

Many women with the onset of menopause experience changes in libido that are too numerous to address in a single blog post. I strongly suggest attending a PCCA HRT Education event to learn about the integral relationship between hormones imbalances and sexual dysfunction. Hormone imbalances can also lead to hypertension, dyslipidemia and insulin resistance in women, all of which impact heart health.

Women also experience separate sexual dysfunction issues such as vulvodynia or vaginal dryness. For many women, standard treatments are unavailable; if they have been offered, success is limited. Fortunately, compounding options exist. Options begin with PCCA formulas: To increase a vaginal tissue sexual flushing response, start with PCCA Formula #13886 or PCCA Formula # 10879. Use of vasodilators will enhance the normal neuronal input and increase blood flow or flushing response, heightening sexual arousal and enjoyment.

Conversely for patients with vulvodynia, baclofen has a distinct effect on muscle relaxation and neuropathic response. Amitriptyline and gabapentin may also help decrease neuropathic pain and provide an exceptional response in patients. PCCA Formulas #6991, #10983 and #10984 are good starting points. You also have the option to combine baclofen, amitriptyline and gabapentin into a single vehicle base.

It is also common to include lidocaine or tetracaine for profound patient outcomes. As with any neuropathic pain, understanding dosing considerations should be explored before making recommendations to the prescribing physician.

I can go only so far before suggesting adding naltrexone to the mix. Remember, the driver for many pain patients is an uncontrolled inflammatory condition, so the use of topical naltrexone in combination with some of these other agents may benefit patients.⁷ Refer to PCCA Formula #12506 as an example. Clinically, before you dispense these medications, offer a sample of the base you want to use to ensure no patient sensitivities. Many of these patients have heightened immune and inflammatory response, leading to a heightened sensitivity to preservatives or other excipients in the base used.

One of the best base options is a MucoLox™/VersaBase® Gel 50:50 combination. The combination provides excellent mucoadhesive properties, as well as acts as a moisturizer, has an absent or very low immune sensitivity response, and finally, is a unique compounded option that cannot be duplicated.

I also recommend using water-soluble salts for these types of compounded medications, as non-soluble drugs can irritate the mucosal tissue and exacerbate the pain the patient is already experiencing. Also look at some of PCCA’s lubrication formulas (PCCA Formulas #0341, #4352, #4890, #8988 or #9953) for female patients who note dryness as a major complaint. MucoLox as a standalone or with aloe vera has been an excellent starting point for vaginal dryness.

Another addition to the base world since 2016 is Ellage® Anhydrous Vaginal — the only anhydrous-mucoadhesive vaginal base currently found in the compounding world. In addition to its mucoadhesive properties and elegant texture, Ellage offers an extended beyond-use date (BUD). Look at PCCA Formula #13862 or PCCA Formula #13934 to view one of many formulations we have developed for Ellage.

Men with hormone imbalances also suffer from low libido. A common complaint is erectile disfunction (ED), which frequently causes a request for prescription drugs. Prior to dispensing, pharmacies should ensure that the patient has had an appropriate cardiovascular (CV) workup. ⁸ What definitely changed since 2016 is the status of a few of these ED drugs: tadalafil and sildenafil changed patent status and are now available in bulk powder form.^{9, 10} The change allowed us to develop new formulations, including rapid dissolve tablets (RDTs) (PCCA Formula #13255) and sublingual suspensions (PCCA Formulas #13267, #13267 and #13267), as well as formulations developed as topical combinations for women!

Knowing February is heart health month, remember every patient who walks into your pharmacy has a heart (robots don’t exist…yet), so consider their heart health, too. Supplements such as magnesium, vitamin D, CoQ-10, omega-3s and others with anti-inflammatory properties are the cornerstone of meeting deficiencies in diets. Speak with the team at Wellness Works for information on any of these or other supplements. And remind your patients to get sleeping, get moving and the romance they seek will be right around the corner.

PCCA members with Clinical Services may also reach out to our Clinical Services team for additional help and guidance on formulas and compounding for patients.

References

1. Reiter R.J., Calvo J.R., Karbownik M., Qi W., Tan D.X. (2000) Melatonin and its relation to the immune system and inflammation. Ann N Y Acad Sci.; 917:376-86. DOI: 10.1111/j.1749-6632.2000.tb05402.x. Accessed January 2016 at https://pubmed.ncbi.nlm.nih.gov/11268363/

2. Kim, S., Jo, K., Hong, K. B., Han, S. H., & Suh, H. J. (2019). GABA and l-theanine mixture decreases sleep latency and improves NREM sleep. Pharm Biol. 2019;57(1):65-73. DOI:10.1080/13880209.2018.1557698. Accessed January 2023 at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6366437/

3. DiNicolantonio, J. J., Liu, J., & O'Keefe, J. H. (2018). Magnesium for the prevention and treatment of cardiovascular disease. Open heart, 5(2), e000775. Accessed January 2023 at https://doi.org/10.1136/openhrt-2018-000775

4. Yuan L., Liu S., Bai X., Gao Y., Liu G., Wang X., Liu D., Li T., Hao A., Wang Z. (2016 Apr 13) Oxytocin inhibits lipopolysaccharide-induced inflammation in microglial cells and attenuates microglial activation in lipopolysaccharide-treated mice. J Neuroinflammation. 13(1):77. DOI: 10.1186/s12974-016-0541-7. Accessed January 2016 at https://pubmed.ncbi.nlm.nih.gov/27075756/

5. Kou, J., Lan, C., Zhang, Y., et al., (Revised 10 January, 2021) In the nose or on the tongue? Contrasting motivational effects of oral and intranasal oxytocin on arousal and reward during social processing. Transl Psych 11, 94. Accessed February 2023 at https://www.nature.com/articles/s41398-021-01241-w#citeas

6. MacDonald, K., Feifel, D. (2012). Dramatic improvement in sexual function induced by intranasal oxytocin. J Sex Med, 9(5), 1407–1410. Accessed January 2016 at https://doi.org/10.1111/j.1743-6109.2012.02703.x

7. Younger J., Parkitny L., McLain D. (2014 April; Epub 2014 Feb 15) The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain. Clin Rheumatol. 33(4):451-9. DOI: 10.1007/s10067-014-2517-2. Accessed January 2016 at https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3962576/

8. Jackson G. (2013 September, Epub 2013 May 3) Erectile dysfunction and cardiovascular disease. Arab J Urol;11(3):212-6. DOI: 10.1016/j.aju.2013.03.003. Accessed January 2016 at https://europepmc.org/article/med/10695101

9. Sommer, F., Klotz, T., Engelmann, U. (2007). Improved spontaneous erectile function in men with mild-to-moderate arteriogenic erectile dysfunction treated with a nightly dose of sildenafil for one year: a randomized trial. Asian J Androl. 9(1):134-141. DOI:10.1111/j.1745-7262.2007.00233.x Accessed January 2016 at https://pubmed.ncbi.nlm.nih.gov/17187165/

10. Mulhall, J. P., Bukofzer, S., Edmonds, A. L., George, M., and Apomorphine SL Study Group (2001). An open-label, uncontrolled dose-optimization study of sublingual apomorphine in erectile dysfunction. Clin Ther, 23(8), 1260–1271. DOI:10.1016/s0149-2918(01)80105-3. Accessed January 2016 at https://pubmed.ncbi.nlm.nih.gov/11558862/