Couple of months ago Clara came to see me for abdominal pains along with nausea and diarrhea. She told me that she had been suffering from irregular periods and hirsutism since she was 15 years old. She had been on birth control for several years as her doctor had given her diagnosis of PCOS but just a year ago she started to work with a naturopath and she was put on LDN (low dose of naltrexone).

She didn’t find much difference in her hirsutism but her periods were not that irregular, they were somewhat regular. Although she was having a kind of regular cycle but she had been fighting with abdominal pain, nausea, and diarrhea since the day she had started taking LDN. It wasn’t any different than other conventional drug, in order to bring some relief in one condition, creating havoc on other. I had to detox the LDN along with other homeopathic remedies to bring back the balance of gut flora of Clara.

Now let us have a look at connection between PCOS and efficacy of LDN

PCOS is a hormonal disorder. Symptoms of PCOS can vary based on the woman and her individualized hormonal imbalances. Women can experience various symptoms like weight gain or obesity, Menstrual irregularities, absent or heavy periods, acne, hirsutism or hair loss, recurrent miscarriage or infertility. Conventional medicine offers various treatment to treat these symptoms. Although not recommended by conventional medicine, multiple studies have shown the positive effect of LDN (low dose of naltrexone) for treating few symptoms related to PCOS like premenstrual syndrome (PMS) and endometriosis.

What is Naltrexone?

Naltrexone is a licenced medication originally used to block the effects of drugs known as opiates, or narcotics like morphine, heroin, or codeine. Now it has also been approved by the U.S. Food and Drug Administration (FDA) as a treatment for alcohol dependency.  

LDN is usually taken at night before bed. During sleep, it begins blocking opioid receptors as well as receptors of endorphins. Endorphins are opiate-like chemicals best known as the “feel good” substances the body makes after exercise. The word endorphin actually comes from 2 words: endogenous (made within the body) and morphine. Endorphins are known to block pain, are very involved with immune function and rapid cell reproduction, particularly an endorphin called Opioid Growth Factor (OGF) or Met-Enkephalin. When these receptors are blocked for a short period, the body responds by creating more receptors, increasing their sensitivity and thus making more endorphins.

Once the LDN wares off, a “rebound effect” is experienced in which the amount of available OGF and its utilization is greatly enhanced having a very positive effect on immunity. It is believed, LDN can work for many different conditions, all of which are affected by immune function and tend to lead to lower levels of endorphin release.

While Naltrexone is still primarily used to treat alcohol and drug addiction, recent research has shown Naltrexone in low doses might also help in few symptoms related to PCOS.

Side effects of LDN

LDN doesn’t come free of any adverse side effects. Many people who are using LDN has complained of abdominal pain, nausea, vomiting, anorexia, diarrhea, headaches, chest and muscle pains. Naltrexone should not be given to patients using opioids chronically, as well as those who have hepatitis or hepatic failure. Since Naltrexone is excreted primarily in the urine, using the drug should be avoided if the patient has a history or is afflicted with renal impairment.

Naltrexone should be administered with caution in the presence of concomitant use of drugs such as acetaminophen and disulfiram, as these drugs are associated with potential liver toxicity. It is listed as a pregnancy category C medication, or a medication that show adverse effects on the fetus.

PCOS and opioids

Let us try to understand relationship between PCOS, Opioids and opioids blocker drug.

Multiple studies have indicated Naltrexone has PCOS benefits. More than PCOS, Naltrexone has been found to treat premenstrual syndrome (PMS) and endometriosis. Other studies suggest its potential benefits for “tail end brown bleeding,” anxiety, sleep disturbance, and low mood.

According to a University of Illinois study, women with PCOS are more likely to have dysregulation of the opioid system both in the brain and elsewhere in the body, with complex interactions.

Opioids are substances in our brain that help regulate pain and pleasure. They also interact with sex hormones. Opioids in other areas of your body help to regulate function of your pancreas and liver, as well as glucose metabolism and insulin resistance, two internal processes critical to women with PCOS. Naltrexone when blocks the opiates you can get the part of the brain known as the hypothalamus to start working better, then the pituitary gland starts to work better, and as a result the ovaries start to work better.

Recent Studies

A recent study, “Medical management of metabolic dysfunction in PCOS” showed that naltrexone administration can reduce the LH response to GnRH in hyperinsulinemic women but fails to be effective in normoinsulinemic subjects.

“Villa and associates found that naltrexone use led to decreased insulin area under the curve only in hyperinsulinemic and not in normoinsulinemic women [41]. However, in contrast, recent trials evaluating hyperinsulinemic women with PCOS failed to detect an improvement of either fasting or glucose-induced insulin levels [45]. Some, but not all studies demonstrated a naltrexone-related reduction of BMI [41,43,44]. To date, there is no evidence that naltrexone has a significant effect on lipid profile, systemic inflammation or endothelial function in women with PCOS.”

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3409585/

In another study, “Naltrexone treatment in clomiphene resistant women with polycystic ovary syndrome” naltrexone monotherapy partly restored the menstrual cyclicity, and further improvement was observed during combined naltrexone + CC treatment indicating a restoration of CC sensitivity in these patients.

https://www.ncbi.nlm.nih.gov/pubmed/18641399

Researchers simply don’t yet know why LDN doesn’t work for 20 to 40 percent of users, or why it improves pain and fatigue in some users, but not others. The answer could be that LDN only works in combination with other factors such as lifestyle and diet, and an additional regime of pharmaceutical medications might also be needed. Some users also reported unpleasant side effects, including more pain, insomnia, anxiety, and flare-ups of their disease.