What You Need To Know

Low Dose Naltrexone (LDN) has been prescribed to patient with a variety of ailments from Chronic Fatigue Syndrome (CFS), Fibromyalgia (FM), Lyme Disease, Multiple Sclerosis, Rheumatoid Arthritis, Hashimoto’s disease, Complex Regional Pain Syndrome, Crohn’s disease, to skin conditions like psoriases.

Naltrexone, at doses of 25-50mg, is an FDA approved medication that has been on the market for decades for the treatment of opioid and alcohol addiction by blocking opiate receptors. However, at significantly lower doses, (low dose naltrexone or LDN), some researchers are finding that naltrexone is very beneficial in helping patients with autoimmune/inflammatory diseases.

How Does LDN work?

The exact mechanism of action of LDN is unknown, but a few theories exist. Researchers believe that LDN works as a neural anti-inflammatory agent in the central and peripheral nervous systems. Other research suggests that LDN may help re-balance and normalize the immune system, which may be why it appears to help people with autoimmune and other immune-system illnesses.

It is well known that our immune system declines with age.  Over the past few decades, research has pointed repeatedly to our own endorphin secretions (our internal opioids) as playing a central role in maintaining a healthy balance in our immune system. LDN is theorized to restore the Th1/Th2 balance of the immune system. Th1 cells promote cell-mediated immunity, while Th2 cells induce humoral immunity. The inability to respond adequately with a Th1 response can result in chronic infections and cancer, while an overactive Th2 response can contribute to allergies and various syndromes (e.g. CFS, FM, RA, and others) and play a role in the development and progression of autoimmune disorders. Restoration of the body’s normal production of endorphins and correcting an overactive Th2 component is believed to be the major therapeutic action of LDN.

Endorphins

A majority (90%) of the body’s endorphin production occurs at night. Peak production of endorphins occurs between the hours of 2am and 4am. Taking low-dose naltrexone at bedtime, in a dosage range of 1.5 – 6mg, causes a significant increase in natural endorphin production. When a tiny dose of naltrexone is taken at bedtime, the body attempts to overcome the temporary opioid block by significantly increasing production of natural endorphins. The generally recommended dosage range for LDN is from 0.5 mg to 6 mg. Dosages below this range are likely to have no effect at all, and dosages above this range are likely to block endorphins for an exaggerated period of time and interfere with its effectiveness. At higher doses naltrexone can cause insomnia, nausea, vomiting, anxiety, headache, abdominal pain, muscle aches, rash, dizziness, fatigue, loss of appetite, constipation, and liver problems. However, at low dosages we see less side effects or toxicities reported by our patients. In our experience with hundreds of patients, an occasional case of insomnia or early awakening, vivid dreaming, or mild GI upset are the only reported adverse effects. These side effects can be minimized by either taking LDN earlier in the evening, and/or taking it with a small snack. We also recommend starting out with a low dose (0.5- 1.5mg) and gradually increasing the dose, over a few weeks, until the desired target dose has been reached. When taken for several months, the increase in natural endorphin levels may significantly impact overall health and wellness. To thoroughly evaluate the effectiveness of LDN, we recommend that you take it for a minimum of six months. Keep a journal of your health symptoms to see if you notice any improvement. If the improvement is noticeable, continue taking it. Your prescriber can determine if/when to stop taking LDN.

Special Note regarding Hashimoto’s disease and patients currently taking thyroid replacement.

Hashimoto’s thyroiditis is the most common cause of hypothyroidism in the United States. Over time, the antibodies produced by this disease lead to an underactive thyroid gland. Most patients with Hashimoto’s disease must take thyroid replacement hormone to supplement their own diminished production. When these patients start taking LDN, and respond favorably, their own natural production of thyroid starts to return. Without making downward adjustments to their replacement dose, they can actually get to a point where they become hyperthyroid (too much thyroid). Symptoms of hyperthyroid include: Heart palpitations, nervousness, anxiousness, panic attacks, difficulty sleeping, sweating, and hunger. Any patient taking thyroid replacement should have their thyroid levels closely monitored when starting on LDN.

Apothecary Options prepares lactose- and gluten-free immediate release naltrexone capsules in a variety of common strengths from 0.5mg to 4.5mg and custom dosages are always available. The recommended dosage is usually one capsule taken at bedtime. If sleep disturbances occur, we recommend taking it earlier in the day, and then gradually taking it later in the evening. There are some patients who simply cannot tolerate the sleep disruption and find that they still get good results by taking LDN in the morning. Our capsules are .

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