What is Low Dose Naltrexone?

Reduce pain, reverse autoimmunity, and fight cancer with...

Low Dose Naltrexone (LDN)

Low Dose Naltrexone, aka LDN, is a safe, non-toxic and inexpensive drug that is used primarily to regulate a dysfunctional immune system, reduce pain, fight inflammation, and prevent cancer. It is especially helpful for people with chronic pain, autoimmune disease, HIV/AIDS, cancer, mental health issues, and neurodegenerative diseases, as well as central nervous system disorders. Treatment is constantly evolving, with new conditions and methods of treatment being shared regularly. Our physicians at Aspen Integrative Medical Center have used it extensively in practice and can advocate for its effectiveness. If you have further questions about this medication and how it might benefit you, please contact us at Aspen Integrative Medical Center.

History of Naltrexone

Naltrexone was approved by the FDA in 1984 for the treatment of opioid addiction at daily doses of 50-300 mg. It works by completely blocking endogenous opiates (endorphins released by the brain) and exogenous opiates (recreational drugs such as heroin). As have many drugs that have been widely used for an extended period, naltrexone has been used in lower doses to treat multiple diseases since 1988. Naltrexone is considered a “standard dose” when given in daily amounts of 25 mg or more and “low dose” (aka LDN) when the daily dose is less than or equal to 10 mg. LDN is NOT a controlled medicine, narcotic or an opioid.

How does Low Dose Naltrexone work?

Naltrexone when given at a low dose has antagonistic activity on opiate receptors and toll-like receptors (TLRs). Opiate receptors are present in multiple biological systems in the human body, as they regulate a great number of biological functions via the central release of natural opiates (endorphins/met-enkephalins). Toll-like receptors (TLRs) are part of the immune system, providing a first line of defense against microbial invasion and possessing the ability to recognize and be activated by not only pathogens but also endogenous signaling molecules. LDN is able to modify biological functions of these receptor groups by suppressing unwanted immune reactions, or by stimulating disease-suppressed immune activity.

What are the health benefits of LDN?

LDN has the following health benefits:

Improves immune system response
Creates an increase in the production of endorphins, which results in a reduction of pain and an increased sense of wellbeing
Increased levels of endorphins can be expected to stimulate the immune system, promoting an increase in the number of T lymphocytes. This increase in T-cell numbers restores a more normal balance of the T-cells such that the effects of the disease process are significantly reduced.
It may also act directly on these immune cells to stimulate or restore normal function
Blocks opiate binding for a short period (4-6 hours) by binding to opiate receptors
Causes rebound increased endorphin release
Increases sensitivity of existing opiate/endorphin receptors
Acts as a pro-kinetic improving movement of stool for constipation
More opiate receptors are formed to capture endorphins

Which conditions are treated with LDN?

LDN can be broadly prescribed for a variety of conditions especially if there is pain or immune system dysfunction including autoimmunity and high levels of inflammation. A list of commonly treated conditions includes, but is not limited to:

Autoimmune diseases including Autoimmune Hepatitis, Multiple Sclerosis,
Hashimoto’s Thyroiditis, Graves Disease, and so forth
Inflammatory Bowel Disease (Crohn’s/Ulcerative Colitis)
CFS/ME
Lyme Disease
Chronic Viral Infections
Mast Cell Activation Syndrome (MCAS)
Chronic Regional Pain Syndrome
Fibromyalgia
Parkinson’s Disease
Diabetes Type I
Vitiligo
Scleroderma
Psoriasis
Anxiety and Depression
PCOS
Nerve Pain (Neuropathic conditions)
Cancer – Melanoma, Glioblastoma, Esophageal and Oral Cancers, Non-Small Cell Cancer, Breast Cancer, Multiple Myeloma, Lymphoma, Ovarian Cancer, Renal Cell Cancer, Colorectal Cancer, Duodenal and Stomach Cancer, Uterine Cancer, Hepatic Cancer
PTSD
Infertility

How does LDN fight cancer?

LDN has shown numerous benefits for cancer prevention, improving cancer treatment outcomes, and preventing recurrence of cancer. LDN is known to have the following effects on cancer:

Intermittent dosing with LDN causes increased cell death and increases cell sensitivity to chemotherapy agents.
Cells treated with LDN upregulate genes that are responsible for cell death
Tumor cells pre-treated with intermittent LDN dosing are far more likely to be killed by chemotherapy drugs
LDN seems to have a direct cytotoxic effect on cancer cells via a P13 kinase, cyclin P21 and downstream G-Protein coupled receptor routes

How do you take LDN?

For many conditions, your prescriber will usually start treatment at a low dose and increase gradually over a period of weeks until you are stable at your goal dose.

Starting dose can vary from 0.5 mg to 1.5 mg daily and is often increased up to 4.5 mg daily. You may have a lower OR higher dose goal with your prescribing clinician depending on your condition.

LDN is safe for use of any age. For children it needs to adjusted to body weight.

LDN is typically taken at bedtime, but it can be taken other times of the day and have the same effectiveness.

Your provider may instruct you to take multiple smaller doses on a daily basis for certain medical conditions, such as for mental health conditions.

Higher, standard doses may be required for poorly controlled autoimmune disease and/or TBI (Traumatic Brain Injury) patients until they are stabilized before transitioning to daily low doses of naltrexone.

Ultra-Low Dose Naltrexone (ULDN), such as 0.1 mg to start, is used for very sensitive patients (such those with Mast Cell Activation) and those with severe chronic pain conditions. The medication may be prescribed twice daily, separating it by 4-6 hours from short acting opioid medications.

For cancer prevention, patients with cancer, and secondary prevention of recurrence, the dose should get to 4.5mg, or the goal dose, although your provider may adjust as necessary. Research has shown it to have best efficacy if taken cyclically meaning 4-5 days on and 2-3 days off. In cancer patients, combining a cannabinoid (CBD) or Sativex (THC/CBD), seems to enhance the anti-tumor effect. No chemotherapy agents are currently contraindicated assuming standard tests are done, however, LDN should not be taken during treatment with immune checkpoint inhibitors (e.g. Opdivo or
Keytruda — PD1 inhibitors)

How quickly do you feel better on LDN?

While symptom improvement can be seen within 1-2 weeks after starting LDN, our physicians recommend at least 4 months of treatment especially those who are chronically ill. For pain conditions, our goal is to see improvements in 3-4 weeks.

Considering the medication’s low side effect profile and numerous health benefits, it’s common for some patients to be on LDN long-term for many years with regular re-evaluation periods. Other patients may try to get their condition under control and then wean off the medication.

Please do not discontinue the medication without discussing it with your prescriber first. Sometimes you might not believe it is helping or working, but it is. Also if the medication “isn’t working” then the dose may need to be adjusted or other therapies may need to be added to improve its efficacy (such as vitamin D and glutathione).

What other therapies amplify the effects of LDN?

While LDN has remarkable health benefits, it’s important to know the medication is most effective when a part of a more comprehensive plan for your condition. It works well with other therapies and shouldn’t be relied upon as a mono-therapy to manage your condition.

LDN works best if your vitamin D levels are optimized, so supplementing vitamin D can be important. It is also synergistic to the addition of glutathione, vitamin C, and polyphenols to your treatment plan. It also works well in conjunction with IV therapies, hyperbaric oxygen therapy, and laser therapy.

What are possible side effects of LDN?

LDN is well tolerated in most patients and the safety profile is excellent when prescribed by an experienced physician. However, care should be taken to titrate the dose up slowly to avoid side effects. Please inform your prescribing physician of any side effects, so they can advise you appropriately.

Common side effects:

Sleep disturbances (insomnia)
Vivid dreams
Mild headache
Mild agitation
Nausea/gastrointestinal effects – may be advised to switch to liquid sublingual LDN to bypass the gastrointestinal tract
Hyperthyroidism in Hashimoto’s patients

Uncommon side effects:

Flu-like symptoms (CFS/ME)
Rash
Herxheimer reactions
Dizziness
Increased fatigue or spasticity (Parkinson’s)

These side effects are usually only present in the initial phase and can be stopped by halving the dose for 2-3 days and then continuing with titration again. The half-life of LDN is about 4-6 hours. Report any side effects to your prescriber.

If LDN is used improperly in patients taking opioid medications, it can result in serious withdrawal symptoms such as sweats, chills, anxiety, nausea/vomiting, body pains, and others.

What are the contraindications to LDN?

LDN may be contraindicated if you are taking long-acting opiate medicines like codeine, tramadol, morphine, fentanyl or oxycodone. LDN is otherwise well-tolerated with all other drugs including chemotherapy agents, steroids, etc.

It is safe to add a narcotic if you are already on LDN. If you are on narcotics and want to add LDN, you can get breakthrough pain. So often ULDN is prescribed and it’s titrated up until it causes breakthrough pain.

Do not use this medicine if you are pregnant or breastfeeding without informing your doctor. Generally doses under 6 mg is safe and not contraindicated for pregnancy and lactating mothers.

Experience the health benefits of Low Dose Naltrexone yourself!

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What is Low Dose Naltrexone?

Reduce pain, reverse autoimmunity, and fight cancer with...

Low Dose Naltrexone (LDN)

History of Naltrexone

How does Low Dose Naltrexone work?

What are the health benefits of LDN?

Which conditions are treated with LDN?

How does LDN fight cancer?

How do you take LDN?

How quickly do you feel better on LDN?

What other therapies amplify the effects of LDN?

What are possible side effects of LDN?

What are the contraindications to LDN?

Experience the health benefits of Low Dose Naltrexone yourself!

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What is Low Dose Naltrexone?

Reduce pain, reverse autoimmunity, and fight cancer with...

Low Dose Naltrexone (LDN)

History of Naltrexone

How does Low Dose Naltrexone work?

What are the health benefits of LDN?

Which conditions are treated with LDN?

How does LDN fight cancer?

How do you take LDN?

How quickly do you feel better on LDN?

What other therapies amplify the effects of LDN?

What are possible side effects of LDN?

What are the contraindications to LDN?

Experience the health benefits of Low Dose Naltrexone yourself!