Low-Dose Naltrexone

Low-dose naltrexone (LDN) holds great promise for the millions of people worldwide facing a possible death sentence from virtually incurable cancers and other diseases.

In the developing world, LDN could provide the first low-cost, easy to administer, and side-effect-free therapy for HIV/AIDS. Naltrexone itself was approved by the FDA in 1984 in a 50mg dose for the purpose of helping heroin or opium addicts, by blocking the effect of such drugs. By blocking opioid receptors, naltrexone also blocks the reception of the opioid hormones that our brain and adrenal glands produce: beta-endorphin and metenkephalin. Many body tissues have receptors for these endorphins and enkephalins, including virtually every cell of the body’s immune system.

In 1985, Bernard Bihari, MD, a physician with a clinical practice in NYC, discovered the effects of a much smaller dose of naltrexone on the body’s immune system. He found that this low dose, taken at bedtime, was able to enhance a patient’s response to infection by HIV, the virus that causes AIDS.

In the mid-1990’s, Dr. Bihari found that patients in his practice with cancer (such as lymphoma or pancreatic cancer) could benefit, in some cases dramatically, from LDN. In addition, people who had autoimmune disease (such as lupus) often showed prompt control of disease activity while taking LDN.

LDN boosts the immune system, activating the body’s own natural defenses.
Up to the present time, the question of “What controls the immune system?” has not been present in the curricula of medical colleges, and the issue has not formed a part of the received wisdom of practicing physicians. Nonetheless, a body of research over the past two decades has pointed repeatedly to one’s own endorphin secretions (our internal opioids) as playing the central role in the beneficial orchestration of the immune system, and recognition of the facts is growing.

Witness these statements from a recent review article of medical progress in the November 13, 2003 issue of the prestigious New England Journal of Medicine: “Opioid-Induced Immune Modulation: …. Preclinical evidence indicates overwhelmingly that opioids alter the development, differentiation, and function of immune cells, and that both innate and adaptive systems are affected.1,2 Bone marrow progenitor cells, macrophages, natural killer cells, immature thymocytes and T cells, and B cells are all involved. The relatively recent identification of opioid-related receptors on immune cells makes it even more likely that opioids have direct effects on the immune system.3″

The brief blockade of opioid receptors between 2 a.m. and 4 a.m. that is caused by taking LDN at bedtime each night is believed to produce a prolonged up-regulation of vital elements of the immune system by causing an increase in endorphin and enkephalin production. Normal volunteers who have taken LDN in this fashion have been found to have much higher levels of beta-endorphins circulating in their blood in the following days. Animal research by I. Zagon, Ph.D., and his colleagues has shown a marked increase in metenkephalin levels as well.

Bihari says that his patients with HIV/AIDS who regularly took LDN before the availability of HAART were generally spared any deterioration of their important helper T cells (CD4+).

In human cancer, research by Zagon over many years has demonstrated inhibition of a number of different human tumors in laboratory studies by using endorphins and low dose naltrexone. It is suggested that the increased endorphin and enkephalin levels, induced by LDN, work directly on the tumors’ opioid receptors — and, perhaps, induce cancer cell death (apoptosis). In addition, it is believed that they act to increase natural killer cells and other healthy immune defenses against cancer.

In general, in people with diseases that are partially or largely triggered by a deficiency of endorphins (including cancer and autoimmune diseases), or are accelerated by a deficiency of endorphins (such as HIV/AIDS), restoration of the body’s normal production of endorphins is the major therapeutic action of LDN.

What diseases has it been useful for and how effective is it?
Bernard Bihari, MD has described beneficial effects of LDN on a variety of diseases:

Cancers: Other Diseases:
  • Breast Cancer
  • Carcinoid
  • Colon and Rectal Cancer
  • Glioblastoma
  • Liver Cancer
  • Lung Cancer (Non-Small Cell)
  • Lymphocytic Leukemia
  • Lymphoma (Hodgkin’s and
    Non-Hodgkin’s)
  • Malignant Melanoma
  • Multiple Myeloma
  • Neuroblastoma
  • Ovarian Cancer
  • Pancreatic Cancer
  • Prostate Cancer (untreated)
  • Renal Cell Carcinoma
  • Throat Cancer
  • Uterine Cancer
  • ALS (Lou Gehrig’s Disease)
  • Alzheimer’s Disease
  • Behcet’s Disease
  • Celiac Disease
  • Chronic Fatigue Syndrome
  • Crohn’s Disease
  • Emphysema (COPD)
  • Fibromyalgia
  • HIV/AIDS
  • Irritable Bowel Syndrome (IBS)
  • Multiple Sclerosis (MS)
  • Parkinson’s Disease
  • Pemphigoid
  • Primary Lateral Sclerosis (PLS)
  • Psoriasis
  • Rheumatoid Arthritis
  • Sarcoidosis
  • Systemic Lupus (SLE)
  • Ulcerative Colitis
  • Wegener’s Granulomatosis

LDN has demonstrated efficacy in hundreds of cases.

  • Cancer. As of mid-2004, Dr. Bihari reports having treated over 300 patients with cancer that had failed to respond to standard treatments. Of that group, some 50%, after four to six months treatment with LDN, began to demonstrate a halt in cancer growth and, of those, over one-third have shown objective signs of tumor shrinkage.
  • Autoimmune disease. Within the group of patients who presented with an autoimmune disease (see above list), none have failed to respond to LDN; all have experienced a halt in progression of their illness. In many patients there was a marked remission in signs and symptoms of the disease. The greatest number of patients within the autoimmune group are people with multiple sclerosis, of whom there are now some 400 in Dr. Bihari’s practice. Less than 1% of these patients has ever experienced a fresh attack of MS while they maintained their regular LDN nightly therapy.
  • HIV/AIDS. As of September 2003, Dr. Bihari has been treating 350 AIDS patients using LDN in conjunction with accepted AIDS therapies. Over the past 7 years over 85% of these patients showed no detectable levels of the HIV virus — a much higher success rate than most current AIDS treatments, and with no significant side effects. It is also worth noting that many HIV/AIDS patients under Dr. Bihari’s care have been living symptom-free for years taking only LDN with no other medications.

How is it possible that one medication can impact such a wide range of disorders?
The disorders listed above all share a particular feature: in all of them, the immune system plays a central role — and low blood levels of endorphins are generally present, playing a role in the disease-associated immune deficiencies. Research by others — on neuropeptide receptors expressed by various human tumors — has found opioid receptors in many types of cancer:

  • Brain tumors (both astrocytoma and glioblastoma)
  • Breast cancer
  • Endometrial cancer
  • Head and neck squamous cell carcinoma
  • Myeloid leukemia
  • Lung cancer (both small cell and non-small cell)
  • Neuroblastoma and others…

These findings suggest the possibility for a beneficial LDN effect in a wide variety of common cancers.

How can I obtain LDN and what will it cost?
LDN can be prescribed by the doctors at the Whole Health Center if LDN appears appropriate for you. It will be prepared by a reliable compounding pharmacy. 

Naltrexone in the large 50mg size, originally manufactured by DuPont under the brand name ReVia, is now sold by Mallinckrodt as Depade and by Barr Laboratories under the generic name naltrexone.

LDN prescriptions are now being filled by hundreds of local pharmacies, as well as by some mail-order pharmacies around the US. Some pharmacists have been grinding up the 50mg tablets of naltrexone to prepare the 4.5mg capsules of LDN; others use naltrexone, purchased as a powder, from a primary manufacturer.


Pharmacies that are good sources of LDN:

Irmat Pharmacy, New York, NY (212) 685-0500
Gideon’s Drugs, New York, NY (212) 575-6868
The Compounder Pharmacy, Aurora, IL (800) 679-4667
The Medicine Shoppe, Canandaigua, NY (800) 396-9970
Skip’s Pharmacy, Boca Raton, FL (800) 553-7429
Smith’s Pharmacy, Toronto, Canada (800) 361-6624

IMPORTANT: Make sure to specify that you do NOT want LDN in a slow-release form.

Reports have been received from patients that their pharmacies have been supplying a slow-release form of naltrexone. Pharmacies should be instructed NOT to provide LDN in an “SR” or slow-release or timed-release form. Unless the low dose of naltrexone is in an unaltered form, which permits it to reach a prompt “spike” in the blood stream, its therapeutic effects may be inhibited.

IMPORTANT: Make sure to fill your Rx at a compounding pharmacy that has a reputation for consistent reliability in the quality of the LDN it delivers.

The FDA has found a significant error rate in compounded prescriptions produced at randomly selected pharmacies. Dr. Bihari has reported seeing adverse effects from this problem. Please see our report, Reliability Problem With Compounding Pharmacies and the above list of recommended pharmacies for some suggested sources.

What is the typical dosage and frequency that is prescribed?

The usual adult dosage is 4.5mg taken once daily at night. Because of the rhythms of the body’s production of master hormones, LDN is best taken between 9pm and 3am. Most patients take it at bedtime.

People who have multiple sclerosis that has led to muscle spasms are advised to use only 3mg daily and to maintain that dosage.

Rarely, the naltrexone may need to be purchased as a solution — in distilled water — with 1mg per ml dispensed with a 5ml medicine dropper. If LDN is used in a liquid form, it is important to keep it refrigerated.

The therapeutic dosage range for LDN is from 1.75mg to 4.5mg every night. Dosages below this range are likely to have no effect at all, and dosages above this range are likely to block endorphins for too long a period of time and interfere with its effectiveness.

IMPORTANT: Make sure to specify that you do NOT want LDN in a slow-release form (see above).

Are there any side effects or cautionary warnings?

  • Side effects: LDN has virtually no side effects. Occasionally, during the first week’s use of LDN, patients may complain of some difficulty sleeping. This rarely persists after the first week. Should it do so, dosage can be reduced from 4.5mg to 3mg nightly.
  • Cautionary warnings: Because LDN blocks opioid receptors throughout the body for three or four hours, people using medicine that is an opioid agonist, i.e. narcotic medication — such as Ultram, morphine, Percocet, Duragesic patch or codeine-containing medication — should not take LDN until such medicine is completely out of one’s system. In addition, LDN should probably not be taken during pregnancy. Full-dose naltrexone (50mg) carries a cautionary warning against its use in those with liver disease. This warning was placed because of adverse liver effects that were found in experiments involving 300mg daily. The 50mg dose does not apparently produce impairment of liver function nor, of course, do the much smaller 3mg and 4.5mg doses. People who have received organ transplants and who therefore are taking immunosuppressive medication on a permanent basis are cautioned against the use of LDN because it may act to counter the effect of those medications.

*Information on this page obtained from http://www.lowdosenaltrexone.org.

This entry was posted in Patient Education Guide and tagged , . Bookmark the permalink.