The statements below have not been evaluated by the FDA.
Naltrexone was first synthesized in 1963 and was initially developed to treat addiction to opioids and was approved by the U.S. Food and Drug Administration (FDA) for the treatment of addiction to drugs such as heroin, morphine, and oxycodone in 1984 as a 50mg dose.
In 1985, Bernard Bihari, MD, a physician with a clinical practice in New York City, discovered the effects of a much lower dose of naltrexone-1.5mg-5mg. 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 Low Dose Naltrexone (LDN). In addition, people who had an autoimmune disease (such as lupus) often showed prompt control of disease activity while taking LDN.
Naltrexone or Naltrexone HCL is available in 50 mg doses – however, low-dose naltrexone (LDN) usually comes in 4.5 mg or lower. Pharmacists compound naltrexone powder depending on the prescription.
LDN comes in tablets, capsules, troches or lozenges, transdermal creams, oral liquids, and more.
Today, when we discuss low dose naltrexone we mean doses that are a 10th or less of the standard dose of Naltrexone. Most of the research studies have used 4.5mg per day. Doses range from 0.001mg – 16mg in clinical practice.
As the off-label use of LDN has gained popularity, it has been widely accepted as an alternative medicine option and is used to treat various medical conditions. These off-label conditions include:
Eastern States Compounding works closely with you, whether you’re a patient looking for more effective medication, or a provider looking for the best solutions for your patients.
Common: Sleep disturbances, Mild headache, Mild agitation, Nausea/GI effects , Hyperthyroidism in Hashimoto’s patients
Uncommon: Flu-like symptoms, Rash, Herxheimer reactions (elevated temperature), Dizziness, Increased fatigue or spasticity (Parkinson’s)
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 (tramadol), morphine, Percocet, Duragesic patch or codeine-containing medication – should not take LDN until such medicine is completely out of one’s system. Patients who have become dependent on daily use of narcotic-containing pain medication may require 10 days to 2 weeks of slowly weaning off of such drugs entirely (while first substituting full doses of non-narcotic pain medications) before being able to begin LDN safely.
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See latest articles about Low Dose Naltrexone and Pain Management
The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain
Jarred Younger & Luke Parkitny & David McLain
Low-dose naltrexone (LDN) has been demonstrated to reduce symptom severity in conditions such as fibromyalgia, Crohn’s disease, multiple sclerosis, and complex regional pain syndrome. We review the evidence that LDN may operate as a novel anti-inflammatory agent in the central nervous system, via action on microglial cells. These effects may be unique to low dosages of naltrexone and appear to be entirely independent from naltrexone’s better-known activity on opioid receptors. As a daily oral therapy, LDN is inexpensive and well-tolerated.
Low-Dose Naltrexone (LDN)—Review of Therapeutic Utilization
Karlo Toljan and Bruce Vrooman
Naltrexone and naloxone are classical opioid antagonists. In substantially lower than standard doses, they exert different pharmacodynamics. Low-dose naltrexone (LDN), considered in a daily dose of 1 to 5 mg, has been shown to reduce glial inflammatory response by modulating Toll-like receptor 4 signaling in addition to systemically upregulating endogenous opioid signaling by transient opioid-receptor blockade. Clinical reports of LDN have demonstrated possible benefits in diseases such as fibromyalgia, Crohn’s disease, multiple sclerosis, complex-regional pain syndrome, Hailey-Hailey disease, and cancer.