Welcome to a new class of medicines: Glial cell modulators used in the management of chronic pain disorders. There is evidence that low dose naltrexone may operate as a novel anti-inflammatory agent in the central nervous system, via action on microglial cells which in turn can help modulate chronic pain. Recall that conventional anti-inflammatories have poor blood brain-barrier permeability.
The brief blockade of opioid receptors between 2 AM and 4 AM 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 encephalin production.
The benefit of low dose naltrexone is entirely independent of its better-known activity on opioid receptors.
Originally put on the market as Narcan (naloxone) this drug was a competitive opioid receptor antagonist. Narcan was used to displace opioids on board when a baby was born to a heroin addicted mom. Revia (naltrexone) is structurally and functionally similar but has greater oral bioavailability and a longer half-life than Narcan. It was marketed in 1984 for the management of alcohol dependence and opioid dependence. If you were trying to kick your addiction to opioids Revia would bind the receptor and block the euphoric high of the opioid. But like Antabuse…. The patient had to be motivated to take a pill daily. The typical dose was 50 to 100mg a day.
Low dose naltrexone is made in a compounding pharmacy at approximately 1/10 th the dose.
It may seem strange that a medication can have an opposite effect when given at a low dosage. Research suggests that there is a small window at which opioid analgesics produce the opposite effects than those typically expected.
Want to read more? The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain Clin Rheumatol (2014) J. Younger Stanford University.
According to the article above these are conditions in which LDN caused a reduction in the severity of symptoms:
Fibromyalgia: musculoskeletal pain/profound fatigue/cognitive disruption/insomnia
Crohn’s disease: 80% of one study exhibited significant improvement
Multiple sclerosis
Complex regional pain syndrome
Advantages of Low Dose Naltrexone:
1) Low cost: It is inexpensive. Cost to patient is about $45.00/month
2) Low side effects: It is well tolerated. None of the side effects we see the NSAIs. However 37% report vivid dreams. Vivid dreams develop with the first dose but decrease over time.
Frequency of headaches was slightly higher than placebo. Studies showed no development of dependence or tolerance. Cessation is followed by a slow return of symptoms to baseline levels.
Dosing Pearl: Typical dose is 4.5mg given approximately an hour before bedtime. Some individuals reporting insomnia as a side effect are moved to a morning dosing. Some doctors ease a patient into therapy and prevent sleep disturbances by dosing 1.25mg HS for 6 weeks, then 3.0mg HS for 6 weeks then 4.5mg QD.
You must take the drug for 2 months to obtain an estimate of its efficacy.
Can you give this to a patient taking an opioid analgesic? It is possible that even a low dose of naltrexone could cause a sufficient blockade or opioid receptors and reduce their effectiveness? Most studies omit individuals taking opioid analgesics.
Count on 4 days to wash out of the receptor should you need narcotics. You need a 10 day washout for surgery.
Functional Medicine doctors prefer the patient be gluten free and on a diet to prevent “leaky gut”.
Measure your patient’s immune activity by collecting an ESR or C-reactive protein before you initiate treatment and use that to monitor your outcome.
Interesting ……….Other glial cell modulators in clinical trials include minocycline, dextromethorphan, stinging nettle, & curcumin. Contrave, latest diet pill has bupropion 90mg and naltrexone 8mg
Want to know more? Read more at this website: www.lowdosenaltrexone.org Questions??
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