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Low Dose Naltrexone (LDN)

T&C Compounding are experts in the compounding of LDN

WHAT IS LOW DOSE NALTREXONE (LDN)

Naltrexone belongs to a class of drugs known as opioid agonists. Naltrexone blocks opiate drugs from binding to the opioid receptors, which can result in increased endorphin and enkephalin release. Therefore, this results in reduced: 1. signaling and release of inflammatory substances, 2. nerve cell inflammation and 3. autoimmune mediators.

Which patients may benefit from LDN therapy?

  • Chronic pain
  • Hashimoto’s
  • Parkinson’s disease
  • Arthritis
  • Graves’ disease
  • Ulcerative colitis
  • Crohn’s Disease
  • Psoriasis
  • Eczema
  • Inflammation
  • Multiple sclerosis
  • Irritable bowel
  • Celiac disease
  • Autism
  • Lupus
  • Cancer
  • HIV/Aids

Why is LDN only available as a compounded medication?

Naltrexone is commercially available only in a 50 mg tablet. However, low dose naltrexone (LDN) therapy is usually prescribed as 1.5 mg to 4.5 mg per day, adjusted to the correct dose depending on the patient’s response. Compounding pharmacies use naltrexone powder from FDA approved facilities to formulate individualized dosing based on a prescription order. Prescribers should ensure that the compounding facility they choose is an accredited compounding lab.

HOW DOES LDN WORK?

• Down regulates inflammatory cytokine release, oncogene expression and auto-immune cascades

• In the Central Nervous System (CNS) it reduces toll-like receptor signaling and glial cell activation resulting in reduced inflammatory cytokines and reduced neuro-inflammation

• In the Peripheral Nervous System (PNS) it modulates T & B lymphocyte production (example: gut inflammation), and reduces inflammatory cytokines (IL6, IL12, TNF alpha) and suppresses tumor growth factor (NF-kB)

When taken at bedtime, the short acting LDN binds to the receptors which leads to a brief blockade of opioid receptors between 2 am and 4 am. This blockade is believed to up-regulate vital elements of the immune system by causing an increase in endorphin and enkephalin production.

Examples of common compounded dosage forms

  • Capsules
  • Suspensions
  • Transdermal creams
  • Rapid dissolve tablets (RDT’s)
  • Other

Dose:

For most patients, a starting titration Rx would be:

Rx: Naltrexone 1.5 mg #63 & Naltrexone 0.5 mg, quantity #42

SIG: Take 1 (1.5 mg capsule) orally daily prior to bedtime, increasing by 0.5 mgweekly (every 7 days) until a dose between 3 mg to 4.5 mg is achieved

Once dose of 3 mg – 4.5 mg/day is achieved, next Rx can be written as:

Rx: Naltrexone __mg capsules, quantity, typically choose #30__ #60__ or #90__ Other__

SIG: Take 1 capsule daily as maintenance therapy

If a lower starting dose is desired, the Rx can be written as:

Rx: Naltrexone 0.5 mg #___ (#100-300 is suggested)

SIG: Take 1 capsule (0.5 mg) daily prior to bedtime and increase each week by 1 capsule (0.5 mg) until an effective dose is reached. (Typically a dose between 3 mg to 4.5 mg)

Once dose of 3 mg – 4.5 mg/day is achieved, next Rx can be written as:

Rx: Naltrexone __mg capsules

SIG: Take one capsule daily as maintenance therapy. (#30, #60, or #90 is typical).

Patients with Hashimoto’s and Graves’ disease: Patients should be monitored for symptoms of fast pulse, palpitations, or sudden onset of insomnia. If any of these occur, thyroid adjustment may be needed.

FAQ: Low Dose Naltrexone (LDN)

No. The effects of narcotics will be blocked by LDN. If a patient has developed any degree of narcotic dependence, LDN may cause withdrawal symptoms, some of which can be extremely uncomfortable or dangerous. Careful consideration should be given to those cases before initiating LDN. We have worked with pain management specialists that have weaned patients off of narcotic analgesics while titrating up LDN therapy. Please call to discuss this with the pharmacists.

Yes. We have seen it prescribed for patients such as those who have psoriasis or eczema (topical) or joint pain (transdermal). Only one route of administration should be used at a time. Do not combine topical and oral therapies.

Side effects of LDN are few and have not been commonly reported.

Most common side effects have been:

• VIVID dreams are common, usually only lasting a few days; if these become bothersome for the patients, the time of dose could be adjusted to the am

• Stomach cramps/diarrhea – rare

• Increased thyroid sensitivity; medication may need adjustment

• Flu-like symptoms; if longer than 24 hours, the dose may be cut in half until symptoms resolve

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