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Low-Dose Naltrexone (LDN) Flex-Dose Tablet
Low-Dose Naltrexone (LDN) briefly blocks opioid receptors, leading to a rebound increase in the body’s natural endorphins. This effect helps modulate the immune system, target inflammation, relieve pain in various chronic and autoimmune conditions, and help with appetite control.
Naltrexone HCl
Compounded LDN tablets are intended for oral use as prescribed by your provider to support your specific health goals whether that is immune modulation, pain management, weight support, or another targeted benefit. LDN is available from Strive in the following compounded flex-dose tablet strengths: 0.4 mg, 1.5 mg, 3 mg, 4.5 mg, and 8 mg.
Autoimmune and Inflammation-related conditions
- Suggested dosing is titrating up to 4.5mg (or lowest beneficial dose) at bedtime
Weight management and food cravings
- Suggested dose is 8mg at bedtime, can increase to 8mg twice daily if needed
Suggested Directions:
- Take 1 tablet by mouth at bedtime. or as directed by your healthcare provider.
- Most patients can start LDN at 1.125 mg dose which is 1/4 of the 4.5 mg flex-dose tablet and slowly work up by adding 1/4 tablet each week until taking 1 full tablet.
- Not all patients need a 4.5mg dose to experience the beneficial effects, and some patients may need higher than the standard 4.5 mg dose.
- Patients with medication sensitivities may benefit from starting with 1/4 of a 1.5 mg tablet or lower dose.
Other custom strengths are available in capsule form.
IMPORTANT INFORMATION ABOUT COMPOUNDED MEDICATIONS
This medication has been compounded (custom-prepared) by a pharmacy. Compounded medications are specially prepared for individual patient needs based on a valid prescription from a prescribing healthcare practitioner and, as such, are not reviewed or approved by the U.S. Food and Drug Administration (FDA) for safety or efficacy. Compounded drugs are intended for patients whose prescriber has determined their medical needs are not met by an available FDA-approved drug. These statements have not been evaluated by the FDA.
This compounded preparation:
- Has not been approved by the FDA
- Has not undergone FDA review for safety, effectiveness, or quality
- Is prepared specifically for you based on your prescriber's order
- Individual outcomes may vary
Dosing is determined by the prescribing provider based on patient-specific factors. Always follow your healthcare provider's instructions. Compounded medications are not subject to FDA approval and lack the same safety and efficacy data as FDA-approved commercial medications. This medication should be prescribed and monitored by a licensed healthcare professional familiar with the condition being addressed and the specific applications of the medication.
This compounded medication is only available when the commercially available product is unavailable or when a prescriber determines that there is a clinically significant difference for the patient.
Medicine Information
- Autoimmune & Inflammatory Conditions: Some peer-reviewed literature has explored naltrexone at low doses in the context of MS, Crohn's, rheumatoid arthritis, and lupus, with preliminary research examining potential effects on immune activity and limit the immune system's tendency to attack the body's own tissues ¹,²
- Chronic Pain Research Area: Early-stage literature has examined low-dose naltrexone in the context of fibromyalgia, chronic widespread pain, and complex regional pain concerns by calming brain pain-signaling cells (microglia) and promoting the body's endogenous endorphin production 3,4
- Weight Management Support: at the 8 mg dose, may support weight goals by influencing appetite regulation and managing food cravings through the brain's reward pathways 5,6
- Mood & Mental Health: early research suggests healthy mood related outcomes, particularly in patients where inflammation may be contributing to mental health symptoms⁷
- Fatigue Concerns: explored as a potential support for ME/CFS and long COVID, with some patients reporting healthy changes in energy levels⁸
- Gut Health & IBD Support: a meaningful body of research in Crohn's and ulcerative colitis shows healthy changes in gut health and improvements in quality of life, including in pediatric populations⁹
- Nervous System Balance: preliminary research has examined a possible protective support for brain and nerve tissue, with ongoing clinical interest in factors relating to long-term neurological health¹⁰
Potential Side Effects
LDN has a well-established tolerability profile when used as directed. Because it is active at such small amounts, potential side effects tend to be mild and transient. Here is what to keep in mind:
- Common (usually temporary): Vivid or unusual dreams, mild sleep disruption, nausea (especially at initiation). These often resolve within the first 2–4 weeks.
Warnings & Precautions
- Pregnancy & breastfeeding: Consult your provider. Safety data in these populations is limited.
Drug interactions
- Do not use LDN with opioid medications, opioid-containing cough suppressants, or medications that contain opioids of any kind — LDN will block their effects and can precipitate withdrawal in opioid-dependent individuals.
- If you are on immunosuppressant therapy, discuss LDN with your prescriber, as the two may interact.
- Some patients on thyroid medication notice their thyroid levels change as LDN supports immune function. Regular monitoring with your provider is recommended.
Handling Requirements
- Keep away from children and pets
This is not a comprehensive list of all possible interactions or considerations. Always share your complete medication list with your Strive pharmacist or your prescribing provider.
LDN works by giving your body's own healing systems a brief, strategic nudge. At low doses, it temporarily blocks opioid receptors for a few hours, typically overnight, causing the brain to compensate by producing a surge of its own endogenous endorphins and enkephalins. This rebound effect sustains potentially higher-than-normal endorphin activity through much of the next day, supporting pain relief and emotional well-being. LDN also quiets overactive immune cells in the brain and spinal cord (called microglia) that drive inflammatory responses in conditions related to immune system and persistent pain — think of it as finally silencing a car alarm that's been going off for months.
LDN also influences the Opioid Growth Factor (OGF) pathway — a system that helps regulate cell growth and immune function. By briefly blocking the OGF receptor, LDN appears to upregulate this entire pathway, supporting immune surveillance and, in some cases, limiting progression of inflammatory or immune-mediated concerns. At the 8 mg dose, this same mechanism may also help regulate hunger signals and reward-based eating behaviors contributing to the weight management efforts seen at this strength.
IMPORTANT INFORMATION ABOUT COMPOUNDED MEDICATIONS
This medication has been compounded (custom-prepared) by a pharmacy. Compounded medications are specially prepared for individual patient needs based on a valid prescription from a prescribing healthcare practitioner and, as such, are not reviewed or approved by the U.S. Food and Drug Administration (FDA) for safety or efficacy. Compounded drugs are intended for patients whose prescriber has determined their medical needs are not met by an available FDA-approved drug. These statements have not been evaluated by the FDA.
This compounded preparation:
- Has not been approved by the FDA
- Has not undergone FDA review for safety, effectiveness, or quality
- Is prepared specifically for you based on your prescriber's order
- Individual outcomes may vary
Dosing is determined by the prescribing provider based on patient-specific factors. Always follow your healthcare provider's instructions. Compounded medications are not subject to FDA approval and lack the same safety and efficacy data as FDA-approved commercial medications. This medication should be prescribed and monitored by a licensed healthcare professional familiar with the condition being addressed and the specific applications of the medication.
Compounded medications are specially prepared for individual patient needs based on a valid prescription and, as such, are not reviewed or approved by the U.S. Food and Drug Administration (FDA) for safety or efficacy. These statements have not been evaluated by the FDA.
IMPORTANT INFORMATION ABOUT COMPOUNDED MEDICATIONS
This medication has been compounded (custom-prepared) by a pharmacy.
This compounded preparation:
- Has not been approved by the FDA
- Has not undergone FDA review for safety, effectiveness, or quality
- Is prepared specifically for you based on your prescriber's order
- Individual outcomes may vary
Dosing is determined by the prescribing provider based on patient-specific factors. Always follow your healthcare provider's instructions. Compounded medications are not subject to FDA approval and lack the same safety and efficacy data as FDA-approved commercial medications. This medication should be prescribed and monitored by a licensed healthcare professional familiar with the condition being addressed and the specific applications of the medication.
1. Younger J, Parkitny L, McLain D. The use of low-dose naltrexone (LDN) as a novel anti-inflammatory treatment for chronic pain. Clin Rheumatol. 2014;33(4):451–459.
2. Cree BA, et al. Low-dose naltrexone for primary progressive multiple sclerosis: a placebo-controlled, double-blind, randomized controlled trial. Mult Scler. 2010;16(9):1077–1083.
3. Younger J, Noor N, McCue R, Mackey S. Low-dose naltrexone for the treatment of fibromyalgia: findings of a small, randomized, double-blind, placebo-controlled, counterbalanced, crossover trial assessing daily pain levels. Arthritis Rheum. 2013;65(2):529–538.
4. Chopra P, Cooper MS. Treatment of complex regional pain syndrome (CRPS) using low dose naltrexone (LDN). J Neuroimmune Pharmacol. 2013;8(3):470–476.
5. Naltrexone/bupropion (Contrave) for obesity. Drug Ther Bull. 2016;54(1):9–12. [Reference for naltrexone's role in appetite/reward pathways at higher LDN doses]
6. Greenway FL, et al. Effect of naltrexone plus bupropion on weight loss in overweight and obese adults. Lancet. 2010;376(9741):595–605.
7. Mischoulon D, et al. A double-blind, randomized, placebo-controlled clinical trial of naltrexone as an antidepressant — preliminary findings. Psychopharmacology. 2022;239(2):485–497.
8. Polo O, et al. Low-dose naltrexone in ME/CFS and long COVID — emerging evidence. Front Neurol. 2022;13:1–8.
9. Smith JP, et al. Pilot study of low dose naltrexone therapy in Crohn's disease. Dig Dis Sci. 2011;56(8):2499–2506.
10. Bhardwaj P, et al. Low-dose naltrexone as a modulator of microglial activation: potential neuroprotective implications. Neuropharmacology. 2018;143:88–97.
Q. How do Flex-Dose Tablets work?
A. The LDN flex-dose tablet is designed for easy and precise dosing:
- The tablet is scored into quarters (1⁄4). It does not require a pill cutter. Place the tablet on a solid surface and firmly press down on the middle of the tablet, scored side up, and it will easily break into quarters.
Q. What are the ingredients in LDN Flex-Dose Tablets?
A. Active ingredient: naltrexone
- Prebiotic filler
- That’s it! They are suitable for vegetarians and vegans. The tablets do not contain common allergenic ingredients like lactose, magnesium stearate, artificial colors, or preservatives.
Q. What are the potential advantages of Flex-Dose Tablets over capsules?
A. Flex-dose tablets let patients easily titrate their dose using a single prescription, rather than requiring multiple prescriptions for different strengths. This may offer prescribers a streamlined prescribing pathway and patients a more convenient titration option.
Q. What do you advise in case of a missed dose?
A. There is no need to make up a missed dose of LDN.
Q. Should LDN be cycled?
A. There is no need to cycle LDN. LDN has a short half-life of 4 to 6 hours so taking it once a day creates a substantial drug-free interval each day.
Q. May LDN be stopped abruptly?
A. There is no harm in stopping LDN abruptly and stopping it does not cause withdrawal effects. It does not need to be tapered down.
Q. How should LDN be titrated?
A. LDN is titrated to minimize side effects like vivid dreams which typically present in the early stages of drug initiation. Most patients can start LDN at a 1.125 mg dose which is 1⁄4 of the standard 4.5 mg dose and slowly work up by adding 1⁄4 tablet each week. Most patients will settle on a maintenance dose of around 4.5mg for immune related concerns.
Q. What is the best time to take LDN?
A. LDN is typically taken at night to better align circadian patterns when endorphin levels are naturally higher.
