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Lotrexone

Lotrexone is a prescription medication used to manage chronic pain and inflammatory conditions. It combines two active ingredients, naltrexone, an opioid receptor antagonist, and low-dose corticosteroids, which work to reduce inflammation and modulate the immune response. This combination makes Lotrexone particularly effective for treating conditions such as chronic pain syndromes, autoimmune diseases, and fibromyalgia, where both inflammation and pain are major components.



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Frequently Asked Questions

How long does it take for Lotrexone to start working?
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The anti-inflammatory effects of Lotrexone can begin within a few days to weeks, depending on the condition being treated. Pain relief may also be noticed within the first week, though it may take longer for full benefits to be achieved.

Can I drink alcohol while taking Lotrexone?
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No, alcohol should be avoided while taking Lotrexone, as naltrexone can increase the risk of liver damage, and alcohol can exacerbate this effect.

Can I stop taking Lotrexone suddenly?
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No, especially if you have been on Lotrexone for a long period, the corticosteroid component requires gradual tapering to avoid withdrawal symptoms and adrenal insufficiency. Consult your doctor before stopping the medication.

What should I do if I miss a dose of Lotrexone?
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If you miss a dose, take it as soon as you remember. If it’s close to the time of your next dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at once.

Is Lotrexone safe for long-term use?
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Lotrexone can be used long-term under medical supervision. However, long-term use of corticosteroids is associated with increased risks of side effects such as bone thinning (osteoporosis), adrenal suppression, and increased infection risk, so regular monitoring is necessary.

Comprehensive Drug Guide

How Does Lotrexone Work?

  • Naltrexone blocks the opioid receptors in the brain, which helps modulate the body's pain response without the sedative or addictive properties associated with opioids.
  • Corticosteroids reduce inflammation by inhibiting various pathways in the immune system that trigger inflammation and immune response, thereby decreasing pain, swelling, and discomfort.


What is Lotrexone Used For?


Common Dosages

  • 50 mg naltrexone with 5 mg corticosteroid
  • 100 mg naltrexone with 10 mg corticosteroid

Typical Dosing

  • For chronic pain: One tablet is typically taken once daily, depending on the severity of the condition and response to the medication. Doses may vary based on the patient’s needs and treatment plan.
  • For inflammation: Dosing varies depending on the condition being treated and the severity of the inflammation. It is important to follow the prescribed regimen closely.


Typical Dosing

FDA Approved Indications

  • Chronic pain management in conditions such as fibromyalgia, neuropathy, and autoimmune diseases.
  • Inflammatory conditions, where corticosteroids help reduce swelling and immune overactivity.


Off-Label Uses


Who Shouldn't Take Lotrexone?

  • Known hypersensitivity to naltrexone, corticosteroids, or any of the formulation's components.
  • Active liver disease or renal impairment, as naltrexone can affect liver function.
  • Conditions where corticosteroid use is contraindicated, such as severe infections or systemic fungal infections.


Advice From The Pharmacist

  • Take Lotrexone as prescribed, ideally at the same time each day. Do not exceed the recommended dose.
  • Do not stop taking Lotrexone suddenly, especially if used long-term, as abrupt discontinuation of corticosteroids can lead to withdrawal symptoms or flare-ups of the underlying condition.
  • Regular monitoring of liver function may be necessary, especially in patients with pre-existing liver conditions.
  • Avoid alcohol, as it can increase the risk of liver damage while taking naltrexone.
  • Monitor for infections, as corticosteroids can suppress the immune system, increasing the risk of infections.


Side Effects of Lotrexone

Common Side Effects

  • Nausea or vomiting
  • Headache
  • Dizziness
  • Fatigue
  • Increased susceptibility to infections


Uncommon/Severe Side Effects

  • Liver toxicity: Signs include yellowing of the skin or eyes, dark urine, or severe fatigue.
  • Increased blood sugar: Corticosteroids can lead to higher blood sugar levels, particularly in diabetic patients.
  • Mood changes: Anxiety, irritability, or depression may occur, particularly with long-term corticosteroid use.
  • Allergic reactions: Swelling, difficulty breathing, or severe rashes should be addressed immediately.


Risks and Warnings of Lotrexone

  • Liver Risk: Naltrexone can increase liver enzyme levels, leading to liver damage in some patients. Regular monitoring of liver function is recommended.
  • Immunosuppression: The corticosteroid component can suppress the immune system, making patients more susceptible to infections. Close monitoring for signs of infection is necessary, and vaccinations may need to be updated before starting therapy.
  • Adrenal Suppression: Long-term corticosteroid use can suppress the adrenal glands, which may result in insufficient cortisol production when the medication is discontinued. Gradual dose reduction is essential to avoid adrenal insufficiency.


Interactions with Lotrexone

Common Drug Interactions

  • Opioid medications: Lotrexone may block the effects of opioid-based pain medications, making them less effective. Inform your doctor if you are taking any opioid medications.
  • NSAIDs: Nonsteroidal anti-inflammatory drugs may increase the risk of gastrointestinal bleeding or ulcers when combined with corticosteroids.
  • Diabetic medications: Corticosteroids can raise blood sugar levels, requiring adjustments in diabetes medications.


Alternatives to Lotrexone

  • Low-dose naltrexone (LDN): Used in some chronic pain and autoimmune conditions as an alternative to standard doses of naltrexone, especially for those who cannot tolerate higher doses.
  • Prednisone: A corticosteroid used for similar anti-inflammatory purposes, often prescribed for autoimmune conditions.
  • Methotrexate: An immunosuppressant often used for autoimmune conditions and chronic inflammatory diseases.
  • Non-opioid pain relievers: Such as gabapentin or pregabalin, for chronic pain management in conditions like fibromyalgia or neuropathy.