
Naltrexone is a prescription medication that comes in the form of an oral tablet or intramuscular (IM) injection. It is used to treat alcohol and opioid use disorders. The medicine blocks the high feeling you get from opioid drugs, including heroin, and can cause withdrawal symptoms in people who are using narcotics. While naltrexone is usually well-tolerated, it may cause some common side effects such as nausea, headache, dizziness, drowsiness, and muscle cramps. In rare cases, naltrexone may cause liver damage and increase thoughts of suicide. There is also research indicating that low-dose naltrexone (LDN) can be used to treat Stiff-Person Syndrome (SPS), a rare neurological disorder characterized by severe and progressively worsening muscle stiffness, rigidity, and painful muscle spasms.
| Characteristics | Values |
|---|---|
| Low-dose naltrexone treatment for | Stiff-Person Syndrome (SPS) |
| Burning Mouth Syndrome (BMS) | |
| Naltrexone side effects | Dizziness |
| Drowsiness | |
| Less alert | |
| Headache | |
| Nausea | |
| Injection site reactions | |
| Muscle cramps | |
| Liver damage | |
| Decreased opioid sensitivity | |
| Euphoric mood | |
| Delirium | |
| Libido decreased |
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What You'll Learn
- Naltrexone is used to treat Stiff-Person Syndrome (SPS), a rare disorder causing muscle spasms
- SPS is characterised by severe and progressively worsening muscle stiffness and rigidity
- Naltrexone is also used to treat Burning Mouth Syndrome (BMS), a chronic intraoral burning sensation
- Naltrexone may cause dizziness, drowsiness, and decreased alertness
- Other side effects include nausea, headaches, and injection site reactions

Naltrexone is used to treat Stiff-Person Syndrome (SPS), a rare disorder causing muscle spasms
Stiff-Person Syndrome (SPS) is a rare neurological disorder characterized by severe and progressively worsening muscle stiffness and rigidity. The severity of symptoms varies from person to person, but it primarily affects the trunk regions and lower extremities. Individuals with SPS may become too disabled to walk or move and can experience heightened sensitivity to noise, touch, and emotional distress. The condition can be very painful due to unpredictable muscle spasms, which can be triggered by various stimuli. While there is currently no cure for SPS, low-dose naltrexone (LDN) has been found to reduce symptoms significantly.
Naltrexone is a drug introduced in the mid-1980s and approved by the FDA to reduce opiate toxicity and addiction. It blocks the activity of opioid receptors, including mu, delta, and kappa receptors. The term "LDN" refers to administering naltrexone in low doses, typically ranging from 2 to 5 mg. In the context of SPS treatment, LDN is believed to operate through multiple mechanisms, including its potential role as a glial cell modulator.
Microglia are immune cells found in the central nervous system. When activated, these cells can produce inflammatory factors and excitatory factors that contribute to pain sensitivity, sleep and cognitive disruptions, mood disorders, and fatigue. Naltrexone exhibits an antagonist effect on non-opioid receptors (Toll-like Receptor 4) found on microglia, thereby reducing pain sensitivity and other associated symptoms.
The benefits of using LDN to treat SPS were observed in a 59-year-old woman who experienced a significant reduction in her symptoms. After being treated with LDN, she reported reductions in pain, anxiety, depression, agoraphobia, and muscle tightness within six weeks. During multiple follow-ups over 12 months, she consistently displayed reduced symptoms and an improved quality of life.
In conclusion, while Stiff-Person Syndrome (SPS) is a rare and challenging disorder, low-dose naltrexone (LDN) has shown promising results in alleviating its symptoms. LDN's ability to modulate glial cells and its antagonist effect on specific receptors contribute to its effectiveness in managing SPS symptoms. Further research is warranted to explore the potential of LDN in treating SPS and other chronic pain conditions.
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SPS is characterised by severe and progressively worsening muscle stiffness and rigidity
Stiff-Person Syndrome (SPS) is a rare neurological disorder characterised by severe and progressively worsening muscle stiffness and rigidity. It primarily affects the trunk regions and lower extremities, and can be so severe that afflicted individuals may be unable to walk or move. SPS is often extremely painful due to unpredictable muscle spasms, which can be triggered by various stimuli, such as noise, touch, or emotional experiences. As such, individuals suffering from SPS may display heightened sensitivity to noise, touch, and emotional distress. SPS affects twice as many women as men.
Historically, treatment for SPS included the administration of some combination of anxiolytics, anticonvulsants, muscle relaxants, or pain medication. There is research indicating the effectiveness of intravenous immunoglobulin (IVIG) treatment in reducing stiffness and lowering sensitivity to triggers in people with SPS.
Low-dose naltrexone (LDN) has been found to reduce symptoms in SPS. Naltrexone and its active metabolite 6-β-naltrexol block activity at mu- and delta-opioid receptors, as well as kappa-opioid receptors. The blockade of opioid receptors is the basis behind its action in the management of opioid dependence. The term “LDN” refers to the administration of naltrexone in low doses in the range of 2–5 mg. The benefit of LDN in SPS is likely due to multiple mechanisms. LDN may work as a glial cell modulator. Microglia are immune cells that reside in the central nervous system and when activated, can produce inflammatory as well as excitatory factors that can lead to pain sensitivity, sleep and cognitive disruption, mood disorders, and fatigue.
There is a reported case of a 59-year-old woman diagnosed with SPS who experienced a dramatic reduction in her symptoms after being treated with LDN. Prior to this treatment regimen, she had tried many treatments with limited success. After starting LDN, she reported reductions in pain, anxiety, depression, agoraphobia, and muscle tightness. Upon multiple follow-ups, up to 12 months, she continually displayed reduced symptoms and improved quality of life.
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Naltrexone is also used to treat Burning Mouth Syndrome (BMS), a chronic intraoral burning sensation
Naltrexone is an opioid antagonist that crosses the blood-brain barrier and inhibits spinal glial activation, including that of TLR4. It has been found to be effective in reducing neuropathic pain. The International Classification of Diseases defines Burning Mouth Syndrome (BMS) as a chronic intraoral burning sensation with no identifiable local or systemic cause. BMS is a chronic pain condition similar to neuropathic pain. It is characterised by a persistent burning sensation in the oral cavity.
Low-dose naltrexone (LDN) has been found to be a feasible and effective treatment for BMS, especially in patients refractory to traditional treatment. LDN is defined as dosages of naltrexone that are approximately 1/10th of the dose used to treat an opioid use disorder (OUD) (50.0–100.0 mg). It reportedly reduces symptom severity in BMS by blocking mu opioid receptors and promoting the production of endogenous opioids. A case report of a 62-year-old woman with a chief complaint of "burning mouth" demonstrated the effectiveness of LDN in treating BMS. The patient reported a burning pain that started after a dental extraction three years prior. The pain, located at the extraction site, resolved over time. However, the patient later experienced a burning sensation on the dorsum of the tongue. After being prescribed LDN, the patient reported a 50% decrease in pain intensity, with no pain upon awakening.
Another case report describes a 66-year-old male with a history of chronic and severe burning mouth pain after a thalamic stroke. The patient experienced severe depression and suicidal thoughts when the pain worsened. Despite numerous medication trials for pain management, including opiates, anticonvulsants, benzodiazepines, tricyclic antidepressants, and medicinal marijuana, the patient's pain did not respond. However, when treated with LDN, his pain responded remarkably.
The benefit of LDN in treating BMS is likely due to multiple mechanisms. LDN may work as a glial cell modulator. Microglia are immune cells that reside in the central nervous system, and when activated, they can produce inflammatory and excitatory factors that contribute to pain sensitivity, sleep and cognitive disruption, mood disorders, and fatigue. LDN exhibits anti-inflammatory actions by attenuating glial cells, decreasing the production of pro-inflammatory cytokines and neurotoxic superoxides.
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Naltrexone may cause dizziness, drowsiness, and decreased alertness
Naltrexone is a prescription medication that comes in the form of an oral tablet and an intramuscular (IM) injection. It is used to treat alcohol and opioid use disorders. While naltrexone can be beneficial for managing these conditions, it is important to be aware of its potential side effects. One of the most commonly reported side effects of naltrexone is dizziness, which can occur in up to 13% of people taking the medication. This dizziness may be accompanied by drowsiness and decreased alertness.
If you experience dizziness, drowsiness, or decreased alertness while taking naltrexone, it is important to refrain from driving, operating heavy machinery, or engaging in other potentially dangerous activities until you understand how the medication affects you. These side effects can increase your risk of accidents or injuries, so caution is advised.
The experience of dizziness and drowsiness may vary among individuals taking naltrexone. Some people may find that these side effects are mild and manageable, while others may find them more bothersome or disruptive to their daily lives. It is important to monitor how you feel and inform your healthcare provider if these side effects are persistent or interfering with your normal activities.
Additionally, it is worth noting that naltrexone may have other side effects that can contribute to decreased alertness. For example, naltrexone can cause insomnia or sleep disorders in about 14% of people. This disruption in sleep can further exacerbate feelings of drowsiness and decreased alertness during the day.
If you are experiencing dizziness, drowsiness, or decreased alertness while taking naltrexone, it is recommended to consult your healthcare provider. They may advise adjusting the dosage or provide strategies to mitigate these side effects. It is important to remember that everyone's experience with medication can vary, and your healthcare provider can help tailor the treatment plan to your individual needs.
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Other side effects include nausea, headaches, and injection site reactions
Naltrexone is a prescription medication that comes in the form of an oral tablet and intramuscular (IM) injection. It is used to treat alcohol use disorder and opioid use disorder. While naltrexone can be effective in treating these conditions, it is important to be aware of its potential side effects.
One of the most common side effects of naltrexone is nausea. This can range from mild to moderate intensity and is typically manageable at home. However, if nausea becomes severe or persists, it is important to consult a healthcare provider.
Headaches are another frequent occurrence among naltrexone users. Similar to nausea, headaches can usually be managed at home with over-the-counter pain relievers such as acetaminophen or ibuprofen. However, if headaches become worse or persist, it is advisable to seek medical advice.
Injection site reactions are also common, particularly with the intramuscular form of naltrexone. These reactions can include redness, itching, swelling, and the formation of a small lump at the injection site. While these reactions are typically not serious, they can be uncomfortable and may take weeks to resolve. It is important to distinguish injection site reactions from more severe allergic reactions, which can also occur with IM naltrexone. Allergic reactions may include symptoms such as skin rashes, facial swelling, or trouble breathing, and require immediate medical attention.
In addition to these side effects, naltrexone may also cause dizziness, drowsiness, decreased appetite, and mood changes such as depression and anxiety. It is important for individuals taking naltrexone to be aware of these potential side effects and to consult their healthcare provider if any concerns arise.
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Frequently asked questions
No, low-dose naltrexone (LDN) is used to treat Stiff-Person Syndrome (SPS), a rare neurological disorder characterized by severe muscle stiffness and painful muscle spasms. LDN has been shown to reduce pain, anxiety, depression, agoraphobia, and muscle tightness in patients with SPS.
The typical dosage of LDN is in the range of 2-5 mg.
Yes, LDN has also been shown to be effective in treating burning mouth syndrome (BMS), a chronic intraoral burning sensation with no identifiable cause.
Common side effects of naltrexone include nausea, headache, dizziness, drowsiness, decreased appetite, and mood changes. Serious side effects include liver damage, decreased opioid sensitivity, and trouble breathing.











































