Originally published November 14, 2022, this article explores the role of naltrexone, often prescribed for opioid use disorders, in weight management. Understanding how naltrexone interacts with the body can help individuals determine if it's a suitable option for their weight loss journey.
Understanding Naltrexone
Naltrexone is a prescription medication primarily used to treat opioid and alcohol use disorders. It functions as an opioid receptor antagonist, binding to these receptors in the brain and blocking the effects of opioids and alcohol, thus reducing cravings. While higher doses are used for addiction treatment, lower doses can aid in weight loss by managing appetite and influencing other weight-related factors.
How Naltrexone Impacts Weight
Naltrexone affects several bodily functions that can contribute to weight management:
Managing Appetite
The body's normal function involves signaling appetite to ensure adequate calorie intake. However, some individuals experience persistent hunger signals even after consuming enough calories, leading to weight gain. Hormonal imbalances can also disrupt these signals, causing the body to demand more calories than necessary. Naltrexone can help restore balance to the body's appetite regulation. Data suggests that opioids may play a significant role in stimulating appetite. A double-blind placebo-controlled study revealed that taking only 50 milligrams of Naltrexone caused individuals to consume significantly less food.
Reducing Inflammation
Inflammation can disrupt various bodily processes, contributing to weight fluctuations through issues like thyroid problems, diabetes, and hormonal imbalances. Individuals already struggling with weight may face additional challenges due to inflammation. Naltrexone, particularly in low doses (LDN), may act as an anti-inflammatory agent, potentially mitigating these effects.
Read also: Naltrexone: Dosage and Uses for Weight Loss
Improving Sleep
Poor sleep can contribute to weight gain by causing inflammation. Sleep problems and weight gain can create a negative cycle, leading to various health issues. Naltrexone may improve sleep quality, potentially breaking this cycle.
Increasing Growth Hormones
Growth hormones, produced in the pituitary gland, regulate fat, bone density, muscle building, and cholesterol management. Weight gain and hormonal imbalances can affect growth hormone levels, leading to increased fat levels. Naltrexone has been shown to augment the growth hormone response, potentially combating obesity caused by hormonal imbalances.
Lowering Insulin Resistance
Insulin resistance can contribute to weight gain. Naltrexone has been proven to improve insulin resistance induced by hyperinsulinemia. By reorienting macrophages toward anti-inflammation, it helps restore healthy insulin levels in the body, which can combat both obesity and type 2 diabetes.
Assisting with Thyroid Issues
Inflammation caused by thyroid issues can contribute to weight fluctuations. Naltrexone can assist with inflammation, often leading to a decreased T3 to T4 conversion resulting in a state of thyroid resistance. Reduced thyroid function impacts metabolism and makes it more challenging to lose weight. Thus, taking Naltrexone can improve T3 levels and increase T4 to T3 conversion, reducing symptoms of hypothyroidism, including weight gain.
Naltrexone and Bupropion Combination
Research suggests that combining naltrexone with bupropion, an antidepressant that can boost energy and stabilize mood, can enhance weight loss effects. This combination has been prescribed for years to enhance weight management efforts in overweight or obese adults. In three clinical trials, the combination of bupropion and naltrexone was more effective in reducing body weight than diet and exercise alone. Together these two medications activate a part of the brain that controls hunger.
Read also: Naltrexone: Uses and Effectiveness
The naltrexone-bupropion combination pill was recently approved for obesity treatment in the USA and Europe. This is a sustained-release combination of 8 mg of naltrexone and 90 mg bupropion. At this time, the recommended dose is a total of 32 mg naltrexone and 360 mg bupropion. The manufacturer has evaluated various doses of naltrexone combined with fixed doses of bupropion and found that 32 mg of naltrexone is the optimum dose.
Dosage and Timing
While the drug manufacturer doesn’t recommend the best time to take Naltrexone, many people take Naltrexone in the morning. Taking Naltrexone in the morning is often easier for many people since taking it after breakfast, or first thing along with other pills is a good reminder. However, some people may feel sleepy after taking Naltrexone as they get used to the medication. If you’re one of the people who become drowsy after taking Naltrexone, you may want to talk to your doctor about taking the medication at night.
The amount of time you take Naltrexone will depend on your weight loss goals. A medical professional will give you a prescription for a low dose of the medication in a pill or as a pellet implanted under the skin.
Additional Weight Loss Options
Besides Naltrexone, other medications and supplements can aid in weight loss:
Semaglutide (Ozempic): This medication, primarily for type 2 diabetes, has shown promise in weight loss by mimicking the hormone GLP-1, regulating appetite, blood sugar, and insulin secretion.
Read also: Naltrexone for Weight Loss
Tirzepatide: A novel agonist for GIP and GLP-1 receptors, tirzepatide has demonstrated efficacy in weight reduction by decreasing food intake and modulating fat utilization.
Phentermine: An appetite suppressant that has been a significant ingredient for weight loss in the US since it was approved by the FDA in 1959. It is used together with diet and exercise to treat obesity, especially in people with risk factors such as high blood pressure, high cholesterol, or diabetes.
Vitamin Shots: Vitamin shots deliver essential vitamins and nutrients to the bloodstream, boosting energy levels, supporting immune function, and promoting health and wellness.
Bella Capsules: A combination of several drugs that independently have shown tremendous promise in supporting weight loss. These medications act on the hypothalamus of the brain to reduce cravings and suppress hunger making it easier for you to control your appetite.
Benefits of Naltrexone for Weight Loss
Naltrexone provides several potential benefits for weight management:
- Lowered appetite: Reduces the frequency and intensity of food cravings.
- Reduced incentive to overeat: Diminishes the satisfaction derived from binging on food.
- Improved mood: Stabilizes mood and reduces stress, especially when combined with bupropion.
- Stabilized blood sugar: Improves insulin sensitivity, reducing blood sugar swings.
- More energy: Combats fatigue often associated with dieting.
Potential Side Effects and Concerns
Naltrexone is not a foolproof weight loss method and has potential side effects. Common issues include gastrointestinal upset, nausea, anxiety, headaches, insomnia, and dizziness. High doses may lead to liver damage. However, it's generally considered a safe medication, with studies showing that patients taking naltrexone reported fewer serious health problems than those taking a placebo.
Who Can Benefit from Naltrexone?
Naltrexone is typically prescribed for individuals with severe weight issues and related health conditions. It's not recommended for those who can lose weight through traditional methods. It is essential that your doctor check your progress at regular visits to make sure this medicine is working properly and to check for unwanted effects.
Naltrexone is not safe for pregnant or nursing women, individuals with acute liver failure, or those planning to continue using opioids, alcohol, or other substances that slow breathing.
Important Safety Information
Do not take naltrexone and bupropion combination with a monoamine oxidase (MAO) inhibitor (eg, isocarboxazid [Marplan®], phenelzine [Nardil®], selegiline [Eldepryl®], tranylcypromine [Parnate®]). Do not start taking naltrexone and bupropion combination during the 2 weeks after you stop a MAO inhibitor. Wait 2 weeks after stopping naltrexone and bupropion combination before you start taking a MAO inhibitor. If you take them together or do not wait 2 weeks, you may have confusion, agitation, restlessness, stomach or bowel symptoms, a sudden high body temperature, an extremely high blood pressure, or severe seizures.
Do not use naltrexone and bupropion combination if you are also using Zyban® to quit smoking or Aplenzin® or Wellbutrin® for depression, because they also contain bupropion. Also, do not take this medicine if you are using or have used narcotic drugs (eg, buprenorphine, methadone, or other habit-forming painkillers) within the past 7 to 10 days.
The Importance of Lifestyle Changes
Naltrexone works best when combined with a healthy diet and exercise routine. Behavioral and lifestyle changes can accelerate weight loss and help individuals achieve their goals more effectively.