Naltrexone/Bupropion (Contrave) for weight loss treament

Naltrexone/Bupropion for Weight Loss
Medically reviewed by Dr. Ola Tarabzuni

Overview

Naltrexone/Bupropion, a combination medication approved for weight loss, represents a novel approach to addressing obesity. Comprising the opioid receptor antagonist naltrexone and the antidepressant bupropion, this drug works synergistically to target multiple neurochemical pathways involved in appetite regulation and energy balance. Naltrexone modulates the reward system, reducing food cravings, while bupropion enhances norepinephrine and dopamine activity, influencing mood and metabolism. The combination has demonstrated efficacy in promoting weight loss, particularly in individuals with obesity-related comorbidities. Moreover, its impact on insulin sensitivity and glycemic control suggests potential benefits for those with obesity-related metabolic disorders. However, like any pharmaceutical intervention, Naltrexone/Bupropion is not without side effects, including nausea and headache, and requires careful consideration of individual patient profiles. Naltrexone/Bupropion presents a viable option as part of an all-encompassing weight-management plan for people looking for workable and well-tolerated ways to fight obesity and enhance general health.

“Think about weight loss as you think about debt. When you’re paying off debt, you do not pay off all at once. You do it in increments. It’s the same for weight loss.”

Lori Nobel MD, physician Penn Medicine

Naltrexone for weight loss

Naltrexone at low doses helps people lose weight, especially those who struggle with overeating or insulin resistance. It frequently produces noticeable benefits when combined with moderate exercise and a good diet. It is commonly administered as Contrave® along with bupropion. An early morning Naltrexone dose can reduce hunger by thirty percent, which can help with weight loss. Morning dosage improves your weight loss plan by suppressing cravings throughout the day. 

Bupropion is a norepinephrine reuptake inhibitor, and it is an antagonist of the opioid receptor. Naltrexone has many applications, including the treatment of chronic pain and weight loss. There have been successful weight loss outcomes using Naltrexone. This medicine works by lowering appetite, which helps people lose weight. Patients with obesity can be successfully treated when paired with bupropion.

Bupropion is an antidepressant that suppresses appetite, which leads to weight loss. When a person takes a modest dose of Naltrexone, their body is not stimulated to crave food since the brain is not receiving hunger signals. The person will eventually develop a habit of suppressing their hunger and feel compelled to alter their diet. Other methods by which Naltrexone aids in weight loss include:

  • Reduced Insulin Resistance
  • Energy Boost
  • Improved Sleep Patterns
  • Growth Hormones Increase
  • Increased Thyroid Hormonal Levels
Ready to explore the benefits of Naltrexone for weight loss? Consult now!

How does low-dose Naltrexone work for weight loss?

Patients and people who are overweight and obese can be treated with the FDA-approved weight-loss drug Naltrexone HLC. Patients’ appetites can be suppressed with low doses of Naltrexone. The combination of weight loss medications will elevate mood and permanently curb cravings for sweets and carbohydrates. Naltrexone at a low dose can aid with the following:

Improve Mood

The combination of LDN weight loss drugs causes a rise in serotonin and dopamine synthesis, which can reduce anxiety and stress. Therefore lowering emotional eating as a result.

Improve sleep

These help boost sleep. Sleep deprivation can cause weight growth and adversely impact a person’s hormonal balance. Naltrexone breaks this damaging pattern.

Regulate appetite

When a person’s metabolism returns to normal, Naltrexone can help them eat in proportion to their resting energy expenditure.

Reduce insulin resistance

Naltrexone controls insulin-resistant cells, which may result in weight loss.

What is the best time of the day to take Naltrexone for weight loss?

The optimal time to take Naltrexone for weight loss can vary based on individual factors and the specific formulation of the medication. However, it is often recommended to take Naltrexone in the morning. This is because Naltrexone, even in its low-dose form used for weight loss, can have mild stimulant-like effects and may cause insomnia or disrupt sleep if taken too close to bedtime.

By taking Naltrexone in the morning, individuals may experience its potential appetite-modulating effects during the daytime, helping to manage cravings and control food intake throughout the day.

Are there specific dosages for Naltrexone when used for weight loss?

Titrating Bupropion weight loss dosage and Naltrexone weight loss dosage is necessary. Patients should take one 8/90-mg tablet once daily in the morning with a low-fat diet during the first week of treatment. The daily dosage should be increased to one tablet in the morning and one pill in the evening by week two. Patients should take two tablets in the morning and one in the evening during week three. By week four, patients will take a maximum of two tablets twice daily. Patients with modest to severe renal impairment should take one tablet twice a day, and those with mild hepatic impairment should take one tablet daily.

After 12 weeks, patients should stop therapy if they have not lost 5% of their starting body weight. This indicates that more treatment is unlikely to be helpful. Up to a year of therapy should be administered if patients continue to lose weight after 12 weeks and show clinically meaningful improvement. No longer than 56 weeks has Naltrexone/Bupropion been examined.

Two tablets taken twice daily is the maximum amount of Naltrexone/Bupropion that should be taken daily.

Can I combine Naltrexone with other weight loss methods or medications?

In some cases, healthcare providers may prescribe a combination of approaches for weight management, such as diet, exercise, behavioral therapy, and medications. However, the safety and efficacy of combining Naltrexone with other weight loss medications or methods depend on various factors, including individual health conditions, potential drug interactions, and the specific medications involved. However, a combination of two drugs, naltrexone and bupropion, can aid in weight loss and maintenance. Your doctor will advise you to use this medication with exercise and a lower-calorie diet. This drug is marketed under the name Contrave®.

Struggling with weight loss? Consult now to know the best plan for you

When should I see a doctor regarding Naltrexone for weight loss?

See your physician or other healthcare practitioner frequently to discuss your progress.

  • Naltrexone side effects include severe skin reactions. These may occur weeks or months after the drug is started. Contact your doctor immediately if you experience fever or flu-like symptoms, including a rash. The rash could start red or purple, progressing to blisters or skin peeling. Alternatively, you may experience a red rash with lip, face, or lymph node enlargement in your neck or under your arms.
  • This medication may impact glycemic levels. If you have diabetes, find out from your doctor if you need to adjust your diet or take any medications.
  • Patients and their relatives should be on the lookout for suicidal thoughts or depression that is new or intensifying. Additionally, be aware of any abrupt mood swings, such as being unable to fall asleep or experiencing extreme restlessness, excessive excitement and hyperactivity, and hostile, aggressive, irritable, unfriendly, harmful, or negative feelings. Contact your healthcare provider if this occurs, particularly during the start of your treatment or following a dose adjustment.
  • If a woman wants to get pregnant or suspects she could be pregnant, she should let her healthcare professional know. It is not recommended to lose weight when pregnant since it could harm the fetus. Consult your healthcare practitioner for further details.

FAQs about Naltrexone for weight loss

How long does it take for Naltrexone to show results in weight loss?

Patients should expect one to two pounds of weight reduction each week. Other steps, such as regular exercise, must be taken to aid with weight loss. The effects of the 50 mg oral pills continue for two to three days. Greater dosages last longer—100 mg lasts 48 hours, while 150 mg lasts 72 hours. Typically, oral naltrexone pills are administered once a day.
Fourteen days after dosage, intramuscular naltrexone blood levels will gradually drop, although they will remain detectable for around a month.

Is Naltrexone safe for long-term use in weight management?

A person’s risk of liver damage may increase with very high doses. The majority of patients experienced more substantial adverse effects at the beginning of their pharmaceutical use, which subsided over time. There is no evidence from research to suggest that long-term naltrexone use carries any risks.

Is Naltrexone suitable for everyone seeking weight loss?

Naltrexone may not be suitable for everyone seeking weight loss, as its effectiveness varies. It is primarily prescribed for alcohol or opioid dependence, and its off-label use for weight management should be discussed with a healthcare professional.

Are there specific dietary restrictions while using Naltrexone for weight loss?

The use of Naltrexone for weight loss is not linked to any particular dietary limitations. A healthy diet and lifestyle is usually advised for the best effects. 

Can Naltrexone be used for weight loss maintenance after achieving the desired goal?

The use of Naltrexone for weight loss maintenance is not well-established, and its primary indications are alcohol or opioid dependence. 

Can Naltrexone be discontinued once weight loss goals are achieved?

After 12 weeks, patients should stop therapy if they have not lost 5% of their starting body weight. This indicates that more treatment is unlikely to be helpful. Up to a year of therapy should be administered if patients continue to lose weight after 12 weeks and show clinically meaningful improvement.

How much weight can you lose with naltrexone?

This decrease in cravings may significantly affect weight loss. According to a 2011 study, naltrexone users had a three times higher chance of losing 15% of their body weight overall. Patients who attempted naltrexone also had a tendency to lose more weight than those who tried conventional weight-loss methods.

Can Naltrexone be prescribed for individuals with a BMI within the normal range?

If an adult is obese (BMI of 30 kg/m2 or higher) or overweight (BMI of 27 kg/m2 or higher) and has at least one weight-related comorbid condition, Naltrexone/Bupropion is recommended as a supplement to increased physical activity and a reduced-calorie diet for long-term weight management.

Your Doctors Online uses high-quality and trustworthy sources to ensure content accuracy and reliability. We rely on peer-reviewed studies, academic research institutions and medical associations to provide up-to-date and evidence-based information to the users.

  • Billes, Sonja K., Puspha Sinnayah, and Michael A. Cowley. “Naltrexone/bupropion for obesity: an investigational combination pharmacotherapy for weight loss.” Pharmacological Research 84 (2014): 1-11.
  • Makowski, Charles T., Katherine M. Gwinn, and Kathryn M. Hurren. “Naltrexone/bupropion: an investigational combination for weight loss and maintenance.” Obesity Facts 4.6 (2011): 489-494.
  • Verpeut, Jessica L., and Nicholas T. Bello. “Drug safety evaluation of naltrexone/bupropion for the treatment of obesity.” Expert opinion on drug safety 13.6 (2014): 831-841.
  • Sherman, Matthew M., Sinziana Ungureanu, and Jose A. Rey. “Naltrexone/bupropion ER (Contrave): newly approved treatment option for chronic weight management in obese adults.” Pharmacy and Therapeutics 41.3 (2016): 164.

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