Unlock the Weight Loss Secret: How Naltrexone Dosage and Uses Can Transform Your Journey

Naltrexone is a medication primarily known as an opioid antagonist. While it's not approved for weight loss on its own, it's a component of a combination drug (Contrave) used for that purpose. This article provides a detailed overview of naltrexone, its approved uses, potential off-label use for weight loss, and essential dosage information.

Understanding Naltrexone

Naltrexone belongs to a class of drugs known as opioid antagonists. It is available as an oral tablet, typically in a strength of 50 mg. Naltrexone is not available in a brand-name version as a single-ingredient medication.

Approved Uses of Naltrexone

The Food and Drug Administration (FDA) has approved naltrexone for two primary uses:

Opioid Use Disorder (OUD): Naltrexone helps manage opioid dependence as part of a comprehensive treatment program. This program often includes counseling, support groups, and other therapeutic interventions.
Alcohol Use Disorder (AUD): Naltrexone is also used to treat alcohol dependence. It is typically prescribed alongside counseling and other AUD treatments. The oral form is approved by the US Food and Drug Administration (FDA) for alcohol dependence and is shown to decrease cravings for alcohol.

Dosage for Approved Uses

Opioid Use Disorder: The typical starting dose is 25 mg once daily. If no withdrawal symptoms occur after the first day, the dosage may be increased to 50 mg once daily.Withdrawal symptoms are side effects that can occur when you stop taking a drug that your body has become dependent on. Naltrexone may cause withdrawal symptoms if you’ve taken opioids within 10 days of starting naltrexone.
Alcohol Use Disorder: The recommended dose is 50 mg once daily.

Naltrexone is meant to be taken as a long-term treatment for OUD. For AUD, the recommended treatment time is up to 12 weeks. However, your doctor may prescribe the drug for longer if you both feel this is best for treating your condition.

How Naltrexone Works for Addiction Treatment

Naltrexone functions as an antagonist of µ, δ, and κ opiate receptors, with its most pronounced actions on µ opiate receptors. It blocks opiate receptors, which may cause dramatic opiate withdrawal in ongoing opiate users, while also completely negating both euphoric and therapeutic antinociceptive effects of opioids for nonusers. By blocking these receptors, naltrexone reduces cravings for alcohol and prevents the euphoric effects of opioids, supporting recovery and preventing relapse.

Naltrexone and Weight Loss

While naltrexone is not FDA-approved for weight loss when used alone, it is a component of Contrave, a medication approved for this purpose.

Can Naltrexone Be Used for Weight Loss?

Naltrexone is not approved for use on its own to help with weight loss. However, the drug may be prescribed off-label for this or other uses. With off-label use, doctors prescribe a drug for a purpose other than what the FDA approved it for. Naltrexone tablet is FDA approved to help treat OUD and AUD in adults.

Naltrexone/Bupropion Combination (Contrave)

The combination of naltrexone and bupropion has shown promise in weight management. Studies have shown that the combination of these two medications is more effective in inducing weight loss, when combined with lifestyle intervention and calorie reduction, than each individual medicine alone. The naltrexone-bupropion combination, when combined with lifestyle intervention and modest calorie reduction, seems to be quite effective for 6-month and 1-year outcomes for clinically significant weight loss (over 5% of total body weight).

Contrave combines naltrexone with bupropion, an antidepressant, to impact areas of the brain involved in appetite and reward. This combination can help reduce cravings and control eating behavior. 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.

How the Combination Works

Naltrexone: May affect food intake through various mechanisms.6 Its nonspecific blockade of opiate receptors also blocks endogenous opioid (ie, endorphin) action. First, craving is a form of anticipatory reward which is regulated through endogenous opioid and mesolimbic dopaminergic systems. Naltrexone attenuation of alcohol craving may be explained by its blockade of anticipatory reward, and so it could be hypothesized that it would reduce food cravings, which induce nonhunger eating. Second, food intake is a very rewarding process in itself. Food consumption is pleasurable, since it induces endorphin release, which is in relative proportion to fat and sugar content of the consumed food. Thus, naltrexone blocks the rewarding aspects of the food and is shown to decrease food consumption in rodents.7 Finally, hypothalamic pro-opiomelanocortin (POMC) cells are important in appetite regulation since they send a “stop-eating” signal to the brain by secreting melanocyte-stimulating hormone (MSH). MSH is cosecreted with β endorphin, which does not have any effect on appetite but provides a feedback inhibition to POMC cells.
Bupropion: Bupropion is a well-studied antidepressant which has been widely used for over 25 years. It is marketed in various generic oral doses in immediate-release, sustained-release, and extended-release formulations.

The medications, in this instance, appear to have a synergistic effect by providing more weight loss than each medication alone. Studies showed a yearly weight loss of nearly 8% TBW with the combination medication in combination with lifestyle intervention and a 500-calorie reduction compared to approximately 1.5% TBW lost in the placebo arm.19 When intensive lifestyle intervention is applied, the weight loss approaches 11% TBW compared to about 7% with placebo.20 Diabetic patients appear to lose less weight with the combo drug, about 6% versus 2% with placebo.21 It is not clear why diabetic patients lose less weight with the drug.

Read also: Weight Loss Guide Andalusia, AL

Dosage and Administration of Contrave

The naltrexone-bupropion combination pill is marketed in a sustained-release tablet consisting of 8 mg of naltrexone and 90 mg of bupropion. Due to seizure and elevated blood pressure risk with sudden increase in bupropion, the manufacturer recommends starting with one tablet a day and gradually increasing over a period of 1 month to 2 tablets twice daily.24

Effectiveness of Contrave

Studies have demonstrated significant weight loss with the naltrexone-bupropion combination when combined with lifestyle interventions and calorie restriction. The aim of the treatment is clinically significant weight loss. This is by convention defined as 5% of TBW. This level of weight loss, although modest, is shown to improve medical outcomes if maintained in the long term.

Important Considerations

Patient Selection: These medications are not devoid of serious side effects, however, and careful patient selection can reduce dramatic complications and increase positive outcomes.
Lifestyle Intervention: Medication treatment with naltrexone-bupropion combination needs to be coupled with a lifestyle intervention and caloric restriction, to be successful.
Medical Indications: The naltrexone-bupropion combination is studied and approved for patients who have a body mass index (BMI) of 30 and over (obese), or people who have a BMI over 27 (overweight) and have one or more obesity-related conditions such as type 2 diabetes.
Potential Side Effects: During the studies, the drug was well tolerated, and the most frequent reported side effect was nausea, which is not surprising as this is the most common side effect for both drugs separately. Nausea is usually time-limited with both drugs and is more pronounced in the beginning of the therapy.

Low Dose Naltrexone (LDN)

Low Dose Naltrexone (LDN) is an off-label use of naltrexone that has garnered attention for its potential benefits in various conditions, including autoimmune diseases, chronic pain, and more recently, weight management.

What is Low Dose Naltrexone?

Naltrexone was originally developed to treat opioid and alcohol dependence by blocking the euphoric effects of those substances. But in very small doses, typically 0.5mg to 4.5mg, it has been shown to have powerful immune-modulating and anti-inflammatory properties with minimal side effects. Unlike traditional naltrexone dosing (50-100mg/day), LDN works not by fully blocking the opioid system, but by temporarily binding to opioid receptors.

Potential Benefits and Uses

LDN has been explored for a wide range of clinical benefits, and over 90 published studies exploring its use in chronic pain, autoimmune disease, fibromyalgia, PCOS, and even cancer. LDN also pairs well with GLP-1 agonists (e.g., Saxenda, Wegovy), particularly for patients with PCOS or leptin resistance.

Dosage and Administration of LDN

Typical LDN doses range from 1.5mg to 4.5mg per day. Providers often start at a low dose (0.5mg) and slowly titrate up to find the individual’s optimal dose.

General Information About Naltrexone

How to Take Naltrexone

Naltrexone comes as a tablet you swallow whole. The drug’s prescribing information does not say whether the tablets may be crushed, chewed, or split. Be sure to take your dose with a full glass of water. You can take your dose with food if naltrexone upsets your stomach.

It may be helpful to take your naltrexone dose around the same time of day. This helps maintain a steady level of naltrexone in your body so the drug can work effectively.

What To Do If You Miss A Dose

If you miss a dose of naltrexone, take it as soon as you remember. If it’s almost time for your next dose, skip the missed dose and take your next scheduled dose. You should not take two doses to make up for the missed one.

Overdose

It’s important that you do not take more of naltrexone than your doctor prescribes.

Call your doctor right away if you believe you’ve taken too much naltrexone. If you have severe symptoms, immediately call 911 or your local emergency number, or go to the nearest emergency room.

How Long Does It Take For Naltrexone To Work?

Naltrexone begins to work after you take your first dose. Naltrexone is fully absorbed into your body within 1 hour.

Based on how naltrexone works, you may not feel the medication working in your body. And you may not feel a reduction in cravings or other symptoms of your condition right away. Your doctor will monitor you during treatment to check whether the naltrexone is working to treat your condition.

Important Precautions and Warnings

Opioid Use: This medicine blocks the euphoric and rewarding feeling you get from opioid drugs, including heroin. Since naltrexone may make you more sensitive to lower doses of opioids than you have previously used, you should not use heroin or any other opioid drugs to overcome what the medicine is doing. You could overdose and develop serious problems.
Liver Problems: Check with your healthcare provider right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, unusual tiredness or weakness, or yellow eyes or skin. These could be symptoms of a serious liver problem.
Mental Health: This medicine may cause some people to be agitated, irritable, or display other abnormal behaviors. It may also cause some people to have suicidal thoughts and tendencies or to become more depressed.
Alcohol Use: Naltrexone will not prevent you from becoming impaired when you drink alcohol.
Pregnancy: Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant during therapy.
Drug Interactions: Do not take naltrexone and bupropion combination with a monoamine oxidase (MAO) inhibitor. 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 within the past 7 to 10 days.

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