Does naltrexone treatment depend on knowing about the naltrexone half-life?

Naltrexone is an opioid antagonist, meaning that it blocks opioid receptors. It is available as a 50 milligram tablet, compounded low dose formulations, known as low dose naltrexone, or LDN, and a long-acting monthly shot. The monthly injectable naltrexone is named Vivitrol.

The tablet form of oral naltrexone is available under the brand names, ReVia and Depade. Another brand, Contrave, is a combination of naltrexone and the antidepressant, bupropion. Contrave is approved for weight loss.

A similar drug, nalmefene, is available in tablet form in Europe. While very similar, nalmefene is not identical to naltrexone, and may work differently for some people.

For some uses, it may not be as important to strictly be aware of naltrexone’s half-life. Yet, for specific uses, knowledge of the half-life is critical.

What exactly is the half-life of naltrexone?

The half-life of a drug is the time that it takes for the amount of the drug remaining in your system to be reduced to half of what it was from the time you start counting. For example, if you take a 50 mg tablet of naltrexone, and the naltrexone half-life is four hours, after four hours, there will be 25 mg in your system.

It turns out that the half-life of the drug ranges between about 4 hours and 10 hours. The difference depends on the person, but for most people, it will be about 4 hours.

As you can imagine, higher dosages will last longer. at 4 hours, the 50 mg becomes 25 mg. Another 4 hours, and it becomes 12.5 mg.

So, if a higher dosage will last longer, should patients be prescribed higher doses? In most cases, the answer would be no. Higher doses of naltrexone increase the risk of side effects.

At very high doses, naltrexone has an increased risk of affecting the liver. Patients also complain of gastrointestinal side effects, even at the standard 50 mg dosage.

Is it better to take the long-acting Vivitrol shot, so naltrexone can last longer?

The Vivitrol shot is given monthly, and acts as a dissolving implant, releasing a steady dose of naltrexone around the clock. Is this the best way to take naltrexone?

For people taking naltrexone to treat opioid use disorder, the monthly Vivitrol shot may be the best form of naltrexone treatment. There are also six-month naltrexone implants under development for treating opioid dependence.

Treating opioid dependence with medication, such as naltrexone, works best when the medication is at a steady level, around the clock. The shot or implant will provide the best experience in keeping naltrexone levels steady long-term.

Opioid addiction to opioid medication or street drugs, such as heroin or fentanyl, can be treated with a long-term naltrexone preparation at a rehab facility, during the client’s stay, after opioids have been detoxed from their system. Addiction treatment with a naltrexone implant, or Vivitrol, must not be started too soon, or it will cause precipitated withdrawal.

While long-acting injectable or implantable naltrexone is ideal for addiction to an opioid drug or opioid analgesics, it is not ideal for alcohol addiction. Alcohol use disorder is best treated with naltrexone oral tablets.

Why is it important to understand the half-life of oral naltrexone when treating alcohol dependence?

One of the most effective ways to use naltrexone to treat substance abuse with alcohol is to start the naltrexone hydrochloride tablets while the person is still drinking. Many healthcare practitioners are not comfortable with this medical advice, to prescribe naltrexone while their patient is still consuming alcohol.

For most types of drug addiction, it is essential that the patient stop taking the drug. For example, there is no addiction treatment method in the US that involves having a patient continue smoking crack or shooting up heroin or fentanyl.

While opioid withdrawal symptoms may be treated with an opioid, buprenorphine , or methadone, there is no rehab in the US that will allow a client to continue using those drugs. Alcohol, a legal recreational drug, is different.

Deerhaven is the first of its kind in the rehab industry to use The Sinclair Method, which is a protocol in which clients take naltrexone and continue to consume alcohol. At Deerhaven, clients in rehab are given medication, and continue to consume alcohol.

At Deerhaven, and in outpatient clinics, where The Sinclair Method, or TSM, is used, it is critical to know about the short half-life of naltrexone. The reason for this is to get the best result with TSM is for the client to drink at a moment when naltrexone levels are at their peak.

When is the best time to take a drink after taking naltrexone on TSM?

The basic instructions for following The Sinclair Method are very simple. Patients are instructed to drink one alcohol-containing beverage, one hour after taking a naltrexone 50 mg tablet, and on days when the patient chooses not to drink at all, they do not take naltrexone.

This is the entire program, summarized in a single sentence. So, why do people need to see a doctor to go on TSM? Why can’t they buy naltrexone in a pharmacy and follow the directions, which could easily be printed on the bottle?

Some people get stomach pain when they first take the opioid-blocking medication. It is also important that patients taking naltrexone tablets do not also take opioid medicine, prescribed for pain relief.

Because of a variety of concerns about safety relating to naltrexone hydrochloride and medical treatments, naltrexone must be prescribed by a health care provider. However, there is a movement working towards FDA approval of over-the-counter naltrexone.

Getting back to the reason for the timing instructions with TSM, the reason for having a drink exactly one hour after consuming the tablet is due to the relatively short half-life of the medication. To get the full benefits of naltrexone combined with alcohol, to essentially erase the alcohol addiction from the brain, it is important that drug levels are at their peak.

For most people taking a 50 mg dose of naltrexone, one hour is about the best time period to be certain that the drug has been absorbed into their system, and it has not started to wear off significantly yet. If the person following TSM drinks too soon or too late, they will not get the full benefit of naltrexone.

How does an alcoholic following The Sinclair Method keep from drinking more alcohol after the first drink?

Addiction doctors and family physicians are often hesitant to recommend TSM, because they are concerned that an alcoholic patient will not be able to stop drinking once they get started. In most cases, this is a legitimate concern.

When a person is addicted to a substance, after consuming the substance, they develop a physical compulsion to keep going. They are often unable to stop drug abuse or alcohol abuse until they are stopped by an external force.

That external force could be running out of money, drugs or alcohol, getting in a car accident, passing out, or getting arrested. An addiction run often plays out until serious consequences occur.

However, TSM changes the way the drinker experiences their alcoholic beverage. Naltrexone significantly reduces the feeling of compulsion to continue drinking.

By removing the endorphin reward feeling that usually comes with taking a drink, the person following TSM can more easily stop at one drink. Alcohol tastes the same to them, but something is different.

One person once told me that drinking after naltrexone felt similar to having a drink after brushing their teeth. Something about drinking was not the same, and it was not the expected pleasurable experience.

It is incredible how a person feels differently when they drink after taking naltrexone. Yet, it is very important to be aware of how long naltrexone lasts when following The Sinclair Method.

The person following TSM must be aware of the time, and they must plan their drinking and when they take naltrexone carefully. Additionally, they must not drink without taking naltrexone first.

Can a person following The Sinclair Method take naltrexone after they drink if they forget to take it before?

Unfortunately, taking naltrexone after a drink will not help much to reduce alcohol consumption. The key to being successful is to take the tablet before taking a drink, and giving it time to work.

Some people who have tried taking naltrexone later, after they are already drinking, have described feeling sick from the effects of naltrexone. Still, for other people, it may still be helpful to take the medication after the first drink, in hopes that it may slow down the current drinking binge.

Not everyone is going to be perfect, or even nearly perfect, in their use of naltrexone to quit drinking, when they first get started. If they do not get it right the first time, they can learn and follow the directions better the next time.

What happens if a person following TSM is out with friends or family, and they are offered an alcoholic beverage at a restaurant? If they do not have naltrexone with them, what will happen?

In this situation, the best thing to do is not to take a drink at all. Without naltrexone, the person will be at risk for having a drinking binge, and it will be a setback in their TSM program.

A better solution is to always carry a naltrexone tablet everywhere they go. There are keychain storage devices that are made to carry a small supply of pills. Many TSM successes carry naltrexone with them everywhere.

When is the best time to take low dose naltrexone?

Low dose naltrexone is very different from the naltrexone 50mg tablet typically used by TSM patients. Low dose naltrexone, or LDN, is usually made by a compounding pharmacist, and it is typically in the range of 0.5mg to 6mg.

There are also very low dose naltrexone or ultra low dose naltrexone protocols. With these ultra low dosages, they may be at or below 0.1mg, or even in the microgram dosage range.

Why would someone take such a small amount of the drug? How can it possibly be effective?

Interestingly, there are medications that have completely different effects at different dosages. Naltrexone is one of these drugs.

At the level of LDN or ULDN, naltexone works by blocking the opioid receptors for a short time. Because of the short half-life and the low dosage, the receptors are only occupied for a brief time.

As a result, the body responds by giving signals to increase the production of natural endorphins. LDN is used for a variety of conditions.

Chronic pain syndromes and autoimmune disease are conditions that may respond to LDN therapy.

In the United States, it may be hard to find a doctor who is knowledgeable about LDN, but they are out there. Many compounding pharmacies are familiar with LDN protocols. They are comfortable making customized LDN capsules for their patients.

The timing of taking LDN depends on the patient, their condition, and what they are comfortable with. Some people take their compounded LDN in the evening, before bedtime.

Others may take LDN in the morning. The important thing is to limit LDN consumption to once daily, in most cases.

While it may seem like more would be better, in the case of LDN, less is better. It may seem counterintuitive, but with LDN, the dosages work best when they are very low.

What is the best way to learn more about how long naltrexone lasts and how to use this knowledge to understand naltrexone treatment better?

You may be interested in listening to our naltrexone podcast to learn more about naltrexone, and how long it lasts. It is important to have some understanding of how long naltrexone lasts in using it for specific treatments.

We also have a variety of articles on this website about the topic of naltrexone treatment. To find more information on these treatments, simply type the name of the drug in the search box.

Another great source of medical information is your doctor. Ask your doctor about naltrexone for TSM, or LDN therapy for various conditions.

If your doctor is not aware of these therapies, they may be interested in researching them further. Your doctor may ask to discuss these therapies in a future visit, after they have time to do some reading.

Another option is to visit a naltrexone doctor who is experienced in prescribing naltrexone for specific conditions, such as alcohol dependence, or various conditions that may respond to LDN.

A private naltrexone doctor can answer your questions about naltrexone. And, the same doctor may be able to provide treatment if and when you are ready to get started.