Side effects of naltrexone

Dangers of Combining Naltrexone and Alcohol

The opioid antagonist naltrexone (brand names: ReVia, Vivitrol, and Depade) is approved to treat those who abuse opioid medications or alcohol. The drug comes in a pill form (Depade and the more popular version ReVia) and as an extended-release injectable form (Vivitrol). Naltrexone is designed to reduce and suppress cravings for alcohol or opiate drugs. It does this by binding to the opioid receptors in the person’s brain (thereby removing any opiate drugs on these receptors) and suppressing cravings.

Naltrexone is considered to have no abuse potential and does not result in the development of physical dependence. An individual must obtain a prescription in order to legally obtain it, and the medication is typically used in situations where individuals are actively recovering from alcohol use disorders or opiate abuse.

Naltrexone does not treat withdrawal symptoms; rather, it is designed to suppress cravings for alcohol or opiate drugs. Individuals with moderate to severe alcohol use disorders who are using naltrexone may experience withdrawal symptoms if they stop drinking that can be potentially fatal due to the development of seizures. These individuals should consult with an addiction medicine physician or psychiatrist before discontinuing their use of alcohol.

Research Findings

The standard method of using naltrexone is for individuals in recovery from alcohol use disorders or opiate use disorders to take the medication in the morning while trying to remain abstinent from these drugs.

Research findings are mixed, but overall, they tend to support the notion that individuals who use naltrexone to treat alcohol abuse reduce the total amount of alcohol they consume and observe a reduction in the number of times they drink alcohol. In addition, heavy drinkers often notice significant reductions in alcohol use. However, the research does not indicate that the use of naltrexone is effective at assisting individuals in remaining totally abstinent, but it does most likely result in a significant reduction in cravings for alcohol and an overall reduction in the amount of alcohol consumed.

Like any drug, naltrexone can only work if an individual uses it, and there is evidence to suggest that issues with compliance often reduce its effectiveness.

Research findings do not suggest that naltrexone is a cure-all for alcoholism. Rather, taking naltrexone should be accompanied by formal substance abuse treatment.

Naltrexone is considered safe to use and associated with few side effects; however, all medications have a side effect profile. Side effects as a result of naltrexone use are reported to be relatively rare, but they do occur in some instances.

  • Nausea, stomach cramps, and diarrhea are the most common reported side effects; however, these typically resolve over time.
  • Some individuals may experience muscle stiffness, cramps, and headaches.
  • Sleep disruptions (including both insomnia and hypersomnia), anxiety, and dizziness have also been reported.
  • Individuals should not use opiate drugs while taking naltrexone. People who use opiate drugs and take naltrexone may experience opioid withdrawal symptoms as naltrexone is an opioid antagonist. The Food and Drug Administration (FDA) recommends that individuals who use naltrexone should be abstinent from opioid drugs for a week to 10 days. Because naltrexone is an opioid antagonist, people using it and who also use opioid medications for their psychoactive effects will not experience the typical “high” that they get from opiate drugs. This may result in individuals taking more opiate drugs than they normally would and potentially overdosing on opiates.
  • Pregnant women should not use naltrexone.

Drinking Alcohol while Taking Naltrexone

There appear to be no significant dangers associated with taking naltrexone and drinking alcohol. Information provided by the FDA and bythe National Institute on Alcohol Abuse and Alcoholism(NIAAA) report that individuals who drink alcohol and use naltrexone:

  • Will still experience the functional impairments that are associated with alcohol use, such as a loss of motor coordination, decreased response time, problems with slowed rates of thinking, etc.
  • May experience less of an urge to drink more alcohol
  • May reduce their alcohol intake

Thus, research supports the notion that naltrexone is effective in reducing alcohol intake but not effective in promoting abstinence from alcohol. Individuals in these studies often continued to drink alcohol while on naltrexone, and there were no significant or dangerous effects noted. In fact, one method of treating alcohol use disorders known as the Sinclair Method suggests that individuals take naltrexone about one hour before they begin drinking alcohol. At least one research study has suggested that taking naltrexone in this manner (only taking the drug one hour before one is planning to drink alcohol) results in a significant reduction in alcohol cravings and intake compared to the suggested use of naltrexone, which is to take it in the morning and attempt to remain abstinent from alcohol. The developer of this method, Dr. Sinclair, reported that using naltrexone before drinking alcohol in this manner is significantly more effective in reducing alcohol intake than using naltrexone as an attempt to help the person become or remain abstinent from alcohol. These research reports still need further investigation and replication.

Using naltrexone in conjunction with alcohol will not:

  • Result in a person becoming significantly more or less intoxicated based on the amount of alcohol they have drank
  • Cause the person to become violently ill in the same way that Antabuse (disulfiram) does
  • Reduce the short-term effects of alcohol use/abuse (unless the individual drinks less alcohol as a result of using naltrexone)
  • Reduce any long-term effects associated with chronic alcohol abuse, including liver damage, cardiovascular damage, kidney damage, an increased potential to develop cancer, and an increased potential to develop neurological issues, such as stroke, seizures, or even dementia (unless the use of naltrexone results in the individual drinking significantly less alcohol over time)
  • >Reduce any cognitive issues associated with becoming intoxicated, such as issues with judgment, memory, mood swings, etc. (unless the person’s use of naltrexone results in them drinking significantly less alcohol)

Conclusions

There appear to be no recorded significant dangers of drinking alcohol while taking naltrexone. There is research that suggests that the drug may be more effective in reducing alcohol intake if it is taken prior to drinking alcohol as opposed to using it and attempting to remain abstinent from alcohol. This research needs to be replicated.

5. Answers to Frequently Asked Medication Questions2

(2 Adapted from Rounsaville, B.J.; O’Malley, S.; and O’Connor, P. “Guidelines for the Use of Naltrexone in the Treatment of Alcoholism.” New Haven, CT: APT Foundation, 1995. Reproduced with the permission of DuPont Pharma.)

5.1. Naltrexone

1. What is naltrexone, and how does it work? Naltrexone is a medication that blocks the effects of drugs known as opiates, or narcotics (a class that includes morphine, heroin, or codeine). It competes with these drugs for opioid receptors in the brain. Originally used to treat dependence on opiate drugs, it now has also been approved by the U.S. Food and Drug Administration (FDA) as treatment for alcohol dependence. People who are dependent on opiate drugs, such as heroin or morphine, must stop their drug use at least 7 days prior to starting naltrexone. Some people should not take naltrexone, such as those suffering from chronic pain who rely on opioid painkillers or people with liver failure or acute hepatitis. Although the precise mechanism of action for naltrexone’s effect is unknown, reports from successfully treated patients suggest the following three kinds of effects:

  1. Naltrexone can reduce a patient’s urge or desire to drink.

  2. Naltrexone helps patients remain abstinent.

  3. Naltrexone can interfere with the patient’s desire to continue drinking more if he/she slips and has a drink.

In most clinical trials evaluating the effectiveness of naltrexone, subjects who received naltrexone were significantly more successful in remaining abstinent and in avoiding relapse than were those receiving an inactive placebo pill.

2. Is it possible to become addicted to naltrexone?

No. Naltrexone is not habit forming or a drug of abuse. It does not cause users to become physically or psychologically dependent.

3. What are the side effects of naltrexone?

In a large open-label safety study on naltrexone, conducted by Dupont Pharma in 570 individuals with alcoholism, the most common side effects affected only a small minority of people; they included the following:

  • Nausea (10 percent of participants)

  • Headache (7 percent of participants)

  • Depression (5 to 7 percent of participants)

  • Dizziness (4 percent of participants)

  • Fatigue (4 percent of participants)

  • Insomnia (3 percent of participants)

  • Anxiety (2 percent of participants)

  • Sleepiness (2 percent of participants).

These side effects were usually mild and of short duration. Patients usually report that they are largely unaware of being on naltrexone. Naltrexone usually has no psychological effects, and users do not feel either “high” or “down.” Naltrexone can have toxic effects on the liver. A patient receives blood tests of liver function prior to the onset of treatment and regularly during treatment to determine if he/she should take it at all, if he/she should stop taking it, or if he/she experiences the relatively rare side effect of liver toxicity. Patients should report any side effects to their medical clinician.

4. What will happen if a patient drinks alcohol while taking naltrexone?

Naltrexone does not reduce the effects of alcohol that impair coordination and judgment. Naltrexone may reduce the feeling of intoxication and the desire to drink more, but it will not cause a severe physical response to drinking.

5. Is it all right to take other medications with naltrexone?

Patients should carry a card explaining that they are taking naltrexone, and it should instruct medical staff on pain management. Naltrexone does not reduce the effectiveness of local and general anesthesia used with surgery. However, it does block pain relief from opiate medications. Many pain medications that are not opiates are available. Patients having elective surgery should stop taking naltrexone at least 72 hours beforehand.

The major active effect of naltrexone is on opiate (narcotic) drugs, which is one class of drugs used primarily to treat pain but is also found in some prescription cough preparations. Naltrexone will block the effect of normal doses of this type of drug. There are many nonnarcotic pain relievers patients can use while on naltrexone.

Otherwise, naltrexone is likely to have little impact on other medications patients commonly use such as antibiotics, nonopioid painkillers (e.g., aspirin, acetaminophen/Tylenol, ibuprofen/Motrin/Advil), and allergy medications. Patients should inform their medical clinician of the medication they are currently taking so that possible interactions can be evaluated. Because the liver breaks down naltrexone, other medications that can affect liver function may affect the dose of naltrexone.

6. What will happen if a patient becomes pregnant while taking naltrexone?

Patients with the biological potential to have a child should be using an effective method of birth control while taking naltrexone. However, if they miss a menstrual period, they should report this to their medical clinician at once and take a pregnancy test.

If a patient becomes pregnant, she will discontinue the medication. The medical clinician should continue to ask after her health throughout her pregnancy as well as the health of her baby after delivery.

7. Should naltrexone be taken with a meal?

There is no information that taking naltrexone with or without meals makes any difference in effect.

8. What happens if a patient stops taking naltrexone suddenly?

Naltrexone does not cause physical dependence, and patients can stop taking it at any time without experiencing withdrawal symptoms.

9. If patients take naltrexone, does it mean that they don’t need other treatment for alcohol dependence?

No. Research studies have shown that naltrexone was most effective when it was combined with treatment from professionals and/or mutual-support groups.

10. What is the relationship of naltrexone to AA and other support groups?

There is no contradiction between participating in support groups and taking naltrexone. In fact, one multisite study showed that naltrexone-taking subjects who attended mutual-support groups, such as AA, had better outcomes. It is most likely to be effective for patients whose goal is to stop drinking altogether. If other mutual-support group members caution against taking any medications, patients should refer them to the pamphlet “The AA Member—Medications and Other Drugs,” which explicitly states that AA members should not “play doctor” and advise others on medication provided by legitimate, informed medical practitioners or treatment programs.

5.2. Acamprosate3

1. What is acamprosate, and how does it work?

Acamprosate is a new, investigative medication for treatment of alcohol dependence approved in several European countries, and it is currently being studied in clinical trials in the United States. It is thought to reduce the urge for alcohol by working directly on certain neurotransmitters in the brain (chemicals that transmit information between nerve cells) whose balance has been disturbed because of regular, heavy drinking.

Although acamprosate can be used in the United States only with permission of the FDA, it has been available in Europe since 1989 and has recently been approved for marketing by prescription in more than 12 European countries, including Belgium, France, Germany, Ireland, Italy, the Netherlands, Spain, Switzerland, and the United Kingdom. It is estimated that more than 1 million patients have been treated with acamprosate since it became available.

2. Is acamprosate addictive?

No. Acamprosate is not habit forming or a drug of abuse. It does not cause users to become physically or psychologically dependent.

3. What are the side effects of acamprosate?

Like virtually all medications, acamprosate can cause side effects, but these are usually minor and go away as patients continue to take the medication. In European controlled clinical trials, the only types of symptoms that were consistently more common in subjects taking acamprosate than in subjects taking placebo were stomach symptoms. These were usually mild, tended to occur when subjects first started taking the medication, and consisted primarily of loose bowel movements or mild diarrhea. Some subjects also had changes in their sex drive—sometimes this was increased and sometimes decreased, but there was no definite pattern. As with many drugs, sometimes people on acamprosate develop skin rashes or itching. In earlier studies, subjects on acamprosate and those on placebo both experienced equal amounts of this type of symptom. Patients should tell their medical clinician of any side effects.

4. What will happen if a patient drinks alcohol while taking acamprosate?

Acamprosate does not change the way the body metabolizes alcohol, so acamprosate will not make patients feel sick if they drink (i.e., it does not work like Antabuse). In addition, there is no evidence of an added effect of alcohol if the patient drinks while taking acamprosate.

5. Is it okay to take other medications with acamprosate?

Because acamprosate is eliminated exclusively by the kidneys, drugs that may be toxic to the kidneys, such as aminoglycoside antibiotics (gentamycin and amikacin), should be avoided. Patients should inform their medical clinician of whatever medication they are currently taking so that possible interactions can be evaluated.

6. What will happen if a patient becomes pregnant while taking acamprosate?

Patients with the biological potential to have a child should be using an effective method of birth control while taking acamprostate. However, if they miss a menstrual period, they should report this to their medical clinician at once and take a pregnancy test.

If a patient becomes pregnant, she will discontinue the medication. The medical clinician should continue to ask after her health throughout her pregnancy as well as the health of her baby after delivery.

Even though acamprosate should not be used during pregnancy, animal studies have not shown any ill effects on either the course of pregnancy or on the offspring, nor is there any evidence from animal studies that acamprosate causes birth defects.

7. Should acamprosate be taken with a meal?

Acamprosate can be taken with food, but food does decrease the amount of medication that the body absorbs. Gastrointestinal symptoms may decrease by taking the medication with food.

8. Is it all right to crush the pills?

Acamprosate pills should not be crushed because they have an enteric coating. Destroying this coating can lead to a worsening of gastrointestinal side effects.

9. What happens if a patient stops taking acamprosate suddenly?

Acamprosate does not cause physiological withdrawal symptoms when it is stopped.

10. What happens if patients miss a dose?

If patients miss a dose of acamprosate, they should not take it simultaneously with the next scheduled dose; there should be a minimum of 2 hours between doses. If this is not feasible, they should not take the skipped dose. Instead, they should wait until their next scheduled dose and take only that dose.

11. If patients take acamprosate, does it mean that they don’t need other treatment for alcohol dependence?

No. Research has shown that acamprosate was most effective when it was combined with treatment from professionals and/or mutual-support groups.

12. What is the relationship of acamprosate to AA and other mutual-support groups?

There is no contradiction between participating in support groups and taking acomprosate. It is most likely to be effective for patients whose goal is to stop drinking altogether. If other mutual-support group members caution against taking any medications, patients should refer them to the pamphlet “The AA Member—Medications and Other Drugs,” which explicitly states that AA members should not “play doctor” and advise others on medication provided by legitimate, informed medical practitioners or treatment programs.

Sofa King Next Level

Look at all the new, beefed up Opioid Growth Factor receptors formed on the cell as a result of LDN… So fluorescent!

I’m definitely into low-tech solutions in life: food over synthetic vitamins, fecal transplants over antibiotics (ew gross, right? I talk a big game but it’s not like I’ve ever tried it). However when I started reading about Low Dose Naltrexone last summer, I just couldn’t get it out of my head. Low Dose Naltrexone, known as “LDN”, is safe, cheap, essentially free of side-effects, and remarkably effective at treating a ridiculously long list of ailments, particularly auto-immune disorders, cancer, AIDs and chronic pain.

Most patients with auto-immune disorders (such as Crohn’s Disease, Multiple sclerosis, Hashimoto’s, Rheumatoid Arthritis, Grave’s disease, Lupus, Psoriasis, Alopecia etc.) are put on a regimen of immunosuppressant drugs. Logically this makes sense, because the patient’s immune system is attacking itself – so if you suppress the immune system it loses ammunition for attack. This usually works pretty well at keeping auto-immune disorders at bay. However, and this is a very big however, when you suppress a patient’s immune system she takes on a higher risk for everything from the common cold to Cancer. This is what I call treating the disease at the expense of the patient.

However if you are living with an autoimmune disease, you are probably in chronic pain of one sort or another, and would rather live with a shorter amount of good years than a longer life in pain. There are a million really good reasons to take immunosuppressive drugs, and not a lot of alternatives.

There are many, many different kinds of immunosuppressive drugs at this point, and they all invariably have some acute side effects. But on the positive side, they usually work by a two-fold mechanism: first they act by suppressing the immune system, either by inhibiting the genes that code for T cell proliferation, or by inhibiting B cell and various antibody production; secondly immunosuppressive drugs are usually also strong antioxidants, so that they work by reducing inflammation in the body which tends to reduce immune system reaction (or over-reaction in the case of auto-immune disorders).

I think we can agree that the while the T/B cell reduction is a dicey move if you’re playing a long game, at least the antioxidant part of the drugs is probably very helpful. After all, inflammation seems to be the cause of just about every problem, so curbing it is pretty useful. (Inflammation has its purpose when you have a physical trauma or infection that needs to be sealed off from the rest of the body and healed – but is overkill as a reaction to food choices, stress, and small environmental inputs. More on inflammation another time!).

HERE’S WHY “LDN” IS DIFFERENT

Rather than suppressing the immune system, Low Dose Naltrexone works on another level “upstream” in the healing cascade and appears to regulate the immune system. Some of the doctors (Dr. Ian Zagan et al) who are developing LDN for autoimmune issues claim that it is immunosuppressive, but while this is technically true – LDN is actually concurrently immunostimulating. It seems to be able to curb inappropriate immune responses while simultaneously increasing immune function. In other words, it helps auto-immune diseases without compromising the patient’s immune system. So it’s basically a miracle. People who take LDN only get sick very rarely, if at all, and do not suffer from prolonged infections the way they would if taking proper immunosuppressant drugs.

FIRST, WHAT IS NALTREXONE? SOUNDS INTENSE

Naltrexone is a drug that was first synthesized in the 1960s in America, and determined as an opiate agonist, meaning it could block opiates so that the subject taking naltrexone would not feel the effects of opium and heroin. There was little market value for naltrexone, however the US Governement stepped in and paid for extensive clinical trials hoping it could be used to cure heroin addiction and other drug ills of society. Naltrexone was determined to be completely safe, to have no negative side effects, and to be useful even during pregnancy and breastfeeding – which is very rare for any drug. By the time the trials were completed, the drug was already off patent – though the government extended the patent to DuPont for another seven years. In the ’80s, DuPont started marketing naltrexone as a treatment for alcoholism as it causes drinkers to feel none of the pleasant effects of alcohol yet all of the unpleasant effects. As you can imagine, the biggest issue was patient compliance. Naltrexone never really took off as a treatment for anything, and as of now is off patent, of little value to manufacturers and available pretty freely on the internet without a prescription (!).

One of the main things naltrexone does is bind with Opioid Growth Factor Receptors (OGFr), which are on every cell in the body, and blocks them so that Opioid Growth Factor (OGF) molecules cannot bind to them. When OGF binds with OGFr, cell growth and division is regulated. When OGFr’s are blocked, the cells respond in three ways: by spontaneously creating new OGFr’s on the surface of every cell, by making those new OGFr’s more sensitive, and by increasing the amount of Opioid Growth Factor released in the body. The terms are often used interchangeably, but when I am talking here about “opioids” I mean the natural endorphins created by the body; when I talk about opiates I am using a blanket term for the various natural and synthetic external drugs that act on the central nervous system like morphine, codeine, heroin, oxycodone, alcohol and even sugar and dairy.

In normal naltrexone therapy (full dose), the patient doesn’t get to benefit from the increased amount of more sensitive OGF receptors nor the surplus of circulating OGF caused by the naltrexone because the patient takes another dose and all the OGF receptors, including the new ones, continue to be blocked. And in fact if the patient has other problems, like AIDs or cancer, those problems will get worse. So it was determined by Dr. Bernard Bihari in the 1980s that OGF and OGFr play a tremendous role in healing, and that by blocking them healing is grossly impaired.

HERE’S HOW THE “LOW DOSE” WORKS INSTEAD

A regular dose of naltrexone is between 50mg and 200mg per day. A “low dose”, however, is between 1mg – 5mg per day – much less than 10%. It is available online at 4.5mg compounded doses, which is usually where people start when they are experimenting on their own because they can’t get their doctor to take an interest in it and prescribe it for them.

When you take a “low dose” of 4.5mg, the suggestion is to take it at 10pm. By 2am, the dose is fully working and manages to block your OGF receptors for about two hours, until 4am. What happens during these two sleeping hours is that the body panics and makes more OGF, more OGF receptors and makes these new receptors more sensitive. However when the drug wears off at 4am, you are left with the benefit of all these extra sensitive receptors and a surplus of OGF. You experience a rebound effect which supercharges healing.

It isn’t all about the OGF and OGFr. There are many other endorphins which are blocked and then subsequently rebound to become more effective. Some of them have been studied. Some are still unknown. A pubmed search for LDN comes up with some fifty-four thousand hits on its efficacy for fibromyalgia, multiple sclerosis, Crohn’s disease etc. It is also being used in at least three different fertility clinics around the world, which suggests it is not only safe for pregnancy but also effective for women trying to get pregnant.

SOME TIPS

If you are going to bother to try this out, you might as well go for the best experience. As LDN is an opiate agonist, it works best when there aren’t any opiates in your system! It may be easy enough for you to avoid heroin and oxycodone, but it is more difficult to avoid everyday minor opiates like sugar, dairy and any excess of carbohydrates. If you are going to go out and drink alcohol one night, skip the LDN at bedtime and start again the next night. (If you drink alcohol on a full dose of naltrexone, it can actually make you really sick).

If you want to try this because you have auto-immune disease, you should know that people don’t have the best response when they continue to take their immunosuppressant drugs at the same time. It has been described as trying to drive (taking LDN) with the brakes on (immunosuppressant drugs). However that’s a pretty big decision that you shouldn’t make impulsively just from reading a blog post.

WARNINGS

This isn’t just some natural herb that has always been around and tested by thousands of years of civilization. Natrexone is a synthesized drug – serious business. Even though LDN is in an incredibly small dose, it still makes meaningful changes to your body. Fortunately, just about all of the meaningful changes are positive. However there remains one common side effect:

The side effect is that in the first three to seven days, people who take LDN at night tend to experience vivid dreams that seem to last forever, and sometimes experience nightmares. After a week at most, the body becomes conditioned and the potential for bad dreams is gone.

That is the only negative side effect.

A positive side effect is that people tend to sleep more restfully, their auto immune disease stops progressing or regresses, their chronic pain is lessened, etc. This is being used to reverse both AIDs and cancer, and the doctors doing these trials not only take LDN themselves as a preventative, but have their spouses take LDN as preventatives. It seems to have powerful inhibitory effects on tumor cell proliferation.

MY STORY

I don’t have any auto immune diseases, though I continue to be very interested in them. However I have some special friends who I thought could benefit from Low Dose Naltrexone. I gave them some reading, which they brought along to their doctors. But since their doctors had never heard of it, they all thought it was dangerous and wouldn’t read about it. So I found a way to order LDN online without a prescription, and then proceeded to “test” the product to see if the lack of side effects story was true. I am generally very healthy and thought I would be able to notice anything negative fairly quickly.

In my first three nights taking 4.5mg of LDN, I experienced extremely vivid dreams which momentarily turned dark. These dreams felt like they were days and days long. Having been an insomniac my entire life, and having tried every sedative and sleeping pill on the market, I was very surprised that within half an hour of taking LDN I felt pleasantly tired and fell asleep. Although I normally wake up a couple times during the night, sometimes for hours, instead I slept through until the morning. The vivid dreams remained for three nights and then stopped. However I continued to have an easy time falling asleep and staying asleep. My entire quality of life has changed for the better.

Usually sleeping pills (such as Trazadone, Atavan, Seconal, Neo Citran, NyQuil etc) would give me a feeling of intense physical drowsiness that would drug me to sleep but not help me stay asleep; also the effect would wear off after a week unless the dose was raised. This was never a good solution for me, so I stuck with natural remedies like intermittent melatonin, valerian, magnesium, meditation and elaborate bedtime rituals. But mostly I had just come to accept that I was never going to have an easy time falling asleep and getting the rest I needed.

There is no literature linking LDN with curing insomnia. In fact, most patients report the opposite effect – that LDN initially gives them vivid dreams and restless nights. However for some reason this has worked for me, and I am deeply grateful for the sleep that now forms a regular part of my life.

MY RAT FRIENDS

My one friend who tried LDN to deal with chronic pain went from taking 6 Aleve pain pills a day to taking none. However she found the 4.5mg/day dose made her sleep too much, so she reduced her dose to 3mg yet has maintained the same reduction in chronic pain.

My other friend with auto immune disease could not risk stopping her immunosuppressant prescriptions so tried LDN at the same time. She did not have any noticeable benefit except good quality sleep; if anything, she experienced some of the worst flare ups she had ever had, requiring her to increase her doses of immunosuppressants. Putting the car in drive while the parking brake was on didn’t work for her.

BUT IS IT REALLY SAFE?

I started going to a fancy private doctor so that I could get every blood test ordered and every hormone level checked. I wanted to be able to say without a doubt that eating LCHF (Low Carbohydrate High Fat) and doing all my weird things isn’t just making me “feel” healthier, but is actually making me healthier. So I came clean to my new doctor about taking LDN without a prescription. She was not excited, and urged me to stop taking it, and offered me some good alternatives for sleep aids (holy basil tea etc)…

However three months later, my doctor got back to me after having done her own research on LDN. She said not only did she think it was extremely safe, and probably a great prophylactic against cancer and the diseases of aging, but that she would write me a prescription herself.

I have settled on a dose of 3mg/night at 10pm. When I travel, I take it at 10pm in whatever time zone I am in. I skip it whenever I drink more than a single glass of wine.

NOW GO DO YOUR OWN RESEARCH

Fortunately there is a lot of research available on Low Dose Naltrexone. Right now (July 2014) there are dozens and dozens of clinical trials taking place for myriad auto immune diseases, AIDs, cancer etc. There is a non-profit website devoted to organizing resources for LDN. There are thousands of users online sharing their stories of successes and failures. And there is a small window where LDN is still under the radar and so loosely monitored that you can order it for yourself without too much fuss.

WHY DID I CALL THIS A “NON-PHARMA” PHARMACEUTICAL?

LDN is a “People’s Medicine” because it is extremely safe, non-toxic, inexpensive, off-patent, easy to get, and incredibly effective. This is a “non-pharma” pharmaceutical because there is barely any profit to be made off of it. A single 50mg generic naltrexone pill can be bought off the internet for less than $6. Dissolved in 50ml of distilled water, a regular person can use a calibrated medicine dropper to administer 3ml at a time for less than $0.40/dose. If LDN cures your cancer, it’s a great bargain. If it doesn’t, you only risked $135 for a year’s supply.

FURTHER READING

The Low Dose Naltrexone Homepage is a non-profit website devoted to the latest news and information about LDN

LDN SCIENCE: A group of researchers pooling their clinical trials and information

LDN Research Trust: resources, videos and conferences in the UK. THEIR DOCTORS CAN ARRANGE TO GET YOU A PRESCRIPTION, REGARDLESS OF YOUR COUNTRY, IF YOUR DOCTOR WILL NOT.

This book, The Promise of Low Dose Naltrexone Therapy, from Amazon is useful but already over six years old – you have to go online to find more recent updates and news. However this is a good start if you want a solid book in your hand to take to a doctor.

LDN for chronic pain sufferers, a citation from Clinical Rheumatology publication

A presentation about LDN used to boost fertility in cases with low ovarian reserve (low AMH)

The serendipitous discovery of low-dose naltrexone (LDN) spurred a revolution in the background of medicine. Although still an experimental and unapproved approach, scientists are researching if LDN can help people with autoimmune diseases, chronic pain, inflammation, and fatigue. Read on for more about its potential uses.

Disclaimer: LDN is not FDA-approved for pain or any other indication. It is still a highly experimental approach. The aim of this post is to outline scientific research for informational purposes only. If you are interested in LDN, it is important to talk to your healthcare provider about its possible effectiveness, side effects, and risks.

What is Naltrexone?

Naltrexone is a drug that blocks the activity of opioids in the brain. Your body normally produces endorphins and enkephalins, natural opioids that contribute to feel-good sensations. In fact, these chemicals are the body’s most powerful reward and pleasure system .

The opioid blocker naltrexone was synthesized in the 60s and approved in the 80s for treating opioid addiction .

Doctors gave naltrexone to opioid addicts in recovery to prevent relapse. The rationale was to completely shut off the ‘high’ of abused narcotics. By blocking all receptors in advance, naltrexone renders narcotics powerless.

Opioid drugs are strong painkillers that can cause addiction if abused. Naltrexone was used to block their effects and treat addiction in the past.

Note: Naltrexone shouldn’t be confused with naloxone (Narcan), although both drugs are opioid blockers. You may have heard about naloxone kits (spray or injection) that can save lives in opioid overdose. Naloxone is a better choice for reversing overdose because it starts to act faster and lasts for a shorter time, as is desirable in emergency situations. Naltrexone, on the other hand, takes a couple of hours just to kick in .

Snapshot

Proponents

  • Used off-label for autoimmune diseases, chronic pain, and inflammation
  • Claimed to increase natural opioids and balance the immune system
  • Limited studies suggest side effects are mostly rare and mild
  • Likely few drug interactions

Skeptics

  • Large-scale studies lacking
  • Not enough data to rate effectiveness
  • Unapproved, unofficial use (off-label)
  • Dosing usually has to be adjusted to each individual
  • Use largely relies on clinical expertise
  • Long-term safety unknown

Potential Uses of Low-Dose Naltrexone

Insufficient Evidence for

The following purported benefits are only supported by limited, low-quality clinical studies.

There is insufficient evidence to support the use of LDN for any of the below listed uses. LDN should never be used as a replacement for approved medical therapies.

1) Autoimmune Conditions

Anecdotes

According to Dr. Bihari, LDN might support a healthy immune response by rebalancing T-helper cells, the so-called “master cells” of the immune system. People with autoimmune issues tend to have impaired T-helper cell function .

A specific subtype of these T-helper cells are Tregs (5% – 10%), which are thought to be responsible for suppressing harmful Th1, Th2, and Th17 overactivation. Scientists think they prevent the immune system from going into an autoimmune overdrive and attacking itself .

The whole hypothetical basis for these potential effects stems from Dr. Bihar’s claims about LDN boosting endorphins. Higher endorphins are thought to subsequently rearranging of cells in the immune system. This mechanism hasn’t been proven .

Although Dr. Bihari claimed that LDN can help people with a range of autoimmune diseases (including lupus, rheumatoid arthritis, eczema, and psoriasis), clinical studies have yet to verify his claims.

Scientists are also investigating whether LDN blocks the activation of microglia, a type of immune cell in the brain and nervous system. Microglia normally stay in a resting state and are woken up only by brain damage or infection .

Their activation is considered to underlie common symptoms in autoimmune and other diseases (see “sickness behavior”): fatigue, fever, inflammation, and pain .

Conditions that have been at least partially researched are listed below.

Some doctors claim that LDN may also help with other diseases with an autoimmune component, such as Hashimoto’s. Anecdotally, it improves thyroid health, lowers antibodies and the need for additional drugs. Research is completely lacking to support these uses, though.

LDN is hypothesized to affect autoimmune disorders by boosting endorphins and rebalancing the immune system via T-helper cells. Clinical trials are yet to confirm this.

Multiple Sclerosis (MS) Studies

The evidence to support LDN use in MS is conflicting. Future trials are yet to determine its safety and effectiveness.

In one study of 96 people with MS, 8 weeks of LDN (4.5 mg/day) did not provide more relief than placebo .

In contrast, LDN improved mental health and quality of life in another pilot study of 60 people with MS, using a similar protocol .

One study tracked 4 women with MS prescribed LDN, suggesting that it might be safe under medical supervision. Women who took LDN didn’t report any side effects and their symptoms stabilized or improved, as did their quality of life and fatigue. We can’t, however, draw any conclusions from a report on four people .

Evidence on LDN in MS patients is mixed. Larger trials should investigate this further.

Rheumatoid Arthritis & Fibromyalgia Research

As with MS, there’s insufficient evidence to rate LDN for rheumatoid arthritis and fibromyalgia. Only a couple of small studies have been carried out, while proper clinical trials are lacking.

In a low-quality study of 10 people with rheumatoid arthritis, LDN reduced joint pain and swelling. A few weeks after they stopped taking LDN, most experienced periods of severe stress and disease worsening .

Fibromyalgia is not technically classified as an autoimmune disease, although it triggers many of the same symptoms. Initial LDN research seems to offer some hope for people suffering from this otherwise hard-to-treat disease, but it’s too early to say whether it works .

A group at Stanford University found that LDN (4.5 mg/day) reduces pain, fatigue, inflammation, and stress in people with fibromyalgia while boosting mood. LDN was safe and well-tolerated .

Another small clinical trial uncovered that people with fibromyalgia have lower endorphins or a “low opioid tone.” LDN reversed their low levels, thereby improving pain tolerance. Interestingly, it also enhanced the patients’ ability to relate interpersonally and engage in relationships .

On the one hand, this hints at the potentially profound physical and emotional effect of endorphins.

On the other hand, these findings indicate that scientists are still just scratching the surface. Much more research on the impact of LDN on people with fibromyalgia and autoimmune diseases is needed.

LDN is being researched for boosting opioids and relieving pain, fatigue, and stress in people with fibromyalgia, but the data are inconclusive.

2) Pain and Inflammation

There is not enough evidence about the use of LDN for chronic pain conditions. However, some doctors prescribe LDN off-label for this indication. Proper clinical research is needed to support this experimental practice.

CRPS

Complex regional pain syndrome (CRPS) is a form of chronic pain that can be excruciating. Limited research suggests that it is worsened by SIBO, obstructive sleep apnea, and microglial activation in the brain .

By keeping the microglia in a resting state and increasing endorphins, low-dose naltrexone is hypothesized to reduce the pain and inflammation in CRPS. Yet, no clinical trials back up this use .

A lot of people with CRPS experience a movement disorder called dystonia, which causes painful muscle contractions. In a report, LDN lowered pain and dystonia in two people with CRPS. The authors claimed that it worked by silencing microglia that trigger inflammation and pain .

However, we can’t know if LDN affects CRPS symptoms based on this case report. Its safety and effectiveness need to be explored in proper human studies.

Some researchers are also investigating whether LDN can also enhance the pain-relieving effects of acupuncture, which people with CRPS might benefit from .

In animals and cells, LDN increases the number of receptors for opioids and cannabinoids, which might theoretically boost the response to these natural painkillers. Combined, LDN and acupuncture are hypothesized to achieve greater synergy, but clinical trials haven’t tested this yet .

LDN has yet to be clinically researched in people with complex regional pain syndrome (CRPS). It’s hypothesized to silencing microglia and boosting internal cannabinoids.

Other Types of Pain

Another group of researchers think that LDN may enhance the effects of cannabinoids and opioids on pain. In 10 people, ultra-low-dose naltrexone enhanced the painkilling effect of an opioid drug, buprenorphine. They concluded that such an effect is not surprising since LDN appears to increase natural opioids. However, their findings haven’t been replicated .

In addition, LDN reduced tolerance to morphine in another study in mice. Thus, clinical trials should examine if it can help people with severe pain stay on lower morphine dose over a longer period of time .

Seizures

The effects of LDN on seizures are unknown. Human data are lacking.

In mice, LDN increased the anti-seizure effects of opioids and cannabinoids. These findings suggest that future studies might focus on people with epilepsy, especially those who use medical cannabis .

The anti-seizure potential of LDN is being researched in animals, but we don’t know how it affects people with epilepsy.

Nerve Inflammation

Transverse myelitis is an inflammation of the spinal cord that can severely damage nerve insulation, myelin. It also causes nerve pain that rarely responds to any medication .

In one case report, a person with this condition experienced pain relief with LDN (3 – 4.5mg/day). The authors hypothesized that it might reverse microglial activation and boost endorphins, which would reduce nerve inflammation and pain. However, it’s impossible to know if LDN has any effect on this condition based on a single case. Both animal and human studies are needed .

Inflammatory Gut Disorders (IBS and IBD)

Despite some promising small studies, there’s not enough data to determine whether LDN helps people with IBS or IBD.

Irritable Bowel Syndrome (IBS) is claimed to have many hidden causes, but stress, inflammation, and autoimmunity are often said to be a large part of it.

In one study of 42 people with IBS, ultra-low doses of naltrexone (0.5 mg/day) reduced pain and provided overall symptom relief in 76% of the cases after 4 weeks. LDN was deemed to be safe and side effects were not reported .

Similarly, a couple of small studies have suggested that low-dose naltrexone may help relieve symptoms of Irritable Bowel Disease (IBD), which encompasses Crohn’s and ulcerative colitis .

In a study of 14 children with Crohn’s, LDN caused remission in one-fourth of the cases, while two-thirds improved. An 8-week course of treatment also improved their overall and social quality of life. Future studies are needed to verify these findings .

In 40 patients with drug-resistant ulcerative colitis, 30% responded to LDN treatment and 20% experienced long-lasting improvements. Many of the long-term responders went into remission while 3 people relapsed. Larger, better-designed studies are needed .

LDN is still an experimental approach for IBD and IBS, despite some early promising research.

3) Fatigue & Nerve Disorders

Aside from sporadic clinical anecdotes, only a couple of small studies looked at the effects of LDN on fatigue and nerve disorders. More research is needed to determine its safety and effectiveness.

Anecdotally, low-dose naltrexone is said to reduce fatigue and overall symptoms in people with Parkinson’s disease. In one small study of 8 people with Parkinson’s, LDN improved fatigue over 8 months without reported side effects .

Other clinical anecdotes mention that LDN may help people with incurable degenerative illnesses such as ALS (Lou Gehrig’s Disease) and PLS. These diseases may have an autoimmune component, so certain doctors believe that LDN may protect the brain from further damage by increasing natural endorphins. Yet, scientific data are lacking.

Reports from 15 ALS patients who used LDN are mixed :

  • About half didn’t experience any effect or were unsure
  • One-third reported moderate efficacy
  • One-fifth reported slight efficacy

“Efficacy” included improvements in balance and speech, more energy and less phlegm, and easier breathing. However, these reports were subjective, un-blinded, and had many other limitations .

It’s unknown whether LDN can help with chronic fatigue and progressive nerve disorders. The available research produced mixed findings.

4) Autism

At first, naltrexone was researched in regular, high doses, in an attempt to see if it can improve symptoms of autism in children. The research rationale was that the opioid system and endorphins have profound effects on social interactions, which are impaired in autism.

For example, one such study used about 15 mg/day for a 66-lbs child – way above the “low-dose” benchmark .

These early studies did report increased endorphins and improved symptoms in autistic children who received naltrexone. The doses ranged from 5 to 50 mg/day, used every other day.

A couple of researchers then suggested that some children with low doses may respond better to low doses, though even these studies had several flaws and inconclusive findings .

All in all, 90% of the published studies were done with high doses.

Nonetheless, some doctors prescribe low-dose naltrexone to children with autism. They claim that only low doses have the potential to boost stress resilience, social bonding, emotional well-being, mood, and immunity.

Dr. Jaquelyn McCandless, an LDN advocate, reported positive effects of LDN formulated as a transdermal cream in children with autism after 8 weeks. Each patch contained 3mg of naltrexone and was given between 9 and 12 pm.

She also included a couple of adults with Crohn’s Disease and one with Chronic Fatigue Syndrome to test the 4.5mg patch. According to her, “everyone responded positively.”

However, Dr. McCandless did not conduct a proper clinical study. Rather, this was a mere clinical observation, which had a high potential for bias. A placebo effect was also likely. We need proper clinical trials to know whether LDN can help some people with autism.

Some physicians claim that LDN helps with autism and prescribe it off-label, but there’s no solid evidence to back this up.

5) Stress & PTSD

The effects of LDN on stress and PTSD are being researched, but no clinical research is yet available to back up its use.

Even doctors who prescribe LDN based on experience say that it should always be part of an integrated psychotherapeutic approach for complex mental health issues.

Some researchers believe that, by raising natural opioid activity, LDN may increase resilience to stress and fine-tune some emotional imbalances. Its immune-balancing effects are also described as having a potentially positive impact on mood .

In one study, LDN (2 – 6 mg/day) helped 11 out of 15 people with severe, trauma-related dissociative disorders and post-traumatic stress disorder (PTSD). They reported a clearer perception of both their own body, their inner life, and their surroundings. These findings have not been replicated and no other trials have been carried out .

LDN is hypothesized to improve emotional and mental perception of reality, which is key for overcoming trauma and PTSD. Yet, proper clinical trials are lacking.

6) Addictions & Withdrawal

High-dose naltrexone (and naloxone) is still a conventional treatment for opioid use disorders. On the other hand, LDN remains experimental and controversial. There’s not enough evidence to determine whether it works.

Some scientists think it may help people with addictions by boosting natural opioids and reducing the need for stronger external triggers such as drugs, alcohol, or cigarettes. This theory hasn’t been verified.

Opioids

In a study that tracked 10,000 people, LDN improved pain tolerance and interpersonal interactions in post-detox patients .

In 127 people undergoing a 6-day methadone taper, very-low-dose naltrexone (0.125 – 0.25 mg/day) with another drug (clonidine) reduced the intensity and stress of withdrawal. It lowered cravings, anxiety, restlessness, bone and muscle aches, and sweating .

Alcohol and Cigarettes

In one study with 130 heavy-drinking smokers, the combination of medium-dose naltrexone (25 mg/day) and the smoking-cessation drug varenicline reduced cigarette and alcohol cravings, as well as the intensity of the “high” from both substances .

The naltrexone dose was relatively high: 5-fold the dose that Dr. Bihari and other clinical studies of LDN used. Scientists consider that this initially higher dose may help stop smoking and drinking to start with, after which the dose can be lowered to boost natural opioid activity. More research is needed .

Cocaine

The effects of LDN on cocaine addiction in humans are unknown. In rats, LDN with a dopamine-blocking drug (L-tetrahydropalmatine) prevented cocaine abuse relapse. It reduced drug-seeking behavior and increased endorphins without causing fatigue and sedation. Human trials are required .

Limited evidence points at the potential of LDN for helping people overcome drug, cigarette, and alcohol addiction, but more research is needed.

Possibly Ineffective for

HIV/AIDS

LDN for HIV/AIDS is highly controversial. The only data about its use comes from Dr. Bihari’s opinions. His claims rely only on clinical experience, and no studies have confirmed them. Thus, LDN is considered an unproven approach to HIV/AIDS management.

The whole concept of low-dose naltrexone started with HIV/AIDS patients, when Dr. Bihari formulated his theory that it enhances a compromised immune system. He claimed to have administered LDN to hundreds of HIV/AIDS patients, some of which allegedly no longer had detectable levels of the virus .

Having in mind that naltrexone is a very affordable drug and that millions of people suffer from HIV/AIDS in the developing world, clinical trials are warranted. In fact, one study mentions that LDN has been approved in Nigeria as an AIDS treatment .

Dr. Bihari considered that low naltrexone doses may also help people with other types of chronic infections, such as tuberculosis, Lyme, genital herpes, and even Hepatitis C. According to him, the same rationale follows: “LDN boosts immunity and the ability to fight off infections.” Yet LDN has not been researched at all in people with these types of chronic infections.

Dr. Bihari proclaimed LDN effective against HIV and other infections, but no clinical trials to support his claims.

Cancer

LDN does not treat cancer. It was never properly researched in cancer patients and should not be recommended due to a lack of data.

Nonetheless, LDN has been popularly proposed as beneficial for various cancers–the list is almost endless and covering bladder, breast, colorectal cancer, brain, liver cancer, lung, blood and bone marrow, skin, cancers of the reproductive organs, and many others.

But before LDN is announced a “miracle cancer drug,” have in mind that the evidence is either anecdotal or stems from animal studies. There’s no proof that it can do anything for people with cancer.

No proper clinical studies have examined its effects on cancer. What’s more, many animal studies used it only as an add-on to conventional treatments.

For example, in mice with ovarian cancer, LDN coupled with chemotherapy (cisplatin) was studied for its potential to increase treatment efficacy and reduce side effects .

The use of LDN in people with cancer is not evidence-based and should not be recommended.

ALA/LDN Protocol

In one study of 10 advanced cancer patients who failed standard therapy, LDN (5mg/day) was given with alpha-lipoic acid (ALA) and hydroxycitrate as part of end-of-life (palliative) care. The sample was extremely small and the study was not blinded or randomized .

ALA/LDN appeared to be safe in the study. Some patients were given this combination in addition to chemotherapy. One patient was described as a responder, five patients were said to have had slower cancer progression, and the remaining four died shortly. These improvements were not ascribed to ALA/LDN, since patients were receiving other therapies as usual .

Long-term survival of a person with advanced cancer treated with LDN and alpha-lipoic acid has been reported. The man had pancreatic cancer and metastases to the liver. He was alive and well almost 7 years later — far beyond expectations. But it’s impossible to know which factors impacted his survival, and LDN might not have been a relevant one .

Three other similar pancreatic cancer cases were described. One was doing well 3 years later, and the other two had confirmed remissions after 5 and 4 months of treatment. Other factors that could’ve impacted survival were not described

Some researchers are looking at the following pathways that the ALA/LDN protocol may affect in cells and animals :

  • ALA on oxidative stress and inflammation (via NFkB) in cancer cells
  • LDN on the immune response and opioid receptors in tumors, which might theoretically change their response to the growth-inhibiting effects of endorphins and the number and activity of immune cells that may be involved in cancer (cytotoxic T cells and natural killer cells)

Scientists are investigating its immune effects in bone marrow cells (via genes that code for immune cells–MHC II, CD40, CD83, CD80, and CD86) .

LDN and alpha-lipoic acid are being researched in cancer, but no large-scale trials have been conducted.

Dr. Bihari’s Experience

Dr. Bihari spoke of witnessing cancer improvements in his patients prescribed LDN. He also observed that, in contrast, high doses of naltrexone may have the opposite effects and worsen cancer growth, probably by reducing opioid activity. Whether there is truth in his claims remains to be determined .

Other studies of LDN for cancer are currently in progress, some of which are funded by the National Cancer Institute .

Further Reading

  • What is Low Dose Naltrexone (LDN)? + Side Effects

Takeaway

Naltrexone is a drug that blocks opioid receptors. Low-dose naltrexone (LDN) is being researched in people with autoimmune diseases, chronic pain, inflammation, fatigue, cancer, and autism. However, there’s still insufficient evidence to back up its use.

LDN is claimed to boost the body’s natural opioids – endorphins and enkephalins – and rebalance the immune system.

LDN is only available from a compounding pharmacy with a doctor’s prescription.

What are the Side Effects of Low Dose Naltrexone (LDN)?

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Naltrexone

How is it used?

Naltrexone is taken as a tablet. The length of the course will depend on each person’s needs and situation.

It can also be administered via an implant. Treatment with naltrexone implants is permitted in Australia under the requirements of the TGA Special access scheme.

To be eligible for the treatment for opioid dependence, a person must:

  • be free of heroin and other opioids for 7–10 days (or 10 days for methadone) before starting naltrexone maintenance treatment; otherwise they may experience acute, instant withdrawal. People who intend to start naltrexone maintenance treatment can expect to be tested in order to confirm that they are clear of opioid drugs. An example of such a test is the Naloxone Challenge Test (NCT), in which the opioid antagonist drug naloxone is administered to determine a person’s current level of physical dependence on opioids.3
  • have no existing liver conditions, such as acute hepatitis.
  • seek advice if they are pregnant or breastfeeding as naltrexone may not be safe for use during pregnancy.2

Alcohol and naltrexone

Naltrexone can be prescribed to people with alcohol dependence. Its use in that context works in several ways, it can:

  • reduce the craving for alcohol
  • reduce the quantity of alcohol consumed1
  • reduce the ‘reward’ effects of alcohol use
  • help people remain abstinent from alcohol
  • reduce the tendency to want to drink more if a person consumes alcohol.

If a person consumes alcohol while using naltrexone, they will still experience the effects of alcohol, so their judgement, coordination and ability to perform tasks such as driving and operating machinery will still be affected.

Regular blood tests to monitor liver function both before and during naltrexone treatment are recommended.6

How effective is it?

Naltrexone may not work for everyone, so it is important to consult a doctor or drug counsellor to find the best approach.

Naltrexone treatment is more likely to be successful if it is part of a comprehensive treatment program that includes counselling, alternative therapies and the development of a positive network of peers, friends and a support group.

Some studies suggest that many clients don’t remain on naltrexone and return to heroin use. Future studies may provide a clearer picture of the drug’s effectiveness.

In terms of its use to treat alcohol dependence, naltrexone may be more effective for preventing relapse to heavy drinking and reducing high levels of alcohol consumption than for maintaining abstinence from alcohol.6

Effects of naltrexone

There is no safe level of drug use. Use of any drug always carries some risk – even medications can produce unwanted side effects. It’s important to be careful when taking any type of drug.

Naltrexone affects everyone differently, based on:

  • the amount taken
  • size, weight and health of the person taking it
  • whether the person is used to taking it
  • whether other drugs are taken around the same time.

Side effects

Naltrexone has few side effects, and these usually go away after the medication is taken for a few days.

The reported side effects include:

  • sleep problems
  • tiredness
  • anxiety
  • headache
  • joint and muscle pains
  • abdominal pain and cramps
  • nausea
  • vomiting.2

Less common side effects include:

  • feeling energetic
  • loss of appetite
  • thirst
  • diarrhoea, constipation
  • depression and irritability
  • dizziness
  • skin rashes
  • decreased potency, delayed ejaculation
  • chills.4

Naltrexone may affect mental alertness and/or coordination. If affected, do not drive a motor vehicle or operate machinery.

Dose-related effects

Large doses of naltrexone may cause liver damage. Seek medical advice immediately if these symptoms are experienced:

  • excessive tiredness
  • unusual bruising or bleeding
  • loss of appetite
  • pain in the upper right area of the abdomen that lasts more than a few days
  • light-coloured bowel movements
  • dark urine
  • yellowing of skin or whites of the eyes.4

Risk of heroin overdose

Naltrexone will lower a person’s tolerance to heroin. This means that there is a serious risk of overdose if they use heroin after a missed dose of naltrexone or after treatment has finished.3

People who plan to use heroin after being on naltrexone should consider themselves ‘new’ users.

If you believe someone has overdosed on heroin, call an ambulance straight away by dialling triple zero (000). Ambulance officers don’t need to involve the police.3

Using naltrexone with other drugs

The effects of taking naltrexone with other drugs – including over-the-counter or prescribed medications – can be unpredictable and dangerous. In particular:

Naltrexone + opioid painkillers: the naltrexone will stop opioid painkillers from working.3

In cases where a person on opioid painkillers is likely to be given naltrexone (or vice versa), medical staff will need to be informed so that a different kind of painkiller can be prescribed. Medic alert bracelets are available for purchase online.

Supporting someone who is on a naltrexone program

People who are taking naltrexone will need both emotional and practical support.

Those who are to give support should decide, in collaboration with the person undergoing treatment, exactly what the support will entail. This might include whether they will inform a doctor if problems arise.

It could also include:

  • being committed to supervising the naltrexone dose for the duration of the treatment
  • knowing what to do in the event of an overdose
  • going with friends/family members to appointments (such as those with doctors, counsellors)
  • encouraging the person to develop their friendship and support networks and to get involved in positive, healthy activities (such as taking a class, joining a support group, being active)
  • attending couples or family counselling if appropriate.5

This is a challenging role, so people offering support will need to take care of themselves and arrange their own support networks.

Naltrexone Therapy for Opiates FAQs

  1. What is Naltrexone therapy, and why is it important for opiate addiction?
  2. What is the Naltrexone implant?
  3. Why use the Naltrexone implant instead of the oral tablets?
  4. Does Naltrexone therapy have any risks and side effects?
  5. How long should I be on Naltrexone therapy?
  6. What happens after Naltrexone implantation?
  7. What is the risk of overdosing following treatment?

1. What is Naltrexone therapy, and why is it important for opiate addiction?

Our ultimate goal with Accelerated Opiate Detox (AOD) is for patients to begin a life of abstinence — rather than treating addiction with a maintenance program that uses other opiates, such as Suboxone or methadone. We recognize that recovery is a challenging path to walk, filled with many opportunities for relapse. So, after AOD, we use Naltrexone therapy to help patients focus on their psychological healing without the temptations to use again.

Naltrexone is a non-addictive, non-narcotic medicine that attaches to the brain’s opiate receptors and completely blocks them. As a result, patients feel no effect from opiates while on Naltrexone and experience virtually no drug cravings.

We believe that 12 months of Naltrexone therapy gives patients the best chance for lasting recovery. This support allows their brain to physically heal from the opiates’ damage while they build the psychological tools and strength they need to Stay Clean for life.

2. What is the Naltrexone implant?

We use a special Naltrexone formulation that releases the medicine slowly over an eight-week period. This small implant goes under the patient’s skin, so they experience a steady dose of opiate blockers and don’t forget or skip their medicine. Licensed pharmacists at a compounding pharmacy manufacture the implant for us. While the Naltrexone implant has not yet been submitted to the FDA for approval, the medications it contains are fully approved by the FDA.

3. Why use the Naltrexone Implant instead of the oral tablets?

When patients get a steady dose of Naltrexone every day for a prolonged period of time, they have a much better outcome. They have fewer cravings, are more likely to abstain from drugs, and more often stay with their treatment and support groups. Patients’ improved outcomes may be physical, because they have a more steady blood level and don’t forget their medicine. We also believe the results may be partly psychological, because once a patient receive their implant, they don’t have to decide every day whether or not to take their Naltrexone or consider relapsing.

4. Does Naltrexone therapy have any risks and side effects?

As with any medical procedure, Naltrexone therapy carries some risks and potential problems. While small and typically painless, the Naltrexone implant does require local anesthesia for insertion. As a result, some patients experience the following symptoms at the implant site:

  • Irritation
  • Inflammation
  • Infection

In addition to these implant risks, Naltrexone therapy can cause withdrawal symptoms if a patient isn’t fully detoxed when treatment begins. To avoid these risks, we carefully monitor patients before beginning Naltrexone therapy and only start treatment when they have completed their Accelerated Opiate Detox.

5. How long should I be on Naltrexone therapy?

We strongly believe that patients should be on Naltrexone therapy for at least 12 months after completing their detox. Recent research shows that it takes a year or more for the brain to fully heal from addiction. And we know that it also takes at least a year for people to learn about alcoholism and recovery, build up a support system, and integrate all of the recovery changes into their lives. Having Naltrexone therapy during the first stages of recovery helps prevent patients from relapsing while giving them time to invest in their long-term health.

6. What happens after Naltrexone implantation?

Opiate dependency is a complex brain disease, and we know that detoxing is just the beginning of recovery. From our experience, ongoing treatment and support are the keys to breaking free from addiction. We require all of our patients to be willing to participate in an appropriate treatment program, which may include individual professional therapy and supportive group treatment. Through our Stay Clean program, we help patients find the resources they need and create a plan for their recovery after Naltrexone therapy begins. We also encourage patients to begin seeing a physician who specializes in substance abuse.

7. What is the risk of overdosing following treatment?

Accelerated Opiate Detox clears patients’ brains of all opiates, which means they are clean — but they also have no built-up tolerance for the substance anymore. We have all patients use Naltrexone therapy immediately following their detox to prevent cravings and provide some overdose protection if they do relapse. However, patients must know that when Naltrexone therapy ends, they will have a very low tolerance to any opiates. As a result, if they relapse, a dose that would have gotten them high before detox can be fatal after treatment.

Very rarely, patients may try to override their Naltrexone therapy and take a very large opiate dose in pursuit of a high. While Naltrexone is an opiate blocker that prevents most overdoses, it is possible to take enough opiates for the dose to be fatal.

What are the potential complications from receiving a naltrexone implant?

March 3, 2017 |By

Naltrexone is a very safe medication that has been used for many years. The implants are generally very well tolerated. Beside the side-effects mentioned above, program participants can report itching, tenderness, swelling, pain, irritation, inflammation, or infection around the surgical site. The majority of cases of irritation or inflammation resolve with time. Often, antihistamines and topical and/or oral steroids are used to help treat the local inflammation. In cases of infection, antibiotics may be needed. In the very unlikely case of severe infection or inflammation, a doctor may recommend removal of the implant. The implant is contraindicated in individuals with acute hepatitis, advanced liver disease, or kidney failure. Pregnant or breastfeeding women should consult with their physician before beginning Naltrexone treatment. The implant is surgically placed, and there will be a small linear surgical scar. Each individual scars differently. In some cases, a small nodule of fibrous tissue may remain palpable under the skin. Although very unlikely, as with any foreign body there is a risk of rejection, tissue breakdown, and necrosis.

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