What is naltrexone and what is the difference between regular naltrexone and LDN?
Naltrexone is an opioid antagonist medication. This means that when the drug enters your system, the molecules block opioid receptors. Naltrexone was first made in a lab in the 1960s.
It was not until the 1980s that the Food and Drug Administration approved it for treating opioid addiction. About a decade later, the FDA approved naltrexone for the treatment of alcoholism.
LDN, or low dose naltrexone, means exactly what it sounds like it means. A typical naltrexone tablet approved by the FDA is available in a 50 mg dosage. LDN refers to treatment with lower dosages, often in the range of about 2 mg to 6 mg.
How do you get a naltrexone dosage that low if the tablets are 50 mg? You might be able to break a tablet in two with your fingers. With a pill splitter, you might be able to split it into four equal pieces. Any further, and the dosage will not be accurate. More likely, the small pieces of your 50 mg naltrexone tablet will crumble into powder.
Compound pharmacies are the solution to safe and accurate LDN dosing.
Fortunately, you can obtain low dose naltrexone in a variety of strengths from a compound pharmacy. There is no need to crush up naltrexone pills and then wonder what to do next.
So, if you bring up LDN therapy to your doctor, you may want to research compound pharmacies first. Your doctor may not be aware of LDN and they may not have experience with compound pharmacies. By doing some research ahead of time, you will help your doctor to learn more about the topic and how to order the medication.
If your doctor is not comfortable with the idea of prescribing low dose naltrexone, you may want to consider seeing a doctor who is experienced in prescribing it and ordering it. This does not mean that you are changing doctors. You are allowed to see another doctor to help with a particular issue and continue seeing your primary care doctor for routine healthcare.
What does LDN look like from a compound pharmacy?
There are a variety of medication delivery systems that most compound pharmacies are able to work with. For oral medications, your compound pharmacist may offer capsules, lozenges, or troches.
Capsules are a convenient way for the pharmacy to measure out a customized dosage of medication. In order to fill the capsules, the compound pharmacist uses a specialized machine that looks a little like a waffle iron. Capsules are loaded in and the compounded medication is loaded into the capsules before they are pressed shut.
Lozenges are like hard candies. You can put them in your mouth to dissolve, or with some medications, you will place them under your tongue. While flavored lozenges are a pleasant way to take compounded medications, they cannot be accurately cut in half. Your doctor will specify the dosage and that will be how you take it.
Troches have been around for a long time but have been updated for the new millennium. Troches are proving to be the ultimate delivery system for certain compounded medications. LDN works particularly well with troches because, if made properly, they can be divided into up to four equal pieces. This gives your doctor flexibility in dosing.
For example, if your doctor orders low dose naltrexone in the form of a 4 mg troche, you have the option to take either 1 mg, 2 mg, 3 mg, or 4 mg, depending on how you divide the individual dose. A troche resembles a chewable candy, like a Starburst, or the chewable Jolly Rancher candies. They may be dissolved in the mouth, or specifically under the tongue for certain medications.
But, why have I never heard of naltrexone or LDN? If it works so well for so many different problems, shouldn’t doctors know about it?
Doctors get much of their information about medications from educational campaigns run by pharmaceutical companies. Unfortunately, these well funded efforts to indoctrinate doctors to prescribe the latest brand-name pills starts in medical school and continues throughout the doctor’s career.
While there have been efforts and laws passed to limit the influence of big pharma over all doctors in the US, these companies are powerful entities that will always find a way to skirt any regulation to continue the task of swaying the minds of working doctors. Your doctor may deny being influenced by the drug companies, but we all have that sense that an older drug is not as good as the latest drug. In many cases, this is completely untrue. Often, older drugs that have stood the test of time are superior to potentially dangerous and possibly less effective newer drugs.
Not long ago, I recorded a podcast interview with actress Claudia Christian. The title was, “The Forgotten Pill,” and the topic was using naltrexone to treat alcohol use disorder.
Why is naltrexone the “forgotten pill”?
Bringing up the topic of naltrexone gets some interesting responses from doctors and other healthcare workers. Older doctors will likely remember a time when naltrexone was the drug to prescribe for opioid addiction in the 80s, and then alcoholism in the 90s. It was the drug of the day.
Well-dressed pharma reps visited their offices with rolling suitcases and colorful, glossy promotional material. Large multicolored graphs represented data that said clearly, “this is the drug you want to prescribe to your patient.” Back then, the reps gave out pens and pads of paper.
Sometimes, they even took doctors to baseball games and skiing trips. They presented easily digestible medical lectures to promote their product during fancy steak dinners at the finest restaurants in town.
So, what happened when a drug was no longer patented and making the company money? It is hard to fully comprehend the psychological grip that the industry has on healthcare workers. When a drug falls out of favor, it disappears, as if by magic, from the consciousness and memories of doctors who once prescribed it.
For doctors who graduate from medical school and residency after the drug is no longer a shiny, new product will not look twice at it in their pharmacy books. They are already under the influence of the industry that wants them to look forward to newer and more profitable drugs.
But don’t doctors still use many older, generic drugs?
In the world of HMOs and recent cost-saving efforts on the part of insurance companies, there has been renewed interest in using generic drugs when possible. And, of course, doctors are typically smart people and not fully susceptible to the marketing efforts of big pharma.
The difference with a drug such as naltrexone is that it is used to treat addiction, a mental health condition with serious stigma attached. And, doctors who work in addiction treatment tend to avoid long-term medical treatment of addiction, so they are often not in favor of a drug such as naltrexone. Abstinence is favored by traditional addiction treatment institutions. They are concerned about “trading one drug for another,” even though naltrexone has no habit-forming properties whatsoever.
Another reason why naltrexone has fallen out of favor is because of the intensive marketing efforts of the company that makes Vivitrol, a monthly naltrexone injection. It is in the best interest of the marketers for Vivitrol to promote the forgetting of naltrexone in any other form. Naltrexone tablets are presented as a footnote in their literature as an old, outdated therapy.
My pharmacist says that LDN is not a good idea and recommends against it.
Healthcare professionals tend to stick to what they are able to offer. Your local pharmacist at the big box pharmacy and supermarket where you shop and pick up prescriptions may recommend against it simply because it is not on the formulary.
In the busy world of modern healthcare, it is always safest to stick to what is approved by insurance formularies and available as manufactured products. Doctors employed by busy medical practices and pharmacists at the big chain drug stores barely have time to get their work done.
We cannot blame them for playing it safe, staying in their lane. There is a great deal of pressure from insurance companies, pharmaceutical companies, and employers.
Is naltrexone a safe medication?
In a way, this is like asking if ibuprofen (advil, motrin) or tylenol are safe. You can buy those drugs over-the-counter without a prescription. Over-the-counter, or OTC, means that you do not even have to go near a pharmacist to buy them. In fact, you can buy these drugs from a gas station attendant in the middle of the night.
The reason I group naltrexone with those OTC drugs is that there is a movement to request the FDA to approve naltrexone to be an OTC drug. Naloxone, a similar opioid antagonist, is already on the path to being approved for OTC use.
Does this mean that naltrexone is completely safe with no safety concerns? No, it does not. Any drug that has a beneficial effect also carries with it the risk of side effects and adverse reactions. However, naltrexone is considered to be safe enough that, in the near future, people will have the power to make their own decision about taking it without going through the approval of a doctor or pharmacist.
Naltrexone does, in rare instances, cause problems with the liver. Also, it must not be taken by people who are prescribed opioid drugs. Precipitated withdrawal sickness, which occurs when a person who takes opioids then takes naltrexone, is the most unpleasant of naltrexone side effects. It is also not recommended for pregnant women.
Keep in mind that LDN is naltrexone at a much lower than normal dosage. Rather than taking 50 mg daily, you would be taking 6 mg or less. In fact, there are proponents of very low dose naltrexone at dosages of less than a milligram. There is even ultra-low dose naltrexone.
By taking a relatively safe drug and then taking one-tenth or less of the usual dosage, it is even safer. While you must keep in mind that it is still a prescription drug at this time and there are potential side effects, LDN can be considered to be relatively safe for most patients.
As promised in the title, below you will find six potential uses for LDN. In fact, before we are done, we will likely have covered more than six possible uses. Because of the various ways in which the treatment works, as proposed by experts, there are many conditions that may benefit from the effects of LDN.
How does low dose naltrexone help with chronic pain conditions?
This is an excellent question. Naltrexone helping with pain seems counterintuitive. You are most likely aware that opioids are used to treat pain by stimulating opioid receptors. So, how can an opioid receptor blocker work to reduce pain?
One of the proposed mechanisms for LDN is that it stimulates production of the body’s natural endorphins. Endorphins are your body’s natural opioids and the main reason why your central nervous system has opioid receptors in the first place.
Endorphins are released during injuries to make the pain more tolerable. For example, someone who breaks their arm may go through a surreal period right after the injury where it does not seem to hurt. Later on, the real pain sets in. Endorphins provide analgesia naturally.
This release of endorphins to dull the immediate pain response makes evolutionary sense. Imagine a caveman breaking his arm while running away from a hungry lion. His best chance for survival is to not be distracted by the pain immediately after the injury.
Another use of endorphins by your brain is to reinforce positive behaviors. This happens in parts of the brain known as the reward system. Drugs and alcohol hijack the reward system and use this endorphin-opioid receptor system to cause you to crave drugs or alcohol when addicted.
As you can imagine, while taking opioids might work to relieve pain in the short term, helping your body to produce more natural endorphins is a better long-term solution in many cases. If low dose naltrexone can do this, it may be an ideal solution for many chronic pain syndromes.
People with a variety of health conditions that cause pain have claimed to have improvement with LDN. There are doctors who believe that fibromyalgia, chronic regional pain syndrome (previously known as RSD), and other types of chronic pain can be helped with LDN treatment.
Is low dose naltrexone good for addiction treatment?
It is known that naltrexone at the full strength of 50 mg is effective in treating both opioid and alcohol addiction. The Vivitrol shot is intended to provide the same effect as taking 50 mg of naltrexone daily for a month with a single injection.
For opioids, the mechanism of full dose naltrexone is to block the opioid receptors. This serves two purposes. If the patient tries to take opioids to get high, they will have little to no effect, because the receptors are blocked. The other effect of naltrexone is to reduce cravings for opioids.
When it comes to alcohol use disorder treatment, you may wonder what blocking opioid receptors has to do with alcohol. It turns out that blocking the opioid receptors in the brain’s reward system helps to reprogram the brain through pharmacological extinction. This is similar to Dr. Pavlov’s dog experiment in making dogs salivate at the sound of a bell.
Full dose naltrexone works to help alcoholics quit drinking. It also works with a protocol known as The Sinclair Method (TSM), where the patient takes a naltrexone 50 mg tablet one hour before having a drink. Many experts believe that TSM is the better way to use naltrexone for reducing and eliminating alcohol use.
So, what are the low dose naltrexone benefits in treating addiction? One issue that people addicted to drugs have during addiction treatment is recovering the normal functioning of their central nervous system. They complain of something known as anhedonia, or a lack or pleasure. They have difficulty enjoying the simple pleasures of everyday life.
By taking LDN, it is believed, by some experts, that stimulating the brain to produce natural endorphins can help in the healing process during addiction recovery. Rather than having ongoing cravings for drugs to get back that good feeling, the patient will be able to start enjoying basic activities again, such as exercise, and eating a healthy meal. In fact, exercise is an excellent way to jump-start the endorphin system during addiction recovery, but LDN may also be helpful.
It is important to differentiate the effects of regular dose naltrexone and low dose naltrexone. At the full strength, naltrexone inhibits the effects of endorphins and may even slow down their production.
So, after a full course of naltrexone treatment for addiction, maintenance with LDN long-term may be helpful. It is not unusual for one drug to have very different effects at different dosage levels. This is a known effect with other drugs as well.
Of course, doctors must make careful decisions on when to discontinue full strength naltrexone for addiction. Typically, the recommended treatment time can be six months or more.
Are there other health conditions that may be helped by the benefits of low dose naltrexone?
Interestingly, there are autoimmune diseases that doctors and patients claim are helped by LDN. It is important to note that there have not been many quality studies done to support the use of LDN. Much of the supporting documentation is anecdotal, meaning that doctors have noted improvement in their patients, but they have not performed formal scientific studies.
There are proposed mechanisms for how naltrexone at a low dose interacts with the human immune system. These models of LDN improving the immune system functioning to improve the course of a chronic disease are complex and not fully understood. Proposed mechanisms include interactions with opioid growth factor and glial activation.
Some of the conditions treated with LDN include multiple sclerosis, rheumatoid arthritis, inflammatory bowel disease (IBS), including Crohn’s disease, ulcerative colitis, and others. Of course, it is important for a specialist to evaluate the patient with these conditions and to first initiate traditional, evidence based treatment before considering LDN.
There are also other conditions said to be helped by LDN, including post traumatic stress disorder (PTSD) and chronic fatigue syndrome. Doctors are also using low dose naltrexone for depression and anxiety treatment.
Should doctors be prescribing a treatment that has not been proven to work by large-scale studies?
When it comes to medical treatments, we must look at safety, efficacy, and cost. Safety is most important of all. As discussed above, LDN is relatively safe. It may be about as safe as taking a baby aspirin every day. Of course, even a baby aspirin can cause problems for some people. Low dose naltrexone side effects are not a major concern.
Efficacy is the big question. There are patients who insist that LDN works. What is their motive for making these claims? We are often told to follow the money whenever anyone makes a claim about anything.
In the case of a patient recommending LDN in a discussion forum, there does not seem to be any significant profit motive. LDN is not a brand-name product and there are not people on the streets selling LDN. It is not like CBD products where everyone seems to have a stake in selling the product one way or another.
Doctors may try LDN with a patient because other options have been exhausted. Also, LDN, being safe and not interacting with many other therapies, is often a relatively harmless add-on.
I remember asking an oncologist if a patient could take various health food store supplements that claimed to help reduce or prevent cancers. His answer was that it was fine as long as it did not interfere with the evidence-based treatments he was providing.
Regarding cost, LDN is not expensive. It is somewhat more costly than naltrexone 50 mg tablets because a compound pharmacist has to perform significant work in preparing the prescription for each individual patient. Still, it is very affordable compared to other generic drugs and most brand-name drugs.
What is the final verdict on LDN?
Low dose naltrexone is relatively safe and affordable. We definitely need more scientific studies to provide better evidence of efficacy. That being said, doctors are allowed to prescribe it off-label to use in treating certain medical conditions.
It does seem like the more you read about LDN, the more testimonials and articles you find that claim low dose naltrexone can help with nearly any medical condition. It is important to take some claims with a grain of salt.
For example, if you read that one of the low dose naltrexone uses is for cancer treatment, you must not think of it in any way as being a treatment for any type of cancer. Cancer treatment is a serious matter and must be administered by doctors who specialize in the field. Only with the permission of the treating cancer specialist may LDN be used in addition to the proven treatments that the specialist has ordered.
However, in the case of other conditions where medical treatment has been tried and not been adequately helpful, you may ask your doctor if LDN is right for you. The treatment is relatively safe and affordable. It might be worth giving it a try to see if it is effective for you.