Low Dose Naltrexone

Sep 28, 2018

By Trevor Shewfelt, Pharmacist at the Dauphin Clinic Pharmacy

"I'm not getting out of this van. I don't want to be here. I've already left that place and you can't make me go back!" Ahhhh. The joys of back to school. Last week was Meet the Teacher Night at MacKenzie Middle School. We went to meet hear the administrators and staff tell us about the new school website, tour the school and meet Eric's teacher. Emily had gotten as far as into the van. However, she decided to dig her heels in at leaving the van to go to the assembly. And her loud protestations were drawing lots of attention from the other parents. My wife was mortified. I was angry and tired. Eric didn't want to be there either. School functions. I've loved them since Eric was a toddler.

We've been getting some questions in the pharmacy about low dose naltrexone, or LDN. To understand low dose naltrexone, first we should go over regular naltrexone. Naltrexone was found to block the body's opioid receptors in the 1960's. Opioids are drugs chemically related to morphine like codeine, oxycodone and hydromorphone. They are often used to treat pain. Why would we want a drug that stops a pain killer from working? Well, one opioid blocker has been in the news a lot lately. That opioid blocker is called naloxone. Naloxone can be given by injection or nasal spray to reverse an opioid overdose. These are the naloxone kits carried by EMT's, police and other first responders. If someone has overdosed on morphine, or heroin or another opioid, an injection of naloxone can reverse the overdose and stop the person from dying. The reason naloxone works is it binds so tightly to the opioid receptors that it pushes the morphine or heroin off of the receptor. Naloxone has a harder time pushing fentanyl off the opioid receptor because fentanyl is so tightly bound. That is one of the reasons why fentanyl overdoses are so dangerous.

Naltrexone is chemically similar to naloxone but works a little differently. It is a pill, not an injection. Naloxone injections work fast and wears off fast. That makes naloxone appropriate for treating overdoses. Naltrexone takes a long time to take effect. It also lasts for a much longer time. That makes naltrexone too slow to work on overdoses, but it still does block opioid receptors. Naltrexone's main indication is to help treat opioid addiction or dependence.

Naltrexone has a half life of about 6 hours. One of Naltrexone's metabolites also blocks opioid receptors. The metabolite's half life is 13 hours. That means one dose of naltrexone lasts for about 24 hours. When we are trying to treat opioid dependence, we use a dose of naltrexone between 50 and 150 mg per day. But there is something very different called low dose naltrexone which uses 1.5 to 4.5 mg per day.

Low dose naltrexone (LDN) treatment has nothing to do with opioid addiction or dependence. People have tried LDN to treat all sorts of different conditions. Often these are conditions that don't have really good treatments in more conventional medicine. The theory behind LDN goes like this. There seems to be a link between the endorphin system of the body and the immune system. Endorphins are the opioids that the body produces on its own. For example, you take a big check in a hockey game. You really don't notice the pain during the game, but the next day it really hurts. Your body produced endorphins to kill the pain during the game. But your body's endorphin system does more than just pain killing. Some of the cells of your immune system have opioid receptors on them. One of these receptors is called the Opioid Growth factor receptor. When naltrexone blocks the Opioid Growth Factor (OGF) receptor and other opioid receptors on immune cells, interesting things happen.

Researchers have found blocking opioid receptors in the immune system reduces inflammation, reduces cell division, increases the body's production of endorphins, help with healing, and reduces how fast the bowel moves. Let's have a look at a few of these. Chronic pain is a very complicated condition. One of the things that might be going on is too many pain receptors. After months and years of pain that part of the body has become hypersensitive so that every sensation is interpreted as pain. LDN might downregulate or reduce the number of pain receptors and increase the amount of the body's pain killers called endorphins. That could make chronic pain better. LDN has been tried to help heal corneal ulcers. It seems to promote DNA synthesis and help some eyeballs heal. It has been used to reduce the number of watery bowel movements in Crohn's disease. That helps the bowel lining heal. The reduction of inflammation has been used to help people with MS.

The list of potential things LDN might be good for is long. Some cancers, neurodegenerative autoimmune diseases like Multiple Sclerosis, Alzheimer's and Parkinson's, autoimmune diseases like Crohn's, psoriasis, and Lupus. Plus, diseases like chronic pain, depression and Lyme disease. The problem with LDN is the list of evidence that it works is very short. There are lots of very small studies on a few people. There is lots of theoretical reasons why LDN might be very good, but no large randomized double-blind placebo-controlled trials. And those big trials probably will never be done. Large trials are expensive to run. They can usually only be paid for by big drug companies. But it is difficult for a drug company to make any money off of an old drug.

Does LDN work? We don't know. There are lots of anecdotes, case studies and small trials. Lots of people are claiming LDN is a miracle cure for lots of things. The short answer is we need more evidence. On the plus side, the chance of harm from LDN is very low. If a patient is not currently taking an opioid, there is very little chance LDN will do them any harm. So, my conclusion is we don't know if LDN will help people, but it probably won't hurt them.

The number of school functions I have to attend has decreased as the kids have gotten older. To increase my odds of Parent of the Year, I'm going to say I'm glad. I've gone to pancake breakfasts, read to me nights, and brown bag lunches. My kids have resented being at each one and thus resented me for bringing them. My most/least favorite were the Christmas concerts when Emily was in Kindergarten and Grade 1. Eric was a toddler. Doris was at bowling. I had to sit through 2 hours of an entire elementary school singing. Then the teacher sang. All with a toddler who didn't want to be there for 5 minutes, let alone 120 minutes. Middle school events seem to be remarkably short and infrequent in comparison. And that, Esteemed Members of the Selection Jury, is why I deserve Parent of the Year. It is because I'm full of so much frickin' milk of human kindness, empathy and compassion that it hurts.

As always if you have any questions or concerns about these or other products, ask your pharmacist.

The information in this article is intended as a helpful guide only. It is not intended to be used as a substitute for professional advice. If you have any questions about your medications and what is right for you see your doctor, pharmacist or other health care professional.

We now have most of the articles published in the Parkland Shopper on our Website www.dcp.ca


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