Opiate Addiction and Detox: Buprenorphine vs Methadone

Opioid Addiction and Detox: Buprenorphine vs Methadone

Last week, I went over the history of opioids, and it really highlighted the trend of addiction that has always been linked with them. According to the World Health Organization, more than 15 million people are suffering from opioid dependence today. It’s clear that the opioid epidemic isn’t a new phenomenon; for as long as the opium poppy has been in existence, so has addiction. Historically speaking, what is relatively new is that physicians and pharma companies are recognizing the need for more effective ways to combat this epidemic, whether through prevention or treatment. As a result, we have some novel compounds that present different options for people who are addicted to these drugs; these include non-narcotic options for pain relief to prevent addiction, as well as medications to help addicted people on their road to recovery from opioid dependence. In a future blog, I’ll talk about a non-narcotic compound currently in patient trials that is showing a great deal of promise in the chronic pain arena. If you’re interested now, I posted a video on it on my YouTube channel, so check it out. But for today, I’m going to talk about the latter: two drugs, one relatively new and one not so much, that are being used to detox opioid addicts and give them a shot at a clean life. These two drugs are buprenorphine and methadone, and one of these is definitely not like the other. I’m going to compare and contrast them: the good, bad, and the ugly. By the end, you’ll not only know my opinion on the matter, but why I’m passionate about it. 

What is Buprenorphine?

On the market for nearly twenty years, buprenorphine is a Schedule III drug used to help treat the physical ramifications of opioid withdrawal. Given as a simple medicine that dissolves under the tongue, buprenorphine satiates the opioid receptors that cause dependent people to crave opioids. It can be prescribed in its solo form, or as a branded compound product with naloxone, which is the familiar ‘resurrection’ drug Narcan. It is the most strictly regulated drug by DEA, and available only from physicians that have been specially certified in its use, a fact that has been the nexus of some controversy. Why? Some physicians and policy makers feel that the hoops that physicians must jump through in order to receive the ‘X Waiver’ required to prescribe it present a barrier to its use; that if certification requirements were relaxed or eliminated, more opioid-dependent people would have access to this option for detox. The objective of someone taking buprenorphine is to help them remain safe and comfortable as they go through detox from opioids so that they can focus on treatment and recovery. While some data claims that buprenorphine may create some feelings of well-being when a person takes it, it does not cause a euphoric high. It’s also worth noting that while it can be used safely long term, the duration of use of buprenorphine tends to be more short-term, which clearly verifies the absence of a high and it’s low potential for addiction. Buprenorphine’s binding action to opioid receptors in the brain blocks the narcotic effects of traditional opioids, so if a drug-dependent person takes buprenorphine and an opioid together, there’s still no “high,” thus eliminating the reason for taking said opioid. And, buprenorphine also has a ceiling effect, meaning that beyond a specific dose, its effects remain unchanged. This essentially does away with the “if one is good, four are better” phenomenon, so overdose is very rare. 

What is Methadone?

Methadone is a drug that some physicians believe can be used to “help” opioid-dependent people as they try to stop using drugs. But that’s about where the similarities end. Old as the hills, methadone is a Schedule II opioid medication that’s been used for detox for 60 years. Methadone has a similar chemical structure to morphine; as such, methadone can, and does, make someone feel high. In theory, methadone doesn’t make people “as high” as some other opioids, and it can take longer for that high to occur, which proponents say translates into less potential for abuse. I say this is total bullshit. Why? Because we’re talking about drug-dependent people here, people! We’re dealing with people that, despite any good intentions they may have, their brains and bodies tell them they must get high. Remember that “if one is good, four are better” phenomenon I mentioned? Yeah. Bottom line is that methadone is a very strong opiate, so when a dependent person takes it, their addicted brain gets a taste of that high, and it’s like a tease…it tends to make them want more. Helllooo! There’s almost nothing that will stop a drug addicted brain from getting what it wants. There’s no blocking action and no ceiling with methadone, so overdoses are not unusual. Regardless, for over sixty years, methadone has been given as a “short-term” treatment to help people stop using opioids. That’s bad enough, but what’s worse is that it’s even more often used as a long-term maintenance drug for the “management” of opioid addiction. In reality, it’s replacing one bad drug with an even worse one. In fact, methadone is also known as “liquid handcuffs” by the people who have managed to successfully get off of their methadone “management” programs. 

While the general objectives of buprenorphine and methadone use may be similar to one another, there are clearly many significant differences.

Methadone is almost exclusively dispensed by clinics on a per diem basis, meaning that people have to head to the clinic every day and line up to get their “medicine.” In contrast, a physician with an X waiver can write for a 30-day supply of buprenorphine. It is less problematic than methadone, largely because it’s less dangerous and less addictive than methadone, thanks to the ceiling effect precluding overdose, and the fact that it doesn’t cause a high. That said, people must keep in mind that buprenorphine is a powerful drug, and not one to be taken (or prescribed) lightly. Saying that it’s less dangerous than methadone, while absolutely true, is sort of like saying that rattlesnake bites are less dangerous than cobra bites. Me personally, I’d just rather not be bitten…but if I have to be bitten, bring on the freaking rattlesnake. 

Buprenorphine vs. Methadone

It’s Science, People!

Both humans and animals have opioid receptors in the brain and spinal cord. Biologically speaking, these receptors facilitate the binding and effect of naturally produced pain-relieving chemicals. Externally sourced opioids like methadone belong to the opioid agonist class of drugs. They work by binding to these specific receptors in the brain and mimicking the effects of those naturally produced pain-relieving chemicals. As a result, the perception of pain is blocked, producing feelings of well-being and euphoria, but also side effects such as nausea, confusion, and drowsiness. While opioid drugs are often very effective in treating pain, people can eventually develop a tolerance, so they require higher doses to achieve the same effects. It’s a vicious cycle, so people become dependent, and will experience symptoms of withdrawal if they decrease or stop opioid dosing. That means that when it comes time to taper off of methadone, it’s intrinsically difficult, and withdrawal is unavoidable. Symptoms of opioid withdrawal can include anxiety, muscle aches, irritability, insomnia, runny nose, nausea, vomiting, and abdominal cramping. It’s seriously un-fun at best.

Buprenorphine belongs to the opioid agonist-antagonist class of drugs, and it is a partial opioid agonist. As such, it activates only a portion of an opioid receptor, so it only causes a portion of the effects of an opioid, specifically eliminating the euphoric effects of opioids like methadone. It has lower potential for causing respiratory depression than methadone, and that translates to little potential for overdose death. And it also effectively blocks the effects of other opioids, including heroin and prescription pain medications like fentanyl and oxycodone, so it’s much more likely to discourage relapse in recovering patients. Buprenorphine prescriptions can be filled and taken home, eliminating the need to go line up at a nasty clinic every single day. And because it’s much longer acting than methadone, buprenorphine doesn’t need to be taken every single day anyway, so patients aren’t tied to it; they have the freedom to spend more time doing activities that are more positive for their recovery. When it comes down to tapering off of buprenorphine, it’s far easier than methadone, with essentially zero physical withdrawal symptoms. All of these factors make a big difference, people.  

Buprenorphine Pros vs Methadone

Newer, safer, more effective 

Long acting, easy taper

Safe for use during pregnancy

Low overdose potential

Prevents opioid usage- blocks euphoria

Covered by most insurance carriers

Typically excluded from employment drug screening

Buprenorphine Cons vs Methadone

Can be more expensive out of pocket

Unpleasant taste sometimes reported

Requires specialized physician

In my practice, I treat a fair number of opioid addicted people, and I do not and will not ever use methadone to treat them…it makes zero sense, when there’s an alternative that is more effective, safer, and easier to use. Methadone doesn’t solve a problem, it creates a bigger one. If I have a new patient that is on methadone, I switch them to buprenorphine as a matter of course. It’s not easy on them, but I use every weapon available in my arsenal. 

Methadone to Buprenorphine

In order to start taking buprenorphine, a patient must be in withdrawal, another un-fun fact. This is because buprenorphine is a bully. When you take it, it preferentially binds to those opioid receptors we talked about before. That means it kicks the true opioid off the receptor and replaces it. Doesn’t sound so horrible in theory, but it’s a very different thing in practice. The opioid addicted brain without its favorite thing- opioids- leads to a brain in withdrawal, which leads to a body in physical withdrawal…shakes, sweats, nausea, vomiting, diarrhea, muscle aches, and joint pain, just to name a few of the symptoms to be expected. 

The patient must be in a state of withdrawal for a proscribed amount of time before you can dose them with buprenorphine, because it can be dangerous to give it sooner. The longer they can tolerate that withdrawal prior to dosing buprenorphine, the better the buprenorphine will work and the easier the process will be. The length of the ideal withdrawal time is based on the half-life of the opioid the patient is addicted to. The half-life of a drug is roughly the amount of time it takes for half of the drug to be metabolized by the body, ie that 50% of it is left. For most opioids, 24 to 36 hours is the ideal withdrawal time. But methadone’s half-life is crazy long; in some people, it can be between 88 and 59 hours. But wait…it gets worse. That’s just for half of the drug to be metabolized. It generally takes six or seven half-lives to fully metabolize out a drug so it is no longer biologically active, so in methadone you need to have ten days off before you can safely introduce buprenorphine. Again, this is because that buprenorphine is a bully, and if you introduce it too soon, when methadone is still parked on the opioid receptors, it’s going to kick that buprenorphine off and throw the person into instant, severe withdrawal, which is not only dangerous, but intolerable to patients. Coming off of methadone requires high doses of buprenorphine for the first 24 to 48 hours, even after waiting for it to metabolize out. Otherwise, you can precipitate major withdrawal where that person starts kicking their legs uncontrollably, sweating, flinging sheets off the bed, and having terrible muscle spasms and cramping- it’s a horror to watch, let alone experience. I had a new patient that had become addicted to strong opioids secondary to chronic, severe pelvic pain and a series of several consecutive pelvic surgeries for ovarian tumors. The whole thing lasted for years and culminated in a hysterectomy. Immediately upon release from the hospital after the hysterectomy, she checked herself in to rehab to detox, and they put her on buprenorphine way too soon. Her withdrawals were very severe, to the point where she vomited so hard that she tore 19 of her abdominal sutures open and had to be taken back to the operating room emergently. Needless to say, she wasn’t too keen on the possibility of that ever happening again.  

So what’s a guy like me to do when a methadone-addicted patient comes in? If they’re committed, there are a couple of ways to handle it. Neither is fun nor risk free. One, you can step down from methadone to another opioid substitute like oxycodone in an incremental ratio for three days or so, stop the substitute for 24 hours, and then start buprenorphine. Or two, stop the methadone, wait as long as you can, which is usually two days, three max, of total misery, while using ancillary drugs like clonidine, benzodiazepines (like Klonopin, Ativan, and Xanax), muscle relaxants like Robaxin, and Mirtazapine to sleep. Basically using every drug possible to make the patient more comfortable, hold off on the methadone for as long as possible, and let the methadone metabolize out. Then put them on high dose buprenorphine for 48 hours, then drop to moderate dose for whatever time period is required. 

In addition, there are some dietary type changes that are helpful. Taking high-dose vitamin C acidifies the urine, enhancing the secretion of methadone out of the system. Taking 1000 mg of vitamin C twice a day, drinking slightly less water if possible, and eating a lot of protein will help further acidify the body and constipate the system, which sounds like hell, but is actually a good thing for withdrawal. 

The best way to deal with the situation is not to, meaning avoid becoming addicted in the first place. But, if you do find yourself addicted, do not choose a methadone detox, and definitely do not choose a methadone maintenance program. There’s just zero reason to do that when we have buprenorphine fairly readily available. 

The clear consensus is that buprenorphine is the gold standard treatment for patients suffering from opioid addiction. As a provider, I’ve had the privilege of seeing patients reclaim their lives with the help of a buprenorphine detox regimen; it allows them to focus on their jobs, their families, and their own well-being, instead of physically, mentally, and emotionally battling their addiction every minute of every day, to the exclusion of all happiness.

So boys and girls, the moral of the story is…

Coming off methadone is not fun, and I have had patients who are still depressed, anxious, and unable to sleep- six months, eight months, even a year- after transitioning from methadone to buprenorphine, to the point where they still require medications to deal with it. Xanax and methadone are my two least favorite pharmaceuticals in the entire world, each for their own specific reasons. Clearly, for patients looking to switch from methadone to buprenorphine, it’s a tough row to hoe; the symptoms can be excruciating, especially if mismanaged, but don’t let that stop you from making the switch. My first and best advice is to avoid becoming an addict, but if you do become one, never go on methadone, for any length of time, ever. It’s a trap, pure and simple. 

I hope you enjoyed this blog and found it educational. Please feel free to share it with family and friends. Be sure to check out my YouTube channel with all of my videos, and I’d appreciate it if you would like, subscribe, leave comments, and share those vids! As always, my book Tales from the Couch has more educational topics and patient stories, and is available in office and on Amazon. 

Thank you and be well people!

MGA

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