Buprenorphine, A Short Start. A Bit About Fentanyl | Episode 199

Let me clarify a few things on buprenorphine. I have to be very careful with this because it is just information, it is not medical advice. I want everybody to understand that. If you're going to ask questions, do it with a health care provider.

Is Buprenorphine Used to Treat Pain?

It does help with pain and it's been approved by the FDA for microgram dosing using Butrans, that's a trade name for a patch, for 24 hour administration for moderate to severe pain. That's the indication. There are others that are either injectable or by buccal (oral) preparation for pain control. 

I talked with the panel in Washington DC recently at the ASIPP annual meeting on medication assisted treatment. Buprenorphine is really important for medication assisted treatment, but that's not the only thing it does. It is not only for addiction. I think it's one of the best medications out there for pain control. It's really good and it's also used for addiction, that's in the milligram strength so that's much much more drug given. Microgram is a fraction of a milligram. 

It is a pain medication, and it's a very very good one. Yes, it's used for addiction. Some folks are very concerned that it causes dental decay and oral erosion. It might, it depends on how you take it. The delivery system may do that. A few people were pretty vociferous about the fact that there's going to be class action suits and lawyers are looking at it and that sort of thing. I'm not going to have a dog in that fight. If you have a side effect from medication, let's try a different route or a different medication.

Problems with Buprenorphine

The American Society of Addiction Medicine has had panel discussions, and they've looked at this for years. Particularly in naloxone because the addiction form of buprenorphine, which is called Suboxone, has naloxone in it, and naloxone is a reversal agent for opioids. 

One of the problems with buprenorphine is that it is, like any other opioid, potentially abused, misused or diverted. It's one of the top drugs for diversion. People don't have awareness of that, it's in the top five. If you snort the drug and it's got naloxone, or you inject it, that's when the naloxone becomes active to reverse the effects of buprenorphine. 

What's naloxone? I can tell you I started using that drug years and years ago as a paramedic in its earliest applications. In another life,  I was a paramedic for the City and County of Denver as a field instructor, and we had naloxone in the ambulances. It was a pretty stunning drug. We'd give it and these people who had heroin overdoses (on a very different kind of heroin than is available now) just come up swinging because it just threw them into automatic reversal. 

Naloxone is in there for safety. Yes, it does work. Are there side effects of stomach hurting or headache? I don't know,for most drugs the PDR has headache, most drugs in the PDR have nausea and vomiting, it's just reported side effects. Talk it over with your health care professional. I have not really seen it. I think it's a really good combination, and naloxone and buprenorphine are fantastic in medication assisted treatment.

If I Take Buprenorphine, Am I Just Substituting One Drug for Another?

No, you're not. Buprenorphine is very tightly bound to the MU opioid receptor. That's one of the receptors that induces euphoria, little pinpoint pupils, and it can cause a problem with respiratory depression in the midbrain. The point with buprenorphine is it's pretty safe because it doesn't have a dose dependent problem like a pure mu opioid analgesic. What that means is you give a morphine-like drug and Oxycodone hydrocodone it just keeps going up it just keeps going up and it keeps going up. Whereas buprenorphine flattens out. It goes up for a while, then flattens out. It is tightly bound to the MU opioid receptors. This drug has both a mu effect and another effect on the KOR, kappa opioid receptor. 

What is the kappa opioid receptor(KOR)?

Kappa opioid receptor(KOR) is an important receptor because it's like the MU opioid receptor. It has characteristics at the cellular level that react and afford a response, and it has to do with activating G protein on the receptor transcription through mRNA, etc. The point is that it has an effect, and side effects are not always bad. Actually the Kappa opioid receptor may have a use with addiction, and it may decrease opioid cravings, maybe alcohol addiction. It still has question marks. I'm not going to say it does or doesn't, but there's a promise there.

What About Buprenorphine and Pregnancy?

We know from the American Society of Addiction Medicine and others that buprenorphine is a good drug and as opposed to methadone. If you are taking methadone that doesn't necessarily mean that you should abruptly stop if you're pregnant, especially in the first trimester. You could have a spontaneous abortion and such. You really have got to consult with your OB GYN (obstetric) healthcare provider. Buprenorphine may have less of the withdrawal effect called “abstinence syndrome” in the little one, but again, talk to your obstetrician, talk to your addiction specialist. Can you use these during pregnancy? That's a discussion for your health care provider. Don't do anything on your own, please please please. Talk to a health care provider before you abruptly start or abruptly stop anything if you're pregnant, if you think you might be pregnant, or if you are of child bearing age, etc. I want to make that point very clear, that you need to talk to your health care professional.

What About Buprenorphine and Surgery?

This is a good drug post-op. I don't even stop it for interop anymore, unless the surgeon wants it stopped. We wean them off, we put them on a regular opioid agonist, a morphine-like drug or oxycodone hydrocodone. Remember, buprenorphine is a mixed opioid drug. It has that flat curve. People wonder if it will be in the way of post-op pain control. Actually interop, or in the operation, and post-operatively we can manage, and we can go ahead with surgery. We can work around that stuff. So be sure to talk to your health care professional if you're going to have surgery and you're on buprenorphine, Suboxone - other names are Sublocade, the long-acting 30-day buprenorphine, or Subutex the one without the naloxone. Let your healthcare provider know.

Open communication is important and there are certain concerns about those being treated for addictions. So if you have an addictionologist, that's great, but they aren't always easily obtainable. Henceforth the Health and Human Services folks have made the NP nurse practitioner and the PA  (or the extenders, we call them, to the medical doctor, doctor of osteopathy) able to prescribe this drug, which is a good thing. Availability of this drug is a very very good thing.

Is the Fentanyl Crisis Really There?

The Texas governor Abbott was recently quoted that since 2021, 380 million lethal doses of fentanyl have been seized. That's from the office of the governor. Lethal doses of fentanyl, it's everywhere. I know it's everywhere. I've unfortunately had family members of patients impacted. I think we're all touched by addiction.

How Strong is Carfentanyl versus Fentanyl?

A trunk full of this drug can kill a state. Carfentanil (also known as carfentanyl)  is a hundred times more potent than the standard fentanyl. Fentanyl is 175 to 100 times more potent than morphine. So you're getting hit.  

What are Some of the Current Street Drugs?

• Flakka, that's kind of like bath salts, it can cause psychosis
• Xylazine, there is this really bad drug called xylazine and it's a veterinary drug. It's something you don’t want to be buying on the street or from your buddy. It's not reversible with Narcan, that I am aware of.  So you need to be really careful.
• Phenibut, it's like a benzodiazepine
• Isotonitazene, it's extremely potent. It's more potent than fentanyl. 

These drugs are out there in the street and they're becoming more available. They are poison, they are absolutely poison. 

Over the past year and a half fentanyl deaths in Texas, according to the government, are up 500 percent, 2,000 deaths last year. Yes, there is a crisis. 

With street drugs you don't know what you're getting. You don't know what the potency is. You don't know what the milligram is. Poor per dosing. 

I can tell you about an individual that I'm aware of who bought some marijuana. Well, it wasn't right, it was laced with fentanyl. They were found unconscious in a parking lot, and thank goodness, resuscitated. You don't know what you're getting out there. 

When we talk about pills, they look just like oxycodone hydrocodone because they can be stamped. It is easy to stamp them, so one pill can kill. You get a little carfentanil in one of these pills, it's over.

I have personally given eight vials of Narcan to somebody, and they didn't want to wake up and remember. Narcan decreases the opioid availability - well it does to a certain degree, if it's given right, because it allows the opioid to be metabolized a little while it's working. Narcan only works for about 20 minutes or so. So people re-narcatize, they get the drug built back up in them so they can get real sleepy and in crisis again. It is not a matter of giving some Narcan in the street and then watching them walk away, it's a matter of getting them to the hospital  - call 911. 

Don't mess around, you don't know what they've got if it's carfentanil, or Xylazine which was with the fentanyl, so you must get them to the hospital. Maybe they got  Isotonitazene, they have got to be supported at a hospital level.

There's distribution everywhere, it's not border states, it's not one country. The way this stuff is working is it's distributed everywhere. It's easy to get places, quite a few thousand doses can be placed in a car door. If it's carfentanil, the size of a grain of rice can be an enormous problem, potentially life-threatening. 

Talk everything over with a qualified healthcare provider. This is something you want to talk about with not only your friends, but if you have kids, you know that a party pill is not a party pill anymore, it's potentially life threatening. It's a time to be cautious. But remember, it's also a time to embrace life and enjoy it.