Buperenorphine a voltage gated sodium channel blocker possibly cardiotoxic?

[purplehaze147]

So I just read that buprenorphine acts as a voltage gated NA channel blocker. This action is what causes cocaine's cardiotoxic effect primarily & also it's strong numbing effect. Would taking it daily long term cause damage to the heart? I'm not sure how powerful of a VGSCB it is. Perhaps I should dissolve it & rub some on my lips & skin to find out, don't feel like wasting one right now though those things are pretty valuable. I doubt it's really bad for you but I don't know.

I'm just asking because heart complications are the leading cause of death in humans (at least in the U.S.). I'd rather not die of a heart attack, preferably I'd like to go peacefully in my sleep or doing something heroic. I just found out my dad has an enlarged heart & my uncle who was like 45ish recently died of heart disease so I'm a little worried & want to keep my heart healthy.

Are opioids in general bad for your heart? I heard that somewhere, she said opioids are toxic to the heart because they lower blood pressure while increasing heart rate. I take what she said with a grain of salt because she said weed is also cardiotoxic & she is an addiction counseler.

... By the way does bupe block endorphines?

 

[sekio]

It's not very potent as a Na channel blocker.

 

[adder]

Are opioids in general bad for your heart? I heard that somewhere, she said opioids are toxic to the heart because they lower blood pressure while increasing heart rate. I take what she said with a grain of salt because she said weed is also cardiotoxic & she is an addiction counseler.

This is not really true. Your heart may start beating faster as a response to an opioid suddenly lowering your blood pressure, but it's not really an opioid effect. However, buprenorphine has a two-stage effect on your heart rate after ingestion. At first it causes a slight increase in heart rate and then there's a more pronounced decrease. I don't know if there has been any research done how it is related to buprenorphine metabolism and levels of its metabolite norbuprenorphine, but I can imagine that the increase in heart rate is due to buprenorphine's kappa antagonism (and perhaps also due to its mu partial agonism) and then the following decrease is due to norbuprenorphine's mu agonism. Norbuprenorphine is less lipophilic than buprenorphine due to the secondary amine, as a result it's more toxic and has a lower therapeutic index because its effect on peripheral opioid receptors (like for instance in the heart) is stronger. I've recently been often experiencing arrhythmia around an hour after taking Suboxone, which seems strongly related to norbuprenorphine starting to take an effect. It's also associated with increasing mu opioid effects when I dosed lower on the previous days. I'm at 4mg a day right now and I take it all at once, so the opioid effects are more pronounced. At different doses (and different ratios of bupe/norbupe levels) the toxicity may be different in theory.

 

[purplehaze147]

Ok so it shouldn't be too bad for ur heart even when used long term? I've never noticed any arrhythmia from it. & yea it probably isn't too powerful as an NA channel blocker I don't notice any numbing under the tongue I feel kind of dumb for saying I should rub it on my lips lol :/

 

[adder]

I seriously doubt that there is much risk unless you've got some problems with your heart unrelated to your buprenorphine treatment. In my case it may be actually more related to vitamin D3 deficiency as my arrhythmias started more or less around the time when I noticed increasing fatigue and problems with my immune system. I've recently got blood work done and it turned out that I had only half as much D3 as the minimum is. I also probably use too much caffeine and nicotine, which can cause arrhythmias themselves.