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Opioids Can You Reverse Grapefruit Juice Potentiation ?

Altered Perception

Altered Perception

Bluelighter
Joined
Dec 13, 2010
Messages
414
Location
On a big Island surrounded by sharks.
I've got this rare medical condition called Dysautonomia and most annoying part is the hypersensitivity I have towards all subtances that have an effect on my damaged Autonomic Nervous system and even the smallest amount of any depressant or stimulant causes an adverse reaction and distruption in my vitals

I had some sucess in the 3 years of attempting to desensitize myself to opiates in order to manage my chronic pain however recently I did something stupid and tried Grapefruit juice potentiation which has ruined all my years of hard work and further distrupted my metobolism and tolerance levels to my medication.

I am now very confused because even after ceasing to drink Grapefruit Juice since 6 days ago I seem to be still experiencing the effects of the potentiation and I' wondering when will this Grapefruit Juice stop interfering with my cytochromethe enzymes and allow my tolerance to return back to normal?

I have not been able to find information online stating how long the effects of Grapefruit Juice continue to influence the effects of opiates however in my case case even after 6 days of absence from Grapefruit Juice I'm still unable to take my regular dose of Oxycodone due increasesd sensitivity and prolonged adverse reactions which seem to last 3 times more longer then they used to before I started on Grapefruit Juice.

I've suddenly had to pull back from my regular 18mg dose to 11mg dose which now feels exactly what 18mg useed to except that the adverse reactions seem to last a lot longer now.

Grapefruit Juice has seemed to have causes some abnormal changes and shifts in my reaction and tolerance levels. today I took a single 50 mg tramadol believing the effects would be milder then Oxycodone and 9 hours after having taken it I am still feeling that familiar tramadol buzz lingering on even though I havent had grapefruit juice in 6 days but obviously as my body indicates the potentiation is still at work. So I want to know is there way to undo all this and reverse the effects of the cytochrome inhibition caused by Grapefruit Juice?
 
I would take an enzyme inducer to reverse the inhibitor.

This makes sense, yes?

Look at what they would be here.

Modafinil and phenobarbital and/or possibly other barbiturates appears to be your best bet. Although St. John's Wort would probably be the "OTC" version of trying to do this.

Pegasus said:
This is probably better suited in ADD, in my opinion...
Click to expand...

Why? We talk about inhibitors here, why not inducers as well as inhibitors?

This is very much so Other Drugs material.
 
^(@C.H.)We do, it's just that ADD definitely has more knowledge on certain medical topics. It's your call of course, I'd like to know the answer for this as well, however it comes about.
 
Altered Perception said:
I posted in there a few days ago but despite all the views no one replied in it, They always act so territorial and anti-social and I don't think they like me either beacuse I've had my share of arguments with them in the past and since they havent responded to any of my topics.
Click to expand...

Well I'm glad I could help you out and not be snide about it! ;)

Altered Perception said:
Captain Heroin, you always come to my rescue, your such a cool and helpful guy, I feel like I owe you alot, thanks.
Click to expand...

:D You're welcome, any time.
 
^(@Altered Perception) That's unfortunate... Maybe no one that read it knows the answer though, as it is a pretty specific question. I've read a great deal about CYP450 inhibition but have never come across this specifically.
 
One final question...

If someone wanted to reduce their opiate tolerance down can they use something like this situation to their advantage?...

Even though 18mg Oxycodone is not alot I have still been meaning to take a break and hopefully reduce my tolerance back down and I noticed since the grapefruit juice I can now only tolerate 11mg because of the potentiation. So 11mg feels exactly like what 18mg did for me before the GFJ (took me a while to find the right dose)...so hypothetically speaking if I continued to do this 11mg and took more grapefruit juice whenever required will i find that eventually (maybe after several months) my tolerance would have dropped down from 18 mg to 11mg even in the absence of any potentiation ?

This is just a hypothetical question , I will never use grapefruit ever again because it is more trouble then its worth but just curious if one can reduce tolerance down through this method.
 
Captain, when I posted here I was reluctant because I was not sure if there was a substance that could act as an "inducer" of cytochorome enzymes but it seems I'm in luck you gave me exactly the help and response I needed.

I will look further into all this but do you know of any natural "inducers" ? As you know there are syntheticly made "inhibitors" like cimetidine, quinine that are phramecuticaly made but you can also find natural ones like "grapefruit" so I wanted to know is there a natural equalant for "inducers" that I can consume from nature or foods ?

EDIT: nevermind I re-read your response and it seems " St. John's Wort " is the natural version.
 
Altered Perception said:
Captain, when I posted here I was reluctant because I was not sure if there was a substance that could act as an "inducer" of cytochorome enzymes but it seems I'm in luck you gave me exactly the help and response I needed.

I will look further into all this but do you know of any natural "inducers" ? As you know there are syntheticly made "inhibitors" like cimetidine, quinine that are phramecuticaly made but you can also find natural ones like "grapefruit" so I wanted to know is there a natural equalant for "inducers" that I can consume from nature or foods ?

EDIT: nevermind I re-read your response and it seems " St. John's Wort " is the natural version.
Click to expand...

I edited it in quick and ninja-style (meaning, there is no "Last Edited by..." link), and there is a list of inducers. There might be other ones from nature that I skipped over or didn't click and read, since there is a lengthy list.

Also, there are "strong", "moderate", and "weak" inducers. So you have many options, as well as multiple strengths.

St. John's Wort is definitely probably going to be the easiest to get since it's found in most grocery stores. :)

The problem with using phenobarbital in this scenario would be that it would potentiate CNS depression from opiates.

And, you may not want to consider using modafinil or other stimulants, because of your unique condition, so it would be best to stick to something like St John's Wort.

I believe it has its own interactions with drugs though, so make sure to compare St. John's Wort to your medicines, and make sure there won't be any negative interactions.

I'm not sure if oxycodone is the only medicine you use regularly or not. :)
 
Yea your right St John Wort is very easy to find, thats exactly why I was considering a natural alternative.

I dont know much about inducers yet but I'm assuming its sort of like a detox for the liver because if "inhibition" slows down absorbtion and increases blood levels then I assume "inducers"would do the opposite by increasing absorbtion and allowing liver to function more rapidly and freely but I dont know yet what side effects this would have, you said it would also " potentiate CNS depression" but I'm not exactly sure what this means, but I assume it causes more sedation?

Because of my sensitivity I keep my medications to a minimum so I'm only taking betablockers (metaprolol) to manage the Dysautonomia and Oxycodone for pain so I should be pretty safe with any interaction.
 
Captain.Heroin said:
Did you read my answer?
Click to expand...

Yeah, I did... I'm not criticizing your idea, I think it probably would work. I just want to know for a fact the answer to this. The action is more complex than just at 3A4, it is also at 2D6 and others.

I still love you man!
 
There is very little chance that the grapefruit juice you drank 6 days ago is having any appreciable inhibitory effect at this point. The clinically measurable effects typically dissipate within 3 to 7 days, but the effects are so small after a few days that there shouldn't be any individually perceivable effects.
 
Dokomo, honestly believe me it is having an effect and its not placebo. I have always had a threshold to opiates due to my hypersensitivity, this threshold does not allow me to go above my acquired tolerance, it has been this way for the past 3 years since Ive been taking opiates everyday, if I happned to go 1mg - 2mg over my dose I end up in the ER often with bradycardia accompanied with hypertension, fever, muscle spasms, headches, neck stiffness so the effects are immidatly visible and measurable when I go over my dose...

The next day after the Grapefruit juice when I took my regular dose believing the effects of the GFJ was only temporary I ended up having one of the worst reactions to this date, it toook me several more horribe reactions to finally work out my new threshold was now at 11mg, thats a 7mg less from my usualy dose.

before the GFJ if I ever took 11 mg it would have been a total waste as it is an innefctive dose for me however on 11 mg I get the same pain relief and the same buzz I got at 18mg and there is no mistaking that sensation from Oxycodone after 3 years of using, its like giving an addict half his dose and expecting them to be satisfied, most wouldnt because you could not placebo that effect but I am quite satisfied on 11 mg since my GFJ usage 6 days ago. How do you explain that?
 
Enzyme inhibitors work by binding to the enzyme in place of the substrate. There are reversible and irreversible depending on type of binding (noncovalent vs. covalent) and a bunch of subsets of irreversible as well depending on the exact mechanism of action.

Enzyme inducers also bind to enzymes thereby making them more active. I don't know what type of inhibitor grapefruit juice is and either way trying to assess how it would react with an inhibitor is well beyond me.

Altered Perception I recommended not playing around with your enzymes in the first place and now recommend not playing around trying to fix them as well. Just let them be and eventually time will get you back to where you were before grapefruit juice.
 
amapola, you did recommend I dont play with my enzymes in the first place and now I regret not having listened to you, I can be so stupid sometimes, I'm also sorry I didnt give you enough credit

I just thought I could pull this off sucessfully but I failed and I guess I have stop messing around with myself and accept I'm not like everyone else because my body is already damaged I have limitations but sometimes I go into denial and try to push myself because I want to be normal again but I just end up making things worse :(

Your right I'm going to give it time and if it dosent resolve then at least I have the option of inducers but thats plan b. Thanks <3
 
There is a difference between being normal and having limitations. Since your incident you've spent years dealing with pain management, body temperature issues and other medical problems. Now you have a dose of oxy which is working for you and I'm sure has greatly improved your quality of life. There are many people who live completely normal lives taking daily medication and just like you lots of them have very precise dosing which they can't afford to change.

I'd hardly say not being able to safely adjust the effects of a dangerous sensitive medication with enzyme inducers and inhibitors is not normal :)
 
Guys, being the curious creature I am a question has been eating away at me...

Lets say for example someone has a 50mg Oxycdone tolerance and this person decided to drink a litre of grapefruit juice together with taking 50mg Oxycodone with it and as a result the 50mg felt way too intense almost as if he took 70 mg and the person began to overdose...can this person hypothetically speaking consume a sufficient amount of rapid acting "inducers" to immedeatly reverse the effects of the "inhibition" caused by the Grapefruit Juice thus reversing the effects of the overdose?

This is just a hypothetical question, nothing I will ever try, I just like to learn =D
 
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