enhancing pain medication

I’ve heard from those who should know that white grapefruit juice amplifies the effect of methadone. My doctor said “Huh? What? Oh fer … ask Cecil!”
So, Cecil, as someone in constant disabling pain from peripheral neuropathy, I must know: Is white grapefruit juice a gift from the comfort gods, or just a nice fluid to mix a double rum into?
RaineyCat, preparing her daily dose of vitamin SeeIfItDoesn’tHurtAnymore

I am not a doctor (and this thread probably belongs in IMHO).

When you take any drugs, your body starts metabolizing it to get rid of it, which happens at some certain rate of speed. (A lot of this happens in your liver) You take more doses to maintain the desired on-going dosage in your bloodstream. The doses prescribed by your doctor, in their size and timing, are calibrated to accomplish this.

There are certain enzymes that do this work. They can only process so much stuff in a given time. Grapefruit juice, it turns out, contains some chemical that is metabolized by the same enzyme that is also in charge of dealing with a great many drugs.

By giving your enzymes this extra load of work to do, when they are already working at capacity cleaning our your methadone (and many other drugs), it follows that the drugs will not get cleaned out as fast. They will stay in your blood longer.

Note the implications. First, this means you will have a greater concentration of the drug in your blood than your dosage was intended to create. It also means that, as you continue taking the drug, your enzymes will fall farther and farther behind in their work, and the blood level of the drug will increase.

So, the drug becomes more effective simply because you have more of it in your system. This is not necessarily a good thing. It also means you are at risk of overdosing on the drug, resulting in whatever adverse effects you could get by having too much drug in your system. This could be dangerous, or even seriously dangerous, or even fatal in the extreme case.

Take a look at this. I see methadone is on the rather long list of drugs that interact with grapefruit.

Welcome to the boards!

Senegoid wrote: By giving your enzymes this extra load of work to do, when they are already working at capacity cleaning our your methadone (and many other drugs), it follows that the drugs will not get cleaned out as fast. They will stay in your blood longer.

Note the implications. First, this means you will have a greater concentration of the drug in your blood than your dosage was intended to create. It also means that, as you continue taking the drug, your enzymes will fall farther and farther behind in their work, and the blood level of the drug will increase.

So, the drug becomes more effective simply because you have more of it in your system. This is not necessarily a good thing. It also means you are at risk of overdosing on the drug, resulting in whatever adverse effects you could get by having too much drug in your system. This could be dangerous, or even seriously dangerous, or even fatal in the extreme case.


Thanks to you (and Wikipedia) I’m now aware of the overdose potential and can adjust the amount of methadone I take with the grapefruit juice. Pain-free isn’t possible – less pain IS possible! YES!!
Having been in chronic pain for 13 years, I’m not particularly concerned with what “might” happen – the reality is constant, grinding discomfort from damaged nerves that has become unbearable and turned my life into a grim daily struggle. Drug abuse changes personalities. No question. So does long-term physical pain, which actually changes the brain’s structure.
I used to be fun to be around. If I could trade what’s left of my life for one month of relatively pain-free existence, I’d do it. Those who used to love me and need me do not need the pitiful thing I’ve become. More important, I don’t like that person. If there’s a chance that grapefruit juice could help bring “me” back again, I’m going for it.
Scrambling for help like this wouldn’t be necessary if doctors were permitted to prescribe sufficient pain medication, rather than look at their patients as drug-seekers out for a quick high. Maybe this makes me a libertarian, but let the over-18 morons who only want to get high GET high. If they’re stupid enough not to understand the risk of overdose maybe the world is better off without them. Sorry if that sounds cruel, but I’ve lost all patience with the “war on drugs” since I’ve become part of the collateral damage.

Grapefruit juice can alter the metabolism of some drugs, because of the CYP (cytochrome P-450) group of liver enzymes. This is why some prescription labels say to avoid it; people have had fatal reactions as a result, or in some cases rendered their medication worthless.

NWH, RPh

No!! I think you’re getting the opposite message here. What you should be doing is not drinking grapefruit juice. You still have no idea about how it might be effecting your medication, and self-adjusting your meds is something I’m pretty sure your doctor will frown upon.

You’re treating “chronic pain” with methadone and talking about how to use grapefruit juice to extend your high. Are you sure that you don’t need addiction treatment? A lot of pain can be caused by the brain trying to get you to use more opiates.

I think you should start by stoping your drug addiction .Methadone is not necessary for peripheral neuropathy . And mixing grapefruit juice with it is a attempt to get higher.

Actually, methadone is about the only opioid to demonstrate some efficacy in treating neuropathies. It would not be my first (or second, or third, or fourth) choice to treat a neuropathy with, but when other approaches have failed to adequately treat the symptoms, it could be considered for use in carefully selected patients.

Trying to use grapefruit juice to alter how your body metabolizes drugs is just silly. And dangerous.

So, do you use methadone with patients who fail SSRIs/anticonvulsants (and the gabapentin/SNRIs/TCA trio of first line stuff, I presume), or is there another option you like better? Is the literature on methadone really better than any of the other opioid agonists?

(Not second guessing you, just interested in what PCPs find works in the real world vs the latest report from the Journal of Pain Models in Rodents that Probably Work Kinda Like People. ;))

And, yes, OP, trying to muck around with your liver biochemistry via grapefruit juice is a really, really bad idea. Stick with the occasional Greyhound or Sea Breeze instead. :cool:

I had to stop eating grapefruit when I started taking some medication (don’t remember what) which was a downer since I loved eating grapefruit. Odd that other citrus fruit doesn’t do that. Now I have to moderate the consumption of some other foods (not too much green and leafys, especially kale, which I love, and chickpeas) because they interact badly to a different medication (warfarin).

It’s more expert opinion at this point. Not the most solid thing to hang one’s hat on, but when one has exhausted other modalities, there it is.

I only employ opioids when other more reasonable agents have failed, and we’ve established definitive objective functional goals to be met due to opioid rx. Fail to meet the goals despite adequate doses, and the rx is stopped. Be seen to be meeting those goals without opioids, and opioids won’t be started.

I’ve one guy on it now for inflammatory autoimmune polyneuropathy, and he’s met his goals thanks to methadone. But I think he’s gaming it a bit, requesting more potent short-acting opioids instead. And his subjective complaints of pain despite methadone use are not consistent with objective evidence.

It’s a tough problem to treat.

Most doctors would just tell them to suck it up. Neuropathy is not that bad, but is a good excuse to start a long term drug addiction.

Says someone who’s never experienced it.

I have had patients, middle-aged homemakers and semi-retired high school math teacher, asking me how they can arrange to have their (affected) limbs amputated. Those folks and others have also contemplated suicide. “Not that bad”?

Phrased differently, you should heed Lincoln’s* sage advice (you know, about “removing all doubt”).

  • some sources attribute it to Mark Twain

Respectfully as possible: you have no idea what you’re talking about.

Drs go round and round about how to quantify pain. I have sufficient pain to comment, but get by on otc nsaids, vodka, meditation, and hot baths, and I’m very happy. I think if I had been through everything a Dr. had to offer and found myself on methadone I’d get completely straight and find out what my pain really is, then start over with a couple Advil and some new Drs. Odds are always high that your Dr is a fool.

Absolutely. You’d have to have a death wish.

That said, the concept has been exploited therapeutically. For instance, when cyclosprine was VERY expensive, attempts were made to diminish its clearance by using a cytochrome enzyme inhibitor, thereby allowing for fewer doses by keeping it in the system longer. That was done here (with ketoconazole playing the role of grapefruit).

I wish this was the right forum to tell you what I think of you after that statement. Like KarlGauss’ patients, I’ve thought many times that killing myself would be preferable to living with the pain I get during a flare-up, but I have 2 kids and I could never do that to them.