Opioids Lower back pain...

[Ksa]

Dad has this fucking LBP again. Tramadol 50mg + metamizole 500mg does fuckall. He doesn't have CYP2D6 so codeine won't do.

Last time he took 3 dilaudid shots one after the other at the hospital to get pain free, so basically the level of CNS de-activation that he requires has to be like...until he only pees in short squirts.

Wondering if the serotonin increase with tramadol can stack after a day or 2, or is it just hopeless?

 

[Rybee]

Metamizole is quite an odd choice for analgesia nowadays - what was the rationale behind that being prescribed/purchased, over a good NSAID such as Diclofenac/Naproxen/Ketoprofen? Totally different mechanisms, I know, but I'd have thought that either of the NSAIDs listed would offer more pain relief?

Often shot down as a rubbish painkiller, but when co-administered, Paracetamol/Acetaminophen, will actually improve the efficacy of Tramadol in providing pain relief. However, I don't understand why he was prescribed Tramadol as an alternative to Codeine, because it is still metabolised by CYP2D6 (as well as CYP2B6 and CYP3A4)?

It's use is advised against in people deficient in CYP2D6 enzymes (which accounts for about 6-10% of Caucasians and 1-2% of Asians) as they are crucial to the therapeutic effects of Tramadol, by means of enabling Tramadol's metabolism to O-desmethyltramadol.

Furthermore...

As with Codeine, in the 6% of the population that have reduced CYP2D6 activity (hence reducing metabolism), there is therefore a reduced analgesic effect. Those with decreased CYP2D6 activity require a dose increase of 30% in order to achieve the same degree of pain relief than those with a normal level of CYP2D6 activity.

Also, considering that 50mg of Tramadol is actually quite a conservative dose, I'm not surprised that he's still in pain and not getting much relief fro the Tramadol & Metamizole.

So perhaps a painkiller that doesn't need the presence of CYP2D6 to be metabolised would be a better option? Such as:
- Fentanyl
- Buprenorphine
- Morphine
- Methadone
- Oxymorphone
- Hydromorphone

... with Morphine probably being the easiest to obtain by prescription for relief of moderate pain and also quite an appropriate first-choice-step-up from Tramadol.

 

[Kilfer]

Meperidine works great for my sciatica when it flares up but it's hard to get it prescribed from younger doctors nowadays who seem to prefer morphine claiming Demerol is the most addictive opioid on the market. Funny 30 years back it was the other way around and morphine was so evilized it was rarely seen outside hospitals but synthetic opioids were a-plenty.

 

[lifterpuller]

If he needs IV dilly to get the pain relief necessary there is NO way 50mg of tramadol is going to suffice, probably not even higher dose trams where you are entering seisure threshold levels. He should try to get some oral morphine, IME it was the best for pure pain relief, however oxycodone made me more functional and less drowsy/noddy.

 

[bobjayne]

Meperidine works great for my sciatica when it flares up but it's hard to get it prescribed from younger doctors nowadays who seem to prefer morphine claiming Demerol is the most addictive opioid on the market. Funny 30 years back it was the other way around and morphine was so evilized it was rarely seen outside hospitals but synthetic opioids were a-plenty.

Each opipid is addictive as the next.

Drs are trying to phase out pethidine as it has s toxic metabolite which builds up in your system after enough time and can prove to be toxic. By rights it should be taken off the market like (forgetting the name right now). Avoid the shit at all costs.

Wondering if the serotonin increase with tramadol can stack after a day or 2, or is it just hopeless?

It works in my experience. I've been using tramadol on and off over 10 yrs in combination with morphine and oxy for a DDD.

 

[Ksa]

You see the thing, 1mg hydrocodone makes him dizzy and works, but 75mg of tramadol or 120mg of codeine has no effect. Would this be grounds for saying he doesn't have the enzyme?

 

[bobjayne]

Can't say for sure myself. It could be that just those particular drugs aren't effective with him.

I found this article.

The clinical report presented here contains the only collection of pain patients with CYP-2D6 deficiencies that have been systematically studied. There is a practical salient point in this article for pain practitioners. Any patient who doesn’t respond to hydrocodone or low dosages of oxycodone may have this genetic defect.


Forest Tennant, MD, DrPH
Since 2005, I have been testing patients for cytochrome P450-2D6 (CYP-2D6) genetic abnormalities. This was when the blood test was first available for use by us clinicians in private practice. An abnormality of the CYP-2D6 enzyme may be referred to elsewhere in this paper as a deficiency or defect. All told, I’ve tested 15 patients who I have suspected—on a clinical basis—of having a CYP-2D6 genetic defect and, indeed, all have shown an abnormality (see Table 1). This includes myself and my brother. Included in this cohort is a single patient who has CYP-2D6 gene duplicity and is termed a rapid- or ultra-metabolizer. The clinical history of these persons is quite typical and I share this information to help practitioners identify pain patients who may have a genetic defect of CYP-2D6. They will likely not respond to some opioids. These patients may require high dosages of opioids or may be falsely accused of drug-seeking behavior

Full article - Non-responsive Pain Patients with CYP-2D6 Defect

I know its related to oxy and hydrocodine but may help you.

 

[Ksa]

Thank you Bob.

 

[bobjayne]

No problem.

 

[JackiePeyton]

Have you visited the Pain Managment Thread?
Pain Management-Megathread-(Chronic and Acute Pain Discusssion