Dr Casey Parker
Dr Casey Parker examines which is best to prescribe.
If you’re like me (as a rural GP), you probably started noticing a trickle – and then a flood – of patients being discharged from big city hospitals on this new drug tapentadol.
Now, I am a simple rural doctor. When I saw the name tapentadol, I immediately assumed that it was a new version of tramadol, but with more letters to confuse the chaps over at the patent office.
I was sort of correct. These drugs are very similar, so it’s worth comparing them.
Tramadol is possibly one of the most maligned medications in a GP’s toolbox.
It’s an opioid used for pain management. But it’s unpredictable, with a lot of side effects, and often just doesn’t provide much relief. It’s an older drug, dating back to 1977.
Tramadol is a prodrug. That means, on its own it doesn’t do much of anything. It gets metabolised in the liver by the cytochrome p450 enzymes into a few active chemicals.
But here is the problem – the actual amounts of each of the active metabolites is a bit of a genetic lottery. Depending on the makeup of your cytochromes, you may get:
- a bunch of destramadol (aka M1), which has a strong mu-opioid receptor affinity and acts like morphine
- some venlafaxine, which is a serotonin/noradrenaline reuptake inhibitor (SNRI)
- a mixture of both of the above
- a whole bunch of other receptors, such as N and M acetylcholine, direct serotonin agonists, and the list goes on.
To some extent, you can ask a patient what effects they felt if they had a dose of tramadol previously.
In my experience, you get pretty clear likes or aversion to tramadol. The most common reply is along the lines of, ‘Oh, the drug that made me spew’.
Then then there is the risk of serotonin syndrome and seizures. This may come about for a few reasons:
- Older patients or people with renal/liver disease don’t clear metabolites and they build up
- Combining it with other serotonin norad-active drugs like antidepressants leads to a double whammy
- Patients with little metabolism to M1 take more and more doses to achieve analgesia and end up with a bunch of the SNRI metabolites in their systems
All in all, a tricky drug to use, since different patients may have a totally different experience with the drug.
Now let’s introduce tapentadol, first released in 2008. It’s the new and improved version of tramadol, which is arguably not hard to do.
So, how is the new kid on the block different?
Tapentadol is not a prodrug – it does not rely on metabolism to get it working. So it is what it says on the box – an opioid analgesic. In addition:
- it has a strong mu-opioid receptor agonist effect, similar to oxycodone
- it has noradrenaline reuptake inhibitory effects, but not much effect on serotonin reuptake, which makes it a little cleaner
- there are no active metabolites yet known – so that sounds cleaner, too.
That all sounds nice and neat. A cleaner, direct-acting opioid with fewer side effects. But there must be a catch, right? There always is.
The biggest issue is that there is just not enough data available about the safety or efficacy of tapentadol. In the trials used to get it registered, the drug was only just better than a placebo for chronic pain. We need to see some real-world safety data and clinical outcome studies to say exactly how much benefit this drug has.
As with any potent opioid, tapentadol is to be used with caution in patients with respiratory failure, other sedatives or noradrenergic agents. It needs to be avoided for at least two weeks after ceasing monoamine oxidase inhibitors (MAOIs) such as moclobemide (though this is rarely used in Australia).
Tapentadol side effects are predictable: constipation, nausea and vomiting with some dizziness in up to a third of patients.
The risk of developing tolerance and potential for abuse or diversion is likely to be similar to other opiates once the word gets out. This is definitely one to watch carefully when prescribing.
Tapentadol is probably better than tramadol. Which is akin to stating it is funnier than the MIMS – it’s a low bar. It has a more predictable pharmacology, but the evidence is not yet in. We just don’t know the full risk/benefits in 2018.
And don’t be fooled by the ‘less abuse potential’ argument; it is a new drug and the same statement was made about oxycodone many moons ago.
Watch this space.
This article is adapted from Dr Casey Parker’s blog, Broome Docs.
drug mechanisms Tapentadol tramadol
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NEVILLE LUDBEY 31/08/2018 10:33:13 AM
GREAT ARTICLE – WISH ALL PHARMACOLOGICAL EXPLANATIONS WERE AS EASY TO FOLLOW.
Nadette 31/08/2018 1:13:40 PM
Thanks Casey, a great read, not often I get a laugh out of analgesic education!
Neel 31/08/2018 2:10:03 PM
Nice article Casey. Very easy to read.
Maria 31/08/2018 3:27:10 PM
Wow, you made that make sense .. answered a lot of questions! Thank you
Jana 2/09/2018 11:15:15 AM
Thanks Casey, good information !
Andrew Lane 4/09/2018 11:11:22 PM
Nicely done. Thanks.
Natalia 5/10/2018 12:48:22 PM
Great article! Look forward to seeing more from you in NewsGP.
Kamlesh meghwal 22/10/2018 11:16:04 PM
Cliff 24/10/2018 5:14:01 PM
Have been on Tapentadol 200mg slow release for chronic knee pain and arthritic pain for approx 6 months. I tend to have addictive traits. Smoker until 6 yrs ago. Drinker
Moderate most days yet i can not say the Tapentadol has any addictive draw to me. Even now i can stop taking it for a few days without withdrawls except return of increased pain. Anyway better than the highly addictive Oxy meds.
Charlotte 8/11/2018 2:45:34 AM
Wow, this was an interesting read! I'm currently on Tramadol, and I've been for nearly 2 years for chronic pain with 2 herniated discs in my neck (C4/C5, C5/C6), impingement syndrome in my left shoulder and so forth. I see now that I am in the latter category, the one that builds up tolerance. And that's a shame, because I'm terrified of drugs like these, but my pain was overwhelming. When I started taking it, I could do with 1-2 a day, and I had days where I didn't take any- mainly because I was too scared, not because the pain had lessened. Now my dose is anywhere from 3-5 in 24 hours, where 5 is a really bad day. I never take 2 at once, being a scaredy cat, and I monitor very intently when I took the pill. I was considering talking to my doctor about going cold turkey, but honestly I'm afraid of the pain becoming worse – and then have no form of lessening it. Should I try this other one, or just quit it all and see how it goes? Been with chronic pain for nearly 5 years now, and I'm 25 years. I'm tired of being in pain and tired of being tired.. Thank you for this post! Very informative, and a fun read.
Stevie 9/11/2018 8:28:10 PM
Is there any ssri or ssni in this drug like tremSR ?
Sandra 12/03/2019 1:46:41 PM
Charlotte, you poor girl, 25 and in so much pain! ☹
I've just had knee surgery, the hospital gave me tapentrool IR 50mg for the pain but I haven't taken any as I find all these things make me sick lol
But what I have started taking is ( now don't laugh, it's working!) Is ….. wait for it….. gelatine! I did the same after shoulder surgery a few years ago and that also worked unbelievably well, yep just plain old gelatine, get on the net and have a look at all the info on this , you will be surprised, I use about 1/2 a sachet a day , have used no painkillers for my knee at all.
Good luck I hope you get this as this post is fairly old.
Duncan 13/07/2019 2:46:19 PM
I have been experiencing pain and tingling in my left arm, which was later diagnosed as from a pinched nerve around C7 in my neck. Had Endone for 2 weeks for pain management, did not like it. Tried twice unsuccessfully to have Spinal MRI, even after taking 2 Endone before my second attempt. GP prescribed Targin – did not like, very wary of addictive properties of these oxycodones. While waiting to see neck specialist, GP suggested Palexia 50mg sustained release (Tapendatol). Started with 2 at night, got down to 1 per night within a fortnight. Used 2 hours before successful MRI. When I finally got results from neck specialist he deferred possible surgical procedure due to my controlled pain situation. Have now been off Palexia for over a week. Have 2 paracetamol tablets a day. Feel confident now that Palexia's Tapendatol worked well in my situation with less side effects than the oxycodones.
Nick 31/07/2019 9:45:49 AM
The mu-opioid receptor effect is much weaker than oxycodone. That’s what makes it safer, less addictive, and less euphoric. It is very effective, however, because unlike oxycodone it also utilizes noradrenaline.
Marie 18/10/2019 10:55:34 PM
My has had chronic pain for over five years tried everything from dry needling nerve blocks nothing worked her doctor gave her palexia to try . First time she took it she was pain free so excited. But this was the start of hell for me she got euphoric feeling from it then she started taking higher does she would be erratic at night scratching herself talking constantly totally different person then sleep till 2 in the afternoon because it kept her up all night . She wouldn’t remember what movie she watched or what she ate . Then it got to the point where she got depressed from it ,crying and saying she didn’t want to live . It is an opioid it’s now 18 months later and she takes opioids I have tried everything to try and get her to stop taking them but there is always a reason why she needs to take them . I wouldn’t wish this on anyone. Opioids maybe great for short term pain but they should never be given to someone with chronic long term pain .please be careful about what medications
Andy McCracken 23/11/2019 1:49:32 PM
Have been taking Tramadol for over 1 year ,was prescribed for pain from torn tendons in the shoulder , but I also found I would wake up feeling good , whereas before I would have to sit in a chair for 1/2 hr feeling crap , now the pain has gone but I was still taking them for the feeling in the morning , then a locum Dr said to get off them and try Palexia sustained release which I have been on for a few days but I wake up feeling crap and walk around like a zombie
Helen 10/01/2020 2:14:29 PM
I've had a really unusual experience with taking Palexia IR before I get out of bed in the mornings. I would do this to get on top of the pain and then take 50 mg with breakfast. The pain has been extreme for 6 approx months. I did this as my usual beginning of the day but the pain felt like it fort back angrily. It was excruciating and now as I have stopped taking the IR before I suffer every morning. Have I finally gone mad.
Kobus 11/05/2020 7:41:23 PM
Thanks for a very straightforward and easy to understand analysis, I've been on oxycodone for sometime now and it's ceased to be effective except at doses that are becoming way in excess of what I'm comfortable with, my pain specialist wants to shift me over to Tapentadol but I like to research these things before I agree to it… your comparison has been the clearest I've read thus far.
Paula 18/05/2020 5:28:01 AM
Been on 100mg SR Tramadol for about 9yrs due to chronic back pain from horse riding accidents. started taking 50mg as needed got to needing it everyday just to be able to get out of bed without back spasms. thank god it works, doesnt leave me feeling like a zombie which simple paracetamol does these days. 1 of them flattens me for 4hrs but i feel drugged up for a couple of days. Not game to try this other drug for fear of it not working and being in constant pain again. Aint broke dont fix it i say.
joy west 7/07/2020 1:38:54 PM
I have been in cronic pain for about five yes , from a pain in the tummy to sever cronic pain, and nobody can tell me what it is, I have had every test, every scan, every thing that is going, I have taken TARGIN 30mls for about two years and I have had to fight doctors to get it, it is the only medicine that gives me relief .I have moved to another doctor because my doctor I was seeing for two years refused to give me any medication at all i was in bed and my husband tried to find out what was going on and I am going to another doctor and the same thing I have to beg for help, what is another medicine that is available to me , I can't go on much longer please help
Tina B 6/08/2020 10:28:31 PM
Been on panadeine forte for many years after a multi trauma accident. Since sleeve operation can’t take them any more due to severe nausea. Have tried Tapentadol and no nausea. Only take prn. Seems to do the trick.
Marie 19/09/2020 11:44:12 PM
My daughter was prescribed palexia in 2018 by her gp for chronic shoulder and neck pain. From the first dose she was hooked on it after 3 months on it became suicidal . Her doctor told her to stop taking it but it was too late she dependant on it getting it from other doctors and different medical reasons. Then got it off a friend without prescription on line and ended up in a bad place. She is now getting help from her pain specialist to taper off it . It has been over 2 years of hell and still a long way to go . I wouldn’t recommend opioids to anyone. It destroys people and there families.
US Tramadol 100mg 23/09/2020 3:50:24 AM
Tigger 18/10/2020 4:08:40 PM
Done everything… Used used et cetera and lost good friends. Stopped until what apparently was my knee blowing out and starting from forte and codeine/Nurofen, and it up on just about everything anti-inflammatory or opiate due to 4 years of misdiagnosis during which I was having 125 mL effusions nearly monthly on my knee. Went back to Sydney after almost 10 years as couldn't work in construction anymore. Had a pharmacy background and when started at the rehab center ass disp tech and told the pharmacist about tramadol in 2000, 153with ABIs were switched much to their distaste. Also Have double Medicinal/organic Chem, couldn't take tramadol myself. Only recently heard of tramadol derivative and in currently ketamine infusion to reset Receptors. At one stage I was the second highest prescribed pain NSW on the equivalent of 5 to 7 g of Morphine, wish I could have started biogenic straightaway
Sandra Johnston 29/10/2020 11:43:19 AM
I’m 66 y/o woman with past history of nursing. I lifted people and my back was bad. Did everything in the book. Have taken analgesia since age 18. Now on Tramadol AND targin 30 twice a day. My doctor wants me to try tapendol but I’m fearful of the amount of pain I have and might feel. I’m desperate to hear someone say they too have done this. Anyone ?
Innerdaze 3/01/2021 12:57:08 AM
Joy, get checked for gallstones. Dr Casey, good understanding of the pharmacology. Be careful with this one as it’s more potent than one would expect, easy to increase the bioavailability beyond the stated 30%, and quite europhoric at first even for someone who put up with the dirty tram Adolf for years before it became contraindicated. Much cleaner than tramadol, which was surprising. IMHO a mistake to prescribe this over oxycodone which is cleaner again and bioavailability doesn’t vary widely. The IR form is particularly problematic due to the easy of increasing bioavailability. Then again, this is Australia and we lack the holy grail of moderate pain management: dihydrocodieine aka Dicodin SR.
Casey 9/02/2021 4:46:10 PM
Been on tramadol for 14yrs, had lumbar fusion in 2010 and now in 2021 I have cervical neck problems, currently on 10/325 Percocets and 50mg Tramadols, my doctor of 4yrs left clinic 2 months ago now the new provider wants to taper me off the trams, says I will not prescribe 2 opiads for you! Im worried about withdrawal from the tramadols, and afraid this new provider will take all meds away in 6 months? Worried in Washington State. USA
Cheryl Firth 5/04/2021 4:29:24 PM
On Palexia, both SR and IR for 2 years and developed neuradrenaline hypertension. Not diagnosed as increase in BP put down to pain. Stopped Palexia and had 24 hour BP monitor to find complete reduction in BP level and irratic behaviour of BP
Paul 14/04/2021 1:11:31 PM
I have been on palexia SR 100mg and IR 50mg for a few months due to cancer in pelvis causing chronic pain in hip and spine. I don't really notice any effect from the SR, but when it really hurts, I take 1 50mg IR and 2 paracetamol and feel some relief within about 30 minutes. No side effects and no issues with this. drug. I do not feel like I have a dependency on it.
L.Collins 26/05/2021 12:19:22 PM
200mg of Paleaxia SR twice a day stopped it yesterday no weaning off severe congestion went to bed for a day feeling very sore from head to toe, but am trying my best to pass on all these meds after 6months back surgery awaiting ankle and shoulder surgery, not looking forward to the Tramadol and Palexia again but I must say it helps but I just don't feel human, so trying to get off the lot no doubt pain wikll have me back on them after next surgeries
Jeanette 17/08/2021 8:35:58 AM
HAVE ANY OF YOU TRIED GETTING A PAIN PUMP. AM TRYING to get one again after a bag experience. Pain pumps work but prayer works better. Thanks for the. Insight
Tali'zorah 27/08/2021 9:07:46 AM
Was on tramadol IR from 2003 until 2017 when doctor suddenly got nervous and said he wouldn't be refilling every 6 months for me anymore and I'd need to go into pain management. No way. Too many hoops to jump through. I've seen a family member deal with pain mgmt and she dropped out because they are so strict to the point of stupidity. Remember guys- according to pharmacists – the day you get filled is not day 1. They think you're just supposed to look at the bottle for a day before beginning treatment for your mild-moderate-severe pain.
Anyway since early 2020 I have used tapentadol 100mg IR. (Tramadol has always been my favorite for pain relief and even mood boosts. I prefer it over more potent opioids such as oxycodone. I definitely did search the streets for hydro or oxy, etc when I had to wait for refill and was experiencing surprisingly terrible WD symptoms.) And I must say that tapentadol is much better pain reliever than tramadol. It is a shame tapentadol has such short legs
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