PharmSteve/What is Ultram?

[hoops2u]

Hi Steve,
It has been a while since I have asked a technicle question of you. Lately my bones have been hurting so bad. In particular my joints, but also my bones. At night the pain has become so severe it either wakes me up or keeps me awake. Memory foam on bed helps a bunch, not enough.

So, for a few months I was taking NSAIDS, 3 to 4 a night. I even got up from time to time at around 2-3 AM and took 2 more. Mostly Asprin, coated. I can't take tylenol or the likes, they give me insomnia, and they really don't kick that particular pain anyhow. The asprin was working fairly well.

Upon a recent visit to my GP for a med check, blood test came back showing low red blood count, anemia. She felt I was bleeding internally and insisted on all these tests. You know, colon, endoscopy, barium swallow, etc. I told her about the asprin and she immediately told me to stop and gave me "Ultram" for the pain.

She prescribed 2, 50 mgs 4 times a day, but not to worry, I only take two (2) at bed time. Once in a great while I may take one in the afternoon.like today, raining all day.

She wanted me to see my PM to be sure this was appropriate. He said he still uses Celebrex which made me sick and said it is an NSAID and I would be better with the Ultram, given the past issue/w bleeding.

No bleeding now, all is good, tests came out fine, must have been a very small lesion. But PM Dr. did say I must take care with the ultram because if taken with prozac it could cause siezures. Now I'm just a tiny bit concerned. I am already being treated for seizure disorder.

But, BUT, the Ultram is working GREAT for the arthritis type pain and BT pain.

Your Thougts? And, as elementary as possible, what is Ultram? Ya know I'm not all that smart, ahem.....

Thank you soooo very much. You ARE the best. I could ask my Pharm, but there are always a bunch of people milling about.

Best to you,
hoops

[Pharmacist.steve]

Ultram taken with a SSRI (Prozac).. there is a risk of serotonin syndrome
http://en.wikipedia.org/wiki/Serotonin_syndrome. This interaction came to the fore-front about a year ago.. It is not real common ... but it is serious when it happens.

Actually taking enteric coated ASA... it normally takes 4-6 hrs to kick in .. because the enteric coating will not start to dissolve until it reaches the intestines.. because it requires a BASIC medium to dissolve as opposed to the ACIDIC medium that is in the stomach.

[hoops2u]

But Steve, STEVE! What is ULTRAM, anyway?

And thanks, by the way, for the answer about the seizures.

hoops.

[Pharmacist.steve]

But Steve, STEVE! What is ULTRAM, anyway?

And thanks, by the way, for the answer about the seizures.

hoops.

Here is a quote from the Ultram insert

ULTRAM is a centrally acting synthetic opioid analgesic. Although its mode of action is not completely understood, from animal tests, at least two complementary mechanisms appear applicable: binding of parent and M1 metabolite to μ-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin

simply put ....

IT IS A PAIN MEDICATION!!

[911]

isnt it odd how the drug companys do NOT know how these drugs work yet they give them to us anyways ?????? thats the case with nearly all the new anti -d's infact theres usually a warning of somesort about the anti-d's causing suicidal thoughts,actions , go figure a drug to help with depresion that can actually coz some to consider suicide the very thing alot of us may have been treated for , now theres an exsplanation i would love to hear ??? sorry if i am a bit bitter about some of this but it just strikes me odd when they prescribe drugs that they do not know how or why it works or if it works at all ???????????????????????????????????????? dave

[Pharmacist.steve]

isnt it odd how the drug companys do NOT know how these drugs work yet they give them to us anyways ?????? thats the case with nearly all the new anti -d's infact theres usually a warning of somesort about the anti-d's causing suicidal thoughts,actions , go figure a drug to help with depresion that can actually coz some to consider suicide the very thing alot of us may have been treated for , now theres an exsplanation i would love to hear ??? sorry if i am a bit bitter about some of this but it just strikes me odd when they prescribe drugs that they do not know how or why it works or if it works at all ???????????????????????????????????????? dave

People go thru a number of stages as they sink into depression and as they come out of depression - with or without some sort of assistance ( medication/talk therapy). For some unknown reason... some of the SSRI's in some people seem to enhance or they linger longer in the "suicide phase" when they are coming out of the depression.

Collectively what medical science knows about how the body works is dwarfed by what they don't know about how the body works. In my life time... I have seen Penicillin going from a "wonder drug" to patients "wondering" why a prescriber would prescribe them JUST PENICILLIN.

[mrsdoubtfyre]

shows potential side effects, and drug interactions:

http://www.rxlist.com/cgi/generic/tramadol_ad.htm

Many people react to this pain reliever in different ways. It is not as
straight forward as aspirin or NSAIDs.
After long term use, many find discontinuing difficult, requiring tapering etc.

So you may not like it, or you may... expect some variance in response.
Alot of patients with fibro or PN seem to have more positive responses.

[Kathi49]

I have to agree with Mrs. D. about the variances in response.

I tried Ultram once a long time ago. It didn't do much for the pain; more like taking Tylenol. But if I recall correctly it made me very sick and dizzy. I went back to my PM for a follow up and he said then and there alot of patients were complaining about it; either not being very effective or making them sick and dizzy. But heck everything makes me sick or dizzy. :rolleyes: Anyway, I just vaguely remember him saying he really wasn't going to prescribe it much anymore...something to that effect anyway. I see another PM today that handles the meds so I will ask HER about it and see what she has to say or what her patients have to say about it. Besides, I want to find out more about Keppra since Lyrica is out. Oh, and sorry I am a little OT but I also asked my PM about Topomax the last time I was there. He just kind of laughed and told me there was probably no way I would be able to tolerate that one either. But I am speaking of nerve meds here and not the opiates.

[lobelsteve]

Drugs. 1997;53 Suppl 2:18-24.Links
[Pharmacology of tramadol][Article in French]


Dayer P, Desmeules J, Collart L.
Service de Pharmacologie Clinique et Consultation de la Douleur, Hôpital Cantonal Universitaire, Gen*ve, Suisse.

(+/-)-Tramadol is a synthetic 4-phenyl-piperidine analogue of codeine. It is a central analgesic with a low affinity for opioid receptors. Its selectivity for mu receptors has recently been demonstrated, and the M1 metabolite of tramadol, produced by liver O-demethylation, shows a higher affinity for opioid receptors than the parent drug. The rate of production of this M1 derivative (O-demethyl tramadol), is influenced by a polymorphic isoenzyme of the debrisoquine-type, cytochrome P450 2D6 (CYP2D6). Nevertheless, this affinity for mu receptors of the CNS remains low, being 6000 times lower than that of morphine. Moreover, and in contrast to other opioids, the analgesic action of tramadol is only partially inhibited by the opioid antagonist naloxone, which suggests the existence of another mechanism of action. This was demonstrated by the discovery of a monoaminergic activity that inhibits noradrenaline (norepinephrine) and serotonin (5-hydroxytryptamine; 5-HT) reuptake, making a significant contribution to the analgesic action by blocking nociceptive impulses at the spinal level. (+/-)-Tramadol is a racemic mixture of 2 enantiomers, each one displaying differing affinities for various receptors. (+/-)-Tramadol is a selective agonist of mu receptors and preferentially inhibits serotonin reuptake, whereas (-)-tramadol mainly inhibits noradrenaline reuptake. The action of these 2 enantiomers is both complementary and synergistic and results in the analgesic effect of (+/-)-tramadol. After oral administration, tramadol demonstrates 68% bioavailability, with peak serum concentrations reached within 2 hours. The elimination kinetics can be described as 2-compartmental, with a half-life of 5.1 hours for tramadol and 9 hours for the M1 derivative after a single oral dose of 100mg. This explains the approximately 2-fold accumulation of the parent drug and its M1 derivative that is observed during multiple dose treatment with tramadol. The recommended daily dose of tramadol is between 50 and 100mg every 4 to 6 hours, with a maximum dose of 400 mg/day; the duration of the analgesic effect after a single oral dose of tramadol 100mg is about 6 hours. Adverse effects, and nausea in particular, are dose-dependent and therefore considerably more likely to appear if the loading dose is high. The reduction of this dose during the first days of treatment is an important factor in improving tolerability. Other adverse effects are generally similar to those of opioids, although they are usually less severe, and can include respiratory depression, dysphoria and constipation. Tramadol can be administered concomitantly with other analgesics, particularly those with peripheral action, while drugs that depress CNS function may enhance the sedative effect of tramadol. Tramadol should not be administered to patients receiving monoamine oxidase inhibitors, and administration with tricyclic antidepressant drugs should also be avoided. Tramadol has pharmacodynamic and pharmacokinetic properties that are highly unlikely to lead to dependence. This was confirmed by various controlled studies and postmarketing surveillance studies, which reported an extremely small number of patients developing tolerance or instances of tramadol abuse. Tramadol is a central acting analgesic which has been shown to be effective and well tolerated, and likely to be of value for treating several pain conditions (step II of the World Health Organization ladder) where treatment with strong opioids is not required.


Based on this and other reviews, I do not consider tramadol an opioid. It binds to the mu opioid receptor as well as salad dressing.;)

:mad: at the FDA for calling this a narcotic because of the fears that go with the classification.

[welsh]

Hi lobelsteve, Ive just read your post,and I just wanted to say that I was taken off Tramadol a week last friday after being on them for far longer than I care to remember,and I was not weaned off them I in fact had to stop them dead in their tracks as it were,just stop right there right then,and Im glad to report that I had NO problems whatsoever coming off them this way at all.The only thing I felt was a little bit iccky a couple of times,but then again that could have been caused by the new opiate meds I was put on instead of tramadol,as I was not getting any valueable pain relief from them at all, as I reckon Id become resisitant to them as Id been on the highest dose plus extra for breakthrough pain for quiet some time!! Anyway just thought Id post that in case anyone else was concerned about tramadol and its affects. Demi aka Welsh