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Question on drug status

  • 13-10-2010 6:19pm
    #1
    Registered Users, Registered Users 2 Posts: 6,752 ✭✭✭


    Hi all, I been wondering about this one for a while it's around tramadol. My understanding it is classified as an opiate, however, whilst I'm aware of abuse in other countries I have only encountered one case of it in my practice.

    As it is a drug that is not of much interest to most opiate users I encounter what's the story with the chemical structure of it. Is it something like bupernorphine which is an agonist and antagonist, of is there something different again that make it different to say DFs or other similar opiates. I hope that question makes some sense.


Comments

  • Closed Accounts Posts: 79 ✭✭Nchd2010


    As far as I know, and I'm no pain specialist, tramadol hcl is an opioid partial agonist, and exerts it's action mainly on the mu opioid receptor. It can be co-administered with other opioids, but as far as I know, its not as addictive as standard opioids due to somehting to do with the limbic system.

    I know that's a great help to you, but thats about all i can remember about tramadol from my pharmacology lectures, which were a few years ago at this stage.


  • Closed Accounts Posts: 1,060 ✭✭✭darkmaster2


    From wiki.
    Structurally, tramadol closely resembles a stripped down version of codeine. Both codeine and tramadol share the 3-methyl ether group, and both compounds are metabolized along the same hepatic pathway and mechanism to the stronger opioid, phenol agonist analogs. For codeine, this is morphine, and for tramadol, it is the M1 metabolite, O-desmethyltramadol. The closest chemical relative of tramadol in clinical use is venlafaxine (Effexor), an SSNRI. The two molecules are nearly identical. Both tramadol and venlafaxine share SSNRI properties, while venlafaxine is devoid of any opioid effects


  • Registered Users, Registered Users 2 Posts: 252 ✭✭SomeDose


    Odysseus wrote: »
    Hi all, I been wondering about this one for a while it's around tramadol. My understanding it is classified as an opiate, however, whilst I'm aware of abuse in other countries I have only encountered one case of it in my practice.

    As it is a drug that is not of much interest to most opiate users I encounter what's the story with the chemical structure of it. Is it something like bupernorphine which is an agonist and antagonist, of is there something different again that make it different to say DFs or other similar opiates. I hope that question makes some sense.

    Strictly speaking tramadol is not an opiate since it doesn't have a morphine-like chemical structure, but it is classified as an opioid because it produces morphine-like effects. It's a bit of an oddball drug, with weak opioid agonist properties but also enhances serotonergic and noradrenergic activity. It has relatively low potential for addiction and abuse, as shown by your experience, although I can't speculate on why that is. In clinical practice it is less constipating than full-dose codeine, so it's a useful weak opioid alternative when stepping up/down analgesia.


  • Registered Users, Registered Users 2 Posts: 5,848 ✭✭✭bleg


    Wow, never realised their chemical structure was so alike.


  • Registered Users, Registered Users 2 Posts: 6,752 ✭✭✭Odysseus


    Thanks for the replies guys, it gave me a bit more info. I am aware of abuse in other countries, but it does not appear to be happening here.


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  • Closed Accounts Posts: 11,001 ✭✭✭✭opinion guy


    Hey.

    Yes as others have said its has partial both opoid and serotinergic activities.

    Also the company that developed tramadol have in the pipeline a more potent related drug - tapentadol I think is the name. Its supposed to have the analgesic effect of morphine with the side effect profile of tramadol.


  • Registered Users, Registered Users 2 Posts: 6,752 ✭✭✭Odysseus


    Hey.

    Yes as others have said its has partial both opoid and serotinergic activities.

    Also the company that developed tramadol have in the pipeline a more potent related drug - tapentadol I think is the name. Its supposed to have the analgesic effect of morphine with the side effect profile of tramadol.

    Cheers, that's interesting to know.


  • Closed Accounts Posts: 11,001 ✭✭✭✭opinion guy


    Odysseus wrote: »
    Cheers, that's interesting to know.

    Well don't hold your breath - so far as I know its been held up in red tape


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