1. Dear Drugs-Forum readers: We are a small non-profit that runs one of the most read drug information & addiction help websites in the world. We serve over 4 million readers per month, and have costs like all popular websites: servers, hosting, licenses and software. To protect our independence we do not run ads. We take no government funds. We run on donations which average $25. If everyone reading this would donate $5 then this fund raiser would be done in an hour. If Drugs-Forum is useful to you, take one minute to keep it online another year by donating whatever you can today. Donations are currently not sufficient to pay our bills and keep the site up. Your help is most welcome. Thank you.
    PLEASE HELP

Tramadol Pharmacology Relevant to Drug Abuse Assessment

Tramadol Pharmacology Relevant to Drug Abuse Assessment

  1. Guigz
    Short answer to this 16 questions by Robert B. Raffa, Ph.D.

    1.Is tramadol an ‘opioid’?
    2.Wasn’t tramadol originally thought to be only opioid?
    3.Are metabolites other than M1 strong opioids?
    4.Is tramadol merely a pro-drug of M1?
    5.Is tramadol analgesia in humans blocked by an opioid antagonist?
    5.Is tramadol’s analgesia in humans blocked by inhibition of CYP450-2D6?
    6.Do non-opioid antagonists inhibit tramadol analgesia in humans?
    7.Does tramadol display morphine-like effects in humans?
    8.What about studies in CYP450-2D6 poor metabolizers?
    9.Could tramadol be ground up and ‘snorted’ (insufflated)?
    10.Could tramadol be ‘smoked’?
    11.Isn’t the non-opioid mechanism of action too weak to explain tramadol’s analgesia?
    12.Does more M1 in the bloodstream translate to an equivalent amount more in the brain?
    13.What would happen to M1 Cmax and Tmax if someone were to grind and dissolve a CR or
    IR formulation and inject it i.v.?
    14.Even though plasma levels of M1 are about the same following i.v. compared to oral
    administration of tramadol, wouldn’t the more rapid kinetics of the i.v. route enhance
    the subjective effects of tramadol?
    15.What if abusers went to even higher doses of tramadol i.v. (e.g., by injecting 300 – 400
    mg from a crushed CR formulation?
    16.Then what if abusers went to even higher doses of tramadol orally (e.g., 300 – 400 mg
    from a crushed CR formulation?