Complexities of Methadone Elimination

Discussion in 'Opiates' started by Maggie Sugar, May 9, 2005.

  1. Maggie Sugar

    Maggie Sugar Senior Member

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    There has been an ongoing discussion about the ability to detect the drug Methadone in urine. This drug has some interesting properties, which can cause the detection level and elimination rate to differ from person to person.

    The info that it only takes a few days to excrete Met is highly suspect. The drug was developed as a LONG ACTING opiate for opiate tolerant and opiate dependent individuals. It works slightly differently than Morphine, but although the analgesic time is 6 hours of less, the half life (the time it takes for HALF of the methadone to leave the body) is variable, but can be as much as 50 hours. When one is calculating Half Lives, you do not add one half life to the next and come up with NONE. One half life eliminates HALF of the drug in the body, the next half life time HALF of what was left is eliminated (with most drugs this is only two half lives and still WELL detectable) the next half life HALF of what was left then is eliminated and so on and so on. Most drug test (but not all, some are more or less accurate or sensitive) will detect a drug like Methadone for about 6 halflives. With a drug with a 50 hour half life this could be well into the 300 hour mark. (estimates of half lives vary from 15 hours to 150 hours.) Thus there is little way to tell a user just HOW LONG methadone will show up in THEIR urine.

    Some more data on this drug and it's elimination.
    Fast Fact and Concept #75: Methadone for Pain

    Return to Fast Facts Index

    Title: Fast Fact and Concept #75: Methadone for Pain

    Author(s): G Gazelle; PG Fine

    Methadone, a potent opioid agonist, has many characteristics that make it useful for the treatment of pain when continuous opioid analgesia is indicated. Although available for decades, its use has gained renewed interest due to its low cost and potential activity in neuropathic pain syndromes. Unlike morphine, methadone is a racemic mix; one stereoisomer acts as a NMDA receptor antagonist, the other is a mu-agonist opioid. The NMDA mechanism plays an important role in the prevention of opioid tolerance, potentiation of opioid effects, and efficacy for neuropathic pain syndromes, although this latter impression is largely anecdotal.

    Any clinician with a Schedule II DEA license can prescribe methadone for pain; a special license is only required to prescribe methadone for the treatment of addiction. In some jurisdictions, it is necessary to apply the words "for pain" on the prescription. Methadone is highly lipophilic with rapid GI absorption and onset of action. It has a large initial volume of distribution with slow tissue release. Oral bioavailability is high, ~ 80%. Unlike morphine there are no active metabolites; biotransformation to an active drug is not required. The major route of metabolism is hepatic with significant fecal excretion; renal excretion can be enhanced by urine acidification (pH <6.0). Unlike morphine, no dose adjustment is needed in patients with renal failure since there are no active metabolites. Methadone is available in tablet, liquid and injectable forms; oral preparations can be used rectally. Parenteral routes include IV bolus dosing or continuous infusion.

    Unlike morphine, hydromorphone or oxycodone, methadone has an extended terminal half-life, up to 190 hours. This half-life does not match the observed duration of analgesia (6-12 hours) after steady state is reached. This long half-life can lead to increased risk for sedation and respiratory depression, especially in the elderly or with rapid dose adjustments. Rapid titration guidelines for other opioids do not apply to methadone. Given recent reports that high-dose methodone MAY be associated with development of Torsades, depending upon life expectancy and goals of care, EKG monitoring may be appropriate when changes in dosage are made. An important property of methadone is that its apparent potency, compared to other opioids, varies with the patient's current exposure to other opioids.

    The chart below indicates the
    Daily Oral Morphine Dose Equivalents
    followed by the
    Conversion Ratio of Oral Morphine to Oral Methadone


    • <100 mg - 3:1 (i.e., 3 mg morphine:1 mg methadone)
    • 101-300 mg - 5:1
    • 301-600 mg - 10:1
    • 601-800 mg - 12:1
    • 801-1000 mg - 15:1
    • >1001 mg - 20:1
    Due to incomplete cross-tolerance, it is recommended that the initial dose is 50-75% of the equianalgesic dose.



    From Erowid:

    METHADONE Examples: Roxane, Dolophine Medical uses: Treatment of opiate addicts in approved program Effects attractive to abuser: Same as opiates (below) Adverse effects: Same as opiates (below) but with lesser degree of physicaldependency (addiction) How abused: Pills taken orally; solution injected intravenously. Period detectable after last dose: 7.5-56 hours (dependingon the individual and the test used.) Substances causing false positive results: doxylamine [Unisom NighttimeSleep Aid]. Presence of this substance would be ruled out by confirmatorytesting.Half-life
    The half-life of a drug is the name given to the time it takes for blood levels of a drug to drop to 50% of the peak concentration. The half-life of diamorphine (heroin) is around 3 minutes. The half-life of methadone depends upon whether it is a first dose or a dose given as part of an ongoing programme.

    Single, first dose
    The apparent half-life of a single oral dose of methadone is shorter than that in extended use. This is because much of the initial dose becomes distributed into the tissue reservoirs and is therefore not available in the blood stream.
     
  2. Maggie Sugar

    Maggie Sugar Senior Member

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    How to apply this:

    Let's say there is a new drug called "Booyatax." The Half life of Booyatax is 24 hours. At the time of ingestion and the start of drug intoxication, the patient has 100 nanograms of the drug per Deciliter of blood. (ng per dcl) Detection of the drug in a standard urine test is about 3 nanograms per deciliter of blood.

    Day Two. After the first 24 hours (first half life) the patient then has 50 ng per dcl.

    Day Three. After the NEXT 24 hours, the drug is not gone! The next half life has to take place. One does not add two half lives together. We left the pateint with 50 ng perdcl. Now after and OTHER half life of 24 hours, the pateint has 25 ng per dcl of blood.

    Day Four After the NEXT 24 hours the next half life take place. The pateint, now at day four after administration has 12.5 ng per dcl of blood.

    Day Five An other half life, now the patient has 6.25 ng per dcl of the drug in his system.

    Day Six An other half life has taken place, the patient now has 3.125 ng per dcl detectable. He is almost at the limit of non detection. Our user may (or may not) pass a drug test at this point.

    Day Seven Now he has 1.5625 ng per dcl of Booyatax in his blood, and will probably pass a drug test.

    Booyatax is not a real drug, most drugs are not as easy as a 24 hour half life and 100 ng per dcl of blood to calculate.

    But you get the idea.

    I hope I haven't wasted my time.

    Good luck to you all.
     
  3. Maggie Sugar

    Maggie Sugar Senior Member

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    All that research towards understanding a really misunderstood thing, and nobody cares.

    :(

    Oh well............
     
  4. makno

    makno Senior Member

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    i dont know what yer gettin at .......but for any severely heroin addicted people out there ....all you need to do is find a place where you can be sick for a month or two .......not an unbearable thing at all .......dont get hooked on methadone ...........the kick is `1000 x worse and can last forrever ......its no answer to your problems ........freedom .............
     
  5. oOflyeyesOo

    oOflyeyesOo Member

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    Methadone is pretty addictive too, my uncle just recently got off methadone and he has been on them for about wow I dont even know, ever since he stoped useing heroin, maybe like 15-20 years ago.
     
  6. Maggie Sugar

    Maggie Sugar Senior Member

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    There have been repeated questions about methadone, and also I just wanted to explain how a half life works, as it is applicable in ALL drugs when taking a drug test.

    That's all you need to do, eh? And, you've done this......and still claim it isn't a big thing? Sheesh!!
     
  7. crackforkids

    crackforkids Senior Member

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    maggie sugar, i had no idea you ever had a heroin problem, your so responsible on these boards :) withdrawl SUCKS!!!!!! but yes methadone is worse, and easier to keep doing cause its perscribed to you :(
    whats that new stuff comming out that starts with a b
    seems to work a lot better, a little more expensive, but i think you ween off it easier fast i believe, im no expert though!
     
  8. Maggie Sugar

    Maggie Sugar Senior Member

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    I've never done heroin. I do have a Chronic Pain disorder and take meds for that, however. Not smack, though.
     
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