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Methadone testing protocol

G.Patton

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Introduction

You bought methadone crystals or tablets and want to carry out pollution and admixture testing experiments before using. Use this article as a guide for experimenting. Here you can find the list of manipulations with methadone product, useful information for home tests and product brief.
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There are (D-)Dextro-methadone (left pic.) and (L-)Levo-methadone (right pic.)

Forms

Methadone, sold under the brand names Dolophine and Methadose among others, is a synthetic opioid agonist used for opioid maintenance therapy in opioid dependence and for chronic pain management. Methadone is usually taken by mouth and rarely by injection into a muscle or vein. The salts of methadone in use are the hydrobromide (free base conversion ratio 0.793) [Quantity of salt * conversion factor = quantity of base], hydrochloride (0.894), and HCl monohydrate (0.850).

Methadone is available in traditional pill, sublingual tablet, crystal, crystal powder and two different formulations designed for the person to drink. Drinkable forms include ready-to-dispense liquid (sold in the United States as Methadose), and Diskets® (known on the street as "wafers" or "biscuits") tablets, which are dispersible in water for oral administration, used in a similar fashion to Alka-Seltzer. The liquid form is the most common, as it allows for smaller dose changes. Methadone is almost as effective when administered orally as by injection. Oral medication is usually preferable because it offers safety, simplicity, and represents a step away from injection-based drug abuse in those recovering from addiction.
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Injecting methadone pills can cause collapsed veins, bruising, swelling, and possibly other harmful effects. Methadone pills often contain talc that, when injected, produces a swarm of tiny solid particles in the blood, causing numerous minor blood clots. These particles cannot be filtered out before injection, and will accumulate in the body over time, especially in the lungs and eyes, producing various complications such as pulmonary hypertension, an irreversible and progressive disease. The formulation sold under the brand name Methadose (flavored liquid suspension for oral dosing, commonly used for maintenance purposes) should not be injected either.

Chirality and Pharmacodynamics

Methadone has an asymmetrical carbon atom in its structure, which means that it exists in two enantiomeric forms, having the same chemical composition but different spatial arrangements, with one enantiomer being the mirror image of the other. Methadone is marketed in almost all countries as a racemic mixture, i.e. a 50:50 mixture of two enantiomers called (R)- or levo- or l-methadone, and (S)- or dextro- or d-methadone. In Germany, until the mid-1990s, only (R)-methadone was used, but as (R)-methadone is more expensive than (R, S)-methadone, the racemic form is increasingly prescribed nowadays. The stereo specificity of most opioids for μ receptors is well known, although for methadone the difference between the two isomers is not dramatic, probably owing to a greater conformational mobility of the molecule. Nevertheless, in vitro binding experiments have shown that the necessary concentration of (R)-methadone to inhibit 50% of [3H]naloxone binding to whole rat brain homogenates is 10 times lower than that of (S)-methadone. A 10-fold dif ference of affinity has also been found between the two enantiomers for the bovine μ1 receptor, which mediates supraspinal analgesia (50% inhibitory concentration [IC50] (the half maximal inhibitory concentration) of 3.0 and 26.4 nmol/L for (R)- and (S)-methadone, respectively) and μ2 receptor, which mediates spinal analgesia [IC50 of 6.9 and 88 nmol/L for (R)- and (S)-methadone, respectively]. In human analgesia, (R)-methadone is about 50 times as potent as the (S)-form.

The metabolic half-life of methadone differs from its duration of action. The metabolic half-life is 8 to 59 hours (approximately 24 hours for opioid-tolerant people, and 55 hours in opioid-naive people), rather than to a half-life of 1 to 5 hours for morphine. The length of the half-life of methadone allows for exhibition of respiratory depressant effects for an extended duration of time in opioid-naive people.

The most popular admixtures and adulterants of methadone

Usually, methadone is not admixtured by adulterants. In seldom cases you can meet methadone with fentanyl or heroin because they have similar effects. Methadone can be substituted for a-PVP crystals, which is looks similar, or, extremely rarely, for mephedrone, ibuprofen. Also, street methadone may be polluted by small amount of by-products such as levacetylmethadol, 1,5-dimethyl-3,3-diphedyl-2-ethylidene pyrrolidine, 2-ethyl-5-methyl-3,3-diphenylpyrrolidine, 2-ethyl-5-methyl-3,3-lbahtnylpyrrolidine, 1,5-dimethyl-3,3-diphenyl-2-pyrrolidinone and etc. Although street drugs of abuse usually has difference purity (from 10-90%), methadone crystals are meets with quite high purity percentage (75-95%).

Algorithm of procedures:

1. Firstly, you have to provide visual checking of your stuff. If your product has different color from semitransparent white, It, probably, has some organic or inorganic pollution, which can change color. Any other colors than this will mean a dirty or substituted product. If your methadone sample in a pill form, skip this step.

2. Secondly, I strongly recommend determining fentanyl or fentanyl derivatives/analogs using special Fentanyl test kit which is containing test stripes. This substance extremely dangerous, especially in a pair of methadone, heroine or any opiates. Tablet form and crystals may be checked by the same method represented below. If you find this substance, I recommend you to get rid of your impure heroin to safe your life. You cannot measure the amount of fentanyl in your street methadone product by any improvised means and cannot define safety dose. There are information about LF tests (drug testing kits).

How to test it?
A: Choose your option.
Option 1:
  • Dissolve all the drugs you plan to use in water by following the instructions in Step B.
  • This is the most accurate way to test your drugs, since fentanyl is not always mixed evenly throughout. If you cannot test your drugs this way, try Options 2 or 3.
  • After testing your drugs this way, you can drink them, snort them using a clean nasal spray device or wait until the water evaporates to use them.
Option 2:
  • Finely crush your drugs on a clean surface.
  • Put the crushed drugs in a small, plastic bag and shake the bag to mix them.
  • Empty the bag and put your drugs to the side. A small amount of drug residue should be left in the bag.
  • Add water to the bag by following the instructions in Step B.
Option 3
  • Put 10 milligrams (mg) of your drugs (enough to cover Abraham Lincoln’s hair on a penny) in a clean, dry container.
  • If you cannot test 10 mg of your drugs, put at least a few grains in a clean, dry container.
  • Add water to the container by following the instructions in Step B.
B: Add water.
  • Add water to your drugs and mix them up.
  • Use half teaspoon of water for every 10 mg of crystal or powder you are testing.
C: Use the test strip.
  • Place the test strip with the wavy side down in the water. Let the strip absorb the water for 15 seconds.
  • Take the strip out of the water and place it on a flat surface for two minutes.
  • Read the results (see “What do the test results mean?”).
  • Tips for testing your drugs:
  • Do not use test strips more than once.
  • Finely crush pills and tablets, add water to the powder and mix thoroughly. If you do not want to test the entire pill, break it in half and test a portion from the middle.
What do the test results mean?
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The fentanyl testing strips are capable of detecting a dozen different fentanyl family members, and there isn’t a single one of them that isn’t life-threatening or dangerous to your health. The members are:
  • 3-Methylfentanyl,
  • 4-Fluorofentanyl,
  • Acetylfentanyl,
  • Alfentanil,
  • Butyrfentanyl,
  • Carfentanil,
  • Fluoroisobutyrfentanyl,
  • Furanylfentanyl,
  • Ocfentanil,
  • Remifentanil,
  • Sufentanil,
  • Thiofentanyl.
3. Thirdly, confirm the compliance of the product with heroin by LF tests (drug testing kits). You will receive clear result about your substance and admixtured narcotic substance (if it takes place to be) and these tests help to choose next step. Take methadone and Heroin drug test strips firstly. Also, check your substances for other narcotic, such as a-PVP, mephedrone (most popular row), and so on (see The most popular admixtures and adulterants of methadone above).

4. Fourthly, check pH of the solution. Product of methadone can be polluted by organic powdery acids (Ibuprofen, ascorbic, citric, etc.), organic powdery bases such as Caffeine etc. «Determination of impurity in synthetic PAS» exactly describe method of determination of them, these methods valid for methadone. Some sugars (sucrose, glucose, fructose) may be admixtured as well.

5. Next, if any pollutants are not found or LF tests (step 3) reveal admixtured narcotic substance, you have to check your methadone sample with test reagents. Use «Drugs testing reagents». These methods help to determine kind of admixtures. There are manuals, which are described checking method procedures and meaning, where you can find methods of reagent synthesis. According to data from testing reagent experiments, you may compare and approve result by TLC.

For instance, you place a methadone sample (couple crystals) into a small white/colorless plate or Petri dish. Add two drops of Mecke reagent and observe the reaction.
  • If the reaction has yellow - green to Green or Green to Brown color changing, it means you have pure methadone.
  • If the reaction has bluish green color after 60 seconds, it means you have heroin contamination in your sample.
  • If the reaction has orange color, it means your methadone is polluted by dextromethorphan. This substance is quite often identified in heroin products, which can be admixtured to your methadone sample.
  • If the reaction has yellow (yellowish) color, it means your methadone is polluted by a-PVP or MDPV. These substances is quite often sold as methadone.
Also, carry out experiment with Mandelin reagent. In addition, couple drops of reagents, you may observe following color reactions:
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I would recommend providing tests with several reagents because you can have a mixture of admixtured drugs in the sample, testing results may show a mix of colors. Different test reagents allow interpreting results of testing more clearly.

For instance, you have received test result with Mecke reagent of a-PVP or MDPV, which gave yellow (yellowish) color. After, you added few drops of Mandeline reagent and the color of drops changes to deep brown. This result confirms the previous. Take TLC plate, polluted sample of methadone, really clear methadone, clear a-PVP and MDPV (if you have), make four spots of substances and elute them, count Rf and compare results with the literature data. If your methadone sample spots will split in two or more parts, which will have the same level of a-PVP and/or MDPV and clear methadone, it means that your sample has a-PVP or/and MDPV contamination.

Conclusion

Melting point verification can be added to the third step to confirm quality compliance and to determine the degree of impurity content if you have a crystalline product. As for methadone, the LF test with test strips is most useful because another test may require a little more skill and experience. The best ways to determine composition of heroin mixture are GC-MS or LC-MS analysis. However, this manual allows identifying most number of methadone impurities and approve results by different methods.
 
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