Methadone was originally developed by the Nazis during World War II. When the supply of opium was cut off, Nazi addicts like Hermann Goering (Commander in Chief of the Luftwaffe and Hitler's designated successor) wanted to avoid the possibility of withdrawal. He instructed the German drug companies to produce a wholly synthetic opiate that didn't need to rely on the poppy. The chemists came up with a drug that not only worked, but also lasted a long time. As a result, Methadone has become the drug of choice for doctors who are trying to help users manage their opiate dependency. Heroin wears off after a couple of hours, thus requiring several hits each day. Methadone, on the other hand, lasts anywhere between 24 and 72 hours, depending on the dose that you take and on your individual metabolism.
The first pharmacological studies of methadone were performed by 1946 at which time the compound was found to be a potent narcotic analgesic. Methadone was approved for use in controlling severe pain. In 1963 methadone was introduced as an experimental drug for the treatment of heroin dependence. The drug-known variously as methadone, dolophine, amidone, physeptone, miadone, butalgin, diadone, and polamidone-bears only a remote stereochemical resemblance to morphine; yet its pharmacological properties are qualitatively similar to those of the natural alkaloid. Methadone itself has considerable abuse potential and is classified as a DEA Schedule II controlled substance.
Methadone has several different apperarances: Liquid mixture, orange, yellow, green or clear; Tablets; Ampoules for injection. When pharmaceutically pure, methadone comes in a variety of strengths. Methadone Mixture most frequently is mixed at 1mg/ml (i.e. 1mg methadone hydrochloride in 1ml of liquid). Methadone Mixture is designed to be taken orally; it is mixed with an irritant to deter injecting. Tablets are also designed to be taken orally. However some users grind up tablets and inject them. Concentrated 50mg/ml are not intended for intravenous use, and are actually intended for subcutaneous or intramuscular use.
- Tablets: 5mg tablets.
- Ampoules: Ampoules are usually mixed at strength of 10mg/ml. They come in the following sizes: 1ml (10mg)
- 2ml (20mg)
- 3.5ml (35mg)
- 5ml (50 mg)
- Also available are concentrated ampoules, containing 50mg/ml.
Methadone is usually administered orally and as such is rapidly absorbed. Methadone is metabolized primarily in the liver by demethylation and subsequent cyclization to form 2-Ethylidene-1,5-dimethyl-3,3-diphenylpyrrolidine (EDDP). This cyclization process yields a primary metabolite molecule quite distinct from the parent molecule. The elimination half-life of a 15mg dose is approximately 14 hours. Methadone and metabolites are primarily excreted in the feces. Unmetabolized methadone excretion in the urine accounts for less than 11% of the administered dose. Following a single dose, the metabolite concentration in urine is approximately one half the unchanged concentration.
When you take methadone it first must be metabolized in the liver to a product that your body can use. Excess methadone is also stored in the liver and blood stream and this is how methadone works its 'time release trick' and last for 24 hours or more (Inturrisi and Verebey, 1972). The higher the dose the more that is stored. This is why patients on blockade doses (70 mg/day or more) are able to go for a day or two without their medication. Of course the down side to this is that when a patient misses a dose they will begin to "destabilize" which places them at risk of overdose should they attempt to administer heroin. They are slowly loosing the blockade effect of methadone and may begin to experience drug hunger and craving. Oral methadone is very different than the IV methadone. Oral methadone is partially stored in the liver for later use. IV methadone acts more like heroin.