Picture of Methadone molecule

Methadone

Chemical Name:
6-dimethylamino-4,4-diphenyl-3-heptan-one
Classification:
Opioid
Primary Uses:
Analgesia, opiate addiction treatment
Brand Names:
Dolophine, Methadose
Slang:

General Information

Methadone was invented in 1937 by German scientists Max Bockmühl and Gustav Ehrhart at IG Farben, who dubbed the chemical Hoechst 10820, and later named it Polamidon.1 The drug was not mass-produced for commercial use at all during World War II, but after the war, the factory that produced the drug fell under American control which spawned the start of the first clinical trials for methadone. Many believe the myth that the brand, Dolophine, was coined in honor of Adolf Hitler; however, the name was actually created by Eli-Lilly, an American pharmaceutical company. Some speculate that the word is a combination of the Latin word dolor (pain) and the French word fin (end). The word dol is also used in pain research to measure the level of pain (e.g. 1 dol = 1 unit of pain).2

After Eli-Lilly introduced methadone as an analgesic, doctors thought it would be the next great painkiller, but by the early 1950s, it was barely being used. In 1964, Dr. Marie Nyswander and Dr. Vincent Dole of Rockefeller University in New York began to research possible treatments for heroin addiction, and after reading about methadone in medical literature they began a clinical trial. Their clinical trials eventually evolved into the first study of opioid substitution therapy. This study resulted in a huge breakthrough in the field of addiction studies. Until this point, drug addiction was viewed as a character flaw, and this supported the fact that addiction is a treatable disease. Methadone maintenance therapy has been the most successful pharmacotherapy treatment of drug addiction in history. It is currently only rivaled by one drug, a relatively newer drug called Suboxone which was released less than a decade ago.3

Pharmacology & Pharmacokinetics

Methadone is a synthetic narcotic analgesic, and full opioid agonist with multiple actions similar to those of morphine, which mostly affect the central nervous system and organs composed of smooth muscle.4 Methadone is metabolized very slowly, and has a half-life ranging from 15-60 hours. The long half-life allows for once-a-day dosing for the treatment of opioid dependency. When taken to control pain, it must be taken 2-3 times per day because the analgesic activity lasts significantly shorter, than its pharmacological half-life. Methadone also has the unique property of having an affinity for NMDA (N-methyl-D-aspartic acid) receptors. NMDA is thought to regulate psychic dependence and tolerance via opioid antagonist-like activity.5

Legal Status

In the United States, this drug is a Schedule II substance, making it illegal to use or possess without a prescription. Schedule II substances, such as dextroamphetamine, morphine, oxycodone, and cocaine, meet the following criteria according to the Controlled Substances Act:

Side Effects

  • Pain relief
  • Euphoria or dysphoria
  • Disorientation
  • Lightheadedness
  • Dizziness
  • Mood changes
  • Anxiety or reduced anxiety
  • Sedation
  • Itching
  • Nausea and vomiting
  • Decreased libido (sex drive)
  • Constipation
  • Facial flushing
  • Vertigo

Withdrawal

If methadone is tapered correctly, withdrawal symptoms will be relatively minimal; however, if a person jumps off of methadone cold turkey, withdrawal can be just plain awful. Some medical professionals claim that methadone withdrawal is not as intense as heroin or oxycodone withdrawal, but recovering addicts are finding out the hard way that methadone withdrawal can be just as intense, not to mention much longer. Methadone withdrawal will last at least one week, but usually lasts about 2-3 weeks. Patients have stated that many withdrawal symptoms can linger for months after complete cessation. Methadone withdrawal symptoms may include:

  • Insomnia
  • Bone and muscle pain
  • Restlessness
  • Anxiety
  • Increased blood pressure
  • Gooseflesh
  • Cold sweats
  • Chills
  • Diarrhea

Sources

[1] History of Methadone. Narconon Southern California. 2001. Accessed: May 3, 2007.
[2] Joycelyn Woods. How Methadone Works. National Alliance of Methadone Advocates. Accessed: May 3, 2007. Last Accessed: February 19, 2009.
[3] Methadone. Wikipedia, the free encyclopedia. 2 May 2007. Accessed: May 3, 2007. Last Accessed: February 19, 2009.
[4] Dolophine (Methadone) Drug Information: Clinical Pharmacology. RxList. 2007. Accessed: May 3, 2007. Last Accessed: February 19, 2009.
[5] Showing Methadone (DB00333). DrugBank. Accession Number: APRD00485. 27 June 2005. Accessed: May 3, 2007. Last Accessed: February 19, 2009.