Methadone is an Opioid, analgesic and it is synthetic by nature. Methadone is basically recommended for the chronic drug abusers. Methadone has been found to be an ideal medication for the treatment of addiction from narcotic substances. Of late, methadone has been widely recommended for patients suffering from chronic pain. Methadone’s effective action remains for long duration. Moreover, Methadone is quite cheap as well. As per the Single Convention on Narcotic Drugs, methadone is included in the list of Schedule II drug.
There are two reasons as to why Methadone effects last longer than other morphine drugs. First, methadone’s lipid solubility is quite high. Second, methadone metabolism is slow. Most importantly, the dependence incidence of patients is low. Hence, there is less danger of a heroin detoxified patient treated on methadone getting hooked to the synthetic opioid. Methadone keeps intact the analgesic effects from a day to two at the most.
IDEAL FOR DE-ADDICTION UNITS
Methadone is ideal for the de-addiction units particularly because of the life of a methadone dosage. Moreover, methadone can be given by injection or even orally. For instance, a single daily dose of methadone is enough to keep under control any heroin addict for the entire day.
TOLERANCE & DEPENDENCE OF METHADONE
The tolerance and dependence of methadone increases as one keeps on taking more doses of the synthetic opioid. In this aspect, methadone is similar to heroin. However, the tolerance factor as well as the effects (physiological) differs. Still, it has been found that methadone leaves no tolerance to constipation. However, the other opioids do leave tolerance effects on the patients especially with respect to constipation. Mentionably, analgesia tolerance appears in the first month after one starts taking the drug. But, tolerance to nausea, sedation and respiratory depression commences within four days after one takes such medications.
METHADONE & NDMA
There is a close link between methadone and the brain receptor known as NMDA (N-methyl-D-aspartic acid). Methadone can even control tolerance and psychic dependence. This is possible because of its strong reaction against opioid. It is due to this reason that patients taking methadone exhibit lesser withdrawal symptoms than those who are into heroin or morphine. Nonetheless, the methadone withdrawal symptoms linger more than the latter.
THE METHADONE LAUNCHER
Methadone was commercially launched by Eli Lilly and Company, a pharmaceutical company.
THE INVENTORS OF METHADONE
German scientists Methadone Gustav Ehrhart and Max Bockmühl jointly synthesized methadone in 1937. They were in search of an analgesic in the Hoechst-Am-Main (IG Farben) laboratory. Their mission was to invent such an analgesic that would solve the twin problems faced by surgeons during surgical operations.
SOLVING SURGEONS’ SETBACKS
First, surgeries were rather problematic with the then extant analgesics. Secondly, the commonly used analgesics were having a high addiction effect. So, both the German scientists found out that synthetic analgesic which would have low addiction effects on the patients and also would be easier to use. They called it Polamidon or Hoechst 10820.
It was on September 11, 1941 that the duo filed for patent rights. The structure of this invention was totally different from and least connected with the opioid alkaloids or morphine. Nonetheless, methadone brings about the same types of effects as heroin or morphine. This is because methadone acts on the opioid receptors. Among the opioids, methadone has the simplest chemical composition.
The Americans came to know of methadone as an analgesic in 1947, courtesy: Eli Lilly and Company. It then rechristened Polamidon or Hoechst 10820 (methadone) as Dolophine. It was under this registered name that methadone was subsequently registered to Roxane Laboratories. Incidentally, the term ‘Dolophine’ has its roots in the German word Dolphium. The Latin word dolor means ‘pain’ while phine means ‘end’. In the USA , Dolophine (Methadone) was first manufactured by the St. Louis-based Mallinckrodt pharmaceuticals. It is a subsidiary of the Tyco International Corporation. Mallinckrodt enjoyed the patent up to the early part of the 1990s. It still remains the major manufacturer of methadone. The producers of methadone generic preparations also collect their bulk consignments from Mallinckrodt. Nonetheless, many other pharmaceutical companies also produce and distribute methadone today. Moreover Mallinckrodt sells its typical brand of methadone named Methadose as oral concentrate and dispersable tablets in the United States
, Dolophine (Methadone) was first manufactured by the St. Louis-based Mallinckrodt pharmaceuticals. It is a subsidiary of the Tyco International Corporation. Mallinckrodt enjoyed the patent up to the early part of the 1990s. It still remains the major manufacturer of methadone. The producers of methadone generic preparations also collect their bulk consignments from Mallinckrodt. Nonetheless, many other pharmaceutical companies also produce and distribute methadone today. Moreover Mallinckrodt sells its typical brand of methadone named Methadose as oral concentrate and dispersable tablets in the
THE HITLER LINK…
There is a belief that the German creators coined the name ‘Dolophine’ as a tribute to Adolf Hitler. The Church of Scientology
Scientologyalso buttresses this with the data that the earlier name for this synthetic analgesic was actually ‘Adolophine’ or ‘Adolphine’. To make matters worse, vocal Scientologist and actor Tom Cruise also backed the literature in 2005. He was giving an interview to the Entertainment Weekly. However, the weekly soon came out with a follow-up story which nullified the claim. It is, however, now established that the term ‘Dolophine’ was coined by the American wing of the Eli Lilly Corporation after the World War. What is more, the magazine put the lid on the controversy by proving that the 1970 nomenclature of ‘Adolphine’ (which wasn’t ever used for the drug) was also brought into being in the States.
THE METHADONE ADVANTAGE
The low cost of methadone as well as its effectiveness over a long period of time made it rather popular too. While 30 days dose of the analgesic Demerol cost $ 125 in the fag end of 2004, the equivalent amount of methadone cost $20.
There are many drugs similar in composition and effects to methadone. They are Buprenorphine, heroin (diamorphine), ORLAM and dextropropoxyphene.
Buprenorphine and methadone are used in the UK
UKand many other countries for the treatment of narcotic addicts. Heroin is also known as diamorphine. Many countries allow heroin to be prescribed for patients undergoing detoxification programs. Heroin is also given to patients taking treatment for many other opiate addictions.
Interestingly enough, an Austrian study shows that orally tendered morphines are more effective than its oral methadone counterpart. Patients developing immunity to many traditional detoxification programs positively respond to a combination of morphine and a low dosage of methadone.
ORLAM is a synthetic compound. It is also known as LAAM. It is composed of levo-alphacetylmethadol. LAAM ‘s effects last from 42 to 72 hours. This compound was okayed as a medication for the patients suffering from chronic narcotics addiction in 1994. LAAM is also included in the US Controlled Substances Act (Schedule II). After reports were received that LAAM intake caused cardiac complications in some people, it was withdrawn from the American and the European markets.
Dextropropoxyphene is popular as a pain reliever. In the USA
USA, more than 100 ton of this oral analgesic is produced annually. It is most effective in patients suffering moderate pains.
Dextropropoxyphene overdose is reported to have been the cause of many deaths especially among the recreational youth generation. In fact, it is among the top 10 such drugs in the USA
USA. Dextropropoxyphene is included within Schedule II of the US Controlled Substances Act. However, medications containing Dextropropoxyphene are put in the Schedule IV. Its strength can be gauzed from the fact that aspirin takes 600 mg to be equal to just 65 mg of Dextropropoxyphene. It was first marketed in 1957 as Darvon.
Methadone abuse is not common primarily because it is not strong. Besides, the addicts prefer such opioids whose effects are instant or fast. In this aspect, methadone is rather slow. But abusers use the snort method to elicit a stronger euphoric and faster effect. There are, of course, occasional reports of deaths occurring due to methadone overdose. Such instances are more among the perennial drug abusers. Such habituated abusers go for methadone species like the ‘Street Meth’. Many illicit drug markets sell methadone as alternatives to other opioids.
Such demands are usually from three types of people. Those addicts who had at one point of time taken methadone as a part of medical regimen may again feel a strong tendency to go for methadone. Moreover, kin of patients having methadone may fall easy prey to the synthetic drug. There can also be a demand for methadone from the habituated opioid abusers if they are unable to get hold of any other brands.
METHADONE ILLICIT MARKET
The methadone consignments enter the illicit drug market via two ways. Methadone packets usually get diverted into the illicit market from the destinations. It can also enter the drug market through theft. This is done mainly from the shippers or from the factories. Such methadone consignments rarely find their ways to the illicit drug market from the patients prescriptions.
THE METHADONE DEBATE
Of late, there has been a growing controversy about the efficacy of methadone. This is notwithstanding its proven track record that methadone is an opioid analgesic. There has been a rise in the number of methadone related deaths around the globe. Many vouchsafe that methadone is intimately connected with the drug abusers. Above all, there has not been a single scientific report that methadone is an ideal medication for relieving chronic pain. One thing is for sure, though. Methadone does not possess any extra-strong pain relieving effects compared to the other opiates. Methadone is far more dangerous than most opiates, because most of the physicians do not prefer methadone usage.