Balls (i_s_d) wrote in _war_on_drugs_,

Reducing Tolerance To Morphine Could Aid Pain Therapy

Morphine is one of the most commonly used drugs in the treatment of severe and chronic pain. A major complication with its use over the long term is that patients develop tolerance to it, as well as becoming addicted.

A way of reducing tolerance would be of great benefit, because it would allow doctors to use lower doses over longer periods and still control pain effectively.

A study published in this week's issue of Cell provides just that, by showing that giving a small level of a different drug at the same time as morphine can reduce the development of tolerance.


Utopian Pharmacology


Can safe, sustainable analogues of MDMA be developed? There is an urgent need for non-neurotoxic empathogens and entactogens suitable for lifelong use. Alas no single "magic bullet" yet exists that replicates the subjective effects of MDMA on a long-term basis. Hence most of us are doomed to display the quasi-psychopathic indifference to each other characteristic of the MDMA-naïve state.

A Brief History of MDMA

MDMA [3,4-methylenedioxy-methamphetamine: 'Ecstasy'] was first1 synthesized in 1912 by the German pharmaceutical company Merck. MDMA was patented in Darmstadt, Germany on May 16th 1914, issue number 274,350; and promptly forgotten. Merck's researchers had no idea of the significance of what they had done. Merck were searching for a good vasoconstrictor, a styptic to reduce bleeding. In 1912 two of their chemists, G. Mannish and W. Jacobsohn, created MDMA as a by-product while attempting to synthesise hydrastinin. MDMA is listed on Merck's patent-application merely as a chemical intermediate "for products of potential pharmaceutical value".

MDMA surfaced again briefly as one of a number of agents used in clandestine US military research during the 1950s. The CIA's Project MK-Ultra was investigating new techniques of brainwashing, espionage and mind-control. MDMA, code-named EA-1475, was tested at the US Army's Edgewood Arsenal in Maryland. However, unlike LSD or the ill-named "truth drug" scopolamine, MDMA was used only on animals: mice, rats, pigs, monkeys and dogs. Thankfully, MDMA's military potential was not realised. For although MDMA is no infallible truth-serum, its effects on the human user might indeed be abused for sinister purposes by skilled interrogators. The heightened emotional responsiveness, lowering of defensive barriers, openness and sense of closeness to others induced by MDMA can promote an honesty of self-disclosure that might be manipulated for malign ends. Fortunately, this hasn't yet happened on an organised scale.


Deadly Short Cuts

Heroin is named after the German word for hero, heroisch. According to popular legend, its substitute, methadone, was initially christened Dolophine in honour of Adolf Hitler. In reality, the name comes from the Latin dolor, meaning "pain", and fin, meaning "end": hence "end of pain".

The consumption of heroin is marked by a euphoric rush, a warm feeling of relaxation, a sense of security and protection, and a dissipation of pain, fear, hunger, tension and anxiety. When heroin is snorted or smoked, the rush is intense and orgasmic. Subjectively, time may slow down. Any sense of anger, frustration or aggression disappears. Users enjoy the feeling of "being wrapped in God's warmest blanket".

Heroin is the most fast-acting of all the opiates. When injected, it reaches the brain in 15-30 seconds; smoked heroin reaches the brain in around 7 seconds. The peak experience via this route lasts at most a few minutes. The surge of pleasure seems to start in the abdomen; a delicious warmth then spreads throughout the body. After the intense euphoria, a period of tranquillity ("on the nod") follows, lasting up to an hour. Experienced users will inject between 2-4 times per day. After taking heroin, some people feel cocooned and emotionally self-contained. Others feel stimulated and sociable. Either way, there is a profound sense of control and well-being. The euphoria gradually subsides into a dreamy and relaxed state of contentment. Higher doses of heroin normally make a person feel sleepy. At higher doses still, the user will nod off into a semi-conscious state. The effects usually wear off in 3-5 hours, depending on the dose. Heroin is not toxic to the organ systems of the body. But in prohibitionist society the mortality of street users is high.


A Brief History of Opium

c.3400 B.C.

The opium poppy is cultivated in lower Mesopotamia. The Sumerians refer to it as Hul Gil, the 'joy plant.' The Sumerians would soon pass along the plant and its euphoric effects to the Assyrians. The art of opium poppy-culling would continue from the Assyrians to the Babylonians who in turn would pass their knowledge onto the Egyptians.

c.1300 B.C.

In the capital city of Thebes, Egyptians begin cultivation of opium thebaicum, grown in their famous poppy fields. The opium trade flourishes during the reign of Thutmose IV, Akhenaton and King Tutankhamen. The trade route included the Phoenicians and Minoans who move the profitable item across the Mediterranean Sea into Greece, Carthage, and Europe.

c.1100 B.C.

On the island of Cyprus, the "Peoples of the Sea" craft surgical-quality culling knives to harvest opium, which they would cultivate, trade and smoke before the fall of Troy.


Future Synthetic Drugs of Abuse


It seems likely that primitive man wished at times to escape his reality and most probably found some natural drug to facilitate this desire. In fact, abuse of the coca leaf and the opium poppy is thought to have been practiced for at least the last 3400 years (Lathrap 1976; Rosengarten 1969) and the use of peyote may have been known as early as 1000 BC (Schultes 1938; 1940). Perhaps due in part to the long history of opiate products, one of the first derivatives of a natural drug to be used pharmaceutically was heroin. The acceptance of heroin as a pharmaceutical was primal in establishing the concept that certain structural modifications of physiologically active compounds can result in new compounds which cause biological responses which are not only similar, but are enhanced as compared to those of the parent compounds. Other works such as the structural elucidation of mescaline and the preparation of N-methyl and N-acetyl derivatives of mescaline has served to strengthen this concept and to broaden the scope of permissible derivatives (Spath 1919). In the ensuing years much knowledge has been gained regarding biologically useful derivatives of the naturally occurring drugs but, most importantly, the structures of the alkaloids and the protoalkaloids have, one by one, been elucidated. This knowledge has then allowed researchers of recent times to deduce many of the structure relationships associated with specific biological responses. The sum of this hardwon knowledge allows one to produce pharmaceutically useful compounds, which have no counterpart in nature, from off the shelf chemicals. Unfortunately there are those people who would take this body of knowledge and, rather than use it for the enhancement of medical science, use it for their own financial gain. Individuals such as these have created the so-called designer drug phenomenon.

Henderson (1986) first described a synthetic drug as one which was designed by a clandestine chemist to produce a certain pharmacological response. However, today designer drugs are universally understood to belong to a group of clandestinely produced drugs which are structurally and pharmacologically very similar to a controlled substance but are not themselves controlled substances (Langston and Rosner 1986). The Drug Enforcement Administration (DEA) has noted that the designer drug terminology tends to cast a somewhat glamorous aura onto the concept, and as a result, the DEA feels that it would be wise to refer to these compounds in some other manner and suggests the use of the term Controlled Substance Analogs (CsA).

In October of 1987 the United States Government amended the Controlled Substance Act in an effort to curtail the illicit introduction of new CsA's. This amendment states that any new drug which is substantially similar to a controlled substance currently listed under the Code of Federal Regulations (CFR), Schedule I or II, and has either pharmacological properties similar to a Schedule I or II substance or is represented as having those properties, shall also be considered a controlled substance and will be placed in Schedule I. The amendment further contains provisions which exempt the legitimate researcher as well as compounds that are already being legally marketed from the provisions of the amendment.

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