Tuesday, December 14, 2010

"Vice Pioneers" : Heroin

Recognizable Bayer brand

Taboo Bayer brand

Afghan poppy fields forever

Felix Hoffman: notable heroin cooker

Of all topics used for the "Vice Pioneers" series, drugs are usually the most fascinating of the bunch. Due to the fact that drugs are such big business and scientifically based, their histories always include involvement by notable, recognizable companies. In heroin's case, Bayer is the culprit. Heroin's history in general is very fascinating. Below is some basic history on the drug.

From Wikipedia: Heroin (diacetylmorphine (INN)), also known as diamorphine (BAN), is a semi-synthetic opioid drug synthesized from morphine, a derivative of the opium poppy. It is the 3,6-diacetyl ester of morphine (di (two)-acetyl-morphine). The white crystalline form is commonly the hydrochloride salt diacetylmorphine hydrochloride, though often adulterated thus dulling the sheen and consistency from that to a matte white powder, which diacetylmorphine freebase typically is. 90% of diacetylmorphine is said to be produced in Afghanistan.

In 1895, the German drug company Bayer marketed diacetylmorphine as an over the counter drug under the trademark name Heroin. The name was derived from the German word "heroisch" (heroic) because of its perceived "heroic" effects upon a user. It was chiefly developed as a morphine substitute for cough suppressants that did not have morphine's addictive side-effects. Morphine at the time was a popular recreational drug, and Bayer wished to find a similar but non-addictive substitute to market. However, contrary to Bayer's advertising as a "non-addictive morphine substitute," Heroin would soon have one of the highest rates of dependence amongst its users.

The opium poppy was cultivated in lower Mesopotamia as long ago as 3400 BCE. The chemical analysis of opium in the 19th century revealed that most of its activity could be ascribed to two alkaloids, codeine and morphine.

Diacetylmorphine was first synthesized in 1874 by C. R. Alder Wright, an English chemist working at St. Mary's Hospital Medical School in London. He had been experimenting with combining morphine with various acids. He boiled anhydrous morphine alkaloid with acetic anhydride for several hours and produced a more potent, acetylated form of morphine, now called diacetylmorphine. The compound was sent to F. M. Pierce of Owens College in Manchester for analysis. Pierce told Wright:

“Doses ... were subcutaneously injected into young dogs and rabbits ... with the following general results ... great prostration, fear, and sleepiness speedily following the administration, the eyes being sensitive, and pupils constrict, considerable salivation being produced in dogs, and slight tendency to vomiting in some cases, but no actual emesis. Respiration was at first quickened, but subsequently reduced, and the heart's action was diminished, and rendered irregular. Marked want of coordinating power over the muscular movements, and loss of power in the pelvis and hind limbs, together with a diminution of temperature in the rectum of about 4°."

Wright's invention did not lead to any further developments, and diacetylmorphine only became popular after it was independently re-synthesized 23 years later by another chemist, Felix Hoffmann. Hoffmann, working at the Aktiengesellschaft Farbenfabriken (today the Bayer pharmaceutical company) in Elberfeld, Germany, was instructed by his supervisor Heinrich Dreser to acetylate morphine with the objective of producing codeine, a constituent of the opium poppy, pharmacologically similar to morphine but less potent and less addictive. Instead the experiment produced an acetylated form of morphine one and a half to two times more potent than morphine itself.

From 1898 through to 1910 diacetylmorphine was marketed under the trademark name Heroin as a non-addictive morphine substitute and cough suppressant. Bayer marketed the drug as a cure for morphine addiction before it was discovered that it rapidly metabolizes into morphine. As such, diacetylmorphine is essentially a quicker acting form of morphine. The company was embarrassed by the new finding, which became a historic blunder for Bayer.

In the U.S.A. the Harrison Narcotics Tax Act was passed in 1914 to control the sale and distribution of diacetylmorphine and other opioids, which allowed the drug to be prescribed and sold for medical purposes. In 1924 the United States Congress banned its sale, importation or manufacture. It is now a Schedule I substance, which makes it illegal for non-medical use in signatory nations of the Single Convention on Narcotic Drugs treaty, including the United States.

The Health Committee of the League of Nations banned diacetylmorphine in 1925 although it took more than three years for this to be implemented. In the meantime, the first designer drugs, viz. 3,6 diesters and 6 monoesters of morphine and acetylated analogues of closely-related drugs like hydromorphone and dihydromorphine were produced in massive quantities to fill the worldwide demand for diacetylmorphine—this continued until 1930 when the Committee banned diacetylmorphine analogues with no therapeutic advantage over drugs already in use, the first major legislation of this type.

Later, as with Aspirin, Bayer lost some of its trademark rights to Heroin under the 1919 Treaty of Versailles following the German defeat in World War I.

Traffic is heavy worldwide, with the biggest producer being Afghanistan. According to U.N. sponsored survey, as of 2004, Afghanistan accounted for production of 87 percent of the world's diacetylmorphine. Afghan opium kills 100,000 people every year worldwide.

The cultivation of opium in Afghanistan reached its peak in 1999, when 350 square miles (910 km2) of poppies were sown. The following year the Taliban banned poppy cultivation, a move which cut production by 94 percent. By 2001 only 30 square miles (78 km2) of land were in use for growing opium poppies. A year later, after American and British troops had removed the Taliban and installed the interim government, the land under cultivation leapt back to 285 square miles (740 km2), with Afghanistan supplanting Burma to become the world's largest opium producer once more. Opium production in that country has increased rapidly since, reaching an all-time high in 2006. War in Afghanistan once again appeared as a facilitator of the trade. Some 3.3 million Afghans are involved in producing opium.

At present, opium poppies are mostly grown in Afghanistan, and in Southeast Asia, especially in the region known as the Golden Triangle straddling Myanmar, Thailand, Vietnam, Laos and Yunnan province in the People's Republic of China. There is also cultivation of opium poppies in the Sinaloa region of Mexico and in Colombia. The majority of the diacetylmorphine consumed in the United States comes from Mexico and Colombia. Up until 2004, Pakistan was considered one of the biggest opium-growing countries.

Conviction for trafficking diacetylmorphine carries the death penalty in most Southeast Asian, some East Asian and Middle Eastern countries, among which Malaysia, Singapore and Thailand are the most strict. The penalty applies even to citizens of countries where the penalty is not in place, sometimes causing controversy when foreign visitors are arrested for trafficking, for example the arrest of nine Australians in Bali, the death sentence given to Nola Blake in Thailand in 1987, or the hanging of an Australian citizen Van Tuong Nguyen in Singapore.

Trafficking history
The origins of the present international illegal diacetylmorphine trade can be traced back to laws passed in many countries in the early 1900s that closely regulated the production and sale of opium and its derivatives including diacetylmorphine. At first, diacetylmorphine flowed from countries where it was still legal into countries where it was no longer legal. By the mid-1920s, diacetylmorphine production had been made illegal in many parts of the world. An illegal trade developed at that time between diacetylmorphine labs in China (mostly in Shanghai and Tianjin) and other nations. The weakness of government in China and conditions of civil war enabled diacetylmorphine production to take root there. Chinese triad gangs eventually came to play a major role in the illicit diacetylmorphine trade. The French Connection route started in the 1930s.

Diacetylmorphine trafficking was virtually eliminated in the U.S. during World War II because of temporary trade disruptions caused by the war. Japan's war with China had cut the normal distribution routes for diacetylmorphine and the war had generally disrupted the movement of opium.

After World War II, the Mafia took advantage of the weakness of the postwar Italian government and set up diacetylmorphine labs in Sicily. The Mafia took advantage of Sicily's location along the historic route opium took westward into Europe and the United States.

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