Heroin Addiction

Heroin

 (INN: diacetylmorphine, BAN: diamorphine) is a semi-synthetic opiate synthesized from morphine, derived from the opium poppy plant. It is the 3, 6-diacetyl ester of morphine (therfore diacetylmorphine) and is processed by acetylation, making it a prodrug for the systemic delivery of morphine. The white crystalline is most commonly the hydrochloride salt diacetylmorphine hydrochloride. Upon crossing the blood-brain barrier, which occurs shortly after introduction of heroin into the bloodstream, heroin is converted into monoacetylmorphine and morphine, the compounds that mimic the action of endorphins, creating a feeling of extreme well-being with the feeling centered in the gut. One of the most common methods of heroin use is by intravenous injection.

As with other opiates, heroin is used both as a physical pain-killer and a recreational drug. Frequent use has a high potential for creating an addiction to heroin and may quickly lead a tolerance to heroin. If a continual, sustained use of heroin for as short as three days is discontinued abruptly, withdrawal symptoms can occur. This can be much shorter than the withdrawal effects experienced from other common prescription painkillers such as oxycodone and hydrocodone.

Internationally, heroin is controlled under Schedules I and IV of the Single Convention on Narcotic Drugs.[3] It is illegal to process, possess, or distribute heroin in the United States and the UK. Slang street names for heroin include smack, black tar, junk, skag, horse, Brain, and others. These words are specific references to heroin and only heroin. Dope is  commonly used to refer to heroin, but may indicate many other drugs as well, from laudanum a century ago to nearly any contemporary illegal drug.

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

Heroin was originally maufactured in 1874 by C.R. Alder Wright, an English chemist enployed at St. Mary's Hospital Medical School in London, England. He had been experimenting with combining morphine with various acids. He boiled anhydrous morphine alkaloid with acetic anhydride over a stove 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, who reported the following to 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 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, combined with a diminution of temperature in the rectum of about 4° (rectal failure).
Wright's invention, however, did not lead to any further developments, and heroin only became popular after it was independently re-synthesized 23 years later by another chemist, Felix Hoffmann. Hoffmann, working at the Bayer pharmaceutical company in Elberfeld, Germany, was given instructions by his supervisor Heinrich Dreser to acetylate morphine with the objective of producing codeine, a natural derivative of the opium poppy plant, similar to morphine but not as potent and less addictive. But instead of producing codeine, the experiment produced an acetylated form of morphine that was actually 1.5-2 times more potent than morphine itself. Bayer would name the substance "heroin", probably from the word heroisch, German for heroic, because in field studies people using the medicine felt "heroic".

From 1898 through to 1910 heroin was advertised as a non-addictive morphine substitute and cough medicine for children. Bayer marketed heroin as a cure for morphine addiction before it was discovered that heroin is converted to morphine when metabolized in the liver, and as such, "heroin" was basically only a faster acting form of morphine. Bayer was somewhat embarrassed by this new finding and it became a historical blunder for Bayer.

As with aspirin, Bayer lost some of its trademark rights to heroin following the German defeat in World War I.

In the United States the Harrison Narcotics Tax Act was passed in 1914 to control the sale and distribution of heroin. The law prohibited heroin to be prescribed and sold for medical purposes. In particular, recreational users could often still be legally supplied with heroin. In 1924, the United States Congress passed additional legislation banning the sale, importation or manufacture of heroin in the United States. It is now a Schedule I substance, and is therefore illegal in the United States.

Heroin is used as a recreational drug for its intense euphoria, which often decreases with increased tolerance to the effects heroin. It is believed that heroin's popularity with recreational users, compared to morphine or other opiates, comes from its somewhat different perceived effects. This belief has not been supported by clinical research. In studies comparing the physiological and subjective effects of heroin and morphine administered intravenously in post-addicts, subjects showed no preference for one or the other of these drugs when administered on a single injection basis. Equipotent intravenous doses had similar action courses. There was no difference observed in their ability to create feelings of "euphoria," ambition, nervousness, relaxation, drowsiness, or sleepiness. Data acquired during short-term heroin addiction studies did not support the statement that tolerance develops more rapidly to heroin than to morphine. These discoveries have been discussed in relation to the physicochemical properties of heroin and morphine and the metabolism of heroin. When compared to other opioids -- hydromorphone, fentanyl, oxycodone, and meperidine, post-addicts showed a strong preference to heroin and morphine over the others, suggesting that heroin and morphine are more liable to abuse and addiction. Morphine and heroin were also much more likely to create feelings of "euphoria" , and other subjective effects when compared to most other opioid analgesics. Heroin can be administered in a number of ways, including snorting and injection. It may also be smoked by inhaling the vapors produced when heated (known as "chasing the dragon").

Some users combine heroin with cocaine in a so-called "speedball" or "snowball", which is usually injected intravenously although it can be smoked or dissolved in water and snorted. This causes a more potent rush effect than heroin alone but is even more dangerous due to the combination of the short-acting stimulant with the longer-acting depressant increases the risk of overdosing on one or both of the drugs.

Once in the brain, heroin quickly metabolizes into morphine by removal of the acetyl groups, thus, it is known as a prodrug. It is the morphine molecule that then binds with opioid receptors and produces the subjective effects of the heroin high.

The onset of heroin's effects is dependent on the mode of administration. Taken orally, heroin is completely metabolized in vivo into morphine before crossing the blood-brain barrier; so the effects are the same as oral morphine. Snorting heroin results in an onset within 3 to 5 minutes. Smoking heroin results in an almost immediate, though mild effect which strengthens the longer it is used 7 to 11 seconds. Intravenous injection results in rush and euphoria within 30 to 60 seconds; while intramuscular or subcutaneous injection takes longer, having an effect within 3 to 5 minutes.

Heroin is a μ-opioid (mu-opioid) agonist. It acts on endogenous μ-opioid receptors that are spread in discrete packets throughout the brain, spinal cord and gut in almost all mammals. Heroin, along with other opioids, are agonists to four endogenous neurotransmitters. They are β-endorphin, dynorphin, leu-enkephalin, and met-enkephalin. The body responds to heroin in the brain by reducing (and sometimes stopping) production of the endogenous opioids when heroin is present. Endorphins are regularly released in the brain and nerves, attenuating pain. Their other functions are still obscure, but are probably related to the effects produced by heroin besides analgesia (antitussin, anti-diarrheal). The reduced endorphin production in heroin users produces a dependence on the drug, and the cessation of heroin results in very uncomfortable heroin withdrawal symptoms including pain (even in the absence of physical trauma). This set of symptoms is called heroin withdrawal syndrome. It has an onset 6 to 8 hours after the last use of heroin.

Large doses of heroin can be fatal. The drug can be used for suicide or, as in the case of Sigmund Freud, physician-assisted suicide. Heroin can also be used as a murder weapon. The serial killer Dr. Harold Shipman used it on his victims as did Dr. John Bodkin Adams (see his victim, Edith Alice Morrell). It can sometimes be difficult to determine whether a heroin death was an accident, suicide or murder. The deaths of Joseph Krecker and Janis Joplin were such cases.


Heroin Regulation

In Canada heroin is a controlled substance under Schedule I of the Controlled Drugs and Substances Act (CDSA). Every person who seeks or obtains heroin without disclosing authorization 30 days prior to obtaining another prescription from a practitioner is guilty of an indictable offense and liable to imprisonment for a term not exceeding seven years. Possession for purpose of trafficking is guilty of an indictable offense and liable to imprisonment for life.

In Hong Kong, heroin is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. It can only be used legally by health professionals and for university research purposes. It can be given by pharmacists under a prescription. Anyone who supplies heroin without prescription can be fined $10000(HKD). The penalty for trafficking or manufacturing heroin is a $5,000,000 (HKD) fine and life imprisonment. Possession of heroin for consumption without license from the Department of Health is illegal with a $1,000,000 (HKD) fine and/or 7 years of jail time.

In the United Kingdom, heroin is available by prescription, though it is a restricted Class A drug. According to the British National Formulary (BNF) edition 50, diamorphine hydrochloride may be used in the treatment of acute pain, myocardial infarction, acute pulmonary oedema, and chronic pain. The treatment of chronic non-malignant pain must be supervised by a specialist. The BNF notes that all opioid analgesics cause dependence and tolerance but that this is "no deterrent in the control of pain in terminal illness". When used in the palliative care of cancer patients, heroin is often injected using a syringe driver.


Production and trafficking of heroin: The Golden Triangle

Manufacturing

Heroin is produced for the black market through opium refinement process - first, morphine is isolated from opium. This crude morphine is then acetylated by heating with acetic anhydride. Purification of the obtained crude heroin as a hydrochloride salt provides a water-soluble salt form of white or yellowish powder

Crude opium is carefully dissolved in hot water but the resulting hot soup is not boiled. Mechanical impurities - twigs - are scooped together with the foam. The mixture is then made alkaline by gradual addition of lime. Lime causes a number of unwelcome components present in opium to precipitate out of the solution. (The impurities include the useless alkaloids, resins, proteins). The precipitate is removed by filtration through a cloth, washed with additional water and discarded. The filtrates containing water-soluble calcium salt of morphine are then acidified by careful addition of ammonium chloride. This causes the morphine to precipitate. The morphine precipitate is collected by filtration and dried before the next step. The crude morphine (which makes only about 10% of the weight of the used opium) is then heated together with acetic anhydride at 85 °C (185 °F) for six hours. The reaction mixture is then cooled, diluted with water, alkalized with sodium carbonate and the precipitated crude heroin is filtered and washed with water. This crude water-insoluble free-base product (which by itself is usable, for smoking) is further purified and decolorised by dissolution in hot alcohol, filtration with activated charcoal and concentration of the filtrates. The concentrated solution is then acidified with hydrochloric acid, diluted with ether and the precipitated white hydrochloride salt of heroin is collected by filtration. This precipitate is the so-called "no. 4 heroin", the standard product exported to the Western markets. (Side-product residues from purification or the crude free base product are also available on the markets, as the "tar heroin" - a cheap substitute of inferior quality.)

The initial stage of opium refining - the isolation of morphine - is very easy to perform in rudimentary setting - even with substituting suitable fertilizers for pure chemical reagents. However the later steps (acetylation, purification, precipitation as hydrochloride) are more involved - they use large quantities of dangerous chemicals and solvents and they require a skill and patience. The final step is particularly tricky as the highly flammable ether can easily ignite during the positive-pressure filtration (the explosion of vapor-air mixture can obliterate the refinery). If the Heroin does ignite, the result is a catastrophic explosion.


History of heroin trafficking

The origins of the present international illegal heroin 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 heroin. At first, heroin flowed from countries where it was still legal into countries where it was no longer legal. By the mid-1920s, heroin production had been made illegal in many parts of the world. An illegal trade developed at that time between heroin labs in China (mostly in Shanghai and Tianjin) and other nations. The weakness of government in China and conditions of civil war enabled heroin production to take root there. Chinese triad gangs eventually came to play a major role in the heroin trade.

Heroin trafficking was virtually eliminated in the U.S. during World War II due to temporary trade disruptions caused by the war. Japan's war with China had cut the normal distribution routes for heroin and the war had generally disrupted the movement of opium. After the second world war, the Mafia took advantage of the weakness of the postwar Italian government and set up heroin labs in Sicily. The Mafia took advantage of Sicily's location along the historic route opium took from Iran westward into Europe and the United States. Large scale international heroin production effectively ended in China with the victory of the communists in the civil war in the late 1940s. The elimination of Chinese production happened at the same time that Sicily's role in the trade developed.

Although it remained legal in some countries until after World War II, health risks, addiction, and widespread abuse led most western countries to declare heroin a controlled substance by the latter half of the 20th century.

Between the end of World War II and the 1970s, much of the opium consumed in the west was grown in Iran, but in the late 1960s, under pressure from the U.S. and the United Nations, Iran engaged in anti-opium policies. While opium production never ended in Iran, the decline in production in those countries led to the development of a major new cultivation base in the so-called "Golden Triangle" region in South East Asia. In 1970-71, high-grade heroin laboratories opened in the Golden Triangle. This changed the dynamics of the heroin trade by expanding and decentralizing the trade. Opium production also increased in Afghanistan due to the efforts of Turkey and Iran to reduce production in their respective countries. Lebanon, a traditional opium supplier, also increased its role in the trade during years of civil war.

Soviet-Afghan war led to increased production in the Pakistani-Afghani border regions. It increased international production of heroin at lower prices in the 1980s. The trade shifted away from Sicily in the late 1970s as various criminal organizations violently fought with each other over the trade. The fighting also led to a stepped up government law enforcement presence in Sicily. All of this combined to greatly diminish the role of the country in the international heroin trade.


Heroin Trafficking


Heroin Trafficking 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 heroin. Opium production in that country has increased rapidly since, reaching an all-time high in 2006. War once again appeared as a facilitator of the trade.

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[citation needed] and in Colombia. The majority of the heroin consumed in the United States comes from Mexico and Colombia. Up until 2004, Pakistan was considered one of the biggest opium-growing countries. However, the efforts of Pakistan's Anti-Narcotics Force have since reduced the opium growing area by 59% as of 2001. Some suggest that the decline in Pakistani production is inversely proportional to the rise of Afghani production, and that rather than anti-narcotics activity, the decline in Pakistan is due more to changed market forces.

Conviction for trafficking in heroin carries the death penalty in most South-east Asia and some East Asia and Middle Eastern countries (see Use of death penalty worldwide for details), 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 or the hanging of Australian citizen Van Tuong Nguyen in Singapore, both in 2005.

Sandra Gregory has written an autobiography covering her experience of getting caught with Heroin at a Thai airport.

In the 1960s, and early 1970's, Frank Lucas organized the smuggling of heroin from Vietnam to the U.S. by using the coffins of dead American servicemen.

Heroin overdose

A heroin overdose is usually treated with an opioid antagonist, such as naloxone (Narcan), which has a high affinity for opioid receptors but does not activate them. This blocks heroin and other opioid antagonists and causes an immediate return of consciousness and the beginning of withdrawal symptoms when administered intravenously. The half-life of this antagonist is usually much shorter than that of the opiate drugs it is used to block, so the antagonist usually has to be re-administered multiple times until the opiate has been metabolized by the body.

Depending on drug interactions and numerous other factors, death from overdose can take anywhere from several minutes to several hours due to anoxia because the breathing reflex is suppressed by µ-opioids. An overdose is immediately reversible with an opioid antagonist injection. Heroin overdoses can occur due to an unexpected increase in the dose or purity or due to diminished opiate tolerance. However, most fatalities reported as overdoses are probably caused by interactions with other depressant drugs like alcohol or benzodiazepines.

The LD50 for a physically addicted person is prohibitively high, to the point that there is no general medical consensus on where to place it. Several studies done in the 1920s gave users doses of 1,600–1,800 mg of heroin in one sitting, and no adverse effects were reported. This is approximately 16–18 times a normal recreational dose. Even for a non-user, the LD50 can be placed above 350 mg though some sources give a figure of between 75 and 375 mg for a 75 kg person.

Street heroin is of widely varying and unpredictable purity. This means that the user may prepare what they consider to be a moderate dose while actually taking far more than intended. Also, those who use the drug after a period of abstinence have tolerances below what they were during active addiction. If a dose comparable to their previous use is taken, an effect greater to what the user intended is caused, in extreme cases an heroin overdose can result.

It has been speculated that an unknown portion of heroin related deaths are the result of an overdose or allergic reaction to quinine, which may sometimes be used as a cutting agent.

A final source of overdose in users comes from place conditioning. Heroin use, like other drug using behaviors, is highly ritualized. While the mechanism has yet to be clearly elucidated, it has been shown that longtime heroin users, immediately before injecting in a common area for heroin use, show an acute increase in metabolism and a surge in the concentration of opiate-metabolizing enzymes. This acute increase, a reaction to a location where the user has repeatedly injected heroin, imbues him or her with a strong (but temporary) tolerance to the toxic effects of the drug. When the user injects in a different location, this place-conditioned tolerance does not occur, giving the user a much lower-than-expected ability to metabolize the drug. The user's typical dose of the drug, in the face of decreased tolerance, becomes far too high and can be toxic, leading to a heroin overdose.

A small percentage of heroin smokers may develop symptoms of toxic leukoencephalopathy. This is believed to be caused by an uncommon adulterant that is only active when heated. Symptoms include slurred speech and difficulty walking.

Heroin Withdrawal
 
Black tar heroinThe withdrawal syndrome from heroin may begin starting from within 6 to 24 hours of discontinuation of sustained use of the drug; however, this time frame can fluctuate with the degree of tolerance as well as the amount of the last consumed dose. Symptoms may include: sweating, malaise, anxiety, depression, persistent and intense penile erection in males (priapism), extra sensitivity of the genitals in females, general feeling of heaviness, cramp-like pains in the limbs, yawning, tears, sleep difficulties(insomnia), cold sweats, chills, severe muscle and bone aches not precipitated by any physical trauma; nausea and vomiting, diarrhea, goose bumps, cramps, and fever. Many users also complain of a painful condition, the so-called "itchy blood", which often results in compulsive scratching that causes bruises and sometimes ruptures the skin, leaving scabs. Abrupt termination of heroin use causes muscle spasms in the legs of the user (restless leg syndrome).


Drug interactions

Opioids are strong central nervous system depressants, but regular users develop physiological tolerance allowing gradually increased dosages. In combination with other central nervous system depressants, heroin may still kill even experienced users, particularly if their tolerance to the drug has reduced or the strength of their usual dose has increased.

Toxicology studies of heroin-related deaths reveal frequent involvement of other central nervous system depressants, including alcohol, benzodiazepines such as diazepam (Valium), and, to a rising degree, methadone. Ironically, benzodiazepines are often used in the treatment of heroin addiction while they cause much more severe withdrawal symptoms.

Cocaine sometimes proves to be fatal when used in combination with heroin. Though "speedballs" (when injected) or "moonrocks" (when smoked) are a popular mix of the two drugs among users, combinations of stimulants and depressants can have unpredictable and sometimes fatal results. In the United States in early 2006, a rash of deaths was attributed to either a combination of fentanyl and heroin, or pure fentanyl masquerading as heroin particularly in the Detroit Metro Area; one news report refers to the combination as 'laced heroin', though this is likely a generic rather than a specific term.