1 History

Heroin was first synthesised in 1874 by C.R.A. Wright, a British chemist working at St. Mary's Hospital Medical School, London. 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. We now call it diacetylmorphine. The compound was sent to F.M. Pierce of Owens College, Manchester, for analysis. He 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 dilated, 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° [1]

Heinrich Dreser (who discovered aspirin), of Bayer in Elberfeld, Germany, noticed that diacetylmorphine was more potent than morphine. Bayer registered heroin (meaning 'heroic treatment' from the German word heroisch) as a trademark. From 1898 through to 1910 it was marketed as a non-addictive morphine substitute and cough medicine for children.

In 1924, the United States' Heroin Act made it illegal to manufacture or possess heroin in that country.

2 Usage and effects

Heroin is a mu-opioid agonist. Like all drugs of its class, it binds to and activates mu-opioid receptors found in the brain, spinal cord and gut. As a medicine, it is administered usually in the form of its hydrochloride as an analgesic for severe pain. It is illegal even for this purpose in the United States, but it is legally used by cancer patients in the United Kingdom and other countries.

Heroin is also widely and illictly used as a powerful and addictive drug producing intense euphoria. Although many other mu-opioid agonists (e.g., morphine) can produce essentially the same effects, it is thought that heroin's popularity with recreational users comes from its especially rapid onset. This in turn comes from its high lipid solubility provided by the two acetyl groups, resulting in a very rapid penetration of the blood-brain barrier after nasal inhalation or intravenous injection. Once in the brain, heroin is rapidly metabolized into morphine by removal of the acetyl groups.

Methadone is another mu-opioid agonist often used to substitute for heroin in treatment for heroin addiction. Compared to heroin, methadone is well (but slowly) absorbed orally and has a much longer duration of action. Thus methadone maintenance avoids the rapid cycling between intoxication and withdrawal associated with heroin addiction. Also, by keeping the addict physically tolerant to opioids, methadone effectively blocks the euphoric effects of heroin. In this way, methadone has shown some success as a 'less harmful substitute'; it is in fact the single most effective treatment known for opioid addiction, and is recommended for those who have repeatedly failed complete detoxification.

Heroin is chemically dissimilar to endorphins, the natural ( endogenous) opioids of the body and less potent. It competes with the endorphins for the specialized endorphine (opioid) receptors found on the surfaces of some body cells. The body responds by reducing (or even stopping) production of endorphins when heroin is consumed. Endorphins are regularly released in the brain and nerves and attenuate pain. Their other functions, if any, are still obscure. The reduced endorphin production in heroin users makes them dependent on the heroin since lack of either endorphins or heroin results in the extreme symptoms including pain (even in the absence of physical trauma). This is what causes the withdrawal symptoms in heroin addicts as the body takes some time to restore endorphin production.

While heroin is a dangerous drug, since it is a central nervous system depressant, it is the lack of available quality information, lack of quality control (few criminal drug dealers meet USP standards in their products), and infected syringes, which can transmit diseases such as AIDS, and hepatitis that cause the most trouble for heroin users. The money which can be made in supplying heroin addicts encourages a continuous supply, and the need to finance purchases generates considerable property crime.

Critics of drug prohibition contend that since addiction can be treated, primarily by counseling and methadone substitution, most of the suffering surrounding heroin is indirectly caused by prohibition, not by the drug itself. Others argue that legalising drug use, to the level of tobacco and alcohol, will eliminate the organized crime associated with it.

3 Production and trafficking

Heroin is a controlled substance, but traffic is heavy worldwide, with the biggest producer being Afghanistan, which after a ban on poppy growing by the Taliban in 2001 dropped its production by 95% but revived it to record numbers following the US military occupation and fall of the Taliban government. Currently, 86% of the global heroin supply is cultivated in Afghnistan, up from 75% in 2003 according to the U.N. Office of Drugs and Crime. The estimated value of the 2003 harvest is 2.8 billion USD. Some observers, particularly political conservatives in the United States, have accused China of being a leading producer of heroin, but the facts do not appear to back up these claims. Heroin is one of the most profitable illicit drugs since it is compact and easily concealed. At present, opium poppies are mostly grown in the Middle East, Pakistan, and Afghanistan, and in Asia, especially in the region known as the Golden Triangle straddling Myanmar, Thailand, Vietnam, Laos and Yunnan province in China. There is also cultivation of opium poppies in the Sinaloa region of Mexico and Columbia. The majority of the heroin consumed in the United States comes from Mexico and Columbia.

4 Direct short and long term effects of heroin use

• mental confusion
• euphoria
• slow and shallow respiration leading to respiratory arrest
• nausea and vomiting
• constipation
• death, caused either directly via overdose, or through intraveneously and sexually transmitted diseases via contaminated injection needles. Some countries have instituted programs to supply clean needles to addicts to reduce these risks, but others — including the United States — have resisted such efforts.

4.1 Other general risks

• HIV/AIDS and hepatitis infections from shared needles
• overdose, sometimes fatal
• long-term criminal involvement to support heroin habits
• malnourishment
• bacterial or fungal endocarditis
• skin conditions from constant injecting, often with poor technique
• poisoning from contaminants added to 'cut' or dilute heroin.

4.2 Withdrawal symptoms

The withdrawal syndrome from heroin (or any other short-acting opioid) can begin within 12 hours of discontinuation of the sustained use of the drug: sweating, malaise, anxiety, depression, persistent and intense penile erection in males ( priapism), general feeling of heaviness, cramp-like pains in the limbs, yawning and lachrymation, sleep difficulties, nausea and vomiting, diarrhea, cramps and fever occur. Many addicts also complain of a painful condition, the so-called "itchy blood". However, it must be noted that each person's symptoms can be unique. There is also a significant risk of tonic-clonic or grand mal seizures (although less so than during withdrawal from sedatives such as barbiturates), which can lead to stroke possibly resulting in permanent disability including blindness or paralysis, or heart attacks which can potentially be fatal.

Two general approaches are available to ease opioid withdrawal. The first is to substitute a longer-acting opioid such as methadone for heroin or another short-acting opioid and then slowly taper the dose. The other approach, which can be used alone or in combination, is to relieve withdrawal symptoms with non-opioid medications.

In the second approach, benzodiazepines such as diazepam (Valium) ease the often extreme anxiety of opioid withdrawal. Many symptoms of opioid withdrawal are due to rebound hyperactivity of the sympathetic nervous system, and this can be effectively suppressed with clonidine (Catapres ), a centrally-acting alpha-2 agonist primarily used to treat hypertension. Many addicts who have been through these programs say that the agony of withdrawal is very much attenuated.

For those who repeatedly fail attempts at complete detoxification and relapse to heroin use, maintenance with regular doses of methadone is recommended.

4.3 Drug interactions

Opiates 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 experienced users.

Toxicology studies of heroin overdose deaths reveal frequent involvement of other central nervous system depressants, including alcohol, benzodiazepines such as valium, and occasionally methadone. Ironically, benzodiazepines and methadone are often used in the treatment of heroin addiction.

Cocaine also proves to be often fatal when used in combination with heroin. Though "speedballs" (when injected) or "moonrocks" (when smoked) are a popular mix of the two drugs used among addicts, combinations of stimulants and depressants can have unpredictable and sometimes fatal results.

A heroin overdose is usually treated with an opioid antagonist, such as naloxone (Narcan) or naltrexone, which have a high affinity for endorphin receptors, and cause an immedeate return to consciousness and start of withdrawal symptoms when administered intraveneously. Contrary to popular belief, propagated mainly by the film Pulp Fiction, an adrenaline injection into the heart is not an effective way to treat a heroin overdose.

5 Cultural influences

Due to both the dramatic effects of the drug on the consumers life and the widespread use of heroin amongst artists, heroin consumption and addiction has been featured in numerous works of art, ranging from songs and films to novels. Amongst these are:

5.1 Novels

• Junkie by William S. Burroughs
• Naked Lunch by William S. Burroughs
• Junk by Melvin Burgess
• The Basketball Diaries by Jim Carroll
• Trainspotting by Irvine Welsh
• Cain's Book by Alexander Trocchi
• Requiem for a Dream by Hubert Selby

5.2 Factual accounts

• Wir Kinder vom Bahnhof Zoo (life story of Christiane F. a teenager German addict)
• Permanent Midnight by Jerry Stahl

5.3 Films

• Sid and Nancy directed by Alex Cox
• Naked Lunch directed by David Cronenberg
• Trainspotting directed by Danny Boyle
• Pulp Fiction directed by Quentin Tarantino
• Permanent Midnight directed by David Veloz
• Requiem for a Dream directed by Darren Aronofsky
• Ray directed by Taylor Hackford
• Wasted directed by Stephen T. Kay

5.4 Songs

• "I'm Waiting for the Man" and "Heroin" by The Velvet Underground
• "Perfect Day" by Lou Reed
• "Space Oddity" and "The Bewlay Brothers" by David Bowie
• "Dead Flowers", "Sister Morphine" and "Monkey Man" by The Rolling Stones
• "Black Balloon" by the Goo Goo Dolls
• " Golden Brown" by The Stranglers
• " Signed D.C. " by Love
• " Aux enfants de la chance " and " My Lady Heroine " by Serge Gainsbourg
• " Chinese Rocks" by Johnny Thunders and Dee Dee Ramone
• "Needle in the Hay" by Elliott Smith
• " Under the Bridge " by Red Hot Chili Peppers
• " Comfortably Numb" by Pink Floyd
• " Cold Turkey " by John Lennon
• "The Needle and the Damage Done" by Neil Young
• "I Believe In You" by Talk Talk

5.5 Musicals

• Rent by Jonathan Larson

6 See also

• recreational drug use
• Notable Heroin Addicts
• Hillbilly heroin

7 External links

• Geopium: Geopolitics of Illicit Drugs in Asia
• Good Drugs Guide
• Heroin Helper
• From Flowers to Heroin, CIA publication.

Aromatic hydrocarbons Esters Ethers Heterocyclic bases Mu-opioid agonists Opiates Schedule I controlled substances Semisynthetic opioids

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