Heroin
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- Not to be confused with Heroine (female hero).
| Heroin | |
| Systematic (IUPAC) name | |
| (5α,6α)-7,8-didehydro-4,5-epoxy- 17-methylmorphinan-3,6-diol diacetate (ester) | |
| Identifiers | |
| CAS number | |
| ATC code | N02 |
| PubChem | |
| Chemical data | |
| Formula | C21H23NO5 |
| Mol. mass | 369.41 |
| Pharmacokinetic data | |
| Bioavailability | <35% |
| Protein binding | 0% (morphine metabolite 35%) |
| Metabolism | hepatic |
| Half life | 2-3 hours |
| Excretion | 90% renal as glucuronides, rest biliary |
| Therapeutic considerations | |
| Pregnancy cat. | ? |
| Legal status | Prohibited (S9)(AU) Schedule I(CA) Class A(UK) Schedule I(US) |
| Dependence Liability | Extremely High |
| Routes | Inhalation, Transmucosal, Intravenous, Oral, Intranasal, Rectal, Intramuscular |
Heroin (INN: diacetylmorphine, BAN: diamorphine) is an opiate processed directly from the extracts of the opium poppy, Papaver somniferum, originally intended to break morphine addictions. It is the 3,6-diacetyl ester of morphine (hence diacetylmorphine) and is processed by acetylation, making it a prodrug for the systemic delivery of morphine. The white crystalline form is commonly the hydrochloride salt diacetylmorphine hydrochloride. Upon crossing the blood-brain barrier, which occurs soon after introduction of the drug into the bloodstream, heroin is converted into morphine, which mimics the action of endorphins, creating a sense of well-being; the characteristic euphoria has been described as an "orgasm" centered in the gut. One of the most common methods of heroin use is via intravenous injection.
Due to heroin's mimicry of endorphins, it is used both as a pain-killer and a recreational drug. Frequent administration has a high potential for causing addiction and may quickly lead to tolerance; however, occasional use does not lead to symptoms of withdrawal. If a continuous, sustained use of heroin for as little as three days is stopped abruptly, withdrawal symptoms can appear. This is much shorter than other common painkillers such as oxycodone and hydrocodone.[1][2]
Internationally, heroin is controlled under Schedules I and IV of the Single Convention on Narcotic Drugs.[3] It is illegal to manufacture, possess, or sell heroin in the United States and the UK. However, under the name diamorphine, heroin is a legal prescription drug in the United Kingdom. Popular street names for heroin are gear, diesel, smack, B, boy, skag, Harry, Bobby, black tar, horse, honk, munge, junk, brok, jack, jenny, brown, brown sugar, brownstone, dark, sweaty, dope, pof, sam, waccocco, lovage, dragon, bitch, skurge, ron, ice cube, A-Stock, jim, jim nix, moop, sweet lady H, big time, holloween, calipop, and H.
Contents
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[edit] History
The opium poppy was cultivated in lower Mesopotamia as long ago as 3400 BC.[4] 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 first processed in 1874 by C.R. Alder Wright, an English chemist working 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 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° (rectal failure).[5]
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 instructed by his supervisor Heinrich Dreser to acetylate morphine with the objective of producing codeine, a natural derivative of the opium poppy, similar to morphine but less 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".[6]
From 1898 through to 1910 heroin was marketed 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 quicker acting form of morphine. The company was somewhat embarrassed by this new finding and it became a historical blunder for Bayer.[7]
As with aspirin, Bayer lost some of its trademark rights to heroin following the German defeat in World War I. [8]
In the United States the Harrison Narcotics Tax Act was passed in 1914 to control the sale and distribution of heroin. The law did allow 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 thus illegal there.
[edit] Usage and effects
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Indicated for:
Recreational uses:
Other uses:
|
Contraindications:
|
| Side effects[citation needed] Severe:[2]
Central nervous system:
Cardiovascular & Respiratory:
Eyes, Ears, nose, and mouth:
Gastrointestinal:
Urinary System:
Musculoskeletal:
Neurological:
Psychological:
Skin:
Diamorphine ampoules for medicinal use |
Heroin is used as a recreational drug for its intense euphoria, which often fades with increased tolerance. It is believed that heroin's popularity with recreational users, compared to morphine or other opiates, comes from its somewhat different perceived effects.[9] 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 comparable action courses. There was no difference found in their ability to produce feelings of "euphoria," ambition, nervousness, relaxation, drowsiness, or sleepiness.[10] Data acquired during short-term addiction studies did not support the statement that tolerance develops more rapidly to heroin than to morphine. These findings 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 produce feelings of "euphoria", and other subjective effects when compared to most other opioid analgesics.[11][12] 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 mix 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 intense rush than heroin alone but is more dangerous because the combination of the short-acting stimulant with the longer-acting depressant increases the risk of overdosing on one or both drugs.
Once in the brain, heroin is rapidly metabolized into morphine by removal of the acetyl groups, therefore, 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 method of administration. Taken orally, heroin is totally 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 creates a dependence on the heroin, and the cessation of heroin results in extremely uncomfortable symptoms including pain (even in the absence of physical trauma). This set of symptoms is called withdrawal syndrome. It has an onset 6 to 8 hours after the last dose 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). Dealers can also supply unwanted customers with unusually pure heroin, or heroin cut with other dangerous drugs such as fentanyl, resulting in a fatal overdose. 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. [13]
[edit] 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.
In Australia heroin is not available for therapeutic purposes.
[edit] Production and trafficking
[edit] Manufacturing
Heroin is produced for the black market through processes of opium refinement. While the production of drugs like LSD requires considerable expertise in chemistry and access to constituents which are now tightly controlled, the refinement of the first three grades of heroin from opium is a relatively simple process requiring only moderate technical expertise and common chemicals. The final grade of heroin favored in the West is more difficult to produce and involves a potentially dangerous chemical procedure.
First, morphine is isolated from crude opium by being dissolved in water, reacted with lime fertilizer such that the morphine precipitates out, and then reacted again with ammonia. What remains is then mechanically filtered to yield a final product of morphine weighing about 90% less than the original quantity of opium. The morphine is reacted with acetic anhydride — a chemical also used in the production of aspirin — in a five-step process used by most refineries in the Golden Triangle. The first step is to cook the morphine at 85 °C (185 °F) for six hours with an equivalent weight of acetic anhydride. In the second, a treatment of water and hydrochloric acid then purifies the product moderately. When the chemists add sodium carbonate, the particulates settle. Step four involves heating the heroin in a mixture of alcohol and activated charcoal until the alcohol evaporates. The fifth step is optional, as it only changes the heroin into a finer white powder, more easily injectable; this so-called "no. 4 heroin" is principally exported to the Western markets. In this last, most dangerous step, the heroin (after being dissolved in alcohol), precipitates out in tiny white flakes when a mixture of ether and hydrochloric acid is injected; this step is dangerous because the ether may explode, leveling or severely damaging the refinery (as has happened to a number of such facilities).
The purity of the extracted morphine determines in large part the quality of the resulting heroin.
Heroin is also rarely made from codeine by first demethylating with pyridine followed by acetylation with acetic anhydride. The resulting product is an impure mixture of heroin and monoacetylmorphine known as Home Bake.
[edit] History of heroin traffic
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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[citation needed] 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[citation needed], but in the late 1960s, under pressure from the U.S. and the United Nations, Iran[citation needed] engaged in anti-opium policies. While opium production never ended in Iran[citation needed], 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[citation needed] to reduce production in their respective countries. Lebanon, a traditional opium supplier, also increased its role in the trade during years of civil war.[citation needed]
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. [citation needed]
[edit] Dr. Alfred W. McCoy's account of the history of the heroin trade
Although it was beginning to become more prevalent by the 1930s, Asian historian and drug traffic expert Dr. Alfred W. McCoy reports that heroin trafficking was virtually eliminated in the U.S. during World War II due to temporary trade disruptions caused by the war. McCoy contends the Mafia was able to gain control of the heroin trade thanks in large measure due to the unintended consequences of a covert deal between top Mafia leader Lucky Luciano and American military intelligence. The deal resulted in a large increase in Mafia influence in Sicily after the 1943 American invasion. [citation needed]
In southeast Asia, the governments of most countries and many colonial officials had been involved in the opium trade for a very long time. Thanks to Corsican Mafia connections in the former French colony of Vietnam, Luciano was able to begin to develop South-east Asia as a new source of Opium. The Vietnam War and CIA operations in Laos had the unintended consequence of first opening up many areas of South-east Asia to modern transportation and then presenting a ready-made market for the drug among the U.S. military personnel stationed in the region. [citation needed]
The major turning point came in 1970-71 when the first high-grade heroin laboratories opened in the Golden Triangle. Prior to this, the chemical skills for refinement had existed only in Europe. This gave the opium producers control over the creation of the final product. The hundreds of thousands of American servicemen in Vietnam provided a perfect market for the heroin producers, and heroin use among soldiers rapidly increased. In 1971 the first large consignments of South East Asian heroin were intercepted in Europe and America, and by the mid-1970s heroin addiction fulfilled its promise as a serious social problem in the United States, Australia, the United Kingdom, and many other nations.[citation needed]
[edit] Trafficking
- See also: Opium production
Traffic is heavy worldwide, with the biggest producer being Afghanistan.[14] According to U.N. sponsored survey,[15] as of 2004, Afghanistan accounted for production of 87 percent of the world's heroin.[16] 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.[17]
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[citation needed]. 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[citation needed]. 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.[citation needed]
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.
[edit] Risks of non-medical use
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- For intravenous users of heroin (and any other substance), the use of non-sterile needles and syringes and other related equipment leads to the risk of contracting blood-borne pathogens such as HIV and hepatitis, as well as the risk of contracting bacterial or fungal endocarditis and possibly venous sclerosis.
- Poisoning from contaminants added to "cut" or dilute heroin
- Chronic constipation
- Addiction and constantly growing tolerance. Like all opiates and opioids, long term use can lead to physical addiction.
- Decreased kidney function. (although it is not currently known if this is due to adulterants used in the cut)[18][19][20][21][22]
Many countries and local governments have begun funding programs that supply sterile needles to people who inject illegal drugs in an attempt to reduce these contingent risks and especially the contraction and spread of blood-borne diseases. The Drug Policy Alliance reports that up to 75% of new AIDS cases among women and children are directly or indirectly a consequence of drug use by injection. But despite the immediate public health benefit of needle exchanges, some see such programs as tacit acceptance of illicit drug use. The United States federal government does not operate needle exchanges, although some state and local governments do support needle exchange programs. Needle exchanges have been instrumental in arresting the spread of HIV/AIDS in many communities with a significant heroin using population,[citation needed] Australia being a leader due to its early inception of needle exchanges. Needle exchange programs have also been attributed to saving the public significant amounts of tax money by preventing medical costs which would have been required otherwise for the treatment of diseases spread through the practice of sharing and reusing needles.
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.[23]
The LD50 for a physically addicted person is prohibitively high,[citation needed] 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.[citation needed] Even for a non-user, the LD50 can be placed above 350 mg[citation needed] though some sources give a figure of between 75 and 375 mg for a 75 kg person.[24]
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 overdose could 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.[3]
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 overdose.[4]
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.
[edit] Harm reduction approaches to heroin
Proponents of the harm reduction philosophy seek to minimize the harms that arise from the recreational use of heroin. Safer means of taking the drug, such as smoking or nasal, oral and rectal insertion, are encouraged, due to the higher risks of overdose, infections and blood-borne viruses associated with drug injection. Where the strength of the drug is unknown, users are encouraged to try a small amount first to gauge the strength, to minimize the risks of overdose. For the same reason, poly drug use (the use of two or more drugs at the same time) is discouraged. Users are also encouraged to not use heroin on their own, as others can assist in the event of an overdose. Heroin users who choose to inject should always use new needles, syringes, spoons/steri-cups and filters every time they inject and not share these with other users. Governments that support a harm reduction approach often supply new needles and syringes on a confidential basis, as well as education on proper filtering prior to injection, safer injection techniques, safe disposal of used injecting gear and other equipment used when preparing heroin for injection may also be supplied including citric acid sachets/vitamin C sachets, steri-cups, filters, alcohol pre-injection swabs, sterile water ampules and tourniquets (to stop use of shoe laces or belts).
[edit] Withdrawal
The 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, pandiculation and lacrimation, 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.[25][26] 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). Users taking the "cold turkey" approach (withdrawal without using symptom-reducing or counteractive drugs), or induced withdrawal with opiate antagonist drugs, are more likely to experience the negative effects of withdrawal in a more pronounced manner.
Two general approaches are available to ease the physical part of opioid withdrawal. The first is to substitute a longer-acting opioid such as methadone or buprenorphine for heroin or another short-acting opioid and then slowly taper the dose.
In the second approach, benzodiazepines such as diazepam (Valium) may temporarily ease the often extreme anxiety of opioid withdrawal. The most common benzodiazepine employed as part of the detox protocol in these situations is oxazepam (Serax). Benzodiazepine use must be prescribed with care because benzodiazepines have an addiction potential, and many opioid users also use other central nervous system depressants, especially alcohol. Also, though unpleasant, opioid withdrawal seldom has the potential to be fatal, whereas complications related to withdrawal from benzodiazepines, barbiturates and alcohol (such as epileptic seizures, cardiac arrest, and delirium tremens) can prove hazardous and are potentially fatal.
Many symptoms of opioid withdrawal are due to rebound hyperactivity of the sympathetic nervous system, which can be suppressed with clonidine (Catapres), a centrally-acting alpha-2 agonist primarily used to treat hypertension. Another drug sometimes used to relieve the "restless legs" symptom of withdrawal is baclofen, a muscle relaxant. Diarrhea can likewise be treated symptomatically with the peripherally active opioid drug loperamide.
Buprenorphine is one of the substances most recently licensed for the substitution of opioids in the treatment of users. Being a partial opioid agonist/antagonist, it develops a lower grade of tolerance than heroin or methadone due to the so-called ceiling effect. It also has less severe withdrawal symptoms than heroin when discontinued abruptly, which should never be done without proper medical supervision. It is usually administered every 24-48 hrs. Buprenorphine is a kappa-opioid receptor antagonist. This gives the drug an anti-depressant effect, increasing physical and intellectual activity. [citation needed] Buprenorphine also acts as a partial agonist at the same μ-receptor where opioids like heroin exhibit their action. Due to its effects on this receptor, all patients whose tolerance is above a certain level are unable to obtain any "high" from other opioids during buprenorphine treatment except for very high doses.
Researchers at Johns Hopkins University have been testing a sustained-release "depot" form of buprenorphine that can relieve cravings and withdrawal symptoms for up to six weeks.[27] A sustained-release formulation would allow for easier administration and adherence to treatment, and reduce the risk of diversion or misuse.
Methadone is another μ-opioid agonist most often used to substitute for heroin in treatment for heroin addiction. Compared to heroin, methadone is well (but slowly) absorbed by the gastrointestinal tract and has a much longer duration of action of approximately 24 hours. Thus methadone maintenance avoids the rapid cycling between intoxication and withdrawal associated with heroin addiction. In this way, methadone has shown some success as a "less harmful substitute"; despite bearing about the same addiction potential as heroin, it is recommended for those who have repeatedly failed to complete withdrawal or have recently relapsed. As of 2005, the μ-opioid agonist buprenorphine is also being used to manage heroin addiction, being a superior, though still imperfect and not yet widely known alternative to methadone. Methadone, since it is longer-acting, produces withdrawal symptoms that appear later than with heroin, but usually last considerably longer and can in some cases be more intense. Methadone withdrawal symptoms can potentially persist for over a month, compared to heroin where significant physical symptoms would subside in 4 days.
Three opioid antagonists are known: naloxone and the longer-acting naltrexone and nalmefene. These medications block the effects of heroin, as well as the other opioids at the receptor site. Recent studies have suggested that the addition of naltrexone may improve the success rate in treatment programs when combined with the traditional therapy. [citation needed]
The University of Chicago undertook preliminary development of a heroin vaccine in monkeys during the 1970s, but it was abandoned. There were two main reasons for this. Firstly, when immunized monkeys had an increase in dose of x16, their antibodies became saturated and the monkey had the same effect from heroin as non-immunized monkeys. Secondly, until they reached the x16 point immunized monkeys would substitute other drugs to get a heroin-like effect. These factors suggested that immunized human users would simply either take massive quantities of heroin, or switch to other drugs, which is known as cross-tolerance.
There is also a controversial treatment for heroin addiction based on a Iboga-derived African drug, ibogaine. Many people travel abroad for ibogaine treatments that generally interrupt substance use disorders for 3-6 months or more in up to 80% of patients.[28] Relapse may occur when the person returns home to their normal environment however, where drug seeking behavior may return in response to social and environmental cues.[citation needed] Ibogaine treatments are carried out in several countries including Mexico and Canada as well as, in South and Central America and Europe. Opioid withdrawal therapy is the most common use of ibogaine. Some patients find ibogaine therapy more effective when it is given several times over the course of a few months or years. A synthetic derivative of ibogaine, 18-methoxycoronaridine was specifically designed to overcome cardiac and neurotoxic effects seen in some ibogaine research but, the drug has not yet found its way into clinical research..
[edit] Heroin prescription
The UK Department of Health's Rolleston Committee report in 1926 established the British approach to heroin prescription to users, which was maintained for the next forty years: dealers were prosecuted, but doctors could prescribe heroin to users when withdrawing from it would cause harm or severe distress to the patient. This "policing and prescribing" policy effectively controlled the perceived heroin problem in the UK until the 1960s. Attitudes eventually began to change, however: in 1964 only specialized clinics and selected approved doctors were allowed to prescribe heroin to users. Eventually, from the 1970s, the emphasis shifted to abstinence and the prescription of methadone, until now only a small number of users in the UK are prescribed heroin.[29]
In 1994 Switzerland began a trial program featuring a heroin prescription for users not well suited for withdrawal programs—e.g. those that had failed multiple withdrawal programs. The aim is maintaining the health of the user in order to avoid medical problems stemming from low-quality street heroin. Reducing drug-related crime was another goal. Users can more easily get or maintain a paid job through the program as well. The first trial in 1994 began with 340 users and it was later expanded to 1000 after medical and social studies suggested its continuation. Participants are prescribed to inject heroin in specially designed pharmacies for about US $13 per dose.[30]
The success of the Swiss trials led German, Dutch,[31] and Canadian[32] cities to try out their own heroin prescription programs.[33] Some Australian cities (such as Sydney) have trialed legal heroin injecting rooms, in line with other wider harm minimization programs. Heroin is unavailable on prescription however, and remains illegal outside the injecting room, and effectively decriminalized inside of the injecting room. [citation needed]
[edit] 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.[34]
[edit] Culture
Heroin has inspired countless writers, musicians and other artists over the past century of use. However, its influence is often misunderstood or unfairly assumed; many creative people have used or been addicted to heroin, but the extent to which the drug affected their creativity is debatable. Relatively few artists with great talent have credited heroin use with major epiphanies. The 1996 Danny Boyle film Trainspotting, based on the book by Irvine Welsh, depicts heroin users in the areas around Edinburgh in Scotland. Other movies that deal with heroin users include the 1955 Frank Sinatra film The Man with the Golden Arm; the 1971 Al Pacino film, Panic in Needle Park; the 2000 film Requiem for a Dream; More; and the 1998 television movie Gia starring Angelina Jolie about drug-addicted supermodel Gia Carangi.