Eroin

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Eroin Eroin Sistematik (IUPAC) adı 4,5-epoksi-17-metilmorfinan-7-en-3,6-diildiasetat Kimlik belirteçleri CAS numarası  ? ATC kodu N02AA09 PubChem 3592 DrugBank  ? Kimyasal özellikler Kimyasal formül C21H23NO5 Moleküler ağırlık  ? Fiziksel özellikler Yoğunluk  ? Ergime noktası  ? Kaynama noktası  ? Çözünürlük (suda)  ? Farmakokinetik özellikler Biyoyararlanım <35% Proteine bağlanma 0% (morphine metabolite 35%) Metabolizma karaciğer Yarılanma ömrü 2-3 dakika Atılma 90% böbrekten glukronidleri olarak, kalanı feçesle Tedavi bilgileri Gebelik kategorisi ABD -  Avustralya -  Kanada: Schedule I, İngiltere: Class A Yasal durum Uygulama yolu inhalasyon, transmukozal, intravenöz, oral, intranazal, rektal, intramüsküler

Eroin yani Diasetilmorfin (diamorfin) yarı-sentetik bir afyon alkaloidi türevidir. Morfinin 3,6-diasetil türevidir ve onun asetilasyonu ile sentezlenir. Beyaz ve kristalize olan formu genellikle hidroklorid tuzu olan diasetilmorfin hidrokloriddir. Endorfinleri taklit eder ve kan dolaşımına katıldığı andan itibaren bir iyilik hissi oluştururlar (genellikle intravenöz enjeksiyon). Tek seferlik kullanımda dahi çok yüksek bağımlılık potansiyeline sahiptir ve özellikle diğer maddelere oranla hızla tolarans gelişir. Buna rağmen nadiren kullanımı durumunda yoksunluk sendromu oluşmaz. Yalnızca üç gün süreyle kullanılıp bırakıldığında dahi yoksunluk sendromu görülür. Birleşik Devletler'de eroinin üretimi, taşınması ve satışı yasak olmasına rağmen; diamorphine adı altında , Birleşik Krallık'ta yasal bir reçete ilacıdır. ABD'de eroin için sıkça kullanılan sokak isimleri gear, diesel, smack, B, skag, Bobby, black tar heroin|black tar, horse, junk, jack, jenny, brown, brown sugar, dark, dope, dragon, bitch, gak, boy, veHdir.

Konu başlıkları 1 Tarihçe 2 Kullanım alanları ve etkileri 3 Üretim ve kaçakçılık 3.1 Üretim 3.2 Eroin kaçakçılığının tarihi 3.3 Dr. Alfred W. McCoy's account of the history of the heroin trade 3.4 Kaçakçılık 4 Tıp dışı kullanımının riskleri 5 Harm reduction approaches to heroin 6 Yoksunluk 7 Eroinin reçetelenmesi 8 İlaç etkileşimleri 9 Eroinin Kültür Üzerindeki Etkisi 10 Ayrıca bakınız 11 Bibliyografya 12 Kaynakça 13 Dış bağlantılar

[değiştir] Tarihçe

Afyon çiçeği aşağı Mezopotamyada M.Ö 3400 yılından beri yetiştirilmektedir..^[1] 19uncu yüzyılda afyonun kimyasal analizi gösterdi ki aktivitesi ,içeriğindeki kodein ve morfine bağlıdır.

Eroin ilk kez 1874 yılında Londra, İngilteredeki St Mary's Hastanesindeki Tıp Fakültesinde çalışan ingiliz kimyacı C.R. Alder Wright tarafından sentezlendi. O sıralar morfini çeşitli asitlerle kombine etmek üzerine deneyler yapıyordu. Morfin anhidr alkaloidini asetik anhidr ile bir fırında sattaler boyunca kaynattı ve morfinin daha etkili asetillenmiş türevi olan diasetil morfin böylece ortaya çıkmış oldu. Bu bileşen daha sonra Manchesterdaki Pierce of Owens Üniversitesi Tıp Fakültesine analiz için yollandı ve Wright'a gelen rapor şu şekilde idi:

Dozlar … genç köpek ve tavşanlara subkutan olarak enjekte edildiğinde … şu genel sonuçlar ile … müthiş bitkinlik , korku , ve uyku hali uygulamanın ardından hızla olmak üzere , hassaslaşan gözler , pupiller kontraksiyon , köpeklerde oluşan hatırı sayılır ölçüde tükrük salgılama oluştu , ve bazı vakalarda kusmaya hafif yatkınlık, ancak gerçekten kusma yok . Solunum başta hızlandı , ancak sonra yavaşladı , ve kalp hareketleri yavaşladı , ve normal dışı çalışmaya başladı.

Buna karşın , Wright'ın bu önemli bilimsel keşfi daha ileri aşamalara gidemedi ve eroin'in ünü 23 yıl sonra bir başka kimyacı olan Felix Hoffmann tarafından bağımsız olarak yeniden sentezlendiği zaman belirmeye başladı. Hoffmann Elberfeld, Almanyadaki Bayer farmasötik ürünler şirketinde çalışıyordu ve bulunduğu laboratuarın başında Heinrich Dreser vardı. Dreser Hoffmann'a afyon sakızının doğal türevi olan ve morfine benzeyen fakat ondan daha az bağımlılık yaratan kodeini elde etmek üzere morfini asetillemesini söyledi. Fakat Hoffmann kodein elde etmek yerine, deneyleri sonucunda morfinden üç kat daha kuvvetli olan başka bir madde elde etti. Bayer bu maddeyi "heroin" olarak adlandırdı (heroisch kelimesinden etkilenildiği düşünülmektedir, bu kelime almanca görkemli anlamına gelmektedir, eroinin denenmesi sürecinde denek olarak kullanılan insanlar kendilerini görkemli,cesur hissettiklerini belirtmişlerdir).^[2]

1898'den 1910 yılına kadar eroin bağımlılık yapmayan morfin ismiyle pazarlanmıştır, ayrıca çocuklar için öksürük ilacı olarak satılmıştır. Bayer eroini karaciğerde parçalanarak morfine dönüştürüldüğünü keşfetmeden önce morfine bağımlılık tedavisi için pazarlamıştır. Şirket için eroinin bu özelliğinin keşfi tarihi bir utanç kaynağı olmuştur.^[3]

Almanya'nın I. Dünya Savaşı'ndan yenik çıkması sonucu aspirin ve eroin gibi ürünlerinin tescil hakkını kaybetmiştir.

Amerika Birleşik Devletleri'nde 1914 yılında Harrison Narkotik Kontrol Yasası senato tarafından eroinin tüketim ve dağıtımını kontrol etmek amacıyla kabul edilmiştir.Yasa eroinin tıbbi sebeplerden dolayı reçetelendirilip satılmasına izin vermekteydi. Bu sayede, bağımlılar bazı yöntemlerle eroin elde etmeye devam edebilmekteydiler. Bunu engellemek için, 1924 yılında senato eroinin satışını, ithalatını ve üretimini tamamen yasakladı.

[değiştir] Kullanım alanları ve etkileri

Endikasyonları: Yüksek derecede ağrının kesilmesi Recreational uses: Öfori Rahatlama Diğer kullanım alanları: Ağrı Kesici Öksürük Bastırıcı Anti-Diyareik

Kontraendikasyonları: Alkol Barbituratlar ve Benzodiazepinler Stimulanlar Diğer opioidler (vücut toleransına göre değişkenlik gösterir)

Yan etkiler: Solunum durması, felç, koma, ölüm Spontan düşük Kardiyovasküler & Solunum: kalp atışında yavaşlama yavaşlamış solunum Gözler, Kulaklar, burun, ve ağız: Ağız kuruluğu Pupiller konstrüksiyon Gastrointestinal: Mide bulantısı Kusma Kabızlık Uriner Sistem: Üriner retansiyon Kasiskelet: Analjezi Ataksi Nörolojik: Analjezi Fiziksel bağımlılık Psikolojik: Anksiyoliz Konfüzyon Öfori Uyuklama Bağımlılık Cilt: Kaşıntı Döküntüler Tıbbi kullanım amaçlı diamorpin ampulleri

Eroin çoğunlukla artan fizyolojik tolerans ile zamanla yok olan yoğun öfori yapıcı özelliği için kullanılan (çoğunlukla) yasal olmayan bir maddedir. Eroinin popülaritesi kullanıcıların anlattıklarına göre bir şekilde diğer afyon alkaloidlerine göre kullanıcıda çok farklı hisler uyandırmasıdır. ^[4] Bu durum eroinin kullanımını takiben iki asetil grubu sayesinde yağdaki yüksek çözünürlüğü ve bu şekilde kan beyin bariyerini çok hızlı şekilde geçmesi ile meydana gelir. Eroin enfiye şeklinde veya enjeksiyon gibi çeşitli yollarla vücuda alınabilir.Ayrıca alttan ısıstarak çıkan buharı içine çekerek de kullanıldığı olur.

Birçok kullanıcı eroini kokainle birlikte eriterek bunu damar yoluyla alirlar .Ancak bu çok riskli bir kombinasyondur.Kokain vücüt dokularına iritandır ve sık temas ettiği dokulardanekroza bile yol açabilir .

Beyinde eroin asetil grupların ayrılmasıyla hızla morfine metabolize edilir. Opioid alıcılarıyla bileşen morfin molekülüdür. Eroin bu yüzden pro-drug(Prekürsör. Vücuda giren etkisiz bir bileşiğin bazen biyotransformasyon sonucu etkili duruma geçmesiyle oluşan aktif metabolit) olarak adlandırılır.

Eroin'in etkisini gösterme hızı, hangi yolla alındığına bağlı olarak değişir. Oral yoldan alındığında, kan-beyin bariyerini geçmeden önce, normal şartlarda tamamen morfine metabolize edildiğinden, etkileri oral yoldan alınan morfinin etkileriyle aynıdır. Burundan çekildiğinde etksisini 10-15 dakika içinde gösterir. Tütün ile birlikte kullanıldığında, neredeyse anında etki eder fakat daha düşük etkiler gösterir ve bu süreç normalden uzun sürer. Damar yoluyla alındığında, madde direk olarak kana karıştığından sadece 7-8 saniye içinde vücutta şiddetli uyuşukluk ve aşırı mutlu olma hali meydana gelirken, kas yoluyla 5-8 dakikada etkiler.

Heroin bir μ-opiattir. (mu-opioid) agonist. Hemen hemen bütün memelilerde beyindeki, omurilikteki ve karındaki düzenli bölümlere yayılarak işlevini görür. Eroin diğer opioidler,gibi vücudun dört endojen nörotransmiterlerine agonisttir. Bunlar β-endorphin, dynorphin, leu-enkephalin, and met-enkephalindir. Vücutta eroin olduğunda, beyin doğal endorfin üretimini azaltır, hatta bazen durdurabilir. Endorfinler genellikle beyinde ve sinir uçlarında görülür ve ağrı hissini azaltırlar. Diğer fonksiyonları hala tam olarak keşfedilememiş olmakla birlikte; eroinin, analjezi dahil olmak üzere hemen hemen tüm etkileriyle benzerliği olduğu bilinmektedir.(antitussin, anti-diarrheal) Düşük endorfin üretimi, eroin kullanıcılarında bağımlılığa sebebiyet verir ve eroin alımının durdurulması, fiziksel travma halinde değilken bile, ağrılı ve oldukça rahatsızlık verici semptomlara yol açar. Butun bu semptomlara genel olarak yokluk sendromu denilebilir. Bu semptomlar son eroin alımından 6-8 saat sonra hissedilmeye başlarlar.

Yüksek dozda Eroin ölümcül olabilir. Sigmund Freud bahsettiği gibi intiharlarda kullanılabilir. Eroin aynı zamanda bir cinayet aleti olarak da kullanılabilir. Seri katil Dr. Harold Shipman kurbanları üzerinde Eroin kullanmıştır. Dağıtıcılar aynı zamanda sevmedikleri müşterilerine alışılmadık şekilde saf eroin verirler, ya da bir başka uyuşturucu ile karıştırırarak verirler fentanyl, sonuç ölümcül dozaşımıdır. Zaman zaman bu tür ölümleri açıklığa kavuşturmak ölümün aşırı doz mu,intihar mı yoksa cinayet mi olduğunun bilinememesi nedeniyle son derece zordur. The death of Joseph Krecker was such a case. ^[5].

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 offence and liable to imprisonment for a term not exceeding seven years. Possession for purpose of trafficking is guilty of an indictable offence 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 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 on 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. Compared to morphine, it may cause less nausea, hypotension, but more sedation and euphoria and can be dissolved in a smaller quantity of liquid.

[değiştir] Üretim ve kaçakçılık

[değiştir] Üretim

Morfin üzerinden elde edilir. Morfin benzende çözünür ve asetanhidridi veya asetilklorür ile asetillendirilir. Daha çok asetanhidrit kullanılır. Bu nedenle asetanhidrit satımı kontrol altında tutulmaktadır. Diasetilmorfin kolaylıkla meydana gelir. Aseton veya etilmetilketondan kristallendirilerek saflaştırılır.

Eroin afyonun işlenmesiyle yasal olmayan ticarette kullanılmak üzere hazırlanır. Unlike drugs such as LSD, the production of which 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 favoured 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 the complicated 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, levelling 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. Most black market heroin is highly impure due to contaminants left after refinement of opium into morphine which then remain in the final product^{[kaynak belirtilmeli]}; even if the final product is in the upper range of purity (80–99% pure), once it reaches the consumer, it has typically been cut multiple times.

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.

[değiştir] Eroin kaçakçılığının tarihi

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.

After the overthrow of the Shah of Iran, the new Iranian regime was much more tolerant of opium production. At the same time, the Soviet-Afghan war led to increased production in the Pakistani-Afghani border regions. Both events led to 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.

[değiştir] 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. ^{[kaynak belirtilmeli]}

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 even as Iranian production declined. 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. ^{[kaynak belirtilmeli]}

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.^{[kaynak belirtilmeli]}

[değiştir] Kaçakçılık

Ayrıca bakınız: Afyon üretimi

Traffic is heavy worldwide, with the biggest producer being Afghanistan.^[6] According to U.N. sponsored survey,^[7] as of 2004, Afghanistan accounted for production of 87 percent of the world's heroin.^[8] 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.^[9]

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 heroin consumed in the United States comes from Mexico and Colombia^{[kaynak belirtilmeli]}. 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^{[kaynak belirtilmeli]}. 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.^{[kaynak belirtilmeli]}

Conviction for trafficking in heroin carries the death penalty in most South-east Asia and some East Asia, southern Asia and Middle East 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.

[değiştir] Tıp dışı kullanımının riskleri

• Overdose, heroin rarely causes death alone, most overdoses are due to multi-drug use (particularly alcohol and/or benzodiazepines)
• 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
• Heroin-induced toxic leukoencephalopathy (very rare, smokers only, probably due to a toxic byproduct of a cutting substance)
• Addiction and constantly growing tolerance. Like all opiates and opiods, long term use can lead to physical addiction. Because endorphin receptors increase in number under continuous stimulation, tolerance also increases quickly.

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 does not support needle exchanges federally by law, and although some state and local governments do support needle exchange programs, they continue to face harassment by police in most areas. Needle exchanges have been instrumental in arresting the spread of HIV/AIDS in many communities with a significant heroin using population^{[kaynak belirtilmeli]}, 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 dollars 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) or naltrexone, which have a high affinity for opioid receptors but do 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 these antagonists is usually much shorter than that of the opiate drugs they are 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.^[10]

The LD₅₀ for a person already addicted 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 addicts doses of 1,600–1,800 mg of heroin in one sitting, and no adverse effects were reported. This is approximately 160–180 times a normal recreational dose. Even for a non-addict, the LD₅₀ can be credibly placed above 350 mg.

Street heroin is of widely varying and unpredictable purity. This means that an addict may prepare what they consider to be a moderate dose while actually taking far more than intended. Also, relapsing addicts 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. [1]

A final source of overdose in addicts comes from place conditioning. Heroin use, like other drug abuse 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 addict has repeatedly injected heroin, imbues the addict with a strong (but temporary) tolerance to the toxic effects of the drug. When the addict injects in a different location, this place-conditioned tolerance does not occur, giving the addict 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.[2]

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.

[değiştir] 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 alone, as others can assist in the event of an overdose. Heroin users who choose to inject should always use new needles and syringes where possible, 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 and safe disposal of used injecting gear.

[değiştir] Yoksunluk

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, yawning and lacrimation, sleep difficulties, cold sweats, chills, severe muscle and bone aches not precipitated by any physical trauma; nausea and vomiting, diarrhea, goose bumps, cramps, and fever. In an addict with a high tolerance, heroin withdrawal may even lead to death, although debate amongst professionals continues about the likelihood of death being an end result of simple withdrawal. ^[11]. ^[12]. Many addicts 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) 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 a great addiction potential, and many opioid addicts also use other central nervous system depressants including barbiturates. 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.

Buprenorphine is one of the substances most recently licensed for the substitution of illegal opioids. 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. ^{[kaynak belirtilmeli]} Buprenorphine also acts as a partial agonist at the same μ-receptor where illicit 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.^[13] 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.

Two opioid antagonists are known: naloxone and the longer-acting naltrexone. These two medications block the effects of heroin, as well as the other opioids at the receptor site. Recent studies have suggested that the addition of naloxone and naltrexone may improve the success rate in treatment programs when combined with the traditional therapy. ^{[kaynak belirtilmeli]}

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 immunised monkeys had an increase in dose of x16, their antibodies became saturated and the monkey had the same effect from heroin as non-immunised monkeys. Secondly, until they reached the x16 point immunised monkeys would substitute other drugs to get a heroin-like effect. These factors suggested that immunised human addicts would simply either take massive quantities of heroin, or switch to other hard drugs, which is known as cross-tolerance.

There is also a controversial treatment for heroin addiction based on a plant-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.^{[kaynak belirtilmeli]} Relapse often occurs when the person returns home to their normal environment however, where drug seeking behaviour may return in response to social and environmental cues.^{[kaynak belirtilmeli]} 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..

[değiştir] Eroinin reçetelenmesi

The UK Department of Health's Rolleston Committee report in 1926 established the British approach to heroin prescription to addicts, which was maintained for the next forty years: dealers were prosecuted, but doctors could prescribe heroin to addicts when withdrawing it would cause harm or severe distress to the patient. This "policing and prescribing" policy effectively controlled the heroin problem in the UK until the 1960s. Attitudes eventually began to change, however: in 1964 only specialised clinics and selected approved doctors were allowed to prescribe heroin to addicts. Eventually, from the 1970s, the emphasis shifted to abstinence and the prescription of methadone, until now only a small number of addicts in the UK are prescribed heroin.^[14]

In 1994 Switzerland began a trial program featuring a heroin prescription for addicts not well suited for withdrawal programs—e.g. those that had failed multiple withdrawal programs. The aim is maintaining the health of the addict in order to avoid medical problems stemming from low-quality street heroin. Reducing drug-related crime was another goal. Addicts can more easily get or maintain a paid job through the program as well. The first trial in 1994 began with 340 addicts 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.^[15]

The success of the Swiss trials led German, Dutch,^[16] and Canadian^[17] cities to try out their own heroin prescription programs.^[18] Some Australian cities (such as Sydney) have trialed legal heroin injecting rooms, in line with other wider harm minimisation programs. Heroin is unavailable on prescription however, and remains illegal outside the injecting room, and effectively decriminalised inside of the injecting room. ^{[kaynak belirtilmeli]}

[değiştir] İlaç etkileşimleri

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 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 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.^[19]

[değiştir] Eroinin Kültür Üzerindeki Etkisi

Eroin geçtiğimiz yüzyılda çok sayıda yazara, müzisyene ve sanatçıya ilham kaynağı olmuştur. Eroinin etkisi bazılarınca yanlış anlaşılmıştır, çok sayıda ilham kaynağı olarak eroini kullanan insan ya eroin kullanmışlardır ya da kullanmaktadırlar ama eroinin hayal güçlerine etkisi tartışılabilir.

1996 yılı yapımı Danny Boyle filmi Trainspotting , Edinburgh, İskoçya'da yaşayan bir grup eroin bağımlısını irdelemektedir. İlk Al Pacino filmi ve More(daha çok) gibi filmlerde eroin konusuna eğilmektedirler.

Yıllar boyunca sayısız Rock müzik sanatçısı eroin üzerine şarkı yazmıştır. Kurt Cobain, Sid Vicious, Anthony Kiedis, Layne Staley, Bradley Nowell, John Frusciante ve Keith Richards eroin kullanan veya kullanmış ünlülerden bazılarıdır.

[değiştir] Ayrıca bakınız

• Morfin
• Afyon
• Haşhaş

[değiştir] Bibliyografya

• Heroin (1998) ISBN 1-56838-153-0
• Heroin Century (2002) ISBN 0-415-27899-6
• This is Heroin (2002) ISBN 1-86074-424-9
• The Heroin User's Handbook by Francis Moraes (paperback 2004) ISBN 1-55950-216-9
• The Little Book of Heroin by Francis Moraes (paperback 2000) ISBN 0-914171-98-4
• Heroin: A True Story of Addiction, Hope and Triumph by Julie O'Toole (paperback 2005) ISBN 1-905379-01-3

[değiştir] Kaynakça

[değiştir] Dış bağlantılar

• EMCDDA drugs profiles: heroin (2007)
• Geopium: Geopolitics of Illicit Drugs in Asia, especially opium and heroin production and trafficking in and around Afghanistan and Burma (Articles and maps and French and English)
• Drugs Factfile what you really need to know
• Heroin Helper
• From Flowers to Heroin, CIA publication.
• The mismanagement of methadone
• Harrowing Heroin by Geoff Morton
• National Alliance of Advocates for Buprenorphine Treatment - non-profit education website for treatment of Heroin addiction
• NIDA InfoFacts on Heroin
• ONDCP Drug Facts
• Role of Government of Pakistan in Narcotics Control
• United States Department of State fact sheet: anti-narcotics efforts in Pakistan - dated June 7, 2002
• BBC Article entitled 'When Heroin Was Legal'. References to the United Kingdom and the United States
• Heroin Facts
• Information on heroin and other illicit drugs
• Can poppy seeds make you test positive for heroin?
• Heroin news page - Alcohol and Drugs History Society
• Discussion forum about heroin and other opiates