A typical dose is 100 mg at street level purity. Heroin from south-east Asia is suitable for direct injection of a solution. Those intending to inject this form of heroin must first solubilise it with, for example, citric acid or ascorbic acid.
Heroin from south-west Asia may be ‘smoked’ by heating the solid on a metal foil above a small flame and inhaling the vapour. As with other naturally occurring drugs of misuse, total synthesis of the active principles is not currently an economic proposition. The corresponding EU legislation is set out in Council Regulation (EEC) No 3677/90 (as later amended), which governs trade between the EU and third countries. Acetic anhydride, an essential precursor in the manufacture of heroin, is listed in Table I of the United Nations 1988 Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances. Heroin is also produced in certain parts of South America, but that material is rarely seen in Europe. Until the late 1970s, nearly all heroin consumed in Europe came from south-east Asia, but now most originates from south-west Asia, an area centred on Afghanistan and Pakistan. Depending on the region, this may be used directly, further purified or converted into the hydrochloride salt. Sodium carbonate is added, causing the crude diamorphine base to separate. The separated morphine is boiled with acetic anhydride. The alkalinity is adjusted by adding ammonium chloride, causing morphine base to precipitate. This material ( opium) is dispersed in an aqueous solution of calcium hydroxide (slaked lime). The latex from the seed capsules of the opium poppy ( Papaver somniferum L.) is allowed to dry. Much morbidity is caused by infectious agents transmitted by unhygienic injection. Diamorphine is associated with far more accidental overdoses and fatal poisonings than any other scheduled substance. Morphine is excreted in the urine largely as the glucuronide conjugate. The plasma half-life of diamorphine is about three minutes. It is difficult to detect in blood because of rapid hydrolysis to 6-monoacetylmorphine and slower conversion to morphine, the main active metabolite. Following injection, diamorphine crosses the blood–brain barrier within 20 seconds, with almost 70 % of the dose reaching the brain. The estimated minimum lethal dose is 200 mg, but addicts may be able to tolerate ten times as much.
Diamorphine is 2–3 times more potent than morphine. Subjective effects following injection are known as ‘the rush’ and are associated with feelings of warmth and pleasure, followed by a longer period of sedation. Cessation of use in tolerant subjects leads to characteristic withdrawal symptoms. Tolerance and physical dependence occur on repeated use. Negative effects include respiratory depression, nausea and vomiting, decreased motility in the gastrointestinal tract, suppression of the cough reflex and hypothermia. Apart from analgesia, diamorphine produces drowsiness, euphoria and a sense of detachment. It behaves as an agonist at a complex group of receptors (the μ, κ and δ subtypes) that are normally acted upon by endogenous peptides known as endorphins. The less common south-east Asian heroin is usually a white powder in the form of the hydrate hydrochloride salt ( CAS-), which is soluble in water but insoluble in organic solvents.ĭiamorphine, like morphine and many other opioids, produces analgesia.
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South-west Asian heroin is a brown powder usually in the form of the free base, which is insoluble in water but soluble in organic solvents. (1) Diacetylmorphine: the principal psychoactive constituent of heroin Although five pairs of enantiomers are theoretically possible in morphine, only one occurs naturally (5 R, 6 S, 9 R, 13 S, 14 R). The systematic name ( IUPAC) is (5α,6α)-7,8-didehydro-4,5-epoxy-17-methylmorphinan-3,6-diol acetate. Chemistry Molecular structure (1)ĭiamorphine (diacetylmorphine CAS-561-27-3) is produced by the acetylation of crude morphine. Whereas opium has been smoked since historical times, diamorphine was first synthesised in the late nineteenth century.
Illicit heroin may be smoked or solubilised with a weak acid and injected. Diamorphine is a narcotic analgesic used in the treatment of severe pain. It is a semisynthetic product obtained by acetylation of morphine, which occurs as a natural product in opium: the dried latex of certain poppy species (e.g. Heroin is a crude preparation of diamorphine.
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