Hosztafi S
Acta Pharm Hung. 2001 Oct;71(3):373-83.
Heroin is prepared by treating morphine with acetyl chloride or acetic anhydride. It is a simple reaction and the yields are generally quantitative. Nowadays the whole process is illegal. Morphine is the major alkaloid present in the opium poppy. Opium is manufactured illicitly then morphine is extracted from it in clandestine laboratories. Numerous studies were carried out on heroin to investigate its rate of hydrolysis. It has been shown that heroin is rapidly deacylated in aqueous solution at alkaline or acidic pH to form 6-acethylmorphine and finally, to morphine. Heroin also rapidly decomposes in biological medium yielding first 6-acetylmorphine and then morphine. Hydrolysis can be performed in blood and in tissue homogenates. Heroin can be administered by several routes. Smoking and intravenous administration are preferred, but intranasal, intramuscular and subcutaneous administration are also common. Recently, there has been a shift in heroin use patterns from injection to sniffing and smoking. Sharing of the injection equipment can result in several severe infectious diseases, such as AIDS, hepatitis B and C. Soon after administration, heroin metabolizes to 6-acetylmorphine and morphine. Most of the pharmacological activities of heroin are due to these active metabolites. Therefore, knowledge of distribution of 6-acetylmorphine and morphine is essential to understand pharmacological properties of heroin. Heroin, which is relatively nonpolar compound compared with morphine, has high lipid solubility facilitating rapid absorption from the bloodstream and passage through the blood-brain barrier. When heroin is administered by intravenously the drug takes 10 s to reach the brain i.e. pharmacological effects appear quickly.
海洛因是通过用乙酰氯或乙酸酐处理吗啡制备而成的。这是一个简单的反应，产率通常很高。如今整个过程都是非法的。吗啡是罂粟中存在的主要生物碱。鸦片是非法制造的，然后在秘密实验室中从鸦片中提取吗啡。人们对海洛因进行了大量研究以调查其水解速率。结果表明，海洛因在碱性或酸性pH的水溶液中会迅速脱酰基形成6 - 乙酰吗啡，最终形成吗啡。海洛因在生物介质中也会迅速分解，首先产生6 - 乙酰吗啡，然后是吗啡。水解可在血液和组织匀浆中进行。海洛因有几种给药途径。吸烟和静脉注射是首选方式，但鼻内、肌肉内和皮下注射也很常见。最近，海洛因的使用模式已从注射转向吸食和吸烟。共用注射设备可能导致几种严重的传染病，如艾滋病、乙型和丙型肝炎。给药后不久，海洛因代谢为6 - 乙酰吗啡和吗啡。海洛因的大多数药理活性归因于这些活性代谢物。因此，了解6 - 乙酰吗啡和吗啡的分布对于理解海洛因的药理特性至关重要。与吗啡相比，海洛因是一种相对非极性的化合物，具有高脂质溶解度，便于从血液中快速吸收并穿过血脑屏障。当通过静脉注射海洛因时，药物在10秒内即可到达大脑，即药理作用很快显现。
