Cone Edward J
ConeChem Research, LLC, 441 Fairtree Drive, Severna Park, MD 21146, USA.
Drug Alcohol Depend. 2006 Jun;83 Suppl 1:S31-9. doi: 10.1016/j.drugalcdep.2005.11.027. Epub 2006 Feb 3.
The magnitude of non-therapeutic use, or misuse of prescription pharmaceuticals now rivals that of illicit drug abuse. Drug and formulation tampering enables misusers to administer higher doses by intended and non-intended routes. Perceived motives appear to be a combination of interests in achieving a faster onset and enhancing psychoactive effects. Narcotic analgesics, stimulants, and depressants are widely sought, examined, and tampered with for recreational use. This review examines tampering methods reported on the Internet for selected pharmaceutical products. The Internet provides broad and varied guidance on tampering methods that are specific to drug classes and unique formulations. Instructions are available on crushing, separating, purifying and chemically altering specific formulations to allow changes in dosage, route of administration, and time course of effects. Many pharmaceutical formulations contain features that serve as "barriers" to tampering. The nature and effectiveness of formulation barriers vary widely with many being overcome by adventurous misusers. Examples of successes and failures in tampering attempts are frequently described on Internet sites that support recreational drug use. Successful tampering methods that have widespread appeal evolve into recipes and become archived on multiple websites. Examples of tampering methods include: (1) how to separate narcotic drugs (codeine, hydrocodone, oxycodone) from excipients and non-desirable actives (aspirin, acetaminophen, ibuprofen); (2) overcoming time-release formulations (beads, layers, matrices); (3) removal of active drug from high-dose formulations (patches, pills); (4) alteration of dosage forms for alternate routes of administration. The development of successful formulations that inhibit or prevent drug/formulation tampering with drugs of abuse should take into consideration the scope and practice of tampering methods available to recreational drug users on the Internet.
目前，处方药物的非治疗性使用或滥用程度已与非法药物滥用相当。药物及制剂篡改使滥用者能够通过有意和无意的途径服用更高剂量的药物。其动机似乎是为了更快起效并增强精神活性效果。麻醉性镇痛药、兴奋剂和抑制剂被广泛寻找、检验并篡改以用于娱乐目的。本综述研究了互联网上报道的针对特定药品的篡改方法。互联网提供了针对特定药物类别和独特制剂的广泛多样的篡改方法指南。有关于碾碎、分离、提纯和化学改变特定制剂以改变剂量、给药途径和作用时间过程的说明。许多药物制剂具有作为篡改“屏障”的特性。制剂屏障的性质和有效性差异很大，许多都被大胆的滥用者克服了。支持娱乐性药物使用的网站经常描述篡改尝试的成功与失败案例。具有广泛吸引力的成功篡改方法演变成配方并在多个网站存档。篡改方法的例子包括：（1）如何从辅料和不需要的活性成分（阿司匹林、对乙酰氨基酚、布洛芬）中分离出麻醉药物（可待因、氢可酮、羟考酮）；（2）克服缓释制剂（小丸、多层、基质）；（3）从高剂量制剂（贴片、药丸）中去除活性药物；（4）改变剂型以用于替代给药途径。开发能够抑制或防止对滥用药物进行药物/制剂篡改的成功制剂时，应考虑互联网上娱乐性药物使用者可用的篡改方法的范围和实践情况。
