![]() The antidote for heroin overdose or poisoning is naloxone. The many infectious and economic effects of heroin dependence add to the risk of death. State and federal legislation are implementing diverse methods to curb this epidemic of heroin overdose deaths. In 2013, roughly 517,000 people reported heroin use in the past year, 1.5 times the amount in 2007. From 2002 through 2013, heroin overdoses went from 0.7 deaths per 100,000 to 2.7. As discussed above, heroin (especially if administered intravenously) is likely to cause an overdose and death due to respiratory depression. With the high rate of prescription opioid addiction (see opioid use disorder) and the lower cost of heroin, many individuals have developed heroin dependence. Professionals thoroughly describe heroin toxicity in the literature and popular media. Practitioners have also attributed cases of compartment syndrome to heroin use. This edema is noncardiogenic and likely relates to increased pulmonary vascular permeability. Some practitioners have described severe, life-threatening pulmonary edema in patients who misuse or overdose on heroin. Miosis represents a minimal concern to healthcare providers or those abusing the drug, though this effect can have diagnostic value. This decreased motility can be problematic enough for users that they may require medical attention to relieve constipation. Heroin reliably causes decreased GI motility, which commonly leads to constipation. Extreme physiologic dependence also represents a major concern in those who misuse heroin. Respiratory depression is likely the most concerning adverse effect, leading to death in an increasing number of misusers. All other effects of heroin could be considered adverse. These are analgesia, euphoria, and often alleviation of opioid withdrawal symptoms. The intended effects of heroin misuse are those classically associated with any opioid effects. 6-monoacetylmorphine and morphine activate opioid receptors. Therefore, unlike intravenous administration, oral ingestion does not cause a rapid onset of effects and is less desirable to users. When taken orally, heroin undergoes first-pass metabolism to morphine via deacetylation. ![]() Many state toxicology labs use the 6-monoacetylmorphine to determine which overdose deaths were due to heroin. ![]() Peripheral tissues metabolize heroin to 6-monoacetylmorphine and then morphine. Heroin metabolizes in the CNS to monoacetylmorphine, which is a more potent mu-receptor agonist than morphine. Delta receptors are more involved in spinal analgesia phenomena. Kappa receptor activation causes some degree of analgesia as well. Activation of Mu2 receptors also causes miosis, reduced gastrointestinal (GI) motility, and physiologic dependence. Mu receptor effects account for both the analgesic effects (Mu1) and the respiratory depression and euphoria (Mu2). Heroin acts agonistically on the central nervous system (CNS) opioid receptors mu, kappa, and delta. Heroin is synthetically derived from the morphine alkaloid in opium and is approximately twice as potent as morphine. Though people in other countries use heroin, in the United States, it has no recognized therapeutic role in managing opioid addiction. In the 21st century, the use of heroin has caused a surge in both dependence and overdose deaths. As an illicit opioid, people have misused heroin for decades. Heroin's chief place in American healthcare remains problematic. The United Kingdom allows the use of heroin, known under the generic name of diamorphine, for diverse analgesic indications such as postoperative pain, chronic pain, palliative care, and even post-cesarean section. Heroin is a Schedule I drug under the Controlled Substances Act of 1970, with no approved medical use in the United States. Heroin currently has no FDA-approved indications for use. Professionals initially touted morphine as a substitute with less addiction potential. Bayer Pharmaceuticals developed the diacetylmorphine molecule in 1898 as an antitussive. Heroin, also known as diacetylmorphine, is derived from the opium poppy plant.
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