Narcotics, or opioids, are primarily used for pain management, but due to ease of availability individuals procure and misuse these drugs, with dire consequences including opioid use disorder and overdose. Nearly 4 million individuals in the United States are current misusers of pain relievers, and globally opioid misuse causes the greatest global burden of morbidity and mortality; disease transmission; increased health care, crime, and law enforcement costs; and less tangible costs of family distress and lost productivity.
Opioids bind to specific opioid receptors in the CNS and elsewhere in the body. These receptors mediate the opiate effects of analgesia, euphoria, respiratory depression, and constipation. Endogenous opiate peptides (enkephalins and endorphins) are natural ligands for the opioid receptors and play a role in analgesia, memory, learning, reward, mood regulation, and stress tolerance.
The prototypic opiates, morphine and codeine, are derived from the juice of the opium poppy. The semisynthetic drugs produced from morphine include hydromorphone (Dilaudid), diacetylmorphine (heroin), and oxycodone (Oxy-Contin). The purely synthetic opioids and their cousins include meperidine, propoxyphene, diphenoxylate, fentanyl, buprenorphine, tramadol, methadone, and pentazocine. All produce analgesia and euphoria as well as physical dependence when taken in high enough doses for prolonged periods of time.
The diagnosis of opioid use disorder as defined in the Diagnostic and Statistical Manual of Mental Disorders, Fifth Edition (DSM-5) requires the repeated use of the opiate while producing problems in two or more areas in a 12-month period. The areas include tolerance, withdrawal, use of greater amounts of opioids than intended, craving, and use despite adverse consequences. A striking recent aspect of illicit opioid use has been its marked increase as the gateway to illicit drugs in the United States. Since 2007, prescription opiates have surpassed marijuana as the most common illicit drug that adolescents initially use, although overall rates of opioid use are far lower than marijuana. The most commonly used opioids are diverted prescriptions for oxycodone and hydrocodone, followed by heroin and morphine, and—among health professionals—meperidine and fentanyl.
All opiates have the following CNS effects: sedation, euphoria, decreased pain perception, decreased respiratory drive, and vomiting. In larger doses, markedly decreased respirations, bradycardia, pupillary miosis, stupor, and coma ensue. Additionally, the adulterants used to “cut” street drugs (quinine, phenacetin, strychnine, antipyrine, caffeine, powdered milk) can produce permanent neurologic damage, including peripheral neuropathy, amblyopia, myelopathy, and leukoencephalopathy; adulterants can also produce an “allergic-like” reaction characterized by decreased alertness, frothy pulmonary edema, and an elevation in blood eosinophil count.
Tolerance and withdrawal commonly occur with chronic daily use after 6–8 weeks depending on the dose and frequency; the ever-increasing amounts of drug needed to sustain euphoriant effects and avoid discomfort of withdrawal strongly reinforce dependence once started.