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Heroin, also known as diacetylmorphine, is derived from the opium poppy plant.
Professionals initially touted morphine as a substitute with less misuse potential. Heroin currently has no FDA-approved indications for use. Though people in other countries use heroin, in the United States, it has no recognized therapeutic role in managing opioid use disorder. This activity outlines the indications, mechanism of action, pharmacodynamics, ificant adverse effects, and toxicity of heroin and increases the knowledge of practitioners regarding how to approach this substance should they encounter patients who use it in their practice.
Objectives: Explain the mechanism of action of heroin. Identify the original indications of heroin before it was made illegal in the USA. Review the adverse effects and toxicity of heroin. Outline interprofessional team strategies for improving care coordination and communication to advance improved outcomes when encountering a patient with heroin use disorder, and how to Can heroin be taken orally collaboratively to guide them to a positive outcome.
Heroin's chief place in American healthcare remains problematic. As an illicit opioid, people have misused heroin for decades. Heroin is synthetically derived from the morphine alkaloid in opium and is approximately twice as potent as morphine. Heroin acts agonistically on central nervous system CNS opioid receptors mu, kappa, and delta. Kappa receptor activation causes some degree of analgesia as well. Heroin metabolizes in the CNS to monoacetylmorphine, which is a more potent mu-receptor agonist than morphine. When taken orally, heroin undergoes first-pass metabolism to morphine via deacetylation.
Therefore, unlike intravenous administration, oral ingestion does not cause a rapid onset of effects and is less desirable to users. As mentioned above, practitioners in the United States do not administer heroin in any sanctioned healthcare setting. Illicitly, people misuse heroin via subcutaneous, intranasal, intramuscular, intravenous methods. Heroin is highly lipophilic and, therefore, rapidly crosses the blood-brain barrier.
Peak serum levels in each of these routes are as follows: five to ten minutes subcutaneously, three to five minutes intranasally and intramuscularly, and less than one minute intravenously. Once absorbed into the serum, heroin reaches the brain in 15 to 20 seconds.
This rapid effect gives the user a rush that typically le to continued use with hopes of achieving that same first experience of euphoria. The intended effects of heroin misuse are those classically associated with any opioid effects. These are analgesia, euphoria, and often alleviation of opioid withdrawal symptoms.
All other effects of heroin could be considered adverse. Respiratory depression is likely the most concerning adverse effect, leading to death in an increasing of misusers. The extreme physiologic dependence also represents a major concern in those who misuse heroin. Heroin reliably causes decreased GI motility, which commonly le to constipation.
Miosis represents a minimal concern to healthcare providers or those abusing the drug, though this effect can have diagnostic value. Some practitioners have described severe, life-threatening pulmonary edema Can heroin be taken orally patients who misuse or overdose on heroin. Practitioners have also attributed cases of compartment syndrome to heroin use. Because the FDA recognizes no medical use for heroin, it has not specified any contraindications. In countries where people use the drug for medicinal purposes, hypersensitivity, and potential for misuse or dependence could be perceived contraindications.
Again, with no approved use for heroin, no therapeutic index exists. However, pharmacodynamically, heroin could be considered to have a very narrow therapeutic window. Due to variations in potency and concentration, users are not aware of the actual amount of the active drug in any given sample .
Therefore the same apparent dose that causes euphoria one day could very well lead to an overdose the next. Drug levels are not typically useful, though toxicology assessments post-mortem may quantify several metabolites.
Professionals thoroughly describe heroin toxicity in the literature and popular media. With the high rate of prescription opioid addiction see opioid use disorderand the lower cost of heroin, many individuals have developed heroin dependence. From throughheroin overdoses went from 0. The many infectious and economic effects of heroin dependence add to the risk of death.
The antidote for heroin overdose or poisoning is naloxone. Naloxone binds with high affinity to the Mu receptors in the CNS . Administration of naloxone is an inverse agonist and, if given in high enough dose, will induce withdrawal in an opioid-dependent patient. Practitioners can administer naloxone intravenously, intramuscularly, and increasingly intranasally. Many first responders now carry intranasal naloxone kits to reverse heroin or opioid overdose in field settings.
Naltrexone, a long-acting opioid antagonist, is available both orally and as a long-acting intramuscular injection. The risk of precipitating a prolonged withdrawal syndrome, however, prohibits the use as an antidote for initial reversal. Medication-assisted treatment represents an effective option for the treatment of heroin dependence and opioid use disorder in general. Buprenorphine and methadone are the chief agents used, with buprenorphine being more safe and effective.
Buprenorphine also has a higher affinity for the mu-opioid receptors than does heroin. Sneader W, The discovery of heroin. Lancet London, England. Addictive behaviors. European addiction research. JAMA psychiatry. The societal cost of heroin use disorder in the United States. Goldstein A, Heroin addiction: neurobiology, pharmacology, and policy.
Journal of psychoactive drugs. Drug testing and analysis. Dinis-Oliveira RJ, Metabolism and metabolomics of opiates: A long way of forensic implications to unravel. Journal of forensic and legal medicine.
Forensic toxicology. Advances in pharmacology San Diego, Calif.
The New England journal of medicine. The American surgeon. It's not just heroin anymore. The Journal of emergency medicine. NCHS data brief. Skolnick P, On the front lines of the opioid epidemic: Rescue by naloxone. European journal of pharmacology. Clinical toxicology Philadelphia, Pa.
Journal of general internal medicine. Continuing Education Activity Heroin, also known as diacetylmorphine, is derived from the opium poppy plant. Indications Heroin, also known as diacetylmorphine, is derived from the opium poppy plant. Mechanism of Action Heroin is synthetically derived from the morphine alkaloid in opium and is approximately twice as potent as morphine.
Monitoring Again, with no approved use for heroin, no therapeutic index exists. Enhancing Healthcare Team Outcomes Medication-assisted treatment represents an effective option for the treatment of heroin dependence and opioid use disorder in general. Feedback: Send Us Your Comments.Can heroin be taken orally
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Oral diacetylmorphine (heroin) yields greater morphine bioavailability than oral morphine: bioavailability related to dosage and prior opioid exposure