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NCBI Bookshelf. Robert C. Oelhaf ; Mohammadreza Azadfard. Authors Robert C. Oelhaf 1 ; Mohammadreza Azadfard 2. Heroin, also known as diacetylmorphine, is a very efficient prodrug and more potent than morphine.
Many deaths are caused by heroin overdoses throughout the world each year. Heroin, which can be sniffed, smoked, or injected, is experiencing a rebound in usage, partially related to the efforts to reduce the abuse of prescription pain relievers. With increased usage, there has been a corresponding increase in overdose-related deaths.
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Heroin is one of the most commonly used drugs among those who misuse intravenous drugs. Objectives: Describe the basic pharmacology of heroin in the human body. Review the s and symptoms expected on examination and evaluation of a patient with suspected heroin toxicity. Outline the management options available for both acute heroin toxicity and long-term management following recovery from heroin toxicity.
Explain possible interprofessional heroin strategies for improving care coordination and communication to advance the evaluation and treatment of heroin toxicity and improve outcomes. Conventionally, chemical compounds that are fractionated from the juice of the opium poppy Papaver somniferum are known as opiates.
Similarly, acting synthetic chemical compounds are known as opioids. The predominant opiate How found in opium poppy juice. The juice of the opium poppy is harvested, which contains a variety of opiates, mostly morphine. Additional processing is necessary to refine the opium poppy liquid into heroin. Heroin is synthesized from morphine by acetylation at both 3 and 6 positions and metabolized in the human body to active opioid compounds first by deacetylation to 6 much acetyl morphine 6MAM then by further deacetylation to morphine.
Heroin is smaller per dose, making it the version of the product preferred by drug smugglers. Heroin is usually used as an illegal drug. In rare settings, heroin is prescribed by doctors for pain control. Heroin given intramuscularly is about two times as potent for pain relief.
Heroin is not allowed to be prescribed by doctors in the United States, but prescription heroin is available in rare settings in other countries. Heroin has an average half-life of three minutes in blood after intravenous administration, but the half-life of 6-acetyl morphine in humans is about 30 minutes. Heroin's peak blood level happens after 5 minutes of usage intranasally or intravenously, but its potency after intranasal usage is about half of intravenous usage. Because of various economic and social factors, heroin is one of the most commonly abused opioids in the world today.
Inannual prevalence rates for heroin use without a needle were 0. For all grades, the annual prevalence of use of heroin with a needle was 0.
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Heroin-related emergency department visits had increased from 33, in toin Heroin-related overdose deaths increased from in to There was a 7 fold increase in the total of heroin overdose deaths in this period. The most recent classification scheme identifies three major classes of opioid receptors, with several minor classes. The three most clinically relevant opioid receptors are the mu, kappa, and delta receptors.
Stimulation of central mu receptors causes respiratory depression, analgesia supraspinal and peripheraland euphoria. Kappa and delta-opioid receptors also have potent analgesic effects, with the kappa receptors being known for causing disassociation, hallucinations, and dysphoria. Delta receptors also modulate mu receptors and are thought to influence mood. Heroin has effects on the opioid receptors, particularly the mu receptor. It also has effects on the kappa and delta receptors.
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There is an evolving body of knowledge that the intensity and quality of response to heroin and much opioids can vary ificantly between patients, which can be unrelated to tolerance. When a patient has hypoxic tissue injury secondary to an heroin of heroin, the tissues show usual s of hypoxic change at the microscopic level. In the setting of overdose death, this can include s of pulmonary edema in lung tissue sections and rhabdomyolysis, including myocardial injury. Heroin is a strong agonist of opioid receptors. As mentioned, heroin has a short half-life, requiring drug users to use it several times per day to maintain the effect.
Additionally, tolerance usually develops over time, requiring consumers to take stronger and stronger doses to How the same effect. Tolerance to respiratory depression may be slower than tolerance to euphoric effects. The level of tolerance to opioids can have ificant effects on an individual's risk of opioid overdose.
Overdose is common as a consumer rarely knows how much they are taking per purchased dose.
Also, in street drugs, there are often contaminants that dilute the percentage of the drug consumed. Heroin's half-life is so short that consumers are usually seen medically in the setting of either overdose or withdrawal. In the overdose setting, there is usually decreased respiratory effort and rate, with sedation and constricted pupils.
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A severe overdose can progress to apnea with coma, which is followed by minutes by cardiac arrest and death unless immediate rescue measures are taken. Opiate withdrawal symptoms are not life-threatening, like alcohol or benzodiazepine withdrawal. Some or all of these symptoms may be seen; the patient does not need all to be diagnosed with heroin withdrawal. In summary, several medications can be used to treat opiate withdrawal symptoms, like methadone long-acting opioidbuprenorphine partial mu agonist and kappa antagonistor alpha-2 adrenergic agents clonidine and lofexidine.
If there is intravenous use, there can be "track marks. Intravenous drug use can lead to infectious complications discussed elsewhere such as cellulitis, thrombophlebitis, endocarditis, septic emboli, and compartment syndrome, for example.
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Adulterants in heroin can be quite diverse and sometimes unknown to the consumer and can confound the evaluator by giving a potentially very broad spectrum of conflicting physical exam findings. Law enforcement may have knowledge of the current adulterant blend of the heroin that is being locally consumed at the time of the encounter.
The evaluation is clinical, with prioritization of airway and breathing in the overdose setting.
Urine drug screening is thought to not be useful in the acute setting but has value in surveillance employment screening or recovery drug rehab setting. On urine drug testing, heroin makes the "opioids" line positive, along with morphine, codeine, hydromorphone, and hydrocodone.
Other opioids usually do not turn this test positive and need to be tested for separately, including methadone, oxycodone, fentanyl, buprenorphine, and tramadol.
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Bedside and office urine cup drug screens have infrequent false positive and false negative for a variety of substances tested for. The only finding in the urine that proves heroin use is the detection of 6-MAM 6 mono acetylmorphine. This metabolite is a specific byproduct of heroin metabolism. Medical review officers control the information obtained during employment-related drug testing in the United States.
Naloxone is a mainstay of therapy in this setting, but the practitioner is warned that first-line treatment is control of the airway and rescue breathing. Bag valve mask ventilation or similar intervention should be initiated immediately by the primary rescuer to restore oxygen supply to vital organs while other rescuers evaluate available methods of naloxone administration. A single rescuer should focus on heroin oxygen to the overdose victim until other rescuers are available to assist.
Basic Life Support and Advanced Cardiac Life Support principles should be followed during the resuscitation of a heroin overdose. An initial intravenous dose of 0. Patients treated with naloxone after heroin overdose may be safely released without transport to the hospital or emergency room if they have normal mentation and vital s. In the absence of co-intoxicants and further opioid use, there is a very low risk of death from rebound heroin toxicity. When there is a very clear history of heroin use or overdose, it can How fairly straightforward to initiate management with management of airway and breathing along with consideration of reversal agents.
However, in the undifferentiated unresponsive patient, with no history of such an ingestion, this can be much more challenging. Traditionally there has been a "coma cocktail," which has now largely fallen out of favor in many regions.
Naloxone can, in theory, cause alertness in the heroin overdose patient. Recently it has been found that if there is contamination with a fentanyl type compound that the naloxone 2 mg dose can be far smaller than would be actually necessary to reverse the ingestion. The action of heroin on the opioid receptors is fairly well characterized at this much.
An ongoing area of investigation is forensic, namely what opioid contaminants might be lurking within the next shipment of heroin coming into the United States from elsewhere. Clinicians who manage overdose patients should establish the need for ongoing treatment of their substance use disorder. In the absence of acute medical and psychiatric complications, the patient can be discharged from the hospital and be referred for addiction care.
As noted elsewhere, the toxicity is primarily due to hypoxia from hypoventilation, making airway management and adequate oxygenation the mainstay of therapy in the heroin overdose patient.
This has become increasingly true as contaminants such as carfentanyl make the dosing of naloxone for such overdoses and the projected duration of naloxone requirement less and less predictable. Heroin substance use disorder is a chronically relapsing disease that is often fatal. There has been a very gradual shift in thinking in the s in the United States regarding what management method is best for managing heroin substance use disorder.
The traditional method of focusing on having the patient remain chemical-free with the assistance of a therapeutic community model of support has unfortunately been plagued by rapid relapse once the intensity of care decreases, such as at the time of departure from inpatient rehab.