Opioids: Definition, Types, Uses, Effects, and Risks

Last Updated: January 6, 2025

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Opioids are a class of drugs that interact with opioid receptors in the brain and body to manage pain. Opioids are natural (like morphine), semi-synthetic (like oxycodone), or synthetic (like fentanyl). This broad category includes prescription medications and illicit drugs, each with varying potency and uses.

According to the World Health Organization (WHO), an estimated 27 million people worldwide suffer from opioid dependence, with the majority using heroin or prescription opioids. In the United States, the National Survey on Drug Use and Health reported that in 2021, approximately 2.5 million individuals aged 12 and older had OUD. The crisis underscores the need for awareness and proper regulation.

Opioids work by binding to receptors in the brain and spinal cord, blocking pain signals and producing euphoria. This mechanism makes opioids effective but also prone to misuse.

Medically, opioids are prescribed for acute and chronic pain, cancer-related pain, and palliative care. They also help with cough suppression and treating opioid dependence through maintenance therapy.

The effects of opioids vary, including short-term euphoria and pain relief but long-term risks like tolerance, dependence, and severe health complications, including organ damage.

Regular opioid use leads to dependence and addiction due to their impact on brain chemistry, particularly by increasing dopamine levels, which reinforces compulsive use despite negative consequences.

Common withdrawal symptoms include anxiety, muscle aches, and nausea, making it challenging for users to quit without medical intervention.

Misuse of opioids results in overdose, marked by respiratory depression and loss of consciousness, a life-threatening condition. In 2019, around 600,000 deaths were linked to drug use globally, with nearly 80% attributed to opioids, according to the World Health Organization (WHO). Of these, approximately 125,000 deaths were caused by opioid overdose, accounting for 25% of opioid-related fatalities.

What Are Opioids?

โ€œOpioids are a class of drugs used to reduce moderate to severe pain. Opioids can be made from the opium poppy plant or in the laboratory. Opioids block pain signals by binding to opioid receptors on nerve cells in the brain, spinal cord, gastrointestinal tract, and other organs in the body. Some opioids may also be used to treat cough and diarrhea. Opioids used for pain relief are usually safe when taken for a short time and as prescribed by a health care provider, but they can be highly addictive and, as a result, have often been misused or abused,โ€ as defined by the National Cancer Institute.

Opioids are a class of drugs that include both natural and synthetic compounds designed to interact with specific receptors in the brain and body, primarily the Mu1,2,3 receptors (MOR), Nociceptin receptors (NOR), Zeta receptors (ZOR), and Delta receptors (DOR) opioid receptors. They are used primarily for their pain-relieving and sedative effects. Their action mimics endogenous opioids like endorphins, which naturally regulate pain and mood.

Chemically, opioids are characterized by their ability to cross the blood-brain barrier and bind to opioid receptors, leading to the inhibition of pain signals. Many opioids share a basic molecular framework, such as a phenanthrene nucleus, which facilitates their binding affinity to these receptors. This structural similarity allows them to produce analgesia but also contributes to their addictive potential and side effects.

Natural opioids like morphine and codeine are derived directly from the opium poppy, while synthetic variants like fentanyl and oxycodone are created to mimic or amplify these effects. According to studies published by the National Institute on Drug Abuse (NIDA), opioids are both a cornerstone of modern pain management and a major contributor to the global addiction crisis, underscoring their dual-edged nature.

How Do Opioids Work?

Opioids work by binding to specific proteins called opioid receptors located in the periaqueductal gray, locus ceruleus (LC), rostral ventral medulla, substantia gelatinosa of the dorsal horn of the spinal cord, and the peripheral afferent nerves, which are part of the central and peripheral nervous systems. Opioid receptors are a type of G protein-coupled receptor (GPCR) that mediate the body’s response to various hormones, neurotransmitters, and medications. They are also involved in sensory functions such as vision, taste, and smell, according to a study by Rosenbaum DM, Rasmussen SG, and Kobilka BK. et al. 2009, titled โ€œThe structure and function of G-protein-coupled receptors.โ€ These receptorsโ€”primarily the mu, delta, and kappa receptorsโ€”are part of the body’s natural pain control system and regulate the perception of pain, mood, and even gastrointestinal function.

When an opioid activates the mu-opioid receptor (MOR) in the midbrain, it leads to a chain reaction that reduces pain signals. This begins with the suppression of GABA interneurons, which normally inhibit certain pathways. This suppression allows impulses to travel to the periaqueductal gray (PAG) and activate neurons that send inhibitory signals down to the spinal cord, according to a study by Toubia T, Khalife T. et al. 2019, titled โ€œThe Endogenous Opioid System: Role and Dysfunction Caused by Opioid Therapy.โ€ These signals stimulate enkephalin-releasing neurons in the dorsal horn, which reduces the transmission of pain signals from the body to the brain. Additionally, opioids directly block pain signals by acting on the dorsal horn of the spinal cord and peripheral nerves.

Mu-opioid receptors (MORs) help regulate the body’s stress response by reducing the release of norepinephrine (NE) from the locus ceruleus (LC). This action counteracts the sustained NE release triggered by corticotropin-releasing hormone (CRH) from the hypothalamus during stress. MOR activation, such as through morphine administration after trauma, lowers the risk of developing post-traumatic stress disorder (PTSD), according to a study by Toubia T, Khalife T. et al. 2019, titled โ€œThe Endogenous Opioid System: Role and Dysfunction Caused by Opioid Therapy.โ€

MORs are highly concentrated in the brain’s limbic system, which controls emotions. By influencing this area, MORs regulate mood, making them potential targets for treating conditions like anxiety and depression. In the brain’s reward system, MOR activation in the ventral tegmental area (VTA) reduces GABA inhibition, leading to increased dopamine release in the mesolimbic system. This dopamine release creates the pleasurable and rewarding effects of opioids, reinforcing their use.

Opioids mimic the action of the body’s natural endorphins, which are neurotransmitters that help cope with stress and pain, as studied by Sprouse-Blum AS, Smith G, Sugai D, Parsa FD.et al. 2010, in โ€œUnderstanding endorphins and their importance in pain management.โ€ However, prolonged opioid use desensitizes receptors, reduces natural endorphin production, and leads to tolerance, requiring higher doses to achieve the same effects. This mechanism underpins the development of opioid dependency and addiction.

What are the 3 Classes of Opioids?

The 3 classes of opioids include Natural Opioids, Semi-Synthetic Opioids, and Synthetic Opioids, each differing in origin, chemical structure, and effects on the body. These classifications help understand their pharmacological action, duration, and therapeutic use.

The 3 classes of opioids are as follows:

  1. Natural Opioids: Natural opioids are directly derived from the opium poppy plant. Examples of natural opioids include opium, morphine, and codeine. They primarily bind to opioid receptors to manage pain and suppress cough reflexes, according to Medical News Today in โ€œWhat to know about natural opioids.โ€ Natural opioids are short to moderate-acting and are used in medical settings for acute or chronic pain management. They cause side effects like drowsiness, constipation, and respiratory depression.
  2. Semi-Synthetic Opioids: Semi-synthetic opioids are chemically modified versions of natural opioids. Examples of semi-synthetic opioids are dihydromorphine, hydrocodone, hydromorphone, dihydrocodeine, nalbuphine, nalorphine, and oxycodone. They are designed to improve potency, absorption, or duration of action. Depending on the compound, they are short or long-acting. These opioids are widely used for moderate to severe pain but carry a higher risk of dependency and overdose due to their enhanced effects, according to Drug Bank in โ€œSemi-synthetic Opioids.โ€
  3. Synthetic Opioids: Synthetic opioids are fully manufactured in laboratories. Examples of synthetic opioids include fentanyl, tramadol, and methadone. They mimic natural opioids’ effects but are more potent and longer-acting. Fentanyl, for instance, is 50โ€“100 times more powerful than morphine and is used in pain management and anesthesia. Synthetic opioids are associated with a high risk of overdose, especially when misused, due to their potency, according to the United States Drug Enforcement Administration (DEA) in โ€œSynthetic opioids.โ€

What Drugs Are Considered Opioids?

The drugs that are considered opioids include morphine, codeine, heroin, and others widely used for pain relief or illicitly misused for their euphoric effects. These substances interact with the body’s opioid receptors to produce analgesia, sedation, and, in some cases, euphoria, but they also come with significant risks of dependency and overdose.

The following drugs are considered opioids:

  • Morphine: Morphine, a natural opioid, is derived from the opium poppy and is primarily used in hospitals to manage severe acute and chronic pain, such as post-surgical or cancer-related pain. Morphine works by binding to opioid receptors in the brain and spinal cord to block pain signals. In the U.S., morphine is one of the most commonly prescribed opioids for severe pain management in controlled settings, though its misuse contributes to opioid dependency in some cases. According to the National Health Statistics Report in 2020 titled โ€œTrends in Opioids Prescribed at Discharge From Emergency Departments Among Adults: United States, 2006โ€“2017โ€ shows that overall morphine prescriptions at ED discharge increased from 19.0% in 2006โ€“2007 to 21.5% in 2010โ€“2011, before declining to 14.6% in 2016โ€“2017, reflecting a 23.2% decrease. The usual starting dose in adults is 0.1 mg to 0.2 mg per kg every 4 hours as needed to manage pain, as explained by Mayo Clinic in โ€œMorphine (oral route).โ€
  • Codeine: Codeine, another natural opioid, is prescribed for mild to moderate pain and cough suppression. It is less potent than morphine but is metabolized into morphine in the liver to exert its effects. In the U.S., it is commonly included in combination medications such as Tylenol with Codeine. While its medical use is widespread, codeine misuse remains prevalent among certain demographics, especially in the form of “syrup abuse.โ€ The University of California San Francisco (UCSF) researchers found the rates of codeine prescriptions decreased from 3.7%to 2.9 % during the last 10 years. A dose of 15 to 60 milligrams (mg) every 4 hours as needed is administered. The doctor increases or decreases the dose of codeine as needed. However, as explained by the Mayo Clinic in โ€œCodeine (oral route),โ€ the dose is usually not more than 360 mg per day.
  • Heroin: Heroin is an illegal semi-synthetic opioid derived from morphine. It is not used medically in the U.S. but is widely abused for its rapid and intense euphoric effects. Heroin has a high addiction potential and is a major contributor to the opioid epidemic, with thousands of overdose deaths reported annually due to its misuse. In 2021, approximately 0.4% of individuals aged 12 or olderโ€”equivalent to about 1.1 million peopleโ€”reported using heroin within the past 12 months, according to the National Institute for Drug Abuse (NIDA), in โ€œWhat is the scope of heroin use in the United States?โ€
  • Fentanyl: Fentanyl is a synthetic opioid that is 50โ€“100 times more potent than morphine. It is used medically for severe pain, such as in cancer patients or during surgery. Illicitly manufactured fentanyl, however, is a leading cause of overdose deaths in the U.S., as small amounts can be fatal. In 2022, around 73,838 people in the United States died from a drug overdose that involved fentanyl, according to Statistica in โ€œFentanyl overdose deaths U.S. 1999-2022.โ€
  • Methadone: Methadone is a synthetic opioid primarily used in medication-assisted treatment (MAT) for opioid addiction. Methadone has been included on the World Health Organization’s List of Essential Medicines. It helps reduce withdrawal symptoms and cravings without producing the euphoric effects of other opioids. Methadone doses of greater than 60mg are most effective, according to a study by the World Health Organization (WHO) titled โ€œWHO/UNODC/UNAIDS. Substitution maintenance therapy in the management of opioid dependence and HIV/AIDS prevention.โ€ Methadone is also prescribed for chronic pain, though it carries a risk of overdose if misused. The percentage of overdose deaths involving methadone decreased steadily from 4.5% in January 2019 to 3.2% by August 2021, with a decline rate of about 0.05% to 0.06% both before and after the take-home policy change, according to a study by Jones CM et al. 2022, titled โ€œMethadone-Involved Overdose Deaths in the US Before and After Federal Policy Changes Expanding Take-Home Methadone Doses From Opioid Treatment Programs.โ€
  • Oxycodone: Oxycodone is a semi-synthetic opioid prescribed for moderate to severe pain management, such as in post-surgical recovery. It is the active ingredient in drugs like OxyContin. Oxycodone has a high potential for addiction and is frequently misused in the U.S., contributing significantly to the opioid crisis. Nearly 1 million U.S. residents aged 12 and older have reported using OxyContin nonmedically at least once, according to the National Household Survey on Drug Abuse. Abuse among high school students is notable, with 4% of high school seniors admitting to using the drug in the past year, as per the University of Michiganโ€™s Monitoring the Future Survey.
  • Hydrocodone: Hydrocodone, a semi-synthetic opioid, is commonly prescribed for moderate to severe pain and cough suppression. It is the active ingredient in medications like Vicodin. Hydrocodone is the most frequently prescribed opioid in the U.S., with over 136.7 million prescriptions dispensed in 2013, 93.7 million in 2016, and 83.6 million in 2017, according to IQVIAโ„ข (formerly IMS Healthโ„ข). Hydrocodone misuse is widespread in the U.S., where it is one of the most prescribed pain medications. In 2022, over 36.5 million people aged 12 and older used hydrocodone products in the past year, with 10.2% (3.7 million people) misusing the drug. Additionally, an estimated 6.1 million people in this age group had an opioid use disorder during the same period, according to the Substance Abuse and Mental Health Services Administration, titled โ€œNational Survey on Drug Use and Health.โ€
  • Tramadol: Tramadol is a synthetic opioid used for moderate pain relief. Unlike stronger opioids, tramadol has a dual mechanism of action, working on opioid receptors and inhibiting serotonin and norepinephrine reuptake. While considered less addictive than other opioids, tramadol misuse and dependency have increased in the U.S. in recent years. In 2022, tramadol was the 55th most commonly prescribed medication in the United States, with around 12.2 million prescriptions, according to Statistica in โ€œNumber of tramadol prescriptions in the U.S. from 2004 to 2022.โ€ The 2022 National Survey on Drug Use and Health reports that among the 14.6 million people aged 12 and older who used tramadol products in the past year, 9.4% misused the drug.
  • Buprenorphine: Buprenorphine is a semi-synthetic opioid used in MAT for opioid addiction treatment. It is a partial opioid agonist, meaning it produces a milder effect, helping reduce cravings and withdrawal symptoms. Buprenorphine’s medical use has expanded during the opioid crisis, making it an important tool in recovery programs. In 2023, the national buprenorphine dispensing rate was 4.7 prescriptions per 100 people, consistent with the 2019 rate, according to the Centers for Disease Control and Prevention (CDC) in โ€œBuprenorphine Dispensing Rate Maps.โ€However, significant state-level variations were observed, with the highest rates in West Virginia, Vermont, Kentucky, and Maine and the lowest rates in Iowa, Texas, California, and Hawaii. In 2019, 29.2% of adults who used buprenorphine in the past year misused it. Among these, 13.3% misused buprenorphine without having an opioid use disorder (OUD), while 15.9% misused it and also had an OUD, according to a study by Han B, Jones CM. et al. 2021, titled โ€œTrends in and Characteristics of Buprenorphine Misuse Among Adults in the US.โ€
  • Meperidine: Meperidine, also known as Demerol, is a synthetic opioid used for short-term pain relief, such as in post-surgical settings. Its use has declined due to the availability of safer alternatives and its potential for neurotoxicity and dependency. In 2021, the distribution of meperidine was highest in Arkansas at 16.7 mg per 10 persons and lowest in Connecticut at 0.8 mg per 10 persons, according to a study by Harrison LR et al. 2022, titled โ€œPronounced Declines in Meperidine in the US: Is the End Imminent?โ€ Additionally, meperidine prescriptions reported by Medicaid decreased by 73.8% from 2016 to 2021.
  • Hydromorphone: Hydromorphone, a semi-synthetic opioid, is 8 times stronger than morphine and is used for severe pain in cases like advanced cancer or post-surgical recovery. It has a high risk of dependency and misuse, though its medical use is necessary in some instances. โ€œThe Key Substance Use and Mental Health Indicators in the United States: Results from the 2022 National Survey on Drug Use and Healthโ€ indicates that approximately 102,000 individuals misused hydromorphone products, including Dilaudid, as mentioned by the Substance Abuse and Mental Health Services Administration (SAMHSA).
  • Oxymorphone: Oxymorphone, another semi-synthetic opioid, is used for managing moderate to severe pain and is known for its potency. It has a rapid onset of action and is highly effective, but its misuse has been linked to opioid addiction cases in the U.S. In 2020, the American Association of Poison Control Centers (AAPCC) reported 89 total oxymorphone exposures, including 38 single exposures and one death, showing a slight decrease from the previous year, according to the United States Drug Enforcement Administration (DEA). A study by Rauck R, Ma T, Adieh H, Kerwin R, et al. (2009), titled “Conversion and titration from oxycodone to oxymorphone extended-release in patients with chronic low back pain,” found that oxymorphone was more effective in patients switching from oxycodone, with a higher success rate among men (56.4%) compared to women (35%).
  • Tapentadol: Tapentadol is a synthetic opioid that combines opioid receptor activity with norepinephrine reuptake inhibition, making it effective for moderate to severe pain. Its unique mechanism of action reduces its abuse potential compared to other opioids but still requires caution in use. A study by Low CY, McCall KL, et al. 2022, titled “Declines and pronounced state-level variation in tapentadol use in the US,” found that the distribution of tapentadol significantly decreased by 53.8% between 2012 and 2020. According to a study by Vosburg SK, Severtson SG, Dart RC, et al. (2018), titled “Assessment of tapentadol API abuse liability with the researched abuse, diversion, and addiction-related surveillance system,” tapentadol has significantly lower abuse rates compared to other opioids. From 2011 to 2016, the average quarterly rate of intentional abuse of tapentadol was just 0.015 per 1,000,000 people, much lower than the abuse rates seen for opioids like oxycodone, hydrocodone, tramadol, and morphine.
  • Carfentanil: Carfentanil is a synthetic opioid used primarily as a veterinary tranquilizer. It is 10,000 times more potent than morphine and is extremely dangerous to humans, contributing to overdose deaths in the U.S. due to its illicit use. According to a study by Chan W et al. 2020, titled “Interpol review of toxicology 2016โ€“2019,” carfentanil abuse was most prevalent in Ohio, which accounted for 77% of all state-level reports in 2017. The number of carfentanil drug seizures in the U.S. increased sharply from 0 in 2015 to 1,292 in 2016, peaked at 5,857 in 2017, and then dropped to 804 in 2018. Overdose deaths from carfentanil abuse surged by 21.4% in 2016 and 10.4% in 2017 before declining by 4.1% in 2018, closely tracking carfentanil seizures in top states like Ohio and Florida, according to a study by Jalal H, Burke DS. et al. 2021, titled “Carfentanil and the rise and fall of overdose deaths in the United States.”
  • Nalbuphine: Nalbuphine is a semi-synthetic opioid used for moderate to severe pain, especially in hospital settings. Its unique property as a mixed opioid agonist-antagonist makes it less addictive than traditional opioids but still effective for pain relief. A CDC report found nalbuphine had one of the lowest long-term opioid use rates, with 5% continuing use after one year and 2.2% after three years, compared to higher rates for morphine and tramadol. Common adverse effects in nalbuphine-treated patients included sedation (36%), nausea (6%), and dizziness (5%), with evidence supporting its effectiveness for pain management and pruritus despite increased sedation, as mentioned in MedCrave titled โ€œNalbuphine and addiction: from the basic science to clinical set.โ€

How are Opioids Consumed?

Opioids are consumed in various forms, depending on the drug type and the user’s preference. The most common method is oral consumption, where opioids are taken as tablets, capsules, or liquid formulations. These are swallowed, allowing the drug to be absorbed slowly through the digestive system. Some individuals crush opioid pills to bypass the digestive process and inhale or inject the drug for faster effects. Snorting involves inhaling powdered forms of opioids, like heroin or crushed tablets, which allows rapid absorption through the nasal membranes.

Intravenous injection is another method where the opioid is injected directly into the bloodstream for an immediate and potent effect. Opioids like fentanyl and carfentanil have been abused via transdermal patches, where the patch is either removed and the gel inside is consumed or it is directly applied to the skin. Each method carries distinct risks, with injection and inhalation particularly increasing the likelihood of overdose due to faster, higher doses entering the bloodstream.

What Conditions are Opioids used for?

Opioids are used for conditions like acute pain, chronic pain, and cancer pain. These conditions are among the most common reasons for opioid prescriptions due to their significant pain-relieving effects. Opioids are highly effective in managing severe pain by binding to opioid receptors in the brain and spinal cord, which block pain signals. In acute pain scenarios, opioids provide rapid relief, while for chronic and cancer pain, they offer ongoing pain management, especially when other treatments are ineffective.

Opioids are used for the following conditions:

  • Acute pain (post-surgical or injury-related): Opioids are commonly prescribed for managing acute pain after surgeries or injuries due to their potent analgesic effects. Opioids like morphine and hydrocodone effectively reduce pain by binding to opioid receptors in the central nervous system, blocking pain signals. In most cases after surgery, oral (PO), intramuscular (IM), or intravenous (IV) opioids are prescribed. In the immediate postoperative period, opioids, such as morphine or oxycodone, are frequently used for initial pain relief, according to a study by Jain Y et al. 2023, titled โ€œEvaluation of Different Approaches for Pain Management in Postoperative General Surgery Patients: A Comprehensive Review.โ€ They provide rapid relief in the immediate postoperative period, though their use is limited to short durations to avoid dependence. Morphine is the standard choice for opiates and is widely used. It has a rapid onset of action with a peak effect occurring in 1 to 2 hours, according to a study by Garimella V, Cellini C. et al. 2013, titled โ€œPostoperative pain control.โ€
  • Chronic pain (non-cancer related): Chronic pain, especially from conditions like osteoarthritis or lower back pain, is treated with opioids when other therapies fail. Opioids like oxycodone and tramadol are prescribed for their long-acting pain relief, as they help manage persistent pain by altering pain perception in the brain and spinal cord. However, chronic use increases the risk of tolerance, dependency, and opioid use disorder, so opioids are used with caution for these conditions. Opioids provide short-term pain relief for chronic low back pain with about 30% pain reduction, according to a study by Deyo RA, Von Korff M, Duhrkoop D., et al. 2015, titled โ€œOpioids for low back pain,โ€ but their long-term effectiveness and impact on functional outcomes have โ€œmoderate quality evidence.โ€
  • Cancer pain: Opioids are important in managing cancer pain, particularly for patients experiencing moderate to severe pain due to the cancer or its treatments. Morphine, fentanyl, and oxycodone are used, as they are effective in controlling both nociceptive and neuropathic pain. According to the American Cancer Society, opioids provide significant relief, improving the quality of life for cancer patients, especially in advanced stages. Opioids are administered via oral, patch, or injectable forms depending on the patient’s condition and needs.
  • Palliative care and end-of-life pain management: In palliative care, opioids are widely used to alleviate pain and improve comfort for patients with terminal illnesses. They are integral in managing severe pain associated with conditions like end-stage cancer, dementia, or heart failure, according to the National Institute for Health and Care Excellence (NICE) titled โ€œPalliative care for adults: strong opioids for pain relief.โ€ Opioids like morphine and fentanyl help reduce suffering by acting on the central nervous system to block pain signals and also promote relaxation, thus enhancing the patient’s quality of life in their final stages.
  • Severe musculoskeletal injuries: For severe musculoskeletal injuries, such as fractures or severe sprains, opioids like hydrocodone or oxycodone are used for their fast and effective pain-relieving properties. These drugs work by targeting pain receptors in the brain and spinal cord, reducing pain signals and improving recovery comfort. Although opioids provide effective short-term pain relief, their use is monitored due to the risk of misuse in high-dosage settings.
  • Post-operative recovery: After surgery, opioids are frequently prescribed to manage moderate to severe pain, as they are highly effective in providing post-surgical pain relief. They work by inhibiting the transmission of pain signals in the nervous system, allowing patients to recover more comfortably. However, due to the risk of prolonged use, clinicians are shifting toward alternative pain management methods and lower opioid prescriptions.
  • Severe burn injuries: In burn victims, opioids like morphine are important in providing relief from severe pain caused by tissue damage and wound healing, according to Jamal S. et al. 2024, titled โ€œLong-term opioid use after burn injury: a retrospective cohort study.โ€ These opioids work by blocking pain signals in the spinal cord and brain, helping patients endure the intense pain associated with burn injuries. The rapid onset of pain relief also helps in managing the acute stress response to trauma.
  • Sickle cell crisis pain: Patients with sickle cell disease experience excruciating pain during sickle cell crises. Opioids such as morphine or hydromorphone are necessary in managing this severe pain. These drugs are highly effective in reducing both nociceptive and ischemic pain by binding to opioid receptors and inhibiting pain signals from the affected tissues. Opioids are administered intravenously within 60 minutes of ER arrival. The American College of Emergency Physicians advises combining opioids with NSAIDs, reassessing pain within 30 minutes, and administering additional doses if pain persists, according to a study by Brandow AM and DeBaun MR. et al. 2018, titled โ€œKey Components of Pain Management for Children and Adults with Sickle Cell Disease.โ€
  • Neuropathic pain: Opioids are sometimes used to treat neuropathic pain, which results from nerve damage. Medications like oxycodone and tramadol provide relief by blocking pain signals in the central nervous system. However, due to the complex nature of neuropathic pain and the risk of opioid misuse, the current guidelines for neuropathic pain treatment do not recommend opioids as a first-line option, according to a study by Attal N, Cruccu G, Baron R, et al. 2010, titled โ€œEFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision.โ€ Opioids are combined with other treatments, such as antidepressants or anticonvulsants, to offer holistic pain management.
  • Pain associated with major trauma: Opioids are frequently administered to patients with major trauma, including those with multiple fractures or injuries. They work by suppressing pain signals and decreasing the overall pain experience. However, due to the severity of trauma and the need for extended recovery, opioid use is closely monitored to prevent misuse and manage long-term pain effectively. Opioids are used in combination with other medications and nonpharmacologic interventions to achieve more effective analgesia. This approach is called opioid-sparing or multimodal analgesic therapy, as studied by Sullivan D, Lyons M, Montgomery R, Quinlan-Colwell A., et al. 2016, in โ€œExploring Opioid-Sparing Multimodal Analgesia Options in Trauma: A Nursing Perspective.โ€
  • Cough suppression (e.g., codeine): Opioids like codeine are sometimes used to suppress severe coughs that do not respond to other medications. Codeine works by acting on the central nervous system to reduce the coughing reflex. It is effective in treating chronic and severe coughing conditions, but it is limited due to its potential for dependence and misuse, according to Bolser DC, Davenport PW. et al. 2007, titled โ€œCodeine and cough: an ineffective gold standard.โ€
  • Diarrhea management (e.g., loperamide): Opioids, especially loperamide, are used to treat diarrhea by reducing gastrointestinal motility. This class of opioids works by binding to opioid receptors in the gut, slowing down peristalsis, and allowing for increased absorption of fluids and electrolytes, as studied by Chan L-N et al. 2008, in โ€œOpioids, especially loperamide, are used to treat diarrhea by reducing gastrointestinal motility.โ€ While loperamide is effective, misuse of this opioid for its central nervous system effects is a growing concern. Between 2008 and 2016, 179 cases of loperamide abuse were reported to the United States National Poison Data System, according to a study by Antoniou T, Juurlink DN, et al. 2017, titled “Loperamide abuse.”
  • Opioid use disorder treatment (e.g., methadone, buprenorphine): Opioids like methadone and buprenorphine are used in the treatment of opioid use disorder (OUD). These medications work by acting on the same opioid receptors in the brain as other opioids but produce less intense effects, which help reduce withdrawal symptoms and cravings without the same level of euphoria. Research by the Substance Abuse and Mental Health Services Administration, 2019, has demonstrated the 60% to 90% effectiveness of these medications, especially methadone, in reducing relapse rates and supporting long-term recovery for individuals with OUD.

What are the Side Effects of Opioids?

The effects of opioids include physical, neurological, and psychological symptoms such as drowsiness, nausea, confusion, respiratory depression, and tolerance. These effects result from opioids’ interaction with receptors in the brain and nervous system, which regulate pain and reward but also affect other bodily functions. Some side effects are short-term, like dizziness, while others, like tolerance and dependence, develop over prolonged use. Opioids also lead to severe outcomes such as respiratory depression, which results in overdose.

The effects of opioids are as follows:

  • Drowsiness: Drowsiness is a state of sedation caused by opioids slowing down central nervous system activity. While intended to manage pain, this side effect is short-term and physically impairs alertness and coordination, increasing the risk of accidents, according to a study by Young-McCaughan S, Miaskowski C. et al. 2001, titled โ€œDefinition of and mechanism for opioid-induced sedation.โ€ It occurs because opioids enhance inhibitory neurotransmitter activity, reducing brain excitability.
  • Nausea: Nausea is a common reaction to opioids caused by their stimulation of the chemoreceptor trigger zone (CTZ) in the brain. Nausea is an opioid side effect that is short-term, and the area detects toxins and signals the body to expel them, leading to physical feelings of sickness, particularly in new users or with higher doses. Up to 40% of patients experience nausea when taking opioids, according to a study by Mallick-Searle T, Fillman M., et al. 2017, titled โ€œThe pathophysiology, incidence, impact, and treatment of opioid-induced nausea and vomiting.โ€
  • Vomiting: Opioid-induced vomiting is an opioid side effect that is short-term, accompanies nausea, and results from the same stimulation of the CTZ. This physical effect also occurs due to slowed gastric motility, as opioids interfere with the normal movement of the digestive system.
  • Constipation: Constipation is a side effect of opioids binding to receptors in the gastrointestinal tract, reducing bowel motility and secretion. This long-term effect is a major reason for discomfort in chronic opioid users, requiring additional medication to manage. Up to 95% of patients taking opioids experience opioid-induced constipation (OIC), according to a study by Kumar L et al. 2014, titled โ€œOpioid-Induced Constipation: Pathophysiology, Clinical Consequences, and Management.โ€
  • Respiratory Depression: Respiratory depression is a potentially fatal side effect, slowing of breathing due to opioidsโ€™ suppression of the brainstemโ€™s respiratory centers. This short-term effect occurs because opioids reduce the brain’s sensitivity to carbon dioxide levels, which normally drive the urge to breathe. Opioid-induced respiratory Depression occurs in about 0.5% of patients treated with opioids for acute postoperative pain, according to a study by Boitor M et al. 2020, titled โ€œRisk factors for severe opioid-induced respiratory depression in hospitalized adults: A case-control study.โ€ A trial study by Ashish K.K et al. 2020, titled โ€œPrediction of Opioid-Induced Respiratory Depression on Inpatient Wards Using Continuous Capnography and Oximetry: An International Prospective, Observational Trial,โ€ indicated that 46% of patients experienced at least one episode of respiratory depression.
  • Confusion: Confusion refers to impaired cognitive function caused by opioids’ side effects on neurotransmitter release in the brain. By altering dopamine and serotonin levels, opioids disrupt thought processes, memory, and decision-making. This short-term effect targets an individual’s neurological aspect.
  • Euphoria: Opioids increase dopamine release in the brainโ€™s reward pathways, causing a sense of intense pleasure or well-being. This short-term side effect contributes to misuse and leads to psychological dependence. According to a study by Caplan M et al. 2023, titled โ€œUse of clinical phenotypes to characterize emergency department patients administered intravenous opioids for acute pain,โ€ 52% of patients who received intravenous opioids for acute pain experienced euphoria or feeling high.
  • Dizziness: Dizziness results from opioids lowering blood pressure or interfering with balance-regulating mechanisms in the brainโ€™s vestibular system. This short-term neurological effect causes lightheadedness and increases fall risk, especially in older adults.
  • Itching: Itching occurs due to histamine release triggered by opioids binding to certain receptors. This short-term side effect causes skin irritation, redness, or a sensation of itchiness, requiring antihistamines for relief. A study by Nguyen E et al. 2021, titled โ€œEvaluation of Therapies for Peripheral and Neuraxial Opioid-induced Pruritus based on Molecular and Cellular Discoveries,โ€ found that between 60โ€“90% of individuals experienced itching following the use of lipophilic opioids such as fentanyl. After morphine use, 60โ€“85% experienced itching as a side effect.
  • Sweating: Sweating is caused by opioidsโ€™ dysregulation of the hypothalamus, which controls body temperature. Excessive sweating occurs even without heat or exertion as a short-term side effect on the physical health of opioid users.
  • Dry Mouth: Dry mouth, or xerostomia, occurs when opioids reduce salivary gland secretion. If prolonged, this side effect leads to physical discomfort, bad breath, and an increased risk of dental issues. The use of oral opioids is associated with a higher incidence of adverse events, with dry mouth reported in 25% of patients, according to Moore, R.A., McQuay, H.J. et al. 2005, titled โ€œPrevalence of opioid adverse events in chronic non-malignant pain: systematic review of randomised trials of oral opioids.โ€
  • Decreased Libido: Chronic opioid use suppresses the hypothalamic-pituitary-gonadal axis, reducing hormone levels like testosterone or estrogen. This hormonal imbalance decreases sexual desire and function.
  • Fatigue: Fatigue is a general feeling of short-term tiredness resulting from opioidsโ€™ sedative effects on the central nervous system. It interferes with daily physical activities and overall productivity. Severe fatigue symptoms were reported by 77% of patients using methadone and 67% of those using buprenorphine as opioid agonist therapy (OAT), as studied by Vold, J.H., Gjestad, R., Aas, C.F. et al. 2020, titled โ€œImpact of clinical and sociodemographic factors on fatigue among patients with substance use disorder: a cohort study from Norway for the period 2016โ€“2020.โ€
  • Tolerance: Tolerance develops as the body adapts to repeated opioid use, requiring higher doses to achieve the same effect. This is a long-term symptom that happens due to opioid receptor desensitization and reduced efficacy of the drug over time.
  • Dependence: Dependence is both a physical and psychological symptom that occurs when the body becomes reliant on opioids for a long time to function normally, leading to withdrawal symptoms upon cessation. According to a study by Boscarino JA et al. 2010, titled โ€œRisk factors for drug dependence among out-patients on opioid therapy in a large US healthcare system,โ€ among those who received four or more opioid prescriptions in a year, 26% met the criteria for โ€œdependence.โ€
  • Withdrawal Symptoms: Withdrawal symptoms such as sweating, muscle aches, anxiety, and irritability occur when opioid use is abruptly stopped. These short-term symptoms result from the brainโ€™s attempt to regain normal function without the drug, as it is physically and psychologically dependent on the drug.
  • Slowed Heart Rate: Slowed heart rate is a cardiovascular side-effect caused by short-term opioids depressing autonomic functions in the brainstem. This can reduce oxygen delivery to vital organs, compounding sedation effects.
  • Low Blood Pressure: Opioids cause vasodilation by acting on the smooth muscle of blood vessels, which leads to hypotension. This physical side effect increases the risk of dizziness and fainting, especially in patients with pre-existing conditions.
  • Mood Swings: Mood swings result from opioidsโ€™ impact on brain neurotransmitters like dopamine and serotonin. Fluctuating levels cause rapid changes in emotional state, such as euphoria, followed by depression.
  • Overdose: Overdose is a life-threatening condition caused by excessive opioid intake, leading to severe respiratory depression. These acute symptoms include pinpoint pupils, unconsciousness, and dangerously slow breathing, requiring immediate medical intervention. In 2019, around 600,000 deaths were linked to drug use globally, with nearly 80% attributed to opioids, according to the World Health Organization (WHO). Of these, approximately 125,000 deaths were caused by opioid overdose, accounting for 25% of opioid-related fatalities.

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What are the Overdose Effects of Opioids?

The overdose effects of opioids include respiratory depression, unresponsiveness, and extreme drowsiness, which rapidly lead to severe health complications or death. Opioid overdose results from excessive consumption that overwhelms the central nervous system and respiratory centers. This leads to life-threatening physical and neurological conditions, including slowed breathing, unconsciousness, and, in severe cases, cardiac arrest or coma.

The overdose effects of opioids are as follows:

  • Respiratory depression: Respiratory depression is a severe reduction in breathing rate caused by opioid overdose suppressing the brain’s respiratory centers. It is the most dangerous physical effect and a leading cause of opioid-related fatalities.
  • Slow or stopped breathing: Opioids relax the muscles controlling respiration, leading to critically low oxygen levels. This causes long-term brain damage or death.
  • Extreme drowsiness: Overdose of opioids results in physical lethargy and an inability to stay awake, increasing the risk of unconsciousness and aspiration.
  • Pinpoint pupils: Pinpoint pupils are a physical sign of opioid overdose where pupils become abnormally small, indicating central nervous system depression.
  • Cold or clammy skin: Cold or clammy skin is a physical effect resulting from reduced blood circulation, signaling severe cardiovascular compromise.
  • Bluish lips or fingernails: Bluish lips and fingernails are a sign of cyanosis due to inadequate oxygenation of the blood. This quickly progresses to cardiac arrest if untreated, โ€œWhat Happens to the Body During Opioid Overdose.โ€
  • Weak or absent pulse: A weak or absent pulse is caused by reduced heart activity. This physical effect requires immediate medical intervention.
  • Unresponsiveness: A neurological symptom where the person does not respond to stimuli preceding coma or death.
  • Seizures: Seizures are rare but severe neurological effects caused by oxygen deprivation or chemical imbalances during opioid overdose.
  • Vomiting: Vomiting is a physical reaction that increases the risk of aspiration and choking, particularly in unconscious individuals.
  • Coma: Coma is a state of prolonged unresponsiveness due to severe central nervous system suppression, requiring urgent medical care to prevent irreversible damage or death.
  • Death: The most severe consequence of an opioid overdose, resulting from the cumulative failure of vital systems, primarily respiratory and cardiovascular. In 2015, opioid overdoses in the U.S. resulted in 100 fatalities, while globally, nearly 20 million people use heroin or opium, with high overdose rates linked to fentanyl in Europe and Asia, according to Schiller EY, Goyal A, Mechanic OJ. et al. 2023, titled โ€œOpioid Overdose.โ€

Can you Die from Opioid Overdose?

Yes, it is possible to die from an opioid overdose. Opioid overdoses lead to respiratory depression, where breathing slows down or stops completely, which is the primary cause of death in these cases. According to the World Health Organization (WHO), approximately 125,000 people died from opioid overdoses in 2019. In the United States, opioids are a leading cause of drug-related deaths, with an estimated 70,000 overdose deaths occurring annually, a significant portion of which involve opioids like fentanyl, heroin, and prescription painkillers. Opioid overdoses are reversed with timely administration of naloxone, an opioid antagonist, but without intervention, overdose results in permanent brain damage or death due to lack of oxygen.

How Do Opioids Affect the Brain?

Opioids affect the brain by binding to specific receptors known as opioid receptors, which are primarily located in the brain, spinal cord, and other parts of the nervous system. When opioids bind to these receptors, they block pain signals and release large amounts of dopamine, a neurotransmitter responsible for feelings of pleasure and reward. This flood of dopamine leads to the euphoric sensations that are associated with opioid use, according to Healthline in โ€œHow Opioids Affect Your Brain in the Long and Short Term.โ€

Opioids influence serotonin levels, which regulate mood, appetite, and sleep, contributing to the sense of well-being or drowsiness. However, prolonged opioid use alters the brain’s chemical balance, leading to tolerance, dependence, and addiction as the brain becomes less responsive to natural rewards. This dependency occurs because the brain adjusts to the constant presence of opioids, requiring more of the drug to achieve the same effects. Over time, this disrupts the brain’s natural ability to produce dopamine and serotonin, contributing to withdrawal symptoms when the drug is not available.

How Does Opioid Use Lead to Addiction?

Opioid use leads to addiction through a process where the brain becomes dependent on the drug due to its impact on neurotransmitter systems, particularly dopamine and serotonin. Opioid addiction, also known as opioid use disorder (OUD), is characterized by compulsive drug-seeking behavior, an inability to control use, and continued use despite negative consequences.

When opioids are used regularly, they bind to opioid receptors in the brain, leading to intense feelings of pleasure or euphoria due to the release of large amounts of dopamine. Over time, the brain’s reward system becomes less responsive to natural stimuli, requiring increasing amounts of the drug to achieve the same effectโ€”a phenomenon known as tolerance. As tolerance develops, the user begins to take higher doses, increasing the risk of dependency. The brain then adjusts to the constant presence of opioids, and without the drug, the person experiences withdrawal symptoms, such as pain, agitation, and anxiety, which are alleviated by taking more opioids. This cycle of drug use, increased tolerance, and withdrawal contributes to addiction.

Opioid addiction occurs when these neurological changes interfere with an individualโ€™s ability to function normally, leading to compulsive use and physical and psychological reliance on opioids, as studied by Kosten TR, George TP. et al. 2002, titled โ€œThe neurobiology of opioid dependence: implications for treatment.โ€ This also highlights that genetic and environmental factors play a significant role in how addiction develops, with some individuals being more vulnerable due to their genetic makeup or life experiences.

What is Opioid Dependence?

Opioid dependence is a state where an individualโ€™s body becomes physically reliant on opioids to function normally, leading to withdrawal symptoms when the drug is reduced or stopped. It differs from addiction in that addiction is characterized not only by physical dependence but also by psychological cravings and compulsive drug-seeking behaviors. While dependence involves the body’s adaptation to the presence of the drug, addiction encompasses a broader spectrum of behavioral and emotional aspects, including a loss of control over use and continued use despite negative consequences.

The process of developing opioid dependence begins when opioids are used regularly over time. The drug works by binding to specific receptors in the brain, primarily the mu-opioid receptors, which regulate pain and emotional responses. This interaction leads to the release of dopamine, which produces pleasurable feelings. However, with chronic use, the brain adapts by reducing its natural production of certain neurotransmitters, including dopamine. As a result, the individual becomes reliant on the drug to achieve normal brain function and avoid withdrawal symptoms. These withdrawal symptoms include agitation, muscle pain, nausea, vomiting, and intense cravings. The bodyโ€™s growing tolerance to the drug means that larger doses are needed to achieve the same effect, which increases the risk of dependence.

A study by Kosten TR, George TP. et al. 2002, titled โ€œThe neurobiology of opioid dependence: implications for treatment.โ€ demonstrates that opioid dependence develops through a combination of neurochemical changes and behavioral patterns. Over time, these physiological adaptations make it difficult for individuals to stop using the drug without experiencing withdrawal, further reinforcing continued use.

What are the Withdrawal Symptoms of Opioids?

The withdrawal symptoms of opioids include physical and psychological reactions that occur when opioid use is reduced or stopped. The most common symptoms include anxiety, muscle aches, and sweating, among others. These symptoms are a result of the bodyโ€™s adaptation to the absence of opioids, which have altered normal brain chemistry during regular use. When opioids are no longer present, the brain and body experience a physical and emotional imbalance that leads to discomfort.

The withdrawal symptoms of opioids are as follows:

  • Anxiety: Anxiety is a common symptom of opioid withdrawal, as the brain’s chemical balance is disrupted. Opioids increase dopamine levels, and when they are absent, anxiety levels rise due to the lack of stimulation to the brain’s reward system.
  • Restlessness: Restlessness or an inability to relax is another symptom caused by the body’s heightened state of alertness as it struggles to adapt without the sedative effects of opioids.
  • Muscle Aches: Opioids are pain relievers, so when they are discontinued, the body experiences muscle aches and pain, referred to as “body aches,” during withdrawal. This is due to the bodyโ€™s nervous system becoming hyperactive and the rebalancing of neurotransmitters.
  • Sweating: Sweating is another physical response to withdrawal, driven by the bodyโ€™s attempt to regulate its temperature as the autonomic nervous system becomes dysregulated.
  • Runny Nose and Tearing Eyes: Opioids suppress certain functions of the autonomic nervous system, and their absence causes the body to react by producing excess fluids such as mucus and tears.
  • Insomnia: As opioids help with sleep by binding to receptors in the brain, withdrawal results in insomnia as the body adjusts to the absence of these calming effects.
  • Nausea and Vomiting: The digestive system is significantly impacted by opioid withdrawal, as the body reacts to the absence of the drug by producing symptoms like nausea and vomiting.
  • Diarrhea: Opioids slow down gastrointestinal motility, so without them, the digestive system becomes overactive, leading to diarrhea.
  • Abdominal Cramps: Abdominal cramps are a result of the digestive system overreacting as it attempts to adjust to the absence of opioids.
  • Goosebumps and Dilated Pupils: Dilated pupils are physical signs of withdrawal as the body enters a hyperactive state in response to the absence of the drug. The sympathetic nervous system is engaged, leading to these reactions.
  • Rapid Heart Rate and High Blood Pressure: As opioids normally slow heart rate and reduce blood pressure, their withdrawal can cause the opposite effect, leading to rapid heart rate and high blood pressure as the body compensates for the loss of the drugโ€™s calming effect.
  • Irritability and Fatigue: Irritability and fatigue are common symptoms due to the emotional and physical strain of withdrawal. The body is struggling to adjust to the absence of the drug, leading to mood swings and fatigue.
  • Cravings for Opioids: Cravings are perhaps the most challenging symptom of opioid withdrawal, as the brainโ€™s reward system is craving the dopamine stimulation that opioids once provided.

What is Opioid Use Disorder?

Opioid Use Disorder (OUD) is a medical condition characterized by the problematic use of opioids that leads to significant distress or impairment. It involves a pattern of opioid consumption that results in a strong craving for the substance, unsuccessful efforts to cut down or control use, and continued use despite negative consequences such as physical, psychological, or social harm. OUD is classified as a chronic relapsing disease and is included in the DSM-5 criteria for substance use disorders.

Globally, OUD is a significant public health concern, affecting millions of individuals. According to the World Health Organization (WHO), an estimated 27 million people worldwide suffer from opioid dependence, with the majority using heroin or prescription opioids. In the United States, the National Survey on Drug Use and Health reported that in 2021, approximately 2.5 million individuals aged 12 and older had OUD. The prevalence of OUD has escalated alongside the opioid epidemic, fueled by the misuse of prescription painkillers and synthetic opioids like fentanyl and heroin.

The condition not only impacts individuals but also places a significant burden on healthcare systems and communities. Treatment for OUD involves medication-assisted therapy (MAT) using methadone, buprenorphine, or naltrexone, along with counseling and behavioral therapies, which have been shown to improve recovery outcomes.

How Does Opioid Detox Work?

Opioid detox works by systematically removing opioids from the body while managing withdrawal symptoms and preparing individuals for long-term recovery. The primary purpose of detox is to safely clear opioids from the system, alleviate the physical and psychological discomfort of withdrawal, and serve as the first step toward a comprehensive treatment plan.

The detox process begins with an evaluation, where medical professionals assess the patientโ€™s physical and mental health, opioid use history, and the severity of dependence. Stabilization follows, involving the use of medications such as methadone, buprenorphine, or clonidine to manage withdrawal symptoms like nausea, anxiety, and cravings. Medications are administered in gradually reduced doses to ease the detox process. Finally, the patient is transitioned to long-term treatment, which includes medication-assisted therapy (MAT), counseling, and support groups.

The duration of detox varies based on factors such as the type of opioid used, the level of dependence, and individual health conditions. For short-acting opioids, such as heroin, symptoms begin 8-24 hours after the last dose and last for 4-10 days. In contrast, long-acting opioids, like methadone, cause withdrawal symptoms that start 12-48 hours after the last use and persist for 10-20 days. Common symptoms include nausea and vomiting, along with other physical and psychological effects such as muscle aches, sweating, and cravings, according to the World Health Organization (WHO) in โ€œClinical Guidelines for Withdrawal Management and Treatment of Drug Dependence in Closed Settings.โ€

How Can You Safely Use Opioids to Manage Pain?

You can safely use opioids to manage pain by following a healthcare provider’s prescription closely, using the lowest effective dose for the shortest time necessary, and avoiding alcohol or other substances that interact with opioids. Regular monitoring by a healthcare provider ensures appropriate dosing and reduces risks of misuse or dependence. The Centers for Disease Control and Prevention (CDC) in โ€œCDC Clinical Practice Guideline for Prescribing Opioids for Pain โ€” United States, 2022โ€ emphasize the importance of co-administering non-opioid therapies, such as NSAIDs or physical therapy, to minimize reliance on opioids. Adhering to these practices significantly lowers the risks of side effects, addiction, and overdose.

What is the Difference Between Opioids and Opiates?

The main difference between opioids and opiates is that opiates are naturally derived from the opium poppy (e.g., morphine, codeine), while opioids include both natural and synthetic drugs that act on the same opioid receptors (e.g., fentanyl, oxycodone).

Opiates like morphine are extracted directly from the plant, while synthetic opioids are chemically manufactured to mimic the effects of opiates, being more potent and long-lasting. Both categories serve similar medical purposes, such as pain relief and cough suppression, but opioids are more likely to include medications designed for stronger or specific effects. Advances in synthetic opioids have contributed to both effective pain management and the opioid epidemic due to their high abuse potential.

Which Types of Opioids are the Strongest?

The strongest opioids are fentanyl and carfentanil. Fentanyl is 50-100 times more potent than morphine, according to the United States Drug Enforcement Administration (DEA) in โ€œDrug Fact Sheet: Fentanyl,โ€ while carfentanil, primarily used for veterinary purposes, is 10,000 times more potent than morphine, according to the National Institute for Health (NIH).

Fentanyl works by rapidly binding to opioid receptors in the brain, causing profound pain relief but also carrying a high risk of respiratory depression and overdose. Carfentanil, due to its extreme potency, is rarely prescribed for humans but is a significant factor in the opioid overdose crisis when found illicitly mixed with other drugs. These opioids are designed for cases of extreme pain, such as cancer or post-surgical care, but their potency makes them particularly dangerous in unsupervised use.

How are Opioids Made?

Opioids are made by either natural extraction or chemical synthesis. Natural opioids, like morphine and codeine, are extracted from the opium poppy (Papaver somniferum). The plant sap undergoes processing to isolate active alkaloids.

Synthetic opioids, such as fentanyl, are created in laboratories using chemical synthesis to mimic the molecular structure and effects of natural opiates. Semi-synthetic opioids, like oxycodone and hydrocodone, are derived from natural opiates but undergo further chemical modification. This process allows for the development of opioids with varying potencies, durations, and uses tailored for specific medical conditions.

Is Opioid Addiction Treatable?

Yes, opioid addiction is treatable through a combination of medication-assisted treatment (MAT) and behavioral therapies. MAT involves using FDA-approved medications like methadone, buprenorphine, or naltrexone to reduce withdrawal symptoms and cravings while normalizing brain function. Behavioral therapies, such as cognitive-behavioral therapy (CBT), address the psychological aspects of addiction.

Integrated treatment approaches significantly improve recovery outcomes by up to 75%, with reduced relapse rates and improved social functioning, according to research by the CDC. However, sustained treatment and support are important, as addiction is a chronic condition that requires long-term management.

What are Synthetic Opioids?

Synthetic opioids are man-made drugs designed to mimic the effects of natural opioids derived from the opium poppy, such as morphine and codeine. These substances interact with opioid receptors in the brain to provide pain relief and other effects. Common examples include fentanyl, which is 50-100 times more potent than morphine; methadone, used for addiction treatment; and tramadol, prescribed for moderate to severe pain.

Synthetic opioids are widely used in medical settings due to their potency and versatility, but they also pose significant risks, including addiction, overdose, and respiratory depression. Their widespread misuse has been a major contributor to the global opioid epidemic, with fentanyl being a leading cause of overdose deaths due to its extreme potency.

How Are Opioids Eliminated from the Body?

Opioids are eliminated from the body by metabolism in the liver and excretion through the kidneys. The liver processes opioids through enzymes, primarily in the cytochrome P450 system, converting them into metabolites, according to a study by Smith HS. et al. 2009, titled โ€œOpioid metabolism.โ€ These metabolites are then excreted in urine. A smaller percentage of opioids is eliminated through bile and feces. The elimination half-life of opioids depends on the type of opioid and individual factors like liver and kidney function.

How Long Do Opioids Stay in Your System?

Opioids stay in your system for varying durations depending on the specific opioid. Short-acting opioids, like heroin, remain detectable for 1-3 days, while long-acting opioids, like methadone, are detected for up to 10 days. Detection times also vary by test type; for example, urine tests detect opioids for 1-4 days, while hair tests show traces for up to 90 days.

How Are Opioids Classified?

Opioids are classified by their origin and potency into three main categories. Natural opioids, such as morphine and codeine, are derived directly from the opium poppy. Semi-synthetic opioids, like oxycodone and hydrocodone, are chemically modified versions of natural opioids. Synthetic opioids, including fentanyl and methadone, are fully man-made. Additionally, opioids are categorized based on their medical use, such as pain management or addiction treatment, and by their binding strength to opioid receptors, which influences their potency and effects.

Are Opioids Legal?

Yes, opioids are legal when prescribed by a healthcare provider for medical purposes, such as managing severe pain or treating opioid addiction. However, illicit use of opioids, like heroin or unprescribed fentanyl, is illegal. Misuse of prescription opioids also leads to legal consequences.

Who is at Risk of Opioid Use Disorder?

Individuals at risk of opioid use disorder include those who use opioids chronically for pain management, particularly at high doses over prolonged periods. People with a history of substance abuse or addiction, co-occurring mental health conditions such as anxiety or depression, or a family history of addiction are also more vulnerable. Social and environmental factors, such as high-stress levels and easy access to opioids, further increase the likelihood of developing this disorder.

What Is Medication-Assisted Treatment (MAT) for Opioid Addiction?

The medication-assisted treatment (MAT) for opioid addiction combines medications like methadone, buprenorphine, or naltrexone with counseling and behavioral therapies to treat opioid use disorder. MAT works by reducing cravings and withdrawal symptoms while addressing the psychological aspects of addiction. MAT significantly improves treatment outcomes and reduces the risk of relapse, according to the Pew Charitable Trusts in โ€œMedication-Assisted Treatment Improves Outcomes for Patients With Opioid Use Disorder.โ€

What is Naloxone, and How Does it Work?

Naloxone, sometimes referred to in combination medications like Suboxone (naloxone and buprenorphine), is a life-saving medication used to reverse opioid overdoses. It works by rapidly binding to opioid receptors in the brain, displacing opioids like heroin or fentanyl, and blocking their effects. Naloxone quickly restores normal breathing in someone experiencing respiratory depression caused by an overdose. While naloxone is not a cure for opioid addiction, it plays an important role in emergencies and harm-reduction strategies. Suboxone, which includes both naloxone and buprenorphine, is used in medication-assisted treatment (MAT) for opioid addiction to manage withdrawal symptoms and cravings, helping individuals stabilize during recovery.

What is the Relationship Between Opioids and Chronic Pain Management?

Yes, there is a relationship between opioids and chronic pain management, but this is complex and controversial. Opioids provide relief for certain types of chronic pain, especially in the short term, by binding to opioid receptors in the brain and reducing the perception of pain. However, their long-term use for managing chronic pain is limited and debated due to risks such as tolerance, dependence, addiction, and side effects like cognitive impairment and hormonal changes.

While opioids are effective for acute and cancer-related pain, their benefits in chronic non-cancer pain are modest at best, not outweighing the risks. For instance, a study by Deyo RA, Von Korff M, Duhrkoop D., et al. 2015, titled โ€œOpioids for low back pain,โ€ shows only about 30% pain reduction in chronic conditions, with unclear improvements in functionality. Consequently, medical guidelines recommend opioids only when other treatments, such as physical therapy, NSAIDs, or antidepressants, have failed, and even then, under strict monitoring and as part of a broader pain management plan.

Are there alternatives to opioids for pain management?

Yes, there are alternatives to opioids for pain management, and they include medications like non-steroidal anti-inflammatory drugs (NSAIDs), acetaminophen, and antidepressants, as well as non-pharmacological therapies. NSAIDs such as ibuprofen and aspirin are commonly used for mild to moderate pain and work by reducing inflammation. Antidepressants, particularly tricyclics and SNRIs, are effective in managing neuropathic pain by modifying neurotransmitters in the brain.

Physical therapy, cognitive behavioral therapy (CBT), acupuncture, and nerve blocks also serve as alternatives. These methods are considered safer for long-term use, with lower risks of addiction and dependence compared to opioids. While opioids are effective for short-term acute pain, alternatives provide similar or better long-term outcomes for chronic pain without the severe risks associated with opioid use.

Are prescription opioids safer than illicit opioids?

No, prescription opioids are not necessarily safer than illicit opioids. While prescription opioids are regulated and prescribed by healthcare providers to treat specific conditions, they still pose significant risks, such as dependence, overdose, and misuse. Illicit opioids, such as heroin or fentanyl purchased from unregulated sources, carry additional dangers, such as contamination with other substances and inconsistent dosages. However, the widespread availability of prescription opioids has contributed to the rise in illicit opioid use and overdose deaths, as individuals transition from prescription opioids to illegal versions when prescriptions are no longer available or become more expensive.

What is the role of opioids in the current addiction epidemic?

The role of opioids in the current addiction epidemic is central, as opioids, both prescription and illicit, have contributed significantly to the rise in substance use disorders and overdose deaths. The widespread prescribing of opioids for pain management in the 1990s and early 2000s for chronic non-cancer pain led to increased misuse and addiction. As prescriptions became harder to obtain, many individuals turned to illicit opioids, such as heroin and fentanyl, which are more potent and cheaper. The opioid epidemic has claimed hundreds of thousands of lives, with opioids involved in the majority of overdose deaths in the U.S. and globally.

Why are opioids so addictive?

Opioids are so addictive because they interact with the brain’s reward system by binding to opioid receptors, triggering the release of dopamine, a neurotransmitter associated with pleasure and reward, according to Mayo Clinic in โ€œHow opioid use disorder occurs.โ€ This surge in dopamine reinforces the behavior of taking the drug, creating a feeling of euphoria. Over time, the brain becomes dependent on the drug to release dopamine, leading to tolerance (requiring more of the drug for the same effect) and physical dependence. Withdrawal symptoms further entrench the addiction cycle, as individuals take the drug to avoid the unpleasant effects of withdrawal, making it difficult to quit.

Should you take opioids while pregnant?

No, you should not take opioids while pregnant unless absolutely necessary and prescribed by a doctor. Opioids pass through the placenta to the developing fetus, which leads to withdrawal symptoms in the newborn (neonatal abstinence syndrome) and other complications such as preterm birth, low birth weight, and respiratory issues, according to Medline Plus in โ€œPregnancy and Opioids.โ€ If opioid use is necessary for pain management, healthcare providers recommend the lowest effective dose and monitor both the mother and baby closely.

Can opioids cause permanent damage?

Yes, opioids can cause permanent damage, particularly with prolonged use or misuse. Long-term opioid use leads to physical dependence, addiction, and changes in the brainโ€™s reward system, which is sometimes irreversible. Chronic opioid use also causes hormonal imbalances, liver damage (especially with acetaminophen-containing opioids), and damage to organs like the heart and lungs, particularly when combined with other substances. Overdose leads to long-term neurological impairment or brain damage from lack of oxygen (hypoxia), according to a study by Winstanley EL et al. 2021, titled โ€œNeurocognitive impairments and brain abnormalities resulting from opioid-related overdoses: A systematic review.โ€

What are street names for opioids?

The street names for opioids vary depending on the specific drug, but some common terms include “oxy,” “percs” (for Percocet), “oxys” (for OxyContin), “smack” (for heroin), “dope,” “China White” (for fentanyl), and “fent” (for fentanyl). These slang terms are used to disguise the illicit nature of opioid use and make the drugs more socially acceptable within certain groups.

What is the most commonly abused opioid?

The most commonly abused opioid is heroin, a powerful illicit drug derived from morphine. It is highly addictive and is linked to a significant number of opioid-related deaths worldwide. Heroin abuse remains prevalent, with many individuals turning to it as a cheaper alternative to prescription opioids. According to the National Center for Drug Abuse statistics in โ€œHeroin Statistics,โ€ annually, 14,000 Americans die from heroin overdoses, while 902,000 use heroin each year, and 6.25 million Americans have used it at some point in their lifetime. The opioid epidemic has exacerbated heroin misuse, contributing significantly to overdose deaths and widespread addiction.

What Is the History of Opioids?

The history of opioids dates back to ancient civilizations where the opium poppy was used for its pain-relieving properties. In the 19th century, morphine was isolated from opium and became widely used, leading to the development of heroin in the late 1800s. In the 20th century, concerns over addiction and abuse led to stricter regulation, particularly in the U.S. The 1970 Controlled Substances Act classified opioids as controlled substances, and the opioid epidemic has since raised significant public health and legal concerns.

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Published on: March 22nd, 2017

Updated on: January 6th, 2025

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A treatment center will attempt to verify your health insurance benefits and/or necessary authorizations on your behalf. Please note, this is only a quote of benefits and/or authorization. We cannot guarantee payment or verification eligibility as conveyed by your health insurance provider will be accurate and complete. Payment of benefits are subject to all terms, conditions, limitations, and exclusions of the memberโ€™s contract at time of service. Your health insurance company will only pay for services that it determines to be โ€œreasonable and necessary.โ€ The treatment center will make every effort to have all services preauthorized by your health insurance company. If your health insurance company determines that a particular service is not reasonable and necessary, or that a particular service is not covered under your plan, your insurer will deny payment for that service and it will become your responsibility.


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Your addiction does not have to define who you are.

You deserve excellent care and a rewarding life in recovery.