Chapter 8 - Drugs to Treat Pain: Opioid Analgesics
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Questions and Answers

Why are nonpharmacologic and nonopioid pharmacologic therapies preferred over opioid therapy in the treatment of chronic pain?

Because the potential risks and harms often outweigh the benefits in treating chronic pain.

According to the CDC guidelines, when should immediate-release opioids be prescribed?

Only for treating acute pain.

What is the primary mechanism of action for opioid drugs?

Binding to opioid receptors, primarily located in the central nervous system, the peripheral nervous system, and the gastrointestinal tract.

What is the significance of the mu-opioid receptor (MOR) in opioid action?

<p>It is the major analgesic opioid receptor, and its activation produces the analgesic, euphoric, and sedative effects associated with opioid addiction.</p> Signup and view all the answers

Why might an oral dose of an opioid need to be higher than a parenteral dose to elicit a therapeutic effect?

<p>Because of the first-pass effect, which reduces the bioavailability of the opioid.</p> Signup and view all the answers

Describe the onset and peak effect of opioid analgesics administered orally.

<p>The onset is approximately 45 minutes, and the peak effect usually occurs 1 to 2 hours after administration.</p> Signup and view all the answers

Explain how nasal insufflation of certain opioids can achieve therapeutic blood levels quickly.

<p>By avoiding first-pass metabolism, nasal insufflation directly delivers the opioid to the bloodstream, resulting in rapid absorption and therapeutic levels.</p> Signup and view all the answers

What are the primary therapeutic effects of opioid analgesics on the central nervous system?

<p>Analgesia, euphoria, sedation, and respiratory depression.</p> Signup and view all the answers

How do opioid analgesics affect different types of pain?

<p>They relieve continuous dull pain more effectively than sharp, intermittent pain.</p> Signup and view all the answers

What are the potential adverse effects of opioid analgesics when administered to pain-free patients?

<p>Drowsiness, difficulty in mentation, apathy, and reduced physical activity.</p> Signup and view all the answers

What is the relationship between dose and the risk of fatal overdose with opioids?

<p>As the dose increases, the risk of fatal overdose increases.</p> Signup and view all the answers

What are the recommended steps for prescribers to follow regarding opioid therapy for chronic pain?

<p>Establish and measure pain and function goals, discuss benefits and risks, recommend nonopioid therapies, start low and go slow, taper and discontinue if needed.</p> Signup and view all the answers

What is the rationale behind the CDC's recommendation to not prescribe extended-release or long-acting opioids for acute pain?

<p>The risk of overdose and adverse effects is higher with extended-release opioids, and they are not necessary for acute pain management.</p> Signup and view all the answers

What is the role of the first-pass effect in opioid pharmacokinetics?

<p>It reduces the bioavailability of opioids, meaning less of the drug reaches systemic circulation after oral administration.</p> Signup and view all the answers

Why is the uptake of opioids by various organs and tissues influenced by both physiologic and chemical factors?

<p>Physiological factors, such as blood flow and tissue permeability, and chemical factors, such as drug binding to specific receptors, all contribute to the distribution of opioids in the body.</p> Signup and view all the answers

What is the primary purpose of opioids in pain management as per the WHO’s analgesic ladder?

<p>Opioids are used to provide effective pain relief after nonopioids and are categorized into low-potency and high-potency.</p> Signup and view all the answers

Differentiate between the terms 'opioid' and 'opiate'.

<p>Opioids refer to drugs or chemicals that interact with opioid receptors, while opiates are natural compounds derived from opium.</p> Signup and view all the answers

Identify the opioid discussed that has an extremely high potency and is associated with many trade names.

<p>Fentanyl is the opioid with extremely high potency associated with many trade names.</p> Signup and view all the answers

What is the role of naloxone in opioid treatment?

<p>Naloxone, marketed as Narcan, is an opioid antagonist used to reverse opioid overdoses.</p> Signup and view all the answers

According to the data from 1999 to 2017, what percentage of drug overdose deaths involved opioids?

<p>67.8% of drug overdose deaths involved opioids.</p> Signup and view all the answers

Explain the meaning of 'endogenous opioids' and give an example.

<p>Endogenous opioids are naturally occurring peptides that bind to opioid receptors, with beta-endorphin being a specific example.</p> Signup and view all the answers

How has the age-adjusted drug overdose death rate changed from 1999 to 2017?

<p>The rate increased from 6.0 to 21.7 deaths per 100,000 people.</p> Signup and view all the answers

What is the historical origin of the term 'narcotic'?

<p>The term 'narcotic' comes from the Greek word 'narkotikos', meaning numbing or stupor.</p> Signup and view all the answers

What is the primary purpose of combining antidepressants and anticonvulsants in pain management?

<p>To enhance analgesic effects and achieve a synergistic outcome in certain pain states.</p> Signup and view all the answers

List two common opioid medications prescribed for pain relief.

<p>Oxycodone and hydrocodone.</p> Signup and view all the answers

What is the maximum daily dosage for Norco containing 325 mg acetaminophen and 5 mg hydrocodone?

<p>8 tablets.</p> Signup and view all the answers

Why might opioids be prescribed on an around-the-clock basis for chronic pain?

<p>To ensure consistent pain management and to prevent breakthrough pain episodes.</p> Signup and view all the answers

What is a common side effect of opioid use that necessitates patient education?

<p>Opioid-induced constipation.</p> Signup and view all the answers

What are two major risks associated with opioid use highlighted by the FDA?

<p>Addiction and life-threatening respiratory depression.</p> Signup and view all the answers

What role do patient assessments play before prescribing opioids?

<p>They help evaluate pain complaints and identify risk factors for opioid misuse or abuse.</p> Signup and view all the answers

How does the FDA recommend handling dosing for opioids?

<p>Using the lowest effective dose for the shortest duration consistent with treatment goals.</p> Signup and view all the answers

What is the significance of the 'Red Flag' sidebar mentioned in opioid prescribing?

<p>It lists characteristics of opioid addiction to help prescribers identify at-risk patients.</p> Signup and view all the answers

Which medications can enhance the analgesic effect when used with opioids?

<p>NSAIDs and non-opioid analgesics.</p> Signup and view all the answers

What is a key consideration when prescribing extended-release opioids?

<p>They should only be used for chronic pain management and not on an as-needed basis.</p> Signup and view all the answers

How do physical dependence and tolerance develop in opioid use?

<p>They result from extended use, especially at higher dosages over time.</p> Signup and view all the answers

What important patient education should occur alongside opioid prescriptions?

<p>Counseling on proper fluid and fiber intake to prevent constipation.</p> Signup and view all the answers

What combination consists of Oxycodone and acetaminophen?

<p>Percocet.</p> Signup and view all the answers

What role do cytochrome P450 enzymes play in opioid metabolism?

<p>Cytochrome P450 enzymes facilitate metabolic reactions necessary for opioid metabolism in the liver.</p> Signup and view all the answers

Identify two key symptoms of opioid use disorder (OUD).

<p>Inability to control opioid use and uncontrollable cravings are two key symptoms of OUD.</p> Signup and view all the answers

Explain why adipose tissue accumulation can be significant for opioids despite lower blood flow.

<p>Adipose tissue can accumulate opioids, especially after frequent high-dose administration, acting as a reservoir even with its lower perfusion.</p> Signup and view all the answers

What is the purpose of the WHO 3-step pain relief ladder?

<p>The WHO 3-step pain relief ladder promotes the use of conservative therapies before initiating opioid therapy.</p> Signup and view all the answers

Why is monitoring renal function important prior to high-potency opioid administration?

<p>Patients with renal insufficiency risk sedation and respiratory depression when given high-potency opioids.</p> Signup and view all the answers

What is the impact of alternating as-needed dosing schedules on pain management?

<p>As-needed dosing can cause fluctuations in analgesic plasma concentrations, leading to uncontrolled pain and sedation.</p> Signup and view all the answers

How do antidepressants like amitriptyline enhance morphine-induced analgesia?

<p>Antidepressants may enhance morphine-induced analgesia by augmenting its effects in chronic neuropathic pain contexts.</p> Signup and view all the answers

What should be considered when transitioning a patient from opioids to anti-inflammatory medications post-surgery?

<p>Patients with high pain tolerance may transition from opioids following surgery to anti-inflammatory medications safely.</p> Signup and view all the answers

What constitutes a vicious cycle in opioid pain management?

<p>A vicious cycle occurs when wide swings in analgesic plasma concentrations necessitate increasing amounts of medication for relief.</p> Signup and view all the answers

Why is the combination of opioids with drugs that have the same mechanism of action generally not warranted?

<p>Combining opioids with drugs that have the same mechanism may lead to unnecessary increased risks without added benefit.</p> Signup and view all the answers

What are endogenous opioids and give one example?

<p>Endogenous opioids are naturally occurring peptide ligands for opioid receptors; an example is beta-endorphin.</p> Signup and view all the answers

How has the rate of drug overdose deaths involving opioids changed between 1999 and 2017?

<p>The age-adjusted drug overdose death rate significantly increased from 6.0 deaths per 100,000 in 1999 to 21.7 in 2017.</p> Signup and view all the answers

Explain the significance of synthetic opioids in the context of overdose deaths.

<p>Synthetic opioids, particularly illicitly manufactured fentanyl, were involved in a significant number of overdose deaths, illustrating their potency and danger.</p> Signup and view all the answers

What is the controversy surrounding the use of opioids in chronic noncancer pain management?

<p>The practice is controversial due to rising overdose rates and concerns about addiction, despite potential effectiveness for pain relief.</p> Signup and view all the answers

Discuss the historical origin of the term 'narcotic' and its relevance today.

<p>The term 'narcotic' originates from the Greek word for 'numbing' and is often legally associated with opioids and drugs that pose addiction risks.</p> Signup and view all the answers

What role does naloxone play in the context of opioid therapy?

<p>Naloxone is an opioid antagonist used to reverse the effects of opioid overdose, providing a critical safety measure for individuals using opioid medications.</p> Signup and view all the answers

How do physical dependence and tolerance manifest in opioid use?

<p>Physical dependence and tolerance develop as the body adapts to the presence of opioids, requiring higher doses to achieve the same effect and leading to withdrawal symptoms upon cessation.</p> Signup and view all the answers

What is the importance of the WHO 3-step pain relief ladder in opioid prescription practices?

<p>The ladder prioritizes nonopioids first and escalates to low- then high-potency opioids, guiding clinicians to promote safer, stepwise pain management.</p> Signup and view all the answers

What is the maximum number of tablets of Norco that can be taken in a 24-hour period?

<p>8 tablets.</p> Signup and view all the answers

What are the risks associated with the concomitant use of opioids and benzodiazepines?

<p>Profound sedation, respiratory depression, coma, and death.</p> Signup and view all the answers

Name an antidepressant that can enhance the analgesic effect of opioids.

<p>Amitriptyline.</p> Signup and view all the answers

What is the clinical significance of opioid-induced constipation (OIC) in patients using opioids?

<p>It impacts patient quality of life and may necessitate additional treatments.</p> Signup and view all the answers

Why is it essential to assess a patient’s risk factors before prescribing opioids?

<p>To minimize the risk of addiction, abuse, and overdose.</p> Signup and view all the answers

What dosing regimen is indicated for opioids during chronic pain management?

<p>Every 3 to 6 hours.</p> Signup and view all the answers

What precaution should be taken when prescribing extended-release opioids?

<p>They should only be used for chronic pain on an around-the-clock basis.</p> Signup and view all the answers

What should patients be counseled about to prevent opioid-induced constipation?

<p>Intake of fluids and fiber, and possibly using a laxative.</p> Signup and view all the answers

What is the maximum recommended daily dosage for Norco containing 5 mg of hydrocodone?

<p>12 tablets, if taken as 1 tablet every 6 hours.</p> Signup and view all the answers

What specific patient evaluations should be conducted prior to opioid prescription?

<p>Assessment of pain, functionality goals, and risk factors for misuse.</p> Signup and view all the answers

Describe a characteristic that defines opioid addiction according to the Red Flag sidebar.

<p>Behavioral changes such as increased tolerance or secretive drug-seeking behavior.</p> Signup and view all the answers

What medications listed can be used in combination with opioids for pain management?

<p>Tramadol and certain antidepressants.</p> Signup and view all the answers

What common side effect of opioids requires patient education regarding dietary adjustments?

<p>Constipation.</p> Signup and view all the answers

In what situation might the use of extended-release opioids be inappropriate?

<p>For acute pain management.</p> Signup and view all the answers

Which opioid medication combination includes acetaminophen and hydrocodone?

<p>Norco.</p> Signup and view all the answers

What factors influence the concentration of opioids in different tissues after entering the bloodstream?

<p>Opioid concentration in tissues is influenced by blood flow, tissue perfusion rate, and the lipophilicity of the drug.</p> Signup and view all the answers

How does first-pass metabolism affect the efficacy of opioid medications?

<p>First-pass metabolism in the liver can significantly reduce the amount of active drug entering systemic circulation, potentially requiring higher doses for effect.</p> Signup and view all the answers

Why are polar metabolites primarily excreted in urine after opioid use?

<p>Polar metabolites are water-soluble, allowing for their efficient elimination through the kidneys into the urine.</p> Signup and view all the answers

Explain the significance of renal insufficiency in the context of opioid dosing.

<p>Patients with renal insufficiency may have impaired drug clearance, which increases the risk of sedation and respiratory depression from opioids.</p> Signup and view all the answers

What are the implications of the WHO 3-step pain relief ladder in opioid therapy?

<p>The WHO ladder advocates for using milder analgesics before escalating to opioids, ensuring pain management starts with the least invasive treatments.</p> Signup and view all the answers

How might a patient's pain tolerance affect their transition from opioids to alternative pain relief methods post-surgery?

<p>Patients with high pain tolerance may effectively transition to non-opioid medications sooner, reducing reliance on opioids for pain management.</p> Signup and view all the answers

What criteria must be present to diagnose opioid use disorder (OUD) based on the symptoms outlined?

<p>A diagnosis of OUD requires at least 2 of 11 specified symptoms to be present within a 1-year period.</p> Signup and view all the answers

Describe the role of combination therapy in opioid pain management.

<p>Combination therapy can provide enhanced pain relief by pairing opioids with non-opioid analgesics while avoiding overlapping effects.</p> Signup and view all the answers

What does the term 'vicious cycle' refer to in the context of opioid pain management?

<p>'Vicious cycle' refers to the scenario where alternating pain and sedation lead to increased medication requirements and dependency.</p> Signup and view all the answers

Why is it important to evaluate the patient's exercise habits and hygiene when diagnosing opioid use disorder?

<p>Changes in exercise habits and hygiene can indicate the impact of opioid use on a patient's overall health and lifestyle.</p> Signup and view all the answers

What are the potential benefits of combining opioid therapy with nonpharmacologic interventions?

<p>Combining opioid therapy with nonpharmacologic interventions can enhance pain relief and improve functional outcomes while potentially reducing the required dosage of opioids.</p> Signup and view all the answers

Why is the measurement of pain and functional goals important prior to initiating opioid therapy?

<p>Measuring pain and functional goals prior to treatment helps clinicians tailor therapy to individual patient needs and assess treatment efficacy over time.</p> Signup and view all the answers

What is the significance of starting with the lowest effective dosage when prescribing opioids?

<p>Starting with the lowest effective dosage minimizes the risk of adverse effects and overdose while allowing for gradual adjustments based on patient response.</p> Signup and view all the answers

Explain why opioids are considered a second-line therapy for chronic pain management.

<p>Opioids are considered second-line therapy because nonpharmacologic and nonopioid pharmacologic treatments are generally preferred due to their lower risk of dependency and side effects.</p> Signup and view all the answers

How does the delay in analgesic effect for oral opioids impact their use in acute pain management?

<p>The delay, which is approximately 45 minutes for onset and 1-2 hours for peak effect, necessitates alternative routes or medications for immediate pain relief in acute situations.</p> Signup and view all the answers

What recommendations does the CDC provide regarding follow-up care for patients on opioids?

<p>The CDC recommends regular follow-up to reevaluate patient risks, adjust dosages, and potentially taper or discontinue opioids if risks outweigh benefits.</p> Signup and view all the answers

Describe how the psychoactive effects of opioids can contribute to the development of addiction.

<p>Psychoactive effects, such as euphoria and sedation, increase the potential for misuse and addiction as patients may seek these effects alongside pain relief.</p> Signup and view all the answers

What role does the mu-opioid receptor play in the action of opioids?

<p>The mu-opioid receptor mediates the analgesic, euphoric, and sedative effects of opioids, and its activation is crucial for their therapeutic action.</p> Signup and view all the answers

In what situations should immediate-release opioids be prescribed according to CDC guidelines?

<p>Immediate-release opioids should be prescribed only to manage acute pain, ensuring they are not used for chronic pain management or routine therapy.</p> Signup and view all the answers

Why is reevaluation of opioid therapy essential during patient follow-up appointments?

<p>Reevaluation is essential to ensure that the treatment remains effective, to monitor for adverse effects, and to adjust or discontinue therapy as necessary.</p> Signup and view all the answers

Discuss how pharmacokinetics can affect the clinical effectiveness of opioid administration routes.

<p>Pharmacokinetics, such as absorption and distribution, vary by route of administration, impacting onset and duration of pain relief and necessitating individualized treatment plans.</p> Signup and view all the answers

What are the implications of the first-pass effect on opioid medication dosing?

<p>The first-pass effect can significantly reduce bioavailability of orally administered opioids, necessitating higher doses compared to parenteral routes to achieve therapeutic effects.</p> Signup and view all the answers

Highlight the risks associated with prescribing extended-release or long-acting opioids for acute pain.

<p>Prescribing extended-release or long-acting opioids for acute pain can increase the risk of overdose and dependency due to prolonged drug exposure without necessary monitoring.</p> Signup and view all the answers

How does the combination of opioids with non-opioid medications enhance pain management?

<p>Combining opioids with non-opioid medications can provide more effective pain relief while reducing the dosage requirements and side effects associated with opioids.</p> Signup and view all the answers

Which term refers to compounds structurally related to products found in opium?

<p>Opiate (D)</p> Signup and view all the answers

The term 'narcotic' exclusively refers to drugs that induce sleep.

<p>False (B)</p> Signup and view all the answers

What is the name of a specific endogenous opioid also referred to as endorphin?

<p>beta-endorphin</p> Signup and view all the answers

The term opioid is generally used to refer to drugs or chemicals that interact with __________ in the body.

<p>opioid receptors</p> Signup and view all the answers

According to the provided information, which category was the most common in opioid-involved deaths?

<p>Synthetic opioids other than methadone (D)</p> Signup and view all the answers

Match the following medications with their respective classifications:

<p>Codeine = Opioid, low potency Morphine = Opioid, medium potency Fentanyl = Opioid, extremely high potency Naloxone = Opioid, antagonist</p> Signup and view all the answers

What is the name of the opioid antagonist?

<p>Naloxone (B)</p> Signup and view all the answers

What term is derived from the Greek word 'opos' meaning 'juice'?

<p>opium</p> Signup and view all the answers

Which of the following tissues serves as the main reservoir for opioid accumulation due to its bulk, despite having lower drug concentrations?

<p>Skeletal muscle (A)</p> Signup and view all the answers

Opioids are primarily excreted unchanged in urine.

<p>False (B)</p> Signup and view all the answers

What class of enzymes in the liver is essential for opioid metabolism?

<p>cytochrome P450 enzymes</p> Signup and view all the answers

The diagnosis for OUD requires presentation of at least 2 of 11 criteria over a ______ period of time.

<p>one year</p> Signup and view all the answers

Match the following terms with their corresponding descriptions:

<p>Lipophilic = Able to cross cell membranes First-pass metabolism = Processing of a drug by the liver before systemic circulation Enterohepatic circulation = Reabsorption of drugs from bile back into circulation PRN dosing = Administering medication as needed</p> Signup and view all the answers

According to the provided text, which of the following symptoms is NOT a characteristic of Opioid Use Disorder (OUD)?

<p>Weight gain (C)</p> Signup and view all the answers

Weaker opioids should always be the initial treatment for all types of pain.

<p>False (B)</p> Signup and view all the answers

What is the typical starting point for opioid dosing schedules?

<p>a starting dose</p> Signup and view all the answers

In a chronic pain state with periodic breakthrough pain, a patient might receive a slow-release opioid for baseline pain relief and a ______ opioid for the breakthrough pain.

<p>rapid-onset</p> Signup and view all the answers

Which of the following is a consequence of as-needed (PRN) dosing schedules for opioids, as discussed in the text?

<p>Alternating states of uncontrolled pain and sedation (A)</p> Signup and view all the answers

Which of the following is NOT a primary effect of opioid analgesics on the central nervous system?

<p>Increased alertness (B)</p> Signup and view all the answers

Extended-release opioids are recommended for the treatment of acute pain.

<p>False (B)</p> Signup and view all the answers

What is the preferred route of administration for opioid medications, whenever possible?

<p>oral</p> Signup and view all the answers

Opioid drugs act by binding to _______ receptors, primarily located in the CNS, the peripheral nervous system, and the gastrointestinal tract.

<p>opioid</p> Signup and view all the answers

Match the opioid effect to the description:

<p>Analgesia = Reduction or disappearance of pain Euphoria = A sense of intense well-being and pleasure Sedation = A state of calm or drowsiness Respiratory depression = Decrease in the rate and depth of breathing</p> Signup and view all the answers

According to the CDC guidelines, what should prescribers do regarding dosages when initiating opioid therapy?

<p>Start low and go slow, using the lowest effective dosage. (D)</p> Signup and view all the answers

Opioid analgesics are more effective at relieving sharp, intermittent (incident) pain than continuous dull pain.

<p>False (B)</p> Signup and view all the answers

What is the main analgesic opioid receptor that binds with opioids like morphine and heroin?

<p>mu-opioid receptor (MOR)</p> Signup and view all the answers

The onset of analgesic effect for oral opioid medications is approximately _______ minutes.

<p>45</p> Signup and view all the answers

Match the administration route with its effect:

<p>Oral = Slower onset of effect (45 min), preferred route when possible Intravenous (IV) = Rapid onset of effect, used when oral is not feasible Intranasal (IN) = Rapid therapeutic blood levels due to avoiding first-pass metabolism Intramuscular (IM) = Moderate absorption rate, useful when IV is not available</p> Signup and view all the answers

Which of the following best describes the CDC’s recommendation regarding opioid therapy for chronic pain?

<p>Nonpharmacologic and nonopioid pharmacologic therapies are preferred. (B)</p> Signup and view all the answers

When opioids are used for chronic pain, they should be prescribed alone, without additional therapies.

<p>False (B)</p> Signup and view all the answers

What is the term for the effect that reduces the bioavailability of an opioid following oral administration?

<p>first-pass effect</p> Signup and view all the answers

The activation of the _______ is responsible for the analgesic, euphoric, and sedative effects of opioid drugs.

<p>MOR</p> Signup and view all the answers

Match the term with its meaning:

<p>Analgesic = A drug that relieves pain Agonist = A drug that binds to a receptor and produces a response Bioavailability = The extent to which a drug is absorbed and reaches the systemic circulation First-pass effect = Metabolism of a drug before it reaches the systemic circulation</p> Signup and view all the answers

Which of the following medications is a combination of hydrocodone and acetaminophen?

<p>Norco (B)</p> Signup and view all the answers

Extended-release opioids are best used for as-needed pain management.

<p>False (B)</p> Signup and view all the answers

What is a common side effect of opioid use that requires patient counseling?

<p>opioid-induced constipation</p> Signup and view all the answers

The FDA recommends that opioids should be reserved for patients for whom alternative treatment options are ______, not tolerated, or otherwise inadequate.

<p>ineffective</p> Signup and view all the answers

Match the following medications with their generic names:

<p>Demerol = Meperidine Dilaudid = Hypromorphone Vicoprofen = Hydrocodone and ibuprofen Ultram = Tramadol</p> Signup and view all the answers

Which of the following is NOT a primary FDA opioid warning?

<p>Increased appetite and weight gain (A)</p> Signup and view all the answers

Physical dependence on opioids can only occur with misuse and abuse.

<p>False (B)</p> Signup and view all the answers

What type of medication, other than opioids, may enhance the analgesic effect and be synergistic in some pain states?

<p>antidepressants and anticonvulsants</p> Signup and view all the answers

The lowest effective ______ for the shortest duration should be used when prescribing opioid medication.

<p>dose</p> Signup and view all the answers

Match the opioid medication with their trade names:

<p>Meperidine = Demerol Hypromorphone = Dilaudid Oxycodone = Oxycontin Tramadol = Ultram</p> Signup and view all the answers

Concomitant use of opioids with what drug class can result in profound sedation, respiratory depression, coma, and death?

<p>Benzodiazepines (A)</p> Signup and view all the answers

Around-the-clock opioid dosing is usually used for breakthrough pain.

<p>False (B)</p> Signup and view all the answers

What is the medication called that is a narcotic pain reliever used to treat moderate to severe pain?

<p>Tramadol</p> Signup and view all the answers

Patients on opioid therapy should be counseled on proper intake of fluids and ______ to mitigate constipation.

<p>fiber</p> Signup and view all the answers

Match the opioid combinations:

<p>Hydrocodone and acetaminophen = Norco, Lortab, Vicodin Oxycodone and acetaminophen = Percocet Codeine and acetaminophen = Tylenol with codeine Hydrocodone and ibuprofen = Vicoprofen</p> Signup and view all the answers

Which of the following terms specifically refers to compounds structurally related to products found in opium?

<p>Opiate (D)</p> Signup and view all the answers

Codeine is classified as an extremely high potency opioid.

<p>False (B)</p> Signup and view all the answers

What is the name of the opioid antagonist that can be used to reverse an opioid overdose?

<p>naloxone</p> Signup and view all the answers

The term narcotic was derived from the Greek word __________, meaning numbing or stupor.

<p>narkotikos</p> Signup and view all the answers

Match the following opioid classifications with their corresponding examples:

<p>Opioid, low potency = Codeine Opioid, medium potency = Morphine Opioid, extremely high potency = Fentanyl Opioid, antagonist = Naloxone</p> Signup and view all the answers

According to the data provided, which category was involved in the most opioid overdose deaths?

<p>Synthetic opioids other than methadone (A)</p> Signup and view all the answers

Endorphins are synthetic opioids produced in labs.

<p>False (B)</p> Signup and view all the answers

What is the origin of natural opiates?

<p>opium poppy</p> Signup and view all the answers

What is the primary organ responsible for the extensive first-pass metabolism of most opioids?

<p>Liver (A)</p> Signup and view all the answers

Adipose tissue has a higher blood flow than highly perfused tissues, which significantly affects opioid accumulation.

<p>False (B)</p> Signup and view all the answers

Name one symptom of opioid use disorder (OUD).

<p>Inability to control opioid use</p> Signup and view all the answers

Opioids should be administered with caution in patients with __________ due to the risk of sedation and respiratory depression.

<p>renal insufficiency</p> Signup and view all the answers

Match the following opioids with their primary use:

<p>Morphine = Chronic pain management Methadone = Pain management and opioid addiction treatment Oxycodone = Moderate to severe pain relief Fentanyl = Severe pain management</p> Signup and view all the answers

Which of the following is a reason for tapering opioid doses?

<p>To avoid withdrawal symptoms (A), To minimize side effects (C)</p> Signup and view all the answers

The use of combinations of opioids with the same mechanism of action is generally recommended.

<p>False (B)</p> Signup and view all the answers

What is the significance of cytochrome P450 enzymes in opioid metabolism?

<p>They facilitate metabolic reactions.</p> Signup and view all the answers

Patients experiencing __________ pain may benefit from a combination of opioids and NSAIDs.

<p>inflammatory</p> Signup and view all the answers

What is a common effect associated with opioid use that requires patient education?

<p>Respiratory depression (B)</p> Signup and view all the answers

Tramadol is used primarily for treating mild pain.

<p>False (B)</p> Signup and view all the answers

Name one opioid medication prescribed commonly in sports medicine.

<p>Demerol</p> Signup and view all the answers

The maximum daily dosage for Norco with 325 mg acetaminophen and 5 mg hydrocodone is _____ tablets.

<p>8</p> Signup and view all the answers

Match the following opioids with their trade names:

<p>Oxycodone = Oxycontin Hydrocodone and acetaminophen = Percocet Codeine and acetaminophen = Tylenol with codeine Tramadol = Ultram</p> Signup and view all the answers

Which of the following statements about opioid-dependent patients is incorrect?

<p>Tolerance to opioids cannot develop. (A)</p> Signup and view all the answers

Opioid-induced constipation is a common side effect of opioid therapy.

<p>True (A)</p> Signup and view all the answers

What should be monitored in patients administered opioids during dose increases?

<p>Respiratory depression</p> Signup and view all the answers

The recommended approach is to use the lowest effective dose for the shortest duration consistent with individual patient _____ goals.

<p>treatment</p> Signup and view all the answers

What is a common condition that might require a stimulant laxative for opioid patients?

<p>Opioid-induced constipation (B)</p> Signup and view all the answers

Patients should not be educated about opioid risks when prescribed opioids.

<p>False (B)</p> Signup and view all the answers

What is one risk associated with concomitant use of opioids and benzodiazepines?

<p>Profound sedation</p> Signup and view all the answers

What class of drugs is often used on the second step of the WHO pain ladder?

<p>Opioids (C)</p> Signup and view all the answers

Opioids are recommended to be used only when _____ treatment options are ineffective.

<p>alternative</p> Signup and view all the answers

What is a characteristic of opioid addiction according to the FDA?

<p>Risk of misuse</p> Signup and view all the answers

Which of the following is NOT a recommendation from the CDC guidelines for prescribers regarding opioid use for chronic pain?

<p>Opioids should be first-line or routine therapy for chronic pain. (A)</p> Signup and view all the answers

The oral route is the preferred method for administering opioid medications.

<p>True (A)</p> Signup and view all the answers

What is the primary effect of opioid analgesics on the central nervous system?

<p>Analgesia (pain relief)</p> Signup and view all the answers

Opioid analgesics bind to ______ receptors, primarily located in the central nervous system, peripheral nervous system, and gastrointestinal tract.

<p>opioid</p> Signup and view all the answers

Match the following terms with their definitions:

<p>Analgesia = The reduction or absence of pain Euphoria = A state of euphoria or feeling of well-being Sedation = A state of calmness or drowsiness Respiratory depression = Reduced breathing rate First-pass effect = The metabolism of a drug by the liver before it reaches systemic circulation</p> Signup and view all the answers

What is the primary mechanism of action for the majority of opioid drugs?

<p>Binding to mu-opioid receptors (A)</p> Signup and view all the answers

Nasal insufflation of certain opioids can lead to rapid therapeutic blood levels due to bypassing the first-pass effect.

<p>True (A)</p> Signup and view all the answers

What is the significance of the first-pass effect in relation to opioid pharmacokinetics?

<p>It reduces the bioavailability of the drug, often requiring a higher oral dose to achieve a therapeutic effect.</p> Signup and view all the answers

Which of the following is an example of a nonopioid pharmacologic therapy that can be used to treat chronic pain?

<p>Gabapentin (A)</p> Signup and view all the answers

Opioid analgesics are more effective at relieving sharp, intermittent pain associated with movement than continuous dull pain.

<p>False (B)</p> Signup and view all the answers

The CDC guidelines recommend that prescribers should ______ the dose or taper and discontinue opioids if the risks of harm outweigh the benefits.

<p>reduce</p> Signup and view all the answers

Match the following routes of administration with their abbreviations:

<p>Intravenous = IV Intramuscular = IM Subcutaneous = SQ Intranasal = IN Oral = PO</p> Signup and view all the answers

What are two common opioid medications prescribed for pain relief?

<p>Oxycodone and Hydrocodone</p> Signup and view all the answers

What is the recommended approach for prescribing opioids for acute pain?

<p>Prescribe only the lowest effective dosage and for the shortest duration necessary. (D)</p> Signup and view all the answers

Opioids are more effective at relieving chronic pain than acute pain.

<p>False (B)</p> Signup and view all the answers

Which of the following tissues serves as the primary reservoir for opioids due to its greater bulk, despite having lower concentrations?

<p>Skeletal Muscle (D)</p> Signup and view all the answers

Opioids are primarily excreted from the body in bile through enterohepatic circulation.

<p>False (B)</p> Signup and view all the answers

What is the main organ responsible for the first-pass metabolism of opioids?

<p>liver</p> Signup and view all the answers

Opioid metabolism in the liver requires that the ___________ enzymes facilitate metabolic reactions.

<p>cytochrome P450</p> Signup and view all the answers

Which of the following is NOT a commonly listed symptom of opioid use disorder (OUD)?

<p>Increased libido (B)</p> Signup and view all the answers

Match the following opioid characteristics with their descriptions:

<p>Lipophilic = Allows crossing of cell membranes to reach target tissues Polar metabolites = Excreted mainly in the urine First-pass metabolism = Occurs extensively in the liver Highly perfused tissues = Where opioids concentrate most densely</p> Signup and view all the answers

According to the WHO pain relief ladder, stronger opioids should be used when:

<p>Moderate and severe pain is not relieved by weaker options (D)</p> Signup and view all the answers

Combination therapy using drugs with the same mechanism of action is generally recommended for pain management with opioids.

<p>False (B)</p> Signup and view all the answers

What type of dosing schedule may result in alternating states of uncontrolled pain and sedation, and should be avoided?

<p>as-needed (PRN)</p> Signup and view all the answers

In a chronic pain state with periodic breakthrough pain, a patient may receive a slow-release form of morphine for baseline pain relief, with a _______ formulation to manage acute pain

<p>rapid-onset</p> Signup and view all the answers

All opioids are derived directly from the opium poppy.

<p>False (B)</p> Signup and view all the answers

What is the specific endogenous opioid also known as beta-endorphin?

<p>β-endorphin</p> Signup and view all the answers

The term narcotic was derived from the Greek word _______ for ‘numbing’ or ‘stupor’

<p>narkotikos</p> Signup and view all the answers

Match the following drug type/class with the drug name:

<p>Opioid, low potency = Codeine Opioid, medium potency = Morphine Opioid, extremely high potency = Fentanyl Opioid antagonist = Naloxone</p> Signup and view all the answers

According to the information provided, what percentage of drug overdose deaths in 2017 involved an opioid?

<p>67.8% (D)</p> Signup and view all the answers

Which category of opioids was the most common in opioid-involved deaths, specifically in reference to deaths from synthetic opioids that are not methadone?

<p>illicitly manufactured fentanyl</p> Signup and view all the answers

The age-adjusted drug overdose death rate decreased from 1999 to 2017.

<p>False (B)</p> Signup and view all the answers

Extended-release opioids are recommended for managing acute pain.

<p>False (B)</p> Signup and view all the answers

What is the preferred route of administration for opioid medications?

<p>oral</p> Signup and view all the answers

The binding of opioids to specific receptors mediates both the ______ and the somatic effects of these drugs.

<p>psychoactive</p> Signup and view all the answers

Match the opioid effect with its description:

<p>Analgesia = Pain Relief Euphoria = Feeling of intense happiness Sedation = Calming effect, reduction of alertness Respiratory depression = Decreased rate and depth of breathing</p> Signup and view all the answers

According to the CDC guidelines, which of the following should be considered before starting opioid therapy for chronic pain?

<p>The benefits must outweigh the risks to the patient (C)</p> Signup and view all the answers

Opioid analgesics are more effective for sharp intermittent pain than for continuous dull pain.

<p>False (B)</p> Signup and view all the answers

What is the most common mechanism of action for opioid drugs?

<p>MOR activation</p> Signup and view all the answers

The reduction in the bioavailability of an opioid due to metabolism in the liver is known as the ______ effect.

<p>first-pass</p> Signup and view all the answers

Match each route of administration with the approximate onset time of pain relief:

<p>Oral = 45 minutes Intravenous = Rapid Intranasal = Rapid Subcutaneous = Variable</p> Signup and view all the answers

Which of the following best describes the CDC's recommendations for starting an opioid dose?

<p>Start low and go slow (A)</p> Signup and view all the answers

Opioid use always results in slurred speech and impaired motor coordination even at therapeutic doses.

<p>False (B)</p> Signup and view all the answers

What are the two main categories of prescription opioids?

<p>natural and semisynthetic opioids and methadone</p> Signup and view all the answers

Opioid drugs act by binding to ______ located in the central and peripheral nervous systems and the gastrointestinal tract.

<p>opioid receptors</p> Signup and view all the answers

Match the opioid administration concern with its impact:

<p>First-pass effect = Reduces bioavailability of oral medications Delayed onset of oral medication = Not ideal when immediate relief is needed High oral dose requirement = Needed due to first-pass metabolism Risk of overdose = Increases with dose escalation</p> Signup and view all the answers

Extended-release opioids are generally used for acute pain on an as-needed basis.

<p>False (B)</p> Signup and view all the answers

What is a common side effect associated with opioid use that may require the addition of a stimulant laxative or stool softener?

<p>opioid-induced constipation</p> Signup and view all the answers

The FDA recommends that opioid use be reserved for patients where alternative treatment options are ________, not tolerated, or otherwise inadequate.

<p>ineffective</p> Signup and view all the answers

Concomitant use of opioids and benzodiazepines carries a low risk and is generally safe because of their similar mechanism of action.

<p>False (B)</p> Signup and view all the answers

What is the recommendation for opioid dosage duration, as per the text?

<p>Shortest duration consistent with patient goals</p> Signup and view all the answers

Physical dependence can occur even with ________ opioid use

<p>appropriate</p> Signup and view all the answers

Which of these could be considered a treatment option for opioid-induced constipation?

<p>Stimulant laxatives (C)</p> Signup and view all the answers

Patients who have no prior experience with analgesics generally do not need to have individualize dosing.

<p>False (B)</p> Signup and view all the answers

What is the name of the narcotic pain reliever that comes in both a regular and extended-release form, mentioned in the text?

<p>Tramadol</p> Signup and view all the answers

Antidepressants and anticonvulsants may enhance the ________ effect when combined with opioids.

<p>analgesic</p> Signup and view all the answers

Match the following medications with their available combinations:

<p>Oxycodone = Oxycodone and acetaminophen Hydrocodone = Hydrocodone and acetaminophen Tramadol = Tramadol extended release Codeine = Codeine and acetaminophen</p> Signup and view all the answers

What is the maximum number of Norco tablets (containing 325 mg acetaminophen and 5 mg hydrocodone) that should be taken in a day, as given in the examples?

<p>8 tablets (B)</p> Signup and view all the answers

Flashcards

Opioid

Drugs that interact with opioid receptors in the body.

Opiate

Compounds related to products found in opium.

Endogenous Opioids

Naturally occurring peptides in the brain that bind to opioid receptors.

Beta-Endorphin

A specific type of endogenous opioid peptide.

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Narcotic

Initially referred to any drug inducing sleep, now often linked to opioids.

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Fentanyl

An extremely high potency opioid, often used in severe pain.

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Naloxone

An opioid antagonist used to reverse opioid overdoses.

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WHO 3-Step Ladder

A guideline for pain management starting with nonopioids then opioids.

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Opioid Metabolism

Most opioids undergo extensive first-pass metabolism in the liver before entering circulation.

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Lipophilic Opioids

Opioids are typically lipophilic, allowing them to cross cell membranes.

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Excretion of Opioids

Polar metabolites of opioids are primarily excreted in urine; small amounts may remain unchanged.

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Renal Insufficiency Consideration

Patients with renal issues should be evaluated carefully before high-potency opioids are given.

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Criteria for OUD Diagnosis

Diagnosis requires at least 2 of 11 criteria within a year for Opioid Use Disorder.

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Symptoms of Opioid Addiction

Inability to control use, cravings, drowsiness, and changes in habits are signs of OUD.

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Dosing Guidelines for Opioids

Initiate therapy based on factors like patient's renal or liver function and pain level.

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Combination Therapy with Opioids

Combining opioids with other analgesics can be beneficial for certain pain types.

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Titration of Opioids

Opioid dosing begins with a starting dose, adjusted based on pain and side effects.

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Breakthrough Pain Management

Utilize rapid-onset formulations for acute pain in chronic pain patients already on opioids.

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Prescription Opioids

Opioids prescribed for pain relief include natural and semisynthetic types.

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CDC Guidelines for Opioids

Recommendations by the CDC for safe opioid prescribing for chronic pain.

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First-line Therapy

Opioids should not be the primary treatment for chronic pain.

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Goals for Pain and Function

Clinicians must set and evaluate goals related to pain level and functional ability.

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Immediate-release Opioids

Prescribed only for acute pain and not for chronic use.

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Start Low, Go Slow

Initiate opioid treatment with the lowest effective dose, then adjust as needed.

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Euphoric Effect of Opioids

Opioids can produce feelings of intense happiness or euphoria.

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Opioid Receptors

Proteins in the CNS and body that opioids bind to for pain and pleasure effects.

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Mu-opioid Receptor (MOR)

The main receptor that opioid drugs activate for their analgesic effects.

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Routes of Administration

Methods by which opioids can be given, including oral, IV, and others.

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First-pass Effect

The reduction in bioavailability of oral opioids because of liver metabolism.

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Analgesic Effect

The reduction or elimination of pain experienced after opioid use.

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Respiratory Depression

A serious side effect of opioids where breathing becomes slower or weaker.

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Acute vs. Chronic Pain

Acute pain is sudden and severe; chronic pain lasts longer and may be ongoing.

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Pharmacodynamics

The effects of opioids on the body, including pain relief and side effects.

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Antidepressants

Medications that can enhance analgesic effects by blocking amine reuptake.

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Anticonvulsants

Drugs like gabapentin that may augment pain relief effects.

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Analgesic combinations

Mixing different pain medications for better efficacy.

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Demerol

Trade name for Meperidine, an opioid pain reliever.

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Dilaudid

Trade name for Hypromorphone, a potent opioid analgesic.

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Norco

Combination of hydrocodone and acetaminophen for pain relief.

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Oxycontin

Time-released formulation of Oxycodone for acute pain management.

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Percocet

Combination of oxycodone and acetaminophen for pain relief.

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Tylenol with codeine

A mix of codeine and acetaminophen for mild to moderate pain.

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Opioid dosing guidelines

Specific dosing limits and schedules for opioid medications like Norco.

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Breakthrough pain

Sudden increase in pain despite ongoing pain management.

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Opioid-induced constipation (OIC)

A common side effect of opioid use, decreasing bowel movement frequency.

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FDA opioid warnings

Three main risks associated with opioid use: addiction, respiratory depression, and CNS depression.

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Minimum effective dose

The smallest dose necessary to achieve the desired therapeutic effect.

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Chronic pain management

Long-term treatment involving careful opioid prescription and patient monitoring.

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Low-Potency Opioids

Opioids used in the first step of WHO's pain management ladder.

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Medium-Potency Opioids

Includes opioids like Morphine, used for moderate pain.

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High-Potency Opioids

Opioids used for severe pain; includes drugs like Oxycodone.

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Heroin

An illegal opioid that is highly addictive.

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Highly perfused tissues

Tissues with high blood flow where opioids concentrate, like brain and liver.

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Skeletal muscle function

Skeletal muscle is a reservoir for opioids but has lower concentrations.

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First-pass metabolism

Process in the liver that reduces the concentration of opioids before they enter circulation.

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Cytochrome P450 enzymes

Enzymes necessary for metabolizing opioids in the liver.

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Polar metabolites

Drug byproducts excreted mainly in urine after opioid use.

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Opioid Use Disorder (OUD)

A condition requiring at least 2 of 11 criteria showing addiction-like symptoms.

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Symptoms of OUD

Includes drowsiness, cravings, and isolation from loved ones.

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WHO 3-step pain relief ladder

Guideline suggesting starting with non-opioids before strong opioids for pain management.

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Titration of opioid doses

Adjusting opioid doses based on patient pain levels and side effects.

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Combination therapy

Using opioids with other analgesics for better pain control, especially for breakthrough pain.

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Nonpharmacologic Therapy

Treatment methods that do not involve medications, such as physical therapy or acupuncture.

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Chronic Pain

Ongoing pain that lasts for months or years, often resistant to treatment.

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Risk-Benefit Analysis

Evaluating if the benefits of opioid therapy outweigh the potential risks.

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CDC Guidelines

Recommendations by the CDC to promote safe prescribing of opioids.

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Monitoring Opioid Use

Regular assessments to evaluate the effectiveness and risks of opioid therapy.

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Tapering Off Opioids

Gradually reducing opioid dosage to lower dependence and manage side effects.

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Analgesic Euphoria

Feelings of happiness or pleasure that can occur with opioid use.

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Pharmacokinetics

How the body absorbs, distributes, metabolizes, and excretes opioid medications.

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Respiratory Depression Risk

Decreased breathing rate and effectiveness, a serious side effect of opioids.

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Opioid Receptor Binding

Process by which opioids attach to receptors in the body to exert effects.

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Sustained Release Opioids

Formulations designed to release medication over a longer period for chronic pain.

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Monitoring for Adverse Effects

Assessment for undesirable side effects from opioid use, essential for patient safety.

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Synergistic Pain Relief

Combining medications like antidepressants and anticonvulsants enhances pain relief.

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Around-the-Clock Dosing

Regular opioid dosing schedule to manage persistent pain effectively.

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Extended-Release Opioids

Opioids dosed consistently for chronic pain, not as needed.

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Opioid-Induced Constipation

A significant decrease in bowel movement due to opioid use.

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Black Box Warnings

Severe safety warnings on opioid medications due to risks.

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Risk Factors for Misuse

Prior assessment of a patient's history before prescribing opioids.

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Lowest Effective Dose

Using the smallest dose needed to achieve the desired pain relief.

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Patient Monitoring

Regular checks on patients for signs of opioid misuse or addiction.

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Management of Chronic Noncancer Pain

Opioids may be prescribed cautiously for chronic pain not linked to cancer.

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Complete Pain Assessment

Thorough evaluation of pain complaints before opioid prescriptions.

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Individualized Dosing

Customizing opioid doses based on patient's past treatments and risks.

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Concomitant Use Warnings

Risks when using opioids with CNS depressants or benzodiazepines.

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Functional Goals Assessment

Evaluating patients’ goals regarding pain and functionality before treatment.

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Chronic Pain Management Strategies

Comprehensive approaches for treating long-term pain, including opioids.

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Codeine

A low potency opioid used for mild pain relief.

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Oxycodone

A medium potency opioid used for moderate to severe pain.

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Opioid Accumulation in Adipose Tissue

Opioids can accumulate in fatty tissues, especially with frequent high doses.

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Symptoms of Opioid Use Disorder (OUD)

Signs include inability to control use, cravings, and isolation.

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WHO Pain Relief Ladder

Guideline recommending stepwise treatment from non-opioids to opioids based on pain severity.

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Combination Opioids

Opioids mixed with other analgesics for better pain management.

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Risk Factors for Opioid Misuse

Considerations of a patient’s history to prevent abuse of opioids.

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Opioid Dependency Risks

Potential for addiction and physical dependence on opioid medications.

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Maximum Daily Dose for Norco

Total daily dosage of Norco should not exceed 8 tablets.

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Opioid Therapy

The use of opioids to treat pain when benefits outweigh risks.

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Euphoria from Opioids

Intense feelings of happiness that can occur with opioid use.

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Epidural Administration

A method of delivering opioids in the lower body through the epidural space.

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Combined Treatment

Using opioids alongside nonopioid therapies for comprehensive pain management.

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Hydrocodone

A medium potency opioid used for pain relief.

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Morphine

A medium potency opioid, often used in hospitals for pain.

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Endorphins

Natural opioid peptides produced by the brain that help relieve pain.

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CDC Guidelines for Prescribers

Recommendations promoting safe opioid prescribing for chronic pain management.

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First-line Therapy for Chronic Pain

Opioids should not be the primary treatment for chronic pain.

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Acute Pain Management

Utilizing opioids for immediate pain relief in short-term situations.

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Opioid Accumulation in Fatty Tissue

Opioids can build up in adipose tissue, affecting drug effects over time.

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Opioids and Renal Insufficiency

Caution is needed when prescribing high-potency opioids to patients with kidney issues.

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Dosing for Opioids

Dosing starts low and is adjusted based on pain relief and side effects such as sedation.

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Combination Drug Therapy

Using opioids with other analgesics to enhance pain relief, especially for chronic pain.

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Opioid Titration

Adjusting the opioid dose based on individual patient pain levels and side effects.

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Antidepressants in Pain Management

Antidepressants can enhance the analgesic effects of opioids for better chronic pain management.

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Tramadol

A narcotic analgesic used for moderate to severe pain management.

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Dosing Guidelines for Norco

Usual adult dosage of Norco is 1-2 tablets every 4-6 hours, with limits.

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Synthetic Opioids

Man-made opioids, often more potent, e.g., Fentanyl.

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Reservoir for Opioids

Skeletal muscle serves as a major reservoir for opioids despite lower concentrations.

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Dosing Schedule

Starts with a dose that is adjusted based on the patient's pain and side effects.

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As-Needed Dosing

Dosing schedule where medication is taken only when needed for pain relief.

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CDC Opioid Guidelines

Recommendations for safer opioid prescribing in chronic pain.

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Risks of Opioid Use

Potential harms include addiction and overdose.

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Therapeutic Effects of Opioids

Includes analgesia, euphoria, sedation, and respiratory depression.

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Opioid Administration Routes

Methods include oral, IV, IN, SQ, and others.

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Follow-up on Opioids

Clinicians should regularly reassess pain management and risks.

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Dosing Considerations

Evaluate patient's history for tailored opioid dosage.

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Adverse Effects Monitoring

Regular checks for undesirable side effects from opioid use.

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Patient Functional Goals

Goals set for pain management and functional ability.

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Medication Combinations

Using opioids with other analgesics to enhance pain control.

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Study Notes

Opioid Analgesics

  • Opioids interact with opioid receptors. Opiates are compounds from opium.
  • Endogenous opioids are naturally occurring peptides for opioid receptors in the brain. Endorphin (β-endorphin) is a specific endogenous opioid.
  • "Narcotic," from the Greek "narkotikos," means "numbing" or "stupor." Legally, narcotics are often associated with opioids.
  • Opioid use in chronic non-cancer pain is controversial. Non-pharmacological and non-opioid strategies are preferred in chronic pain management.
  • Opioids are often used in the second step on the WHO pain ladder for acute pain. This is controversial; opioids can be addictive and misused.
  • Drug selection should consider patient preferences, effectiveness, pharmacokinetics, pharmacodynamics, and side effects.
  • Patients should be counseled on fluid and fiber intake for OIC (opioid-induced constipation).
  • Opioids include analgesic drugs like codeine and morphine, and many semisynthetic and synthetic derivatives.
  • Natural opiates are derived from the opium poppy.
  • Opioid examples include: Codeine (low potency), Morphine (medium potency), Hydrocodone, Oxycodone, Fentanyl (extremely high potency), and Heroin (illegal). Naloxone (Narcan) is an opioid antagonist.
  • Examples of trade names: Codeine (many), Morphine (MS Contin), Hydrocodone (Zohydro), Oxycodone (OxyContin), Fentanyl(many), Heroin(illegal drug), Naloxone(Narcan).
  • Opioids, such as morphine, codeine, oxycodone, and hydrocodone are listed as examples of low to medium potency. Fentanyl is listed as an example of extremely high potency opioid.

Opioid Overdose Statistics

  • Between 1999 and 2017, over 700,000 drug overdose deaths occurred in the US, with 67.8% involving opioids (70,237 deaths in 2017).
  • Synthetic opioids (excluding methadone, including illicit fentanyl), were the leading cause of opioid-related deaths (28,466 deaths in 2017); prescription opioids were second (17,029).
  • Age-adjusted drug overdose death rates increased significantly from 6.0 in 1999 to 21.7 in 2017 per 100,000 people.
  • Prescription or illicit opioids were linked to 67.8% (47,600) of these deaths.

CDC Guidelines for Opioid Prescribing

  • Opioids should not be first-line treatment for chronic pain.
  • Clinicians need to establish and track pain and function goals.
  • Discuss benefits and risks of opioid treatment with patients and offer non-opioid alternatives.
  • Prescribe immediate-release opioids only for acute pain.
  • Start with the lowest effective dose and increase cautiously.
  • For acute pain, prescribe the minimal effective opioid dose.
  • Do not prescribe extended-release/long-acting opioids for acute pain.
  • Follow up with patients, reassess risk, and reduce/discontinue as needed.

Therapeutic Effects of Opioids

  • Opioids primarily affect the CNS.
  • Key effects include analgesia, euphoria, sedation, and respiratory depression.
  • Opioids effectively relieve continuous, dull pain over sharp, intermittent pain.
  • Therapeutic doses may offer pain relief or euphoria.
  • Higher doses increase sedation and adverse effects like respiratory depression, raising the overdose risk.

Mechanism of Action

  • Opioid drugs bind to opioid receptors in the CNS, peripheral nervous system, and gastrointestinal tract.
  • Morphine and heroin are mu-opioid receptor (MOR) agonists.
  • MOR activation is the primary mechanism causing analgesia, euphoria, and sedation.
  • Opioid binding mediates psychoactive and somatic effects.

Routes of Administration

  • Oral administration is preferred.
  • Intravenous, intranasal, subcutaneous, intraspinal, and intramuscular routes may also be used.
  • Oral opioids have a 45-minute onset and peak effect within 1-2 hours. Nasal insufflation can offer rapid relief.

Pharmacodynamics and Pharmacokinetics

  • Opioids generally have similar pharmacokinetics, despite various forms.
  • Absorption: Subcutaneous, intramuscular, and oral routes are generally well-absorbed. Reduced oral bioavailability often results from the first-pass effect. Oral bioavailability can be reduced by the first-pass effect, so higher doses may be needed orally than by other routes.
  • Distribution: Binding to plasma proteins leads to rapid clearance from the blood. Opioids concentrate in highly perfused tissues (brain, lungs, liver, etc.).
  • Metabolism: Primarily in the liver via cytochrome P450 enzymes. Opioids are lipophilic, crossing cell membranes easily.
  • Excretion: Polar metabolites primarily excreted in urine; some enter enterohepatic circulation. Patients with renal insufficiency with high-potency opioids require careful monitoring.

Opioid Addiction

  • Opioid Use Disorder (OUD) significantly impacts health and relationships.
  • OUD diagnosis requires at least 2 of 11 criteria in a 1-year period.
  • Symptoms include: inability to control use, cravings, drowsiness, sleep changes, weight loss, flu-like symptoms, decreased libido, lack of hygiene, exercise changes, isolation, stealing, and financial difficulties.

Dosing Guidelines

  • Patient factors (e.g., kidney/liver function) affect opioid selection.
  • WHO 3-step pain relief ladder recommends non-opioid alternatives first.
  • Opioids are considered sooner in severe pain cases.
  • Dosing schedules typically start with a baseline dose, adjusted based on pain and side effects.
  • PRN (as needed) dosing can lead to inconsistent drug levels, alternating pain and sedation states, potentially escalating use.
  • Extended-release opioids are for chronic, continuous pain, not acute pain, and are dosed around the clock.

Combination Therapy

  • Combining drugs with same mechanisms or overlapping/opposing targets isn't generally recommended (e.g., Morphine + Methadone).
  • Opioid combinations may benefit baseline/breakthrough pain.
  • Opioids can be combined with other analgesics (acetaminophen, NSAIDs).
  • Antidepressants (amitriptyline, duloxetine) and anticonvulsants (gabapentin) may enhance opioid effects.

Combinations of Analgesics, Opioids, and NSAIDs

  • Common opioid & analgesic combinations (e.g., Norco, Percocet, Tylenol with codeine) are listed.

Example Dosing Guidelines (Norco)

  • Provides dosage guidelines for Norco (hydrocodone/acetaminophen) PRN and total daily dosages.

Indications and Precautions

  • Opioid use is for acute and some chronic pain scenarios.
  • Choice should consider patient factors, effectiveness, pharmacokinetics, and side profiles, patient acceptance, analgesic effectiveness, and pharmacokinetic, pharmacodynamic, and side-effect profiles.
  • Opioids are often used in the second step of the WHO pain ladder after non-opioids for acute pain and are controversial in chronic non-cancer pain.
  • Opioids should be used in the second step of the WHO pain ladder after non-opioids for acute pain; they are controversial in chronic non-cancer pain.
  • Opioids are often considered sooner in cases of severe pain.

Opioid-Induced Constipation (OIC)

  • OIC is a common opioid side effect, reducing spontaneous bowel movements.
  • Is a significant problem for patients.

FDA Opioid Warnings

  • Risks of addiction, abuse, misuse.
  • Life-threatening respiratory depression (monitor, especially with dose changes).
  • Concomitant use with CNS depressants (e.g., benzodiazepines, alcohol) is very dangerous.
  • Opioids have black box warnings for potential harm.
  • Opioids reserved when alternatives are ineffective or inadequate.
  • Lowest effective dose for shortest duration, individualized.
  • Prescribers must individualize doses considering patient history and risk factors.
  • Specific drugs with example trade/generic names.
  • Opioids recommended as second-line treatment.

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Description

This quiz covers key concepts related to opioid analgesics, including their interaction with receptors, the origins of the term 'narcotic,' and statistics on opioid overdoses in the US. Additionally, it summarizes guidelines for opioid prescribing as advised by the CDC. Test your knowledge on this critical and timely topic.

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