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Questions and Answers
What are the two main categories of endogenous opioids?
What are the two main categories of endogenous opioids?
Endorphins and enkephalins
Which of the following is NOT a function regulated by endogenous opioids?
Which of the following is NOT a function regulated by endogenous opioids?
What is the original prototype for opioid analgesics?
What is the original prototype for opioid analgesics?
Morphine
Which opioid receptor is considered the most important for mediating the analgesic effects of many opioids, especially morphine?
Which opioid receptor is considered the most important for mediating the analgesic effects of many opioids, especially morphine?
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Which of the following is NOT a classification of opioids?
Which of the following is NOT a classification of opioids?
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Which of the following opioids is considered a strong agonist?
Which of the following opioids is considered a strong agonist?
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Which of the following opioids is a mixed agonist-antagonist?
Which of the following opioids is a mixed agonist-antagonist?
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Naloxone is an opioid agonist that produces analgesia.
Naloxone is an opioid agonist that produces analgesia.
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Which of the following is a common route of administration for opioid analgesics?
Which of the following is a common route of administration for opioid analgesics?
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What is the primary site of metabolic inactivation for opioid analgesics?
What is the primary site of metabolic inactivation for opioid analgesics?
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What is the mechanism of action for opioid analgesics?
What is the mechanism of action for opioid analgesics?
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Which of the following is NOT a common adverse effect of opioid analgesics?
Which of the following is NOT a common adverse effect of opioid analgesics?
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Tolerance to opioids is a common phenomenon, where higher doses are required to achieve the same effect over time.
Tolerance to opioids is a common phenomenon, where higher doses are required to achieve the same effect over time.
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Which of the following is the most serious adverse effect associated with opioids?
Which of the following is the most serious adverse effect associated with opioids?
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What is the most commonly used medication to treat opioid addiction?
What is the most commonly used medication to treat opioid addiction?
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Glucocorticoids are nonsteroidal anti-inflammatory drugs (NSAIDs).
Glucocorticoids are nonsteroidal anti-inflammatory drugs (NSAIDs).
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Which of the following is a common adverse effect of nonsteroidal anti-inflammatory drugs (NSAIDs)?
Which of the following is a common adverse effect of nonsteroidal anti-inflammatory drugs (NSAIDs)?
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Acetaminophen has significant anti-inflammatory properties like aspirin.
Acetaminophen has significant anti-inflammatory properties like aspirin.
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What is the primary mechanism by which NSAIDs work?
What is the primary mechanism by which NSAIDs work?
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Which of the following is NOT a subtype of the cyclooxygenase (COX) enzyme?
Which of the following is NOT a subtype of the cyclooxygenase (COX) enzyme?
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Aspirin is a selective COX-2 inhibitor.
Aspirin is a selective COX-2 inhibitor.
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Which of the following is a COX-2 selective drug?
Which of the following is a COX-2 selective drug?
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What is the name of the syndrome associated with aspirin use in children and teenagers?
What is the name of the syndrome associated with aspirin use in children and teenagers?
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Acetaminophen is generally preferred over NSAIDs for long-term management of rheumatoid arthritis (RA).
Acetaminophen is generally preferred over NSAIDs for long-term management of rheumatoid arthritis (RA).
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What is the primary goal of drug treatment for rheumatoid arthritis (RA)?
What is the primary goal of drug treatment for rheumatoid arthritis (RA)?
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Which of the following drug categories is typically NOT employed in the initial treatment of RA?
Which of the following drug categories is typically NOT employed in the initial treatment of RA?
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DMARDs (Disease-Modifying Antirheumatic Drugs) typically show immediate effects, reducing inflammation and pain within a few days.
DMARDs (Disease-Modifying Antirheumatic Drugs) typically show immediate effects, reducing inflammation and pain within a few days.
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Which of the following is a type of DMARD?
Which of the following is a type of DMARD?
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Glucocorticoids are generally considered safer for long-term use than DMARDs.
Glucocorticoids are generally considered safer for long-term use than DMARDs.
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Which of the following is a characteristic of osteoarthritis (OA)?
Which of the following is a characteristic of osteoarthritis (OA)?
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The primary focus of treatment for OA is to reduce inflammation.
The primary focus of treatment for OA is to reduce inflammation.
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Which of the following is a common nonpharmacological intervention for OA?
Which of the following is a common nonpharmacological intervention for OA?
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What is the name of the drug category that aims to slow or reverse the pathological changes in OA?
What is the name of the drug category that aims to slow or reverse the pathological changes in OA?
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Viscosupplementation is a form of drug therapy specifically designed to treat rheumatoid arthritis (RA).
Viscosupplementation is a form of drug therapy specifically designed to treat rheumatoid arthritis (RA).
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Patient-controlled analgesia (PCA) is most commonly used for which type of pain?
Patient-controlled analgesia (PCA) is most commonly used for which type of pain?
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In PCA, patients are typically given a single, large dose of medication at the start of treatment.
In PCA, patients are typically given a single, large dose of medication at the start of treatment.
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Which of the following is NOT a route of administration commonly used in PCA?
Which of the following is NOT a route of administration commonly used in PCA?
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What is the term for the minimum amount of time allowed between each demand dose in PCA?
What is the term for the minimum amount of time allowed between each demand dose in PCA?
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PCA is typically associated with a high risk of serious side effects.
PCA is typically associated with a high risk of serious side effects.
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Which of the following is a potential rehab implication of PCA?
Which of the following is a potential rehab implication of PCA?
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PTs should closely monitor patients using PCA for any signs of respiratory depression or excessive sedation, as this could indicate an overdose.
PTs should closely monitor patients using PCA for any signs of respiratory depression or excessive sedation, as this could indicate an overdose.
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Study Notes
Opioid Analgesics
- Opioids are used to treat moderate to severe pain, often after surgery, trauma, or in advanced cancer or end-of-life care.
- They can cause substance use disorder and tolerance.
- Morphine is the original prototype opioid.
- Opioids are classified as: strong agonists, mild-to-moderate agonists, mixed agonist-antagonists, and antagonists.
Endogenous Opioids
- Endogenous opioids (endorphins and enkephalins) regulate functions like pain relief, euphoria, stress resilience, cardiovascular protection, and food intake control.
Opioid Receptors
- Three major opioid receptor categories exist: mu, kappa, and delta receptors.
- Each receptor class has several subclasses.
- Stimulation of any of these receptors causes analgesia.
- Mu receptors are in the brain and spinal cord, and are most important for mediating analgesic effects of opioids, especially morphine.
- Mu receptor stimulation leads to more significant side effects like respiratory depression and constipation, as well as opioid abuse and addiction.
Classification of Opioids
- Strong Agonists: Used for severe pain; examples include morphine, fentanyl, meperidine (Demerol), and methadone (Methadose).
- Mild-to-Moderate Agonists: More effective for moderate pain; examples include codeine, hydrocodone, and oxycodone.
- Mixed Agonist-Antagonists: Exhibit both agonist and antagonist activity; examples include buprenorphine – used for opioid treatment disorders; reduce the risk of fatal overdose and have fewer addictive qualities, but may have psychotropic effects like hallucinations and vivid dreams
- Antagonists: Block opioid receptors; examples include naloxone (Narcan) and used to treat opioid overdoses and addiction; they do not produce analgesia.
Pharmacokinetics
- Opioids can be administered orally, suppository form, IV, Subcutaneous or intramuscular injection, transdermal patches (e.g., fentanyl), lozenges or lollipops.
- Long-acting formulas (extended-release) are needed for some opioids due to poor intestinal absorption and first-pass effects..
- Iontophoresis may be used to enhance effects.
- Opioids are distributed equally throughout body tissues, and their main effects occur after reaching the central nervous system (CNS).
- Metabolic inactivation takes place in the liver, with some in the lungs, kidneys, and CNS.
- Excretion is in urine.
Mechanism of Action
- Opioids act on neuronal receptors in the brain, spinal cord, and peripheral tissues.
- The analgesic effects arise from modifying synaptic activity at these receptors.
Effects
- Spinal Effects: Opioids act in the spinal cord to inhibit painful impulses traveling to the brain.
- Supraspinal (Brain) Effects: Opioids act in the brain to remove inhibition in descending pathways that decrease pain.
- Peripheral Effects: Opioids act in the periphery to decrease the excitability of sensory neurons, inhibiting transmission of pain toward the spinal cord.
Treatment of Pain
- Opioid analgesics work best for moderate to severe, constant pain.
- They are less effective for sharp, intermittent pain.
- Clinically used for surgery, trauma, MI, and chronic pain with cancer.
- Mild-to-moderate opioid agonists are often administered first, followed by stronger agonists, and then parenteral administration.
- Opioids often alter pain perception more than eliminate pain; patients may not perceive pain, and experience euphoria.
- Parenteral routes like epidural or intrathecal injections may be more effective for chronic severe pain.
- Oral opioids given at regular intervals are most effective.
- Plasma levels should be maintained within a therapeutic range for optimal results.
Other Uses of Opioids
- Used as premedication or an adjunct to general anesthesia.
- Used as cough suppressors (e.g., codeine).
- Decrease GI motility to control severe diarrhea.
Adverse Effects of Opioids
- Sedative properties (mental slowing and drowsiness).
- Euphoria.
- Respiratory depression (most serious side effect).
- GI distress (nausea, vomiting, constipation).
Addiction, Tolerance, and Dependence
- Addiction: Repeated ingestion for mood alteration and pleasure.
- Tolerance: Progressive increase in dosage to achieve a therapeutic effect.
- Physical Dependence: Onset of withdrawal symptoms when drug is abruptly removed.
- Withdrawal symptoms include body aches, diarrhea, fever, goosebumps, irritability, shivering, sweating, tachycardia, nausea and vomiting, and weakness.
- Risk of tolerance and dependence is low if opioids are used appropriately.
Opioid-Induced Hyperalgesia
- Some patients don't respond to opioids or experience increased pain.
- Possible causes include genetic factors.
- The physician needs to be notified if a patient does not improve or experience worsening pain after starting opioid therapy.
Treating Addiction of Opioids
- Methadone is used to treat opioid addiction.
- It's an opioid agonist (like morphine) with milder withdrawal symptoms.
- Buprenorphine and naltrexone are also used for opioid dependence, with buprenorphine acting as a mixed agonist-antagonist and naloxone acting as an antagonist.
Rehab Considerations Regarding Use of Opioids
- Side effects, such as sedation and GI discomfort, can be problematic during therapy.
- Pain relief from opioids allows for better tolerance of therapy sessions.
- Schedule sessions around peak effect of the medication.
- These drugs can cause respiratory depression and hypoxia and hypercapnia may be seen.
- Respiratory response during rehab exercises can be reduced.
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
- NSAIDs decrease inflammation and relieve mild to moderate pain.
- They also reduce the risk of blood clotting (inhibiting platelet aggregation).
- Aspirin is the original NSAID.
- Acetaminophen is similar to aspirin but doesn't have anti-inflammatory or anticoagulant properties.
- NSAIDs interfere with the synthesis of prostaglandins, which are hormones that regulate cell function under normal and pathological conditions.
Prostaglandins
- Prostaglandin production increases with injury.
- Prostaglandins play a critical role in inflammation, pain, and fever.
- Inhibiting prostaglandin synthesis can help manage inflammation, pain, and fever.
How NSAIDs Work
- NSAIDs work by inhibiting cyclooxygenase (COX) enzymes, which are crucial in prostaglandin synthesis.
- COX exists in two forms; COX-1 and COX-2.
- COX-1 produces prostaglandins that maintain homeostasis in various cells.
- COX-2 is primarily produced in injured cells for inflammation and pain responses.
- Aspirin and traditional NSAIDs are nonselective, inhibiting both COX-1 and COX-2, potentially causing adverse effects due to inhibition of beneficial COX-1.
- Selectively inhibiting COX-2 minimizes side effects linked to widespread reduction of prostaglandins, such as gastric damage.
COX-1 and COX-2
- COX-1 produces prostaglandins that maintain normal cell activities.
- COX-2 produces prostaglandins that mediate pain and other aspects of the inflammatory response.
Aspirin
- The oldest NSAID, chemically known as acetylsalicylic acid.
- Used to manage musculoskeletal pain and joint disorders.
- Reduces the need for opioids after surgery.
- Used to prevent blood clots in conditions like heart attacks and strokes (CVA).
- Effective in treating fever in adults.
- Can help prevent colorectal cancer and other GI cancers.
- Can cause gastric damage and kidney damage if used long term.
Side Effects of NSAIDs
- GI Damage: GI hemorrhage and ulceration due to loss of protective prostaglandins.
- Cardiovascular Issues: Decreases platelet activity, reduces clots, but may increase blood pressure, increasing risk of thrombotic events. This risk is greatest for patients with pre-existing hypertension (HTN) or other cardiac risk factors, particularly with COX-2 selective drugs.
- Hepatic and Renal Effects: Excessive use or existing liver disease can cause adverse changes in hepatic function. Potential for increased risk of kidney problems in patients with impaired renal function, diabetes mellitus (DM), heart failure, or those with decreased body water.
- Aspirin Toxicity: Overdose can cause aspirin intoxication or poisoning, leading to various symptoms, including headaches, tinnitus (ringing in the ears), difficulty hearing, confusion, gastrointestinal distress, and metabolic acidosis.
- Reye's Syndrome: Aspirin is associated with Reye's syndrome (only in children and teens, with high fever, vomiting, liver dysfunction, coma, and potentially death).
Aspirin vs. NSAIDs
- NSAIDs are often more costly than aspirin.
- Some NSAIDs cause less GI discomfort than aspirin but have other potential adverse effects.
- Certain NSAIDs may be less toxic to other organs than aspirin (like the liver and kidneys).
COX-2 Selective Drugs
- Selective COX-2 inhibitors (e.g., celecoxib) have fewer gastrointestinal issues than nonselective NSAIDs but may increase the risk of cardiovascular problems, some of which were withdrawn from the market because of these increased risks.
- Celecoxib remains the only COX-2 selective drug on the market.
Acetaminophen
- Commonly known as Tylenol.
- Equivalent to NSAIDs and aspirin for pain relief and fever reduction.
- Not associated with upper GI irritation (in contrast to NSAIDs).
- Used widely for non-inflammatory conditions that have mild to moderate pain, especially when previous ulcers are a concern, such as in people with osteoarthritis (OA).
- Appropriate for children and teenagers with fever
Acetaminophen, High Doses
- Large doses can be toxic to the liver, potentially fatal (15 grams or more).
- People with pre-existing liver disease are at particular risks from acetaminophen.
Thoughts for Physical Therapists
- The drugs discussed provide analgesia without significant sedation.
- Patient concerns include stomach discomfort.
- Patients may need clarification on differences in over-the-counter pain medications like aspirin, acetaminophen, and ibuprofen.
Management of RA & OA
Rheumatoid Arthritis (RA)
- A chronic, systemic disease causing synovitis and cartilage destruction.
- RA causes pain, stiffness, and inflammation in joints; often impacting small joints in the hands and feet and larger joints like the knee.
- RA is a progressive condition, leading to severe joint destruction and bone erosion.
- Juvenile rheumatoid arthritis affects children younger than 16 in the same way as adult RA.
- RA leads to decreased quality of life and increased risk of cardiovascular and other co-morbidities.
- The cause is an autoimmune response.
Drug Treatment of RA
- Goals include decreasing joint inflammation and halting disease progression.
- Treatment types include Nonsteroidal anti-inflammatory drugs (NSAIDs), glucocorticoids, and disease-modifying antirheumatic drugs (DMARDs).
NSAIDs and RA
- Aspirin and NSAIDs were commonly used initially to treat RA but are now often used when combined with other medications.
- Glucocorticoids help reduce inflammation more strongly than NSAIDs but have potential for serious side effects.
- NSAID selection for patients with RA is often based on trial and error to find the most effective type for that person.
COX-2 Inhibitors and RA
- COX-2 inhibitors might be less toxic to the stomach and other tissues in patients with RA than traditional NSAIDs but pose a risk of heart attack and stroke.
Acetaminophen and RA
- Not recommended primary treatment for RA because of its lack of anti-inflammatory effects.
Glucocorticoids
- Effective in reducing inflammation (corticosteroids).
- Helpful for acute flares and exacerbations of RA.
- Often necessary in combination with DMARDs; used to manage inflammation while awaiting the effect of the less potent DMARD.
- Often given in higher doses in severe cases that last for a short period.
- Should be avoided in those with pre-existing osteoporosis or other risks of osteoporosis.
Adverse Effects of Glucocorticoids
- Increased risk of osteoporosis and other adverse effects like muscle wasting, hypertension, aggravation of diabetes mellitus, glaucoma, cataracts, and infections.
- Patients should use these medications cautiously and in accordance with their physician's recommendations.
Disease-Modifying Antirheumatic Drugs (DMARDs)
- Medications that slow the progression of RA, halt and reverse the disease, and improve quality of life, potentially halting bone erosion.
- It includes subgroups like Antimalarials, Nonbiological DMARDs, Biological DMARDs, Tumor Necrosis Factor Inhibitors, and Other DMARDs.
Antimalarials
- Medications from this class are used to treat RA by affecting immune cells.
- Hydroxychloroquine is FDA-approved, and chloroquine may be prescribed off-label.
- High doses are associated with eye damage.
- Should have regular eye exams.
Methotrexate
- Used in cancer treatment and RA, especially in children and adults.
- More potent than other DMARDs; generally shows faster results in controlling RA symptoms.
- Much lower doses are needed than in cancer treatment.
- Adverse effects: severe gastrointestinal problems, pulmonary problems, and hematological disorders.
Tumor Necrosis Factor Inhibitors
- Medications aimed at reducing inflammation through targeting TNF-a.
- Used in initial treatments for RA.
- Effective, but may have negative side effects..
JAK Inhibitors
- Used as a last resort if other DMARDs fail to control the RA.
- Orally administered.
- Potential for serious cardiovascular issues and gastrointestinal perforation.
Other DMARDs
- Immunosuppressants used in preventing rejection after transplants, treating cancer, or treating inflammatory bowel disease (IBS).
- Reserved for those who don't respond to other, more common, DMARDs due to their more significant potential for toxicities.
Combining DMARDs
- Using combinations can help increase benefits by keeping doses lower for each medication.
- Increased potential for drug interactions and toxicity.
- Combining different DMARDs is a common strategy to treat RA effectively.
Diet and RA
- Diets containing fish oil and omega-3 fatty acids may lessen RA symptoms by controlling inflammation.
- Foods with antioxidant properties may lessen symptoms such as those rich in fruits and vegetables.
Osteoarthritis (OA)
- A degenerative joint disease that causes articular cartilage deterioration and resulting in bone changes, with high prevalence among the older adults.
- Not an autoimmune disease.
- Treatment focuses primarily on nonpharmacological interventions such as physical therapy (PT), weight loss, or surgery.
OA: Acetaminophen and NSAIDs
- Acetaminophen and NSAIDs are often the first-line treatments for managing OA pain, but do not actually change the course of the disease.
- NSAIDs may also possess anti-inflammatory properties that help with joint inflammation present with OA
Viscosupplementation
- A type of DMOAD for OA that uses hyaluronan (hyaluronic acid) to replace synovial fluid in joints to improve viscosity & joint mobility, decreasing joint destruction and improving pain and function.
Glucosamine & Chondroitin Sulfate
- Dietary supplements that may protect or reverse cartilage deterioration in OA, and are sometimes used in conjunction with other treatments.
Acetaminophen Dosages
- Geriatric patients and healthy adults have different maximal daily limits
- Common dosages for acetaminophen are 325mg, 500mg and are found in various combination products like Norco®
What Kind of Pain Medication is it?
- This table lists common over-the-counter and prescription pain medications, and indicates their category (opioid, NSAID, or acetaminophen).
Comparison of Side Effects
- Detailed table comparing potential side effects of opioids, NSAIDs (aspirin, ibuprofen, etc), Cox-2 Selective Drugs, and Acetaminophen.
Patient-Controlled Analgesia (PCA)
- A drug delivery method where patients control their analgesic administration through a pump.
- Reduces side effects because drug concentrations are consistently administered; this is typically used during or after surgery in patients with chronic pain or cancer pain.
- Different types of pumps for PCA are available, including intravenous (IV) pumps, epidural pumps, regional pumps, and oral pumps.
PCA Terminology
- Loading dose: Initial large dose to rapidly achieve therapeutic window.
- Demand dose: Amount of drug the patient can self-administer at a given time.
- Lockout interval: Minimum wait time between demand doses.
- Background infusion rate: Continuously administered low dose in some PCA systems.
Types of Analgesia used for PCAs
- Opioids: The primary medication for PCAs.
- Non-opioid analgesics: Can be combined to reduce the need for strong opioids, improving patient tolerance.
- Local anesthetics: Used for localized pain relief, such as epidural analgesia.
IV PCA
- Intravenous (IV) administration is the most common type of PCA.
- Small, intermittent doses are delivered directly into the systemic circulation through a catheter.
Epidural PCA
- Drugs are administered into the area outside the spinal cord's meninges.
- Less risky than other administration methods; better for longer-term use.
Regional PCA & Oral Route
- Peripheral sites - Medication injected locally.
- Oral route: Medication for pain relief given through oral administration.
Comparison of PCA to Other Analgesics
- PCA is rated higher by patients, often preferred to other methods like continuous infusions.
PCA Adverse Effects
- Side effects of opioids used in PCA are similar to other opioid administration methods such as sedation, GI problems, and respiratory depression.
Rehabilitation Implications
- Patients receiving PCA demonstrate reduced sedation and increased alertness.
- Therapy scheduling can be simplified without need to coordinate around medication administrations, because drug levels are more steady.
- Improved mobility is possible because pain relief is maintained between therapy treatments.
- Clinicians should be aware of PCA dysfunction risks that could lead to harmful side effects like respiratory depression or excessive sedation.
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This quiz covers essential concepts related to opioid analgesics, including their classification, uses, and effects on pain management. You'll learn about endogenous opioids and the major opioid receptors, focusing on how they regulate analgesia and other physiological functions. Test your knowledge on this critical topic in pharmacology.
