Analgesic Drugs Overview
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Questions and Answers

Which condition may be paradoxically induced by prolonged exposure to opioids?

  • Respiratory depression
  • Euphoria
  • Hyperalgesia (correct)
  • Hypotension
  • What effect is primarily associated with μ receptor activation in opioids?

  • Dysphoria
  • Hallucinations
  • Respiratory depression (correct)
  • Increased gastrointestinal motility
  • What unwanted effect can occur with the use of codeine, even at subanalgesic doses?

  • Nausea
  • Euphoria
  • Hyperalgesia
  • Constipation (correct)
  • What typically happens to nausea and vomiting following morphine administration over time?

    <p>They usually disappear with repeated administration (B)</p> Signup and view all the answers

    What is a common gastrointestinal effect of opioids?

    <p>Increased intestinal smooth muscle tone (B)</p> Signup and view all the answers

    What specific feature is indicative of opioid poisoning?

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

    Which of the following is NOT a consequence of opioid use?

    <p>Euphoria through κ receptor activation (B)</p> Signup and view all the answers

    What rapid intervention can reverse respiratory depression caused by opioids?

    <p>Intravenous administration of naloxone (A)</p> Signup and view all the answers

    What is primarily responsible for the development of tolerance to opioids?

    <p>Down-regulation of opioid receptors (D)</p> Signup and view all the answers

    Which opioid is least likely to cause significant physical dependence when used?

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

    The symptoms of withdrawal syndrome from opioids may include all of the following EXCEPT:

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

    Which of the following methods can reduce withdrawal syndrome in opioid-dependent individuals?

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

    Which type of opioid is known as a mixed agonist/antagonist?

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

    Which drug is primarily used to manage severe pain in conditions like myocardial infarction?

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

    What is the primary route for administering methadone for chronic pain management?

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

    What are µ-receptor antagonists used for in opioid treatment?

    <p>To relieve withdrawal symptoms (D)</p> Signup and view all the answers

    What is the main action of major analgesics on the body?

    <p>They block pain pathways at the central nervous system level. (D)</p> Signup and view all the answers

    Which of the following best describes visceral pain?

    <p>It originates from thoracic or abdominal structures and is poorly localized. (B)</p> Signup and view all the answers

    Which neurotransmitter is NOT known to inhibit pain transmission in the nociceptive pathway?

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

    What function do anti-inflammatory drugs serve in the context of pain management?

    <p>They inhibit the inflammatory process to alleviate pain. (C)</p> Signup and view all the answers

    What is the role of endogenous opioids in pain modulation?

    <p>They inhibit the transmission of pain signals. (D)</p> Signup and view all the answers

    Which of the following substances is classified as a minor analgesic?

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

    The latex from the capsule of which plant is a source of opioid alkaloids?

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

    What defines neuropathic pain?

    <p>It originates from damage to the peripheral nervous system. (C)</p> Signup and view all the answers

    What is a significant reason for using fentanyl over morphine in anesthesia?

    <p>Fentanyl has minimal cardiovascular effects. (B)</p> Signup and view all the answers

    Which opioid is specifically indicated for analgesia during labor?

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

    What is a notable pharmacological action of methadone?

    <p>Effective long-term treatment for opioid use addiction. (D)</p> Signup and view all the answers

    Which statement about morphine is true?

    <p>It causes respiratory depression in overdose situations. (D)</p> Signup and view all the answers

    What is the primary reason naloxone is administered?

    <p>To reverse respiratory depression caused by opioids. (D)</p> Signup and view all the answers

    Why is codeine rarely addictive compared to other opioids?

    <p>It causes less euphoria than morphine. (C)</p> Signup and view all the answers

    What adverse effect is related to meperidine's antimuscarinic profile?

    <p>Blurring of vision. (D)</p> Signup and view all the answers

    Which of the following opioids is less potent than morphine?

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

    Which statement correctly describes the mechanism of action of tramadol?

    <p>It inhibits the reuptake of serotonin and noradrenaline while being a weak agonist. (A)</p> Signup and view all the answers

    What is a primary indication for buprenorphine as an opioid analgesic?

    <p>Treatment of opioid dependence in outpatient settings. (A)</p> Signup and view all the answers

    Which property makes naloxone a suitable choice for treating opioid overdose?

    <p>It is rapidly metabolized and has a quick onset of action. (B)</p> Signup and view all the answers

    What potential effect can buprenorphine have on a person who is physically dependent on a full opioid agonist?

    <p>It may precipitate withdrawal symptoms. (C)</p> Signup and view all the answers

    What differentiates naltrexone from naloxone in terms of duration of action?

    <p>Naltrexone has a longer half-life than naloxone. (C)</p> Signup and view all the answers

    Which of the following conditions is tramadol NOT typically indicated for?

    <p>Severe acute pain from trauma (C)</p> Signup and view all the answers

    What is a significant safety feature of tramadol compared to most opioids?

    <p>It produces minimal cardiovascular and respiratory depression. (C)</p> Signup and view all the answers

    Which of the following accurately describes why opioids might be contraindicated in certain patients?

    <p>They can lead to respiratory depression especially in asthmatics. (C)</p> Signup and view all the answers

    Which statement accurately describes the use of naltrexone in patients with opioid addiction?

    <p>It should only be used after completing medically supervised opioid withdrawal. (D)</p> Signup and view all the answers

    What is typically indicated for chronic primary pain conditions?

    <p>Conditions like fibromyalgia lack an identifiable cause. (B)</p> Signup and view all the answers

    How do opioids combined with paracetamol or aspirin primarily interact?

    <p>They produce synergy rather than simple additivity. (A)</p> Signup and view all the answers

    What is a common feature of neuropathic pain?

    <p>It is caused by dysfunction in the nervous system. (D)</p> Signup and view all the answers

    Which of the following medications is primarily used to manage trigeminal neuralgia?

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

    What characterizes fibromyalgia in terms of symptoms?

    <p>It is known for widespread pain and allodynia. (A)</p> Signup and view all the answers

    Which of the following is not a characteristic of chronic secondary pain?

    <p>It includes non-specific low back pain. (C)</p> Signup and view all the answers

    What is considered a benefit of using various antidepressants in pain management?

    <p>They provide therapeutic benefits for chronic pain. (A)</p> Signup and view all the answers

    Flashcards

    Analgesia

    The elimination of pain sensation by blocking pain pathways or mediators, or by disconnecting pain centers.

    Analgesic drug

    A drug designed to relieve pain.

    Inflammation

    The process of the body protecting itself against infection by inflammation.

    Anti-inflammatory drug

    A drug that can stop the inflammation process.

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    Major Analgesics (Opioids/Morphine-like)

    Strong analgesics that act on the central nervous system (CNS). Used for strong pain like post-surgery, cancer, etc.

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    Minor Analgesics (Paracetamol & NSAIDs)

    Weaker analgesics that work at the periphery, blocking inflammation mediators.

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    Local anesthetics

    A drug that numbs a specific area by acting on the local nervous system.

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    Somatic Pain

    Pain that is well-defined and can be pinpointed in specific body tissues.

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    Visceral Pain

    Pain that originates in internal organs and is often poorly defined or referred to other areas.

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    Neuropathic Pain

    Pain caused by nerve damage, often due to compression or inflammation.

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    Glutamate

    A neurotransmitter involved in pain transmission.

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    Substance P

    A neurotransmitter responsible for transmitting pain information.

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    CGRP

    A neurotransmitter associated with regulating pain.

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    Serotonin

    A neurotransmitter that can reduce pain.

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    Papaver somniferum

    The plant source of opium, containing morphine and other alkaloids.

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    Tolerance (Opioids)

    A decrease in the initial pharmacological effect of a drug after repeated or long-term use.

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    Physical Dependence (Opioids)

    A physiological state where the body depends on a drug to function normally.

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    Opioid Withdrawal Syndrome

    A syndrome of symptoms that occur when a person who is physically dependent on opioids stops taking the drug.

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    Opioid Rotation

    The process of switching from one opioid to another to regain effectiveness when tolerance develops.

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    Opioid Agonists

    Opioids that bind to and activate mu-receptors, producing analgesia and other effects.

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    Opioid Antagonists

    Opioids that bind to and block mu-receptors, reversing opioid effects.

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    Morphine

    A strong opioid agonist used for severe pain, particularly in IV, oral, transdermal, and intrathecal forms.

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    Fentanyl

    A potent synthetic opioid agonist used for severe pain, particularly in IV and transdermal forms.

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    Opioid-induced hyperalgesia

    A state where opioid use leads to increased pain sensitivity, potentially causing pain even with light touch.

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    Respiratory depression from opioids

    A symptom of opioid use characterized by a decreased respiratory rate. It can be dangerous due to the risk of overdose.

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    Opioid-induced cough suppression

    The suppression of the cough reflex caused by certain opioids, often used to treat coughs.

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    Nausea and vomiting from opioids

    A common side effect of opioid use, affecting about 40% of patients. It's believed to be caused by the activation of the chemoreceptor trigger zone.

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    Gastrointestinal effects of opioids

    Opioids increase muscle tone in the digestive tract, leading to constipation and changes in bile flow and bladder control.

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    Pupil constriction (miosis) from opioids

    A characteristic sign of opioid use, caused by the activation of μ receptors and their interaction with the nervous system.

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    Histamine release from opioids

    Morphine can trigger histamine release from mast cells, leading to skin reactions and potential bronchoconstriction.

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    Immune system effects of opioids

    Opioids can affect the immune system, particularly natural killer cells, which help fight infections.

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    Alfentanil

    A powerful opioid analgesic that is similar to morphine but with a more rapid onset and shorter duration of action. It is used in anesthesia and can be administered intravenously, through a patient-controlled infusion, or as a transdermal patch.

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    Meperidine

    An opioid analgesic that is shorter acting than morphine and similar in potency. It is less likely to cause respiratory depression or constipation. It is used for pain relief during labor.

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    Methadone

    A synthetic opioid used for pain relief, treating opioid addiction, and managing chronic pain. It has long-lasting effects and helps to reduce craving for heroin.

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    Codeine

    An opioid analgesic that is used for both its analgesic and cough-suppressing effects.

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    Naloxone

    A drug that is used to reverse the effects of opioid overdose.

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    Opioid Side Effects

    A common side effect of opioid analgesics, such as morphine and codeine. It can cause constipation, respiratory depression, and drowsiness.

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    Tramadol: Mechanism of Action

    A type of opioid analgesic that acts as a weak agonist at µ opioid receptors, offering a better safety profile compared to other opioids. It also inhibits the neuronal reuptake of serotonin and noradrenaline.

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    Tramadol: Indications

    Tramadol is used for moderate to severe chronic pain, postoperative pain, and pain associated with neuropathy.

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    Buprenorphine: Mechanism of Action

    Buprenorphine, a mixed opioid agonist/antagonist, partially activates µ-opioid receptors while blocking -opioid receptors.

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    Buprenorphine: Indications

    Buprenorphine is approved for outpatient treatment of opioid dependence and indicated for moderate to severe pain. However, be aware that it might trigger withdrawal symptoms in individuals dependent on full opioid agonists.

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    Naloxone: Mechanism of Action

    A pure opioid antagonist that blocks the actions of both endogenous opioid peptides and morphine-like drugs by binding to all three classic opioid receptors.

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    Naloxone: Indications

    Naloxone is used to reverse opioid overdosage, treat newborn respiratory depression, detect opioid addiction, and manage opioid-induced constipation.

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    Naltrexone: Mechanism of Action

    A longer-acting opioid antagonist than Naloxone, used to block the effects of opioid drugs.

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    Naltrexone: Indications

    Naltrexone is used to treat opioid addiction, including alcohol dependence, and is available as a slow-release subcutaneous implant.

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    Opioid Addiction Maintenance Therapy

    The use of a drug, such as naltrexone, to reduce opioid cravings and prevent relapse in individuals who have undergone detoxification.

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    Opioid Synergy

    Combining opioids with other pain relievers, like paracetamol (acetaminophen) or aspirin, can enhance pain relief while minimizing side effects.

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    Chronic Secondary Pain

    Pain that persists for a long time and has a known underlying cause, such as diabetes, shingles, or surgery.

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    Chronic Primary Pain

    Pain lasting for an extended period without a clear identifiable cause.

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    Fibromyalgia

    A chronic disorder characterized by widespread musculoskeletal pain, fatigue, and sleep disturbances.

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    Allodynia

    An exaggerated pain response to a normally non-painful stimulus.

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    Cancer Pain

    Pain caused by a tumor pressing on surrounding tissues, nerves, or bones, or due to treatments like surgery or chemotherapy.

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    Study Notes

    Analgesic Drugs

    • Analgesia is the elimination of pain sensation by blocking pain pathways or disconnecting pain centers.
    • Analgesic drugs are designed to relieve pain.
    • Inflammation is the body's response to protect against infection and injury.
    • Anti-inflammatory drugs inhibit the inflammatory process by targeting factors involved in inflammation and pain.

    Types of Analgesics

    • Major Analgesics (opioids/morphine-like): act centrally and are used for post-operative, oncological, myocardial infarction, acute or chronic pain.
    • Minor Analgesics (paracetamol and NSAIDs): act peripherally by blocking inflammation mediators.
    • Local Anesthetics (e.g., lidocaine): provide local action on peripheral nerves.

    Types of Pain

    • Somatic pain: well-localized pain in skin, subcutaneous tissue, or musculoskeletal tissue.
    • Visceral pain: poorly localized pain originating in thoracic or abdominal structures, often referred to somatic areas.
    • Neuropathic pain: pain caused by nerve damage (e.g., nerve compression, inflammation, diabetes).

    Modulatory Mechanisms in Nociceptive Pathway

    • Nociceptors are activated by stimuli (chemical, mechanical, thermal).
    • Ascending pain pathways transmit pain signals from nociceptors to the brain.
    • Descending inhibitory pathways from the brain reduce pain signals.
    • Key neurotransmitters involved include glutamate, substance P, and CGRP.
    • Analgesics can either activate or inhibit these pathways.

    Analgesic Drugs - Opioids

    • Opioid: any substance that produces morphine-like effects.
    • Opiate: compounds found in opium poppy (e.g., morphine, codeine).
    • Narcotic Analgesic: older term for opioids, referring to their sleep-inducing properties.
    • Opioids act by inhibiting neurotransmitter release and causing hyperpolarization.

    Opioid Receptors

    • Opioid receptors are linked to Gi/Go proteins.
    • µ-receptors are primarily responsible for analgesia and can cause euphoria, sedation, respiratory depression, and constipation.
    • δ-receptors contribute to analgesia at the spinal level and may cause sedation, dysphoria, and hallucinations.
    • κ-receptors contribute to analgesia at the spinal level as well, and may cause sedation, dysphoria, and hallucinations.
    • NOP receptors have an anti-opioid effect and are involved in reducing learning and causing immobility

    Opioid Effects

    • Analgesia: pain relief.
    • Dysphoria/Euphoria: mood changes, can range from unpleasant to pleasurable depending on circumstances
    • Inhibition of cough reflex,
    • Miosis (pupillary constriction)
    • Physical dependence
    • Respiratory Depression
    • Tolerance:Decreased effectiveness with chronic use.

    Opioids - Specific Drugs

    • Morphine: used for acute severe pain. Available as IV, oral, transdermal patches, and intrathecally. Has slow-release preparations to increase duration of action
    • Fentanyl: potent opioid agonist; more rapid onset & shorter duration of action, minimal cardio effects. Used in anesthesia and chronic pain.
    • Meperidine : Used for analgesia during labor and short-term acute pain treatment . It does not reduce uterine contraction strength.
    • Methadone: heroin substitution treatment. Acts on opioid receptors, reducing withdrawal symptoms without euphoria
    • Codeine: antitussive, reliable oral absorption but weaker than morphine.
    • Oxycodone/Hydrocodone: moderate to severe pain, slow-release oral preparations.
    • Tramadol: weak u-opioid agonist; better safety profile, minimal tolerance/dependence.
    • Buprenorphine: mixed opioid agonist/antagonist; safer in cases of overdose, opioid dependence treatment.
    • Naloxone Pure Opioid antagonist, used to reverse respiratory depression.
    • Naltrexone: longer-acting than naloxone, useful for prolonged opioid addiction treatment.

    Chronic pain

    • Secondary chronic pain originates from known causes like nerve damage, infection etc.
    • Primary chronic pain has no known cause.

    Other Pain Relieving Drugs

    • Cannabinoids: useful for multiple sclerosis neuropathic pain (Nabilone, Dronabinol)
    • Botulinum toxin: relieves back pain and spasticity.
    • Nefopam: amine uptake inhibitor, treats persistent pain unresponsive to non-opioid drugs.
    • Dopamine receptor agonists: (ropinirole, pramipexole, Rotigotine): useful for restless leg syndrome.

    Use of Opioids and Pain Killers in Combination

    Opioids combined with paracetamol or aspirin can produce synergy (stronger effect) rather than simple additivity.

    Mechanism of Action of Opioids

    • Opioids primarily work by activating Gi/Go protein-coupled receptors.
    • Activation of these receptors leads to the opening of K+ channels and preventing voltage-gated Ca2+ channels.
    • This decreased neuronal excitability and reduced transmitter release result in an inhibitory effect at a cellular level.

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    Description

    This quiz covers the essential concepts of analgesic drugs, including the different types such as major, minor, and local anesthetics. Learn about how these drugs function to relieve various types of pain and the body's inflammatory response. Ideal for students and professionals in the medical and pharmaceutical fields.

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