Pharm - Neuro 1 MCQ (MD2)

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Questions and Answers

Which of the following best describes analgesia?

  • Increased sensitivity to painful stimuli.
  • Heightened emotional response to pain.
  • The presence of pain in response to stimulation.
  • Absence of pain in response to stimulation that would normally be painful. (correct)

What is the primary mechanism by which non-steroidal anti-inflammatory drugs (NSAIDs) exert their analgesic, anti-inflammatory, and anti-pyretic effects?

  • Inhibiting the synthesis of prostaglandins (correct)
  • Enhancing the reuptake of serotonin and norepinephrine in the brain
  • Stimulating the release of endogenous opioids
  • Directly blocking pain receptors in the central nervous system

Which of the following best describes the role of COX-1 in the body?

  • Primarily involved in platelet aggregation
  • Primarily involved in the production of fever.
  • Primarily involved in inflammation and pain.
  • Responsible for the production of prostaglandins that protect the stomach lining. (correct)

Which of the following is a potential adverse effect of non-selective NSAIDs related to their inhibition of COX-1?

<p>Increased risk of bleeding. (B)</p> Signup and view all the answers

Why are COX-2 selective inhibitors considered to have a potentially higher risk of thrombotic events compared to non-selective NSAIDs?

<p>They inhibit prostacyclin production, leading to unopposed platelet aggregation. (B)</p> Signup and view all the answers

What is the primary mechanism of action of aspirin in preventing cardiovascular events?

<p>Irreversibly inhibiting COX-1 in platelets to reduce thromboxane A2 production. (A)</p> Signup and view all the answers

Why is aspirin typically discontinued several days before a surgical procedure?

<p>To allow for the production of new platelets with functional COX-1. (A)</p> Signup and view all the answers

Which of the following statements best describes the mechanism of action of paracetamol?

<p>Inhibits prostaglandin synthesis centrally in the brain. (D)</p> Signup and view all the answers

In which of the following patient populations is paracetamol generally considered the first-line analgesic?

<p>Patients with impaired renal function. (A)</p> Signup and view all the answers

What is the primary pathway of paracetamol metabolism, and how does an overdose affect this pathway?

<p>Glucuronidation; in overdose, NAPQI production overwhelms glutathione stores (D)</p> Signup and view all the answers

What concerning effect can result from paracetamol overdose due to the accumulation of NAPQI?

<p>Fulminant liver failure. (A)</p> Signup and view all the answers

Which of the following is NOT a typical effect of NSAIDs?

<p>Anti-coagulant effects (B)</p> Signup and view all the answers

Which of the following conditions would require cautious use of NSAIDs?

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

Which non-selective COX inhibitor is administered intramuscularly?

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

Which mechanism is responsible for NSAID-induced gastric ulcers?

<p>Inhibition of prostaglandin synthesis (A)</p> Signup and view all the answers

What is a key advantage of selective COX-2 inhibitors over non-selective NSAIDs concerning gastrointestinal adverse events?

<p>Reduced risk of bleeding/ulcers (C)</p> Signup and view all the answers

In the context of pain management, what are eicosanoids?

<p>A class of lipids including prostaglandins and leukotrienes, involved in inflammation and pain. (A)</p> Signup and view all the answers

A patient with a known hypersensitivity to aspirin needs an analgesic. Which of the following would be the safest option?

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

A patient reports taking high doses of paracetamol daily for chronic pain. Which of the following lab values is MOST important to monitor regularly?

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

Which of the following best describes the impact of NSAIDs on renal function?

<p>NSAIDs can compromise renal function, especially in patients with pre-existing renal disease (A)</p> Signup and view all the answers

You are treating a patient who has a history of GI ulcers. Which analgesic regimen would pose the LEAST risk for GI complications?

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

Which of the following NSAIDs is available in an intravenous formulation?

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

A patient with a history of myocardial infarction is prescribed an analgesic for osteoarthritis. Which of the following analgesics should be used with caution?

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

In the arachidonic acid pathway, which enzyme is targeted by NSAIDs to reduce inflammation and pain?

<p>Cyclo-oxygenase (COX) (C)</p> Signup and view all the answers

Which of the following best explains why acetaminophen is preferred over NSAIDs in patients with severe renal impairment?

<p>It does not affect renal prostaglandins. (C)</p> Signup and view all the answers

Which of the following NSAIDs is known for its irreversible inhibition of COX-1?

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

A patient has overdosed on paracetamol. What is the antidote that can prevent liver damage if administered early?

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

In which specific scenario should aspirin treatment be stopped 7 days before surgery?

<p>To allow for the production of new, functional platelets. (C)</p> Signup and view all the answers

What is the greatest risk for a 6-year-old child given aspirin for a viral infection?

<p>Reye's syndrome (D)</p> Signup and view all the answers

Which type of pain is most effectively treated with non-opioid analgesics like NSAIDs and paracetamol?

<p>Moderate nociceptive or inflammatory pain (A)</p> Signup and view all the answers

A patient with a history of heart failure is prescribed an NSAID for osteoarthritis. Which potential adverse effect is of greatest concern?

<p>Exacerbation of heart failure (D)</p> Signup and view all the answers

What is the key difference between the analgesic effect of paracetamol and NSAIDs?

<p>Paracetamol has no clinically significant anti-inflammatory effects, whereas NSAIDs do. (C)</p> Signup and view all the answers

What is the primary reason for the black box warning on COX-2 selective inhibitors?

<p>Increased risk of cardiovascular events (C)</p> Signup and view all the answers

A patient with rheumatoid arthritis is taking a high dose of aspirin daily. Which adverse effect is most likely to occur?

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

Which of the following is the most accurate statement regarding the use of paracetamol during pregnancy?

<p>It is the preferred analgesic and antipyretic during pregnancy. (B)</p> Signup and view all the answers

A patient with a known sulfonamide allergy is prescribed celecoxib. What is the appropriate course of action?

<p>Avoid celecoxib due to the potential for cross-reactivity. (D)</p> Signup and view all the answers

A patient is taking low-dose aspirin for secondary prevention of cardiovascular events. They now need to start ibuprofen regularly for arthritis pain. What is the most important consideration regarding their medication regimen?

<p>Ibuprofen can block aspirin's antiplatelet effects, reducing its cardioprotective benefit. (D)</p> Signup and view all the answers

A patient presents with signs of liver failure after taking too much paracetamol. Besides laboratory tests, what is the next immediate step in their management?

<p>Administer IV acetylcysteine (A)</p> Signup and view all the answers

What is the underlying reason why aspirin should be avoided in children presenting with influenza-like symptoms?

<p>There is a risk of Reye's syndrome, a rare but serious condition. (C)</p> Signup and view all the answers

A researcher is investigating a new drug that selectively inhibits COX-1. Which of the following would be an expected effect of this drug?

<p>Reduced platelet aggregation. (B)</p> Signup and view all the answers

Which of the following is an example of physiological pain?

<p>Nociceptive pain experienced after touching a hot stove (D)</p> Signup and view all the answers

The activation of which receptor is most directly involved in the sensation of pressure?

<p>DEG/ENaC? (D)</p> Signup and view all the answers

Which of the following is the most accurate statement regarding the relationship between NSAIDs and afferent arteriolar resistance in the kidneys?

<p>NSAIDs lead to afferent arteriolar constriction, which can reduce renal blood flow, particularly under physiological stress. (D)</p> Signup and view all the answers

Which of the following describes the action of meloxicam?

<p>Non-selective COX inhibitor (C)</p> Signup and view all the answers

The primary advantage of using selective COX-2 inhibitors over non-selective NSAIDs relates to:

<p>Decreased incidence of gastrointestinal ulceration (D)</p> Signup and view all the answers

Which of the following is an adverse effect associated with COX-2 inhibition?

<p>Increased risk of thrombotic events (A)</p> Signup and view all the answers

Aspirin's antiplatelet effect is due to:

<p>Irreversible inhibition of cyclooxygenase-1 (COX-1). (A)</p> Signup and view all the answers

Why is aspirin typically discontinued before surgery?

<p>To prevent the risk of increased bleeding (A)</p> Signup and view all the answers

Which of the following best describes paracetamol's mechanism of action?

<p>Central inhibition of prostaglandin synthesis. (C)</p> Signup and view all the answers

In which situation is paracetamol generally considered the first-line analgesic?

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

What is the primary metabolic pathway of paracetamol, and what happens during an overdose?

<p>Glucuronidation is the primary pathway; overdose leads to increased levels of NAPQI. (D)</p> Signup and view all the answers

What direct consequence results from paracetamol overdose due to the accumulation of NAPQI?

<p>Fulminant liver failure (A)</p> Signup and view all the answers

Which adverse effect is NOT typically seen with NSAIDs?

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

In which condition would NSAIDs need to be used with caution?

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

Which route of administration is specific to ketorolac?

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

What is a key benefit of selective COX-2 inhibitors over non-selective NSAIDs regarding gastrointestinal adverse events?

<p>They decrease the risk of gastric ulcers. (C)</p> Signup and view all the answers

What are eicosanoids?

<p>Lipid mediators involved in inflammation and pain. (D)</p> Signup and view all the answers

A patient with known aspirin hypersensitivity requires pain relief. Which is the safest option?

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

A patient on high-dose paracetamol for chronic pain necessitates monitoring of which lab value?

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

How do NSAIDs typically impact renal function?

<p>Reduce renal blood flow. (A)</p> Signup and view all the answers

Which analgesic regimen poses the LEAST risk for GI complications in a patient with a history of GI ulcers?

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

Which NSAID is available in an intravenous (IV) formulation?

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

For a patient with a history of myocardial infarction needing analgesia for osteoarthritis, which is safest?

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

Which enzyme is targeted by NSAIDs in the arachidonic acid pathway to reduce inflammation and pain?

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

Why is acetaminophen preferred over NSAIDs in severe renal impairment?

<p>Acetaminophen does not significantly affect renal blood flow. (B)</p> Signup and view all the answers

Which NSAID is known for its irreversible inhibition of COX-1?

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

Which drug is used as an antidote for paracetamol overdose if administered early?

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

For which surgical scenario is aspirin typically stopped 7 days prior?

<p>Coronary artery bypass grafting (A)</p> Signup and view all the answers

What is the greatest concern when administering aspirin to a 6-year-old with a viral infection?

<p>Reye's syndrome (A)</p> Signup and view all the answers

Which type of pain do non-opioid analgesics like NSAIDs and paracetamol treat most effectively?

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

If a patient with heart failure is prescribed an NSAID for osteoarthritis, which adverse effect is of greatest concern?

<p>Sodium and fluid retention (A)</p> Signup and view all the answers

What is the primary difference between the analgesic effect of paracetamol and NSAIDs?

<p>Paracetamol primarily acts centrally, while NSAIDs have peripheral effects. (D)</p> Signup and view all the answers

What is the main reason for the black box warning on COX-2 selective inhibitors?

<p>Elevated risk of cardiovascular events (A)</p> Signup and view all the answers

What adverse effect is most likely in a patient taking high-dose aspirin daily for rheumatoid arthritis?

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

Which statement is true regarding paracetamol use during pregnancy?

<p>Paracetamol is the preferred analgesic and antipyretic. (D)</p> Signup and view all the answers

What is the proper course of action if a patient with a sulfonamide allergy is prescribed celecoxib?

<p>Avoid celecoxib and choose a different analgesic. (B)</p> Signup and view all the answers

A patient takes low-dose aspirin for cardiovascular prevention and needs ibuprofen for arthritis. What is most important?

<p>Separate doses of aspirin and ibuprofen. (D)</p> Signup and view all the answers

A patient shows signs of liver failure after a paracetamol overdose. After lab tests, what's the next step?

<p>Start intravenous acetylcysteine. (A)</p> Signup and view all the answers

Why should aspirin be avoided in children with influenza-like symptoms?

<p>It is associated with Reye's syndrome. (D)</p> Signup and view all the answers

A researcher tests a new drug that selectively inhibits COX-1. What effect would be expected?

<p>Increased risk of bleeding. (B)</p> Signup and view all the answers

Which of the following best accounts for why paracetamol is considered an antipyretic?

<p>Directly inhibits the temperature-regulating center in the hypothalamus (D)</p> Signup and view all the answers

Which of the following best describes the term 'opiate'?

<p>Naturally occurring substances with morphine-like properties. (C)</p> Signup and view all the answers

What is the significance of the year 1973 in the context of opioid pharmacology?

<p>The year opioid receptors were discovered. (B)</p> Signup and view all the answers

Activation of the mu (µ) opioid receptor is most likely to result in which of the following?

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

Which of the following best describes the primary location of mu (µ) opioid receptors responsible for analgesia within the central nervous system (CNS)?

<p>Brain stem. (A)</p> Signup and view all the answers

Which of the following is a common adverse effect directly related to opioid-induced reduced gut motility?

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

A patient has been taking morphine for chronic pain for several months and now requires a higher dose to achieve the same level of pain relief. This phenomenon is best described as:

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

Which of the following statements accurately distinguishes between physical dependence and addiction in the context of opioid use?

<p>Physical dependence can occur without addiction and is a physiological adaptation to the drug. (D)</p> Signup and view all the answers

Which of the following is a key consideration when titrating morphine for pain management?

<p>Titrating to effect while minimizing life-threatening adverse effects like sedation and respiratory depression. (A)</p> Signup and view all the answers

Morphine undergoes metabolism in the liver, primarily into which of the following metabolites?

<p>Morphine-3-glucuronide. (C)</p> Signup and view all the answers

Which of the following statements is most accurate regarding the use of morphine in patients with renal impairment?

<p>Morphine should be used with caution in renal impairment because its metabolites can accumulate. (A)</p> Signup and view all the answers

Codeine exerts its analgesic effect through which of the following mechanisms?

<p>Demethylation to morphine. (A)</p> Signup and view all the answers

A patient is identified as a 'rapid metabolizer' of codeine. What is the primary implication of this genetic variability?

<p>Increased risk of adverse effects at normal doses. (C)</p> Signup and view all the answers

Why is codeine no longer recommended for mild to moderate acute pain?

<p>Due to evidence that low dose preparations have no benefit over simple analgesia. (B)</p> Signup and view all the answers

Which of the following best describes the mechanism by which naloxone reduces abuse potential when combined with oxycodone (Targin)?

<p>Naloxone is an opioid antagonist that deters abuse. (D)</p> Signup and view all the answers

Which of the following statements regarding oxycodone is most accurate?

<p>Oxycodone is a synthetic opioid and predominantly a mu opioid receptor agonist. (A)</p> Signup and view all the answers

How does tramadol exert its analgesic effects?

<p>Primarily as a weak opioid agonist, it also affects non-opioid pathways. (A)</p> Signup and view all the answers

A patient taking tramadol should be cautioned about which of the following potential adverse effects or interactions?

<p>Increased seizure risk, especially with a history of epilepsy. (B)</p> Signup and view all the answers

In contrast to morphine, what advantage does tramadol offer in certain clinical situations?

<p>Reduced incidence of respiratory depression and constipation. (C)</p> Signup and view all the answers

Why is tapentadol considered distinct from other opioids like morphine or oxycodone?

<p>It's a weak opioid agonist and noradrenaline reuptake inhibitor. (B)</p> Signup and view all the answers

A patient with severe renal impairment requires opioid analgesia. Which of the following opioids should be used with extreme caution?

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

Which of the following is considered a strong opioid that is available in both immediate-release (IR) and sustained-release (SR) oral formulations, as well as an intravenous (IV) formulation?

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

Methadone is particularly useful in which of the following clinical scenarios?

<p>Opioid replacement in addiction. (C)</p> Signup and view all the answers

Why is pethidine generally avoided for pain management?

<p>It has a very short half-life and a high risk of side effects, including seizures. (A)</p> Signup and view all the answers

According to the principles of pain management, which of the following best describes a multimodal approach?

<p>Addressing pain using a combination of pharmaceutical and non-pharmaceutical strategies. (D)</p> Signup and view all the answers

How does the WHO analgesia ladder guide treatment for cancer pain?

<p>By starting with simple analgesics and escalating to stronger opioids as needed. (D)</p> Signup and view all the answers

In the context of acute nociceptive pain management, what is the 'Reverse WHO Ladder' approach?

<p>A method of pain management that involves starting with stronger opioids and then stepping down to milder analgesics as the acute pain subsides. (A)</p> Signup and view all the answers

Which of the following strategies is most appropriate in efforts to combat the opioid epidemic?

<p>Promoting education for health professionals in appropriate opioid prescribing. (D)</p> Signup and view all the answers

Which of the following should be considered when determining the need to prescribe opioid analgesics?

<p>Opioids may be appropriate for effective analgesia in moderate to severe acute pain, or chronic cancer pain. (D)</p> Signup and view all the answers

Which one of the following is the MOST likely adverse effect occurring alongside analgesia, once opioid analgesics are administered?

<p>Analgesia and adverse effects. (D)</p> Signup and view all the answers

What is the most appropriate approach regarding opioid prescriptions for patients with chronic, non-cancer pain?

<p>Opioids should be avoided due to adverse effects outweighing benefits. (D)</p> Signup and view all the answers

What is the most significant risk associated with indiscriminate, long-term opioid prescribing, exemplified by trends observed in the US?

<p>High rates of opioid abuse, addiction, and overdose deaths. (B)</p> Signup and view all the answers

What is the recommended approach to manage expectations and outcomes when prescribing opioids for patients?

<p>Setting realistic goals and ensuring patients understand the potential benefits and risks of opioid therapy. (D)</p> Signup and view all the answers

A patient presents with chronic, severe disabling pain that has not responded to non-opioid analgesics. Which of the following opioids would be most beneficial in this scenario?

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

Which of the following are examples that would contribute to physical harm, regarding an opioid's addictive qualities?

<p>Physical, psychological and social harm. (C)</p> Signup and view all the answers

Opioid induced constipation can result from:

<p>Reduced gut motility. (C)</p> Signup and view all the answers

A very rare but harmful side effects that can occur with some opioid analgesics are:

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

What are some symptoms that a patient might expect when stopping opioid analgesics?

<p>Anorexia, diarrhea, depression. (A)</p> Signup and view all the answers

Understanding the implications of opioid usage is important for patients. Which of the following statements embodies the best description of opioid tolerance:

<p>Increased dose may be required to achieve the same level of pain relief as before. (B)</p> Signup and view all the answers

Following abdominal surgery, a patient reports a pain level of 7 out of 10. The patient chart shows codeine is suitable. What considerations are necessary before administering?

<p>If the patient is documented to lack CYP2D6 enzyme or is a rapid metaboliser. (D)</p> Signup and view all the answers

Following abdominal surgery, a patient reports a pain level of 7 out of 10. What would be the next step to assist this patient?

<p>Administer the lowest dose of opioid analgesics. (A)</p> Signup and view all the answers

What is the defining characteristic of an 'opiate'?

<p>It exclusively refers to naturally occurring substances with morphine-like properties. (C)</p> Signup and view all the answers

Which of the following is a crucial characteristic of opioid receptors?

<p>They are inhibitory G-protein coupled receptors that inhibit neurotransmitter release. (A)</p> Signup and view all the answers

Which of the following is a commonly reported effect associated with mu (µ) opioid receptor activation?

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

Opioid receptors are located in what part of the brain?

<p>All of the above (D)</p> Signup and view all the answers

What is the primary implication of opioid effects being dose-dependent?

<p>The intensity of both analgesic and adverse effects increases with higher doses. (B)</p> Signup and view all the answers

In the context of opioid use, what does 'tolerance' specifically refer to?

<p>The need to increase the dose to achieve the same analgesic effect (D)</p> Signup and view all the answers

Which of the following differentiates physical dependence from addiction in opioid use?

<p>Physical dependence involves physiological adaptation leading to withdrawal symptoms, while addiction involves compulsive substance use despite harm. (D)</p> Signup and view all the answers

Which action will reduce physical harm from an opioiod's addictive qualties?

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

What is the recommended strategy to avoid precipitating withdrawal symptoms when discontinuing opioids?

<p>Wean opioids slowly (D)</p> Signup and view all the answers

What is a symptom a patient is likely to experience when they have stopped opioid analgesics?

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

How can opioid-induced constipation be explained?

<p>Reduced gut motility (D)</p> Signup and view all the answers

A very rare harmful side effect that can occur with some opioid analgesics is:

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

Which of the following is the primary route of morphine metabolism?

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

A patient with severe hepatic impairment requires opioid analgesia. Which of the following would be the MOST appropriate initial action?

<p>Administer morphine at a reduced dose and titrate carefully. (A)</p> Signup and view all the answers

What is the mechanism by which codeine exerts its analgesic effect?

<p>Demethylation to morphine via CYP2D6 (B)</p> Signup and view all the answers

What is the implication of identifying a patient as a 'rapid metabolizer' of codeine?

<p>Increased risk of adverse effects due to increased morphine production (C)</p> Signup and view all the answers

What best describes a drug that is a prodrug?

<p>A drug that is inactive until metabolized into an active form in the body. (A)</p> Signup and view all the answers

Why is codeine no longer the top analgesic to use for mild to moderate acute pain in some guidelines?

<p>Because it has been shown to have no benefit over simple analgesia in low doses (A)</p> Signup and view all the answers

A child is prescribed codeine for pain relief after a tonsillectomy. The parents are concerned about potential side effects. What is the MOST important consideration?

<p>Whether the child is a known CYP2D6 ultra-rapid metabolizer (A)</p> Signup and view all the answers

What distinguishes Targin®, a controlled-release formulation of oxycodone with naloxone, from other oxycodone formulations?

<p>The inclusion of naloxone reduces opioid-induced constipation and deters abuse. (D)</p> Signup and view all the answers

Adverse effects similar to which one, can occur when taking oxycodone?

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

What is a unique mechanism of action of tramadol, compared to traditional opioids?

<p>Serotonin and noradrenaline reuptake inhibition (D)</p> Signup and view all the answers

In comparison to morphine, what is an advantage tramadol may offer in clinical settings?

<p>Less respiratory depression (C)</p> Signup and view all the answers

Under which conditions would you be cautious of while treating a patient with Tramadol?

<p>If the patient takes Serotonergic agents (D)</p> Signup and view all the answers

Tapentadol has a unique mechanism of action with?

<p>An adrenaline reuptake inhibitor (D)</p> Signup and view all the answers

A patient with which condition, would you want to be cautious when treating with Tapentadol?

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

Which strong opioid has good parental and mucosal absorption but ineffective as an oral route?

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

Which of the following is a key characteristic that makes methadone distinct from other strong opioids?

<p>NMDA receptor antagonist effect (B)</p> Signup and view all the answers

What does 'multimodal analgesia' involve?

<p>Using multiple medications that target different pathways to treat pain (A)</p> Signup and view all the answers

What is the primary focus of the WHO analgesia ladder?

<p>Treatment of cancer pain (A)</p> Signup and view all the answers

In the context of the WHO Analgesia Ladder, what is the 'Reverse WHO Ladder' approach primarily used for?

<p>To manage acute nociceptive pain. (C)</p> Signup and view all the answers

What is MOST suggestive of opioid tolerance?

<p>The patient requires a higher dose of opioid for the same pain relief (D)</p> Signup and view all the answers

What is the underlying cause of the opioid epidemic that has been seen in the US?

<p>Indiscriminate long-term prescribing (C)</p> Signup and view all the answers

What are important aspect(s) can we 'do' to combat opioid prescribing and abuse?

<p>All of the above (D)</p> Signup and view all the answers

Which is an appropriate opioid prescription for patients with chronic, non-cancer pain?

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

Following abdominal surgery, a patient reports a pain level of 7 out of 10 and the patient chart shows codeine is suitable. What should happen next?

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

Consider a patient that cannot be orally medicated, and is suffering severe pain. Which of the following analgesics could assist?

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

Which opioid, if any, can be useful for neuropathic pain?

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

According to the International Association for the Study of Pain (IASP), which statement defines pain?

<p>Pain is an unpleasant sensory and emotional experience associated with, or resembling that associated with, actual or potential tissue damage. (C)</p> Signup and view all the answers

What is the primary differentiating factor between nociceptive and neuropathic pain?

<p>Nociceptive pain arises from actual or threatened damage to non-neural tissue, while neuropathic pain is caused by a lesion or disease of the somatosensory nervous system. (A)</p> Signup and view all the answers

Neuropathic pain is best described as:

<p>A clinical description requiring evidence of a lesion or disease. (D)</p> Signup and view all the answers

When diagnostic investigations reveal an abnormality or there is obvious trauma associated with neuropathic pain, the term most commonly used is:

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

For neuropathic pain, if the underlying reason for the 'lesion' is known, the appropriate term to use would be:

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

What percentage of Australians aged 45 and over are estimated to have a chronic pain condition?

<p>1 in 5 (C)</p> Signup and view all the answers

Which of the following statements is true regarding chronic pain?

<p>People with chronic pain are more likely to report limitations to daily activities. (A)</p> Signup and view all the answers

What percentage of Australians are estimated to have neuropathic pain?

<p>7-10% (C)</p> Signup and view all the answers

How can intensively treating the disease process relate to the paradoxes of neuropathic pain?

<p>Intensively treating the disease process may be associated with worse outcomes through intensive blood sugar management. (B)</p> Signup and view all the answers

Which describes a paradox of neuropathic pain?

<p>Neuropathic pain may be the consequence of a disease treatment, and not ceasing that treatment has long term consequences (C)</p> Signup and view all the answers

When prescribing medication for neuropathic pain, what is the best approach to determine therapeutic benefit?

<p>Start with a low dose and titrate slowly. (B)</p> Signup and view all the answers

What should you consider when prescribing for neuropathic pain?

<p>All of the above (D)</p> Signup and view all the answers

What strategy is the best component of a multidimensional management plan?

<p>Assess for potentially dangerous interactions. (B)</p> Signup and view all the answers

When assessing a patient, which of the following characteristics would be associated with neuropathic pain?

<p>Painful cold. (B)</p> Signup and view all the answers

When assessing a patient, which of the following sensations would be associated with neuropathic pain?

<p>Pins and needles. (B)</p> Signup and view all the answers

What is the definition of allodynia?

<p>Pain due to a stimulus that does not normally provoke pain. (D)</p> Signup and view all the answers

What best describes hyperaesthesia?

<p>Increased pain from a stimulus that usually provokes pain. (C)</p> Signup and view all the answers

Which of the following medications would be considered first-line treatments for neuropathic pain?

<p>SNRIs and tricyclic antidepressants (B)</p> Signup and view all the answers

What is the mechanism of action of Serotonin Norepinephrine Reuptake Inhibitors (SNRIs)?

<p>Inhibiting the reuptake of serotonin and norepinephrine. (A)</p> Signup and view all the answers

Duloxetine and Venlafaxine are?

<p>SNRIs used in neuropathic pain. (A)</p> Signup and view all the answers

An important element to consider, regarding SRNIs, is?

<p>Start with low dose to avoid side effects. (A)</p> Signup and view all the answers

What is a common adverse effect to Seretonin Syndrome?

<p>When prescribed with another drug altering serotonin levels. (A)</p> Signup and view all the answers

What is especially important to note with Amitriptyline?

<p>Prolongs QT interval. (A)</p> Signup and view all the answers

How are Tricyclic Antidepressants (TCAs) used in treatment?

<p>In lower doses for neuropathic pain than for depression. (D)</p> Signup and view all the answers

What is a primary mechanism of action?

<p>block aâ‚‚d subunit-containing voltage-dependent calcium channels (A)</p> Signup and view all the answers

Which factor significantly affect the pharmacokinetics of gabapentin?

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

What is the time to effective dose using recommended titrations?

<p>is 14 days for gabapentin and 7 days for pregabalin (C)</p> Signup and view all the answers

A patient has gait disturbances and also visual blurring, which adverse effect may they be experiencing?

<p>From prescribed Gabapentinoids (D)</p> Signup and view all the answers

Gabapentinoids has which notable effect? (select all that apply)

<p>There is respiratory depression when used in combination with opioids (A), Increased liklihood of increased opioid related mortality (B)</p> Signup and view all the answers

Withdrawal symptoms for Gabapentinoids is...

<p>Tapering reduction in dosage (e.g. twice weekly reduction of 10-25% of dosage) minimises risks of withdrawal. (A)</p> Signup and view all the answers

A patient with chronic kidney disease is experiencing toxicity signs, what could be prescribed to cause this?

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

Which is not an off-label use of gabapentinoids?

<p>Neuropathic Pain. (B)</p> Signup and view all the answers

Which of the following is a characteristic of lidocaine patches?

<p>Used for 12 hours on and off. (B)</p> Signup and view all the answers

Which is the method of action for Lidocaine Patches?

<p>Blocks sensitized Na+ channels in nociceptors (D)</p> Signup and view all the answers

Capsaicin is highly selective to what?

<p>TRPV-1 agonist. (D)</p> Signup and view all the answers

Capsaicin has been shown to be efficacious for neuropathic pain, what other conditions?

<p>Improves sleep quality in patients with painful diabetic peripheral neuropathy (A)</p> Signup and view all the answers

Tramadol differs from traditional Opioid Analgesics by:

<p>Not an opioid (C)</p> Signup and view all the answers

What contributes to why tramadol is prescribed?

<p>Generally less respiratory depression (A)</p> Signup and view all the answers

Which medications must CYP2D6 be concerned with?

<p>TCAs, MAOIs, SNRIs SSRIs, BDZ and alcohol (C)</p> Signup and view all the answers

What is the most important takeaway message to remember when assessing neuropathic pain?

<p>Follow the principles so you don't cause strife. (B)</p> Signup and view all the answers

What differentiates an opiate from an opioid?

<p>Opiates are naturally occurring substances with morphine-like properties, while opioids are a broader term including synthetic substances. (C)</p> Signup and view all the answers

In what year were opioid receptors first discovered?

<p>1973 (A)</p> Signup and view all the answers

What is the direct result of opioid agonists binding to receptors?

<p>Inhibition of neurotransmitter release. (A)</p> Signup and view all the answers

Which of the following effects is primarily associated with the activation of the mu (µ) opioid receptor?

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

Which opioid receptor primarily leads to sedation and depression?

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

Besides the brainstem, where in the CNS are mu receptors responsible for analgesia most concentrated?

<p>Dorsal horn of the spinal cord (A)</p> Signup and view all the answers

What is the most common dose-dependent adverse effect of opioid analgesia?

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

Following long term use of opioid analgesics, what statement defines opioid tolerance?

<p>The need for increased doses of opioids to achieve the same analgesic effect. (A)</p> Signup and view all the answers

Which of the following is primarily attributed to physical dependence rather than addiction?

<p>Withdrawal symptoms upon cessation. (B)</p> Signup and view all the answers

What is the primary consideration when titrating morphine?

<p>Minimizing life-threatening adverse effects. (C)</p> Signup and view all the answers

Which statement most accurately describes the use of morphine in patients with renal impairment?

<p>Morphine dose should be reduced. (C)</p> Signup and view all the answers

What is the process by which codeine exerts its analgesic effect?

<p>Demethylation to morphine. (D)</p> Signup and view all the answers

The statement best describes the implications of a patient being identified as a 'rapid metabolizer' of codeine?

<p>The patient is at an increased risk of adverse effects. (A)</p> Signup and view all the answers

What is the rationale for administering naloxone with oxycodone?

<p>Reduce opioid induced constipation. (A)</p> Signup and view all the answers

Besides opioid agonism, how does tramadol exhibit its analgesic effects?

<p>Inhibits reuptake of serotonin and noradrenaline. (C)</p> Signup and view all the answers

What is a potential adverse effect of tramadol?

<p>Lowered seizure threshold (A)</p> Signup and view all the answers

Why might tramadol be preferable to morphine in certain clinical settings?

<p>Lower risk of respiratory depression. (D)</p> Signup and view all the answers

In what patient population would taking Tramadol require caution?

<p>Age &gt; 65yr (B)</p> Signup and view all the answers

How does Tapentadol relieve pain?

<p>Centrally acting opioid agonist, with no active metabolites. (D)</p> Signup and view all the answers

What is the most important to consider when administering Tapentadol?

<p>Caution should be taken when administering to patients with severe renal impairment. (C)</p> Signup and view all the answers

In what specific clinical scenario is methadone particularly useful?

<p>Opioid replacement in addiction. (A)</p> Signup and view all the answers

What is the best example of multimodal approach to pain management?

<p>Use of pharmaceutical interventions with multiple non-pharmaceutical interventions. (C)</p> Signup and view all the answers

How is the 'Reverse WHO Ladder' approach best applied in pain management?

<p>Treating acute nociceptive pain. (C)</p> Signup and view all the answers

Consider the strategies a physician can implement to improve combating the opioid use epidemic. Which one has the ability to create the greatest impact?

<p>Ensure the judicious prescribing of opioids analgesics. (C)</p> Signup and view all the answers

Which of the following is MOST important when prescribing opioid analgesics?

<p>Potential benefits outweigh the risks. (A)</p> Signup and view all the answers

For a patient with chronic, non-cancer pain, what approach should be considered with opioid prescriptions?

<p>Optimize non-opioid therapies and consider opioids. (B)</p> Signup and view all the answers

What would opioid tolerance be described as?

<p>When higher doses are needed for equal effect. (C)</p> Signup and view all the answers

What is a rare but harmful side effect that can occur with some opioid analgesics?

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

What is the next immediate step after abdominal surgery when a patient reports a pain level of 7 out of 10?

<p>Assess the patient's pain more thoroughly to see available options. (D)</p> Signup and view all the answers

Which opioid is known for having no active metabolites?

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

In cases of chronic cancer pain requiring strong opioid analgesia, which of the following would be most suitable according to the WHO analgesia ladder?

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

The accumulation of which primary metabolite of morphine is of particular concern in patients with decreasing renal function?

<p>Morphine-3-glucuronide (C)</p> Signup and view all the answers

Which of the following best describes the mechanism by which tolerance to the emetic effects of morphine develops?

<p>Downregulation of dopamine receptors in the chemoreceptor trigger zone. (C)</p> Signup and view all the answers

Which of the following accurately describes the role of delta (δ) opioid receptors?

<p>Involved in analgesia, antidepressant effects, and physical dependence. (A)</p> Signup and view all the answers

A researcher discovers a novel compound that selectively activates opioid receptors on peripheral sensory neurons but does not cross the blood-brain barrier. What effect would this drug likely have?

<p>Localized analgesia with minimal central side effects. (D)</p> Signup and view all the answers

A patient with a known history of seizures is experiencing severe, chronic pain. Which opioid analgesic would be MOST contraindicated, and why?

<p>Tramadol, due to the risk of lowering the seizure threshold. (D)</p> Signup and view all the answers

Flashcards

Pain

An unpleasant sensory and emotional experience associated with actual or potential tissue damage.

Nociceptive Pain

Pain arising from actual or threatened damage to non-neural tissue due to activation of nociceptors.

Neuropathic Pain

Pain caused by a lesion or disease of the somatosensory nervous system.

Allodynia

Pain due to a stimulus that doesn't normally provoke pain.

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Hyperaesthesia

Increased pain from a stimulus that usually provokes pain.

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SNRIs

A class of antidepressant drugs that include duloxetine and venlafaxine.

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SNRI Mechanism

Inhibit the presynaptic neuronal uptake of serotonin and norepinephrine, increasing their availability in the synaptic cleft.

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SNRI Pharmacokinetics

Mainly hepatically excreted through P-450; formulations allow for once-daily dosing; half-life approximately 12 hours.

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SNRI Adverse Effects

Nausea, vomiting, constipation, dizziness, insomnia, fatigue, headache, sexual dysfunction, and serotonin syndrome.

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TCAs

A class of antidepressants including amitriptyline, used in lower doses for neuropathic pain due to side effects.

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Amitriptyline Pharmacokinetics

Large first-pass metabolism, ~50% bioavailability, maximum blood levels in 4 hours, active metabolites, 21-hour elimination half-life.

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Amitriptyline Adverse Effects

Similar to SNRIs but also causes transient increase in LFTs, prolongs QT interval, and can cause significant electrocardiac abnormalities in overdose.

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Gabapentinoids

Gabapentin and pregabalin, which bind to α2δ ligands and Ca2+ channels, originally developed as anti-epileptics and used as first-line treatment for neuropathic pain.

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Gabapentinoid Pharmacokinetics

Minimal metabolism, excreted renally; time to effective dose is 14 days for gabapentin and 7 days for pregabalin.

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Gabapentinoid CNS Adverse Effects

Dizziness, somnolence, gait disturbances, visual blurring, impaired concentration, confusion, memory loss, altered mood, movement disorders, sleep disorder, speech impairment, and vertigo.

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Gabapentinoid Respiratory Depression

Commonly prescribed in conjunction with opioids, this requires dose adjustment in patients with compromised respiratory function.

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Gabapentinoid Withdrawal Symptoms

Agitation, confusion, disorientation, and symptoms similar to benzodiazepine and alcohol withdrawal.

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Gabapentinoid Toxicity

Increased sedation, confusion, unsteady gait, myoclonus, ataxia, episodic leg spasm, asterixis and tremulousness.

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Lidocaine Patch Mechanism

Works by blocking sensitized Na+ channels in nociceptors.

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Capsaicin Mechanism

Transient receptor potential vanilloid-1 (TRPV-1) agonist that reduces pain and improves sleep quality, with single applications having long-term effects.

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Tramadol

A 'mongrel' drug that acts on the Mu opioid receptor, prevents 5-HT reuptake, and inhibits noradrenaline reuptake.

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Study Notes

Pain

  • Pain is an unpleasant sensory and emotional experience associated with, or resembling that associated with, actual or potential tissue damage as classified by IASP
  • Two broad categories of pain include Nociceptive and Neuropathic

Nociceptive Pain

  • Nociceptive pain arises from actual or threatened damage to non-neural tissue
  • This pain is caused by the activation of nociceptors
  • Subcategories of nociceptive pain include somatic and visceral pain

Neuropathic Pain

  • Neuropathic pain is caused by a lesion or disease of the somatosensory nervous system
  • Neuropathic pain is a clinical description and not a diagnosis
  • A demonstrable lesion or disease must satisfy established neurological diagnostic criteria for neuropathic pain
  • The term "lesion" refers to an abnormality revealed by diagnostic investigations or obvious trauma
  • The term "disease" is used when the underlying cause of the lesion is known

Relevance of Chronic Pain

  • 1 in 5 Australians aged 45 and over have a chronic pain condition
  • People with chronic pain are more likely to be female, older, have long-term conditions, stay longer in hospital, and report limitations to daily activities
  • 7-10% of Australians have neuropathic pain (AIHW 2020)

Paradoxes of Neuropathic Pain

  • Neuropathic pain may be a consequence of a disease process
  • Intensively treating that disease process may be associated with worse outcomes
  • For example, diabetes mellitus intensive blood sugar management with insulin regimens where patients may have a hypoglycaemic episode
  • Neuropathic pain may also be a consequence of a disease treatment
  • Ceasing that treatment may have long-term consequences
  • This may be exemplified by HIV infection where HIV-associated pneumocystic pneumonia treatment can cause psychiatric pain but if stopped can result in Kaposi sarcoma developing

Prescribing Principles for Neuropathic Pain

  • Prescribing for neuropathic pain recommends using a targeted history and physical examination
  • Consider using a validated screening tool (e.g., DN4) to diagnose neuropathic pain and determine therapeutic approach
  • If neuropathic pain is not adequately managed with non-pharmacological approaches, select a medicine based on individual patient factors and medicine properties
  • Optimize benefits by starting with a low dose and titrating slowly, assessing response in relation to individual treatment goals
  • Recognize medicines often have limited effectiveness and that non-pharmacological strategies are a key component of a multidimensional management plan
  • Assess for potentially dangerous interactions and discuss the risks associated with their medicines with patients

Allodynia

  • Allodynia is pain due to a stimulus that does not normally provoke pain
  • This stimulus leads to an unexpectedly painful response
  • Allodynia is a clinical term that does not imply a mechanism
  • The original modality is normally nonpainful, but the response is painful
  • Allodynia involves a change in the quality of a sensation, whether tactile, thermal, or of any other sort

Hyperaesthesia

  • Hyperaesthesia is increased pain from a stimulus that usually provokes pain
  • Hyperaesthesia may refer to various modes of cutaneous sensibility including touch and thermal sensation without pain, as well as to pain
  • The word is used to indicate both diminished threshold to any stimulus and an increased response to stimuli that are normally recognized

First-Line Drugs

  • Drugs used as first-line treatments include: SNRI's like duloxetine and venlafaxine
  • Tricyclic antidepressants like amitriptyline,
  • Gabapentin,
  • Pregabalin.

SNRI

  • SNRIs (Serotonin Norepinephrine Reuptake Inhibitors) are a class of antidepressant drugs
  • They may be used to treat major depressive disorder (MDD), anxiety disorders, obsessive–compulsive disorder (OCD), social phobia, attention-deficit hyperactivity disorder (ADHD), chronic neuropathic pain, fibromyalgia syndrome (FMS), and menopausal symptoms
  • SNRIs inhibit the presynaptic neuronal uptake of 5-HT (serotonin) and norepinephrine following release from the synaptic cleft leading to increased persistence of monoamines in the cleft

SNRIs for Neuropathic Pain

  • Venlafaxine and duloxetine are SNRIs used in neuropathic pain
  • Venlafaxine inhibits serotonin more than norepinephrine, with both having initial influence on serotonin then norepinephrine, reflecting the side effect profile

SNRI Pharmacokinetics

  • SNRIs are mainly hepatically excreted through P-450
  • Both SNRIs have formulations allowing once daily dosing
  • SNRI half life is approximately 12 hours
  • Recommendations include an initial low dose to avoid side effects
  • Doses should be reduced incrementally rather than sudden cessation to avoid rebound effects

SNRI Adverse Effects

  • General adverse effects include nausea and vomiting, constipation, dizziness, insomnia, fatigue, and headache
  • Sexual dysfunction may include low libido, erectile dysfunction, and anorgasmia
  • Serotonin Syndrome" can occur, usually when prescribed with another drug altering serotonin levels

Tricyclic Antidepressants (TCAs)

  • TCAs include amitriptyline, imipramine, doxepin, dothiepin, and nortriptyline
  • TCAs were for many years primary treatment for depression, but are now replaced with drugs classes with safer profiles
  • TCAs are used in lower doses for neuropathic pain than for depression, offering better tolerated side effects

Amitriptyline

  • Amitriptyline has large first pass metabolism
  • Amitriptyline bioavailability is ~50%
  • Maximum blood levels occur in 4 hours
  • Amitriptyline has active metabolites
  • The elimination half life is 21 hours

Amitriptyline Adverse Effects

  • In general, amitriptyline adverse effects are similar to that of SNRIs
  • Amitriptyline generally results in a transient increase in liver function tests (LFTs)
  • Amitriptyline prolongs the QT interval, creating a risk of arrhythmias
  • An overdose of amitriptyline cases significant electrocardiac abnormalities

Gabapentinoids

  • Gabapentinoids consists of gabapentin and pregabalin
  • Gabapentinoids bind to α2δ ligands and Ca2+ α2δ ligands and are GABA analogues
  • Gabapentinoids were originally developed as anti-epileptics
  • They serve as first line treatment of neuropathic pain
  • Gabapentinoids block α2δ subunit-containing voltage-dependent calcium channels
  • Mechanisms of action for Gabapentinoids remain unclear
  • Gabapentinoids use is increasing off-label

Gabapentinoid Pharmacokinetics

  • What matters most is that Gabapentinoids have minimal metabolism: They are excreted renally
  • Time to effective dose using recommended titrations is 14 days for gabapentin and 7 days for pregabalin

Gabapentinoid Adverse Effects

  • Cause discontinuation in 11% of patients, but serious adverse effects are very infrequent

Gabapentinoid CNS Adverse Effects

  • Central nervous system adverse effects include dizziness (19%), somnolescence (14%), gait disturbances (14%), and visual blurring (7%)
  • Other adverse effects include impaired concentration, confusion, memory loss, altered mood, movement disorders, sleep disorder, speech impairment, and vertigo
  • Most side effects are dose dependent
  • The adverse effects includes needing to be warned re driving and operating machinery
  • Commencement of initial dosage at night is recommended
  • The effects often occur during the initiation of treatment and can diminish after several weeks of treatment

Gabapentinoid Respiratory Depression

  • Respiratory depression is often described when used in combination with opioids, it also causes and increased risk of opioid related mortality
  • Approximately 20-25% of patients newly prescribed gabapentinoids are already prescribed opioids
  • Dose adjustment is required in patients with compromised respiratory function, respiratory or neurological disease, renal impairment, concomitant use of CNS depressants, and for the elderly

Gabapentinoid Withdrawal Symptoms

  • Gabapentinoid withdrawal symptoms are common
  • They generally occur within 12 hours and 7 days, most frequently within 24-48 hrs
  • Symptoms include agitation in >50% of patients
  • Confusion and disorientation in 45%
  • Other symptoms are similar to benzodiazepine and alcohol withdrawal
  • Impacts are worse in elderly
  • Tapering reduction in dosage (e.g. twice weekly reduction of 10-25% of dosage) minimises risks of withdrawal from Gabapentinoids

Gabapentinoid Toxicity

  • Concerns include accidental vs intentional toxicity
  • More common in patients with renal disease
  • Higher risk in patients on dialysis
  • Symptoms and signs include increased sedation, confusion, unsteady gait, myoclonus, ataxia, episodic leg spasm, asterixis and tremulousness
  • Treatment generally supportive

Topical Treatments

  • A key option can be topical treatments
  • Lidocaine is a key compound

Lidocaine

  • Lidocaine (lignocaine, Xylocaine ®) patches were Discovered in 1948
  • Primary Use: As a local anaesthetic
  • Secondary Use: As an antiarrhythmic and neonatal antiepileptic agent
  • Has many OTC uses

Lidocaine Patches

  • Were made possible by developments in drug delivery technology
  • Administered with a 12 hours on and 12 hours off Schedule
  • Designed to block sensitized Na+ channels in nociceptors
  • May also inhibit NO production and regulate T-cell activity
  • Also offers, A possible central feedback signal
  • Should be implemented with: Correct patient selection
  • Analgesic effects, which are likely to appear quickly (v. up to 6 weeks for oral treatments)
  • But will NOT lead to, cutaneous anaesthesia
  • The approach results in being able to, Reduce treatment frequency
  • Has a low risk of, Broken skin where it increases- increased risk of lidocaine toxicity
  • Generally is well tolerated
  • They should be used with: Correct patient selection + Analgesic effects likely to appear quickly (v. up to 6 weeks for oral treats) = the approach will- will NOT lead to cutaneous anaesthesia âžœ reduces treatment frequency but Beware:broken skin – increased risk of lidocaine toxicity + well tolerated

Capsaicin

  • Capsaicin methods effects - Transient receptor potential vanilloid-1 (TRPV-1),
  • A thermal nociceptor, which plays an important role in the detection of painful stimuli such as heat, acids and irritant chemicals as:
  • a potent and highly selective TRPV-1 agonist
  • Activation happens initially with: TRPV-1-expressing nociceptors on the skin, resulting in erythema
  • With continued exposure, the nociceptors become less sensitive and no longer respond to capsaicin or various other stimuli
  • And finally resulting generally in Single applications with may have long term effects

Capsaicin Indications

  • Method provides for Relieves pain and improves sleep quality in patients with painful diabetic peripheral neuropathy + Provides rapid and sustained pain relief in patients with postherpetic neuralgia + Efficacious (less evidence) in neuropathic pains; post-traumatic, post-surgical, polyneuropathy, chemotherapy-induced, lumbosacral 4 âžœ Pelvic Neuralgia and critical ischaemia and refractory neuropathic pain and neurofibromatosis and Phantom Pain

Tramadol

  • Tramadol is considered a mongrel of a drug
  • Tramadol is often classified with opioids, but structurally is not an opioid Has actions on what
  • acts on the Mu opioid receptor
  • The effects are not completely reversed by naloxone, as the action is that of a non-selective and competitive opioid receptor antagonist
  • It is of a Racaemic mixture (+)-tramadol has: greater affinity for μ-opioid receptor and additional prevention of 5- hydroxy tryptamine reuptake (-)-tramadol: leads to successful noradrenaline reuptake inhibitor and further intensifies its release

Administration: Prescribed?

  • Less potent and less abuse potentia
  • It causes a lower respiratory depression with however can be prescribed for respiratory depression.
  • Available in both IR and SR preparations

Caution: Problems?

  • Undergoes Metabolised by CYP2D6 to an active metabolite:
  • Genetic variations must be considered
  • Medications with; TCA.MAOI 3 âžœ SNRI.SSRI 5 âžœBDZ . alcohol should also be factored in.
  • Be careful of Epilepsy, factors that could cause Seizures, other genetics

Take Home Messages

  • Neuropathic pain is common, and often misdiagnosed
  • There are limited treatments, but treatment is relatively successful
  • Follow the principles and you won't get into strife
  • Make the most of acute and chronic pain services within hospitals (both public and private)

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