Pharmacology: Codeine Overview
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Questions and Answers

Which of the following is a property of meperidine compared to morphine?

  • It has weaker analgesic effects. (correct)
  • It has a higher bioavailability. (correct)
  • It exhibits vagal stimulation effects.
  • It has stronger spasmogenic effects.

    • What is the primary use of methadone?

  • Only for treating seizures.
  • Analgesic and treatment for chronic opiate addiction. (correct)
  • Only for acute pain management.
  • Analgesic only.

    • How does tramadol differ from traditional opioids?

  • It binds to the δ-opioid receptor only.
  • It is only effective for treating cancer pain.
  • It inhibits serotonin and norepinephrine reuptake. (correct)
  • It has no risk of addiction.

    • Which synthetic opioid is the most potent and has the shortest duration of action?

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

    What is a common adverse effect associated with tramadol?

    <p>Seizures in epileptic patients</p> Signup and view all the answers

    What characterizes the autonomic effects of meperidine?

    <p>It has atropine-like actions.</p> Signup and view all the answers

    What is the main reason methadone is used in treating opiate addiction?

    <p>It satisfies craving needs with less severe withdrawal symptoms.</p> Signup and view all the answers

    How does fentanyl compare to oral morphine in terms of dosage for pain management?

    <p>A 12 microgram patch of fentanyl is approximately equivalent to 30 mg of oral morphine daily.</p> Signup and view all the answers

    What is the primary difference between codeine and morphine in terms of their oral bioavailability?

    <p>Codeine has a bioavailability of 60%, while morphine has 25%.</p> Signup and view all the answers

    Which of the following statements regarding the analgesic potency of codeine is true?

    <p>Codeine's analgesic potency is 20% that of morphine.</p> Signup and view all the answers

    In which of the following scenarios is meperidine specifically used over morphine?

    <p>During labor due to its short duration and minimal spasmogenic action.</p> Signup and view all the answers

    What major adverse effect is associated with codeine use?

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

    Which semisynthetic mixed agonist-antagonist is noted to have a different mechanism of action regarding the mu receptors compared to others in its class?

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

    Why are heroin and hydromorphone not commonly used clinically despite their potency?

    <p>They are highly addictive.</p> Signup and view all the answers

    What is the mechanism by which codeine exerts most of its systemic effects?

    <p>Conversion in the liver into morphine.</p> Signup and view all the answers

    What is a primary reason for the contraindication of semisynthetic mixed agonists-antagonists in patients with acute myocardial infarction?

    <p>They enhance systemic and pulmonary vascular resistance.</p> Signup and view all the answers

    Which synthetic full antagonist has a longer half-life and can be administered orally?

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

    What key therapeutic use sets codeine apart from morphine, in terms of its effect?

    <p>It is a more effective cough suppressant.</p> Signup and view all the answers

    Which statement about the risk of addiction for codeine compared to morphine is accurate?

    <p>Codeine has a lower addiction liability than morphine.</p> Signup and view all the answers

    What significant effect do naloxone and naltrexone have when administered to opioid-addicted patients?

    <p>They can precipitate severe withdrawal syndrome.</p> Signup and view all the answers

    What is the immediate therapeutic use of naloxone in cases of acute opioid toxicity?

    <p>It reverses the adverse respiratory and cardiovascular effects.</p> Signup and view all the answers

    Semisynthetic mixed agonists-antagonists display what characteristic when administered to opioid-addicted patients?

    <p>They can lead to withdrawal symptoms.</p> Signup and view all the answers

    Which of the following statements about naloxone is true?

    <p>Its half-life is approximately 1 hour.</p> Signup and view all the answers

    What should be prioritized over efficacy when considering the administration of analgesics to patients at risk of respiratory depression?

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

    Diphenoxylate is classified as a semisynthetic mixed agonist-antagonist.

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

    All semisynthetic mixed agonists-antagonists, including nalbuphine, exhibit agonist activity on mu receptors.

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

    Naloxone has a longer half-life than naltrexone and is typically administered orally.

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

    All semisynthetic mixed agonists-antagonists lead to decreased cardiac load.

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

    The primary therapeutic use of naloxone is to prevent severe withdrawal syndrome in opioid-addicted patients.

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

    Synthetic full antagonists compete with opioids at all opioid receptor sites.

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

    Semisynthetic mixed agonists-antagonists can precipitate withdrawal symptoms in patients who are opioid addicts.

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

    Naltrexone can be used to reverse the respiratory depression effects of opioids immediately.

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

    Codeine has a higher oral bioavailability than morphine.

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

    Mepiridine has stronger analgesic potency than morphine.

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

    Codeine is considered a strong analgesic with a potency equal to that of morphine.

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

    Heroin is a semisynthetic opioid that is used clinically due to its rapid onset.

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

    Codeine is more effective as a cough suppressant than morphine.

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

    Meperidine has a stronger analgesic effect than morphine.

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

    Mepiridine is preferred over morphine for patients experiencing bradycardia.

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

    Both codeine and morphine have the same potential for addiction.

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

    Fentanyl is a synthetic opioid with the shortest duration of action.

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

    The therapeutic use of codeine is limited to its role as an analgesic.

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

    Tramadol exclusively binds to the μ-opioid receptor for its analgesic effects.

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

    Methadone offers a longer duration of action compared to morphine due to its longer half-life.

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

    Meperidine exhibits vagal stimulation effects.

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

    Fentanyl provides equivalent analgesic effects to 30 mg of oral morphine when using a 12 microgram transdermal patch.

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

    Tramadol has more side effects compared to most opioids.

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

    Both Fentanyl and alp etkda are synthetic derivatives of morphine.

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

    What are the two main mechanisms of action for tramadol?

    <p>Tramadol binds to the μ-opioid receptor and inhibits the reuptake of serotonin and norepinephrine.</p> Signup and view all the answers

    Identify the key difference in bioavailability between morphine and meperidine.

    <p>Morphine has a bioavailability of 25%, whereas meperidine's bioavailability is greater at 50%.</p> Signup and view all the answers

    What is a significant cardiovascular effect of semisynthetic mixed agonists-antagonists when administered to patients?

    <p>They increase systemic and pulmonary vascular resistance, leading to increased cardiac load.</p> Signup and view all the answers

    How does the analgesic potency of fentanyl compare to that of morphine?

    <p>Fentanyl is significantly more potent than morphine, requiring a much lower dose for similar analgesic effects.</p> Signup and view all the answers

    Describe the differing half-lives of naloxone and naltrexone.

    <p>Naloxone has a short half-life of about 1 hour, while naltrexone has a longer half-life of approximately 48 hours.</p> Signup and view all the answers

    Which opioid is indicated for use in treating chronic opiate addiction and why?

    <p>Methadone is indicated for treating chronic opiate addiction due to its less addictive features and milder withdrawal symptoms.</p> Signup and view all the answers

    What can result from administering semisynthetic mixed agonists-antagonists to opioid-addicted patients?

    <p>They can precipitate withdrawal symptoms in opioid-addicted patients.</p> Signup and view all the answers

    What autonomic effects are associated with meperidine, and how do they differ from those of morphine?

    <p>Meperidine has atropine-like actions leading to dry mouth and tachycardia, while morphine causes vagal stimulation.</p> Signup and view all the answers

    Describe the clinical significance of the analgesic effect of alfentanil compared to other opioids.

    <p>Alfentanil is known for its rapid onset and is used in severe pain management scenarios, similar to fentanyl.</p> Signup and view all the answers

    What role does naloxone serve during labor for mothers who have received opioids?

    <p>It is administered to prevent neonatal respiratory depression.</p> Signup and view all the answers

    How do naloxone and naltrexone function as opioid antagonists?

    <p>They are competitive blockers of all opioid receptors.</p> Signup and view all the answers

    Why is the risk of seizures a concern when using tramadol, particularly in certain patients?

    <p>Tramadol can induce seizures in epileptic patients due to its effects on neurotransmitter reuptake.</p> Signup and view all the answers

    What makes fentanyl patches a preferred option for chronic pain management?

    <p>Fentanyl patches provide a long-lasting analgesic effect, allowing for consistent pain control without frequent dosing.</p> Signup and view all the answers

    What is the primary therapeutic use of naloxone in cases of acute opioid toxicity?

    <p>It is used to reverse adverse respiratory and cardiovascular effects of opioids.</p> Signup and view all the answers

    Why is the potency of the analgesic important for opioid analgesics, particularly in relation to respiratory depression?

    <p>Analgesic potency should be considered more important than efficacy because respiratory depression is dose-dependent.</p> Signup and view all the answers

    Describe the agonist and antagonist properties of semisynthetic mixed agonists-antagonists.

    <p>They exhibit agonist activity on kappa receptors and antagonist or partial agonist activity on mu receptors.</p> Signup and view all the answers

    What is the primary reason codeine is considered to have a lesser addiction liability compared to morphine?

    <p>Codeine has a lower euphoric effect than morphine.</p> Signup and view all the answers

    Why is meperidine preferred over morphine during labor?

    <p>Meperidine has a shorter duration and does not prolong labor.</p> Signup and view all the answers

    Explain how the pharmacological effects of codeine primarily occur.

    <p>Codeine is metabolized in the liver to morphine, which accounts for most of its systemic effects.</p> Signup and view all the answers

    What differentiates heroin from morphine in terms of clinical use?

    <p>Heroin is not used clinically due to its high potential for addiction despite being more potent.</p> Signup and view all the answers

    Identify one key therapeutic use of codeine aside from its analgesic properties.

    <p>Codeine is used as a central antitussive.</p> Signup and view all the answers

    What systemic effect does codeine share with morphine, despite its lower potency?

    <p>Both can cause constipation as an adverse effect.</p> Signup and view all the answers

    Discuss the oral bioavailability of meperidine compared to morphine.

    <p>Meperidine has better oral absorption and greater bioavailability than morphine.</p> Signup and view all the answers

    What is the typical analgesic potency of meperidine relative to morphine?

    <p>Mepiridine has an analgesic potency of about 10% that of morphine.</p> Signup and view all the answers

    Codeine is considered a ______ analgesic with only 20% of the potency of morphine.

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

    Most of the systemic effects of codeine are due to its conversion in the liver into ______.

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

    Mepiridine has a greater oral ______ compared to morphine.

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

    Meperidine is preferred during labor because it has a short ______ and does not prolong labor.

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

    Heroin and hydromorphone are more potent than ______ but are not used clinically due to their addictive nature.

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

    Codeine is more effective as a ______ suppressant compared to morphine.

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

    The analgesic potency of meperidine is ______% of morphine.

    <p>10</p> Signup and view all the answers

    Adverse effects of codeine include constipation and ______ depression.

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

    Meperidine has ______ analgesic effect compared to morphine.

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

    Fentanyl and alfentanil are the most potent and the shortest duration ______ agonists.

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

    Methadone can satisfy the craving needs of the patient with ______ addictive features.

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

    Tramadol binds to the μ-opioid receptor and inhibits the reuptake of ______ and NA.

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

    The analgesic effect of methadone is equal to that of ______.

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

    A transdermal fentanyl patch equates to approximately ______ mg oral morphine daily.

    <p>30</p> Signup and view all the answers

    Tramadol administers relatively fewer ______ than most opioids.

    <p>side-effects</p> Signup and view all the answers

    In terms of bioavailability, meperidine has a greater value than ______.

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

    Nalorphine and nalbuphine exhibit agonist activity on ______ receptors.

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

    The analgesic activity of semisynthetic mixed agonists-antagonists is ______ than that of morphine.

    <p>less marked</p> Signup and view all the answers

    Synthetic full antagonists like naloxone and naltrexone are competitive blockers of all ______ receptors.

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

    Naloxone has a short half-life of approximately ______ hours.

    <p>1</p> Signup and view all the answers

    Naltrexone has a longer half-life of about ______ hours.

    <p>48</p> Signup and view all the answers

    The primary therapeutic use of naloxone is to reverse the adverse respiratory and ______ effects of opioids.

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

    Withdrawal symptoms can occur if semisynthetic mixed agonists-antagonists are given to ______ patients.

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

    Efficacy should be considered less important than ______ when administering pain relief to patients susceptible to respiratory depression.

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

    Match the following opioids with their key characteristics:

    <p>Codeine = 20% analgesic potency of morphine Mepiridine = Better absorbed orally than morphine Heroin = Diacetylmorphine Hydromorphone = More potent than morphine</p> Signup and view all the answers

    Match the following opioids with their primary clinical uses:

    <p>Codeine = Analgesic and antitussive Mepiridine = Preferred during labor Heroin = Not used clinically Hydromorphone = Not specified in the content</p> Signup and view all the answers

    Match the following opioids with their bioavailability:

    <p>Morphine = 25% Codeine = 60% Mepiridine = Greater than morphine Heroin = Not specified in the content</p> Signup and view all the answers

    Match the following medications with their adverse effects:

    <p>Codeine = Less risk for respiratory depression Mepiridine = Weaker addiction liability than morphine Heroin = Highly addictive Hydromorphone = Not specified in the content</p> Signup and view all the answers

    Match the following opioids with their conversion in the body:

    <p>Codeine = Converted to morphine in the liver Mepiridine = Not primarily metabolized to morphine Heroin = Rapidly converted to morphine Hydromorphone = Not specified in the content</p> Signup and view all the answers

    Match the following opioids with their effects on cough suppression:

    <p>Morphine = Weak antitussive effect Codeine = Strong antitussive effect Mepiridine = Not specified in the content Hydromorphone = Not specified in the content</p> Signup and view all the answers

    Match the opioids with their respective key points:

    <p>Codeine = Methylmorphine Mepiridine = Used for inferior MI Heroin = Not clinically used due to addiction Hydromorphone = Similar to morphine with rapid onset</p> Signup and view all the answers

    Match the following opioids with their duration of action:

    <p>Morphine = Long duration Mepiridine = Short duration Codeine = Not specified in the content Heroin = Short duration</p> Signup and view all the answers

    Match the opioid with its primary effect:

    <p>Fentanyl = Most potent synthetic opioid Methadone = Long duration of action Tramadol = Dual mechanism of action Meperidine = Vagal stimulation effects</p> Signup and view all the answers

    Match the opioid to its typical use:

    <p>Methadone = Chronic opiate addiction treatment Fentanyl = Severe pain management via skin patch Meperidine = Analgesic for specific pain types Tramadol = Moderate to severe musculoskeletal pain</p> Signup and view all the answers

    Match the opioid with its bioavailability:

    <p>Morphine = 25% Meperidine = Greater (50%) Tramadol = Variable depending on formulation Fentanyl = High through transdermal system</p> Signup and view all the answers

    Match the opioid to its risk of addiction:

    <p>Methadone = Lower risk compared to others Meperidine = Higher risk in multiple uses Tramadol = Moderate risk with potential seizures Fentanyl = High risk due to potency</p> Signup and view all the answers

    Match the opioid with its mechanism of action:

    <p>Tramadol = μ-opioid receptor binding and serotonin reuptake inhibition Meperidine = Atropine-like action Methadone = Full agonist with longer half-life Fentanyl = Full agonist, highly potent</p> Signup and view all the answers

    Match the opioid with its spasmogenic effects:

    <p>Morphine = Present spasmogenic effects Meperidine = Absent spasmogenic effects Methadone = Equal spasmogenic effects as morphine Tramadol = Minimal spasmogenic effects</p> Signup and view all the answers

    Match the synthetic opioid with its distinct feature:

    <p>Fentanyl = Short-acting Meperidine = Atropine-like side effects Methadone = Efficacious for addiction management Tramadol = Dual action in pain modulation</p> Signup and view all the answers

    Match the opioid with its adverse effects:

    <p>Tramadol = Seizure risk in epileptics Meperidine = Dry mouth and tachycardia Methadone = Less severe withdrawal symptoms Fentanyl = Potential overdose due to dosage sensitivity</p> Signup and view all the answers

    Match the following semisynthetic mixed agonists-antagonists with their notable characteristics:

    <p>Nalorphine = Agonist activity on κ receptors Nalbuphine = Partial agonist on μ receptors Butorphanol = Used to relieve pain of acute MI Pentazocine = Respiratory depression similar to morphine</p> Signup and view all the answers

    Match the following drugs with their primary administration routes and pharmacokinetic properties:

    <p>Naloxone = Intravenous administration, short half-life (~1h) Naltrexone = Oral administration, long half-life (~48h) Butorphanol = Intranasal administration, rapid onset Pentazocine = Subcutaneous administration, slower onset</p> Signup and view all the answers

    Match the following statements with their corresponding drug types:

    <p>Naloxone = Precipitates severe withdrawal symptoms in opioid addicts Naltrexone = Used for opioid maintenance therapy Pentazocine = Alternative to morphine for pain relief Butorphanol = Commonly induces vascular resistance increase</p> Signup and view all the answers

    Match the following characteristics with the correct therapeutic use of naloxone:

    <p>Reversal of opioid overdose = Acts within 1-2 minutes Prevention of neonatal respiratory depression = Administered to mothers during labor Emergency treatment in acute MI = Contraindicated due to increased cardiac load Opioid withdrawal management = Used to mitigate withdrawal symptoms</p> Signup and view all the answers

    Match the following responses of semisynthetic mixed agonists-antagonists in opioid-addicted patients:

    <p>Nalbuphine = May cause withdrawal symptoms Pentazocine = Can increase cardiac load Butorphanol = Less respiratory depression than morphine Nalorphine = Not effective in managing acute pain</p> Signup and view all the answers

    Match the following opioids with their effects regarding respiratory depression:

    <p>Naloxone = Reverses respiratory depression effects Naltrexone = Long-term blockade of opioid effects Pentazocine = Moderate respiratory depression relative to morphine Metamizole = Not an opioid, less respiratory impact</p> Signup and view all the answers

    Match the following types of opioid receptors to their roles in the pharmacology of pain relief:

    <p>μ receptors = Primary mediators of analgesia κ receptors = Associated with dysphoria δ receptors = Contribute to analgesia but less understood σ receptors = Not directly involved in pain relief</p> Signup and view all the answers

    Match the following opioid-related concepts with their definitions:

    <p>Therapeutic use of naloxone = Reversal of opioid overdose effects within minutes Withdrawal symptoms in opioid addicts = Caused by misuse of mixed agonist-antagonists Agonist activity on κ receptors = Characteristic of semisynthetic mixed agonists Cardiac load increase = Effect of some mixed agonists during administration</p> Signup and view all the answers

    Study Notes

    Codeine

    • Codeine is a methylmorphine derivative with 60% oral bioavailability due to reduced first-pass metabolism.
    • Analgesic potency is 20% compared to morphine, but codeine is a more effective cough suppressant.
    • Minimal euphoric effects, with systemic actions primarily from conversion to morphine in the liver.
    • Therapeutic uses: analgesic for mild to moderate pain (often combined with paracetamol) and as a central antitussive.
    • Adverse effects are less severe than morphine and include constipation, respiratory depression, and lower addiction potential.

    Comparison of Codeine and Morphine

    • Codeine:
      • Bioavailability: 60%
      • Analgesic effect: Weak (20% of morphine)
      • Antitussive effect: Strong
    • Morphine:
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Antitussive effect: Weak

    Synthetic and Semisynthetic Opioid Agonists

    • Heroin and Hydromorphone: Semisynthetic opioids; more potent than morphine with rapid onset and shorter duration; highly addictive and not used clinically.
    • Meperidine (Pethidine):
      • Synthetic opioid with greater oral bioavailability.
      • Analgesic potency is 10% of morphine.
      • Used for inferior myocardial infarction and during labor due to quick action.
      • Adverse effects include respiratory depression, weaker addiction liability, histamine release, and atropine-like symptoms.

    Comparison of Meperidine and Morphine

    • Meperidine:
      • Chemistry: Synthetic opioid
      • Bioavailability: >50%
      • Analgesic effect: Weak (10% of morphine)
      • Spasmogenic effects: Absent
    • Morphine:
      • Chemistry: Natural opioid
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Spasmogenic effects: Present

    Fentanyl and Alfentanil

    • Synthetic derivatives of meperidine; the most potent opioids with the shortest duration of action.
    • Utilized for severe pain relief, often delivered via long-acting transdermal patches.

    Methadone

    • A synthetic opioid comparable to morphine in analgesic effect but with a longer duration of action (half-life of 24 hours).
    • Applications include chronic opioid addiction treatment, providing less addictive features and milder withdrawal symptoms.

    Tramadol

    • Functions through dual mechanisms: binds to μ-opioid receptors and inhibits serotonin and norepinephrine reuptake.
    • Effective for moderate to severe pain, especially musculoskeletal.
    • Fewer adverse effects than most opioids, but may induce seizures in epilepsy patients.

    Semisynthetic Mixed Agonists-Antagonists

    • Include nalorphine, nalbuphine, pentazocine, and butorphanol; they exhibit agonist activity on κ receptors and partial agonist/antagonist activity on μ receptors.
    • Offer analgesic alternatives to morphine with less marked analgesic activity and respiratory depression.
    • Blacklisted in acute myocardial infarctions as they increase cardiac load and may prompt withdrawal symptoms in opioid-dependent patients.

    Synthetic Full Antagonists

    • Naloxone and naltrexone are competitive blockers for all opioid receptors.
    • Naloxone has a short half-life (~1 hour), administered intravenously; naltrexone has a longer half-life (~48 hours), can be given orally.
    • Administered in cases of acute opioid toxicity to reverse harmful respiratory and cardiovascular effects, acting in 1-2 minutes with effects lasting 1-2 hours.
    • Used during labor to mitigate neonatal respiratory depression caused by maternal opioid use.

    Codeine

    • Codeine is a methylmorphine derivative with 60% oral bioavailability due to reduced first-pass metabolism.
    • Analgesic potency is 20% compared to morphine, but codeine is a more effective cough suppressant.
    • Minimal euphoric effects, with systemic actions primarily from conversion to morphine in the liver.
    • Therapeutic uses: analgesic for mild to moderate pain (often combined with paracetamol) and as a central antitussive.
    • Adverse effects are less severe than morphine and include constipation, respiratory depression, and lower addiction potential.

    Comparison of Codeine and Morphine

    • Codeine:
      • Bioavailability: 60%
      • Analgesic effect: Weak (20% of morphine)
      • Antitussive effect: Strong
    • Morphine:
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Antitussive effect: Weak

    Synthetic and Semisynthetic Opioid Agonists

    • Heroin and Hydromorphone: Semisynthetic opioids; more potent than morphine with rapid onset and shorter duration; highly addictive and not used clinically.
    • Meperidine (Pethidine):
      • Synthetic opioid with greater oral bioavailability.
      • Analgesic potency is 10% of morphine.
      • Used for inferior myocardial infarction and during labor due to quick action.
      • Adverse effects include respiratory depression, weaker addiction liability, histamine release, and atropine-like symptoms.

    Comparison of Meperidine and Morphine

    • Meperidine:
      • Chemistry: Synthetic opioid
      • Bioavailability: >50%
      • Analgesic effect: Weak (10% of morphine)
      • Spasmogenic effects: Absent
    • Morphine:
      • Chemistry: Natural opioid
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Spasmogenic effects: Present

    Fentanyl and Alfentanil

    • Synthetic derivatives of meperidine; the most potent opioids with the shortest duration of action.
    • Utilized for severe pain relief, often delivered via long-acting transdermal patches.

    Methadone

    • A synthetic opioid comparable to morphine in analgesic effect but with a longer duration of action (half-life of 24 hours).
    • Applications include chronic opioid addiction treatment, providing less addictive features and milder withdrawal symptoms.

    Tramadol

    • Functions through dual mechanisms: binds to μ-opioid receptors and inhibits serotonin and norepinephrine reuptake.
    • Effective for moderate to severe pain, especially musculoskeletal.
    • Fewer adverse effects than most opioids, but may induce seizures in epilepsy patients.

    Semisynthetic Mixed Agonists-Antagonists

    • Include nalorphine, nalbuphine, pentazocine, and butorphanol; they exhibit agonist activity on κ receptors and partial agonist/antagonist activity on μ receptors.
    • Offer analgesic alternatives to morphine with less marked analgesic activity and respiratory depression.
    • Blacklisted in acute myocardial infarctions as they increase cardiac load and may prompt withdrawal symptoms in opioid-dependent patients.

    Synthetic Full Antagonists

    • Naloxone and naltrexone are competitive blockers for all opioid receptors.
    • Naloxone has a short half-life (~1 hour), administered intravenously; naltrexone has a longer half-life (~48 hours), can be given orally.
    • Administered in cases of acute opioid toxicity to reverse harmful respiratory and cardiovascular effects, acting in 1-2 minutes with effects lasting 1-2 hours.
    • Used during labor to mitigate neonatal respiratory depression caused by maternal opioid use.

    Codeine

    • Codeine is a methylmorphine derivative with 60% oral bioavailability due to reduced first-pass metabolism.
    • Analgesic potency is 20% compared to morphine, but codeine is a more effective cough suppressant.
    • Minimal euphoric effects, with systemic actions primarily from conversion to morphine in the liver.
    • Therapeutic uses: analgesic for mild to moderate pain (often combined with paracetamol) and as a central antitussive.
    • Adverse effects are less severe than morphine and include constipation, respiratory depression, and lower addiction potential.

    Comparison of Codeine and Morphine

    • Codeine:
      • Bioavailability: 60%
      • Analgesic effect: Weak (20% of morphine)
      • Antitussive effect: Strong
    • Morphine:
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Antitussive effect: Weak

    Synthetic and Semisynthetic Opioid Agonists

    • Heroin and Hydromorphone: Semisynthetic opioids; more potent than morphine with rapid onset and shorter duration; highly addictive and not used clinically.
    • Meperidine (Pethidine):
      • Synthetic opioid with greater oral bioavailability.
      • Analgesic potency is 10% of morphine.
      • Used for inferior myocardial infarction and during labor due to quick action.
      • Adverse effects include respiratory depression, weaker addiction liability, histamine release, and atropine-like symptoms.

    Comparison of Meperidine and Morphine

    • Meperidine:
      • Chemistry: Synthetic opioid
      • Bioavailability: >50%
      • Analgesic effect: Weak (10% of morphine)
      • Spasmogenic effects: Absent
    • Morphine:
      • Chemistry: Natural opioid
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Spasmogenic effects: Present

    Fentanyl and Alfentanil

    • Synthetic derivatives of meperidine; the most potent opioids with the shortest duration of action.
    • Utilized for severe pain relief, often delivered via long-acting transdermal patches.

    Methadone

    • A synthetic opioid comparable to morphine in analgesic effect but with a longer duration of action (half-life of 24 hours).
    • Applications include chronic opioid addiction treatment, providing less addictive features and milder withdrawal symptoms.

    Tramadol

    • Functions through dual mechanisms: binds to μ-opioid receptors and inhibits serotonin and norepinephrine reuptake.
    • Effective for moderate to severe pain, especially musculoskeletal.
    • Fewer adverse effects than most opioids, but may induce seizures in epilepsy patients.

    Semisynthetic Mixed Agonists-Antagonists

    • Include nalorphine, nalbuphine, pentazocine, and butorphanol; they exhibit agonist activity on κ receptors and partial agonist/antagonist activity on μ receptors.
    • Offer analgesic alternatives to morphine with less marked analgesic activity and respiratory depression.
    • Blacklisted in acute myocardial infarctions as they increase cardiac load and may prompt withdrawal symptoms in opioid-dependent patients.

    Synthetic Full Antagonists

    • Naloxone and naltrexone are competitive blockers for all opioid receptors.
    • Naloxone has a short half-life (~1 hour), administered intravenously; naltrexone has a longer half-life (~48 hours), can be given orally.
    • Administered in cases of acute opioid toxicity to reverse harmful respiratory and cardiovascular effects, acting in 1-2 minutes with effects lasting 1-2 hours.
    • Used during labor to mitigate neonatal respiratory depression caused by maternal opioid use.

    Codeine

    • Codeine is a methylmorphine derivative with 60% oral bioavailability due to reduced first-pass metabolism.
    • Analgesic potency is 20% compared to morphine, but codeine is a more effective cough suppressant.
    • Minimal euphoric effects, with systemic actions primarily from conversion to morphine in the liver.
    • Therapeutic uses: analgesic for mild to moderate pain (often combined with paracetamol) and as a central antitussive.
    • Adverse effects are less severe than morphine and include constipation, respiratory depression, and lower addiction potential.

    Comparison of Codeine and Morphine

    • Codeine:
      • Bioavailability: 60%
      • Analgesic effect: Weak (20% of morphine)
      • Antitussive effect: Strong
    • Morphine:
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Antitussive effect: Weak

    Synthetic and Semisynthetic Opioid Agonists

    • Heroin and Hydromorphone: Semisynthetic opioids; more potent than morphine with rapid onset and shorter duration; highly addictive and not used clinically.
    • Meperidine (Pethidine):
      • Synthetic opioid with greater oral bioavailability.
      • Analgesic potency is 10% of morphine.
      • Used for inferior myocardial infarction and during labor due to quick action.
      • Adverse effects include respiratory depression, weaker addiction liability, histamine release, and atropine-like symptoms.

    Comparison of Meperidine and Morphine

    • Meperidine:
      • Chemistry: Synthetic opioid
      • Bioavailability: >50%
      • Analgesic effect: Weak (10% of morphine)
      • Spasmogenic effects: Absent
    • Morphine:
      • Chemistry: Natural opioid
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Spasmogenic effects: Present

    Fentanyl and Alfentanil

    • Synthetic derivatives of meperidine; the most potent opioids with the shortest duration of action.
    • Utilized for severe pain relief, often delivered via long-acting transdermal patches.

    Methadone

    • A synthetic opioid comparable to morphine in analgesic effect but with a longer duration of action (half-life of 24 hours).
    • Applications include chronic opioid addiction treatment, providing less addictive features and milder withdrawal symptoms.

    Tramadol

    • Functions through dual mechanisms: binds to μ-opioid receptors and inhibits serotonin and norepinephrine reuptake.
    • Effective for moderate to severe pain, especially musculoskeletal.
    • Fewer adverse effects than most opioids, but may induce seizures in epilepsy patients.

    Semisynthetic Mixed Agonists-Antagonists

    • Include nalorphine, nalbuphine, pentazocine, and butorphanol; they exhibit agonist activity on κ receptors and partial agonist/antagonist activity on μ receptors.
    • Offer analgesic alternatives to morphine with less marked analgesic activity and respiratory depression.
    • Blacklisted in acute myocardial infarctions as they increase cardiac load and may prompt withdrawal symptoms in opioid-dependent patients.

    Synthetic Full Antagonists

    • Naloxone and naltrexone are competitive blockers for all opioid receptors.
    • Naloxone has a short half-life (~1 hour), administered intravenously; naltrexone has a longer half-life (~48 hours), can be given orally.
    • Administered in cases of acute opioid toxicity to reverse harmful respiratory and cardiovascular effects, acting in 1-2 minutes with effects lasting 1-2 hours.
    • Used during labor to mitigate neonatal respiratory depression caused by maternal opioid use.

    Codeine

    • Codeine is a methylmorphine derivative with 60% oral bioavailability due to reduced first-pass metabolism.
    • Analgesic potency is 20% compared to morphine, but codeine is a more effective cough suppressant.
    • Minimal euphoric effects, with systemic actions primarily from conversion to morphine in the liver.
    • Therapeutic uses: analgesic for mild to moderate pain (often combined with paracetamol) and as a central antitussive.
    • Adverse effects are less severe than morphine and include constipation, respiratory depression, and lower addiction potential.

    Comparison of Codeine and Morphine

    • Codeine:
      • Bioavailability: 60%
      • Analgesic effect: Weak (20% of morphine)
      • Antitussive effect: Strong
    • Morphine:
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Antitussive effect: Weak

    Synthetic and Semisynthetic Opioid Agonists

    • Heroin and Hydromorphone: Semisynthetic opioids; more potent than morphine with rapid onset and shorter duration; highly addictive and not used clinically.
    • Meperidine (Pethidine):
      • Synthetic opioid with greater oral bioavailability.
      • Analgesic potency is 10% of morphine.
      • Used for inferior myocardial infarction and during labor due to quick action.
      • Adverse effects include respiratory depression, weaker addiction liability, histamine release, and atropine-like symptoms.

    Comparison of Meperidine and Morphine

    • Meperidine:
      • Chemistry: Synthetic opioid
      • Bioavailability: >50%
      • Analgesic effect: Weak (10% of morphine)
      • Spasmogenic effects: Absent
    • Morphine:
      • Chemistry: Natural opioid
      • Bioavailability: 25%
      • Analgesic effect: Strong
      • Spasmogenic effects: Present

    Fentanyl and Alfentanil

    • Synthetic derivatives of meperidine; the most potent opioids with the shortest duration of action.
    • Utilized for severe pain relief, often delivered via long-acting transdermal patches.

    Methadone

    • A synthetic opioid comparable to morphine in analgesic effect but with a longer duration of action (half-life of 24 hours).
    • Applications include chronic opioid addiction treatment, providing less addictive features and milder withdrawal symptoms.

    Tramadol

    • Functions through dual mechanisms: binds to μ-opioid receptors and inhibits serotonin and norepinephrine reuptake.
    • Effective for moderate to severe pain, especially musculoskeletal.
    • Fewer adverse effects than most opioids, but may induce seizures in epilepsy patients.

    Semisynthetic Mixed Agonists-Antagonists

    • Include nalorphine, nalbuphine, pentazocine, and butorphanol; they exhibit agonist activity on κ receptors and partial agonist/antagonist activity on μ receptors.
    • Offer analgesic alternatives to morphine with less marked analgesic activity and respiratory depression.
    • Blacklisted in acute myocardial infarctions as they increase cardiac load and may prompt withdrawal symptoms in opioid-dependent patients.

    Synthetic Full Antagonists

    • Naloxone and naltrexone are competitive blockers for all opioid receptors.
    • Naloxone has a short half-life (~1 hour), administered intravenously; naltrexone has a longer half-life (~48 hours), can be given orally.
    • Administered in cases of acute opioid toxicity to reverse harmful respiratory and cardiovascular effects, acting in 1-2 minutes with effects lasting 1-2 hours.
    • Used during labor to mitigate neonatal respiratory depression caused by maternal opioid use.

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    Description

    This quiz explores the pharmacological properties of codeine, highlighting its similarities and differences with morphine. It delves into its oral bioavailability, analgesic potency, and therapeutic uses, particularly as an analgesic for mild to moderate pain. Understanding codeine's conversion in the liver and its effects is essential for healthcare professionals.

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