Textbook Chpt. 11 Opioids

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Questions and Answers

What aspect of methadone treatment is primarily linked to its effectiveness in preventing withdrawal symptoms?

  • Daily attendance requirements at the clinic
  • The progressive increase in dosage over time
  • The use of short-acting opioids prior to treatment
  • The establishment of a trusting relationship with well-trained staff (correct)

Why is the development of tolerance to methadone considered unusual compared to short-acting opioids?

  • Patients often misuse methadone, reducing tolerance effects
  • Methadone binds more effectively to the opioid receptors
  • Methadone has a faster onset of action than short-acting opioids
  • Methadone is an NMDA-receptor antagonist (correct)

What is a common side effect of methadone treatment?

  • Excessive sweating (correct)
  • Increased alertness
  • Improved mood stability
  • Rapid weight loss

How does the withdrawal period of methadone compare to that of morphine when abruptly discontinued?

<p>It lasts longer but is milder (C)</p> Signup and view all the answers

What is a notable societal challenge faced by individuals undergoing methadone treatment?

<p>Discrimination in various social and economic areas (B)</p> Signup and view all the answers

What is the typical approach to detoxifying a patient from methadone once they are ready to discontinue its use?

<p>Lowering doses over an extended period (D)</p> Signup and view all the answers

What percentage range represents the retention rates within the first year for patients on methadone?

<p>70% to 84% (D)</p> Signup and view all the answers

Which factor can interfere with a patient's life while undergoing methadone maintenance treatment?

<p>The requirement for daily clinic attendance (C)</p> Signup and view all the answers

Which term is often used to describe the restrictive nature of methadone treatment in relation to daily life?

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

What must patients demonstrate before being allowed to take methadone home rather than attending the clinic daily?

<p>Evidence of long-term sobriety from heroin (A)</p> Signup and view all the answers

What is a primary effect of repeated opioid use on tolerance development?

<p>Pain sensitivity may increase with chronic use. (B)</p> Signup and view all the answers

Which of the following opioid effects does not disappear over time, even with continued use?

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

What mechanism is involved in the development of opioid tolerance?

<p>Changes in the density or properties of opioid receptors. (A)</p> Signup and view all the answers

Which symptom is commonly associated with opioid withdrawal?

<p>Intense cravings for opioids (C)</p> Signup and view all the answers

What is a potential consequence of opioid addiction highlighted by the content?

<p>Physical dependence and withdrawal symptoms. (A)</p> Signup and view all the answers

Why might methadone be used in treating opiate dependency?

<p>It helps alleviate withdrawal symptoms without causing significant intoxication. (D)</p> Signup and view all the answers

What happens to μ and δ receptors following stimulation by an agonist?

<p>They are internalized into the cell. (A)</p> Signup and view all the answers

How is the rate of tolerance development different for various opioid effects?

<p>Tolerance to analgesic effects develops more rapidly than to constipating effects. (A)</p> Signup and view all the answers

What was the observed effect on the monkeys' behavior during opioid withdrawal in the study by Thompson and Schuster?

<p>Deterioration in shock-avoidance behavior (C)</p> Signup and view all the answers

Which statement accurately reflects the relationship between detoxification and addiction treatment?

<p>Long-term treatments follow detoxification due to brain changes from chronic opioid use. (D)</p> Signup and view all the answers

What is the primary pharmacological mechanism utilized in the abrupt approach to detoxification for opioid addiction?

<p>Total abstinence from opioids or administration of opioid antagonists (D)</p> Signup and view all the answers

Which aspect of opioid withdrawal is most notably uncomfortable for individuals undergoing detoxification?

<p>Severe physical discomfort and behavioral disruption (A)</p> Signup and view all the answers

What role does methadone play in the treatment of opiate dependency?

<p>It acts as a full opioid agonist to replace lost opioids. (A)</p> Signup and view all the answers

What is the typical timeline for the onset of withdrawal symptoms following the last administration of heroin?

<p>6 to 12 hours (C)</p> Signup and view all the answers

Which of the following substances is least likely to cause fatal withdrawal symptoms?

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

What neurotransmitter system, besides endogenous opioids, is involved in opioid-induced hyperalgesia?

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

Which opioid is associated with increased sensitivity to pain during treatment?

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

What is a classic withdrawal symptom that starts shortly after ceasing opioid use?

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

Prolonged administration of which opioid can produce neurotoxic effects on cells in the dorsal horn of the spinal cord?

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

During opioid withdrawal, how long can basic symptoms persist before improving?

<p>1 to 2 weeks (D)</p> Signup and view all the answers

What describes the risk of psychological dependence on methadone when treating opiate dependency?

<p>Can lead to increased risk of addiction (C)</p> Signup and view all the answers

What effect does acute administration of remifentanil have on opioid-naïve individuals?

<p>Increased pain sensitivity after cessation (C)</p> Signup and view all the answers

Which of the following is true about opioid tolerance?

<p>Leads to decreased effectiveness of pain relief over time (B)</p> Signup and view all the answers

What is the primary mechanism of acute tolerance related to opioid receptors?

<p>Reduction in the number of membrane opioid receptors (A)</p> Signup and view all the answers

Which opioid receptor is preferentially recycled back to the cell surface, promoting recovery in signaling?

<p>Mu (μ) receptors (C)</p> Signup and view all the answers

How does internalization of delta (d) receptors affect opioid tolerance?

<p>It increases opioid tolerance through degradation (A)</p> Signup and view all the answers

Which of the following drugs is noted for causing rapid endocytosis of opioid receptors?

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

What challenge arises when estimating the therapeutic dose during opioid rotation?

<p>Cross-tolerance effects between opioids (D)</p> Signup and view all the answers

What is hyperalgesia as related to opioid use?

<p>Increased sensitivity to painful stimuli (D)</p> Signup and view all the answers

What is a potential consequence of miscalculating cross-opioid dose conversions?

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

Which aspect of methadone prescribing poses a significant risk during opioid dependency treatment?

<p>Its wide range of lethal doses (D)</p> Signup and view all the answers

Which of the following drugs would show little to no cross-tolerance effect with opioids?

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

What may occur as opioid receptors undergo endocytosis and are later recycled?

<p>Enhanced ligand binding sensitivity (B)</p> Signup and view all the answers

Flashcards

Opioid Tolerance

The body's decreasing response to an opioid over time, requiring higher doses to achieve the same effect.

Opioid Sensitization

The process where the body becomes more sensitive to an opioid's effects, even with lower doses, often leading to amplified pain.

Opioid Withdrawal

The physiological changes that occur when an opioid is stopped, resulting in unpleasant symptoms.

μ (mu) Receptor

The primary receptor responsible for opioid's analgesic (pain-relieving) effects, also contributing to tolerance.

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Opioid Receptor Internalization

The process where opioid receptors are removed from the cell membrane, reducing their effectiveness.

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δ (delta) Receptor

A receptor subtype involved in opioid's effects, but its role in tolerance is less clear.

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κ (kappa) Receptor

The receptor type that helps regulate pain but its role in tolerance is still being studied.

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Opioid-Metabolizing Enzymes

Specific enzymes involved in breaking down opioids in the body.

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Methadone: Liquid Handcuffs

Methadone maintenance programs require consistent visits to a clinic, often daily.

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Methadone's Lack of Tolerance

Methadone's unique property of not requiring dose increases due to tolerance is linked to its ability to block NMDA receptors.

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Methadone Dosage Adjustment

Methadone treatment involves a gradual increase in dosage over several weeks to reach a level that alleviates withdrawal symptoms.

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Therapist-Patient Relationship

Methadone maintenance programs prioritize building trusting relationships between patients and staff, which is crucial for success.

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Methadone's Long Duration

Methadone's prolonged duration of action helps patients avoid the constant need to seek out the illicit drug.

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Methadone's Side Effects

Methadone treatment can lead to uncomfortable side effects, such as excessive sweating, sexual dysfunction, and constipation.

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Methadone's Purpose

Methadone is used in a controlled setting to help heroin addicts manage their addiction and avoid withdrawal symptoms.

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Methadone Detoxification

Gradually reducing methadone dosage over several months helps minimize withdrawal symptoms when a patient chooses to discontinue the drug.

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Methadone's Impact on Lifestyle

Methadone treatment can help patients transition to a more normal lifestyle, encouraging them to seek further treatment and address underlying issues.

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Methadone's Challenges

Methadone treatment, despite its benefits, faces challenges, such as stigma and restrictions in areas like insurance, licensing, and housing.

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Opioid Detoxification

The process of helping an addict overcome physical opioid dependence by managing withdrawal symptoms.

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Abrupt Detoxification

A method of detoxification that involves immediately stopping opioid use or administering opioid antagonists to block receptors.

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Opioid Antagonists

Opioid antagonists like naltrexone or naloxone that displace opioid molecules from receptors, causing rapid withdrawal.

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Gradual Detoxification

A less immediate detoxification method that gradually reduces the opioid dose over time.

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Brain Changes Beyond Withdrawal

The understanding that chronic opioid use alters the brain long-term, exceeding the effects of immediate withdrawal symptoms.

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Opioid-induced sensitization

The phenomenon where repeated opioid use leads to increased pain sensitivity, even with lower doses.

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Remifentanil

A short-acting synthetic opioid that can cause hyperalgesia (increased pain sensitivity) even in people without prior opioid exposure.

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Glutamate

A key neurotransmitter involved in pain signaling and can be affected by prolonged opioid use, contributing to opioid-induced hyperalgesia.

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NMDA receptor

A receptor in the nervous system that can be affected by prolonged opioid use, ultimately contributing to the development of hyperalgesia.

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Opioid metabolism

The process by which the body eliminates opioids, breaking them down into inactive metabolites. This can vary greatly depending on the specific opioid.

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Opioid Receptor Downregulation

The reduction in the number of opioid receptors on the cell surface, contributing to tolerance.

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Opioid Receptor Sorting

The different fates of internalized opioid receptors. Some are recycled back to the surface, restoring their function, while others are degraded, reducing receptor availability.

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μ Receptor Recycling

The tendency of μ receptors to be preferentially recycled back to the cell surface, contributing to a recovery in opioid signaling and a decrease in tolerance.

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δ Receptor Degradation

The tendency of δ receptors to be preferentially degraded after internalization, leading to a significant increase in opioid tolerance.

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Opioid-Induced Receptor Internalization Rate

The ability of different opioids to cause varying degrees of receptor internalization, explaining why some opioids can lead to faster tolerance development than others.

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Opioid Rotation

The strategy of switching between different opioid medications to manage chronic pain, potentially delaying or minimizing tolerance development.

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Cross-Tolerance

The phenomenon where tolerance to one opioid can extend to other opioids, making dose estimation for switching medication challenging.

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Opioid Dose Miscalculation

The potentially dangerous consequence of miscalculating opioid dosage during medication switching, leading to overdose.

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Study Notes

Opioid Dependence

  • Repeated opioid use leads to rapid tolerance to many effects.
  • Daily doses of opioid can increase tenfold or more over months.
  • Tolerance to some opioid effects, like constipation, persists even during abstinence.
  • Opioid tolerance may involve changes in opioid metabolizing enzymes or receptor density.
  • Opioid receptors can be internalized (removed from cell membrane) which leads to acute tolerance.
  • Internalized receptors can be degraded or recycled, affecting receptor density and tolerance.
  • Endocytosis (internalization) of mu receptors may lead to opioid sensitization.
  • Mu receptors are recycled.
  • Delta receptors are degraded, leading to increased tolerance.
  • Cross-tolerance exists between some opioids but not all.
  • Withdrawal from opioids is not immediately fatal.
  • Withdrawal symptoms begin 6-12 hours after last dose and peak at 26-72 hours.
  • Withdrawal often resolves within a week.
  • Common symptoms include restlessness, agitation, yawning, chills, and sweating.
  • Withdrawal symptoms may also cause vomiting, diarrhea, and muscle cramps.

Withdrawal from Opioids

  • Withdrawal symptoms are often incorrectly portrayed in media.
  • Opioid withdrawal is not as dangerous as withdrawal from barbiturates or alcohol.
  • Symptoms usually peak within 26–72 hours and typically resolve within a week.
  • Withdrawal can be managed with medical supervision.

Pharmacotherapies for Opioid Addiction

  • Detoxification aims to eliminate physical dependence and is a step toward long-term treatment.
  • Abrupt detoxification involves total abstinence or opioid antagonist (e.g., naltrexone).
  • Gradual detoxification involves tapering illicit opioid use and substituting a medication like methadone or buprenorphine.

Opioid Maintenance Therapies

  • Methadone and buprenorphine are first-line treatments for opioid addiction.
  • Methadone is a full mu-receptor agonist that controls withdrawal symptoms for 24 hours or more.
  • Buprenorphine is a partial mu-receptor agonist that has fewer side effects than methadone but still controls cravings and withdrawal symptoms.

Antagonist Therapies

  • Antagonist therapies use drugs like naltrexone to block opioid effects, reduce craving, and encourage abstinence.
  • Naltrexone is a pure opioid antagonist with a long half-life.
  • Naltrexone blocks the euphoric and reinforcing effects of opioids.
  • Treatment success depends on high patient motivation and support from family or legal supervision.

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