Textbook Chpt. 11 Opioids

Choose a study mode

Play Quiz
Study Flashcards
Spaced Repetition
Chat to Lesson

Podcast

Play an AI-generated podcast conversation about this lesson

Questions and Answers

Which opioid is primarily metabolized to its active form morphine?

  • Oxymorphone
  • Codeine
  • Heroin (correct)
  • Methadone

What is the metabolic consequence of CYP3A4 inhibitors on opioid medications?

  • They speed up opioid metabolism.
  • They slow down opioid metabolism. (correct)
  • They have no effect on opioid metabolism.
  • They enhance opioid efficacy.

Which opioid receptor is primarily associated with mediating analgesia and sedation?

  • κ receptor
  • µ receptor (correct)
  • ORL1 receptor
  • δ receptor

What is a distinctive characteristic of methadone compared to other opioids?

<p>It has a long half-life of 25-40 hours. (C)</p> Signup and view all the answers

Which opioid is classified as a mixed agonist-antagonist?

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

Which of the following opioids is selective for µ receptors?

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

Which opioid undergoes glucuronidation to yield both active and inactive metabolites?

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

What pharmacological action does a full agonist opioid have?

<p>It binds and fully activates opioid receptors. (D)</p> Signup and view all the answers

Which of the following peptides is produced endogenously in the brain?

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

What effect does caffeine have on opioid metabolism?

<p>It speeds up metabolism. (A)</p> Signup and view all the answers

Which opioid is considered to have the highest permeability across the blood-brain barrier compared to morphine?

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

Which statement accurately describes the pharmacokinetics of morphine in terms of oral administration?

<p>Morphine is quickly ionized in the stomach, resulting in low oral bioavailability. (B)</p> Signup and view all the answers

Which factor is most responsible for the long half-life of lipophilic opioids like fentanyl?

<p>High protein binding in the bloodstream (A)</p> Signup and view all the answers

Which of the following opioids has zero percent protein binding, allowing for rapid brain distribution?

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

What type of formulations do extended-release opioids use to control the release of the active ingredient?

<p>Multiple layers or matrixes that break down at different rates (B)</p> Signup and view all the answers

Which phase of opioid metabolism is primarily responsible for modifying the drug molecule by cytochrome P450 enzymes?

<p>Phase 1: modification phase (C)</p> Signup and view all the answers

In which of the following scenarios would a parenteral administration of an opioid be preferred over oral administration?

<p>When immediate pain relief is critical (A)</p> Signup and view all the answers

Which opioid is least affected by first-pass metabolism and thus allows better absorption from the gastrointestinal tract?

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

Which of the following opioids is commonly used in the treatment of opioid addiction?

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

Which opioids have predominantly shorter durations of action due to lower protein binding?

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

Which of the following is a common synthetic opiate?

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

What is the primary medical use of methadone in addiction therapy?

<p>Opioid dependence management (B)</p> Signup and view all the answers

Which opiate is known for having the highest potency per dose?

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

How is buprenorphine primarily administered in medical settings?

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

What is the mechanism of action for most opiates in the central nervous system?

<p>Agonizing opioid receptors (D)</p> Signup and view all the answers

Which factor primarily influences the metabolism rate of opioids?

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

Which of the following statements about the kappa opioid receptor is true?

<p>It modulates emotional responses and anxiety. (D)</p> Signup and view all the answers

Which opioid acts as a partial agonist at the µ receptor and a full agonist at δ receptors?

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

Which opiate is most commonly used in the treatment of severe acute pain?

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

What is the primary mechanism of action for naloxone?

<p>Non-selective antagonist blocking several opioid receptors (D)</p> Signup and view all the answers

What is a common side effect associated with opioid analgesics?

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

Which of the following opioids primarily acts as a serotonin-norepinephrine reuptake inhibitor?

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

What type of administration is most likely to enhance the reinforcing effects of opioids?

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

What is the primary metabolite of codeine that contributes to its analgesic effects?

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

Which of these is a key characteristic of opioid tolerance?

<p>Necessitating higher doses for the same effect (C)</p> Signup and view all the answers

All of the following are methods to manage opioid overdose except:

<p>Increasing opioid dosage (B)</p> Signup and view all the answers

Which receptor does naltrexone act on as a non-selective antagonist?

<p>µ, κ, δ, and ORL1 receptors (B)</p> Signup and view all the answers

What is a potential consequence of opioid abuse?

<p>Development of tolerance and dependence (A)</p> Signup and view all the answers

Which of the following is true regarding methadone's pharmacological actions?

<p>It also functions as an NMDA antagonist (A)</p> Signup and view all the answers

What effect does rapid onset of opioid action generally have?

<p>It enhances the reinforcing effects of the opioid (A)</p> Signup and view all the answers

Flashcards

Prodrug

A drug that is inactive until it is metabolized into its active form by the body.

Metabolism

The process by which the body breaks down and transforms drugs into different forms.

CYP3A4 (Cytochrome P450 3A4)

A specific enzyme responsible for metabolizing many medications.

CYP3A4 inducer

A substance that speeds up the breakdown of a drug in the body.

Signup and view all the flashcards

CYP3A4 inhibitor

A substance that slows down the breakdown of a drug in the body.

Signup and view all the flashcards

Genetic polymorphisms

Differences in how individuals metabolize drugs due to genetic variations.

Signup and view all the flashcards

µ (mu) receptor

The primary target of most opioid drugs, responsible for analgesia, sedation, euphoria, and dependence.

Signup and view all the flashcards

Endogenous opioid peptide

A chemical substance produced by the body that binds to opioid receptors.

Signup and view all the flashcards

Opioid agonist

A drug that activates opioid receptors by binding to them.

Signup and view all the flashcards

Opioid antagonist

A drug that blocks opioid receptors and prevents them from being activated.

Signup and view all the flashcards

Full Opioid Agonist

A type of opioid medication that works by activating mu-opioid receptors, which are responsible for pain relief, sedation, and euphoria.

Signup and view all the flashcards

Partial Opioid Agonist

A type of opioid medication that only partially activates mu-opioid receptors, leading to weaker pain relief and reduced risk of overdose.

Signup and view all the flashcards

Opioid Tolerance

The tendency for the body to become less sensitive to opioids with repeated use, requiring higher doses for the same effect.

Signup and view all the flashcards

Opioid Dependence

A state of physical dependence on opioids, where withdrawal symptoms occur upon stopping use.

Signup and view all the flashcards

Opioid Overdose

A potentially fatal complication of opioid abuse, characterized by slowed breathing, decreased heart rate, and coma.

Signup and view all the flashcards

Opioid Substitution Therapy (OST)

Treatment options for opioid addiction, including medications like methadone and buprenorphine, that help manage withdrawal symptoms and reduce cravings.

Signup and view all the flashcards

Injection

A common route of administration for opioids which involves injecting the drug into the bloodstream.

Signup and view all the flashcards

Inhalation

A route of administration for opioids where the drug is inhaled through the nose or mouth.

Signup and view all the flashcards

Oral

A route of administration for opioids where the drug is taken orally, usually in pill or liquid form.

Signup and view all the flashcards

Opioid absorption: Parenteral vs. Oral

Opioids are more easily absorbed when injected directly into muscles, under the skin, or into veins compared to being swallowed.

Signup and view all the flashcards

Morphine absorption: Ionization and lipid solubility

Morphine's structure makes it poorly absorbed into the bloodstream when taken orally due to its high ionization and low lipid solubility.

This means it doesn't easily pass through the gut's acidic environment.

Signup and view all the flashcards

First-pass metabolism: Opioids

First-pass metabolism breaks down a drug in the liver before it reaches the bloodstream, limiting its effectiveness.

Morphine and heroin are significantly degraded by enzymes in the digestive system and liver, decreasing their oral bioavailability.

Signup and view all the flashcards

Extended-release opioids: Mechanism

Extended-release opioids have multiple layers that break down at different rates, ensuring a sustained release of the drug over time.

Signup and view all the flashcards

Buccal absorption: Fentanyl

Some opioids, like fentanyl, are highly fat-soluble and readily pass through the protective membranes of our mouths, making buccal absorption a preferred route.

Signup and view all the flashcards

Opioid distribution: Target organs

Opioids accumulate in vital organs such as the heart, lungs, and brain due to their ability to cross cell membranes.

Signup and view all the flashcards

Opioid distribution: Protein binding

Highly lipophilic opioids have a strong affinity for proteins, leading to prolonged retention within the body.

Signup and view all the flashcards

Opioid distribution: Protein binding (Codeine, Morphine, Hydromorphone)

Codeine, morphine, and hydromorphone lack extensive protein binding compared to highly lipophilic opioids.

Signup and view all the flashcards

Opioid metabolism: Liver enzymes

The liver's enzymes break down opioid molecules, converting them into forms that can be easily eliminated.

Signup and view all the flashcards

Opioid metabolism: Two phases

Opioid metabolism involves two main phases: Phase 1 modifies the drug molecule, and Phase 2 attaches a hydrophilic substance to make it easier to excrete.

Signup and view all the flashcards

Opioid Analgesics

A class of drugs that bind to opioid receptors in the brain and nervous system, relieving pain and producing euphoria.

Signup and view all the flashcards

Pharmacology

The study of how drugs affect the body, including their absorption, distribution, metabolism, and excretion.

Signup and view all the flashcards

Mu-Opioid Receptor

A type of opioid receptor in the brain that is involved in regulating pain, mood, and reward.

Signup and view all the flashcards

Kappa Opioid Receptor

A type of opioid receptor in the brain that is involved in regulating stress, anxiety, and motivation.

Signup and view all the flashcards

Delta Opioid Receptor

A type of opioid receptor in the brain that is involved in regulating pain, pleasure, and reward.

Signup and view all the flashcards

Pharmacokinetics

The process by which a drug is absorbed into the body, distributed throughout the body, metabolized (broken down), and eliminated.

Signup and view all the flashcards

Pharmacodynamics

The study of the effects of drugs on the body, how they work and their therapeutic effects.

Signup and view all the flashcards

Drug Half-Life

A measure of how quickly a drug leaves the body.

Signup and view all the flashcards

Addiction

The state of dependence on a substance and the unpleasant symptoms that occur when the substance is withdrawn.

Signup and view all the flashcards

Neurobiology

The science of the brain and its functions.

Signup and view all the flashcards

Study Notes

Opioid Analgesics

  • Opioids are cornerstone analgesics for moderate to severe pain.
  • Their potency, onset, duration, metabolism, and interactions with other drugs vary.
  • Individual responses differ due to genetics, medical conditions, and prior opioid use.
  • Pharmacokinetics (absorption, distribution, metabolism, and excretion) and pharmacodynamics (effects on the body) influence effectiveness.

Absorption

  • Opioids are less effective when taken orally due to their basic nature (pH).
  • Oral absorption is slower, with significant first-pass metabolism (destruction in stomach, intestines, and liver) reducing bioavailability.
  • Bioavailability is typically 15-40% for oral morphine.
  • Extended-release formulations have multiple layers to improve absorption rates.
  • Lipid solubility and decreased enzymatic degradation in the gastrointestinal tract improve bioavailability.
  • Codeine has approximately 90% bioavailability orally.
  • Hydrocodone is also well-absorbed from the gastrointestinal tract and reaches peak blood levels in ~80 minutes.
  • Oxycodone bioavailability varies between immediate-release (60-87%) and extended-release (up to 100%).

Distribution

  • Opioids distribute to major organs: heart, lungs, kidneys, liver, spleen, and muscles, with some concentration in the brain (basal ganglia, amygdala, periaqueductal gray).
  • Highly lipophilic opioids (e.g. buprenorphine, fentanyl, methadone) are more likely to bind to proteins.
  • This results in longer half-lives due to slower release of the drugs from initial distribution sites.
  • Opioids cross the placental barrier and enter breast milk.

Elimination

  • Opioids are metabolized in the liver and intestines.
  • Metabolites are actively excreted by the kidneys and other fluids like urine, feces, and sweat.
  • Cytochrome P450 enzymes (primarily CYP3A4 and CYP2D6) play a crucial role in metabolism.
  • Phase 1 metabolism involves enzymatic modification of the opioid molecule.
  • Phase 2 metabolism involves conjugation with hydrophilic substances (e.g., glucuronic acid).
  • Some metabolites are inactive; others are more potent than the parent molecule.
  • Opioid metabolites are excreted in urine, feces, and other bodily fluids.

Neuropharmacology

  • Opioid receptors (μ, κ, δ, ORL1) are found throughout the brain and spinal cord.
  • Endogenous opioid peptides (endorphins, enkephalins, dynorphins, and nociceptin) interact with these receptors.
  • Opioid receptors are metabotropic and exert their effects via intracellular signaling pathways.
  • Activation influences mood, behavior, pain, stress, and reward.
  • Different opioid receptors have varying effects, with μ receptors playing a key role in analgesia and reward.

Opioid Agonists, Antagonists, and Mixed Agonist-Antagonists

  • Opioid agonists activate opioid receptors to produce effects.
  • Mixed agonist-antagonists exert both agonist and antagonist effects.
  • Some opioids are mixed agonists, meaning that they act as agonists on some receptors and as antagonists on others.
  • Opioid antagonists block opioid receptors, preventing agonist effects.

Studying That Suits You

Use AI to generate personalized quizzes and flashcards to suit your learning preferences.

Quiz Team

More Like This

Opioid Analgesics
7 questions

Opioid Analgesics

WellMadeNephrite4235 avatar
WellMadeNephrite4235
Use Quizgecko on...
Browser
Browser