Opioid Pharmacology Quiz
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Questions and Answers

What is one of the main actions of opioid agonists on μ (MOP) receptors?

  • Enhances glutamate transmission
  • Increases serotonin release
  • Inhibits the activity of adenylyl cyclase (correct)
  • Promotes calcium ion influx

Which event occurs as a result of K+ channel opening in postsynaptic neurons?

  • Hyperpolarization of the neuron (correct)
  • Inhibition of G protein activation
  • Enhanced neurotransmitter release
  • Increased positive charge inside the neuron

What is the effect of opioids on neurotransmitter release in relation to glutamate?

  • Increases glutamate release from presynaptic neurons
  • Has no effect on glutamate release
  • Reduces glutamate release from presynaptic neurons (correct)
  • Stimulates excessive glutamate release

Which endogenous substances act on opioid receptors within the body?

<p>Enkephalins, Endorphins, Dynorphins (D)</p> Signup and view all the answers

Which pharmacological effect of opioids is characterized by a strong feeling of well-being?

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

Which category of opium includes heroin and oxycodone?

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

What is the prototype mixed agonist-antagonist in opioid pharmacology?

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

Which opioid receptor is primarily associated with the action of analgesia and positive reinforcement?

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

Which opioid receptor is known for its involvement in respiratory depression and cardiovascular effects?

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

What effect does naloxone have when administered to an opioid-dependent individual?

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

What is a primary mechanism through which opioids produce euphoric effects?

<p>Activation of mu receptors leading to increased dopamine release (C)</p> Signup and view all the answers

Which of the following accurately describes the effects of opioids on respiration?

<p>Depression of respiration due to brainstem effects (A)</p> Signup and view all the answers

What secondary effect is characteristic of opioid ingestion?

<p>Pupillary constriction (miosis) (C)</p> Signup and view all the answers

What is a common consequence of chronic opioid treatment on the gastrointestinal system?

<p>Constipation due to decreased motility (C)</p> Signup and view all the answers

How do opioids influence hormonal balance in men and women?

<p>Reduce libido and cause menstrual irregularities (C)</p> Signup and view all the answers

What is the main characteristic of acute pain?

<p>It serves as a useful warning system. (B)</p> Signup and view all the answers

Which type of pain is associated with increased sensitivity to painful stimuli?

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

What is a common side effect associated with the use of naltrexone?

<p>Flu-like symptoms (D)</p> Signup and view all the answers

Where are the cell bodies of primary afferent nociceptive sensory neurons located?

<p>In the dorsal root ganglia (B)</p> Signup and view all the answers

Which class of medications can reduce firing of primary afferent neurons at the injury site?

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

What is the primary use of naloxone in medical settings?

<p>Reversing respiratory depression in overdoses (A)</p> Signup and view all the answers

Which statement accurately describes naltrexone?

<p>It is a pure opioid antagonist approved for treating heroin dependence. (A)</p> Signup and view all the answers

Which neurological activity is involved in pain signaling between the brain and the spinal cord?

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

How is naloxone primarily administered?

<p>Not effective via gastrointestinal absorption (D)</p> Signup and view all the answers

What kind of pain is caused by noxious stimuli and does not involve conscious awareness?

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

What is one role of antidepressants in pain management?

<p>They activate descending pathways to inhibit pain signals. (A)</p> Signup and view all the answers

What results from physical dependence on opioids?

<p>Altered physiological state with biological reactions opposite to pharmacological effects (B)</p> Signup and view all the answers

What is the estimated single daily oral dose of naltrexone for treating heroin dependence?

<p>40 to 100 mg (B)</p> Signup and view all the answers

Which of the following is true regarding morphine?

<p>It crosses the blood-brain barrier fairly slowly (C)</p> Signup and view all the answers

What type of pain lasts for more than three months?

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

How is codeine primarily metabolized in the body?

<p>By the enzyme CYP-2D6 to morphine (A)</p> Signup and view all the answers

What can occur due to maternal opioid use during pregnancy?

<p>Withdrawal symptoms in infants at birth (D)</p> Signup and view all the answers

What distinguishes heroin from morphine?

<p>Heroin is three times more potent than morphine (B)</p> Signup and view all the answers

What is a primary characteristic of Fentanyl as an opioid?

<p>It can be administered through various routes. (A)</p> Signup and view all the answers

Which opioid is known for having a ceiling effect limiting its analgesic effectiveness?

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

What distinguishes Meperidine from Morphine in terms of side effects?

<p>Meperidine can cause convulsions and delirium. (D)</p> Signup and view all the answers

What is one of the uses of Methadone?

<p>Maintenance treatment for opioid addiction. (C)</p> Signup and view all the answers

What is the potent potency comparison of Propoxyphene?

<p>More potent than codeine, less potent than morphine. (D)</p> Signup and view all the answers

Which of the following actions does Tramadol achieve?

<p>Blocks presynaptic reuptake of norepinephrine. (B)</p> Signup and view all the answers

Why is Morphine associated with a high risk when smoked with crack cocaine?

<p>It leads to intense euphoria and significant mental health risks. (D)</p> Signup and view all the answers

In opioid rehabilitation, what is a significant advantage of using Buprenorphine?

<p>It reduces needle-associated diseases and illicit drug use. (B)</p> Signup and view all the answers

Flashcards

Opioid Agonist

A drug that binds to and activates opioid receptors, producing effects like analgesia and euphoria.

Opioid Antagonist

A drug that binds to opioid receptors but does not activate them, blocking the effects of opioids.

$\mu$ Receptor

The primary opioid receptor responsible for analgesia, respiratory depression, and addiction.

Partial Agonist

A drug that binds to and activates opioid receptors, but produces a weaker effect than a full agonist.

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Mixed Agonist/Antagonist

A drug that acts as an agonist at one receptor subtype and an antagonist at another.

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Pain: Definition

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

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Acute Pain

Short-lasting pain that typically resolves as the body heals.

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Chronic Pain

Pain lasting more than 3 months.

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Nociceptive Pain

Caused by noxious stimuli to nociceptors, like heat, physical damage, or chemical injury.

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Neuropathic Pain

Caused by damage to the nervous system, often leading to increased sensitivity to pain.

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Pain Signaling: Sensory Neurons

Primary afferent nociceptive sensory neurons detect noxious stimuli and transmit the pain signal to the spinal cord.

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Pain Signaling: Pathways

The pain signal travels through the spinal cord, brainstem, and midbrain before reaching the cortex in the forebrain, resulting in the perception of pain.

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Descending Pathways: Pain Inhibition

Brain structures send descending fibers back down to the spinal cord, inhibiting pain signals.

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Opioid Agonist Action

When an opioid agonist binds to a μ (MOP) receptor, it triggers a cascade of events.

  1. Activates a G protein.
  2. The G protein's α subunit detaches, inhibiting the enzyme adenyl cyclase.
  3. The G protein's βγ subunits detach.
  4. Potassium (K+) channels open, leading to an outflow of potassium.
  5. Calcium (Ca2+) channels are blocked.
  6. The postsynaptic neuron hyperpolarizes (becomes more negative), making it less likely to fire.
  7. Neurotransmitter release is reduced, resulting in decreased pain transmission.
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Opioid Hyperpolarization

Opioid agonists cause hyperpolarization of the postsynaptic neuron by opening potassium (K+) channels, leading to an outflow of positive ions, making the inside of the neuron more negative.

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Opioid Presynaptic Effect

Opioid agonists reduce the release of neurotransmitters like glutamate and substance P from the presynaptic neuron, reducing the signaling of pain.

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Endogenous Opioids

These are naturally occurring substances in the body that bind to opioid receptors and produce similar effects to opium. Examples include enkephalins, endorphins, and dynorphins.

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Opioid Reward Pathway

Opioids act on the reward pathway. This effect is mediated by the release of dopamine in the nucleus accumbens, creating a feeling of euphoria and pleasure.

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Opioid Euphoria

Activation of mu receptors in the mesolimbic system leads to dopamine release in the nucleus accumbens, producing a feeling of euphoria.

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Opioid Overdose Risk

Opioids depress the respiratory center in the brainstem, reducing sensitivity to carbon dioxide. This can cause respiratory failure and death.

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Opioid-Induced Constipation

Opioids slow down the digestive process, reducing intestinal motility and causing constipation.

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Opioid Tolerance

Repeated use of opioids leads to receptor desensitization, causing a need for higher doses to achieve the same effects.

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Pupillary Constriction (Miosis)

Opioids cause pupillary constriction. This is a common sign of opioid ingestion.

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Opioid Cross-Tolerance

Tolerance to one opioid leads to tolerance to all other opioids, both natural and synthetic.

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Opioid Dependence Withdrawal Symptoms

These symptoms occur after stopping opioid use and are the opposite of the drug's effects. They can vary in severity depending on the dose, frequency of use, and duration of dependence.

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Morphine Administration Routes

Morphine can be given as an injection, inhaled, taken orally, rectally, or even directly into the spinal cord.

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Codeine Effects

Codeine's pain relief and euphoria are actually caused by its conversion to morphine in the body.

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Heroin Potency

Heroin is three times more potent than morphine.

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Naloxone

A pure opioid antagonist that blocks the effects of opioids, often used to reverse opioid overdose. It does not have analgesic effects and is not subject to addiction.

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Naltrexone

A long-acting, orally administered pure opioid antagonist used for treating heroin dependence. It blocks opioid receptors preventing effects like euphoria and preventing cravings.

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Naltrexone: Side Effects

Common side effects include flu-like symptoms, headache, sweating, sleep problems, nausea, and mood swings. These are often transient and can be managed.

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Naloxone: Duration of Action

Naloxone's effect typically lasts for 15 to 30 minutes. It is more effective in emergency situations to reverse overdose than for long-term addiction treatment.

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Naltrexone: Long-term Treatment

Naltrexone's effectiveness for chronic therapy depends on the individual's commitment to abstinence, and cannot be used concurrently with opioid agonists.

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Morphine's Advantage

Morphine's slightly altered chemical structure makes it more lipid-soluble, enabling it to pass through the blood-brain barrier faster.

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Propoxyphene vs. Codeine

Propoxyphene, similar to methadone, is less potent than codeine but more potent than aspirin, posing a risk of fatal heart problems and overdose.

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Meperidine's Difference

Though a synthetic opioid, meperidine differs structurally from morphine, leading to more excitatory side effects like tremors and seizures instead of the usual sedative effects.

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Fentanyl's Delivery Methods

Fentanyl, a short-acting opioid, can be administered through various routes: intravenous injection, skin patches, mouth, gum, or lollipop.

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Tramadol's Unique Action

Tramadol is a unique analgesic that acts as a partial agonist at mu receptors, inhibits norepinephrine reuptake, and releases serotonin, offering a multifaceted pain-relieving approach.

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Methadone's Dual Role

Methadone, a synthetic mu agonist, suppresses withdrawal symptoms and acts as a long-acting analgesic for chronic pain, offering relief and stability.

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Buprenorphine's Ceiling Effect

Buprenorphine, a partial mu opioid agonist, has a limited analgesic effect due to its ceiling effect, but it produces long-lasting respiratory depression and euphoria.

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Buprenorphine's Binding Power

Buprenorphine binds strongly to mu receptors, making it useful in treating opioid addiction, even when taken orally or through a patch.

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