Nervous System Drugs: Analgesics
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Questions and Answers

What is the primary concern when using mu agonists in pain management?

  • They may result in increased sedation without analgesia.
  • They can lead to respiratory depression. (correct)
  • They provide excellent pain control in all species.
  • They can cause hypertension.

Which opioid antagonist is most commonly used for reversing the effects of opioids?

  • Buprenorphine
  • Naloxone (correct)
  • Butorphanol
  • Fentanyl

What is the recommended starting approach for titrating Naloxone?

  • Only give Naloxone if the patient is in severe pain.
  • Dilute to 50mL and give 1mL every 10 minutes.
  • Draw up 0.04mg/kg and administer 10% at intervals until alert. (correct)
  • Administer a full dose immediately.

What is a significant disadvantage of using analgesics in dogs compared to cats?

<p>Dogs have less effective metabolism of certain analgesics. (D)</p> Signup and view all the answers

Which combination of medications should be avoided to prevent serotonin syndrome?

<p>Opioids and serotonin reuptake inhibitors. (D)</p> Signup and view all the answers

What is a significant characteristic of opioids in relation to pain management?

<p>They can be combined with other anesthetics to reduce required drug levels. (A)</p> Signup and view all the answers

Which opioid receptor is primarily associated with pain modulation?

<p>Mu-receptor (D)</p> Signup and view all the answers

What effect do opioids predominantly have on neurotransmitter release?

<p>Decrease the release of excitatory neurotransmitters. (C)</p> Signup and view all the answers

What is a key side effect associated with the use of opioid drugs?

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

Which of the following statements is true regarding hydromorphone?

<p>It is a pure Mu agonist that can be reversible. (A)</p> Signup and view all the answers

What condition can excessive use of morphine potentially lead to?

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

How do mixed opioids differ from full agonists?

<p>They can attach fully or partially to more than one opioid receptor. (B)</p> Signup and view all the answers

Which of the following is NOT a common side effect of opioid usage?

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

What is a characteristic of opioid full agonists?

<p>They have a maximum analgesic effect. (C)</p> Signup and view all the answers

What is the common use of opioids in relation to gastrointestinal function?

<p>They can cause constipation by decreasing GI secretions and movements. (C)</p> Signup and view all the answers

What is the primary function of CNS drugs?

<p>To alter nerve impulse transmission (D)</p> Signup and view all the answers

Which type of CNS drug binds to a receptor and produces a maximum response?

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

What is the role of nociceptors in the pain pathway?

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

Which of the following best describes a partial antagonist?

<p>A weaker drug that replaces a stronger drug at the receptor (D)</p> Signup and view all the answers

During which phase of the pain pathway does sensory electric stimulus convert into a pain signal?

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

What defines a competitive antagonist in the context of drug activity?

<p>It blocks the effect of a drug by binding to the same receptor (D)</p> Signup and view all the answers

Which statement about partial agonists is true?

<p>They cause a lesser effect than full agonists (B)</p> Signup and view all the answers

What impact do endogenous opioid endorphins have on the pain pathway?

<p>They dampen pain response (A)</p> Signup and view all the answers

What is a key advantage of Fentanyl in comparison to other opioids?

<p>Very limited vomiting (B)</p> Signup and view all the answers

What is a disadvantage of using Fentanyl?

<p>Higher risk of dysphoria (A)</p> Signup and view all the answers

What is the primary mechanism of action for Butorphanol?

<p>Mixed mu agonist and kappa agonist (B)</p> Signup and view all the answers

How long does it take for a Fentanyl transdermal patch to reach full effectiveness?

<p>12-24 hours (B)</p> Signup and view all the answers

What is the primary reason for caution when using Fentanyl patches?

<p>Potential for patch to be lost or ingested (D)</p> Signup and view all the answers

Which opioid is considered to have weaker analgesic properties compared to morphine?

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

Which aspect of Fentanyl's administration contributes to its lower likelihood of causing vomiting?

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

What is a primary effect of administering high doses of Fentanyl?

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

What is the method of delivery that allows for continuous analgesia when using Fentanyl?

<p>CRI (constant rate infusion) (A)</p> Signup and view all the answers

Which factor is NOT a consideration when applying a Fentanyl patch?

<p>Cutting the patch to fit (B)</p> Signup and view all the answers

What is a significant advantage of using partial agonists like buprenorphine in compromised patients?

<p>Less respiratory depressant effects (D)</p> Signup and view all the answers

Which of the following is a disadvantage of methadone?

<p>Can cause respiratory depression (A)</p> Signup and view all the answers

What primarily limits the effectiveness of the analgesic effect of buprenorphine at high doses?

<p>Partial agonism leading to a plateau (C)</p> Signup and view all the answers

Which property of tramadol contributes to its ability to reduce pain perception?

<p>Mu agonist effects and neurotransmitter reuptake prevention (D)</p> Signup and view all the answers

Why should buprenorphine not be given with pure Mu agonists?

<p>It can block Mu receptors and reduce effectiveness of the Mu agonist (C)</p> Signup and view all the answers

What effect does buprenorphine have on sedation in dogs compared to cats?

<p>More sedative effects in dogs (D)</p> Signup and view all the answers

Which of the following describes the primary mechanism of action of methadone?

<p>Mu agonist and NMDA receptor binding (C)</p> Signup and view all the answers

What duration of analgesia is typically expected for buprenorphine in cats?

<p>6-8 hours (C)</p> Signup and view all the answers

What is a noted pharmacological disadvantage of tramadol?

<p>Potential for abuse pronounced (D)</p> Signup and view all the answers

What primary clinical circumstance makes the use of partial agonist analgesics favorable?

<p>In patients with mild to moderate pain preferably (B)</p> Signup and view all the answers

Flashcards

CNS Drugs

Drugs that influence the nervous system, affecting communication between the spinal cord and brain.

Agonist

A drug that binds to a receptor and initiates a response, providing a full effect.

Antagonist

A drug that binds to a receptor but does not trigger a response, preventing other drugs from binding.

Mixed Agonist Antagonist

A drug that both activates and blocks the effects of a receptor, offering a partial response.

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Transduction

The process of converting painful stimuli into electrical signals.

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Transmission

The transmission of pain signals through the nervous system from the site of injury to the spinal cord and then to the brain.

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Modulation

The process where the body attempts to reduce the intensity of the pain signals.

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Perception

The awareness and perception of pain.

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Analgesic Drugs

A class of drugs that act on all parts of the pain pathway, providing pain relief, but also causing significant side effects like respiratory depression, sedation, and constipation.

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Opioids

A category of analgesic drugs that are highly effective for pain management, but are also controlled substances due to their potential for abuse and addiction.

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Narcosis

A term used to describe a state of drowsiness or unconsciousness.

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Mu Receptor

The opioid receptor primarily responsible for pain relief.

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Kappa Receptor

The opioid receptor involved in sedation, or the feeling of being calm and relaxed.

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Opioid Mechanism of Action

The process by which opioids reduce pain by decreasing the release of excitatory neurotransmitters, thus reducing the transmission of pain signals.

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Respiratory Depression

A side effect of opioid use that can lead to breathing difficulties and even death if not managed properly.

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Morphine

The "original" opioid, often used as a standard for comparison with other opioids. It boasts a long history of pain relief with broad applications.

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Hydromorphone

A potent opioid known for its strong pain-relieving properties, and often used for moderate to severe pain.

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Ileus

A condition caused by opioids, characterized by decreased intestinal motility leading to difficulty passing stools.

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Fentanyl (Duragesic, Fentadon)

Fentanyl is a potent opioid used for pain management in animals. It's a mu agonist, meaning it binds to mu opioid receptors to produce analgesia.

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Fentanyl Advantages

Fentanyl's primary advantage is its effectiveness in reducing pain without causing significant vomiting. It has minimal histamine release, making it a good choice for patients prone to allergies.

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Fentanyl Disadvantages

Although very effective, fentanyl has a relatively short duration of action (30 minutes to 2 hours). High doses can lead to dysphoria (a feeling of unease).

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Fentanyl Administration

Fentanyl can be administered intravenously, as a continuous rate infusion (CRI), or transdermally (patch). The patch provides a longer duration of action compared to the other routes.

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Meperidine (Demerol)

Meperidine (Demerol) is another opioid, but it's considered less common in veterinary medicine due to its weaker analgesic properties compared to morphine. It's also a stronger cardiac depressant, meaning it can negatively affect the heart.

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Butorphanol (Torbugesic)

Butorphanol (Torbugesic) is a mixed opioid, meaning it interacts with multiple opioid receptors (mu and kappa). It can act as a partial mu agonist (weakly activating the mu receptor) and a strong kappa agonist.

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Longer Duration of Action

Opioids, like fentanyl, often exhibit a longer duration of action compared to other pain medications. This allows for sustained pain relief without frequent doses.

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Fentanyl Transdermal Patches

Fentanyl patches are designed to provide a controlled release of the medication over a specific duration. The surface area of the animal dictates the size of the patch needed.

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Fentanyl Patch Application

Prior to applying a fentanyl patch, it's important to shave and clean the application site. Warming the patch and the animal's skin before application can enhance absorption.

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Fentanyl Patch Placement

The specific placement of the fentanyl patch is crucial for efficient absorption. Refer to the manufacturer's instructions for recommended locations and ensure the patch is covered for optimal effectiveness.

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Alpha 2 Agonists

These drugs block receptors that normally respond to acetylcholine and may stimulate alpha 2 receptors to produce sedation and analgesia. They offer some analgesic effect but are not a primary choice for pain management.

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Opioid-Induced Respiratory Depression

Opioids like morphine can suppress the respiratory system, leading to potential hypoventilation and even respiratory arrest, ultimately causing cardiac arrest. This is a serious concern, especially in cases of overdose or prolonged use.

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Naloxone (Narcan) Action

Naloxone (Narcan) is a medication that reverses the effects of opioids like morphine. It works by competing for receptor sites on the opioid receptors, effectively blocking the opioid from attaching and causing its effects.

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Alternatives to Full Opioids

When a patient needs pain relief but the side effects of a full opioid are undesirable, try Butorphanol or Buprenorphine. These drugs offer some pain relief while minimizing the risk of respiratory depression.

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Titration of Naloxone

Titration of Naloxone involves slowly administering increasing doses of the drug until the patient regains alertness, aiming to reduce sedation while preserving some pain relief. This is a precise method used to tailor the dose to the individual patient.

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Partial Agonist

A drug that binds to a receptor and activates it, but doesn't produce the full effect of a full agonist.

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Full Agonist

A drug that binds to a receptor and produces a full effect.

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Buprenorphine

A type of opioid that partially activates mu receptors, reducing pain but with a lower ceiling effect than full agonists.

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Partial Opioid Agonist

A type of opioid that can be used to partially reverse the effects of a full mu agonist.

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Methadone

This opioid is a mu agonist and also binds to NMDA receptors, helping control windup pain.

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Mixed Mu/Kappa Agonist

A type of opioid that binds to both mu and kappa receptors, offering a unique combination of analgesia and sedation.

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Tramadol

This opioid is known for its dual action: it's a mu agonist and also works by inhibiting serotonin and norepinephrine reuptake.

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Sedative Opioid

A type of opioid that offers pain relief but also causes sedation, which can be useful in some cases.

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Analgesia Plateau

The point at which increasing the dose of a drug no longer provides a greater effect.

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Study Notes

Nervous System Drugs: Analgesics

  • CNS drugs alter nerve impulse transmission between the spinal cord and brain. These drugs can be stimulatory or depressive.
  • Agonists have good receptor affinity and produce maximum response. They attach to the receptor to trigger a response.
  • Antagonists have good receptor affinity but block response, lacking intrinsic activity, inhibiting the drug's response. They attach to the receptor, preventing the agonist from binding.
  • Mixed agonist-antagonists can bind to and activate opioid receptors while also blocking other opioid effects.
  • Partial agonists exert only a partial effect, while partial antagonists replace stronger drugs, producing reduced effects at the receptor. The resulting effect is similar to the stronger drug but weaker.
  • Competitive antagonists block the actions of other drugs by attaching to the same receptors, preventing the other drug from binding.

Pain Pathway

  • Transduction: Painful stimuli (chemical, thermal, mechanical) are converted into electrical signals.
  • Transmission: Electrical signals travel from peripheral nerves to the spinal cord and CNS.
  • Modulation: The CNS dampens pain signals using the sympathetic nervous system.
  • Perception: Conscious awareness of pain. Nociceptors, (free nerve endings) transmit signals to the spinal cord, then to the thalamus, reticular formation, limbic system and the cerebral cortex, ultimately resulting in the perception of the pain.
  • Pain signals travel through peripheral nerves to the dorsal horn of the spinal cord, and then to the brain. This includes the thalamus, reticular formation, limbic system, and the cerebral cortex.

Analgesic Drugs (Opioids)

  • Act on all parts of the pain pathway. Highly controlled due to their addictive potential.
  • Used in pain management, especially during surgery and to minimize the amount of anesthetic needed.
  • Used initially to treat diarrhea. Reduce ileus (prevent constipation). Used for suppressing coughs.
  • Opioids have Mu and Kappa receptors, found throughout the pain pathway.
  • They decrease the release of excitatory neurotransmitters, influencing postsynaptic sites.
  • These receptors have sub-receptors; not all animal species react to opioids in the same way.

Effects of Opioids

  • Respiratory depression (decreased respiratory rate and volume, leading to increased carbon dioxide levels and decreased oxygen levels).
  • Possible respiratory and cardiac arrest in overdose cases.
  • Sedation.
  • Nausea, vomiting, hypersalivation.
  • Reduced gastrointestinal secretions, and decreased movement.
  • Euphoria (positive effects) or dysphoria (negative effects).
  • Pupil constriction or dilation.
  • Slowing of the heart rate (Bradycardia).
  • Histamine release (hives, redness; mostly with Morphine).

Opioid Receptors

  • Mu (pain): Primary target for analgesics, causes reduced GI motility.
  • Kappa (sedation): Causes sedation, analgesia, and reduced respiratory depression compared to Mu agonists.

Analgesic Drug Classifications

  • Full agonists produce maximal response.
  • Partial agonists produce less effective responses than full agonists.
  • Full antagonists block agonist effects and prevent binding.

Opioid Antagonists (Reversal)

  • Naloxone (Narcan): works by competing with opioid receptors, reversing their effects.
  • Used for opioid overdoses to reverse respiratory depression, sedation, and other negative effects. Start low and titrate upwards as needed in overdose cases. Bolus dosages are often used in emergencies.

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Pharmacology 2 - Lecture 2: Nervous System Drugs PDF

Description

Explore the different classifications and mechanisms of nervous system drugs, particularly analgesics. This quiz covers agonists, antagonists, mixed agonist-antagonists, and the pain pathway of transduction. Test your knowledge on how these medications influence pain management.

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