Central Nervous System Drug pt 3

What are agonist-antagonist opioids?

Agonist-antagonist opioids are a class of medications that act as agonists at certain opioid receptors and antagonists at others.

What is the prototype agonist-antagonist opioid?

Pentazocine (Talwin)

What is the indication for Pentazocine?

It is indicated for mild to moderate pain.

How does Pentazocine compare to morphine in terms of effectiveness?

Pentazocine is less effective than morphine.

What receptors does Pentazocine act on?

It acts as an agonist at kappa receptors and an antagonist at mu receptors.

What effects does Pentazocine produce?

It produces analgesia, sedation, and respiratory depression, but not as severe as morphine.

What can happen if Pentazocine is given to a patient dependent on pure opioid agonists?

It can precipitate withdrawal.

What is the trade name for Nalbuphine?

Look up the trade name.

What are the pharmacologic actions of Nalbuphine compared to Pentazocine?

Nalbuphine has similar pharmacologic actions to Pentazocine.

What is a key characteristic of Nalbuphine's analgesic effect?

It has a ceiling to analgesia, with maximal pain relief much lower than morphine.

How can Nalbuphine be administered?

It may be given IV, IM, or SubQ.

What is a key characteristic of Butorphanol?

It has actions similar to Pentazocine but provides less analgesia than morphine.

What should Butorphanol not be given to?

Patients with myocardial infarction.

How can Butorphanol be administered?

It can be given IM, IV, or by nasal spray.

What are the trade names for Buprenorphine?

Buprenex, Butrans, Belbuca, Suboxone.

What are the analgesic effects of Buprenorphine compared to morphine?

Its analgesic effects are similar to morphine, but significant tolerance has not been observed.

What additional use does Buprenorphine have besides analgesia?

It is used to treat opioid addiction.

What cardiac risk is associated with Buprenorphine?

It can prolong the QT interval, potentially leading to lethal arrhythmias.

How can Buprenorphine be administered?

It can be given transdermal, as a solution for injection, sublingual, buccal strips, intradermal implant, or sublingual film.

What are the indications for the different forms of Buprenorphine?

The patch and solution are used for pain; sublingual is approved only for opioid addiction.

What is essential for pain management?

Pain assessment

What pain scale is used for children aged 4-8?

Wong-Baker scale

What assessment tool is used for children younger than 4?

FLACC scale

How should opioid dosages be determined?

Must be adjusted to accommodate individual variation

What is the recommended dosing schedule for opioids in the first 24 hours after surgery?

Administered on a fixed schedule rather than PRN

What may develop when opioids are given in high doses for 20 days or more?

Dependence

What should be done to avoid withdrawal when tapering off opioids?

Doses should be tapered down

What is physical dependence?

An abstinence syndrome will occur if the dependence-producing drug is abruptly withdrawn.

What is drug abuse?

Drug use that is inconsistent with medical or social norms.

What is addiction?

A primary, chronic disease characterized by an individual pathologically pursuing rewards and/or relief by substance use and behaviors. Physical dependence is not required for addiction.

Is significant physical dependence common when opioids are used short term for pain relief?

No, it is extremely rare.

Do patients who develop physical dependence on opioids typically continue use after pain subsides?

No, they rarely develop addictive behavior and continue opioid administration after their pain has subsided.

Is there justification for withholding opioids from patients in pain due to concerns about physical dependence?

No, there is no justification for withholding opioids from patients in pain on this basis.

Is the development of addiction to opioids from clinical exposure common?

No, it is extremely rare.

If addiction occurs during a hospital stay, what might it reflect?

It is probable that these behaviors reflect tendencies that existed before the patient entered the hospital.

What is PCA in medical terms?

PCA stands for Patient-Controlled Analgesia.

What is the primary purpose of PCA?

PCA is primarily for relief of patients experiencing post-operative pain.

What type of drugs does PCA allow patients to self-administer?

PCA permits the self-administration of parenteral opioids.

What is a PCA device?

A PCA device is an electronically controlled infusion pump that can be activated by the patient to deliver a preset bolus dose of an opioid.

What is the effect of opioids on postoperative pain?

Opioids provide increased comfort through reduction of pain but can cause constipation, urinary retention, and suppression of reflex cough.

What are the effects of opioids on obstetric analgesia?

Opioids such as morphine or meperidine may depress fetal respiration and uterine contractions when administered parenterally.

What is the opioid of choice for myocardial infarction?

Morphine is the opioid of choice for myocardial infarction.

How do opioids affect blood pressure during a myocardial infarction?

Morphine lowers blood pressure and can decrease cardiac work.

What caution should be taken when using opioids in patients with head injury?

Opioids must be employed with caution as they can cause respiratory depression accompanied by elevation of intracranial pressure (ICP).

What is the objective when treating cancer-related pain with opioids?

The objective is to maximize comfort and give as much medication as needed to relieve pain.

When should opioids be used for chronic noncancer pain?

Opioids should be used only after nonopioid analgesics or more conservative methods have failed.

What is the goal of using opioids for chronic noncancer pain?

The goal is to reduce discomfort, improve mood, and enhance function, allowing patients to complete their activities of daily living (ADLs).

What are opioid antagonists?

Opioid antagonists are drugs that block the effects of opioid agonists.

What are the therapeutic uses of opioid antagonists?

They are used for treatment of opioid overdose, relief of opioid-induced constipation, reversal of postoperative opioid effects, and management of opioid addiction.

Name four pure opioid antagonists.

Naloxone (Narcan), methylnaltrexone (Relistor), naloxegol (Movantik), alvimopan (Entereg), naltrexone (ReVia, Vivitrol).

What is naloxone (Narcan)?

Naloxone (Narcan) is a structural analog of morphine that acts as a competitive antagonist at opioid receptors.

What effects does naloxone reverse?

Naloxone reverses effects of opioid agonists, including respiratory depression, coma, and analgesia.

What are the pharmacologic effects of naloxone when no opioids are present?

Naloxone has no significant effects when administered in the absence of an opioid.

How can naloxone be administered?

Naloxone can be administered IV, IM, or SubQ.

What is the half-life of naloxone?

The half-life of naloxone is approximately 2 hours.

What is methylnaltrexone used for?

Methylnaltrexone is a selective mu opioid antagonist indicated for opioid-induced constipation.

Does methylnaltrexone block opioid receptors?

No, methylnaltrexone does not block opioid receptors.

What is alvimopan used for?

Alvimopan is a selective, peripherally acting mu opioid antagonist developed to counteract the adverse effects of opioids on bowel function.

What is Naltrexone?

A pure opioid antagonist used for opioid and alcohol abuse.

What is the goal of using Naltrexone?

To prevent euphoria if the abuser should take an opioid.

How does Naltrexone affect opioid users?

It takes away the high from the drug.

What is Tramadol and its brand names?

Tramadol is a moderately strong analgesic with brand names Ultram, UltramER, Ryzolt, and Rybix.

What is the potential for dependence and abuse of Tramadol?

Tramadol has a low potential for dependence, abuse, or respiratory depression.

How does Tramadol relieve pain?

Tramadol relieves pain through a combination of opioid and nonopioid mechanisms.

What is Clonidine and its brand names?

Clonidine is a medication with brand names Catapres and Duraclon.

What are the approved applications of Clonidine?

Clonidine is approved for the treatment of hypertension and relief of severe pain.

How is Clonidine administered for pain relief?

Clonidine is given by continuous epidural infusion for pain relief.

What effect does Clonidine have on blood pressure?

Clonidine is given to bring blood pressure down immediately.

What is Ziconotide?

A centrally acting analgesic with a novel structure and mechanism.

How is Ziconotide administered?

Given intrathecal (IT).

Who is Ziconotide prescribed for?

Only given to patients where intrathecal therapy is warranted.

What type of molecule is Ziconotide?

A small synthetic peptide.

Where is Ziconotide injected when administered?

Injected into the back.

What is Dexmedetomidine also known as?

Precedex

What type of drug is Dexmedetomidine?

A selective alpha-adrenergic agonist

What effects does Dexmedetomidine cause?

Sedation and analgesia

What are the indications for using Dexmedetomidine?

Short term sedation in critically ill patients who are intubated and sedation for nonintubated patients before, during surgical or other procedures

What category of analgesics does Dexmedetomidine belong to?

Nonopioid centrally acting analgesics

What is the purpose of the therapeutic goal in nursing implications for pain management?

Relief or prevention of moderate to severe pain while causing minimal respiratory depression, constipation, urinary retention, and other adverse effects.

What should be included in a pre-administration assessment for pain management?

Baseline data and pain assessment, including location, time of onset, quality of pain, and any psychological factors.

What vital signs (VS) should be monitored in nursing implications for pain management?

Vital signs should be monitored as part of the assessment.

Who are considered high-risk patients for opioid administration?

All opioids are contraindicated for preemies, and morphine is not for patients following biliary tract surgery, while meperidine is contraindicated for patients on MAOIs.

What are some examples of Agonist-Antagonist Opioids?

Buprenorphine, Butorphanol, Nalbuphine, Pentazocine

What is the goal of using Agonist-Antagonist Opioids?

Relief of moderate to severe pain.

How does the maximal relief of Agonist-Antagonist Opioids compare to pure opioid agonists?

Maximal relief is generally lower than pure opioid agonists.

What can Agonist-Antagonist Opioids precipitate in patients physically dependent on opioid agonists?

An abstinence syndrome.

What is the therapeutic goal of Naloxone (Narcan)?

Reversal of opioid effects, opioid-induced neonatal respiratory depression, and overdose with pure opioid agonists.

What are the routes of administration for Naloxone (Narcan)?

IV, IM, and SubQ.

What should be done when administering Naloxone (Narcan)?

Titrate carefully; it can precipitate withdrawal.

What are the routes of administration for opioids?

IV, oral, transdermal, and others.

What is the recommended dosage consideration for patients with cancer?

Dosage may need to be adjusted based on individual patient needs.

How should IV injections of opioids be administered?

Slowly, over 4 to 5 minutes.

When should therapeutic effects of opioids be evaluated?

1 hour after opioid administration.

What should be done if analgesia is insufficient after opioid administration?

Notify the provider.

What are some adverse effects to monitor for in opioid administration?

Respiratory depression, sedation, orthostatic hypotension, constipation, urinary retention, biliary colic, emesis, cough suppression, miosis, neurotoxicity.