CH7 Opioids PP

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Which of the following is true about opioids?

Opioids have a chemical structure composed of three rings of phenanthrene.

What distinguishes synthetic opioids from natural opioids?

Synthetic opioids have a different chemical structure than natural opioids.

What are the major pharmacodynamic differences between different opioids?

All of the above.

Which of the following is true about the chemical structure of opium alkaloids?

Opium alkaloids consist of three rings of phenanthrene composed of 14 carbon atoms. Signup and view all the answers

Which of the following is true about synthetic opioids?

Synthetic opioids are manufactured by synthesis rather than chemical modification of morphine. Signup and view all the answers

Which of the following is true about opioids?

Opioids produce analgesia without loss of touch, proprioception, or consciousness. Signup and view all the answers

Which of the following locations primarily contain opioid receptors in the brain?

Locus ceruleus Signup and view all the answers

Where are opioid receptors found in the spinal cord?

Dorsal horn Signup and view all the answers

Outside of the central nervous system, where can opioid receptors be found?

Sensory neurons and immune cells Signup and view all the answers

Which of the following is true about opioid receptors in the brain?

Opioid receptors are primarily found in the periaqueductal gray. Signup and view all the answers

Where are opioid receptors found in the spinal cord?

Opioid receptors are found in interneurons in the dorsal horn. Signup and view all the answers

Where can opioid receptors be found outside of the central nervous system?

Opioid receptors can be found in immune cells. Signup and view all the answers

Which of the following is the most likely effect on the cardiovascular system in a supine normovolemic patient?

Orthostatic hypotension Signup and view all the answers

What can cause a decrease in venous return and cardiac output in the cardiovascular system?

Histamine release Signup and view all the answers

What can increase activity over vagal nerves and directly affect the cardiovascular system?

Drug-induced bradycardia Signup and view all the answers

Which of the following is a possible effect of opioid administration on the cardiovascular system?

Activation of sympathetic compensatory mechanisms Signup and view all the answers

What is a characteristic of orthostatic hypotension observed with opioid administration?

Increased venous pooling Signup and view all the answers

Which of the following can contribute to a decrease in blood pressure following opioid administration?

Drug-induced bradycardia Signup and view all the answers

Which of the following is true about the effect of opioids on the cardiovascular system?

Opioids protect the myocardium from ischemia. Signup and view all the answers

What is a characteristic of opioid-induced depression?

Interference with pontine and medullary ventilatory centers. Signup and view all the answers

What factors can aggravate opioid-induced depression?

All of the above. Signup and view all the answers

Which opioid is known to have a greater effect on cough suppression due to its bulky substitution on carbon #3?

Codeine Signup and view all the answers

Which opioid is associated with the prominent side effect of skeletal muscle rigidity and/or myoclonus, particularly in thoracic and abdominal muscles?

Fentanyl Signup and view all the answers

Which opioid-induced effect on the autonomic nervous system can be antagonized by atropine?

Miosis Signup and view all the answers

Which of the following can relieve the pain of sphincter of Oddi spasm caused by opioids?

Glucagon Signup and view all the answers

Which of the following gastrointestinal symptoms can be caused by opioids?

Constipation Signup and view all the answers

What can opioid-induced spasm of GI tract smooth muscle enhance the tone of?

All of the above Signup and view all the answers

Which medication can relieve both sphincter of Oddi spasm and angina pectoris pain caused by opioids?

Nitroglycerin Signup and view all the answers

What is a possible gastrointestinal symptom that can be caused by opioids?

Vomiting Signup and view all the answers

Which medication can reverse opioid-induced spasm of biliary smooth muscle?

Glucagon Signup and view all the answers

Which of the following is a possible effect of opioids on the genitourinary system?

Increase the tone and peristaltic activity of the ureter Signup and view all the answers

Which of the following can contribute to nausea and vomiting following opioid administration?

Direct stimulation of the chemoreceptor trigger zone in the floor of the fourth ventricle Signup and view all the answers

Which of the following is true about the placental transfer of opioids?

Opioids are readily transported across the placenta Signup and view all the answers

Which of the following is true about the side effects of opioids?

Opioids can cause miosis, hypoventilation, and coma in overdose. Signup and view all the answers

Which of the following is true about pharmacodynamic tolerance and physical dependence with opioids?

Tolerance can occur without physical dependence. Signup and view all the answers

Which of the following can lead to exaggerated ventilatory depressant effects of opioids?

All of the above Signup and view all the answers

Which of the following is a common side effect of morphine administration?

Decreased ability to concentrate Signup and view all the answers

What is the peak effect of morphine and how long does it typically last?

Peak effect at 15 to 30 minutes, duration of about 4 hours Signup and view all the answers

Which of the following factors contribute to poor penetration of morphine into the central nervous system?

High degree of ionization and rapid conjugation with glucuronic acid Signup and view all the answers

Which of the following is true about the pharmacokinetics of morphine in the cerebrospinal fluid (CSF)?

CSF concentrations of morphine decay more slowly than plasma concentrations Signup and view all the answers

Which of the following organs does morphine rapidly accumulate in?

Kidneys, liver, and skeletal muscle Signup and view all the answers

Which of the following is a difference between morphine and Fentanyl in terms of first-pass uptake into the lungs?

Morphine does not undergo significant first-pass uptake into the lungs, unlike Fentanyl Signup and view all the answers

Which of the following is true about the elimination half-life of morphine in the neonate during the first 4 days of life?

The elimination half-life is decreased Signup and view all the answers

What is the primary elimination route for normeperidine, the metabolite of meperidine?

Renal excretion Signup and view all the answers

What is the elimination half-life of normeperidine in patients with renal failure?

35 hours Signup and view all the answers

Which of the following statements about fentanyl is true?

Fentanyl has a longer elimination half-time than morphine Signup and view all the answers

What is the main advantage of using large doses of fentanyl as the sole anesthetic?

Suppression of stress responses to surgery Signup and view all the answers

What is a potential postoperative problem associated with fentanyl?

Persistent or recurrent depression of ventilation Signup and view all the answers

Which of the following is true about the effects of fentanyl on the cardiovascular system?

Fentanyl causes bradycardia less frequently than morphine Signup and view all the answers

Which of the following is true about the elimination half-life of morphine in the neonate during the first 4 days of life?

The elimination half-life of morphine is decreased in the neonate during the first 4 days of life. Signup and view all the answers

Which of the following is true about normeperidine?

Normeperidine is half as active as meperidine and acts as a CNS stimulant. Signup and view all the answers

Which of the following is true about meperidine?

Meperidine has an elimination half-life of 3-5 hours. Signup and view all the answers

Which of the following is true about the metabolism of fentanyl?

Fentanyl is metabolized to norfentanyl and hydroxyproprionyl-fentanyl. Signup and view all the answers

Which of the following is true about the clinical use of fentanyl?

Fentanyl is administered intrathecally for surgery. Signup and view all the answers

Which of the following is true about the side effects of fentanyl?

Fentanyl can cause mydriasis and dry mouth. Signup and view all the answers

Which of the following is true about the cardiovascular effects of fentanyl?

Fentanyl may occasionally decrease blood pressure and cardiac output. Signup and view all the answers

Which opioid has a greater protein binding compared to fentanyl?

Sufentanil Signup and view all the answers

Which opioid has a faster onset compared to fentanyl and sufentanil?

Alfentanil Signup and view all the answers

Which opioid causes a decrease in cerebral metabolic oxygen requirements and may decrease cerebral blood flow?

Morphine Signup and view all the answers

Which of the following is NOT true about the pharmacokinetics of alfentanil?

Renal failure alters the clearance of alfentanil. Signup and view all the answers

Which of the following is a characteristic of alfentanil's effect-site equilibration?

It allows for faster crossing of the blood-brain barrier. Signup and view all the answers

What is the primary elimination route for alfentanil?

Metabolism by piperidine N-dealkylation Signup and view all the answers

What is the context-sensitive half-time of alfentanil compared to sufentanil for infusions up to 8 hours in duration?

It is longer Signup and view all the answers

Which opioid has a faster onset of action compared to fentanyl and sufentanil?

Alfentanil Signup and view all the answers

Which opioid has a greater protein binding compared to fentanyl?

Sufentanil Signup and view all the answers

Which opioid has an elimination half-time intermediate between fentanyl and alfentanil?

Sufentanil Signup and view all the answers

Which of the following is true about the pharmacokinetics of alfentanil compared to fentanyl and sufentanil?

Alfentanil has a shorter elimination half-time than fentanyl and sufentanil. Signup and view all the answers

Which of the following is true about the effect of cirrhosis of the liver on the elimination half-time of alfentanil?

Cirrhosis of the liver prolongs the elimination half-time of alfentanil. Signup and view all the answers

Which of the following is true about the effect of renal failure on the clearance and elimination half-time of alfentanil?

Renal failure has no effect on the clearance and elimination half-time of alfentanil. Signup and view all the answers

Which of the following is true about the effect-site equilibration characteristic of alfentanil?

The effect-site equilibration of alfentanil is a result of its low pKa. Signup and view all the answers

Which of the following opioids has the shortest context-sensitive half-time?

Remifentanil Signup and view all the answers

Which of the following opioids is not recommended for spinal or epidural administration?

Remifentanil Signup and view all the answers

Which of the following opioids is associated with the potential side effect of hyperalgesia?

Remifentanil Signup and view all the answers

Which of the following is a characteristic of remifentanil's metabolism?

Metabolized by nonspecific plasma and tissue esterases Signup and view all the answers

What is a unique characteristic of remifentanil's pharmacokinetics?

Rapid effect-site equilibration Signup and view all the answers

Which of the following is true about dosing regimens for remifentanil?

Based on ideal (lean) body mass Signup and view all the answers

Which of the following opioids has a context-sensitive half-time that is independent of the duration of infusion?

Remifentanil Signup and view all the answers

Which of the following opioids is not recommended for spinal or epidural administration?

Remifentanil Signup and view all the answers

Which of the following opioids is associated with the possibility of acute opioid tolerance and hyperalgesia when infused intraoperatively?

Remifentanil Signup and view all the answers

Which of the following is a characteristic of remifentanil's metabolism?

Remifentanil's metabolism is characterized by ester hydrolysis by nonspecific plasma and tissue esterases. Signup and view all the answers

Which of the following is true about remifentanil's pharmacokinetics?

Remifentanil's pharmacokinetics is highly variable between individuals. Signup and view all the answers

What is a unique pathway of metabolism for remifentanil?

Hydrolysis by specific plasma and tissue esterases Signup and view all the answers

Study Notes

Opioids Overview

Opioids can be classified into natural opioids, semisynthetic opioids, and synthetic opioids.
Synthetic opioids are chemically synthesized and have a different chemical structure compared to natural opioids.

Pharmacodynamic Differences

Different opioids have varying pharmacodynamic effects due to differences in their chemical structures and receptor binding affinities.

Chemical Structure of Opium Alkaloids

Opium alkaloids have a specific chemical structure that distinguishes them from synthetic opioids.

Opioid Receptors

Opioid receptors are primarily found in the brain, spinal cord, and peripheral tissues.
Opioid receptors in the brain are localized to specific areas, including the cerebral cortex, thalamus, and brainstem.
In the spinal cord, opioid receptors are found in the dorsal horn and dorsal root ganglia.
Outside the central nervous system, opioid receptors are found in peripheral tissues, including the gastrointestinal tract, heart, and lungs.

Cardiovascular System

Opioids can affect the cardiovascular system, causing changes in blood pressure, heart rate, and cardiac output.
Opioids can cause a decrease in venous return and cardiac output.
Opioids can increase activity over vagal nerves, directly affecting the cardiovascular system.
Orthostatic hypotension can occur due to opioid administration.

Respiratory System

Opioids can cause respiratory depression, which can be life-threatening.

Gastrointestinal System

Opioids can cause nausea, vomiting, and constipation.
Opioids can also cause spasm of the sphincter of Oddi and increase smooth muscle tone in the gastrointestinal tract.
Opioids can relieve the pain of sphincter of Oddi spasm caused by opioids.

Genitourinary System

Opioids can cause urinary retention and decreased uterine tone.

Placental Transfer

Opioids can cross the placenta and affect the fetus.

Pharmacodynamic Tolerance and Physical Dependence

Opioids can cause pharmacodynamic tolerance and physical dependence.

Morphine

Morphine is a natural opioid with a peak effect at 30-60 minutes and a duration of action of 4-6 hours.
Morphine can cause nausea, vomiting, and respiratory depression.
Morphine is poorly absorbed orally due to first-pass metabolism.
Morphine accumulates rapidly in the liver, kidneys, and lungs.

Fentanyl

Fentanyl is a synthetic opioid with a rapid onset and short duration of action.
Fentanyl has a greater protein binding and lipid solubility compared to morphine.
Fentanyl is metabolized by the liver and excreted in the urine.

Alfentanil

Alfentanil is a synthetic opioid with a fast onset and short duration of action.
Alfentanil has a greater protein binding and lipid solubility compared to fentanyl.
Alfentanil is metabolized by the liver and excreted in the urine.

Remifentanil

Remifentanil is a synthetic opioid with a rapid onset and short duration of action.
Remifentanil is metabolized by blood esterases and has a context-sensitive half-time that is independent of the duration of infusion.
Remifentanil is associated with the potential side effect of hyperalgesia.

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