Lecture # 03_Fall Flashcards
Define opioid.
any natural, synthetic, or endogenous substance with morphine-like properties
Name the 2 endogenous opioids.
[Met]-Enkephalin and Beta-Endorphin
What are the 2 most common opioid receptors?
Mu and Kappa
Opioids that act on the ___ receptors cause analgesia and sedation.
Kappa
Opioids that act on the ___ receptors case analgesia, respiratory depression, pruritis, and constipation.
Mu
T or F. Morphine provides analgesia without loss of touch or proprioception, but use is limited due to significant respiratory depression and loss of consciousness.
False. Morphine does not cause loss of consciousness. All other statements are true.
Where what is the function of nociceptive neurons and where can their receptors be found?
These neurons transmit pain. Receptors can be found throughout the CNS and in peripheral nerves.
What is the mechanism of action for opioids?
They inhibit release of and response to excitatory neurotransmitters in nociceptive neurons
Which opioid receptor is responsible for causing nausea, vomiting, and pupillary constriction?
it is unknown
What is the most rapid and complete route of absorption for opioids?
IV
IM absorption of Morphine and Meperidine takes about ___minutes.
20-60
Transmucosal absorption of Fentanyl takes about ___ minutes.
10
Transdermal absorption of Fentanyl takes about ___ hours.
14-24 hours
Benefits of neuraxial absorption of opioids includes ___, ___, and ___.
no sympathectomy, no motor blockade, no loss of proprioception.
10 mg of morphine IV = ___ epidural = ___ intrathecal (spinal).
10mg IV = 1mg epidural = 100mcg intrathecal
Biotransformation of opioids occurs mostly where?
Liver
Which opioid does not undergo metabolism in the liver? Where is it metabolized?
remifentanil is metabolized by plasma esterases by ester hydrolysis.
Which of the following need to be used more carefully with ESRD patients? Why?
A. Fentanyl B. Morphine C. Sufentanil D. Remifentanil E. Demerol
B (morphine) and E (Demerol / Meperidine) because they have active metabolites and are renally cleared.
What is the active metabolite of meperidine?
normeperidine
What is the active metabolite of morphine?
Morphine-6-glucuronide (M6G)
Morphine-3-glucuronide is a metabolite of morphine but it is not active as an opioid agonist - it does have some action as a convulsant, which does not appear to be mediated through opioid receptors; it is mediated by GABA/glycinergic system. As a polar compound, it has a limited ability to cross the blood–brain barrier, but renal failure may lead to its accumulation and result in seizures. (from Wikipedia)
How long does it take to develop a tolerance to opioids?
2-3 weeks
A tolerance to which of the following side effects of opioids can be acquired? Indicate all that apply.
A. analgesia B. euphoria C. sedation D. ventilatory depression E. Constipation
A tolerance to all except constipation can be acquired.
Define addiction.
physical and psychological dependence
Although some degree occurs within ___ days, addiction to opioids usually takes about __ days to develop.
2 days, 25 days
T or F. Addiction to opioids is usually life threatening.
False.
Symptoms of opioid withdrawal mimic severe flu-like illness. List the 11 symptoms seen with opioid withdrawal.
rhinorrhea, sneezing, yawning, lacrimation, abdominal cramping, leg cramping, piloerection, nausea, vomiting, diarrhea, and dilated pupils.
Peak symptoms of opioid withdrawal occur within ___ hrs and last up to ___ days.
72 hrs, 7-10 days
A patient that is over-narcotized will have ___ pupils whereas a person who is going through opioid withdrawals will have ___ pupils.
pinpoint, dilated
T or F. Seizures, altered mental status, and hallucinations are commonly experienced by a person going through opioid withdrawals.
False. These are all rare.
What receptor does Morphine act on?
Mu
What is used to reverse opioid overdose?
naloxone (narcan)
Does morphine cross the BBB?
Yes, but slowly
Is morphine protein bound?
yes - binds to albumin
Why does morphine cause hypoventilation?
it blunts hypercapnic response
Why does morphine cause itching?
It causes a histamine release
What is the advantage of hydromorphone over morphine?
it does not have active metabolites
10mg of morphine = ___mg dilaudid IV
1.5
Methadone is most commonly used for ___ and ____.
treatment of opioid withdrawal and chronic pain
T or F. Heroin produces fast euphoria without nausea.
True
___ is the only opioid with some local anesthetic properties.
Meperidine (Demerol)
___ is often used in the PACU to reduce shivering.
Meperidine (Demerol)
____ can cause CNS excitation, tremors, myoclonus, and seizures
Meperidine (Demerol)
___ is a synthetic Mu receptor agonists that is about 100x more potent than morphine.
Fentanyl
Why do Fentanyl, Sufentanil, and Alfentanil have rapid onset and redistribution to inactive sites?
they are very lipid-soluble and rapidly cross membranes
T or F. Fentanyl is highly protein bound.
True. It is pH dependent though…acidosis leads to unbinding and more free drug
___ is about 1000x more potent than morphine and 10x more potent than Fentanyl.
Sufentanil
Chest wall rigidity is most commonly associated with high doses of ____.
Fentanyl
The potency of ___ is between morphine and fentanyl.
Alfentanil
Respiratory depression seen with Fentanyl is exacerbated when given with ____.
Versed
T or F. Ultiva is metabolized by pseudocholinesterases.
False. Remifentanil (Ultiva) = ester hydrolysis by blood and tissue esterases.
Remifentanil can decrease MAC by up to __%.
90%
Partial agonists bind to Mu-receptor with lower ____.
Efficacy
Which opioid is associated with hyperalgesia?
Remifentanil
___ has good bioavailability, is a strong cough suppressant, and gets converted in to morphine in the body.
codeine
___ + Acetaminophen = Roxicet, Percocet, or Percodan
Oxycodone and OxyContin
____ + Acetaminophen = Vicodin or Lorcet
Hydrocodone (Lortab)
Codeine + _____ = Tylenol #2, #3, #4
Acetaminophen
100mg meperidine ~ ___mg Morphine ~ 1mg____ ~ ____mcg Fentanyl ~10mcg ____
100mg meperidine ~10mg Morphine ~ 1mg Hydromorphone ~ 100mcg Fentanyl ~10mcg Sufentanil
10mg Morphine = ____ Fentanyl
100mcg
Nalbuphine (Nubain) is a strong __ receptor agonist and ___ receptor antagonist.
Kappa agonist (analgesia and sedation)
Mu antagonist (analgesia, respiratory depression, pruritis, and constipation)
Buprenorphine (Buprenex) is a partial ___ receptor agonist and ___receptor antagonist.
Mu agonist (analgesia, respiratory depression, pruritis, and constipation)
Kappa antagonist (analgesia and sedation)
____ could reverse morphine-induced respiratory depression without compromise of analgesia
Nalbuphine (Nubain)
____ has 50x greater affinity for the Mu receptor than morphine
Buprenorphine (Buprenex)
_____ is used in management of chronic pain as well as opioid dependence . It binds more strongly to receptors than other opioids do.
Buprenorphine (Buprenex)
T or F. Buprenorphine (Buprenex) has a prolonged duration of action due to slow dissociation from receptors and is resistant to antagonsim with narcan.
True
Suboxone = ____ + ____
Buprenorphine + Naloxone
___ is an opioid antagonist
Naloxone (Narcan)
What does “context” refer to in “context-sensitive half time?” What is “context-sensitive half time?”
Context is the duration of the infusion prior o stopping it. Context-sensitive half time is the amount of time required for drug concentration in the central compartment to decrease by 50%
Ccontext-sensitive half time increases as a function of the duration of infusion before it was stopped due to ____
movement of drug stored in the peripheral compartments back into the central compartment
