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NU 600

Exam 4 - Opioids and Induction Agents

T/F: Pain is thought to be always unpleasant. True
Objective signs of pain are based on _______, while subjective signs of pain are based on ________. Vital signs; experiences
What does tissue injury activate and what does this result in? Activates inflammatory mediators and results in increased sensitivity of nociceptors
Where do peripheral nociceptors carry pain signals to? Dorsal horn of the spinal cord
Output neurons from the dorsal horn ascend the spinal cord after crossing into what feature? Anterior lateral quadrant
Pain impulses ascend via what two fibers and in what tract? Alpha and Delta fibers in the spinothalamic tract
Prior to terminating in the somatosensory cortex, what structure do Alpha and Delta fibers enter? Thalamus
Where do somatosensory fibers terminate? Primary somatosensory cortex
What is the general method of action of opioids? Block transmission of pain by decreasing action potentials of sensory neurons
What channels do opioids affect? Sodium, potassium, calcium
How does pain affect the SNS? Increases SNS tone
How does pain affect global O2 demand? Increases
In what 3 ways does pain affect breathing? Hypoventilation, atalectasis, decreased cough
What two hormones do opioids reduce? Adrenocorticotropic, cortisol
How do opioids contribute to dynamic fluid stability? Decrease stress response
True/False: Opioids have negative cardiac effects and should be used sparingly. False = cardiac friendly and can be used in large doses
Which enzyme is inhibited by opioid binding? Adenylate cyclase
The neuron is (hyper/hypo)-polarized as a result of opioid binding. Hyper-polarized
The presynaptic effects of opioids blocks the release of what 3 neurotransmitters? Dopamine, norepinephrine, substance P
Mu I receptors are located (above/below) the spinal cord. Above
(Mu I/Mu II) receptors provide supraspinal analgesia. Mu I
What are the side effects of Mu I receptor stimulation? Euphoria, miosis, pruritis, urinary retention, N/V
What are the negative side effects of Mu II receptors? (4) Sedation, bradycardia, respiratory depression, ileus
Apnea and hypoventilation are caused by stimulation of (Mu I/Mu II receptors). Mu II
(Mu I/Mu II) receptors are associated with more side effects. Mu II
Delta, Kappa, and Sigma are types of _______ receptors. opiate
Mu activity and dependence are related to stimulation of (Delta/Kappa/Sigma). Delta
What are the responses of kappa receptor stimulation? Spinal analgesia; sedation; myosis
What are the responses of sigma receptor stimulation? Dysphria, hypertonia
How much more potent is fentanyl over morphine? 100x
Fentanyl has a/an (stable/unstable) cardiac profile. Stable
Fentanyl ideal as a (primary/adjunct) analgesic. Adjunct
Fentanyl is associated with more (Mu I/Mu II) symptoms. Mu II
Which medication is associated with chest wall rigidity? Fentanyl
All opioids have the capability of causing _______. Nausea
What is the Vd for fentanyl? 4L/kg
What is the onset and duration of effect fentanyl? Onset=immediate; Duration=30min to 1hr
The ½ life of fentanyl is _____ minutes. 219
Fentanyl undergoes 1st pass effect in the ______. Lungs
How much of the initial dose of fentanyl is metabolized in the lungs? 75%
Fentanyl metabolites are (active/inactive). Inactive
How much fentanyl is cleared in the urine? How much is excreted unchanged in urine? 75%; 10%
1st pass metabolism of fentanyl occurs in the ________. Liver
Describe the mechanism by which fentanyl’s effects may be prolonged. Continuous infusion or boluses lead to saturation of inactive tissues
What should be given in the event of chest wall rigidity with fentanyl? NMB
What are the low, moderate, and large doses for fentanyl? 1-3mcg/kg; 3-10mcg/kg; 50-150mcg/kg
Name the scenarios in which low, moderate, and large doses of fentanyl would be used. L=minor procedures; M=DL or w/surgical stimulation; L=cardiac anesthesia
Moderate dosing of fentanyl blunts the ______ pathway. Nociceptive
What dose of fentanyl is required to blunt the response to directly laryngoscopy? 3-10mcg/kg
Fentanyl is associated with the release of what 2 hormones? Prolactin, HGH
What are the non-analgesic effects of fentanyl? Respiratory depression, bradycardia, euphoria, sedation, dysmotility, prolactin and growth hormone release
Where are Mu receptors located in the body? Cerebral cortex, thalamus, hypothalamus, midbrain and medulla, dorsal horn, gut, peripheral tissues
What neurological effect are Kappa receptors associated with? Dysphoria
Kappa receptors have (weaker/stronger) analgesic and respiratory effects than Delta and Mu receptors. Weaker
Pain is generally (under/over) reported in the elderly. Under
What are three systems breakdowns that affect the dosing of analgesics for the elderly? GI malabsorption, decreased hepatic fxn, decreased CYP enzymes
What is the effect of the GG variant of the A118A polymorphism in men? Lower pain threshold
Men have lower pain threshold d/t what genetic variant? GG variant of Au8A
Chronic ETOH use leads to enzyme (induction/inhibtion). Induction
Give an example of cross tolerance. Chronic ETOH leads to enzyme induction, requiring higher doses of pain medication for effect
Which opiate analgesic is least affected by genetic variability of the CYP system? Fentanyl
What are the 5 methods of administration for fentanyl? PO, IV, intrathecal, epidural, transdermal
What does preemptive analgesia decrease? Sensitization of the CNS to pain impulses
When should pre-emptive analgesia be given? Almost any time: upfront prior to painful stimuli, intra-operatively, after discharge home
What are the benefits of multimodal analgesia vs. opiate analgesia? Improved pain relief, reduced SE, opiate sparing
What are three types of medications used with multimodal therapy? NSAIDS, COX2 inhibitors, APAP
What does the Equianalgesic Theory state? Doses of different opioids can provide equivalent pain relief
10mg IV morphine = _____ mg IV dilaudid = _____ mcg IV fentanyl. 1.5; 100
Which medication serves as the “Gold Standard” for opioids? Morphine
What type of metabolism does morphine undergo? Phase II glucuronidation
Name the 2 metabolites of morphine and describe the differences. Morphine-6-glucuronide=active=1/4 potency of morphine; morphine-3-glucuronide=inactive
Which pain receptors exhibit characteristics for physical dependence/abuse potential, and which do not? High abuse potential=MuII/Delta; Low abuse potential=MuI, Kappa
Inhibition of peristalsis, nausea, and vomiting are associated with which pain receptor? MuII
Which pain receptor exhibits diuretic symptoms when stimulated? Kappa
Which pain receptor inhibits the release of vasopressin? Kappa
Which pain receptor is associated with psychomimetic (i.e. hallucinations, delirium) reactions? Kappa
Individuals with (renal/liver) failure are at risk for increased levels of active morpine metabolites. Renal
What is the ½ life for morphine and its active metabolite? Morphine=114min, M6G=173min
Sufentanil is a _______ derivative. Phenylpiperidine
Sufentanil is _______ times more effective than fentanyl. 10
In what surgical scenarios is sufentanil used? High dose cardiac and spinal procedures
Which opioid is ideal for continuous infusions? Sufentanil
How are fentanyl and sufentanil dosed? mcg/kg/hr
Which opiate has the highest lipophilic profile? Sufentanil sufentanil
The bolus dose of sufentanil is _________ mcg. 10-25
In spinal cases, when should sufentanil be stopped? 40min before expected wake-up
After sufentanil is stopped, _______ should continue running at _____________ to GA. Propofol; 150mcg,kg,min
Post-op pain control is better obtained with periop use of (sufentanil/remifentanil). Sufentanil
Which opioid does not undergo organ-dependent elimination? Remifentanil
True/False: Remifentanil is effective as a bolus because of its rapid onset. False = infusion only d/t profound apnea
How is remifentanil metabolized? Ester hydrolysis by tissue and blood esterases
Remifentanil (does/does not) depend on plasma cholinesterase for metabolism. Does not
What is the onset, duration of effect and ½ life of remifentanil? Immediate; 5-10min; 10-20min
Renal and hepatic issues (do/do not) affect metabolism of remifentanil. Do not
What classification of opioid is dilaudid and when is it used? Intermediate acting semisynthetic used for moderate to severe pain
The onset of dilaudid is ______ min with a duration of ______ hrs. 5; 4-5
What are two significant benefits of dilaudid? No active metabolites and diminished SE profile
Demerol is a member of the _______ group. Phenylpiperidine
Demerol forms (active/inactive) metabolites. Active
What is the active metabolite of demerol and what can it cause? Normeperidine; seizures
Which opioid has pro-epileptic qualities? Meperidine
In what patients is demerol not recommended for use? Sickle cell, CNS d/o, renal failure, children
What is the post-op dose of meperidine used for rigors? 6.25mg -> 12.5mg -> 25mg
Meperidine is potentially lethal when combined with what other class of medications? MAOIs
What two physiological symptoms may result from the use of meperidine with MAOIs? Hypotension, respiratory depression
Besides Mu receptors, receptors in what other areas may contribute to respiratory depression? Cortical and brainstem
What is the potential problem with narcotic use in cholangiograms? Biliary spasms
Which is the better indicator for patient satisfaction: PONV or post-op pain? PONV
Nausea is triggered by stimulation of what three receptors? Dopamine, serotonin, histamine Dopamine, serotonin, histamine
(Men/Women) are more prone to PONV. Women
What is the classification of nalbuphine? Synthetic opioid agonist-antagonist
Nalbuphine is a _____ receptor agonist, and a _______ receptor antagonist. Kappa, Mu
What are the possible benefits of nalbuphine if used during a cholangiogram? Reverses respiratory depression and sphincter of Oddi spasm
Nalbuphine is equipotent to which opiate? Morphine
Buprenorphine is a/an (agonist/partial-agonist) of the ______ receptor. Partial-agonist; Mu
The effects of buprenorphine can last up to _______ hrs. 8
What are two characteristics of the relationship between buprenorphine and naloxone? Buprenorphine not readily reversed by naloxone; used together in drug rehab
Which medication is often paired with naloxone in its use for drug rehabiliation? Buprenorphine
Buprenorphine can cause withdrawal symptoms in what types of patients? Patients who have been receiving Mu opioid agonists
What type of receptor does Narcan primarily influence? Mu
Besides Mu receptors, what other receptors are affected by Narcan? Kappa and Delta
What is the serum ½ life of Narcan? 64 minutes
Narcan blocks both ______ and ______ opioids. Endogenous; exogenous
_______ administration can precipitate flash pulmonary edema. Narcan
True/False: The effects of Narcan last as long as opioids. False – does not last as long
What is the drawback to rapid administration of Narcan? Acute w/d manifested as sz, dysrhythmias, intense pain
How is Narcan prepared for administration? 1amp (0.4mg/ml) is diluted in a syringe of 10cc NS to yield 40mcg/ml
After dilution in a 10cc syringe, how much and how often is Narcan administered? 0.5-1.0ml q5min until desired effect is achieved
What is the benefit of the anesthesia method of naloxone administration? Antagonizes only the MuII receptor (sedation, respiratory depression) while analgesia is maintained
What does the anesthesia method of Narcan administration reduce? The dramatic effect of Mu agonism reversal
What are the physiologic effects of rapid Mu agonism reversal? Acute narcotic w/d, seizures, flash pulmonary edema
What is the classification of Precedex? Highly selective and potent alpha-2 adrenergic agonist
Precedex is ______ times more selective for alpha-2 receptors than clonidine. 10
What is Precedex an isomer of? It is a dextro isomer of medetomidine
What are the 3 sites of action of dexmedetomidine? Brain, spinal cord, autonomic nerves
What are the CNS effects of dexmedetomidine? Sedation/hypnosis, anxiolysis, analgesia
What are the autonomic effects of dexmedetomidine? Decreased sympathetic activity (i.e. decreased BP and HR)
Post-op controlled ventilation may be achieved with an infusion of _________. Dexmedetomidine
What is the reversal medication for dexmedetomidine? Atipamezole
What are the benefits of dexmedetomidine for children in anesthesia? Effective for emergence agitation/delirium
Name 2 different alpha-2 agonist medications. Dexmedetomidine & clonidine
What does dexmedetomidine inhibit that gives it vasodilating properties? Catecholamines and renin
Induction agents (can/cannot) be utilized for TIVA. Induction agents (can/cannot) be utilized for TIVA. can
What types of surgical cases benefit from TIVA? Cases involving neuro-monitoring
What is the keystone of barbiturate induction agents? Sodium thiopental
What is STP derived from? Barbituric acid
Barbituric acid (does/does not) have CNS activity. does not
What provides barbituric acid with its sedative hypnotic effects? Changes at the 2 and 5 carbon positions
How are pro-epileptic effects of barbiturates obtained? Methyl radical substitution on the #5 carbon
How are anti-convulsive effects achieved with phenobarbital? Phenol group addition at #5 carbon
True/False: Barbituratic inductiona agents do not burn on injection. False
What is the trade name for methohexital? Brevital
What does addition of a phenol group to the #5 carbon of phenobarbital produce? Enhanced anti-convulsive properties
Where is the sulfur placed that produces sodium thiopental? #2 carbon
What does the sulfur addition in STP produce? Increased hypnotic potency, fast onset, shortened duration
What is the trade name for sodium pentothal? Thiopental
What medication has been used for physician assisted suicide? Pentobarbital
What is the trade name for pentobarbital? Nembutal
Which channels does the barbiturate-GABA relationship influence and how does it affect these channels? Influences duration of chloride channel opening (hyperpolarization)
What creates the hangover effect from barbiturate administration? High fat affinity (reservoirs)
What is the primary determinant of barbiturate distribution? What other factors play a role in distribution? Lipid solubility; cardiac output, blood volume, protein binding ionization
What is the cause of cessation of effects with barbiturates? Redistribution away from CNS
What should be used to calculate barbiturate dosing. Lean body mass (not actual body weight)
Barbiturates (do/do not) provide analgesia. Do not
Barbiturates (do/do not) obtund airway reflexes. Do not
What is the difference between transient and global ischemia in terms of barbiturates? Barbiturates may offer protection w/focal, little benefit w/global
True/False: Methohexital is effective for muscle relaxation on induction. False = induces involuntary muscle contractions
Which patient population are barbiturates contraindicated in? Patients with inducible porphyria’s (Vampire’s Dz)
What reaction can thiobarbiturates cause? Mast cell histamine release
True/False: Oxybarbiturates are implicated in mast cell mediated histamine release. False
What is the treatment for extravasation d/t barbiturate administration? 1% procaine and local application of heat for pain
What are the building blocks for heme and what body systems do they affect? Porphyrins; skin and nervous
What steps are taken in the event that a barbiturate is injected into an artery? Sympathetic block to affected area; heparinization; alpha-adrenergic antagonist for vasopasms
What is the classification of etomidate? Carboxylated imidazole
What induction agent is water soluble in storage, then molecularly changes to become lipid soluble after injection? Etomidate
What is similar about etomidate and barbiturates in regards to adverse drug reactions? Can cause inducible porphyrias
What three types of medications can be given to blunt hyperdynamic responses? BZD, sevoflurane, beta-blocker
What is a drawback and benefit of ketamine in relation to dysrhythmias? May reverse digitalis induced dysrhythmias; may predispose myocardium to dysrhythmias when local anesthetics w/epinephrine are used
What should be given simultaneously with ketamine to reduce its adverse effects? Antisialogogue b/c ketamine increases oral/bronchial secretions
What induction medication leaves upper airway reflexes intact? Ketamine
What must simultaneously be given with ketamine and why? Antisialogogue d/t increased oral and bronchial secretions
What are two pulmonary benefits of ketamine? Leaves upper airway reflexes intact; potent bronchodilator
What are the effects of ketamine on pulmonary vasculature? Increases pulmonary vascular resistance, leading to increased RV workload
What induction agent has been effective as treatment for status asthmaticus? ketamine
What is the classification of propofol? Non-barbiturate sedative hypnotic
Where does propofol primarily exert its influence? GABA receptors
What does the 1st pass pulmonary effect of propofol yield? 2,6 – diisopropoyl – 1,4
SSEPs (are/are not) significantly altered by propofol. are not
Unused portions of a propofol should be discarded within _______ hours of opening. 6
Created by: philip.truong