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148 Cards in this Set
- Front
- Back
Meperidine
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Demerol
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Fentanyl
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Sublimaze
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Sufentanil
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Sufenta
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Alfentanil
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Alfenta
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Remifentanil
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Ultiva
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Naloxone
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Narcan
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Naltrexone
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Narcan
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Nalmafene
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Revex
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Enkephalins
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Leu
Met |
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4 groups of chemicals in the body that relieve pain
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Enkephalins
Beta Endorphins Dynorphins Endomorphins |
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Precursor for enkephalins
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proenkephalin A
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Precursor for beta-endorphins
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pro-opiomelanocortin
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precursor for dynorphins
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prodynorphin
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precursor for endomorphin
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unknown
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How many amino acids are in enkephalins?
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pentapeptide (5 amino acids long)
Tyr-gly-gly-phe-leu (met) |
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What is pro-opioimelanocortin (precursor for beta-endorphin) broken down into?
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ACTH (which is further broken down to alpha MSH)
and Beta-Lipotropin (which is further broken down to Beta Endorphin and Beta MSH) |
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What is prodynorphin broken down into?
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alpha neoendorphin, dynorphin A, dynorphin B
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Name for pain receptors.
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nociceptors
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What is another name for pain relievers/narcotics?
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antinociceptors
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What is the goal of multimodal therapy for pain relief?
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-decrease the dose of a single agent
-improve nociception -reduce side effects -avoid sedation and respiratory depression |
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highest concentration of mu receptors are found where?
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thalamus
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How do you feel pain?
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Electrical signal travels down the neuron must signal for the release of the neurotransmitter that produces pain. Neurotransmitter travels across the synapse between neurons and attaches to the appropriate receptor. A pain signal is then sent up the spinalthalamic tract.
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What spinal tract sends pain signals up the spinal cord to the brain?
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spinothalamic tract
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How is pain block by endorphins, etc.?
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Opiate receptors on the presynaptic neuron are activated, a conformational change takes place that prevents the release of the pain neurotransmitter.
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Opiates work as...
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a presynaptic agonist on the pain neuron by stimulating the opiate receptor
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What is the difference between mu1 and mu2 receptors in humans?
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there is none
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The amount of analgesic a narcotic produces is equal to ...
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the amount of respiratory depression and the amount of addiction.
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The 3 primary subtypes of opiate receptors.
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mu
kappa delta |
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What is the main receptor for producing anything to do with a narcotic?
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mu receptors
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what ligands work at the mu receptors?
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endomorphin 1 & 2
met-enkephalin dynorphin A and B |
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What ligands work on the kappa receptors?
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dynorphin A and B
Beta endorphin |
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What ligands work on the delta receptors?
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Leu and met-enkephalins
beta endorphin |
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What receptors does Narcan reverse?
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all of the opiate receptors
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Partial agonists will give you 100% efficacy for analgesia but not respiratory depression. T/F
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False. No matter how high the dose partial agonist will never reach 100% efficacy.
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Why would you give a partial agonist knowing that it won't reach 100% efficacy?
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to decrease the amount of respiratory depression experienced
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What are the natural occurring phenanthrene alkaloids?
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Morphine
Codeine Thebaine |
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What are the semi synthetic phenanthrene alkaloids?
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Heroin
Vicoden Dilaudid Oxycontin Oxymorphone |
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What are the synthetic opioids?
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Levorphanol
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What are the phenylpiperidine derivatives?
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Meperidine
Fentanyl Sufentanil Alfentanil Remifentanil |
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What are the propionilide derivatives?
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Methadone
Propoxyphene (Darvon) |
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If someone is truly allergic to Dilaudid, can you give them Morphine?
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No; because they fall within the same class of phenanthrene alkaloids
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If someone tells you they are allergic to morphine because they experienced severe nausea and vomiting the last time they were given a dose, is this a correct statement?
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No; they experienced the normal effects of opioid drugs
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There is a cross allergy _____ chemical classes but not _____ chemical classes.
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within; between
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What are all opioids compared to when determining their potency?
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Morphine
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Opioids are have a high degree of anesthetic potency. T/F
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False. They do not provide any anesthesia only analgesia
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Analgesia goes hand in hand with what other effects when discussing opioids?
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analgesia, respiratory depression, and addiction
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Where are opiates metabolized?
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in the liver by the cytochrome enzymes in the endoplasmic reticulum
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What happens to opiate levels when someone is enzyme inhibited?
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will have prolonged response to the opiates because they are not being metabolized as quickly
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What happens to opiate levels when someone is enzyme induced?
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levels drop very quickly because of excessive metabolism. Patient requires higher doses of opiate.
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What happens to opiate levels in a liver disease patient?
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unable to metabolize the drug so the drug effect stays around longer
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What is the only opiate that is not metabolized in the liver?
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Remifentenil
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Where is Remifentenil metabolized? by what?
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Remifentenil is hydrolized in the plasma by nonestherase dependent enzymes
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What happens when Demerol is metabolized?
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It is metabolized to active/toxic metabolite normeperidine
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What is the problem with the metabolite normeperidine?
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It is toxic with prolonged administration. Increased levels can cause seizures.
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What demographic of patients are at higher risk for toxic levels of metabolite when given demerol?
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Elderly and renal patients
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What is the chemical make up of Remifentanil that allows it to be easily hydrolized in the plasma?
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has an esther group
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Remifentenil is a long acting opioid. T/F
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False. It is very short acting. Must be given by continuous infusion with a plan for analgesia to be given as soon as the drip is discontinued.
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What procedure takes the most analgesia to block the stress response?
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intubation
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What cardiac effects are produced by opiates?
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-slight bradycardia
-minimal vasodilation w/ phenanthrene drugs -hypotension will be seen if pt is dehydrated |
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What cardiac effect is noted with Demerol?
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tachycardia
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What are the emetic drugs that we have discussed thus far?
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opiates
Etomidate Ketamine Nitrous Oxide |
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What are the anti emetic drugs?
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Propofol
Droperidol |
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What is the only affect of narcotics that is not diminished with tolerance?
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miosis
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What produces the miotic effects of narcotics?
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Constriction of the pupil is caused by an exictatory action on the parasympathetic nerve innervating the pupil. Opioids abolish the cortical inhibition of the Edinger-Westphal nucleus
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Acute effects of Opioids
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analgesia
Ventilatory depression Sedation Euphoria Vasodilation Bradycardia Cough Suppression Miosis Nausea and Vomiting Skeletal muscle ridgidity Smooth muscle spasm Constipation Urinary retention Biliary Spasm pruritus Antishivering (meperidine) |
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Where is the CTZ located?
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the area postrema of the brain stem
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The CTZ contains opiate receptors as well as what other neurotransmitters?
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dopamine, serotonin, histamine, and muscarinic acetylcholine
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Opiates stimulate ____ but inhibit _____.
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CTZ; vomiting center
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The frequency of nausea and vomiting goes ____ after several days of taking opiates.
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down; this is due to the inhibition of the vomiting center
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What can cause vomiting if released into the CTZ?
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histamine; antihistamines can have an antiemetic effect
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Where does the vomiting center receive its input from?
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the CTZ and peripheral sites via the vagus nerve
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Anesthetic Risk factors for PONV
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Volatile agents
Nitrous oxide Opioids High doses of neostigmine Ketamine Etomidate |
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Patient Risk factors for PONV
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Female gender
History of PONV or motion sickness Pain High levels of anxiety |
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Surgical Risk factors for PONV
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Long surgical procedures
Certain types of surgery (ie. intra abdominal, major gynecologic, laparoscopic, breast, ears/nose/throat) |
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What is the CTZ?
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Chemoreceptor Trigger Zone
area in one of the ventricles where there is no BBB. It has direct access to the chemicals in the blood. There is an immediate response to vomiting. |
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What effect do anticholinergic drugs have on the CTZ?
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antiemetic effects
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What area of the brain is responsible for chronic nausea?
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vomiting center
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What class of drugs causes the most nausea and vomiting?
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opiates
|
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Frequency of nausea and vomiting (increases/decreases) the longer the duration of treatment.
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decreases
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Nausea and vomiting is worse in patients that are...
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ambulatory
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Therapy that involves giving more than one drug that acts on different receptors for the same thing.
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multimodal
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A single dose of what drug can be given for PONV prophylaxis?
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dexamethasone
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What are the risk factors used for the scale to determine the managment of PONV?
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female gender
nonsmoker history of PONV postoperative opioids |
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How do narcotics depress ventilation?
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shifts the CO2 response curve to the right (depressing the respiratory center sensitivity to CO2-require a higher CO2 to get the same amt of respirations as a nonanesthetized patient)
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What does a PCO2 shift to the right mean?
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requires a higher CO2 for increased RR
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What combination of circumstances cause chest wall ridgidity?
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-dose of narcotic
-speed of administration -use of nitrous oxide at the same time -use of narcotics in older patients -absence of muscle relaxants |
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What two opiates cause the greatest incidence of rigidity?
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alfentanil and remifentanil
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When does ridgidity occur?
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can be immediately after dose or it can occur several hours after the last dose of narcotics has been given
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How do you treat chest wall ridgidity?
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succinylcholine or nondepolarizing muscle relaxant
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What is primarily responsible for difficulty ventilating a patient that has been given opiates?
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vocal chord closure
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What is primarily responsible for delayed or postoperative muscle ridgidity?
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second peak in plasma opioid concentration after redistribution
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What is the pathway that causes miosis with opiates?
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abolishing the cortical inhibition of the Edinger Westphal nucleus
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Patients can have an allergic reaction to opiates that causes pruritis. T/F
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False-pruritis is a normal effect of the medication not an allergic reaction
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What opiate can be given to stop post operative shivering?
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Demerol
mediated through kappa receptors |
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Use of what drugs can prevent increases in intraocular pressure during induction of anesthesia?
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fentanyl, sufentanil, and alfentanil
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What receptors cause constriction of the pupil?
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mu and kappa receptors
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What receptor mediates itching?
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mu receptors
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What drugs will reduce pruritis related to opioid use?
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naloxone and zofran
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What happens in the biliary tree with opiate administration?
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they cause constriction of the sphincter in the biliary tree via the vagus nerve
-more potent the narcotic the more pressure produced in the biliary tree |
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What drugs can reverse the pressure in the biliary tree?
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1. atropine and glycopyrrolate
(counteracts the vagal effect) 2. nitrolycerine (NTG is smooth muscle relaxer) 3. glucagon (also smooth muscle relaxer) 4. naloxone (reverse narcotic) |
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What drug is five times more potent than fentanyl?
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Sufentanil
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What drug is ten times less potent than fentanyl?
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Alfentanil
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What is the duration of action for Narcan?
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30-60 min
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What is the name of the opiate antagonist that is 100% soluble at all times in the body?
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Alvimopan (Entereg)
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Does alvimopan pass the BBB?
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no it is not lipid soluble-100% water soluble
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What does Alvimopan block?
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the GI effects normally caused by opiates but still gives analgesic effects
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What is front loading?
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giving a bolus dose (highest dose) at the beginning of the case so that the blood level of drug drops by the end of the case to reduce the incidence of respiratory depression
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Opioid will (increase/decrease) the MAC of the gas anesthetic.
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decrease
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What receptors are the classical pharmacologic effects of morphine mediated by?
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mu receptors
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What drug is contraindicated with MAO inhibitors?
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demerol
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What is the most potent opiate in the world?
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sufentanil
|
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What class of drugs cause amnesia?
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benzodiazepines
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Is a decrease in ventilatory rate a sensitive indicator of opioid effect?
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No a patients drive to breathe may be abnormal despite an apparently normal ventilatory rate and state of consciousness
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Does sleep affect the ventilatory response?
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yes-sleep further depresses the response to CO2 and potentiates the ventilatory depression caused by opioids
|
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Which opiate produces the most respiratory depression?
|
They all produce equivalent amounts of ventilatory depression in equivalent doses
|
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How do opiods suppress cough?
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by depressing cough centers in the medulla
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What is a pathognomonic sign of opioid overdose?
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pinpoint pupils
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Why is it difficult to reverse respiratory depression without reversing analgesia?
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because the same receptor is responsible for both-reverse one you reverse the other
|
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What is stimulated in ambulatory patients that makes them more likely to experience nausea and vomiting than nonambulatory patients?
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stimulation of the vestibular apparatus
|
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Hypertonus of the skeletal muscle is most commonly experienced with which drugs?
|
fentanyl, alfentanil, sufentanil, and remifentanyl
|
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What potent opioids do not release histamine?
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fentanyl, alfentanil, sufentanil, and remifentanyl
|
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What effects do opioids have on the GI system?
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delay gastric emptying and increase antral tone
|
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What effects do opioids have on the gall bladder?
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contraction of smooth muscle in the gall bladder and spasm of the sphincter of Oddi which can precipitate biliary colic
|
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Neonatal withdrawal can occur ____ after delivery.
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shortly
|
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When tolerance to an opioid occurs, there is simultaneous development of cross tolerance to all other opioid agonists. T/F
|
True
|
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What effects caused by opioids do people develop tolerance to most rapidly?
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analgesia, ventilatory depression, euphoria
|
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What drug has a low lipid solubility that gives it some of morphine's characteristics as a selective spinal analgesic?
|
hydromorphone
|
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This drug is a long lasting synthetic mu opioid approximately equipotent with morphine.
|
Methadone
|
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What accounts for the rapid onset and short duration of fentanyl?
|
high lipid solubility
|
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Do narcotics increase ICP?
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No-the respiratory depression can cause an increase in CO2 that causes vasodilation in the brain increasing blood flow and increasing ICP
|
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Opioids produce a dose related _____ in the need for volatile anesthetics.
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decrease
|
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Naloxone acts as a ________ at ___ opioid receptors.
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competitive antagonist; all
|
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What two drugs cause the most biliary spasm?
|
morphine and fentanyl
|
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Are all NSAIDS antiinflammatory?
|
no acetaminophen is not
|
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All NSAIDS are antipyretic and analgesic. T/F
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True
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What is the primary mechanism by which NSAIDS exert their analgesic effect?
|
inhibition of cyclooxygenase and synthesis of prostaglandins
|
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NSAIDS act only as peripheral analgesic agents. T/F
|
False. They also have analgesic effects through inhibition of spinal COX
|
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What are the functions of the COX 1 enzymes?
|
they participate in platelet aggregation, hemostatsis, and gastric mucosal protection
|
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What are the functions of the COX 2 enzymes?
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they participate in pain, inflammation, and fever
|
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Why is perioperative use of NSAIDS associated with a higher incidence of gastrointestinal bleeding?
|
inhibition of COX 1 inhibitors that are necessary for the synthesis of cytoprotective gastric mucosal prostaglandins
|
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What major affect can NSAIDS have after surgery?
|
NSAIDS affect bone osteogenesis during bone repair
|
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What population of patients should you use caution with when giving Toradol?
|
patients with impaired renal function or history of kidney disease-it is a potent inhibitor of prostaglandin synthesis
|
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How is Toradol and its metabolites eliminated from the body?
|
primarily by the kidneys
|
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When is Toradol contraindicated?
|
in patients with serum creatinine concentrations indicating advanced renal impairment
|
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How do you measure the effect of ASA on patients?
|
check the bleeding time
|
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What is the principal use of ASA?
|
platelet inhibition-irreversibly inhibits platelet function for 8-10 days
|
|
What is the max dose of Tylenol per day?
|
4 gm
|
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What drug will Tylenol increase the effects of ?
|
Warfarin-increasing the aticoagulant effect
|