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56 Cards in this Set
- Front
- Back
Define Nociceptive pain
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Stim. of peripheral nerve
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Are All of the following are considered nociceptive pain?
Cold, Burn, Alc. on wound Herptetic neuralgia, Phantom limb pain |
Cold, burn, alc. on wound are nociceptive pain
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MOA of Opioids?
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G-protein coupled receptors in CNS and spinal cord regions involved in modulation of pain
Close voltage-gated Ca2+ channels on presynaptic nerve terminals --> reducing transmitter release Hyperpolarize = inhibit post-synaptic neurons by opening K+ channels |
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What receptors do opiods have actions at?
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Mu, Kappa and delta
They can be agonists at one and antagonists at another |
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What are the actions of the mu receptor acted on by opiods?
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Supraspinal and spinal analgesia, inhibition of respiration, slowed GI transit, modulation of hormone and NT release, euphoria
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What are the actions of the delta receptor acted on my opioids?
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suprespinal and spinal analgesia, modulation of hormone and NT release
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What are the actions of the kappa receptor acted on by opioids?
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Supraspinal and spinal analgesia, psychomotor effects, slowed GI transit, dysphoria
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T/F: If you give exogenous Opioids, you can spur release of endogenous opioids
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TRUE
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What are the sites of opioid action in the ascending pathway?
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Periphery, Dorsal Horn, ventral caudal thalamus
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What is the role of the descending pathway in opioid drugs?
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Lesser understood - thought to inhibit pain transmission neurons
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What are the sites of opioid action in the descending pathway?
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Periaquaductal gray
Rostral ventral medulla Dorsal Horn |
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Frequent repeated doses of a drug produce a gradual loss of effectiveness. What does this describe?
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Tolerance
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When a drug is stopped or antagonist administered and the pt. experiences withdrawal syndrome, what does this define?
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Dependence
(The Symptoms themselves are the withdrawal) |
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What are the possible hypotheses for tolerance?
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cAMP upregulation
NMDA Receptor recycling Receptor uncoupling Note - persistent administration of opioids increases the sensation of pain |
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A pt comes in after stopping an opioid, describing the sensation of euphoria and analgesia, mental clouding b/c they can't do their taxes, sedation, respiratory depression, Anti-diuresis, N, V, and cough suppression. What level of Tolerance does this describe?
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HIGH
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A pt stops their opioid med and you note bradycardia on PE. What level of tolerance are they experiencing?
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Modertate
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What are the symptoms of LOW tolerance?
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Miosis, Constipation, Convulsions
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T/F: Opioids are well absorbed through most routes, but undergo significant first pass effect
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TRUE - Subcu, IM, Oral
Codeine + Ocycodone do NOT undergo significant first pass effects |
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do Opioids localize rapidly or slowly to highly perfused tissue sites?
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Rapidly to places like brain, kidney, lung, liver, spleen
= what makes them fun to abuse |
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Whats the main reservoir of opioids?
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Skeletal muscle
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A pt is elderly an thus their metabolism has slowed substantially. After giving them codeine, would you expect to see more codeine or morphine in their system?
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Codeine
Codeine --> Morphine via CYP2D6 Slow metabolizers can't covert it fast, thus we'll see build up of Codeine Note: Oxycodone and Hydrocodone are also metabolized by CYP2D6 |
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What are the CNS affects of Opioids?
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Euphoria, Dysphoria, Sedation, Respiratory Depression, Cough suppression, miosis, truncal rigidity, N, V, Temp (u agonists = hyperthermia, kappa agonist = hypothermia)
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What are the effects of opioids on CV?
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MOST cause bradycardia,
Meperidine causes Tachycardia |
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What do opioids do to GI tract, Biliary tract, and Renal system?
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GI = constipation b/c they dec. motility
Biliary = contract biliary sm. m = biliary colic, Inc. amylase and lipase Renal = depressed due to dec. renal plasma flow |
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A Preggo Pt on an opioid wants to know what SE's she can exect in terms of her uterus. (and neuroendocrine, pruritis, immune system). what do you tell her?
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Uterus = prolong labor
Neuroendocrine = stimulate release of ADH, prolactin, somatropin, inhibit LH Pruritis = flushing and warming of skin Immune function = inhibit or augments it |
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What do we need to monitor in a pt who has been on opioids for a long time?
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Their immune function
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What are the clinical uses of opioids?
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Analgesia, Acute pulm edema, cough, D, Shiverring
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A pt suffers from the shivers every time he sees a cup of sugar. What do you give him to tx?
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Meperidine = anti-shiver via alpha-2 receptor subtype
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Pt going in for Sx gets opioids for what reason?
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Pre-Sx = sedative, analgesic
During -Sx = they can minimize CV depression |
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What are the Strong Agonist Opioid agents to know?
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Morphine, Hydromorphone, Heroin, Methadone, Meperidine, Fentanyl
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What are the Mild-moderate opioid agents to know?
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Codeine, Hydrocodone, oxycodone, diphenoxylate, Loperamide, Buprenorphine, Naloxone, Naltrexone, Tramadol, Dextromethrophan
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How do all the opioids we learned about work?
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Agonists of the Mu receptor
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What is methadone used for?
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Heroine addicts = suppresses opioid withdrawal symptoms, analgesia
Tolerance and physical dependence develop slowly and withdrawal symptoms are more mild, but more prolonged than morphine |
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Whats one of the major side effects of Methadone?
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Prolonged QT = why its black boxed
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Whats the primary use of codeine?
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Antitussive (anti-cough), pain relief
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Between Fentanyl and Meperidine, which one is more widely used?
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Fentanyl
(DON'T USE meperidine with tachycardia b/c it can cause QT prolongation) |
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T/F: Hydrocodone and Oxycodone are less efficacious than morphine
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TRUE
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How do we get a fatal overdose of Hydrocodone or oxycodone?
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Drugs that have been modified to release all of the drug at once --> fatal
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What are Loperamide and Diphenoxylate used for?
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Diarrhea
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What do we combine Loperamide and Diphenoxylate with to reduce abuse?
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Atropine
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What receptor do Naloxone and Naltrexone work through?
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Mu
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T/F: Naloxone and Naltrexone have little action in the absence of agonist
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TRUE
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T/F: in the presence of agonist for ex. morphine, the opioids effects are reversed in 3 minutes with Naloxone and Naltrexone
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TRUE
= normalizes repiration, level of consciousness, pupils, bowel activity, awareness of pain |
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Whats one of the main problems associated with administering Naloxone?
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Within 3 minutes, you can see withdrawal symptoms
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A pt comes in having overdosed on opioids, and is now in a coma. What do you use to tx?
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Naloxone
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Why does Buprenorphine have a long DOA?
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Slow dissociation from the receptor
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T/F: Buprenorphine is as effective as Methadaone for tx of opioid dependence
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TRUE
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What is Tramadol used for? SE's?
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Use = Pain
SE = Lowers seizure threshold, serotonin uptake syndrome |
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Dextromethorphan use?
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Anti-tussive
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What do the withdrawal symptoms from opioids depend on?
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Strength of opioid
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When does tolerance from an opioid begin?
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After the first dose
Minimize tolerance by giving smaller doses with longer intervals between dosing |
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T/F: Physical dependence develops as tolerance develops
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TRUE
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What are the withdrawal symptoms seen with opioids?
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Rhinorrhea, lacrimation, yawning, chill, goosebumps, hyperventilation, hyperthermia, mydriasis, muscular aches, V/D, Anxiety, hostility
# and severity depend on degree of dependence |
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T/F: The longer the half life of the drug, the longer time it takes to reach withdrawal symptoms
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TRUE
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How do we prevent dependence on opioids?
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Establish therapeutic goal before starting therapy, once effective dose is established, limit dose to this level, Look at other options, Evaluate frequently
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In what pt. populations should we need to watch use of opioids?
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Preggos, impaired hepatic function, endocrine disease, head injuries, impaired pulmonary function
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