pharm opiod and algesics

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pharm opiod and algesics
2012-02-07 01:28:40
Pharm Mod3 test

exam 2
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  1. What are some of the members of the opiod family
    fetanyl, codeine, oxycodone, propoxyphene
  2. define opioid
    any drug natural or synthetic that has actions similar to those of morphine.
  3. endogenous opioid peptides
    enkephalins, endorphins, dynorphins bodies natural peptides. they have opioid like properties they are found in the CNS and peripheral tissues.
  4. three classes of opioid receptors
    Mu, Kappa, delta
  5. which of the three opioid receptors is most important
    Mu. opiod analgesics act primarily by activating mu recepotrs, weak activation of kappa and do not interact with delta receptors.
  6. what are the responses to activation of mu receptors
    • analgesia
    • respiratory depression,
    • euphoria
    • sedation
    • (also activation is related to physical dependence.)
  7. what are the responses to activation of kappa receptors
    • analgesia
    • sedation
  8. partial agonist
    a drug that produces low to moderate receptor activation when administered alone. but will block the action of a full agonist if given together.
  9. what is transduction in the phases of pain
    • •Transduction—cell damage stimulates pain
    • receptors (nocioceptors) to activate nerve messages
  10. phases of pain
    • •Transduction—cell damage stimulates pain receptors (nocioceptors) to activate nerve messages
    • •Transmission—peripheral nerves carry in messages to the CNS
    • •Perception— CNS recognizes & interpretes pain sensations
    • •Modulation- CNS releases neurotransmitters in response to pain to prevent further tissue damage
  11. Morphine what is it
    • (named after morpheus greed god of dreams)
    • a prototype of strong opioid analgesics. produces analgesia
    • sedation
    • euphoria
    • respiratory depression
    • cough supression
    • supression of bowel motility
  12. pharmacologic effect of morphine
    • causes drowsiness
    • mental clouding
    • anxiety reduction
    • sense of well -being
    • respiratory depression
    • constipation
    • urinary retention
    • orthostatic hypotension
    • emesis
    • cough supression
    • biliary colic
  13. morphine is more effective against what type of pain
    contant, dull sharp, acts at mu receptors
  14. adverse effects of morphine
    • respiratory depression- serious resp rate should be obtained prior to administration. if rate less than 12/min hold
    • -avoid drugs that speeds this process
    • constipation-can be given with stimulant laxative to elleviate constipation
    • orthostatic hypotension- from morphine induced release of histamine causes vasodialtion
    • urinary retention- increases bladder sphincter tone. suppresses awareness of bladder-intervention palpate bladder every 4-6hours. notify prescriber
    • cough suppression-
    • biliary colic
    • emesis- nausea and vomiting
    • Miosis
  15. Emesis
    nausea and vomiting
  16. how to you elleviate sedation caused by analgesic
    take less at more frequent intervals
  17. miosis
    pupillary constriction
  18. morphine routes of administration
    All Oral, Iv, IM
  19. in order to relieve pain what must morphine do
    cross blood brain barier, morphine is inactivated by the hepatic system, but morphine is not lipid soluble. oral doses must be larger because of the first past effect
  20. Physical dependence
    an abstinence syndrome will occur if drug use is abruptly stopped
  21. morphine precautions
    • can cause further respiratory issue- use with caution in patients with asthma, emphysema, kyphoscoliosis, extreme obesity, chronic pulmonale
    • can cause respiratoryy depression in neonate- resp depression can be reversed with naloxone.
    • head injury- use with caution
  22. morphine toxicity
    • coma
    • respiratory depression resp as low as 2-4b/min
    • pinpoint pupils - pupils may dilate as hypoxia sets in rpolonged hypoxia results in shock
  23. treatment of morphine toxicity
    give opiod antagonist (naloxone ( narcan), or nalmefene (revex) longer acting than naloxone), and ventillary support
  24. what to do prior to opioid admin
    • resp rate- resp below 12 hold drug
    • bp - if below pretreatment value
    • pulse - if below pretreatment value
  25. Fentanyl
    Sublimaze- high potency 100 times that of morphine metabolized by cyp3a4 isozyme of cp450
  26. sublimaze has what kind of action
    • rapid action, short duration
    • lipid soluble crosses blood brain barier
  27. methadone
    • like morphine, acts on mu and delta receptors.
    • effective orally, long duration action. treats pain and treat opioid addicts.
    • effects QT interval- may cause fatal dysrhythmias
    • use with caution in patients with patients taking other QT polonging meds (amiodarone, quinidine, erythromycin, tricyclics
  28. methadone client teaching needs
    • take as directed
    • avoid cns depressants benzos, alcohol and other opioids drugs that inhibit CYP3A4 (clarithomycin, fluvoxamine, fluconazole, and nelfinavir
  29. usual dozage range for adult methadone
    2.5 to 20mg q 3 to 4 hours as needed
  30. Heroin
    strong opioid agonist similar to morphine, used in europe US prohibits use
  31. Hydromorphine, oxymorphone, levorphanol
    strong opiod agonist for moderate to severe pain
  32. NSAID
    aspirin, ibuprofen
  33. NSAID adverse effect
    gastric ulceration, acute renal failure, and bleeding
  34. how do NSAID produce effect
    • ihibits cyclooxygenase
    • celebrex
    • ibuprofen
  35. what NSAID is safe for patients with thrombocytopenia
    the nonacetylated salicylates ie magnesium salicylate. COX -2 inhibitors such as celecocib (celebrex)
  36. Acetaminophen
    Does not inhibit COX in periphery, lacks anti inflammatory actions, does not inhibit platelet aggregation and does not promote gastric ulceration, safe for patients with thrombocytopenia
  37. NSAIDS side effect
    Causes ulceration, bleeding
  38. important interaction of acetaminophen
    • alcohol and wafaran (anticoagulant)
    • with alcohol causes liver damage
    • wafarin increases risk of bleeding inhibits wafarin metabolism and causes it to acumulate to dangerous levels
  39. what opioid is preferred for cancer patients
    pure opioid agonists
  40. which opiod have prolonged half life
    methadone (dolopine, methadose), Levorphanol (Levo-dromoran)
  41. What is pain?
    protective sensory warning system
  42. where are pain receptors?
    Peripheral tissue
  43. what does pain do
    provide an early warning system about impending or actual tissue injury which threathens physiological intergrity of the individual
  44. what are your pain meds
    • NSAIDS - tradition and COX 2 inhibitors
    • Opiod- agonist and agonist /antagonists, adjuvant drugs, opioid antagonists
  45. NSAIDS what do they do
    • They decrease production of inflammatory and chemicals (prostaglandins, prostacyclin, thromboxane A) by inhibiting Cyclooxygenase production.
    • they reduce inflammation and nocioreceptor stimulation that cause pain
  46. what are the two enzymes are involved on nocioperception
    • COX-1
    • COX - 2
  47. What is the good enszyme and what does it do
    • Cox -1
    • Gastric protection- prostaglnadins-keep stomach from being irritated
    • reduce gastric acid
    • increase bicarbonate and mucus production
    • promotes mucosal blood flow
    • promotes platelet aggregation- thromboxane A
    • Vasodilation with improved renal blood flow- prostacyclin
    • uterine contraction drugin labor- prostaglandins
  48. Cox 2 - function
    • tissue inflammation- prostaglandins
    • fever - central effect of prostaglandins/prostacyclin
    • CNS sensitization to pain
    • Tissue/blood flow changes promoting colorectal cancer development
  49. acetaminophen why is it prefered
    • good for fever not much antiinflammatory, higher safety index than NSAID, safer for stomach, but not liver
    • acts primarily in brain. limited peripheral activity
  50. What is the ceilling effect
    • means you take drug once it hits the ceilling taking more will not increase effectiveness.
    • thus increasing dose will increase toxicity without improving analgesia.
  51. what can happen if NSAID is used long term
    • increse b/p by decreasing renal blood flow and produce gastric irritation through decreased GI mucus protection.
    • inhibit platelets contributing to bleeding risk.

    If NASAID is affecting bp don't take. Aspiring keeps platelet from aggregating
  52. Adverse effects of aspiring
    • GI effects
    • bleeding
    • renal impairment
    • salicylism- toxicity metabolic acidosis
    • hypersensitivity reactions- hive
    • bronchoconstriction
    • rhinorrhea
    • nasal polyps
  53. Nursing implication with aspirin
    • give with adequate flui/food to prevent gastric irritationk, monitor signs of gastri irritation/bleeding
    • monitor bp for hypertension
  54. what does aspirin do
    • inhibit prostaglandins, thromboxane A and prostacyclin production in both CNS and peripheral tissue
    • Reduces inflamation
    • produces peripheral and central analgesia
    • antipyretic effect in hypothalamus
  55. therapeutic uses of aspirin
    • anti-inflammatory and analgesic for arthritis, headache, musculoskeletal pain; dysmysmenorrhea
    • used in MI and stroke
    • Treatment of fever in adults
    • pushes body to metabolic acidosis
  56. how does aspirin effect platelets
    irreversibly inhibits platelet aggregation; widely used in antiplatelet agents in losw doses to prevent MI and Stroke (325mg)
  57. pharmacokinetics of aspirin
    • abrsorbed in small intestin
    • rectal route is less reliable and is rapidly converted to sallicylicacid; active metabolite in the liver
    • highly albumin bound; crosses blood brain barrier and placenta
  58. how is aspirin available
    po or RP(rectal syppository)
  59. drug interaction of aspirin
    • anticoagulants- wafarin and heparin effects potential with increased risk of bleeding.
    • alcohol and glucocorticoids - increases risk of gastric ulceration and GI bleeding
    • ACE inhibitors and angiotensin receptor blockers concurrent reduction in renal blood flow can lead to renal failure
  60. aspirin contraindication
    • children with influenza/viral illness- risk for reye's syndrome (hematic encephalopathy
    • pregnancy cat D;increased risk of bleeding and anemia; fetal grwth retardationd
    • severe renal disease
    • allergy- may worse asthma or contribute to nasal polyps in sensitive individuals.
  61. signs of salicylate toxicity
    • Metabolic acidosis
    • hyperventilation, tinnitus
    • nausea/vomitting
    • abdominal pain
    • sweating
    • renal impairment
  62. how does salicylate toxicity effect the body
    • it intefers with energy use for cellular ATP formation leadin to : hyperthermia
    • increased production of lactic and pyruvic acid
    • increased co2 production and respiratory acidosis
  63. treatment of aspirin toxicity
    • respiratory support
    • colling to treat hyperthermia
    • Iv hydration/sodium bicarb
    • hemodialys
  64. characteristics of Ibuprofen
    • Propionic Acid Derivative NSAID
    • Least likely to cause GI irretation/bleeding
  65. whart are the effects of ibuprofen (motrin/advil)
    • analgesi,
    • antipyretic
    • antiinflammatory effects
  66. what is ibuprofen used for
    • fever in adults and children
    • moderate to mild arthritis
  67. how is ibuprofen avalable
    PO, oral suspension or pediatric drop
  68. what is the max ibuprofen adults can take
  69. what is the effect of ibuprofen with long term use
    GI and renal toxicity with long term use or overdose
  70. drug interactions of ibuprofen
    can interfere with anti platelet activity of aspirin and increase CV risk
  71. What is Naproxin
    a propionic acid derivative ; that is higlhy cox 1 selective enzyme; some anti platelet effecs
  72. why is naproxen good
    it has a long half life
  73. what is naproxen used for
    • fever, arthritis
    • moderate pain
    • headaches,
    • dysmenorrhea
  74. adverse effects of naproxen (aleve/naprosyn)
    gi bleeding and renal failure
  75. what can be done to counter the bleeding effects of naproxen
    it can be conbined with proton pump inhibitor (lansaprazole) to reduce bleeding
  76. Ketorolac (toradol)
    parenteral NSAID - potent analgesia with limited anti inflammatory effect
  77. what is ketorolac used for
    for actue/postoperative pain expecially orthopedic or gynecological procedures.
  78. how is ketorolac (toradol ) given
    • IV push should be diluted with normal saline and given slowly to reduce vein irritation.
    • Deep IM in large muscle to reduce tissue irritation. Ztrack
  79. how long should ketorolac be used
    not longer than 5 days
  80. how is ketorolac administered post op
    with opioid agonist for better postoperative pain control.
  81. acetaminophen acts how
    • Centrally acting- inhibition of prostaglandin production primarily in CNS
    • less peripheral antiinflammatory effects than other NSAID
    • NO GI irritation
    • No iffect on renal blood flow or platelets
  82. what is acetaminophen use for
    • pain or fever, less effect on inflammatory or dysmenorrhea,
    • can be used in pediatric and pregnancy; safe for those who have aspirin allergy
  83. how is acetaminophen administered
    readily absorbed orally ; metabolized by the liver and excreted renally.
  84. adverse effects of acetaminophen
    few reduce doses with liver disease
  85. drug interaction of acetaminophen
    • alcohol no more than 3 drinks
    • anticoagulants- warfarin- bleeding risks
  86. symptom of acetaminophen overdose
    nausea/vomitting, abd pain, liver failure from toxic metabolite- metabolites injure liver tissue
  87. treatment of acetaminophen overdose
    • acetylcystein (mucomyst) po or IV to break down the toxic metabolite; start within 10 hrs of OD
    • Serever overdose require liver transplant
    • chronic overdose - bone marrow suppression
  88. what are opioid agonis most effective for
    • nocioceptive pain in soft tissue
    • not shapr neuropathic pain - since calcium channels in nerves are not effectively blocked by opioid binding
  89. how is nerve pain treated
    give higher dose opiod with adjuvant drugs
  90. morphine what is it
    opiod agonist
  91. how does morphine act in body
    bindst and activates endogenous opiate receptors, primarily mu receptors in CNS and peripheral tissue
  92. therapeutic use of morphine
    • for mederate to severe pain
    • relieves anxiety
    • antitussive
    • dilates pulmonary vasculatrue and relieves left ventricular heart failure. dyspnea and pulmonary edema in congestive hear failure and Mi
    • antidurrheal
  93. how is morphine given
    PO, MI, IV, SC, Ipidural and intrathecal routes
  94. how much morphine reaches CNS
    • small amount morphine is water soluble.
    • much of oral dose is loss in first pass. thus oral doses are larger
  95. how does liver disease effect morphine
    prolongs action
  96. how does morphine effect renal disease pt
    more neurotoxic effects including myoclonus (muscle jerks and confusion
  97. what are the caustions with morphine
    • respiratory disease
    • use of depressants
    • head injury
    • pregnancy and childbirth
    • hypotension
    • all blood trhough GI goes through liver
  98. how should sustained release morphine be given
    never crush because it causes overdose
  99. morphine adverse effects
    • sedation/rep depression
    • hypotension- histamine effects- itching, flushing, temporary flair reaction with undiluted IV admin
    • vomitting/nausea
    • urinary retention
    • pruritis/itching
    • constipation
    • pinpoint pupils
    • with morphine you have more histamine release
  100. physiologic tolerance
    when pure opiod agonist given for 2-3 weeks causes an increase in opioid receptor sites in the CNS
  101. what happen if opiod agonist are abruptly stoped
    • rhinorrea, goosebups
    • tremmors,
    • gi upset
    • diarrhea
    • irritability
    • anxiety
  102. what is addiction
    a state of ongoing drug craving with excalating use unrelated to pain control;
  103. what is hydromorphine (dilaudid)
    potent semi synthetic opioid agonist use as pare nteral alternative to morphine for moderate to severe acute pain
  104. how is hydromorphine useful
    • useful if tolerance is build to morphine or morphine is not tolerated
    • has less itching then morphiene
  105. adverse effects of hydromorphine
    similar to morphine
  106. what is fentanyl (sublimaze
    • very poten synthetic opioid receptor agonists acts mostly on mu receptors in the brain.
    • has rapid onset; short duration activity
    • lipid soluble so it crosses membranes
  107. what happen if fentanyl is given IV rapigly
    muscle rigidity occurs, laryng ospams if given with enzyme inhibitors they can increase drug concentrations
  108. what is the oral form called-
    oralet lollipop for anesthesia induction and breakthrough cancer pain.
  109. fenatanyl in body
    • higly lipid soluble
    • dose in micrograms
  110. transdermal fentanyl
    • cannot be cut
    • hyperthermia may increase rate of absorption
    • avoid heat on patch
    • decreased perfusion may impair absorption
  111. nursing implication with fentanyl
    • handle with gloves
    • apply to intact skin of upper trunk
    • rotate sites; date/time when applied
    • dispose of as biohazard
  112. Methadone (dolopphine) what is it used forn morphine

    • acts on mu and delta receptors in CNS
    • used primarily for treating opioid addiction adn chronic pain management. low cosst
    • less euphoria /dysphoria than morphine
    • long half life
  113. symptom of overdose
    late resp. depression and cardiac arrhythmias (prolonged QT interval) can occure
  114. codeine uses
    opioid agonis used for moderate pain or non productive cough
  115. hos is codeined metabolized
    metabolized in liver; genetic variation on metabolism
  116. what if patient has resp, renal or elderly hos is codeine given
    lower doses
  117. adverse effects of codeine
    • nausea /vomitting most frequent problem
    • it is effective in cough syrup
  118. oxycodone (roxicodone; oxycontin)
    • semi-synthetic opiod for moderate pian - analgesia equivalent to codeine
    • often combined with acetaminophen (percocet ) or apirin (percodan)
  119. how is oxycodone administered
    PO imediate release, long acting controlled relase
  120. adverse effects of oxycodone
    risk for acetaminophen/asmpirin toxicity in pts using high dose
  121. hydrocodone (vicodin /Lortab/vicoprofen)
    • most prescribed
    • semi synthetic opioid used for moderate pain and cough ; efficacy as that of codeine
  122. how is hydrocodone available
    combined with acetaminophen orally. does not need new written prescription each time dispensed.
  123. outpatient consideration with hydrocodone
    avoid driving, hydration, constipation, execessive NASAI.
  124. Pentaxocine (talwin
    • agonist/antagonist drug acts by activating kappa receptors in spinal cord and blocks mu recpeotr in the brain
    • less risk of resp depression since less activity on mu recpeotrs in brain
  125. what happen if high dose of pentazocine (talwin) is taken
    dysporia, nightmares, and anxiety from excessive kappa stimulation
  126. why should pentazocine should never be given with an opioid agonist
    opioid agonist and opioid agonist/antagonist should not be given together because the antagonist will block effectiveness of opioid agonist (agonist/antagonist- buprenorphine)
  127. Naloxone (narcan)
    opiod antagonist- blocks opiod receptors in opiod overdose.
  128. opiod overdose symptoms
    respiratory depression, sedation Miosis (constricted pupils)
  129. how is narcan administered
    IV. adminiter dilute in saline for IV give slowly assess for response.
  130. why should pt given naloxone for opiod overdose be monitored
    because naloxone will leave system before opoid and send pt back to rep depression
  131. what are adjuvent drugs good for
    • anticonvulsant
    • antidep
    • local anesthesia
  132. opioid adverse effecs
    • respiratory depression
    • Nausea/vomittin
    • orthostasi
    • urinary retention
    • itchin (pruritis)
    • constipation
  133. nursing assessment with opioid
    • assess pain
    • monitor resp/bp/pulse/sao2 prior to giving opioid
    • stop med if reps<12/min, encourage deep breathing get o2 order if needed
    • re assess client 30 minute after iv med or 1 hour po
    • use safety with ambulation
    • i and o breath sounds
    • abdomen for distention or nausea
  134. when to use narcan
    if resp <10 or physical stimulation insuficient.
  135. why nausea with opioids
    • due to receptor stimulation and GI motility
    • nausea and vomiting is most common with codeine
    • can premedicate with anti emetics initially
  136. what is orthostasis
    • hypotension associated wth vasodilation and histamine release
    • more severe with fluid deficit --IV and oral hydration help to minimize assess b/p before ambulation chage position slowly
    • monitor i and o.
  137. Urinary retension how to manage
    • due to increased tone of urinary sphincter and decreased awareness of bladder distention
    • is most sever with epidural/spinal admin
    • monitor i and o
    • catherter if neededo
    • often temporary
    • tr
  138. itching management and cause
    • antihistamine or a very dilute naloxone infusion may be used cool compresses/lotion;
    • swithc opiod
    • itching less frequent with hydromorphone (dilaudid)
  139. constipation management
    • opioids directly decrease GI peristalsis for as long as client are taking them.
    • give stool softener (docusate) and stimulant laxative (senna) often combined for treatment
    • lactulose may be added
    • fiber, fluids and activity helpful
  140. PRN analgesic what are they good for
    recurrent rather than acute pain.
  141. Intravenous PCA
    • used for acute postoperative trauma
    • morphine, fentanyl, hydromorphone are used
    • programable
    • patient activated for breakthrough dosing
    • use effectively age 8 and older
  142. nursing care with PCA
    • review physican order
    • establish iv access
    • obtain/;rogram pump
    • give loading dose and client teaching
    • assess resp
    • maintain Iv infusion to deliver drug doses
    • assess client ability to use effectively
    • document pain
    • cosign waste drug and when D/C'd
  143. epidural analgesia
    • used for lower extremeties surgery, childbrith refracory or other therapy
    • catherter place in epidural spac outside dural covering of spine
    • small doses of opiod and or local anesthetis diffuse across dura and bind to opiate receptors in spinal nerve
  144. advantage of epidural analgesia
    • less CNS and respiratroy depressant effects than IV route since lower boses
    • small risk for bleeding if client anticoagulate with epidural placemtn
  145. nursing implication in epidual analgesia
    • monitor respiratory rate, depth and level of sedation hourly
    • vital sign q 4 hours
    • assess pain
    • assess dressing for drainage q shift
    • asses catherter for dislodgement q shift
    • assess sensation/stength of lower extremites if local anesthetic used in infusion.