Drugs for Pain & HA.docx - Opioids Mu receptors activation includes analgesia respiratory depression euphoria and sedation Kappa receptors produces

Drugs for Pain & HA.docx - Opioids Mu receptors activation...

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Opioids Mu receptors : activation includes analgesia, respiratory depression, euphoria and sedation Kappa receptors : produces analgesia, sedation, and respiratory depression Pure Opioid Agonists : activate Mu and Kappa receptors, product analgesia, euphoria, sedation, respiratory depression, physical dependence, constipation Two subgroups Strong opioid agonists: morphine Moderate to strong opioid agonist: codeine oxycodone, hydrocodone, Agonist-Antagonist Opioids : when administered alone they produce analgesia, in combination with pure opioid agonist they can antagonize analgesia caused by the pure agonist Ex: Pentazocine (Talwin), butorphanol, buprenorphine Pure Opioid Antagonist: acts as an antagonist to Mu and Kappa receptors, used for reversal of CNS depression Ex: Naloxone (Narcan) Opioid Agonists Morphine : pure opioid agonists, used for moderate to severe pain Adverse Effects Respiratory depression Constipation Orthostatic Hypotension Urinary retention Emesis Euphoria and dysphoria Sedation Neurotoxicity Precautions Give sparingly with pts with impaired pulmonary function (asthma, emphysema, kyphoscoliosis, chronic cor pulmonale, extreme obesity) With other respiratory depressant drugs Pt with inflammatory bowel disease can cause toxic megacolon or paralytic ileus Could be intensified in pts with liver impairment Pt with BPH could have urinary retention Infants and older adults are more prone to respiratory depression Pt with hypotension and reduced blood volume Toxicity: coma, respiratory depression, pinpoint pupils
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Fentanyl: (Duragesic) strong opioid agonist, 100x more potent than morphine Routes: parental transdermal: change patch q72h, do not exposure to heat, not to be used for post-op pain transmucosal: approved only for breakthrough pain in pts with CA at least 18 yeas old who already take opioids around the clock and have tolerance intranasal Adverse effects: same as morphine, but greatest concern is respiratory depression -levels can be increased by CYP34A inhibitors (ritonavir & ketoconazole) Hydromorphone : (diladid) strong opioid agonist -less N/V than morphine Routes IR, ER, Oral Suppositories Oxymorphone : (Opana) strong opioid agonist, can cause less N/V than morphine Routes IR, 2mg q4-6h ER Oral Suppositories Codeine : moderate to strong opioid agonist, also used as a cough suppressant, acts on Mu receptors -schedule II alone but schedule III when combined with other drugs -only available in tablets Hydrocodone: Equivalent to codeine, indicated for moderate to severe pain and cough suppression -Schedule 2 drug, can be reversed with naloxone. - IR 5mg tablet, can be combined with Acetaminophen or Ibuprofen (Norco, Vicodin, Lortab). ER every 12-24hours.
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  • Spring '14
  • AnnMaradiegue

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