Barry Opioids Study
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| What is an Opiate | derived from opium
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| What is an opioid | natural or synthetic substance that binds to opioid receptors and possess agonist activity
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| Why are opioids used in anesthesia | to decrease the SNS response to laryngoscopy, and for analgesia
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| What are the 3 types of opioids | natral, semi-synthetic and synthetic
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| Natural opioids | morphine and papaverine
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| Semi-synthetic | result from simple modifications to the morphine molecule, heroin, hydromorphone, thebaine
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| Synthetic | Demerol, methadone, su-al-remi-fentanyl
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| Opioid mech. Of action | opioid receptor agonists
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| Where are opioid receptors found | the brain (activation of post-synaptic opiod receptors in midbrain and medulla), dorsal horn of spinal cord(activation of presynaptic opiods receptors), and peripheral tissues (activation of receptors in afferent neurons)
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| What are endogenous opioid receptor agonists | endorphins, enkephalins, dynorphins
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| Opioid receptors | mu 1& mu 2, delta, kappa
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| Mu-1 location and effects | primarily brain(supraspinal), euphoria, miosis, urinary retention
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| Mu-2 location and effects | primarily spinal, resp. depression, bradycardia, physical dependence, constipation, itching
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| Kappa location and effects | spinal, supraspinal, peripheral; sedation, dysphoria
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| Delta location and effects | primarily spinal, resp depression, physical dependence
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| Opioid effects | dose dep. resp depression, do not reliably produce unconsciousness, stimulation of chemo-trigger zone (N/V), biliary smooth muscle spasm
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| Morphine (MSO4) dose, side effects, metabolism | dose intra-op: 0.1-1mg/kg IV, post-op: 0.05- 0.2mg/kg IM or 0.03-0.15 mg/kg IV (2-10mg); Major histamine release(avoid in severe asthma), broken down in liver into Morphine 3-glucuronide and Morphine 6-glucuronide.
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| What is Morphine 6-glucuronide | active metabolite of morphine (more potent and stays longer in renal pt)
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| What is the E ½ time of morphine | 1.5-3 hrs (for 50% of morphine to clear the plasma)
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| Hydromorphone dose, side effects, metabolism | 10x more potent than morphine; 0.2-1mg IV, (less N/V, itching, dysphoria), broken down to non-active metabolite Hydromorphone 3-glucuronide(may cause excitation)
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| Meperidine dose, side effects, metabolism | (Demerol) 1/10th as potent as morphine; 0.5-1mg/kg IM, 0.2-0.5 mg/kg IV (14-35 mg); structurally similar to atropine: increases HR, mydriasis, dry mouth; broken down into normeperidine, excreted by kidneys, and neurotoxic in high [] (seizures, myoclonus)
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| Meperidine is used post-op for this | to decrease shivering
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| What is the E ½ time of meperidine | 3-5 hrs (for 50% of meperidine to clear the plasma)
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| Do not given Meperidine to pts on MAOIs (nardil) | causes severe excitatory state, incr. HR, B/P, temp, seizures
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| Fentanyl dose, side effects | 100x more potent than morphine, dose intra-op: 2-10mcg/kg, CT surg:30-50mcg/kg, Post-op: 0.5-1.5mcg/kg; minimal CV side effects, decrease HR, chest wall rigidity (tx with NMB)
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| Fentanyl is always in what concentration | 50mcg/ml
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| What is the E ½ time of fentanyl | 3-6 hrs (for 50% of fentanyl to clear the plasma)
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| Sufentanyl dosage | 7-10x more potent than fentanyl , dose intra-op: 0.2-0.8 mcg/kg, CT surg: 10-30mcg/kg
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| What is the E ½ time of sufentanyl | 2-4 hrs (for 50% of sufentanyl to clear the plasma)
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| Alfentanyl dose, onset | 1/10th as potent as fentanyl, intra-op dose:10-100mcg/kg, faster onset shorter duration than fent or sufent.
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| What is the E ½ time of Alfentanyl | 1.5 hrs (for 50% of Alfentanyl to clear the plasma)
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| Remifentanyl dose, onset | same potency as fent., extremely rapid onset and recovery, dose: 1mcg/kg IV, dose infusion: 0.05-2mcg/kg/min
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| What is the E ½ time of Remifentanyl | 15-30min (for 50% of Remifentanyl to clear the plasma), no analgesia once infusion is stopped.
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| Naloxone dose, side effects, mech. of action, onset, duration | incremental dose: 0.02mg-0.04mg IV, (Mix narcan 0.4mg/ml in 9ml saline=0.04mg/ml) give in 1cc increments, in this dose it reverses resp. dep.but maintains analgesia; opioid receptor competitive antagonist; Onset 1-2min, duration 30-45min
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| Abrupt reversal with large doses of narcan can cause | increased HR, B/P, N/V, pulm, edema
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| Naltrexone | (trexan), longer acting (upto 24 hrs), given PO
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| What are 2 common opioid agonists/antagonists | Butorphanol (stadol), Nalbuphine (nubain)
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| Butorphanol dose, side effects | (Stadol) dose : 0.5-3mg IV, causes resp. dep. and analgesia similar to 10mg MSO4, more sedation than nalbuphine(nubaine)
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| Butorphanol (Stadol) can be used to stop | post-op shivering
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| Nalbuphine dose, side effects | (nubain) partial agonist at kappa and mu, dose: 5-10mg IV, reverses resp. depression caused by narcotics,but maintains analgesia; antagonizes itching from epidural and intrathecal MSO4
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| Nalbupine is contraindicated in | pts addicted to opioids (do not give to them)
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| Flumazenil dose, side effects | (Romazicon), benzo antagonist, dosed incrementally: 0.2mg IV up to 1mg, reverses effects of benzos, but effect does not last as long as benzo effect
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