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Barry Basics Opiod Slides

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OPIOIDS   show
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TYPES OF OPIOIDS   show
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show Morphine and Papaverine: Derived from opium, an extract of the poppy plant.  
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SEMI SYNTHETIC OPIOIDS   show
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show Demerol, Methadone, Fentanyl, Butorphanol, Pentazocine: Manufactured by synthesis rather than chemical modification of morphine.  
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CLASSIFICATIONS OF OPIOIDS   show
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show Capable of eliciting full agonist (morphine-like) effects  
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AGONIST-ANTAGONISTS   show
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show Competitive: binds to receptor but can be knocked off if a higher concentration of the agonist is present.Non-competitive: Very strong affinity for receptor. NOT DISPLACED by high concentrations of the agonist.  
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MOA   show
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show The actions of endogenous ligands (endorphins, enkephalins and dynorphins) by binding to the opioid receptor which activates pain modulating systems.  
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show By activating postsynaptic opioid receptors in the midbrain and medulla (results in inhibition of pain pathways.  
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HOW DO OPIOIDS CAUSE SPINAL ANALGESIA?   show
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HOW DO OPIOIDS CAUSE PERIPHERAL ANALGESIA?   show
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OPIOID RECEPTORS   show
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show Primarily supraspinal analgesiaSome spinal analgesiaEuphoriaMiosisUrinary retention  
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MU-2 RECEPTORS   show
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show Spinal and supraspinal analgesiaSedationDysphoria (psychosis)  
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show Mostly spinal analgesiaSome supraspinal analgesiaSome respiratory depressionPhysical dependence  
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show Dose-dependent ventilatory depression (decreased RR with compensatory increased TV)Not reliable at producing LOC: some sedation,but main effect is analgesia.May stimulate chemoreceptor trigger zone.Cause spasm of biliary smooth muscle.  
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HOW IS BILIARY SMOOTH MUSCLE SPASM TREATED?   show
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show The Prototype: E 1/2 time is 1.5-3hrs.Doseages: Intra-op- 0.1-1 mg/kg IV Post-op- .05-0.2mg/kg IV .03-0.15 mg/kg IV  
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WHAT IS THE MAJOR FEATURE OF MORPHINE?   show
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WHAT ARE THE ACTIVE METABOLITES OF MORPHINE?   show
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HOW IS MORPHINE METABOLIZED?   show
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show Pharmacokinetic profile similar to morphine.8-10X more potent than morphine.Similar SE profile (less n/v, itching, and dysphoria).No active metabolite.  
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MEPERIDINE   show
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WHICH OPIOID IS GIVEN IN PACU FOR SHIVERING?   show
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WHAT IS THE METABOLITE OF MEPERIDINE?   show
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show Meperidine:Causes a severe excitatory state: signs and symptoms include: Increase in HR, BP and Temp. Delerium, seizures and possible death.  
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show Structurally related to meperidine.100x more potent than morphine.E 1/2 time: 3-6 hours.Doseages: Intra-op- 2-10 mcg/kg. CT surgery- 30-50 mcg/kg. Post-op-0.5-1.5 mcg/kg.Minimal CV depression: may decrease HR.1cc = 50 mcg.  
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WHICH OPIOID CAUSES CHEST WALL RIGIDITY?   show
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show 7-10x more potent than fentanyl.Intra-op dose: 0.2-0.8 mcg/kgCT surgery: 10-30 mcg/kgE 1/2 time: 2.5-3.5 hours  
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show 1/5-1/10 As potent as fentanyl.Intra-op dose: 10-100 mcg/kgE 1/2 time: 1.5 hrs.More rapid onset and shorter duration of action then fentanyl and sufentanyl.  
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show Similar potency as fentanyl.Extremely rapid onset, clearance and recovery.E 1/2 time: 15-30 min.Dose: 1 mcg/kg IV over 60-90sec then 0.25-1mcg/kg or 0.05mcg/kg/min.  
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HOW IS REMIFENTANYL METABOLIZED?   show
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WHAT ARE THE OPIOID ANTAGONISTS?   show
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show Also known as Narcan.Most frequently used.Great affinity for Mu receptors and is a competitive antagonist.Used to reverse unconciousness from narcotic overdose.Reverses respiratory depression: give in 20-40mcg increments.  
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HOW LONG DOES NARCAN LAST?   show
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show Mix 1 amp (0.4mg) in 9cc of NS. Give one cc at at a time (20 mcg).  
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WHAT HAPPENS WITH ABRUPT REVERSAL OF OPIOIDS?   show
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show Also known as Trexan.Longer acting anatagonist given in PO form for addicts.May last up to 24 hoursPatients who take this may have a temporary resistance to narcotics.  
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show Butorphanol (Stadol)Nalbuphine (Nubain)  
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BUTORPHANOL   show
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NALBUPHINE   show
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show Nubain (nalbuphine)  
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WHAT IS FLUMAZENIL?   show
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