In each blank, try to type in the
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If your not sure what answer should be entered, press the space bar and the next missing letter will be displayed. When you are all done, you should look back over all your answers and review the ones in red. These ones in red are the ones which you needed help on. Question: Answer: Exogenous substances that specifically bind to several sub-populations of opioid receptors and produce agonist (morphine like) effects.Used during induction to decrease sympathetic to laryngoscopy and during maitenance and post-op for analgesia. Question: TYPES OF Answer: occurringSemi syntheticSynthetic Question: NATURALLY OPIOIDSAnswer: Morphine and Papaverine: Derived from opium, an extract of the plant. Question: SEMI SYNTHETIC Answer: , Hydrmorphone, Thebain (not used by itself - is a precursor for oxycodone and oxymorphone): Result from simple modifications of the morphine molecule. Question: OPIOIDSAnswer: Demerol, Methadone, Fentanyl, Butorphanol, Pentazocine: Manufactured by synthesis rather than chemical of morphine. Question: OF OPIOIDSAnswer: -antagonistsAntagonists (Competitive and Non-competitive) Question: AGONISTSAnswer: Capable of eliciting full agonist (morphine-like) Question: -ANTAGONISTSAnswer: Bind to Mu receptors and produce limited responses (partial agonist) or no effect (competitive antagonist) But.....may also have effects at other receptors. Question: Answer: Competitive: binds to receptor but can be knocked off if a higher concentration of the is present.Non-competitive: Very strong affinity for receptor. NOT DISPLACED by high concentrations of the agonist. Question: Answer: Bind at receptors to block transmission of pain.Receptors in dorsal horn of cord, the brain (supraspinal), and peripheral tissue.Receptors endogenously activated by: endorphins, enkephalins and dynorphins. Question: WHAT DO MIMIC?Answer: The actions of endogenous ligands (endorphins, enkephalins and ) by binding to the opioid receptor which activates pain modulating systems. Question: HOW DO OPIOIDS CAUSE SUPRASPINAL ?Answer: By activating postsynaptic receptors in the midbrain and medulla (results in inhibition of pain pathways. Question: HOW DO OPIOIDS CAUSE ANALGESIA?Answer: By activating presynaptic opioid (results in decreased release of neurotransmitters involved with nociception). Question: HOW DO OPIOIDS CAUSE ANALGESIA?Answer: By activating receptors on primary afferent neurons (antinociceptive activity). Question: RECEPTORSAnswer: Discovered: Early 1970'sConstantly revised: intitially thought to be Mu, Kappa and Sigma, NOW Mu, Delta and Kappa which have many subtypes.Each receptor has a different .Desired effects come mostly from action at Mu receptors. Question: MU-1 Answer: Primarily supraspinal analgesiaSome analgesiaEuphoriaMiosisUrinary retention Question: MU-2 Answer: spinal analgesiaRespiratory depressionBradycardiaPhysical dependenceConstipation N/VItching Question: RECEPTORSAnswer: Spinal and analgesiaSedationDysphoria (psychosis) Question: RECEPTORSAnswer: Mostly analgesiaSome supraspinal analgesiaSome respiratory depressionPhysical dependence Question: COMMON TO ALL OPIOIDS.Answer: Dose-dependent ventilatory (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. Question: HOW IS BILIARY SMOOTH MUSCLE SPASM ?Answer: , Atropine,Naloxone,Glucagon,and Benadryl (?) Question: Answer: 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 Question: WHAT IS THE FEATURE OF MORPHINE?Answer: release!Signs and symptoms: local redness, itching and hives. Decreased BP and Increased HR and flushing.Slow administration reduces this risk! Question: WHAT ARE THE METABOLITES OF MORPHINE?Answer: Morphine 3-glucuronideMorphine 6-glucuronideMorphine 6-glucuronide is a more and longer acting agonist than morphine! Question: HOW IS METABOLIZED?Answer: It biotransformation in the liver.Excreted by the kidneys (problem for pts. who have renal dx.) Question: HYDROMORPHONEAnswer: Pharmacokinetic profile similar to morphine.8-10X more potent than morphine.Similar SE profile (less n/v, , and dysphoria).No active metabolite. Question: Answer: 1st synthetic opioid.1/10 the potency of morphine.E 1/2 time: 3-5hrsDose: 0.5-1 mg/kg IM and 0.2-0.5 mg/kg : Similar to atropine. Increases HR, Mydiasis (eyes dilate) and dry mouth. Question: WHICH OPIOID IS GIVEN IN PACU FOR ?Answer: Meperidine: Mechanism is unclear, but it is believed that meperidine stimulates the kappa receptors decreases the shivering threshold. Is an agonist at alpha-2 receptors. Question: WHAT IS THE OF MEPERIDINE?Answer: : Excreted by the kidneys. Is neurotoxic at high concentrations causing myoclonus and seizures. Question: WHICH OPIOID IS UNSAFE TO GIVE TO ON MAOI'S LIKE NARDIL?Answer: :Causes a severe excitatory state: signs and symptoms include: Increase in HR, BP and Temp. Delerium, seizures and possible death. Question: Answer: 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 HR.1cc = 50 mcg. Question: OPIOID CAUSES CHEST WALL RIGIDITY?Answer: Question: SUFENTANYLAnswer: 7-10x more potent than fentanyl.Intra-op dose: 0.2-0.8 mcg/kgCT : 10-30 mcg/kgE 1/2 time: 2.5-3.5 hours Question: ALFENTANYLAnswer: 1/5-1/10 As 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. Question: REMIFENTANYLAnswer: Similar potency as fentanyl.Extremely rapid onset, 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. Question: HOW IS REMIFENTANYL ?Answer: By non-specific plasma and esterases. Question: WHAT ARE THE ANTAGONISTS?Answer: Naloxone and Question: NALOXONEAnswer: Also known as Narcan.Most frequently used.Great affinity for Mu receptors and is a competitive .Used to reverse unconciousness from narcotic overdose.Reverses respiratory depression: give in 20-40mcg increments. Question: HOW LONG DOES LAST?Answer: Peaks in 1-2 min and lasts 30-45 min.May redosing. Question: HOW IS MIXED?Answer: Mix 1 amp (0.4mg) in 9cc of NS. Give one cc at at a time (20 mcg). Question: WHAT HAPPENS WITH REVERSAL OF OPIOIDS?Answer: Execessive sympathetic stimulation!Arrythmias, Inc HR, Inc BP, N/V, and edema. Question: NALTREXONEAnswer: Also known as Trexan.Longer acting anatagonist given in PO form for .May last up to 24 hoursPatients who take this may have a temporary resistance to narcotics. Question: WHAT ARE THE AGONISTS-ANTAGONISTS (PARTIAL-AGONISTS)?Answer: (Stadol)Nalbuphine (Nubain) Question: Answer: Partial AgonistProduces analgesia and respiratory depression similar to 10mg of .More sedation than Nubain.Incidence of dysphoris is low.Does not increase biliary pressure.Can be used to tx post-op shivering.Dose: 0.5-3mg IV. Question: Answer: Partial agonist at kappa and Mu recceptors.Like morphine analgesia.Less sedative than Stadol.Will reverse respiratory depression but not analgesia.Used for from morphineCan be given IV or IMDose: 5-10mgCan cause withdr Question: WHICH PARTIAL AGONIST WITHDRAWL IN ADDICTS?Answer: (nalbuphine) Question: WHAT IS ?Answer: A BENZODIAZEPINE ANTAGONIST!!!!! (competitive)Reversal can be total or , depends on dose.High affinity for Benzo receptors but minimal intrinsic activity.Dose: usually 0.2mg increments titrated to effect. Not to exceed 1mg. |
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