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Basics Opioid Slides Test

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1.
OPIOID RECEPTORS
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2.
WHAT DO OPIOIDS MIMIC?
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3.
WHAT HAPPENS WITH ABRUPT REVERSAL OF OPIOIDS?
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4.
WHICH PARTIAL AGONIST CAUSES WITHDRAWL IN ADDICTS?
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DELTA RECEPTORS
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CHARACTERISTICS COMMON TO ALL OPIOIDS.
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NALTREXONE
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SYNTHETIC OPIOIDS
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9.
FENTANYL
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10.
HOW IS MORPHINE METABOLIZED?
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WHICH OPIOID IS GIVEN IN PACU FOR SHIVERING?
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SUFENTANYL
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AGONIST-ANTAGONISTS
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HOW DO OPIOIDS CAUSE PERIPHERAL ANALGESIA?
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MEPERIDINE
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REMIFENTANYL
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NALOXONE
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WHAT IS THE MAJOR FEATURE OF MORPHINE?
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NALBUPHINE
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CLASSIFICATIONS OF OPIOIDS
A.
Partial agonist at kappa and Mu recceptors.Like morphine analgesia.Less sedative than Stadol.Will reverse respiratory depression but not analgesia.Used for itching from morphineCan be given IV or IMDose: 5-10mgCan cause withdr
B.
Histamine release!Signs and symptoms: local redness, itching and hives. Decreased BP and Increased HR and flushing.Slow administration reduces this risk!
C.
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 IVStructure: Similar to atropine. Increases HR, Mydiasis (eyes dilate) and dry mouth.
D.
Bind to Mu receptors and produce limited responses (partial agonist) or no effect (competitive antagonist) But.....may also have agonist effects at other receptors.
E.
It undergoes biotransformation in the liver.Excreted by the kidneys (problem for pts. who have renal dx.)
F.
Nubain (nalbuphine)
G.
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.
H.
By activating opioid receptors on primary afferent neurons (antinociceptive activity).
I.
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
J.
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 function.Desired effects come mostly from action at Mu receptors.
K.
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.
L.
Mostly spinal analgesiaSome supraspinal analgesiaSome respiratory depressionPhysical dependence
M.
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.
N.
Execessive sympathetic stimulation!Arrythmias, Inc HR, Inc BP, N/V, and Pulmonary edema.
O.
The actions of endogenous ligands (endorphins, enkephalins and dynorphins) by binding to the opioid receptor which activates pain modulating systems.
P.
Demerol, Methadone, Fentanyl, Butorphanol, Pentazocine: Manufactured by synthesis rather than chemical modification of morphine.
Q.
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.
R.
Meperidine: Mechanism is unclear, but it is believed that meperidine stimulates the kappa receptors which decreases the shivering threshold. Is an agonist at alpha-2 receptors.
S.
AgonistsAgonist-antagonistsAntagonists (Competitive and Non-competitive)
T.
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.
Type the Answer that corresponds to the displayed Question.
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21.
WHICH OPIOID CAUSES CHEST WALL RIGIDITY?
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22.
WHAT ARE THE OPIOID ANTAGONISTS?
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23.
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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24.
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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Partial AgonistProduces analgesia and respiratory depression similar to 10mg of morphine.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.
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Heroin, Hydrmorphone, Thebain (not used by itself - is a precursor for oxycodone and oxymorphone): Result from simple modifications of the morphine molecule.
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Primarily spinal analgesiaRespiratory depressionBradycardiaPhysical dependenceConstipation N/VItching
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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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29.
A BENZODIAZEPINE ANTAGONIST!!!!! (competitive)Reversal can be total or partial, 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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30.
Naturally occurringSemi syntheticSynthetic

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