Opioids Flashcards

Question

Fentanyl in your epidural

Answer 1

makes a denser block 2 mechs of action LA; block transmission via VGNaC opioid activity on Mu receptors but mostly Mu2 [[ spinal analgesia; M2]]

Answer 2

opioids work on G alpha i opioid receptors G alpha i decreased cAMP increases K conductance [[hyperpolarizes]] increased K out of the cell hyper polarizes the cell and inhibits VGCa and decreases Ca into the cell *when you have pain Ca is sent into the cell and releases NT [[substance P]] signals pain by increasing K conductance and hyperpolarizing the cell it decreasing Ca into cell and decrease the release of pain NT decreasing nociceptive [[pain]] receptor activity

Answer 3

Direct; directly decreases neurotransmission [[decreases Ca into cell]] inhibits the release of excitatory NT [[substance P]]

Answer 4

higher % not protein bound higher % unionized ^faster onset of action all opioids are weak bases B + B = nonionized! B + A = ionized [[pt is acidotic pH under 7.35; will need a larger dose; more ionized]] only unionized and not protein bound can diffuse

Answer 5

Sufentanil 20% nonionized 93% protein bound NOT Highly nonionized and highly protein bound [[would think it would be a weaker; slow onset]] BUT 1000x stronger than morphine VERY diffuse-able [[partition coeff. 1727]] *attributed to molecule size/ structure

Answer 6

most potent to least Sufentanil Remifentanil Fentanyl Alfentanil Dilaudid Morphine Demerol more potent; smaller dose

Answer 7

Age -neonates; give less [[decrease rate of elimination; bc immature CYP 450]] -elderly; give less [[weaker BBB]] Weight dose based on ideal body weight [[not actual]] Renal Failure decrease dose Hepatic failure decrease dose ^both kidney and liver failure will effect metabolism and elimination oof opioid DECREASE DOSE

Answer 8

analgesia produces by receptor activation in the spinal cord and dorsal root ganglion pain [[sensory; afferent; approaching; dorsal root ganglion to the dorsal horn of gray matter --> laminae II and III]] pain signals synapses in the substantial gelatenosa [[laminae II & III]] Direct stimulation of these receptors produces intense analgesia [[pain relief]] how? Gi; decrease cAMP; increase K conductance; decrease Ca into cell decrease/ inhibit release of substance P [[pain NT]]; decreases activity at nociceptive [[pain]] receptors Mu2 and kappa and delta

Answer 9

analgesia produced by receptor activation in the BRAIN [[periaquaductal/ periventricular gray matter]] Mu1 and kappa and delta

Answer 10

more lipophilic drug will go right into venous system and you'll have an immediate response; less lipophilic delayed response less lipophilic drug more CEPHALAD movement; doesn't diffuse right away so travels up less lipophilic drug more cephalic movement Morphine more cephalic movement than Fentanyl

Answer 11

Analgesia Euphoria Sedation; Drowsiness/ sleepy respiratory depression miosis nausea [[direct via chemoreceptors; indirect via GI]] decrease in CBF and ICP [[modest]] ****NO AMNESIA or ANESTHESIA [[big doses in cardiac OR can get anesthesia but NO amnesia --> give Benzes or gases

Answer 12

ALL dose dependent no impairment of CV function -dose dependent Bradycarid

Answer 13

ALL dose dependent no impairment of CV function -dose dependent Bradycardia decreases workload and increases supply; decreases demand [[except DEMEROL; tachycardia]] - vasodilation - decrease CO and BP

Answer 14

Meperidine [[DEMEROL]] tachycardia demerol structure similar to atropine; antimuscarininc effects

Answer 15

Meperidine [[DEMEROL]] tachycardia and DIRECT myocardial depression demerol structure similar to atropine; antimuscarininc effects

Answer 16

Morphine and Nitrous **not with morphine alone

Answer 17

dose dependent respiratory depression [[give more; more depression]] **drop RR but increase TV [[slower deeper breaths]] hypoxia and hypercarbia [[lower RR blowing off less C02]] decrease chest wall compliance; muscle rigidity [[think fent--> right chest]] constricts pharyngeal and laryngeal muscles

Answer 18

decrease RR increase TV decrease hypoxic ventilation drive [[normal person its ok, C02 level is drive to breath; can become a problem in COPD patient]] ventilatory response curve is shifted the the R [[takes more C02 two get brain to breath; when waking pt up let C02 level rise; will need much higher C02 level to start breathing r/t opioids]]

Answer 19

Peak of respiratory depression is slower with morphine than with Fentanyl respiratory depression with morphine lasts longer than with fentanyl Why? bc fentanyl is more lipophilic respiratory depression right away [[give morphine 30 min before bringing pat to pacu fentanyl you can give 5 min before bringing them to pacu]]

Answer 20

larger opioid dose synergistic effect [[opioid given with other anesthetic]] *speed of injection continuous vs intermittent injection decreased clearance liver and kidney failure pt alkalosis B + B = more nonionized more crosses BBB age lower does in babies; immature CYP 450 lower dose in elderly; weaker BBB secondary peak in plasma level from reuptake of opioid in muscle, fat, lungs and intestine [[fentanyl first pass pulmonary; sits in lungs and comes back for second peak]]

Answer 21

Skeletal muscle rigidity ^makes ventilation difficult and sometimes impossible [[decrease chest wall compliance]] *give some muscle relaxant - laryngeal muscle - inhibition of GABA - increase in dopamine

Answer 22

increased peristaltic tone of ureters [[Mu1, kappa and delta receptor activity cause s urinary retention; now they also have a sense of urgency]] **blocked catecholamine release and cortisol [[reduced stress response during surgery]] spasm of sphincter of oddi [[spinchter between GI and gallbladder]] constipation; decreased GI motility [[Mu2, kappa and delta receptor activity]] prolonged gastric emptying [[indirect effect of Nausea]] Nausea direct effect --> chemoreceptors

Answer 23

GLUCAGON | -reverses the spasm

Answer 24

'fentanyl nose itch' cause unknown histamine release with demerol and morphine can cause the itch occurs mostly on face and nose

Answer 25

Morphine Demerol

Answer 26

opioids placed in epidural space can undergo uptake into - fat - systemic absorption - diffusion into CSF *diffusion into CSF depends on lipid solubility [[just like all diffusion]] more lipid soluble drug faster diffusion into CSF; quicker peak CSF concentration more lipid soluble less cephalad movement bc diffuses into CSF so quickly less lipid soluble more cephalad movement bc doesn't diffuse into CSF as quickly morphine more cephalad movement than fentanyl [[more less lipid soluble than morphine]]

Answer 27

-purities 'fentanyl nose itch' -N/V [[direct via chemoreceptors indirect via prolonged gastic emptying GI]] -urinary retention -ventilatory depression [[more rapid with lipophilic agents]]

Answer 28

more pronounced in less lipophilic drugs

Answer 29

natural occurring; endogenous ``` poorly lipid soluble; highly ionized and protein bound 23% nonionized 35% protein bound 1 potency E1/2 t 1.7 - 3.3 hours [[DOA 4 hours]] ``` Histamine Releaser Active metabolite Morphine-6-glucuronide IM peak effect 45 min IV effect 15-30 min effects; analgesia euphoria sedation nausea purities dry mouth ventilatory depression [[slower effect than fentanyl]] Bradycardia [[direct effect of vagus and inhibition of SA node]] metabolized by the liver kidneys --> extra hepatic metabolism or morphine Renal Failure don't give morphine

Answer 30

Morphine-6-glucuronide | ** active metabolite stronger than morphine

Answer 31

DIRECT effect of the vagus nerve and inhibition of SA node

Answer 32

RENAL FAILURE

Answer 33

synthetic [[exogenous]] -Phenylpiperdine Only Opioid with DIRECT cardiac depressant effects ACTVIE metabolite; normeperidine ^lasts ups to 3 days [[can cause seizures]] only 1/2 as potent as meperidine structurally similar to atropine [[exhibits anti-muscarinis effects]] blocks VGNaC [[like Locals]] potent alpha 2 receptors agonist [[calms patient; sedation]] ``` 1/10th as potent as morphine 7% nonionized 70% Protein bound E1/2t 3-5 hours [[DOA 2-4]] ``` produces the same amount of euphoria, sedation and analgesia as morphine; but 1/10th as potent used to treat post shivering [[kappa and alpha 2 receptor activity]]

Answer 34

DIRECT cardiac depressant activity

Answer 35

normeperidine lasts up to 3 days but only half as potent as meperidine long duration of active metabolite can cause seizures

Answer 36

treats post op shivering [[activity on kappa and alpha2]]

Answer 37

Seizure patient active metabolite hangs around a long time [[risk for seizures]]

Answer 38

Semisynthetic; analog [[derived]] from morphine 5 potency [[5 x as potent as morphine]] DOA [[4 hours]] need q 4 hour dosing rapid elimination and redistribution more sedation less euphoria ^compared to morphine

Answer 39

synthetic [[exogenous]] -Phenylpiperdine ``` more lipid soluble than morphine *faster onset 100 potency [[100 x more potent than morphine]] 8.5% nonionized 84% protein bound ``` shorter DOA than morphine [[but DOA can be longer with multiple doses or infusion]] Very CV stable [[hemodynamic stability]] **good for helping with HR and BP changes with intubation 75% of initial dose undergoes first pass pulmonary uptake into the lungs rapid redistribution to inactive tissue; fat muscles lungs multiple IV doses OR continuous IV infusion can SATURATE inactive tissue **shut off infusion 45 min- 1 hour before case ends plasma concentration DOES NOT decrease rapidly DOA is prolonged [[2nd peak plasma concentration]]

Answer 40

75 % of initial dose undergoes first pass pulmonary uptake plasma concentration does NOT decrease rapidly and DOA is prolonged ^2nd peak plasma concentration large Vd because more lipid soluble

Answer 41

75% of initial dose goes to the lungs [[inactive tissue]] then mobilized from lung can saturate your reserve [[accumulate in the lungs]] with multiple doses or continuous infusion DOA can be prolonged from this second peak **turn infusion off 45 min -1 hour before the case

Answer 42

PAIN analgesia adjunct for surgery Blunts stimulation of incision; intubation [[prevent the SNS response]] very CV stable [[large dose can be sole anesthetic]] wide range of doses 1 - 20mcg/kg cardiac can be 50 mcg/kg *fentanyl lollipop for pediatrics 5-20 mcg/kg *45 min prior to induction

Answer 43

Syntheic [[exogenous]] -Phenylpiperdine --Fentanyl Analog [[also undergoes first pass pulmonary effect]] --CV stable [[like fentanyl]] [[helps decrease SNS stem with intubation/ incision]] **most potent 1000 x more potent than morphine and 10 x more potent than fentanyl 2x more lipid soluble than Fentanyl 20% nonionized Highly protein bound 93% ACTIVE metabolite; Desmethylsufentanil rapidly metabolized by the liver E1/2t 2 - 5 hours

Answer 44

desmethylsufentanil | **weak

Answer 45

adjunct for surgery and induction used as infusion for OUTpatient surgery *turn off 30 min before; as opposed to 45- 60 with fentanyl [[QUICK on QUICK off]] compared to morphine and fentanyl; produces quicker induction earlier emergence earlier extubation

Answer 46

synthetic [[exogenous]] --Phenylpiperdine --Fentanyl Analog [[blunt SNS stim]] 10 - 20 x more potent than morphine 1/5th as potent as fentanyl RAPID onset [[1.4 min]] 89-90% in nonionized state fent [[6.8 min]] sufentanil [[6.2 min]] Highly protein bound 92% *even though more protein bound than fentanyl; greater diffusion than fentanyl

Answer 47

RAPID onset [[1.4 min]] 90% nonionized useful for blunting hemodynamic responser to noxious stim [[intubation; incision]] used for infusion in OUTpatient surgery

Answer 48

synthetic [[exogenous]] - -Phenylpiperdine - -chemically similar to fentanyl * *unique r/t ester linkage 100 x more potent than morphine [[slightly more potent than fentanyl]] -metabolized by tissue/ plasma esterase - rapid onset - short DOA [[plasma esterase]] Small Vd minimal accumulation in tissues even with infusion

Answer 49

blunt noxious stim [[just like fentanyl and other analogs]] infusion for intermediate/ long surgeries; where rapid recovery is desired - neurosurgery [[scoliosis]] - outpatient surgery * great for extracting eggs [[very painful procedure but once procedure is over pain is gone and patient goes home]]

Answer 50

able to quickly wake patient up halfway through case to check motor movement/ reflex

Answer 51

ANTAGONIST at Mu Agonist at Kappa NO ventilatory depression !! less physical dependance Analgesia with little ventilatory depression side effects similar to opioid agonist can have some dysphoria from kappa receptor ``` [[Kappa receptor effects]] analgesia [[supraspinal and spinal]] dysphoria sedation mitosis diuresis ``` ex. Nalbuphine [[Nubain]] Butorphenol [[Stadol]]

Answer 52

Agonist/ Antagonist analgesia = to morphine works on Kappa [[and sigma]] antagonizes opioid induced respiratory depression **analgesia with no ventilatory depression no adverse CV problems **reverses spasm of sphincter of Oddi [[antagonizing]]

Answer 53

Agonist/ Antagonist agonist on Kappa weak antagonist or partial agonist of Mu [[dose dependent]] 5 x more potent than morphine for analgesia **nasal spray for migraines

Answer 54

Antagonist Pure opioid antagonist Blocks receptor site; reverses analgesia and respiratory depression Competitive antagonist for Mu, Kappa and Delta [[can be overcome with higher opioid doses]] DOA less than opioids [[use trip bc shorter acting than the opioid your reversing]] Titratable [[dilute give slowly and tribute drip to effect]] onset 1-2 min reversal is dose dependent Reversal is NOT benign

Answer 55

tachycardia HPTN ventricular dysrhymias severe pain pulmonary edema in patient with CV disease [[pulmonary HPTN, hydrostatic pulmonary edema]] pulmonary edema in healthy patient [[catecholamine release, increased SNS activity; that you blunted with opioid, increased preload]]

Answer 56

epinephrine norepinephrine

Answer 57

moprhine [[morphine-6-glucuronide]] meperidine [[normeperidine]] sufentanil [[desmethylsufentanil]]

Opioids Flashcards

(84 cards)