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Anesthesia Pharm Exam 2 > Opioids > Flashcards

Opioids Flashcards

1
Q

Inhibitory Neurotransmitters

A

gaba

glycine

Epi

NE

ACh

Endorphins

Serotonin

Histamine

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2
Q

Excitatory Neurotransmitters

A

Glutamate

Inotropic glutamate receptors - NMDA

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3
Q

Glutamate

A
  • located in the hippocampus, cortex, and substantia gelatinosa
  • learning, memory, recall
  • central pain transduction
  • excitotoxic neuronal injury
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4
Q

Opioids

A
  • most efficacious analgesic drug available
  • agonists on mu, kappa, delta receptors
  • may not totally eliminate pain
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5
Q

Opioid activation of mu receptor

A
  • produce analgesia
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6
Q

Opioids _______ Ca++ influx and _____ K+ efflux.

A

Opioids block Ca++ influx and increase K+ efflux.

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7
Q

Opioid MOA on receptors

A
  • agonist at stereospecific opioid receptors in pre- and post- synaptic sites in CNS and peripheral nerves
  • activate opioid receptors on primary afferent sensory neurons (also activated by enkephalins, endorphins, dynorphins)
  • need to be ionized for strong bonding to receptors
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8
Q

Levo-rotary opioid molecules

A
  • only levo-rotary opioid molecules exhibit agonist activity (so anything besides levo-rotary won’t give us pain relief!)
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9
Q

Opioid MOA 2 - neurotransmission

A
  • Principal effect of opioid receptor activation is by decreased neurotransmission!
  • occurs by presynaptic inhibition of release of NTs (ACH, dopamine, NE, substance P)
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10
Q

Opioid receptor occupied by agonist

A
  • increased K+ conductance hyperpolarizes membrane
  • and/or Ca+ ch inactivation
  • leads to decreased NT release and decreased transmission of pain!
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11
Q

Opioid action on peripheral nerves

A

Opioids do NOT alter the responsiveness of peripheral nerves to noxious stimuli nor do they impair impulse transmission

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12
Q

Opioids cross the BBB based on 4 things:

A
  1. Molecular size (smaller = better)
  2. lipid solubility (more lipid sol = better)
  3. non-ionized is better (more lipid soluble)
  4. protein binding (greater protein binding = less drug available to cross BBB)
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13
Q

Lipid Solubility and Protein Binding Chart

A
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14
Q

Morphine Lipid Solubility and Protein binding

A

23% nonionized at pH 7.4 (able to cross BBB)

1.4 lipid solubility (slow onset of action)

35% protein binding (65% available for action)

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15
Q

Fentanyl Lipid Solubility and Protein binding

A

9% nonionized at pH 7.4

816 lipid solubility

84% protein binding

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16
Q

Alfentanyl Lipid Solubility and Protein binding

A

89% nonionized at pH 7.4

128 lipid sol

92% protein binding

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17
Q

Remifentanyl Lipid Solubility and Protein binding

A

58% nonionized at pH 7.4

18 lipid solubility

70% protein binding

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18
Q

Opioid Receptors and Endogenous Opioids

A
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19
Q

Mu Receptors Location and Actions

A
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20
Q

Kappa Receptors (dynorphin) Location and Actions

A
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21
Q

Delta Receptors Location and Action

A
22
Q

Nagelhout and Plaus Table 12-2

A
23
Q

Generalizs opioid SE - Resp, GI, CV

A
  • sedation (precursor to respiratory depression)
  • resp dep (prevented by intense pain)
  • N/V (give antiemetics)
  • decreased GI motility (give stool softener)
  • CV effects: orthostatic hypotension, bradycardia, and peripheral vasodilation (2/2 histamine release)
24
Q

Generalized opioid SE 2

A
  • euphoria (meperidine)
  • antitussive (codeine)
  • miosis (pupillary constriction)
  • pruritis
  • biliary spasm (gallbladder surg)
  • myoclonus/sz’s
  • chest wall rigidity (high doses may cause difficult mast ventilation, give muscle relaxer)
25
Q

Sites of Action Figure

A
26
Q

Serotonin Syndrome

A

Meperidine inhibits reuptake of serotonin when given to pt taking MAOI or SSRIs.

  1. delirium (AMS, agitation, excitement, confusion)
  2. fever (tachycardia/tachypnea, autonomic hyperactivity and diaphoresis)
  3. convulsions (tremor, clonus, hyperreflexia)
27
Q

Opioid Effect on Inhaled Anesthetics MAC

A
  1. increased opioid = reduced ISO MAC
  2. MAC reduction may be >75%
  3. MAC reduction occurs at moderate plasma levels of opioid
  4. ISO canNOT be eliminated
28
Q

Morphine

A
  • mu, kappa, delta agonist
  • influences motivational-effective aspect of pain
  • T1/2 2-3 hours
  • DOA 4-6 hours
  • onset of resp dep = onset of analgesia
  • tolerance and hyperalgesia
  • metabolized in liver via glucuronidation
29
Q

Morphine Metaboites by Kidney

A

M-3 glucuronide: 75-85% inactive metabolite - no analgesia!

M-6 glucuronide: 5-10% active metabolite - 10x more potent than morphine!

So renal dx and accumulation of M6 = bad

30
Q

Renal disease and elimination of morphine

A

M6G secreted by organic ion transporters in kidney which is impaired w renal dx (M3 also accumulates).

Pt w high doses morphine who develops renal insufficiency may experience prolonged sedation or coma.

31
Q

Hydromorphone (Dilaudid)

A
  • 5x more potent than morphine
  • onset in 5 min, peak 10-20
  • 1-2mg IV dilaudid = 10-20 mg IV morphine
    dose: oral 2-4 mg q 4-6 hours, onset 20-40 min, peak 1.5 hr
32
Q

Codeine

A

morphine derivitive

  • analgesia = 10% conversion to morphine
  • low affinity for opioid receptors
  • less 1st pass metabolism orally (more effective than morphine)
33
Q

Tylenol #3

A

30mg codeine + 300mg Tylenol

34
Q

Tylenol #4

A

60mg codeine + 300 mg Tylenol

35
Q

Oxycodone

A

morphine derivitive

  • less 1st pass metab than morphine
  • Percocet and Oxycontin SR
36
Q

Percocet

A

5mg oxycodone + 325 acetaminophen

  • adults 5-15 (1-3 tabs) q6
  • peds 0.05 - 0.15 mg/kg q 4-6 hr
  • beware tylenol dose limits!*
37
Q

Oxycontin SR

A

10-20mg q 12

  • 80-160mg for opioid tolerant (CA pts)
  • SR when taken whole, bolus high when crushed/chewed (abuse)
38
Q

naloxone (Narcan)

A
  • competitive opioid antagonist at mu, kappa, delta
  • IV, IM, SQ
  • peak 1-2 min
  • metabolized via liver (glucuronidation), excreted urine
  • T1/2 65 min adults, 3 hr neonates (redosing required)
39
Q

Standard ampule narcan

A
  1. 4 mg or 400 mcg
    - adult dose 0.5-1.5 mcg/kg (40-100 mcg)
    - will reverse excessive opioid induced resp dep
    - give 400 mcg or whole amp in Code Blue resp dep narc overdose

beware: withdrawal, HTN, tachycardia, pulm edema, PONV

40
Q

meperidine (Demerol)

A
  • 1/10th potency of morphine but more lipid soluble (faster onset!)
  • less bradycardia and resp dep than equianalgesic dose morphine
  • dysphoric and psychomimetic effects (k receptor)
  • >histamine release than morphine
  • liver metabolism
  • active metabolite normeperidine T1/2 14-21 hours
  • txs post op shivering via K receptor
41
Q

Fentanyl

A
  • u receptor agonist
  • 50-100x more potent than morphine

100 mcg fentanyl = 10 mg morphine

  • effects and SE similar at equianalgesic doses
  • onset 3-5 min (rapid resp dep)
  • w induction, fentanyl will reduce MAC requirement
  • no direct reduction in myocardial contractility (BP will drop if pain relieved)
  • no histamine release = no hypotenseion
  • synergistic w benzos = resp dep
  • 100% hepatic extraction inactive metabolites (clearance related to liver blood flow)
42
Q

Fentanyl Infusion Dose

A

Loading dose 8-12 mcg/kg

Maintenance 1-2 mcg/kg/hr

43
Q

Alfentanyl

A
  • u receptor agonist
  • 10x more potent than morphine
  • 1/10th as potent as fentanyl
  • 1000mcg alfentanyl = 100mcg fentanyl = 10mg morphine
  • rapid onset 1-2 min (rapidly crosses BBB)
  • metabolized in liver to inactive metabolites, clearance related to liver blood flow, reduced w p450 inhibitors (cimetidine, e’mycin)
44
Q

Alfentanil Dose

A
  • Loading Dose 35-70 mcg/kg
  • Maintenance 0.25 - 0.50 mcg/kg/min
  • rapid onset = rapid resp dep*
45
Q

Remifantanil

A
  • u receptor agonist
  • equipotent to fentanyl
  • rapid onset 1 min
  • clearance by NON-SPECIFIC plasma esterases (NOT pseudoholinesterase)
  • clearance constant, not affected by liver blood flow, renal failure or length of infusion
  • infusion only way to administer
46
Q

Remifentanil Dose

A
  • Loading dose 1-2 mcg/kg
  • Infusion 0.05 - 0.25 mcg/kg/min
  • CSHT 3 min (metabolism by nonspecific esterases)
  • duration 6-9 min

UIHC Policy:

mix 4mcg/cc (1mg/250cc) for non-intubated

mix 10mcg/cc (1mg/100cc) for intubated/GA

47
Q

CSHT for Fentanyls

A
48
Q

Spinal Opioids (preservative free)

A
  • spinal mu receptors in dorsal horn
  • morphine or fentanyl via spinal is analgesic
  • can be administered intrathecally (directly into CSF) for chronic pain or epidurally (just outside SC) for acute pain
  • controls pain w less sedation and resp dep than IV for same amounts of analgesia
  • SE: can have resp dep, N/V, sedation, and itching
49
Q

Opioid Synergism

A
  • benzos = minimal resp dep
  • propofol = mild resp dep
  • opioids = potent resp dep

benzo + opioid or opioid + propofol = synergy!!!

50
Q

Opioids w Active Metabolites

A

morphine

hydrocodone

meperidine

oxycodone

codeine

tramadol

Anesthesia Pharm Exam 2 (5 decks)

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