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Pharm Semester 2 > Pain > Flashcards

Pain Flashcards

1
Q

Opioid Agonist-Antagonists advantages

A

analgesia
limited depression of ventilation
Low potential for physical dependence
Ceiling effect prevents additional responses

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2
Q

Ceiling effect

A

Higher dose = no higher effect/ wont OD.

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3
Q

Pentazocine receptors

A

Agonist effects on δ and κ receptors with weak antagonist activity

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4
Q

Pentazocine potency

A

1/5th as potent as Nalorphine (morphine)

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5
Q

Pentazocine Excretion

A

Glucoronide conjugates = urine

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6
Q

Pentazocine Elimination half-time

A

2-3 hr

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7
Q

Pentazocine Moderate Chronic Pain Dose

A

10 to 30 mg IV or 50 mgs PO (equivalent to Codeine 60 mgs)

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8
Q

Pentazocine analgesia sedation and depression of ventilation

A

20 to 30 mgs IM: analgesia sedation and depression of ventilation similar to 10 mgs of Morphine

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9
Q

Pentazocine S/E

A

S/E: sedation, diaphoresis, dizziness, dysphoria (high doses), increased HR, BP, PA bp, LVEDP.
Crosses placental barrier  fetal depression

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10
Q

Butorphanol potency

A

Agonist 20x and antagonist 10x to 30x > Pentazocine
more potent than morphine

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11
Q

Butorphanol Receptors

A

low affinity for µ receptors to produce antagonism
moderate affinity for κ receptors to produce analgesia and anti-shivering effects
minimal affinity for σ receptors so dysphoria is low

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12
Q

Butorphanol dose comp to morphine

A

2 to 3 mg IM = 10 mg Morphine (depression of ventilation)
Rapidly & completely absorbed with IM.

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13
Q

Butorphanol Elimination half-time

A

2.5 to 3.5 hours

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14
Q

Butorphanol caution

A

difficult to use with another opioid agonist

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15
Q

What receptor has a moderate affinity for Butorphanols effects to mitigate shivering and produce analgesia

A

Kappa

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16
Q

Butorphanol Elimination site

A

Bile > urine

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17
Q

Nalbuphine potency

A

equally potent to Morphine
1/4th as potent as Nalorphine

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18
Q

Nalbuphine receptor

A

µ receptors agonist

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19
Q

Nalbuphine on cv

A

no increase in BP, PA BP, HR, or atrial filling pressures ->√√√ cardiac catheterization patients

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20
Q

Nalbuphine Elimination half-time

A

3 to 6 hours

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21
Q

Buprenorphine potency

A

µ receptors agonist affinity is 50x > Morphine
Analgesic potency 0.3 mg IM = 10 mg Morphine

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22
Q

Buprenorphine onset and duration

A

Onset: 30 mins
Duration: 8 hours

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23
Q

Buprenorphine and naloxone

A

prolonged resistance to Naloxone

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24
Q

Nalorphine

A

Equally potent with Morphine
Not used clinically: high incidence of dysphoria (σ receptors)

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25
Q

Bremazocine

A

κ receptors 2x potent > Morphine
Naloxone = not effective as reversal (could be other receptors)

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26
Q

Dezocine

A

δ & µ: analgesia, no CV
0.15 mg/kg IM= Morphine
10 to 15 mg IM rapid absorption
Onset: 15 mins.

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27
Q

Meptazinol

A

mu1 receptors
100 mg = 8 mg Morphine
Rapid onset
Duration: < 2 hrs
Protein binding: 25%

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28
Q

Which opioid agonist- antagonist is more potent than morphine

A

Buprenorphine

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29
Q

Naloxone, Naltrexone, and Nalmefene receptor

A

Pure µ opioid receptor antagonists

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30
Q

Naloxone moa

A

Nonselective antagonist with all 3 opioid receptors

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31
Q

Naloxone dose

A

1 to 4 µg/kg IV

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32
Q

Naloxone continuous infusion

A

5 µg/kg IV

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33
Q

Naloxone shock dose

A

> 1 mg/kg IV

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34
Q

Naloxone for Epidural S/E

A

0.25 µg/kg/hour IV

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35
Q

Naloxone Duration of action

A

30 to 45 minutes

give slow

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36
Q

Naloxone Elimination half-time

A

60-90 min

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37
Q

Naloxone S/E

A

reversal of analgesia*, N/V**, increased SNS (HR, BP, pulmonary edema, cardiac dysrhythmias [v-fib])

38
Q

Naltrexone

A

More effective PO
Duration: 24 hours
Uses: alcoholism

39
Q

Nalmefene

A

Equipotent to naloxone
Dose: 15 to 25 µg IV (q 2 to 5 mins) -> 1 µg/kg
Elimination half-time: 10.8 hours

40
Q

Methylnaltrexone

A

Highly ionized (quarternary): peripheral
Promotes gastric emptying and antagonizes N/V
No alteration in centrally mediated analgesia

41
Q

Alvimopan

A

Newer, µ-selective PO peripheral opioid antagonist
Uses: post op ileus
Metabolism: gut flora
Limitations: long term use -> CV events

42
Q

Fentanyl effect on MAC

A

3 µg/kg IV 25 to 30 minutes before surgical incision = decreased Minimum Alveolar Concentration (MAC) of Iso or Desflurane to 50%

43
Q

Sufentanyl on MAC

A

Sufentanyl decreases MAC with Enflurane by 70 to 90%

44
Q

Alfentanyl on MAC

A

up to 70% decrease in MAC

45
Q

Remifentanyl on MAC

A

50 to 91% decrease

46
Q

Neuraxial opioids Receptors

A

Opioid Receptors in substantia gelatinosa (lamina 2) of spinal cord

47
Q

Epidural dose

A

Dose is 5 to 10x more because the drug still needs to diffuse through the duramatter

Diffusion of drugs across the dura -> systemic absorption

48
Q

Epidural on morphine

A

slower onset, but longer duration

49
Q

Epidural systemic Uptake

A

Epidural venous plexus = systemic absorption
Intervention: Add epinephrine

50
Q

Epidural Lipid solubility
Fentanyl

A

Fentanyl (800x > morphine)
Peak: 20 mins

51
Q

Epidural Uptake Lipid solubility
Sufentanil

A

Sufentanil (1,600x > morphine)
Peak 6 mins

52
Q

EPIDURAL ADMIN/
CSF PEAK
fent

A

20 MIN

53
Q

EPIDURAL ADMIN/
CSF PEAK
SUFENTANIL

A

6 MIN

54
Q

EPIDURAL ADMIN/
CSF PEAK
MORPHINE

A

1-4 hrs

55
Q

EPIDURAL
ADMIN/
PLASMA PEAK
Fent

A

5-10 min

56
Q

EPIDURAL
ADMIN/
PLASMA PEAK
Sufent

A

< 5 min

57
Q

EPIDURAL
ADMIN/
PLASMA PEAK
morphine

A

10-15 min

58
Q

INTRATHECAL/CSF/
CERVICAL LEVELS
morphine

A

1-5 hrs

59
Q

Neuraxial Opioids Depression of Ventilation

A

Early: within 2 hours
Delayed: 6 to 12 hours after
Most reliable sign: depressed LOC secondary to hypercarbia
Treatment: Naloxone (0.25 µg/kg/hour IV) is effective in attenuating the side effects (nausea and vomiting, pruritus)

60
Q

What is the emphasis of multimodal anesthesia for general anesthesia includes these two aspects

A

short acting anesthetic agents
opioid sparing

61
Q

Gabapentin MOA

A

Structural analogue of GABA
No activity in GABA neurotransmission
Binds voltage gated Ca++ channels
Enhances descending inhibition
Inhibits excitatory neurotransmitter release

62
Q

What medications can be given in both preop and post op

A

gabapentin and acetaminophen

63
Q

Gabapentin’s Preemptive Analgesia dose

A

300-1200 mg PO; 1 to 2 hrs prior to OR

64
Q

Gabapentin’s C/I

A

MG and myoclonus; reduce dose in elderly.

65
Q

Gabapentin S/E

A

Abrupt withdrawal in seizure pts: seizures

66
Q

COX-1

A

ubiquitous
“physiologic”
Inhibition is responsible for many adverse affects

67
Q

COX-2

A

“pathophysiologic”
Expressed at sites of injury
Not protective…oncogenic processes
Sensitization, “wind-up”

68
Q

COX-2 Selective
vs.
Nonspecific Inhibitors

A

Comparable analgesia
Lack effects on platelets
May be assoc. with ↓ GI effects
Possible ↑ in MI and CVA
Dosage ceiling
-↑ in side effects

69
Q

Celecoxib (Celebrex) dose

A

200 to 400 mg PO QD

70
Q

Celecoxib (Celebrex) dose

A

200 to 400 mg PO QD

71
Q

Celecoxib (Celebrex) Peak

A

3 hours

72
Q

Ofirmev dose

A

1000 mg IV Q4-6H; max 3000-4000 mg QD

73
Q

Ofirmev Peak PO and IV

A

PO: 1-3 hours
IV: 30 mins to 1 hour

74
Q

Ofirmev Duration

A

6-8 hours

75
Q

Ofrimev MOA

A

Reduces prostaglandin metabolites

76
Q

Ofirmev C/I

A

Hepatic Dysfunction

77
Q

Ketorolac (Toradol) MOA

A

inhibits PG synthesis by inhibiting COX 1 and 2

78
Q

Ketorolac (Toradol) C/I

A

Severe renal impairment, significant risk for bleeding, CAD, CABG, pregnancy; decrease dose in. elderly, NSAID allergy

79
Q

Ketorolac (Toradol) Peak

A

45 to 60 mins IV

80
Q

Ketorolac (Toradol) dose

A

15-30 q6H (1/2 dose in elderly): Max 60-120 mg QD

81
Q

Ibuprofen MOA

A

anti-inflammatory, analgesic, and antipyretic; inhibits COX 1 and 2.

82
Q

Ibuprofen Dose

A

200 to 800 IV over 30 mins Q6H PRN (3200 mg/day max).

83
Q

Ibuprofen peak

A

1 to 2 hours

84
Q

Lidocaine dose initial

A

1 to 2 mg/kg IV (initial bolus) over 2 - 4 min.

85
Q

Lidocaine gtt dose

A

1 to 2 mg/kg/hour
terminated 12 - 72 hours

86
Q

Mag MOA

A

N-methyl-D-aspartate (NMDA) receptor antagonist

87
Q

MagnesiumDose

A

50mg/kg IV preop, then …
8 mg/kg/hr intraoperatively

88
Q

Ondansetron Duration/Plasma ½ life

A

4 hrs

89
Q

Ondansetron dose

A

4 mg IV (up to 8 mgs)
Pediatrics: 0.1 mg/kg IV

90
Q

Corticosteroids moa for nausea

A

Glucocorticoid receptors in nucleus tractus solitarius
Increase effectiveness for 5 HT3 antagonists and droperidol

91
Q

Dexamethasone (Decadron) dose

A

8-10 mgs

92
Q

Dexamethasone (Decadron) efficacy persists for

A

24 hrs
onset = 2 hr delay

Pharm Semester 2 (6 decks)

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