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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
Bremazocine
κ receptors 2x potent > Morphine Naloxone = not effective as reversal (could be other receptors)
26
Dezocine
δ & µ: analgesia, no CV 0.15 mg/kg IM= Morphine 10 to 15 mg IM rapid absorption Onset: 15 mins.
27
Meptazinol
mu1 receptors 100 mg = 8 mg Morphine Rapid onset Duration: < 2 hrs Protein binding: 25%
28
Which opioid agonist- antagonist is more potent than morphine
Buprenorphine
29
Naloxone, Naltrexone, and Nalmefene receptor
Pure µ opioid receptor antagonists
30
Naloxone moa
Nonselective antagonist with all 3 opioid receptors
31
Naloxone dose
1 to 4 µg/kg IV
32
Naloxone continuous infusion
5 µg/kg IV
33
Naloxone shock dose
> 1 mg/kg IV
34
Naloxone for Epidural S/E
0.25 µg/kg/hour IV
35
Naloxone Duration of action
30 to 45 minutes give slow
36
Naloxone Elimination half-time
60-90 min
37
Naloxone S/E
reversal of analgesia*, N/V**, increased SNS (HR, BP, pulmonary edema, cardiac dysrhythmias [v-fib])
38
Naltrexone
More effective PO Duration: 24 hours Uses: alcoholism
39
Nalmefene
Equipotent to naloxone Dose: 15 to 25 µg IV (q 2 to 5 mins) -> 1 µg/kg Elimination half-time: 10.8 hours
40
Methylnaltrexone
Highly ionized (quarternary): peripheral Promotes gastric emptying and antagonizes N/V No alteration in centrally mediated analgesia
41
Alvimopan
Newer, µ-selective PO peripheral opioid antagonist Uses: post op ileus Metabolism: gut flora Limitations: long term use -> CV events
42
Fentanyl effect on MAC
3 µg/kg IV 25 to 30 minutes before surgical incision = decreased Minimum Alveolar Concentration (MAC) of Iso or Desflurane to 50%
43
Sufentanyl on MAC
Sufentanyl decreases MAC with Enflurane by 70 to 90%
44
Alfentanyl on MAC
up to 70% decrease in MAC
45
Remifentanyl on MAC
50 to 91% decrease
46
Neuraxial opioids Receptors
Opioid Receptors in substantia gelatinosa (lamina 2) of spinal cord
47
Epidural dose
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
Epidural on morphine
slower onset, but longer duration
49
Epidural systemic Uptake
Epidural venous plexus = systemic absorption Intervention: Add epinephrine
50
Epidural Lipid solubility Fentanyl
Fentanyl (800x > morphine) Peak: 20 mins
51
Epidural Uptake Lipid solubility Sufentanil
Sufentanil (1,600x > morphine) Peak 6 mins
52
EPIDURAL ADMIN/ CSF PEAK fent
20 MIN
53
EPIDURAL ADMIN/ CSF PEAK SUFENTANIL
6 MIN
54
EPIDURAL ADMIN/ CSF PEAK MORPHINE
1-4 hrs
55
EPIDURAL ADMIN/ PLASMA PEAK Fent
5-10 min
56
EPIDURAL ADMIN/ PLASMA PEAK Sufent
< 5 min
57
EPIDURAL ADMIN/ PLASMA PEAK morphine
10-15 min
58
INTRATHECAL/CSF/ CERVICAL LEVELS morphine
1-5 hrs
59
Neuraxial Opioids Depression of Ventilation
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
What is the emphasis of multimodal anesthesia for general anesthesia includes these two aspects
short acting anesthetic agents opioid sparing
61
Gabapentin MOA
Structural analogue of GABA No activity in GABA neurotransmission Binds voltage gated Ca++ channels Enhances descending inhibition Inhibits excitatory neurotransmitter release
62
What medications can be given in both preop and post op
gabapentin and acetaminophen
63
Gabapentin’s Preemptive Analgesia dose
300-1200 mg PO; 1 to 2 hrs prior to OR
64
Gabapentin’s C/I
MG and myoclonus; reduce dose in elderly.
65
Gabapentin S/E
Abrupt withdrawal in seizure pts: seizures
66
COX-1
ubiquitous “physiologic” Inhibition is responsible for many adverse affects
67
COX-2
“pathophysiologic” Expressed at sites of injury Not protective…oncogenic processes Sensitization, “wind-up”
68
COX-2 Selective vs. Nonspecific Inhibitors
Comparable analgesia Lack effects on platelets May be assoc. with ↓ GI effects Possible ↑ in MI and CVA Dosage ceiling -↑ in side effects
69
Celecoxib (Celebrex) dose
200 to 400 mg PO QD
70
Celecoxib (Celebrex) dose
200 to 400 mg PO QD
71
Celecoxib (Celebrex) Peak
3 hours
72
Ofirmev dose
1000 mg IV Q4-6H; max 3000-4000 mg QD
73
Ofirmev Peak PO and IV
PO: 1-3 hours IV: 30 mins to 1 hour
74
Ofirmev Duration
6-8 hours
75
Ofrimev MOA
Reduces prostaglandin metabolites
76
Ofirmev C/I
Hepatic Dysfunction
77
Ketorolac (Toradol) MOA
inhibits PG synthesis by inhibiting COX 1 and 2
78
Ketorolac (Toradol) C/I
Severe renal impairment, significant risk for bleeding, CAD, CABG, pregnancy; decrease dose in. elderly, NSAID allergy
79
Ketorolac (Toradol) Peak
45 to 60 mins IV
80
Ketorolac (Toradol) dose
15-30 q6H (1/2 dose in elderly): Max 60-120 mg QD
81
Ibuprofen MOA
anti-inflammatory, analgesic, and antipyretic; inhibits COX 1 and 2.
82
Ibuprofen Dose
200 to 800 IV over 30 mins Q6H PRN (3200 mg/day max).
83
Ibuprofen peak
1 to 2 hours
84
Lidocaine dose initial
1 to 2 mg/kg IV (initial bolus) over 2 - 4 min.
85
Lidocaine gtt dose
1 to 2 mg/kg/hour terminated 12 - 72 hours
86
Mag MOA
N-methyl-D-aspartate (NMDA) receptor antagonist
87
Magnesium Dose
50mg/kg IV preop, then … 8 mg/kg/hr intraoperatively
88
Ondansetron Duration/Plasma ½ life
4 hrs
89
Ondansetron dose
4 mg IV (up to 8 mgs) Pediatrics: 0.1 mg/kg IV
90
Corticosteroids moa for nausea
Glucocorticoid receptors in nucleus tractus solitarius Increase effectiveness for 5 HT3 antagonists and droperidol
91
Dexamethasone (Decadron) dose
8-10 mgs
92
Dexamethasone (Decadron) efficacy persists for
24 hrs onset = 2 hr delay

Pharm Semester 2 (6 decks)

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