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Pharm-AL > Exam 2 > Flashcards

Exam 2 Flashcards

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1
Q

Synergistic analgesia with local anesthetic when given neuraxially EXCEPT:

A

2-chlorprocaine

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2
Q

1 mL of sodium bicarbonate per 10 mL of lidocaine will hasten blockade by

A

3-5 minutes

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3
Q

How does epi prolong local anesthetic activity?

A

Prolongation of local anesthetic block and decreased systemic absorption due to vasoconstriction slowing clearance from injection site

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4
Q

What are some techniques to increase local anesthetic activity?

A

-Epinephrine (1:200,000)

-Alkalization

-Opioids

-Alpha2 agonists

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5
Q

Does tachyphylaxis occur if re-dosing local anesthetics before pain occurs

A

No

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6
Q

Which enantiomers have greater efficacy but greater systemic toxicity?

A

R-enantiomers

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7
Q

Three anesthetics that produce their own vasoconstriction?

A

Cocaine, Ropivicaine and Levobupivicaine

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8
Q

What local anesthetics are NOT racemic mixtures?

A

Lidocaine, ropivicaine and levobupivicaine

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9
Q

Local Anesthetics physical properties

A

-pKa (dissociation constant) is the pH at which the 2 forms occur equally

-Lower pKa agents have more rapid onset

-Increased lipophilicity slows the rate of onset and prolongs the duration of action

-Increased protein binding increased the duration of action

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10
Q

Lower pKa agents have more rapid or slower onset?

A

More rapid

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11
Q

What is the solubility of esters?

A

Lipid soluble natural form in equilibrium with hydrophilic charged form

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12
Q

Are esters an acid or a base?

A

Weak Base

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13
Q

What are the Esters?

A

-Cocaine

-Procaine

-2-chloroprocaine

-Tetracaine

-Benzocaine

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14
Q

What are the Amides?

A

-Lidocaine

-Prilocaine

-Mepivicaine

-Ropivicaine

-Bupivicaine

-Levobupivicaine

-Etidocaine

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15
Q

Structure activity relationships of local anesthetics

A

Lipophilic substituted benzene ring linked to a hydrophilic amine group (tertiary or quaternary) through either an ester or amide linkage

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16
Q

Alfred Einhorn synthesized ________ as a degradation product of cocaine

A

Procaine

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17
Q

Cocaine downfalls

A

Significant toxicity, short duration, high cost and addiction

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18
Q

Who utilized cocaine as a local anesthetic? (Tongue numbing and corneal anesthesia)

A

Carl Keller and Sigmund Freud

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19
Q

Precedex as analgesia for labor

A

-10-15 mcg

-decreases shivering

-BUT hypotension, bradycardia, crosses placenta and can depress fetal HR so limit dose.

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20
Q

Use of precedex in an epidural

A

-10-20mcg

-increased quality of block, prolongs analgesia, prevents shivering

-less hypotension

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21
Q

Use of precedex in intrathecal dosing

A

-5-10mcg

-Less vasoconstriction than epi

-Decreased cardiac output decreases clearance of local

-Increased quality and duration of block, BUT . . .may cause hypotension

-No more than 1 mcg/kg when co administered with a local

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22
Q

Alpha2 adrenergic agonist uses:

A

Pre-op medication for sedation/anxiolysis/amnesia

-Anesthetic sparing

-Sedation

-Prevention of drug withdrawal syndrome

-Hemodynamic stability

-Enhancement of local anesthetic block

-Analgesia for labor

-Chronic Pain

-Cancer Pain

-Prevention of drug withdrawal

-Prevention/treatment of shivering

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23
Q

can be used post extubation without causing respiratory depression?

A

Dexmedetomidine

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24
Q

Precedex is a good pre-op medication for sedation/anxiolysis/amnesia due to?

A

-May decrease dose of anesthetics/analgesics required intra-op

-Can cause xerostomia and decreased GI transit

-Blunts sympathetic response to intubation/induction

-May cause prolonged anesthesia and delayed emergence

-Use is limited by hypotension and bradycardia

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25
What special populations show the increased benefit from precedex?
-Drug addicts and alcoholics (increased sympathetic tone) -Chronic cancer/non-cancer pain (require large doses of opioids) -Hypertension -Procedures where hypotension advantageous -Ophthalmic surgery (lowers IOP) -Adjuvant to ketamine (prevents post op delirium)
26
What is one of the few sedation drugs that can be left on through extubation?
Precedex
27
Clinical effects of precedex (Dexmedetomidine)
-Analgesia—more prominent after spinal or epidural administration than intravenous -Sedation—mimics normal sleep; deeply sedated, but can rouse themselves to all most full consciousness -Hypotension/bradycardia -Anti-shivering properties -Mild ventilatory depression
28
Dexmedetomidine metabolism
-Undergoes extensive liver metabolism (weak cytochrome p450 inhibitor) -Methyl and glucuronide conjugates are excreted via kidneys
29
Highly bound to albumin and alpha1 glycoprotein
Dexmedetomidine
30
Distribution and elimination half life of precedex
Distribution half life: 6 minutes Elimination half life: 2 hours
31
Has 8x greater alpha2 activity than clonidine
Dexmedetomidine
32
Clonidine elimination half life
12-24 hours
33
Onset of action of clonidine
IV: 60-90 minutes Epidural: 15-20 minutes
34
Physical properties of clonidine
-200x more potent at alpha2 than alpha1 -Moderately lipid soluble -Complete absorption after oral administration
35
Chemical categories of alpha2 adrenergic agonists
-Phenylethylates (methyldopa, quanabenz) -Imidazolines (clonidine, dexmedetomidine) -oxaloazepines
36
alpha2 adrenergic agonist elated hypotension responds to?
Fluid, ephedrine, phenylephrine and dobutamine, less of a reversal is seen with norepinephrine and dopamine
37
Sedation of alpha2 adrenergic agonists is linked to?
The inactivation of the locus ceruleus (natural sleep cycle)
38
Hemodynamic effects of alpha2 adrenergic agonist
Hemodynamic effects are primarily hypotension and bradycardia and are mediated at the vasomotor center of the brainstem and the nucleus tractus solitarius
39
For alpha2 adrenergic agonists analgesia occurs at the _________?
Spinal cord level
40
Intrathecal and Epidural dose for Precedex
Intrathecal dose: 5-10 mcg Epidural dose: 10-20 mcg
41
Alpha2c
learning and startle response
42
Alpha2b
mediates vasoconstriction, antishivering action, analgesia
43
Alpha2a
sedation, hypnosis, analgesia, sympatholysis
44
Clonidine MOA
Activate Alpha2 receptors
45
________ first developed as a nasal decongestant
Clonidine
46
Which NSAIDs cannot be used post-op CABG?
IV ibuprofen and IV Diclofenac
47
Diclofenac IV (Dyloject) dose
-37.5 mg over 15 seconds every 6 hours not to exceed 150 mg/24 hour -contraindication against use in CABG patients
48
When is Ibuprofen IV ( Caldolor) contraindicated
Contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft surgery
49
Ibuprofen IV (Caldolor)
400-800 mg over 30 minutes every 6 hours (max 3200 mg/24 hour)
50
Acetaminophen IV (Ofirmev) dose
1000 mg given as a 15 minute infusion
51
Max dose of acetaminophen a day
No more than 4 grams per day to prevent hepatotoxicity associated with glutathione depletion
52
Effective analgesic and antipyretic, but lacks anti-inflammatory properties.
Acetaminophen
53
What is Samter’s Triad?
-Chronic inflammatory lung and sinus condition that involves sensitivity to ASA and NSAIDs. -Characterized by Asthma, chronic rhinosinusitis and reoccurring nasal polyps.
54
NSAIDs contraindications and precautions
-History of hypersensitivity to NSAIDs -Bleeding complications -GI disease -Elderly patients -Children -Congestive heart failure -Hepatic impairment -Renal impairment -Hypertension -Drugs--multiple NSAIDs, probenecid, pentoxifylline, lithium, or anticoagulant therapy.
55
Celecoxib dosing:
100-200 mg twice daily (higher doses for RA)
56
Naproxen dosing:
250-375 mg twice daily up to 375-750 mg twice daily
57
Ibruprofen dosing
-Analgesic dose 200-400 mg po q4-6 hours -Anti-inflammatory dose 400-800 mg po q6 hours
58
Diclofenac dosing:
75-150 mg/day in divided doses.
59
Aspirin dosing
-Analgesic/anti-inflammatory dose of 3 grams per day. -Cardioprotective doses are much lower (81-325 mg per day seems to be the new “in” dose).
60
Ketorolac use should be limited to ___ days
-5 Days
61
Ketorolac dosing
-60 mg IM -30 mg IV/IM q6h for patients <65 -15mg IV/IM q6h for patients >65 -oral max dose is 40mg/day (10mg po q6h) Loading doses are unnecessary and decrease the amount that can be administered in 24hrs
62
In addition to less PONV what is another post-op benefit to NSAIDs?
Less sedation, less impaired respiratory function, less sleep disturbances, less ileum/constipation and urinary retention
63
Do NSAIDs or Opioids have longer half-lives?
NSAIDs Can prolong the duration of relief and may reduce PONV since less post-op analgesics are required
64
What NSAID is the best choice for patients with a need for cardiac safety medications?
Ketorolac (Toradol)
65
Preoperative administration may have benefits as compared to post operative administration, but pre-emptive dosing may increase risk of bleeding complications.
Ketorolac
66
As one of the more potent NSAIDs has been shown to be a more effective analgesic in surgical models when compared with other NSAIDs; also its parenteral availability makes it more practical than other NSAIDs
Ketorolac
67
important element in balanced multimodal post surgical regimens (combination with opioids); but may also be an alternative to opiates in minor surgical procedures.
NSAIDs
68
Do you see anticoagulant interactions and risk of renal insufficiency in COX-2 inhibitors?
You do not. Much more of a risk in NSAIDs than COX-2
69
COX-2 Inhibitors
Celebrex (celecoxib), Vioxx (rofecoxib), and Bextra (valdecoxib)
70
How to COX-2 Inhibitors differ from NSAIDs in physical properties?
Highly lipophilic, neutral, nonacidic molecules with limited aqueous solubility (with the exception of parecoxib which is a water soluble pro-drug of valdecoxib and may be available soon for IV or IM administration.
71
NSAID distribution and metabolism
Distribution: -Highly protein bound -Found within most tissues including synovial fluid and CSF Metabolism: -Varies greatly (from non-specific esterases to complex hepatic pathways) -Excretion is primarily renal
72
73
NSAID absorption
Rapidly and well absorbed from GI tract
74
NSAIDs: Irreversible inhibitors
Aspirin
75
NSAIDs: Mixed kinetic inhibitors (slow weakly binding)
Naproxen
76
NSAIDs: Time-dependent inhibitors
Indomethacin
77
NSAIDs: Competitive, reversible inhibitors
Ibuprofen
78
How are prostaglandins and Thromboxanes produced?
Arachidonate —(COX)—> PGG2 PGG2—(oxidized)—> PGH2 PGH2—> Prostaglandins and Thromboxanes
79
COX-2 distribution
-Inflammatory cells/response to cytokines such as interleukin-1 and tumor necrosis factor-alpha -Female reproductive tract -Brain -Kidney -Cancer cells
80
COX-1 distribution
-GI tract -Platelet -Kidney -Most other tissues
81
Perception of pain: Production of prostaglandins
-inflammatory process triggers COX to produce prostaglandins which increase the sensitivity of the nociceptive neurons to bradykinin, histamine, serotonin, and other mechanical, chemical, and thermal stimuli.
82
Nociception
-Extremes of temperature, painful mechanical stimuli, and noxious chemical stimuli are detected by the distal ends of primary afferent neurons. -These neurons then terminate in the dorsal horn of the spinal cord with their cell bodies located within the dorsal root ganglia.
83
The newer COX-2 inhibitors are thought to have a more favorable side effect profile since they spare
The COX-1 isoform
84
Conventional NSAIDs are non-specific inhibitors of both isoforms thus providing anesthesia and anti-inflammatory action but also affecting?
platelet function and protection of the gastric mucosa.
85
Conventional NSAIDS are
Non-specific inhibitors of both isoforms
86
COX-1 is expressed in low levels in many tissues, including:
lung, liver, spleen, kidney and stomach and is responsible for maintaining homeostasis
87
COX-2 is induced by
cellular cytokines in localized areas of injury and in the spinal cord in response to tissue damage
88
bark of the willow tree, Salic alba contain derivatives of?
These plants contain derivatives of salicylic acid and were used to treat pain and fever.
89
NSAIDs: Originally derived from natural sources such as the bark of the
Willow tree, Salix alba
90
What can NSAIDs be used to treat?
Pain and inflammation -Surgical procedures -Inflammatory diseases -Osteoarthritis and rheumatoid arthritis -Migraine -Dysmenorrhea -Myalgia -Dental pain
91
Properties of NSAIDs
-Analgesic -Anti-inflammatory -Anti-pyretic
92

Pharm-AL (4 decks)

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