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RUSVM Pharmacology > Analgesics- Local and NSAIDs > Flashcards

Analgesics- Local and NSAIDs Flashcards

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1
Q

The detection of a noxious stimulus at the tissue

A

Nociception

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2
Q

Free nerve endings of primary afferent neurons that detect noxious stimuli

A

Nociceptors

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3
Q

What are the 5 processes that play a role in nocicpetion

A 
Transduction -> stimuli to AP
Transmission -> peripheral nerves to CNS
Modulation ->dorsal horn of spinal cord 
Projection ->2nd order to thalamus 
Perception -> integration
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4
Q

What are the types of primary sensory nocicpetion nerve fibers

A

AB fibers
A-delta (pinpoint; mechanical/thermal)
C-fibers (diffuse; many stimuli )

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5
Q

Pain that persists longer than it is providing protection

A

Chronic pain

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6
Q

Exaggerated perception of pain produced by a noxious stimuli

A

Hyperalgesia

Primary-> occurs in area of tissue damage
Secondary-> occurs beyond region of injury

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7
Q

non-noxious stimuli that elicits pain

A

Allodynia

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8
Q

________________ activate nociceptors

A

Inflammatory mediators

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9
Q

Pain receptor change from high to low threshold

A

Primary hyperalgesia

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10
Q

Inflammatory mediators activate more nociceptors adjacent to injury

A

Secondary hyperalgesia

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11
Q

Where does central pain sensitization occur and what receptors are involved

A

Dorsal horn of the spinal cord

NMDA receptors

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12
Q

What is pain sensitization

A

Changes occur in sensory processing enabling low intensity stimuli to produce pain.

NMDA and Glutamate - increase in excitatory neurotransmitters cause hyper-excitability in dorsal horn neuron

Occurs in acute and chronic pain

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13
Q

What receptor plays a central role in chronic pain

A

NMDA receptor

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14
Q

What is the main effect of local anesthetic?

A

Reversible blockade of transmission

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15
Q

What drugs can be used for local anesthesia

A 
Lidocaine 
Bupivicaine 
Mepivicaine 
Ropivicaine
Proparacaine 
Procaine
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16
Q

Local anesthetics belong to what two chemical groups

A

Amides

Esters

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17
Q

Are local anesthetics weak bases or acids?

A

Weak bases

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18
Q

What are the amide local anesthetics ?

A

Lidocaine
Bupivacaine
Mepivacaine

Metabolized in the liver

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19
Q

What are the ester local anesthetics

A

Procaine
Proparacaine

Hydrolyzed by plasma esterases

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20
Q

What is the MOA of local anesthetics?

A

Cross lipid membrane of nerve cell into the cytoplasm

Prevent depolarization and block the propagation of an action potential by inhibiting the influx of sodium

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21
Q

What is the onset of blockade of local anesthetics??

A

Small. Myelinated A-delta fibers (sensory)
Unmyelinated C fibers (sensory/autonomic)
Large myelinated Aa fibers(motor)

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22
Q

The effect of local anesthetic is usually terminated by ____________

A

Redistribution

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23
Q

Why would you use epinephrine in conjunction with a local anesthetic

A

Epinephrine causes vasoconstriction which decreases the distribution of the anesthetic from its site of action => longer lasting effect

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24
Q

The duration of a local anesthetic will be affected by?

A

Lipophilicity

Ability to bind sodium channel

Underlying disease -> hepatic disease=increased duration of amides

Drug-drug interaction

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25
Esters are broken down by?
Plasma esterases
26
Where are amides metabolized
Liver
27
Where are local anesthetic metabolites excreted
Urine
28
How does the half life of esters compare to amide local anesthetics?
Esters- few minutes; rapidly broken down by plasma cholinestersase Amides- hours (2-6); metabolized in the liver
29
Increasing the _______________ of urine will increase local anesthetic elimination
Acidity Local anesthetics are all weak bases
30
What routes of administration can be used for local anesthetics?
Topical - skin/wound/splash block Local infiltration -peripheral nerve block/intra-aricular/epidural Intravenous -Bier's block
31
What are the clinical uses of local anesthetics?
Regional anesthesia Pre and post-operative analgesia Wound management Peri-operative analgesia
32
When is regional anesthesia used?
Minor procedures Lameness localization Epidural -completely block nociception at site of injury or surgery
33
What kind of regional analgesia can be used for injury/surgery distal to the elbow
Brachial plexus block
34
What kind of regional analgesia could be used for thoracotomy, chest tube, or rib fractures
Intercostal nerve block Injections -> three ribs anterior and two ribs posterior to site of injury
35
What are the benefits to regional analgesia ?
``` Less sedation Decreased nausea and vomiting Decreased CV and pulmonary complications Shorter hospitalization Decreased infection Decreased morbidity and mortality ```
36
What are the major risks of using regional analgesia?
Local anesthetic toxicity Nerve injury -trauma, toxicity, ischemia, or combination ->result from needle, intraneural injection, compression, or stretch
37
What are the contraindications to using epidurals
Coagulopathy Anatomy Skin infection/ sepsis Neurological disease
38
What are the complications that can arise from an epidural
``` Horners Hypotension Hypoventilation Schiff-Sherrington Muscle twitching Hypoglycemia Urinary retention ```
39
What is the most commonly used local anesthetic in vet med
Lidocaine
40
What is the onset of action and duration of lidocaine?
Rapid onset -5mins | Duration -40-60mins
41
Lidocaine is metabolized where
Liver
42
What animals are sensitive to lidocaine
Do not exceed 4-7mg/kg Cats more than dogs Sheep may be more sensitive than other livestock
43
_______________ is used as a topical gel/ointment for dermal analgesia
5% ELMA cream (2.5%lidocaine / 2.5% prilocaine)
44
What is a lidocaine solution for injection
Lidocaine (Xylocaine) -local use
45
What are the clinical uses of lidocaine?
``` Systemic Antiarrhythic (IV)- class 1B antiarrhythmic- control arrhythmias ``` Preanesthetic (IV) Analgesic with anti-inflammatory properties Antioxidant GI prokinestic -increase GI motility in horses
46
What is the most cardiotoxic of the local anesthetics?
Bupivacaine
47
Local anesthetic that is infused through thoracostomy tubes or wound soaker catheters
Bupivacaine
48
What is a precaution to using Bupivacaine?
Cardiotoxic ->Should not used in patients post pericardectomy Phrenic nerve paresis or paralysis
49
Why do cats generally have lower dose of analgesics than dogs?
Cats are deficient in hepatic metabolism Sensitive to anesthetics Amides are degraded in the liverr
50
What is the drug of choice for diagnostic nerve blocks in horses
Mepivacaine
51
How does the duration of action differ between the amide anesthetics?
Lidocaine < Mepivicaine < Bupivicaine
52
What local anesthetic is used topically for corneal and conjunctival manipulation
Proparacaine
53
What is the onset and duration of proparacaine?
``` Rapid (30sec) Short duration (10-20mins) ```
54
What are the contraindications to proparacaine use?
Long term corneal use --> toxic
55
What ester anesthetic is a class 1a antiarrhythmic
Procainamide
56
What ester analgesic is not used as a local anesthetic but is present in some Penicillin G preparations
Procaine
57
What ester analgesic is VERY toxic to cats and can cause Heinz body anemia and blood dyscrasia
Benzocaine
58
What nociception process is least affected by the administration of local anesthetic drugs ?
Perception | Projection
59
What two nocicpetion processes are affected by NSAIDs ?
Transduction and modulation
60
What is the main effect of NSAID
Inhibiting cyclooxygenase (COX) enzymes
61
What is the role of COX1 enzyme
Production of prostaglandins Mediates Thromboxane A2 -> platelet aggregation Prostaglandin E1 -> maintain GI mucosa
62
What is the role of COX2
Production of prostaglandin in times of inflammation
63
what are the COX2 selective inhibiton NSAID
``` Carprofen Derocoxib Robenacoxib Firocoxib Meloxicam Piroxicam ```
64
What are the non-selective COX1 and COX2 inhibitors
Phenylbutazone | Flunixin meglumine
65
What is a selective COX1 inhibitor
Aspirin
66
T/F: NSAID are all weak bases
F Weak acids
67
What are the 4 effects of NSAIDs
Anti-inflammatory -> inhibit eicosanoids synthesis (thromboxane, prostacyclin, and prostaglandin) Analgesic -> decrease PG sensitization of neurons Antipyretic -> reduce fever Antiendotoxic (if given before endotoxic challenge)
68
What is the strongest acid of NSAIDs
Aspirin ->salicylic acid
69
What is a COX1 selective inhibitor
Aspirin
70
What are the non specific COX inhibitors
Flunixin Phenylbutazone Ketoprofen
71
What are the COX2 preferential inhibitors
Deracoxib Carprofen Meloxicam
72
What are the COX2 selective inhibitors
Firocoxib | Robenacoxib
73
T/F: NSAIDs can cross the BBB
T
74
Where does NSAID metabolism take place and how are NSAIDs excreted?
Liver Urine and Biliary excretion (some NSAIDS have enterohepatic recirculation)
75
Antithrombotic effect of NSAID?
Inhibits thromboxane A2 -> no platelet aggregation
76
What are the antineoplastic effects of NSAIDs
COX2 is expressed by some cancers Eg Transitional cell carcinoma Osteoscarcoma
77
What NSAID is used often for its antineoplastic effects?
Piroxicam
78
What are the adverse effects of using NSAIDs
GI irritation/ ulceration -> prostaglandins maintain GI homeostasis Renal damage and decreased blood flow -> PG control vasodilation --> decrease renal flow and papillary necrosis Post operative analgesia and hypotension Hepatotoxicity (acetaminophen metabolized to toxic intermediate)
79
What species is at a higher risk of renal damage from NSAIDs?
Cats
80
What drug is commonly used for colic/visceral pain in horses/cattle?
Flunixin Meglumine
81
What is the proper route of administration of Flunixin Meglumine
PO, IV, IM Do NOT give IM to horse -> muscle necrosis
82
What species should you avoid using Flunixin Meglumine in due to its renal toxicity in
Birds
83
What drug is commonly used in horses to treat musculoskeletal pain
Phenylbutazone
84
What are the route of admin for Phenylbutazone
PO or IV
85
What is a washout period and when should you use one
Period, based on half life, that it takes for a drug to leave the system (usually 1-2wks) Changing from steroid to NSAID Changing from two different NSAIDs
86
What is the MOA of acetaminophen
Interferes with convertibility endoperoxides to PG and TX
87
When is acetaminophen used clinically?
Dogs -sometimes after neurological surgery NEVER in cats
88
What are the toxic effects of Acetaminophen ?
Methemoglobinemia->MOST important Hepatic necrosis Hemolysis, icterus, anemia, Heinz bodies Facial swelling, edema
89
What non-NSAID is an antagonist at prostaglandin E2 (PGE2) EP4 receptor
Grapiprant what
90
What is used to control neuropathic pain and prevent allodynia in dogs, cats, and horses
Gabapentin Pre-emptively for acute pain or treat laminitis
91
What are the precautions to using Gabapentin
Sedation/ataxia ->dose dependent effects Renally excreted-> caution in renal insufficiency
92
What is used to treat neuropathic pain or dorsal horn "windup" pain
Amantadine Less common in small Amina's
93
What is the MOA of Amantidine
Antiviral with NMDA receptor antagonist
94
``` Which of the following drugs is NOT a selective COX2 inhibitor ? A. Carprofen B. Phenylbutazone C. Robenacoxib D. Meloxicam ```
B. Phenylbutazone
95
What is the mechanism of action for the antithrombotic effects of aspirin
Irreversible thromboxane A2 inhibition Binds to thromboxane receptor on platelet for the lifespan of the receptor (8-10days)
96
Why is IM injection of flunixin meglumine contraindicated in horses?
Risk of muscle necrosis
97
Do you use NSAIDs with glucocorticoids
NO! ARE YOU INSANE!?!?!?

RUSVM Pharmacology (18 decks)

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