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Pain Medications Flashcards

1
Q

Aspirin
-COX selectivity
-Effect
-Disposition/Elimination

A

-inhibits COX in all tissues (COX-1>COX-2)
-decrease kinins, stabilizes lysosomes, removes energy for oxidative phosphorylation, irreversible platelet defects by suppressing TxA
-50-70% bound to albumin, hepatic elimination, renal excretion

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2
Q

Asprin
-adverse reaction
-Dog vs cats

A

-chondrotoxic (decreases GAG)
-hepatoxicity, nephrotoxicity
Dogs: dose-dependent gastric ulceration
Cats: glucuronidation deficient

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3
Q

Flunixin Meglumine
-COX selectivity
-Effect
-Dog vs cats

A

-nonselective COX inhibitor, approved for horses
-visceral pain, anti-endotoxic effects in septic shock
Dogs: visceral or PO pain
Cats: enterohepatic circulation

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4
Q

Ibuprofen
-COX selectivity
-effect
-reactions
-Dog vs cats

A

-propionic acid derivative, nonselective COX inhibitor
-anti-inflammatory, less effective than aspirin
-LEAST SAFE NSAID in dogs –> GI signs, death
-Dogs, AVOID

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5
Q

Ketoprofen (UK)
-COX selectivity
-effects
-Disposition/Elimination

A

-propionic aci derivative (COX 1 selective)
-Strong anti-inflammatory, analgesic, and antipyretic
-inhibits bradykinin
-99% protein bound, hepatic metabolism, urine excretion

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6
Q

Ketoprofen (UK)
-adverse reactions
Dogs vs cats

A

-Upper GI upset
-CNS (headaches, dizziness)
-Nephritis
Dogs: analgesia for 12-24 hr
Cats: rapid antipyretic, analgesia 8h

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7
Q

Ketorolac
-COX selectivity
-effects
-adverse reactions

A

-Carboxylic acid derivative
-Cox inhibitor (COX-1>COX2)
-moderately effective as anti-inflammatory, potent analgesic
-GI upset

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8
Q

Naproxen
-COX selective
-Disposition/elimination
-Dogs vs Cats

A

-proprionic acid derivative, non-selective COX inhibitor
-extensive enterohepatic circulation
Dogs: AVOID, GI toxicity, long half life

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9
Q

Phenylbutazone
-COX selective
-effects
-disposition/elimination

A

-pyrazolidine, nonselective COX inhbitor (slightly COX 2 > COX 1)
-decreased pain and swelling due to inhbition of PGH synthase and prostacyclin synthase
-hepatic metabolism
-excretion in urine

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10
Q

Phenylbutazone
-adverse effects
-Dogs vs cats

A

-Chondrodistructive effects
-hemorrahge, biliary stasis, hepatitis, renal failure, blood dyscrasias
Dogs: more tolerant
Cats: AVOID, high incident of toxicity with 80% mortality, toxicity in bone marrow

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11
Q

Piroxicam
-COX selective
-effects
-Dogs vs cats

A

Non-selective COX inhibitor
-potent anti-inflammatory, reduces bladder TCC
Dogs: gastric lesions and renal papillary necrosis
Cats: shorter half life

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12
Q

Tolfenamic Acid (UK)
-COX selective
-effects
-disposition/elimination

A

-Anthranilic NSAID, nonslective COX inhibitor
-anti-inflammatory and antipyretic
-enterohepatic circulation

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13
Q

Tolfenamic Acid (UK)
-adverse effect
Dogs vs cats

A

-use only for 3 days and can be repeated weekly
Dogs: approved for long term use
Cats: approved for short term use

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14
Q

Indomethacin
-COX selective
-effects
-adverse effects

A

-indole acetic-acid derivative, non-selective COX inhibitor
-abate inflammatory response to indolic hormones (serotonin and tryptophan)
-CNS side effects in humans
-Dogs: GI hemorrhage from gastric ulcers

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15
Q

Carprofen
-COX selective
-Effects
-Disposition and elimination

A

COX 2 selective
-MOA not understood, inhibit eicosanoid synthesis, antipyretic, analgesic, anti-inflammatory
-highly protein bound, hepatic metabolism, 70-80% excreted in feces

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16
Q

Carprofen
-adverse reactions
-Dogs vs cats

A

-minimal side effects and limited to GI toxicity due to favorable COX 1:COX 2 ratio
-hepatotoxicity, nephrotoxicity, high doses inhibit polysulfated glycosaminoglycan synthesis
Dogs: safe
Cats: half life twice as long, COX 2 selectivity not proven

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17
Q

Vedaprofen
-COX selectivity
-Adverse reactions

A

-COX 2 selective
-safety comparable to meloxicam
-GI side effects in 11-12%

18
Q

Mavacoxib (UK)
-COX selectivity
-Disposition/elimination
-Dogs vs cats

A

-COX 2 selective
-very slow clearance, therapeutic concentrations maintained for 1 month
-half life 40 days
-biliary tract elimination
Dogs: treatment cycle not exceeds 6.5 months

19
Q

Deracoxib
-COX selectivity
-effect
-Disposition/elimination

A

-COX 2 selective, but loses specificity at higher concentrations
-limited efficacy in dogs
-half life 3h

20
Q

Deracoxib
-adverse effects
Dogs vs cats

A

-GI toxicity
-may cause sulfonamide related reactions–> KCS
-Dogs: not evaluated in dogs <4mths, not evaluated in pregnant or lactating animals

21
Q

Firocoxib
-COX selective
-effects
-disposition/elimination

A

-HIGHLY COX 2 selective
-analgesia, anti-inflammatory
-large volume of distribution and rapid clearance —> SID dosing

22
Q

Firocoxib
-adverse effects
-Dogs vs cats

A

-fatty liver in young dogs
-juvenile polyarthrits, thrombocytopenia, decreased albumin and elevated liver enzymes
-Dogs: avoid in <6mth

23
Q

Robenacoxib
-COX selective
-effects
-disposition/elimination

A

-COX 2 selective
-analgesia, anti-inflammatory
-great targeting to sites of inflammation–> SID dosing
-efficacy HIGH when given WITHOUT food, hepatic metabolism, primarily biliary excretion

24
Q

Meloxicam
-COX selective
-effects
-disposition/elimination

A

-COX 2 selective
-analgesia, anti-inflammatory
-potent (low dosing)
-100% oral bioavailability

25
Meloxicam -adverse effects Dogs vs cats
-Low GI and renal toxicity -GI perforation when given with underlying GI disease - Dogs: safe and effective for OA -Cats: shorter half life, narrow therapeutic margin with renal disease Cats: licensed for long term use in cats with OA in Europe, Australia, NZ
26
Etodolac -COX selective -effects -disposition/elimination
-Carboxylic acid (indole), COX 1 sparing -Primarily inhibits COX 1 -anti-inflammatory effects to interference with macrophage chemotaxis, anti-inflammatory by inhibiting chondrocyte and synoviocyte synthesis of PGE-2 -food prolongs elimination, biliary excretion and enterohepatic circulation
27
Etodolac -adverse effects Dogs vs cats
-GI toxicity -decreased TP, albumin, and globulin -KCS Dogs: not used, caution with hepatic, renal or hematologic dysfunction
28
Acetaminophen -MOA -effects Dogs vs cats
-NO COX INHIBITION -poor anti-inflammatory -potent analgesic (cannabinoid receptors) and antipyretic , -stimulate inhibitor pain by activating serotonin receptors -interferes with endoperoxide intermediates of AA conversion Dogs: safe with no renal or gastric injury, depression, MetHb, vomiting Cats: NOT TO USE, requires glucuronidation, form toxic metabolites --> metHb and hepatic necrosis
29
Amantadine -MOA -Effects Dogs vs cats
-NMDA receptor antagonist -neurobiologic changes underlying sensory disturbances with prolonged inflammatory pain -Dogs: benefits when given with meloxicam
30
Gabapentin -MOA -effects -disposition/elimination -adverse effects
-GABA analog, suspect involving voltage gated calcium channels -neuropathic pain -excreted by kidney -dizziness, drowsiness, peripheral edema
31
Codeine (methylmorphine) -MOA -effect -disposition/elimination
-natural alkaloid found in opium -no reports on OA in dogs, -metabolized in vivo to morphine (5-10%), codeine -6-glucuronide (70%), norcodeine (10%) , hydromorphone (1%)
32
Corticosteroids -effects -adverse effects
-IA injections for joint inflammation with minor systemic absorption -long lasting: methylprednisone acetate, triamcinolong acetonide, triamcinolone hexacetonide -with multiple uses may cause harmful effects on cartilage
33
Polysulfate glycosaminoglycans (adequan) -MOA -effects -Dogs vs cats
-MOA unknown -maintain chondrocyte viability, stimulates chondrocyte division and protects against ECM degradation -Dogs: IM twice weekly for 4 weeks
34
Chondroitin sulfate -MOA -effects -disposition/elimination
-MOA unknown -not to used in intact articular cartilage -anti-inflammatory effect, reduce neutrophil and macrophage infiltration in soft tissues -5% bioavailability in dogs after single dose
35
Glucosamine sulfate or hydrochloride -MOA -effects -disposition/elimination
-MOA unknown -may influence chondrocyte metabolism by increases glycosaminoglycan synthesis and stimulating proteoglycan core protein production -weak anti-inflammatory -90% absorbed
36
Essential fatty acids -MOA -effects -disposition/elimination
-compete for incorportation into phospholides as substrains for COX-1, COX 2, and 5-lipoxygenase -N-3: antiinflammatory: reduce mRNA levels for COX2 -N-6: inflammatory -promotes produciton of inflammatory prostoglandins, leukotrienes, and thromboxanes -Eicosapentaenoic acid most effect n-3 anti-inflammatory fatty acids
37
Zileuton -MOA -Effects -Adverse effects
-selective 5-LOX inhibitor -limited efficacy -hepatotoxicity
38
Tepoxalin -MOA -effects -disposition/elimination
-Nonselective COX and LOX inhibitor -Anti-inflammatory (inhibits COX 1, COX2, 5-LOX) -Analgesic- inhibits IL1 and NFKappaB -effect on leukotriene activity may be responsible for protection against GI toxicity -enhance absorption with food, highly protein bound, hepatic metabolism, eliminated in feces
39
Tepoxalin -adverse effects Dogs vs cats
-GI toxicity in 10% -Hepatotoxicity-inhibit other redox-active systems -Dogs: ameliorate degradation of collagen -Cats: well tolerated SID, antipyretic, analgesic
40
Licofelone -MOA -effects -dogs vs cats
-di-tert butylphenol -impairs PDE production, prevent formaiton of LTB4, anti-oxidant Dogs: not approved for use
41
Pentoxifylline -MOA -effects -disposition/elimination
-leukotriene receptor anatagonist -anti-inflammatory, inhibits IL1 IL6 TNFa -**increases flexibility of RBCs and decreases blood viscosity -hepatic metabolism

Drugs (3 decks)

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