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1. Pharmacology > NSAIDS > Flashcards

NSAIDS Flashcards

(58 cards)

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1
Q

Non-steroidal anti-inflammatory drugs that include:

A

Over the counter (OTC)
Prescription
Non-opiods

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2
Q

Clinical uses of NSAIDS

A

Musculoskeletal pain (OA, muscle, tendon/lig, fracture)
Visceral pain (abdominal and thoracic)

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3
Q

Pain pathway intervention

A

Anti-inflamm. agents, COX 2 inhibitor

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4
Q

COX 1(constitutive)

A

Housekeeping function: physiological stimuli
PGI2: renal function
TXA2: platelet function
PGE2: gastric protection

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5
Q

PGI2 (prostacyclin)

A

Localized in vasculature tissue
Potent vasodilator
Exerts antiaggregaotry activity on blood platelets

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6
Q

TXA2 (thomboxane)

A

Vasoconstrictor and proaggregate in thrombus formation
Dominates in platelets

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7
Q

PGE2

A

Direct vasodilator
Relaxes smooth muscle
Inhibits NE release
Suppresses T cell receptors signaling
Fever

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8
Q

COX2 (inducible)

A

Pathological condition: inflammatory stimuli
Inflammatory sites (macros) → Pro-inflammatory PGs and other inflammatory mediators → Inflammation

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9
Q

NSAIDs are more selective for __________

A

COX2

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10
Q

Screening test: COX ratio

A

IC50 (COX1) :IC50 (COX 2)
Compare potency of drug towards COX isofroms

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11
Q

<1 or close to 1 COX ratio

A

Less concentration to inhibit COX1
More concentration to inhibit COX2
Classic NSAID

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12
Q

> 1 COX ratio

A

Less concentration to inhibit COX2
More potent for COX2
Preferential or selective NSAID

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13
Q

Side effects of prolonged COX 2 inhibition

A

Disturb balance between p PGI2 andp TxA2
LEADING TO ↑ PLATELET AGGREGATION AND VASOCONSTRICTION

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14
Q

Classical NSAIDs

A

Aspirin
Flunixin meglumine
Phenylbutazone
Acetaminophen* (paracentamol)

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15
Q

What do classical NSAIDS do?

A

Inhibits COX 1 and COX2 equally leading to ↓ inflammatory response

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16
Q

Preferential NSAIDs

A

Inhibits COX2 more than COX1
Carprofen and meloxicam

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17
Q

COX2 selective (Coxib) NSAIDs

A

Inhibits COX2 wayyy more than COX1
Firocoxib, robenacoxib, deracoxib

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18
Q

EP4 Antagonist drugs

A

Grapiprant (galiprant)

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19
Q

NSAID adverse effects on the GI tract

A

Gastroduodenal ulcer, GI bleeding
Dogs > cats, horses (colitis)
Most common cause: OVERDOSING
Risk factors: geriatric patients, concurrent use of gluccos

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20
Q

Pathogenesis of COX inhibitors

A

Direct irritation (acid)
Inhibition of gastro protection

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21
Q

Prevention and treatment

A

Accurate dosing
Anti-ulcer drugs: H2 antagonists (famotidine), proton pump inhibitors (omeprazole), PGE analogue (misoprostol)

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22
Q

How do PGs affect the kidney?

A

Insure intramedullary renal blood flow
Urine formation

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23
Q

NSAID Renal adverse effects

A

Analgesic nephropathy
Doesn’t occur in healthy animals with free water
↓ GFR, water retention, hypertension

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24
Q

Patients at risk for renal adverse effects

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A

↓ blood flow to kidneys
Geriatric patients
Concurrent use of nephrotoxic/ active drugs

25
Effects of Classical NSAIDS on normal blood vessels
Inhibits COX 1, COX2 andPGI2 →vasodilation and inhibiting platelet aggregation
26
Effects of classical NSAIDS on damaged BVs
Inhibits COX 1 and TxA2 → vasoconstriction and promotes platelet aggregation
27
Effects of aspirin on BVs (damage and normal)
Prolonged bleeding time (withhold aspirin before surgeries)
28
Effects of Coxib on BVs (damage and normal)
Enhance blood clot formation and induce cardiovascular disease (banned for humans)
29
Hemopoietic NSAID adverse events
Stop platelet aggregation and prolonged bleeding time Bone marrow depression Thromboembolic disease (COX2 selective NSAIDs)
30
What drug cannot be used in cats due to bone marrow depression?
Phenybutazone
31
NSAID effects on Reproduction
Prolonged gestation (inhibition of uterine PGF2 and PGE2) Lysis of corpus luteum Initiates uterine contractions
32
NSAID PK
Weak acids (stomach ulcers), oral absorption Highly > 90% bound to albumin Hepatic Metabolism Enantiomers
33
Acetaminophen (parcetamol)
Inhibition of peroxidase (POX) Centrally acting analgesic and anti-pyretic Poor anti-inflammatory
34
Acetaminophen contraindications
CATS Deficiency in glucuronyl trasnsferase → hepatic toxicity and methemoglobinemia
35
Acetaminophen toxicity treatment
Promote glutathione formation (N-acetylcysteine and SAMe) Microsomal enzyme inhibitor (cimetidine) Anti-oxidants (vitamin C and SAMe)
36
Aspirin
Salicylic acid Hepatic conjugation with glucuronide and renal excretion
37
Adverse effects of aspirin
Irreversible inhibition of platelet activity CS: depression, vomiting, electrolyte imbalances, hyperthermia, convulsions, death, cartilage damage
38
Flunixin meglumine
Nicotonic acid Used for visceral pain (horse colic) and endotoxemia Injectable, oral paste, granules
39
Flunixin meglumine in food animals
Approved for use in cows for pyrexia Prohibited (veal calves and lactating dairy cattle)
40
Adverse effects of Flunixin meglumine
Mask surgical pain in equine patients Gastric ulceration Clostridial myositis from IM injection
41
Phenylbutazone
Pyrazolone (enolic acid) Used for musculoskeletal pain in horses and cattle Used in dogs, toxic in cats
42
Phenylbutazone disposition
Metabolized by liver, highly protein bound (may displace other drugs) Excreted in urine (alkaline ↑ excretion)
43
Phenylbutazone adverse agents
Narrow TI Gastrointestinal ulcerations Low serum protein concentrations Extravasation of IV product Renal papillary necrosis
44
GI ulceration treatment
Proton pump inhibitors (omeprazole) PGE replacement (misoprostol)
45
Carprofen
Proprionic acid First COX2 preferential drug approved in use in animals Treats OA, preoperative management of pain
46
Carprofen adverse effects
Safest of new NSAID Hepatotoxicity Renal tubular disease
47
Meloxicam
Oxicam OA in dogs Post operative pain in cats Popular in zoo, exotic wildlife
48
Meloxicam in dogs and cats
Cats: single dose only, renal failure, death, black box warning Dogs: GI perforation
49
Firocoxib
Canine chew and equine injectable and paste Used for OA Loading dose required
50
Deracoxib
First coxib approved for use in animals For OA in dogs and operative pain
51
Robenacoxib
OA for dogs and cats and post-operative pain Tissue selective - longer at the site of inflamm
52
Gapiprant (galliprant)
EP4 receptor antagonist located @ sensory nerve ending Dogs to control pain and inflamm. (OA)
53
Nerve growth factor
Produced by inflammatory cells Binds to sensory nerve ending (↑ pain signal rate, releases more cytokines and proliferation)
54
NGF Inhibitor
Reduces pain signals Reduce production of inflammatory repsonse Monoclonal Ab Ex: Bedinbetmab (dogs), frunevetmab (cats)
55
Bendinvetmab (Librela in dogs)
Monthly SC injection for OA pain in dogs Contraindication: hypersensitivity, dogs under 12m, lactating, breeding or pregnant animals
56
Frunevetmab (Solensia in cats)
Pain due to OA, monthly Sc injection Contraindications: Under 12 m or under 2.5 kg, breeding, lactating or pregnant animals
57
Side effects of frunevetmab
Scabbing on head and neck, dermatitis and pruritus
58
Contraindications for NSAIDs
Acute renal and hepatic insufficiency Dehydration Hypotension ↓ circulating blood volume: CHF ascites, hemorrhage, shock Bleeding disorders/ coagulapathies GI ulceration

1. Pharmacology (29 decks)

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