Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Introduction to Pharmacology > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

What are the 2 classifications of NSAIDs?

A
  1. inhibitors of prostanoids (PGs, TXA2)
  2. miscellaneous anti-inflammatory drugs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

NSAID mechanism of action:

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What 5 NSAIDs commonly used in humans can cause poisoning in small animals?

A
  1. Aspirin
  2. Acetaminophen
  3. Ibuprofen
  4. Indomethacin
  5. Naproxen
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are 9 signs of NSAID toxicity in animals?

A
  1. GI ulceration, hemorrhage, and perforation**
  2. vomiting
  3. diarrhea
  4. hepatotoxicity
  5. renal toxicity
  6. cardiovascular and blood toxicity
  7. CNS depression
  8. circulatory disturbances
  9. drug-drug interactions
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What does COX-1 usually due in the GI mucosa? What happens when it is inhibited?

A

produces PGE2 responsible for gastric protection
- increases mucus secretion
- increases bicarbonate
- increases mucosal blood flow

peptic ulcers, GI bleeding

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What do COX-1 and COX-2 do in the kidneys? What happens when they’re inhibited?

A

produces PGE2 and PGI2 responsible for afferent arteriolar vasodilation which increases GFR and increases Na and water excretion

  • Na and water retention
  • hypertension
  • hemodynamic acute kidney injury
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What do COX-1 and COX-2 do in the cardiovascular system? What happens when they’re inhibited?

A

produces PGI2
- vasodilation
- inhibition of platelet aggregation

produces TXA2
- vasoconstriction
- platelet aggregation

COX-2 > COX-1 —> stroke, myocardial infarction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

NSAID side effects:

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are the 8 desirable features of NSAIDs?

A
  1. deactivate/desensitize nociceptors - decreases pain
  2. attenuates inflammatory response
  3. synergistic with opioids
  4. no addiction or dependence
  5. no respiratory depression
  6. minimal nausea/vomiting
  7. long duration of action
  8. no cognitive side effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

How do COX-1 and COX-2 compare? Why is drug selectivity important?

A

COX-1 = mediates physiological responses, like GI protection and platelet aggregation
COX-2 = expressed by cells involved in inflammation, like macrophages and monocytes and is responsible for the synthesis of PGs and TXA2

selective inhibition of COX-2 may have better therapeutic responses

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

How is the selectivity of an NSAID expressed? What is the inhibitory effect?

A

selectivity of COX-2 vs COX-1 = COX1/COX2

(IC50) = COX1/COX2 > 1 = drug more specific for COX2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What are 5 dual inhibitors of the LOX and COX pathway?

A
  1. Tepoxalin (Zubrin)* - approved in Europe and America for osteoarthritis in dogs
  2. Benoxaprofen
  3. Ketoprofen
  4. Licofelone
  5. Corticosteroids - adverse effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are the 4 major classifications of NSAIDs? What are some examples of each?

A
  1. selective COX-1 inhibitors - low-dose aspirin
  2. non-selective COX inhibitors - Naproxen (Aleve), Ibuprofen (Motrin, Advil), Ketoprofen (Anafen), Aspirin, Flunixin meglumine
  3. selective COX-2 inhibitors - Meloxicam, Etodolac, Phenylbutazone, Carprofen, Deracoxib, Firocoxib, Robenacoxib
  4. dual inhibitors - Tepoxalin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are the main side effects associated with the different classifications of NSAIDs?

A
  1. selective COX-1 inhibitors - GI ulceration, excessive bleeding
  2. non-elective COX inhibitors - paradoxical hyperpyrexia
  3. selective COX-2 inhibitors - increased blood clotting, stroke
  4. dual inhibitors - none to note
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

NSAID classification and adverse effects:

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Currently available NSAIDs for dogs:

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What are the 4 main uses of Aspirin? How is it used in low doses?

A

reduces pain, fever, inflammation, and platelet aggregation

prevents heart attacks and strokes (myocardial infarction)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is Aspirin derived from?

A

salicylic acid from willow bark is modified into acetyl salicylic acid (ASA) = Aspirin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What is the mechanism of action of Aspirin? What are the 4 major effects?

A

irreversibly inhibits COX-1, resulting in decreased PG and TXA2 synthesis

  1. analgesic
  2. antipyretic
  3. anticoagulant - reduced platelet aggregation
  4. anti-inflammatory - reduced PG expression
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What adverse effects are common with Aspirin usage in cats, dogs, and sheep?

A

CATS: sensitive to aspirin toxicity (long half-life)

DOGS: sensitive to GI effects (bleeding), chronic use in dogs with OA can aggravate joint disease

SHEEP: pulmonary edema

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What are 6 common adverse effects of Aspirin? What drug does Aspirin commonly interact with?

A
  1. GI distress: vomiting, diarrhea, anorexia, ulceration
  2. paradoxical hyperpyrexia (>106.7 F)
  3. hyperventilation, respiratory acidosis
  4. metabolic acidosis
  5. dehydration
  6. chronic use = bleeding during surgery

Warfarin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

In what 4 ways is Aspirin toxicity treated?

A
  1. induce emesis in cases of acute toxicity
  2. increase removal of the drug by gastric lavage followed by administration of activated charcoal
  3. increase urinary excretion by administering alkalizing agents
  4. initiate IV fluid therapy to address dehydration and metabolic acidosis
23
Q

In what 4 situations is it contraindicated to use Aspirin?

A
  1. active GI bleeds
  2. bleeding disorders
  3. asthma
  4. renal insufficiency
24
Q

What is Flunixin meglumine (Banamine)? How does its mechanism of action compare in horses and dogs?

A

non-selective COX inhibitor with potent analgesic and anti-inflammatory effects

HORSES = greater COX-2 selectivity
DOGS = greater COX-1 selectivity

25
Q

What exceptional property does Flunixin meglumine (Banamine) have? How is it used in horses and cattle?

A

alleviates visceral pain related to colic
- treats acute, visceral, and surgical pain

HORSES = longest duration of postoperative analgesia (~13 hrs)
CATTLE = controls pyrexia associated with respiratory disease, endotoxemia, and mastitis (not FDA-approved)

26
Q

What are 3 adverse effects of Flunixin meglumine (Banamine)?

A
  1. myonecrosis upon IM injection
  2. overdose in horses causes ulcers on the tongue, gingiva, lips, and stomach; CNS depression, and anorexia
  3. dogs: renal failure and GI damage
27
Q

What is Ketoprofen (Ketofen)? What is its mechanism of action? When is it most commonly used?

A

non-selective COX inhibitor with anti-inflammatory and analgesic effect

inhibits COX-1, COX-2, and LOX pathway (lowers LTB4 synthesis)

horses with acute and chronic musculoskeletal disorders

28
Q

How does Ketoprofen (Ketofen) compare to flunixin and phenylbutazone? What are 3 possible adverse effects?

A

safer profile

  1. PO administration can cause GI injury including ulceration and bleeding
  2. caution in animals with hemostatic disorders
  3. caution in animals with compromised renal function
29
Q

What is the most commonly used NSAID in horses? What is its mechanism of action?

A

phenylbutazone, especially used as an analgesic for racehorses due to its safety, efficacy, and affordability

preferential COX-2 inhibitor in both horses and dogs

30
Q

What are the 5 most common uses of Phenylbutazone?

A
  1. osteoarthritis
  2. lameness
  3. rheumatism
  4. other painful conditions of the limbs
  5. nonspecific inflammation in other conditions
31
Q

What active metabolite does Phenylbutazone produce? What are 3 adverse effects?

A

oxyphenylbutazone

  1. GI distress: erosions, ulcers, anorexia, colic, diarrhea
  2. renal papillary necrosis
  3. death by hypovolemia, shock, and ulcer-mediated sepsis
32
Q

When is it contraindicated to use Phenylbutazone?

A

patients with serious cardiac, renal, or hepatic injury, or hematologic disorders

33
Q

What is Carprofen (Rimadyl)? What is its mechanism of action? What is it commonly used for?

A

preferential COX-2 inhibitor with analgesic and anti-inflammatory effects

potency for canine COX-2 is more than 100x relative to canine COX-1

short- and long-term pain management and musculoskeletal disorders

34
Q

What are the main 3 adverse effects of Carprofen (Rimadyl)? How does this compare to other NSAIDs? In what patients is it not recommended for use?

A

diarrhea, anorexia, vomiting

lower frequency of GI ulceration and hemorrhage

  • patients with hepatic or renal dysfunction and hemostatic disorders
  • pregnant, lactating, or breeding bitches
35
Q

What is Meloxicam (Metacam)? What is its selectivity ratio? When is it used?

A

preferential COX-2 inhibitor with analgesic and anti-inflammatory effects

COX-2/COX1 = 10

chronic pain and inflammation related to osteoarthritis and surgery (FDA-approved in cats)

36
Q

Meloxicam (Metacam) is a relatively safe NSAID in dogs and cats. What are 3 possible adverse effects? What caution should be taken with cats?

A
  1. GI distress
  2. anemia
  3. lethargy
    - rare and transient

repeated use can evoke acute renal failure and death

37
Q

When is it contraindicated to use Meloxicam (Metacam)?

A

pregnant, lactating, or young animals < 4 months

38
Q

What is Etodolac (EtoGesic)? When is it most commonly used?

A

preferential COX-2 inhibitor with analgesic and anti-inflammatory effects

dogs with osteoarthritis

39
Q

What is a unique adverse effect of Etodolac (EtoGesic)? What else can it cause? When is use contraindicated?

A

may cause keratoconjunctivitis sicca in dogs (monitor tear production)

GI distress, CNS depression, hepatotoxicity, nephrotoxicity

patients with hematological, renal, or hepatic impairment

40
Q

What is Tepoxalin (Zubrin)? What is its mechanism of action?

A

dual inhibitor: non-selective COX inhibitor with potent effect on LOX

inhibits COX-1, COX-2, and 5-LOX, which reduces the production of prostaglandin mediators of pain, fever, and inflammation

41
Q

In what 3 situations is Tepoxalin (Zubrin) used?

A
  1. osteoarthritis in dogs
  2. allergic conditions in dogs
  3. postoperative pain control
42
Q

What are 4 common adverse effects of Tepoxalin (Zubrin)?

A
  1. GI distress: vomiting, diarrhea, anorexia, ulceration
  2. CNS depression
  3. hepatotoxicity
  4. nephrotoxicity
43
Q

What are the 2 selective COX-2 inhibitors?

A

(“coxibs”)
1. Deracoxib (Deramaxx) - dogs
2. Firocoxib (Previcox, Equicox) - dogs, horses

44
Q

When is Deracoxib and Firocoxib used?

A

D = osteoarthritis and post-operative pain/inflammation in dogs

F = osteoarthritis in horses and dogs

45
Q

What are the most common adverse effects of Deracoxib? Firocoxib?

A

D = GI distress

F = horses: diarrhea, mouth ulcers, excitation
dogs: vacuolization in the brain at high doses

46
Q

Which NSAIDs are rarely used in veterinary medicine?

A

non-selective COX inhibitors
- Aspirin
- Acetominophen (Tylenol): particularly unsafe in cats
- Ibuprofen (Motrin, Advil)
- Naproxen (Aleve): can treat myositis and lameness in horses
- Indomethacin

47
Q

What is dimethyl sulfoxide (DMSO)? What are 6 common effects?

A

miscellaneous anti-inflammatory that is a solvent for many aromatic, organic, and inorganic compounds (colorless, straw-yellow, highly hygroscopic)

  1. anti-inflammatory: inhibits PG synthesis and traps free radicals
  2. diuretic
  3. analgesic
  4. skin penetrating
  5. anticholinesterase
  6. weak antibacterial/antifungal
48
Q

In what 9 situations is dimethyl sulfoxide (DMSO) commonly used?

A
  1. acute swelling (musculoskeletal trauma)
  2. cerebral edema and paralysis from spinal cord trauma
  3. cystitis (urethral obstruction in cats)
  4. superficial burns
  5. skin grafts
  6. transient ischemic conditions
  7. edema of limbs from fractures
  8. swelling and engorgement of mammary glands
  9. severe inflammation resulting from extravascular injection of irritating drugs or lick granulomas
49
Q

What are 5 possible adverse effects of dimethyl sulfoxide?

A
  1. transient local effects
  2. high dose, long usage = myopia
  3. IV = hemolysis, hemoglobinuria
  4. hepatic and renal damage, pulmonary edema
  5. CNS: sedation, coma, seizures
50
Q

What is osteoarthritis? What usually protects joints from this?

A

degenerative joint disease that affects the spine and lower limbs leading to stiffness and excruciating pain

synovial lining and synovial fluid usually ensure smooth and easy bothy movement (hyaluronic acid is the natural lubricant of the joints and found in SF)

51
Q

What is polysulfated glycosaminoglycan (PSGAG), or Adequan? What are its 2 mechanisms of action?

A

disease-modifying osteoarthritis drug (DMOAD)

modulates clinical signs of OA by indirectly promoting chondroprotective effects
- improves joint articular function by affecting synovial fluid
- anti-inflammatory: inhibits PGE2 biosynthesis, leukocyte migration, and IL levels

52
Q

How is polysulfated glycosaminoglycan (PSGAG), or Adequan used in dogs and horses? What is the most common adverse effect?

A

DOGS = treat OA and prevent hip dysplasia
HORSES = treat traumatic joint dysfunction

associated with drug administration - septic arthritis

53
Q

What are the 3 mechanisms of action of hyaluronate sodium? How is it used in dogs and horses?

A
  1. cushioning - reduces cell migration
  2. lubricating effect on articular soft tissue
  3. scavenges and removes O2-derived free radicals

treats synovitis associated with OA

54
Q

What are 6 general guidelines for the safe use of NSAIDs?

A
  1. individualize dosage based on drug’s efficacy, age of the animal, and duration of action
  2. screen patients for underlying renal and hepatic dysfunction
  3. monitor hydration status - hypovolemic animals should not be placed on NSAIDs
  4. allow an adequate wash out period prior to administering
  5. administer the lowest possible dose for the shortest period of time to minimize injury risk
  6. concurrent use of glucocorticoids and NSAIDs should be avoided due to increased risk of GI complication

Introduction to Pharmacology (39 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions