Pharmacology of Analgesic Agents II: NSAIDs & NSAID-like Drugs Flashcards

1
Q

What pKa is expected of an NSAID?

A

3-5 (weak acid)

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2
Q

NSAIDs are considered highly…

A

protein bound

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3
Q

What are the main routes of administration of NSAIDs?

A

IV, SQ, PO, IM

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4
Q

NSAIDs are metabolised in the

A

liver, go through enterohepatic circulation

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5
Q

NSAIDs are excreted by the

A

kidney

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6
Q

What are the main effects of NSAIDs?

A
  • anti-inflammatory (local)
  • analgesia (local & systemic)
  • antipyretic
  • antiendotoxic
  • anti-thrombotic
  • antispasmodic
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7
Q

What are adverse effects of NSAIDs?

A

GIT & kidney mostly

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8
Q

What are GIT adverse effects from NSAIDs?

A
  • V/D
  • melena
  • ulcers
  • anorexia
  • STOP ADMIN IMMEDIATELY
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9
Q

What are renal adverse effects of NSAIDs?

A

Vasoconstriction (afferent/efferent blood vessels) –> glomerular dysfxn –> renal failure

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10
Q

What are the two different ways of classifying NSAIDs?

A
  • Physiochemical properties (carboxylic acids, enolic acids, coxibs)
  • according to action on COX (non-selective, COX-2 selective, COX-2 specific, Dual inhibitors)
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11
Q

Phenylbutazone

Give routes, classification, animals used in, cautions

A
  • Classification: Non-selective COX inhibitor (COX-1 activity)
  • Routes: PO, IV
  • Animals: horses, dogs w/ caution
  • Illegal in animals for human consumption
  • Caution: hepatotoxicity in dogs
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12
Q

Flunixin meglumine

Give routes, classification, animals used in, cautions

A
  • Classification: Non-selective COX inhibitor (COX-1)
  • Routes: PO, IV, some in IM prep
  • Animals: Horses, large animals
  • Caution: severe renal effects in dogs
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13
Q

Meloxicam

Give routes, classification, animals used in, cautions

A
  • Classification: COX-2 selective
  • Routes: PO, SQ, IV
  • Animals: dogs, cats, horses, cattle
  • Cautions: less side effects
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14
Q

Carprofen

Give routes, classification, animals used in, cautions

A
  • Classification: COX-2 selective
  • Routes: PO, IV, IM, SQ
  • Animals: dogs, cats, cattle
  • Caution: idiosyncratic liver failure in dogs (Golden retrievers), dogs love to eat the chews –> easy to overdose if eat the bottle
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15
Q

Robenacoxib (Onsior)

Give routes, classification, animals used in, cautions

A
  • Classification: Highly COX-2 selective
  • Routes: PO, SQ
  • Animals: dogs, cats
  • Cautions: CAUTION in hyperproteinaemia
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16
Q

Ketoprofen

Give routes, classification, animals used in, cautions

A
  • Classification: Non-selective COX inhibitor (COX-1)
  • Routes: PO, Injection
  • Animals: Pigs
  • Cautions: not licensed in perioperative period
17
Q

Firocoxib (Previcox)

Give routes, classification, animals used in, cautions

A
  • Classification: COX-2 selective
  • Routes: oral, others?s
  • Animals: horses, dogs
  • Cautions: Not licensed in perioperative period
18
Q

Cimicoxib (Cimalgex)

Give routes, classification, animals used in, cautions

A
  • Classification: ?
  • Routes: ?
  • Animals: Dogs
  • Cautions: not licensed in perioperative period
19
Q

Paracetamol

Give routes, classification, use, animals used in, cautions

A
  • Routes: PO, IV
  • MOA: inhibition of COX-3, weak COX-1/2 inhibition, endocannabinoid, vallinoid
  • Use: Analgesia, antipyretic
  • Animals: NOT IN CATS
  • Cautions: saturation of gluronide pathway, production of NAPQI, inadeq glutathione availability –> Toxicity (cell & protein damage, methaemoglobinaemia, hepatic necrosis)
20
Q

Grapiprant (Galliprant)

Give routes, classification, use, animals used in, cautions

A
  • Classification: Non-COX-inhibiting PGE2EP4 receptor antagonist
  • Route: Oral, others?
  • Use: OA in dogs
  • Animals: Dogs
  • Cautions: V in the beginning of txt
21
Q

Gabapentin

Give routes, classification, use, animals used in, cautions

A
  • Route: Oral, other?
  • Classification: Structural analoge of GABA, does not act on GABA
  • MOA: blocks Ca2+-gated channels on neurons, possible NMDA antagonism, opioid antagonist, Na+ or monoaminergic pathways
  • Use: neuropathic pain
  • Animals: dogs/cats
  • Cautions: Assoc’d w/ foetal loss & teratogenic effects in lab settings
22
Q

Pregabalin

A

Use: neuropathic pain in dogs
Like gabapentin but $$$

23
Q

Amitriptyline

Give routes, classification, use, animals used in, cautions

A
  • Routes: oral only
  • Classification: tricyclic antidepressant
  • Use: behavioural disorders, FLUTD, neuropathic pain
  • Animals:
  • Cautions: tachycardia, fatal V-tach, hypersalivation, V, weight gain, sedation, serotonin syndrome
24
Q

Ketamine

Give routes, classification, use, animals used in, cautions

A
  • Route: ?
  • Classification: Dissociative anaesthetic agent, NMDA-receptor antagonist
  • Use: Anaesthetic agent, chronic pain mgmt
  • Animals: ?
  • Cautions: CV depression in shock/moribund animals
25
Q

Amantadine

Give routes, classification, use, animals used in, cautions

A
  • Route: Local, oral
  • Classification: Dopamine agonist, NMDA antagonist
  • Use: chronic pain, arthritis, neuropathic pain
  • Animals: ?
  • Caution: serotonin syndrome, CNS stimulation
26
Q

Memantine

Give routes, classification, use, animals used in, cautions

A
  • Route: Liquid, tablets
  • Classification: Non-competitive inhibitor of NMDA receptor
  • Use: chronic pain, arthritis, neuropathic pain? Alzheimer’s txt, Canine cognitive dysfunction txt
  • Animals: ?
  • Cautions: possible abuse potential
27
Q

What is serotonin syndrome?

A

Variety of clinical signs caused by excessive serotonin in the body

28
Q

What are clinical signs of serotonin syndrome?

A
  • V/D
  • changes in conscious state (anxious, restless)
  • autonomic dysfxn (hypertension, tachycardia, hyperthermia)
  • neuromuscular signs (muscle rigidity & tremors, seizures)
29
Q

How do you treat serotonin syndrome?

A
  • discontinuarion of drugs
  • gastric lavage
  • supportive care