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Pharmacology > NSAID 1 > Flashcards

NSAID 1 Flashcards

1
Q

Clinical uses of NSAIDs (2)

A
  • musculoskeletal: OA, muscle, tendon/lig., fractures
  • visceral pain: abdominal( small & lg intestines), thoracic
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2
Q

What part of the body do centrally acting analgesics act on?

A

Brain

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3
Q

What part of the body do COX-2 inhibitors act on?

A

Nociceptors

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4
Q

Arachicdonic Acid Cascade

A
  • phospholipids->arachidonic acid via phospholipase A2
  • COX 1 & 2 turn arachidonic acid -> Prostaglandin G2
  • Prostaglandin G2-> PGH2 via peroxidase
  • PGH2 -> thromboxane A2, PGI2, PGE2, PGF2 alpha
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5
Q

Function of COX 1

A
  • homeostasis
  • maintains renal funct. (PGI2), platelet funct. (Thromboxane A2), and gastric protect. (PGE2)
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6
Q

Function of COX 2

A
  • inflammatory stimuli
  • triggers macrophages, mast cells, neutrophils, etc.
  • stims. Proinflammatory PGs & other inflammatory mediators
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7
Q

PGI2

A
  • prostacyclin
  • localized in vasc. Tissue, potent vasodilator, inhibits platelet coag.
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8
Q

TXA2

A
  • vasoconst.
  • promotes thrombus form.
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9
Q

PGD2

A
  • prod. by mast cells
  • recruits Th2 cells, eosin., & basoph.
  • causes bronchial airway contract.
  • vasodil.
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10
Q

PGE2

A
  • direct vasodil. (Generally relaxes smooth m.)
  • inhibits NE release
  • induces fever
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11
Q

PGF2-alpha

A

Incr. in response to oxytocin elevation in uterus

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12
Q

COX 1 renoprotection

A

PGI2 & PGE2

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13
Q

COX 1 gastroprotection

A

PGE2

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14
Q

Purpose of the COX 1:COX 2

A
  • compares potency (IC50) of drug towards COX isoforms
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15
Q

Meaning when COX 1: COX 2 is< or close to 1

A

Less drug needed to inhbit COX 1

More drug needed to inhibit COX 2

(Classical NSAID)

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16
Q

Meaning when COX 1: COX 2> 1

A

Less drug needed to inhibit COX 2 -or- drug is more potent towards COX2

(Preferential or selective NSAID)

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17
Q

Name the classical NSAIDs (5)

A

Aspirin

Flunixin meglumine

Phenylbutazone

Acetaminophen

Tepoxalin

18
Q

List preferential NSAIDs (2)

A

Carprofen

Meloxicam

19
Q

List the Coxibs (COX 2 selective)

A

Firocoxib

Robenacoxib

Deracoxib

20
Q

Most common/serious side effects of NSAID use

A

Gastroduodenal ulcers & GI bleeding

21
Q

T or F: non-specific NSAIDs cause ulcers more frequently than the specific ones

A

True

22
Q

NSAIDs cause R dorsal colitis in which species

A

Horses

23
Q

Are dogs or cats more prone to GI ulcers due to NSAIDs

A

K9

24
Q

Risk factors for NSAID caused GI ulceration

A
  • old patients
  • concurrent glucocorticoid & other NSAID use
25
Q

Most common cause of GI ulcer.

A

OD

26
Q

Pathogenesis of GI adverse effects caused by NSAIDs

A
  • direct irritation (acid)
  • inhibiton of PGE2, PGI2, & TXA2 (loss of mucous secretion, bicarb. prod, mucosal epithelialization, and increased bleeding risk)
27
Q

Prev. & Tx of GI issues caused by NSAIDs

A
  • Prev: ACCURATE DOSING
  • Tx: proton pump inhibitors, h2 blockers, PGE analogues
28
Q

Under what conditions does Renal issues due to NSAIDs generally NOT occur?

A

If P is …

  • healthy
  • free H2O access
29
Q

Which prostaglandins are important in renal blood flow?

A

PGE2 & PGI2

30
Q

What do PGE2 and PGI2 do in the kidneys?

A

Ensure intramedullary renal blood flow & urine form.

31
Q

Clincal presentation of analgesic nephropathy

A
  • decre. GFR
  • H2O retention
  • hypertens.
32
Q

Risk factors for analgesic nephropathy

A
  • decreased blood flow to kidney
  • older patients
  • concurrent use of nephrotoxic/active drugs ( amino-glycoside antibiotics, diuretics, ACE inhib.)
33
Q

Prev. & Tx of analgesic nephropathy

A
  • Prev: avoid use in at risk P, adequate hydration, minimize drug interac.
34
Q

Aspirin effect on platelets and endothelium

A

Prolonged bleeding time

35
Q

Coxib effects on platelets and endothelium

A

Enhances thrombus prod.

36
Q

What drug CANNOT be used in CATS & why?

A
  • phenybutazone
  • causes bone marrow depression
37
Q

Adverse effects of NSAIDs on repro.

A

Prolonged gestation due to inhibition of PGF2-alpha and PGE2

38
Q

Clinical uses of prostaglandins

A
  • lyse CL
  • initiate uterine contractions
39
Q

2 drugs and the prostaglandins they affect that lyse CL

A
  • Cloprostenol: PGF2-alpha
  • Lutalyse: PGF2-alpha
40
Q

What prostaglandin initiates uterine contractions

A

PGE2

Pharmacology (20 decks)

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