Steoid/nonsteroidal Pharm Flashcards

1
Q

Anti-inflammatory effects glucocorticoids

A

Limits visible & microscopic signs of inflammation
Radiant, physical, chemical, infectious, hypersensitivity, immunmedited

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2
Q

What type of inflammation do NSAIDS not work against?

A

Hypersensitivity and immune mediated inflammation

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3
Q

GC mechanism of action

A

Transactivation of anti genes
- activate gene at locus by presence of particular gene at another locus
Transrepression of pro inflame genes
- one protein represses that activity of second protein

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4
Q

Action & effects of GC

A

Anti-inflammation
Immunosuppression
Adverse
Dose dependent effects

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5
Q

Physiologic doses - GC

A

Use low dose
- form of replacement therapy (dog w hypoadrenocorticism)
Prednisone & prednisolone (mineralocorticoid) + DOCP (desoxycorticosterone pivalate)
Fludrocortisone acetate

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6
Q

Dosing GC - anti inflame dose

A

Inhibit phospholipase A2
Decrease movement of WBC into inflamed tissue
Inhibit release of inflame mediators /enzymes
Stabilization of micro vascular integrity

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7
Q

Inhibit phospholipase A2

A
  • proximal mediator of arachidonic acid cascade
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8
Q

Decrease movement of WBC into inflamed tissue

A
  • reduce release of cytokines
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9
Q

Inhibit release of inflame mediators /enzymes

A
  • histamine, bradykinin
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10
Q

Stabilization of micro vascular integrity

A
  • for shock or CNS inflame
  • penetrate BBB (NSAIDS dont)
  • reduce edema
  • reduce cellular extravasation
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11
Q

Immunosuppressive doses of GC

A

Decrease macrophage function
Decrease lymphocyte function
T cell&raquo_space;> B cell

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12
Q

Chronic/cumulative dosing

A

Anti inflame or immunosuppressed dose
Chronic use can result in inhibition of Bcell antibody production

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13
Q

Dermatology & soft tissue effects

A
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14
Q

GIT adverse effects

A
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15
Q

Neuropsychiatric adverse effects

A
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16
Q

Eye adverse effects

A
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17
Q

Renal adverse effects

A
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18
Q

Bone adverse effects

A
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19
Q

Cardio adverse effects

A
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20
Q

Muscle adverse effects

A
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21
Q

Endocrine adverse effects

A
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22
Q

Minimizing adverse effects

A

Alternate date therapy
Taper dosing
Alternative routes of admin
Alternative therapeutic options
(Minimize not prevent)

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23
Q

Average blood work on GC - CBC

A

Neutrophilia
Lymphopenia
(Eosinopenia)
(Monocytosis)
(Basopenia)
“Stress leukogram”

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24
Q

Average chemistry work on GC

A

Hyperglycemia - glucosuria
Increased ALP/ALT - dogs esp
Hyperalbuminemia - cats esp
Dyslipidemias - cholesterol

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25
Q

Dosing for dogs - prednisolone

A

Prenisolone
Physiologic replacement - 0.2-0.3 mg/kg
Anti inflame - 0.55-1.1 mg/kg
Immunosuppressive - 2.2-4.4mg/kg

26
Q

Dosing for cats - prednisolone

A

2.2-8.8mg/kg
Fewer # of GC receptors
Lower affinity of GC receptors

27
Q

Action of prednisone

A

Intermediate action (12-36hr)
3.5x more potent than endogenous cortisol
Mineralocorticoid action (less than endo)
Oral in dogs - cheap
Cats & horses - low bioavailability

28
Q

Action of prednisolone

A

Intermediate action (12-36 hr)
4x more potent than endogenous cortisol
Mineralocorticoid activity (< endo)
Active metabolism of prednisone
Oral in cats, dogs, horses & non rum species
IV use - prednisolone sodium succinate - ER drugs, wide species spectrum

29
Q

Action of dexamethasone

A

Long action >48 hr
30x more potent than endo
No mineral activity

30
Q

Dexamethasone injection

A

2mg/mL
Polyethylene glycol base - caution repeated use in cats

31
Q

Dexamethasone sodium phosphate

A

4mg/mL
Equivalent to 3mg/mL dex - adjust dose

32
Q

Dexamethasone PO tablet & powder

A

Fine just adjust dose

33
Q

Triamcinolone base

A

Intermediate action 24-48 hrs
5x more potent
No mineral activity
Oral

34
Q

Triamcinolone ester

A

Long action (weeks)
8x more potent
No mineral activity
IM/SC, intra-articular, intralesional

35
Q

Methylprednisolone Na suc

A

Intermediate acting (12-36hr)
5x more potent
No mineral activity
IV/IM

36
Q

Methylprednisolone acetate

A

Long acting (days to weeks)
2x more potent than prednisolone
No mineral activity
IM/SC, Intra articular intralesional

37
Q

When to use GC

A

Immune mediated diseases
Hypersensitivity
Neurological disease / TBI (crosses BBB)
Shock

38
Q

When to use NSAIDS

A

Musculoskeletal disease (DJD)
Infections
Fever
Peri-operative
Wounds

39
Q

Atypical NSAIDS

A

Acetaminophen (therapeutic not toxin)
Dipyrone
Grapirant

40
Q

Acetaminophen - similarities to other NSAIDS

A

Anti-inflame properties
- pain, fever, loss of function, fever, redness
Same clinical indications as COX-2 inhibitors

41
Q

Acetaminophen- differences from other NSAIDS

A

Minimal effects on COXI/COX2 in peripheral inflame
Toxicity profile is different - liver, blood, not GI or kidney

42
Q

Paracetamol

A

Same thing as acetaminophen

43
Q

Mechanism of action for acetaminophen

A

Analgesics effects are centrally mediated (CNS)
Reaches high concentrations in CNS
Interacts w opioid receptors
Increases serotonin in brain
Inhibits substance P
Inhibit COX 3 ? (Found in CNS of some species including dog)

44
Q

clinical use for acetaminophen in horses

A

Pain/lameness - alone or combined w NSAIDS
Fever

45
Q

Clinical use for acetaminophen in dogs

A

Combined w codeine
Tablet strength 300/60
Dose 10-15 mg/kg & 1-2 mg/kg

46
Q

What species should you not use acetaminophen in ?

A

Cats - absolutely not
They lack the liver enzyme to break down for proper function - hepatotoxic

47
Q

Dipyrone

A

“Metamizole”
IV use in horses
Fever, PO ?
Prohibited in food animals

48
Q

Why is Dipyrone banned in food animals?

A
  • causes blood of dyscrasias in humans
    Pulled from human market
49
Q

Action of Dipyrone

A

Spasmolytic
- inhibits release of intracell Ca
- blocks muscle contraction (GIT)
Rapidly metabolized
- multiple active metabolites (4-MMA)
- prodrug

50
Q

Clinical uses for Dipyrone

A

Fever
Colic (+butylscopolamine), anticholinergic/spasmolytic
Analgesics & anti-pyretic in dogs
Analgesics & anti inflame in cats

51
Q

Grapiprant

A

First in class piprant
Non-cox inhibiting prostaglandin receptor antagonist
Specifically blocks EP4 receptor

52
Q

Labeled use of grapiprant

A

Control of pain /inflammation associated w OA in dogs
Safe up to 15x label dose for up to 9 months
- dose dependent decreases in albumin
Effective when compared to placebo

53
Q

Adverse effects of grapiprant

A

Diarrhea, hemorrhagic
MDR1 mutant

54
Q

Grapiprant in cats

A

Orally absorbed - levels similar to therapeutic concentrations in dogs
Safe after 28 days of admin

55
Q

grapiprant in horses/alpacas

A

Not absorbed well
- horses 30mg/kg = $6400/week
Baby goats is fine

56
Q

Efficacy of grapiprant

A

Some analgesics in dog spays
Not as good as carprofen
Minimal analgesics in cat spays

57
Q

PSGAGs

A

Adequan - canine & equine
Disease modifying osteoarthritis drug
- IM 2x /week for 4 weeks
Heparin analog

58
Q

Cautions with PSGAGs

A
  • avoid use in animals w bleeding disorders
  • avoid concurrent use w COX1 or non selective NSAIDS
59
Q

DMSO

A

Free radical scavenging properties
Used in horses to treat
Endo tox, GIT, neurological disease, laminitis, rhabdomyolysis, HIE

60
Q

Admin of DMSO

A

IV of 5-10% DMSO
Lack efficacy data
Cannot use in dairy operations