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Pharmacology > Glucocorticoids (starred Info) > Flashcards

Glucocorticoids (starred Info) Flashcards

1
Q

List the 3 types of formulations glucocorticoids can come in

A
  • aqueous
  • alcoholic
  • suspensions
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2
Q

Aqueous glucocorticoids

A
  • double esters (na phosphate or na succinate)
  • IM/IV for large doses
  • emergencies
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3
Q

Alcoholic solution glucocorticoids

A
  • glucorcorti. base w/o a salt
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4
Q

Suspension glucocorticoids

A
  • insoluble esters
  • opaque consistency
  • salts (acetate, diacetate, tebutate, valerate)
  • SQ or IM; no IV
  • slow onset; last for about 2-4wks
  • acetonide and pivalate: very insoluble, slow onset, last for >4 wks
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5
Q

Cortisol (hydrocortisone)

A
  • 1 hr gluco
  • ++ mineralo
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6
Q

Cortisone (prodrug)

A
  • .8 hours gluco
  • ++ Mineralo
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7
Q

Prednisone (prodrug)

A
  • 4 hrs gluco
    • mineralo
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8
Q

Prednisolone

A
  • 4 hrs gluco
    • mineralo
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9
Q

Methyprednisolone

A
  • 5 hrs gluco
    • mineralo
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10
Q

Short acting glucocorticoids (5)

A
  • cortisol
  • cortisone
  • prednisone
  • prednisolone
  • methyprednisolone
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11
Q

Intermediate acting glucocorticoids (2)

A
  • triamcinolone
  • triamcinolone actonide
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12
Q

Triamcinolone

A
  • 5 hrs gluco
  • 0 mineralo
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13
Q

Triamcinolone acetonide

A
  • 35 hrs gluco
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14
Q

Long acting glucocorticoids (3)

A
  • flumethasone
  • dexamethasone
  • betamethasone
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15
Q

Flumethasone

A
  • 15 hrs gluco
  • 0 mineralo
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16
Q

Dexamethasone

A
  • 30 hrs gluco
  • 0 mineralo
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17
Q

Betamethasone

A
  • 30 hrs gluco
  • 0 mineralo
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18
Q

Aldosterone+fludrocortisone=

A

Mineralocorticoid effects

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19
Q

Dexamethasone/ betamethasone/ flumethasone

A

Glucocorticoid effects

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20
Q

Mineralocorticoids

A
  • maintaining electrolyte homeostasis
  • triggers wound healing
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21
Q

Glucocorticoids

A
  • carb, protein, & lipid metabolism
  • role in immune response
  • natural glucocorticoids have some mineralocorticoid activity
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22
Q

Major endogenous glucocorticoid

A

Cortisol

23
Q

Major mineralocorticoid

A

Aldosterone

24
Q

Pharmacology of glucocorticoids

A
  • binding strength=potency & duration
  • PK of circulating glucocorticoids have little effect on potency or duration
  • activity depends on proteins produced
25
Q

Glucose metabolism

A
  • incr. gluconeogenesis and glyconeogenesis
  • decre. glucose uptake in periph. Tissues
  • insulin resistance
26
Q

Protein & lipid metabolism

A
  • decreased protein synth
  • increased protein catabolism
  • incre. Lipolysis
27
Q

Anti-inflamm. Effects

A
  • lipocortin prod.
  • inhibit PL A2 activity ( blocks synthesis of inflamm. Mediators)
  • affects COX & LOX paths
  • decrease vasc. Permeability
  • microcirculation & membrane integrity
  • stabilize lysosomal enzymes, decr. Histamine form., antagonize toxins and kinins
28
Q

Immunosuppression

A
  • suppress cell-mediated immunity via induce apoptosis in normal lymphoid organs
  • inhibit clonal expansion of T and B lymph.
  • decr. IgG & Complement levels
  • reduce leukocyte accumulation @ inflamm. Site
  • reduce # circulating eosin, basop, & monoc
  • inhibit interferon synth
  • immunosuppressive @ medium to high doses
29
Q

Other important effects

A
  • prednisolone & methylprednisolone: enhance K+ excretion and Na+ retention
  • incr. renal excretion
  • decr. Intestinal Ca2+ absorp.
  • bone healing affected
  • endocrine suppression of ACTH, GH, TSH
30
Q

Clinical uses of glucocorticoids

A
  • physiological replacement therapy
  • intensive short term & shock therapy
  • anti-inflamm. & anti-allergic
  • immunosupp. For autoimmune diseases
  • chronic palliative therapy
  • alternate day therapy
31
Q

Physiological replacement therapy

A
  • adrenalectomized & addisonian K9s and Cats
  • 0.2-1 mg/kg/day of hydrocortisone
  • 0.1-0.2 mg/kg/day of prednisolone
  • moderate stress: 2-5x per day
  • severe stress: 5-20x per day, until stressful experience gone
32
Q

Intensive short term & shock therapy

A
  • improve survival in hemorrhagic & septic shock
  • Tx should be started in 4hrs
  • high dose recomm.
  • H2O soluble glucocorts
  • include aggressive H2O therapy & broad-spectrum abx in septic shock
33
Q

Anti-inflamm. & anti-allergic therapy indications

A
  • pruritic dermatoses
  • allergic pulmonary disease
  • allergic gastroenteritis
34
Q

Anti-inflamm. & anti-allergic drugs

A
  • most common in SMALL ANIMALS: prednisolone or prednisone
  • most common in LARGE ANIMALS: dexamethasone (high potency & low cost)
  • induction: 0.55 mg/kg q12h PO
  • maintenance: 0.55-2.2 mg/kg q48h PO
35
Q

What drug is ONLY USED IN CATS to TX inflammation and allergic rxns

A

Prednisolone!!!!!!

36
Q

Induction and Maintenance for immunosuppressive therapy for autoimmune diseases

A
  • Induction: prednisolone 2.2-6.6 mg/kg q12h; dexamethasone 0.33-1.1 mg/kg q12h
  • maintenance: prednisolone 1.0-2.2 mg/kg, alternate day
37
Q

Autoimmune diseases glucocorticoids are used for

A
  • IMHA
  • immune mediated thrombocytopenia
38
Q

Important facts to know for using glucocorticoids to treat autoimmune diseases

A
  • use highest recomm. Dose until clinical signs reduce
  • don’t stop Tx until autoimmune disease is gone for 2-3 mos
  • create Dx plan that excludes infectious dieases before starting Tx
39
Q

Chronic palliative therapy

A
  • used when NSAIDs aren’t successful @ managing chronic conditions
  • used for chronic arthritis & K9 hip dysplasia
  • intermittently used or on alternate-day basis
40
Q

Alternate day therapy

A
  • long term therapy w/ glucocorts or large doses-> HPAA suppression & increases side effects
  • allows HPAA to recover on off days
  • change to alternate day use should be gradual to avoid withdrawal
41
Q

Why can prednisolone be used as an alternate day drug and not dexamethasone

A
  • prednisolone has a long DOA & dexamethasone has short DOA
  • prednisolone has intermediate potency & is easier to taper dose
42
Q

Drugs used to treat acute dermatitis

A
  • hydrocortisone
  • prednisolone
43
Q

Drugs used to Tx chronic dermatitis

A

Dexamethasone, betamethasone, triamicinolone

44
Q

Intraarticular admin.

A
  • primarily in horses for jt pain and inflamm. From arthritis and bursitis
  • triamcinolone acetonide
45
Q

Ophthalmic applic.

A
  • Tx for retinitis, choroiditis, optic neuritis, orbital cellulitis
  • forms: solutions, ointments, susp.
  • contraindicated in corneal ulcers
46
Q

Neurological applic.

A
  • Tx for numerous problems

(Acute spinal/CNS trauma, acute cervical pain, peripheral neuropathies

47
Q

What disease is a common adverse effect

A

Cushing’s syndrome

48
Q

Clinical signs of cushing’s

A
  • PU/PD
  • symmetric, bilat. Alopecia
  • periph. Myopathy
  • fat redist.
  • muscle atrophy
  • increased infection susc.
49
Q

Adverse effects part 2

A
  • gluconeogenic & insulin antagonistic effects-> onset of diabetes mellitus
  • long term HPAA-adrenal gl. Atrophy-> iatrogenic secondary hypoadrenocorticism
  • abrupt stopping-> addisonian-like crisis
  • glycogen accumulation in hepatocytes (hepatomegaly & hepatopathy)
  • slow turnover of enterocytes & inhibit. Of protective PG
50
Q

Adverse effects part 3

A
  • reduce collagen synth.
  • laminits (due to high doses in horses)
  • suscept. To infect (UTIs)
  • can be reduced via alternate day regimen
51
Q

HPAA

A

Hypothalamic-pituitary-adrenal axis

52
Q

Mineralocorticoids affect which layer

A

Zona glomerulosa

53
Q

Glucocorticoids affect which zones

A

zona fasiculata & zona reticulariss

54
Q

Epi & norepi. Affect which zone

A

Medulla

Pharmacology (20 decks)

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