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1. Pharmacology > Glucocoricoids > Flashcards

Glucocoricoids Flashcards

1
Q

Which parts of the adrenal gland produce glucocorticoids?

A

Zona fasciculata and reticularis

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2
Q

Exogenous glucocorticoids

A

Clinical application
Negative long feedback loop (HPPA)
Strong inhibitor of hypothal.
Leads to adenohypertrophy

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3
Q

Examples of prodrugs

A

Cortisone, prednisone, methylprednisone

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4
Q

Aqueous solutions

A

Soluble esters- Na phosphate or Na- succinate
Given IM/IV in large doses for emergencies

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5
Q

Suspensions

A

Insoluble esters with opaque consistency- salts
Given Sc or IM, slow onset

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6
Q

Short-acting glucocorticoids (<24 hours)

A

Cortisol (hydrocortisone) - 1 gluco, ++ mineralo
Cortisone (prodrug)- 0.8, ++
Prednisone- 4, +
Prednisolone- 4, +
Methylprednisolone- 5, +
^^ alternate-day therapy possible

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7
Q

Intermediate-acting (24-48 hrs)

A

Triamcinolone- 5, 0
Triamcinolone acetonide- 35, 0

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8
Q

Long-acting (>48 hours)

A

Flumethasone- 15, 0
Dexamethasone- 30, 0
Betamethasone- 30, 0
^^ produce glucocorticoid effects

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9
Q

What drugs produce mineralocorticoid effects?

A

Aldosterone + fludrocortisone

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10
Q

Mineralocorticoids

A

Maintains electrolyte homeostasis
Trigger wound healing

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11
Q

Glucocorticoids

A

Carb, protein and lipid metabolism
Immune and stress response

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12
Q

Major endogenous glucocorticoid is ___________ and mineralocorticoid is _________

A
  1. Cortisol
  2. Aldosterone
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13
Q

Strength of binding determines _________

A

Potency and duration

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14
Q

Glucose metabolism

A

↑ gluconeogenesis and glycogenolysis (hyperglycemia)
↓ glucose uptake in peripheral tissues
Insulin resistance

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15
Q

Protein and lipid metabolism

A

↓ protein synthesis (anabolism)
↑ protein catabolism and lipolysis

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16
Q

Anti-inflammatory effects

A

Stimulates lipocortin production
Inhibits PL A2 activity
↓ vascular permeability
COX and LOX affected
↓ induced histamine formation
Antagonize toxins and kinins

17
Q

Immunosuppression

A

Inducing apoptosis (lymphoids)
Inhibits clonal expression of T and b cells and interferon synthesis
↓ igG and complement, leukocyte accum.

18
Q

When is Immunosuppression seen?

A

When medium to high doses are used (treating life threatening conditions)

19
Q

What does glucocorticoids do to water and electrolyte balance?

A

Prednisolone and methylprednisolone enhances K+ excretion and Na+ retention

20
Q

How do Glucocorticoids affect the kidney

A

↑ renal excretion
↓ intestinal absorption of Ca causing hypocalcemia

21
Q

How do Glucocorticoids affect bones

A

Inhibits osteoblasts, stimulates osteoclasts, ↑ parathyroid secretion affecting bone healing

22
Q

How does Glucocorticoids affect the endocrine system?

A

Suppression of ACTH, GH and TSH

23
Q

Glucocorticoids PK

A

~90% of cortisol reversibly bound to plasma proteins
Bound to albumin
Excreted in urine

24
Q

Physiological replacement therapy

A

Adrenalectomized and addisonian dogs and cats
In moderate stress (2-5 times), severe (5-20)
Hydrocortisone or cortisone
Prednisolone or prednisone

25
Q

Intensive short-term and shock therapy

A

Improve survival in hemorrhagic and septic shock
Use high dose, water soluble

26
Q

Antiinflammatory and antiallergic therapy

A

Pruritic dermatoses
Allergic pulmonary disease
Allergic gastroenteritis
Prednisolone or prednisone (small animals)
Dexamethasone (large animals)

27
Q

_________ only used in cats

A

Prednisolone

28
Q

Immunosuppressive therapy for autoimmune diseases

A

Immune-mediated thrombocytopenia
Autoimmune hemolytic anemia
Prednisolone and dexamethasone for induction

29
Q

Chronic palliative therapy

A

Used when NSAID therapy not working
Chronic arthritis
Hip dysplasia in dogs

30
Q

Alternate-day therapy

A

Allows HPAA to recover on “off” days
Prednisolone (short-duration)
Less practical for large animals

31
Q

Special uses

A

Topical and intralesional usage
Dermatitis
HPAA suppression
Lymphoma

32
Q

Acute dermatitis

A

Hydrocortisone or prednisolone

33
Q

Chronic dermatitis

A

Dexamethasone, betamethasone, triamicinolone

34
Q

Intraarticular administration

A

Horses to manage joint pain and inflammation (arthritis and bursitis)
Triamcinolone acetonide (osteoarthritis)

35
Q

Ophthalmic applications

A

Treating retinitis, choroditis, optic neuritis, orbital cellulitis
Contraindicated in corneal ulcers

36
Q

Neurological applications

A

Acute spinal/CNS trauma
Acute cervical pain
Peripheral neuropathies

37
Q

What syndrome does Glucocorticoids cause?

A

Cushing’s → PU/PD, symmetric alopecia, ↑ susceptibility to infection, peripheral myopathy, muscle atrophy, body fat redistribution

38
Q

Adverse effects

A

Diabetes mellitus
Iatrogenic secondary hypoadrenocorticism
Glycogen accumulation in liver
Slow turnover of enterocytes
Inhibits protective PG
↓ collagen synthesis
Mood/ behavior changes

39
Q

High doses in horses cause ________

A

Laminitis

1. Pharmacology (29 decks)

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