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Endo/Repro Exam II > PHARM - Adrenal Corticosteroid Drugs > Flashcards

PHARM - Adrenal Corticosteroid Drugs Flashcards

1
Q

What are the 3 primary uses of CS? What are the 3 Endocrine uses?

A

Inflammation, allergic rxns, and immunologic disorders

Dx of Cushing’s Syndrome, Tx of Adrenal Insuff, Tx of CAH

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2
Q

How do CS upregulate transcription of specific genes?

A

CS will bind to either Glucocorticoid receptors or Mineralcorticoid receptors, thus displacing the hps90 protein and allowing binding to occur

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3
Q

What two key enzymes are functional during the conversion between active sterols and inactive sterols?

A

11beta HSD2 (11b- dehydrogenase) == Cortisol (active) to cortisone (inactive)

11beta HSD1 (11-ketoreductase) == cortisone to Cortisol

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4
Q

What are the durations of the short, intermediate and long acting CS?

A

Short = less than 12 hours

Intermediate = 12-36 hours

Long = 36-72 hours

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5
Q

What are the 5 short acting Glucocorticoids?

A
  1. Hydrocortisone (cortisol)
  2. Cortisol
  3. Prednisone
  4. Prednisolone
  5. Methylprednisone
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6
Q

What is the one intermediate acting glucocorticoid?

A

triamcinolone

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7
Q

What are the two long acting glucocorticoids?

A

Betamethasone

Dexamethasone

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8
Q

Criteria for starting therapy?

A

Medical emergency == give high dose for a few days

Chronic therapy == various dose and frequency

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9
Q

Common Applications:

  1. Endocrine replacement tx for what?
  2. Immunosuppresion of ?
  3. Inflamm and allergies such as?
A
  1. primary adrenal insuff (addisons) and CAH

give Hydrocortisone and fludracortisone for both

  1. following bone marrow transplant, autoimmune dz, leukemia
  2. RA, IBD, COPD, allerig rhinitis, psoriasis
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10
Q

What is the ultimate metabolic effect of CS?

effects on 3 organs

A

HYPERGLYCEMIA

liver = increaed gluconeogenesis

adipose == increased glucose output

sk ms == increased glycogen synth

and decreased glucose synth

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11
Q

Two known inhibitors of 11b-HSD2

and result

A

Glycyrrhizin and carbenoxolene

cortisol not inactivated results in Na and H20 retention, K+ loss

and ultimately increased BP

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12
Q

Key Adverse effects of CS

ROS

A

Psych == sleep disturbances, mood

Skin = cushingoid, striae, acne, hirsituism

CV = HTN

MSK = osteoporosis and myopathy

Endo = diabetes and adrenal cortex suppresion

Immuno = lymphocytopenia and immunosuppression

Eyes = Cataracts

Develop = growth retardation

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13
Q

What is the dosing of CS?

A

Lowest does for shortest duration

give locally to reduce systemic distribution (topical and inhalation)

give single dose in AM

gradually taper off dose if possible

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14
Q

Glucocorticoid drug of choice

MOA

IND

PK

Adverse

A

Prednisolone

activates GR thus increasing gene txn

Inflammation, or organ transplant

DOA is longer than 1/2 life

Suppression of Adrenal

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15
Q

GC-receptor Antagonist

MOA

IND

PK

Adverse

A

Mifeprostone

blocks GC and Progesterone receptors\

Medical Abortion

oral

Vaginal bleeding and Abd pain

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16
Q

Mineralcorticoid Agonist

MOA

IND

PK

Adverse

A

Fludrocortisone

stims MC and GC receptors

Adrenal Insuff (Addisons)

Long DOA

excess Na and H20 retention == CHF

17
Q

Mineralcortiocoid Antagonists (2)

MOA

IND

PK

Adverse

A

Spirolactone

block MC receptor, tx for hyperaldosteronsim or hypokalemia

slow on and off (24-48 hours), A = hyperkalemia, gynecomastia

Eplerone

blocks binding of aldosterone, tx of HTN

short 1/2 life (3-6 hours), A = hyperkalemia

18
Q

Synthesis Inhibitors

MOA

IND

PK

Adverse

A

Ketoconazole

blocks fungal and mammalian CYP 450s thus blocking steroid synth

fungal infections or excess steroid

oral topical

many drug-drug interactions hepatic dysfunction

19
Q

In general, what is the most common endogenous Mineralcorticoid?

where does it act?

what is the result?

A

Aldosterone

kindey

increases Na and H20 retention and excretion of K+

20
Q

Patient populations in which GC admin is problematic

Many (8)

think ROS and adverse effects

A
  1. Immunocompromised (HIV AIDS)
  2. Diabetics
  3. Infections
  4. Peptic Ulcers
  5. CV conditions
  6. Psych conditions
  7. Osteoporosis
  8. Children

Endo/Repro Exam II (3 decks)

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