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Steroids

Physiology

Glucocorticoid secretions

  • Oscillates with a circadian rhythm
    • For those on a diurnal sleep cycle, cortisol levels are highest just before waking and lowest in the evening
  • Regulation
    • Hypothalamus stimulated to secrete Corticotropin-releasing hormone (CRH)
    • CRH binds to receptors on the anterior pituitary
    • Anterior cells synthesize POMC
    • POMC is cleaved to form ACTH
    • ACTH stimulates cholesterol desmolase and increases the conversion of cholesterol to pregnenolone

 

Glucocorticoid Actions

  • Physiologic
    • Negative nitrogen balance due to increased protein breakdown
    • Increased blood glucose due to stimulation of gluconeogenesis
    • Increased plasma fatty acids and ketone body formation via lipolysis and redistribution of body fat
    • Decreased intestinal reabsorption of calcium
    • Increase kaliuresis
    • Promote sodium and water retention
  • Anti-inflammatory effects
    • Inhibition of classic signs of inflammation
    • Inhibition of antigenic response
    • Inhibition of vascular permeability
    • Inhibition of arachidonic acid and prostaglandin production
    • Inhibition of cytokine production

Pharmacologic Properties

  • Binding
    • 80% of circulating cortisol is bound to corticosteroids-binding globulin (CBG); 10% is bound to plasma albumin
    • Dexamethasone does not bind CBG and exists only in the free state
  • Half-life
    • Short-acting: cortisol (8-12 hours)
    • Intermediate-acting: prednisone (12-36 hours)
    • Long-acting: dexamethasone (39-54 hours)
  • Administration
    • Attempt to pattern circadian rhythm (double dose in AM and single dose in afternoon)

 

Therapeutic Uses

  • Replacement therapy for primary or secondary insufficiency
  • Inflammation or immunosuppression
  • Sarcoidosis
  • Dermatologic disorders
  • Shock
  • Neuromuscular disorders
  • Adrenocortical hyperplasia
  • Stimulation of surfactant production
  • Neoplastic diseases
  • Diagnosis of Cushing’s syndrome

Adverse Effects

  • Iatrogenic Cushing’s disease
  • Mineralocorticoid activity, hypokalemic, hypochloremic alkalosis
  • Hyperglycemia
  • Osteoporosis
  • Peptic ulcers
  • Cataracts and glaucoma
  • Edema
  • Hypertension
  • Poor wound healing
  • Immunosuppression
  • Muscle weakness and tissue loss

 

Characteristics of Therapeutic Corticosteroids

Corticosteroids

Route

Properties

Hydrocortisone

PO/IV/IM

Identical to cortisol. Weak mineralocorticoid. Short-acting.

Prednisone

PO

Intermediate duration of action. Compared to hydrocortisone four times the glucocorticoid effects and half the mineralocorticoid. Drug of choice for asthma maintenance.

Prednisolone

PO/IV/IM

Intermediate duration. Compared to hydrocortisone five times more potent and half the mineralocorticoid. Drug of choice for acute asthma attacks.

Triamcinolone

PO/IV/TOP/INH

Intermediate duration. Compared to hydrocortisone thirty times the corticocoid effect and no mineralocorticoid.

Dexamethasone

PO/IV/IM/INH

Used to reduce intracranial pressure. Few mineralocorticoid effects. Used in dexamethasone suppression test.

Fludocortisone

PO

Potent mineralocorticoid effects. Only oral mineralocorticoid available.

Properties of Corticosteroids

 

Activity

 

Agent

Anti-inflammatory

Topical

Na-retaining

Equivalent oral dose

Short-acting

 

 

 

 

Hydrocortisone (cortisone)

1

1

1

20

Cortisone

0.8

0

0.8

25

Prednisone

4

0

0.3

5

Prednisolone

5

4

0.3

5

Methylprednisolone

5

5

0

4

Meprednisone

5

 

0

4

Intermediate-acting

 

 

 

 

Triamcinolone

5

5

0

4

Paramethasone

10

 

0

2

Fluprednisolone

15

7

0

4

Long-acting

 

 

 

 

Betamethasone

25-40

10

0

0.6

Dexamethasone

30

10

0

0.75

Mineralocorticoids

 

 

 

 

Fludrocortisone

10

10

250

2

Desoxycorticosterone acetate

0

0

20

 

 

Prednisone

Adrenal insufficiency: 5 to 60 mg/day ORALLY initially, vary dose depending on patient response
Pericarditis - Pulmonary histoplasmosis, acute: 0.5 to 1 mg/kg daily (maximum 80 mg daily) in tapering doses over 1 to 2 weeks (guideline dosing)

Prednisolone

Asthma: (moderate and severe exacerbation; NHLBI asthma guidelines) 40 to 80 mg/day ORALLY in 1 or 2 divided doses until PEF reaches 70% of predicted or personal best; outpatient burst, 40 to 60 mg ORALLY in 1 or 2 divided doses for a total of 3-10 days

Methylprednisolone Sodium Succinate

Asthma: (moderate and severe exacerbation; NHLBI asthma guidelines) 40 to 80 mg/day IV in 1 or 2 divided doses until PEF reaches 70% of predicted or personal best

Triamcinolone

Asthma: ORAL, initial, 8 to 16 mg/day
Disorder of skin: ORAL, initial, 8 to 16 mg/day

Dexamethasone

Cerebral edema, Associated with primary or metastatic brain tumor, craniotomy, or head injury: (dexamethasone sodium phosphate), initial, 10 mg IV, followed by 4 mg IM every 6 hr until symptoms of cerebral edema subside
Bacterial meningitis; Adjunct: (suspected or proven S. pneumoniae meningitis) 0.15 mg/kg IV every 6 hr for the first 2 to 4 days of antibiotic treatment with first dose given 10-20 min before or concomitantly with the first antibiotic dose
Septic shock; Adjunct: 12 mg/day IV or less; taper the dose at the end of therapy

Adrenal Suppression

  • Adrenal suppression occurs after steroid use for more than 2 weeks
  • For stress/infections
    • Minor: give 2-fold increases for 24-48 hours
    • Major: give up to 10-fold increase for 48-72 hours

 

Tapering Steroids

  • If large doss are being used, an alternative day schedule may be useful once symptoms are under control
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