20 Questions
What is the most common long-term side effect of using glucocorticoids?
Osteoporosis
What is the main function of aldosterone in the kidneys?
To increase water and electrolytes
What is the effect of spironolactone on the body?
It competes for the mineralocorticoid receptor and inhibits sodium reabsorption
What is the use of fludrocortisone?
To treat Addison disease
What is the effect of ketoconazole on the body?
It inhibits gonadal and adrenal steroid synthesis
What is the benefit of using eplerenone over spironolactone?
It has less affinity for androgen receptors
What is the primary use of glucocorticoids in asthma and COPD?
To reduce inflammation in the lungs
Which of the following glucocorticoids is used to hasten fetal lung maturation in preterm infant delivery?
Betamethasone
What is the primary mechanism of the dexamethasone suppression test in diagnosing Cushing syndrome?
Suppressing ACTH production to diagnose cortisol excess
What is the primary complication of glucocorticoid deficiency in congenital adrenal hyperplasia?
Virilization of females and prepubertal males
What is the primary function of the steroid-receptor complex in the nucleus?
To act as a transcription factor to regulate gene expression
Which of the following glucocorticoids has the longest half-life?
Dexamethasone
What is the primary use of glucocorticoids in inflammatory skin disorders?
To reduce inflammation and swelling
What is the effect of glucocorticoids on muscle protein?
Muscle protein breakdown
What is the primary mechanism of glucocorticoids' anti-inflammatory effect?
Inhibition of phospholipase A2
What is the effect of glucocorticoids on lymphoid tissue?
Lymphoid tissue wasting
What is the role of coactivator or corepressor proteins in the mechanism of glucocorticoid action?
To recruit other proteins to the steroid receptor complex
What is the effect of glucocorticoids on bone metabolism?
Osteoporosis
What is the primary naturally occurring glucocorticosteroid?
Cortisol (hydrocortisone)
What is the effect of glucocorticoids on cell-mediated immunologic functions?
Decreased cell-mediated immunologic functions
Study Notes
Mechanism of Action of Glucocorticoids
- Bind to steroid receptors in the cytosol, forming a steroid-receptor complex
- The complex translocates to the nucleus, recruiting coactivators or corepressors, and binds to hormone response elements or gene promoter elements (GRE or MSE)
- Acts as a transcription factor to turn genes on or off, depending on the tissue and complexed proteins
Effects of Glucocorticoids
- Metabolic: promote gluconeogenesis, proteolysis, lipolysis, and lipogenesis, leading to net fat deposition
- Catabolic: muscle protein breakdown, lymphoid, connective tissue wasting, fat and skin, and osteoporosis
- Immunosuppressive: decrease cell-mediated immunologic functions, especially lymphocytes
- Anti-inflammatory: inhibit phospholipase A2, increase neutrophils, and decrease chemotaxis, basophils, monocytes, eosinophils, and lymphocytes
Glucocorticosteroids
- Cortisol (hydrocortisone): the major naturally occurring glucocorticosteroid
- Synthetic glucocorticosteroids: prednisone, triamcinolone, dexamethasone (longest half-life), betamethasone (topical), beclomethasone, and budesonide (short half-lives)
Uses of Glucocorticosteroids
- Asthma and COPD: inflammatory lung diseases
- Addison disease: primary glucocorticoid insufficiency
- Diagnosis of Cushing syndrome: dexamethasone suppression test
- Congenital adrenal hyperplasia: deficiency of cortisol and aldosterone synthesis
- Inflammatory skin disorders, allergic reactions, and urticaria
- Rheumatological and autoimmune disorders, such as TMJ and RA
- Blood cancers, such as lymphatic leukemia
- Preterm infant delivery: hasten lung maturation prior to delivery
Side Effects of Glucocorticosteroids
- Dose-related: primary dose-related side effects
- Osteoporosis: most common long-term side effect
- Gastritis: most common short-term side effect
- Cushing-like syndrome
- Hyperglycemia
- Cataracts
- Skin atrophy, ecchymosis, and purple striae with long-term topical use
- Immunosuppression: increased infection
- Inhaled: oral candidiasis, hoarseness, and throat irritation
- CNS: mood changes, including swings, euphoria, and depression
Mineralocorticosteroids
- Aldosterone: the major naturally occurring mineralocorticosteroid in humans
- Synthetic mineralocorticosteroids: fludrocortisone (has significant glucocorticoid activity)
- Corticosteroid antagonists: spironolactone and eplerenone
- Antagonize mineralocorticoid receptors, inhibiting sodium reabsorption and increasing potassium reabsorption
Corticosteroid Antagonists
- Spironolactone: antagonizes mineralocorticoid receptors, competes for the receptor, and inhibits sodium reabsorption and increases potassium reabsorption
- Eplerenone: selective aldosterone antagonist with less affinity for androgen receptor
- Uses: resistant hypertension, heart failure, hyperaldosteronism, and hirsutism in women
- Adverse effects: hyperkalemia, gynecomastia, menstrual irregularities, and skin rashes
This quiz covers the mechanism of action of glucocorticoids, including their role in immunity and how they bind to steroid receptors. It's a great resource for students of pharmacology and medicine.
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