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Questions and Answers
What is the primary reason prednisone is prescribed for treating asthma in children?
What is the primary reason prednisone is prescribed for treating asthma in children?
- It reduces inflammation in the airways. (correct)
- It enhances exercise tolerance.
- It directly dilates the airways.
- It increases mucus production in the lungs.
What could cause Johnny's respiratory infection after switching to inhaled glucocorticoids?
What could cause Johnny's respiratory infection after switching to inhaled glucocorticoids?
- Abrupt cessation of oral prednisone. (correct)
- Inhaled medication causing lung damage.
- A decrease in dietary intake.
- Increased exercise during therapy.
Why are inhaled glucocorticoids generally considered safer than oral glucocorticoids for long-term asthma management?
Why are inhaled glucocorticoids generally considered safer than oral glucocorticoids for long-term asthma management?
- They are available over the counter.
- They are less effective than oral glucocorticoids.
- They have fewer systemic side effects. (correct)
- They do not require prescriptions.
What was a significant concern for Johnny's doctor regarding the use of oral prednisone?
What was a significant concern for Johnny's doctor regarding the use of oral prednisone?
In the context of Addison's disease, what major hormone replacement therapy is the patient likely to receive?
In the context of Addison's disease, what major hormone replacement therapy is the patient likely to receive?
What indicates that the patient likely has primary adrenal insufficiency based on the ACTH stimulation test results?
What indicates that the patient likely has primary adrenal insufficiency based on the ACTH stimulation test results?
What could not contribute to Johnny's asthma exacerbation after stopping prednisone?
What could not contribute to Johnny's asthma exacerbation after stopping prednisone?
What symptom is NOT typically associated with Addison's disease?
What symptom is NOT typically associated with Addison's disease?
What is the primary site of action for aldosterone in the kidney?
What is the primary site of action for aldosterone in the kidney?
What effect does aldosterone have on potassium levels in the body?
What effect does aldosterone have on potassium levels in the body?
Which receptor type is primarily involved in the genomic effects of aldosterone?
Which receptor type is primarily involved in the genomic effects of aldosterone?
What is the half-life of aldosterone in circulation?
What is the half-life of aldosterone in circulation?
How does spironolactone affect the expression of ENaC and Na+/K+ ATPase?
How does spironolactone affect the expression of ENaC and Na+/K+ ATPase?
Which of the following substances significantly influences the synthesis of aldosterone?
Which of the following substances significantly influences the synthesis of aldosterone?
What is a primary physiological effect of aldosterone?
What is a primary physiological effect of aldosterone?
What percentage of aldosterone is typically bound to circulating proteins?
What percentage of aldosterone is typically bound to circulating proteins?
Which drug is primarily indicated for the treatment of severe Cushing's disease?
Which drug is primarily indicated for the treatment of severe Cushing's disease?
What is a common adverse effect associated with the use of Ketoconazole?
What is a common adverse effect associated with the use of Ketoconazole?
What is the mechanism of action for Metyrapone?
What is the mechanism of action for Metyrapone?
Which of the following drugs is not recommended during pregnancy?
Which of the following drugs is not recommended during pregnancy?
What is the primary clinical use of Mifepristone?
What is the primary clinical use of Mifepristone?
Which of the following adverse effects is associated with Levoketoconazole?
Which of the following adverse effects is associated with Levoketoconazole?
Which site of action is targeted by both Osilodrostat and Metyrapone?
Which site of action is targeted by both Osilodrostat and Metyrapone?
Which condition is Ketoconazole used to treat off-label?
Which condition is Ketoconazole used to treat off-label?
What is an indication for Osilodrostat?
What is an indication for Osilodrostat?
Which drug acts on the side-chain cleavage enzyme?
Which drug acts on the side-chain cleavage enzyme?
Which of the following glucocorticoids is NOT considered biologically active when applied topically?
Which of the following glucocorticoids is NOT considered biologically active when applied topically?
What is one of the key advantages of local administration of glucocorticoids?
What is one of the key advantages of local administration of glucocorticoids?
Which drug combination includes both a long-acting beta2-agonist and an inhaled glucocorticoid?
Which drug combination includes both a long-acting beta2-agonist and an inhaled glucocorticoid?
What is a common adverse effect associated with inhaled glucocorticoids?
What is a common adverse effect associated with inhaled glucocorticoids?
In the context of topical corticosteroids, which of the following is considered very high potency?
In the context of topical corticosteroids, which of the following is considered very high potency?
Which glucocorticoid is preferred for treatment during pregnancy?
Which glucocorticoid is preferred for treatment during pregnancy?
What is a significant risk associated with the prolonged use of systemic glucocorticoids?
What is a significant risk associated with the prolonged use of systemic glucocorticoids?
What characteristic makes intra-articular glucocorticoids particularly effective in treating joint conditions?
What characteristic makes intra-articular glucocorticoids particularly effective in treating joint conditions?
What is the primary indication for using inhaled glucocorticoids?
What is the primary indication for using inhaled glucocorticoids?
Which enzyme is responsible for the activation of prednisone in the maternal liver during pregnancy?
Which enzyme is responsible for the activation of prednisone in the maternal liver during pregnancy?
Which glucocorticoid crosses the placenta in its active form and is indicated for fetal lung maturation?
Which glucocorticoid crosses the placenta in its active form and is indicated for fetal lung maturation?
Which condition is a commonly treated indication for intra-articular glucocorticoids?
Which condition is a commonly treated indication for intra-articular glucocorticoids?
What is the main reason why topical glucocorticoids must be biologically active?
What is the main reason why topical glucocorticoids must be biologically active?
Which drug is a common component of the combination therapy for asthma with LABAs?
Which drug is a common component of the combination therapy for asthma with LABAs?
What is the most common cause of primary hypoaldosteronism?
What is the most common cause of primary hypoaldosteronism?
What physiological change is primarily associated with hyperaldosteronism?
What physiological change is primarily associated with hyperaldosteronism?
Which condition requires the use of fludrocortisone as part of its treatment regimen?
Which condition requires the use of fludrocortisone as part of its treatment regimen?
Which of the following is NOT a mechanism of action for mineralocorticoid receptor antagonists like spironolactone?
Which of the following is NOT a mechanism of action for mineralocorticoid receptor antagonists like spironolactone?
What is a significant adverse effect associated with spironolactone?
What is a significant adverse effect associated with spironolactone?
Which condition is characterized by a deficiency of 21β-hydroxylase?
Which condition is characterized by a deficiency of 21β-hydroxylase?
What is a common effect of aldosterone on the body's electrolytes?
What is a common effect of aldosterone on the body's electrolytes?
Which medication is considered the most widely used mineralocorticoid?
Which medication is considered the most widely used mineralocorticoid?
How does eplerenone differ from spironolactone in its action?
How does eplerenone differ from spironolactone in its action?
What clinical consequence can arise from hyperaldosteronism?
What clinical consequence can arise from hyperaldosteronism?
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Study Notes
Introduction to Adrenal Cortex Pharmacology
- Focus on glucocorticoids, mineralocorticoids, and adrenal androgens.
- Discuss routes of administration, inhibitors of corticosteroid synthesis, and receptor antagonists.
Glucocorticoids
Routes of Administration
- Oral: Tablet, solution, syrup.
- Parenteral: Intravenous (IV), intramuscular (IM), intra-articular injection.
- Topical: Lotion, cream, gel, ointment.
- Inhaled: Aerosol application, primarily used for asthma.
- Ophthalmic and otic: Solutions, ointments for eye and ear treatments.
Inhaled Glucocorticoids
- Common drugs: Fluticasone, Beclomethasone, Budesonide.
- Indications: Chronic asthma management.
- Often used in combination with Long-Acting Beta2-Agonists (LABA) like Salmeterol and Formoterol.
- Adverse effects: Oropharyngeal candidiasis.
Topical Glucocorticoids
- Must be biologically active as the skin lacks the 11β-HSD1 enzyme.
- Key drugs: Hydrocortisone, Methylprednisolone, Dexamethasone; not Prednisone.
- Indications: Atopic dermatitis and psoriasis.
- Potency varies: Betamethasone dipropionate and Clobetasol propionate noted for high potency.
Intra-Articular Administration
- Depot glucocorticoids such as Methylprednisolone acetate.
- Indications: Rheumatoid arthritis and gout.
- Must be biologically active due to the absence of 11β-HSD1 in joints.
Local Administration
- Benefits include high local concentration, reduced systemic adverse effects, and prevention of HPA axis suppression.
Use in Pregnancy
- Prednisone is safe during pregnancy; converted to prednisolone by maternal liver.
- Dexamethasone is used for promoting fetal lung maturation in high-risk cases.
Corticosteroid Synthesis Inhibitors and Receptor Antagonists
Inhibitors of Corticosteroid Synthesis
- Drugs: Mitotane, Aminoglutethimide, Ketoconazole, Metryrapone, Osilodrostat, Levoketoconazole.
- Clinical use: Primarily Cushing’s syndrome and adrenocortical carcinoma.
- Site of action varies by drug; example: Ketoconazole affects multiple steroidogenesis pathways.
Glucocorticoid Receptor Antagonist
- Mifepristone (Korlym®): Antagonizes both glucocorticoid and progesterone receptors.
- Indications: Early pregnancy termination and hyperglycemia due to Cushing's syndrome.
Mineralocorticoids
Aldosterone
- Main endogenous mineralocorticoid with minimal glucocorticoid effects.
- Synthesized in the zona glomerulosa, primarily regulated by the renin-angiotensin system.
- Functions to increase sodium reabsorption and potassium excretion, maintaining blood pressure.
Treatment for Aldosterone Deficiency
- Hypoaldosteronism: Can occur in conditions like Addison's disease or congenital adrenal hyperplasia.
- Treatment involves replacement therapy with Fludrocortisone.
Mineralocorticoid Receptor Antagonists
- Examples: Spironolactone, Eplerenone.
- Clinical use includes heart failure management, hyperaldosteronism, and edema control.
- Side effects include endocrine-related issues and hyperkalemia.
Adrenal Androgens
Dehydroepiandrosterone (DHEA)
- A weak androgen and major precursor of estrogens.
- Increased production seen in congenital adrenal hyperplasia due to 21β-hydroxylase deficiency.
- Treatment requires glucocorticoid and mineralocorticoid replacement to maintain balance.
Case Studies and Clinical Implications
- Highlight scenarios involving asthma treatment with glucocorticoids and the importance of careful monitoring for side effects and growth in children.
- Present hypoadrenalism case indicative of Addison's disease leading to hormone replacement therapy.
Key Considerations
- Corticosteroids may cause various systemic effects; careful management of doses and routes is essential, especially in vulnerable populations such as children and pregnant women.
- Awareness of the pharmacologic properties and side effects is crucial for effective treatment of conditions involving adrenal hormones.
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