Flashcards in Endocrine Drugs - Corticosteroids And Antagonists Deck (22):
What are the clinical applications of prednisone?
1. Many inflammatory conditions
2. Organ transplantation
3. Hematologic cancers
What are the pharmacokinetics of prednisone?
Duration of activity is longer than pharmacokinetic half-life of drug owing to gene transcription.
What is the toxicity of prednisone?
1. Adrenal suppression
2. Growth inhibition
3. Muscle wasting
5. Salt retention
6. Glucose intolerance
7. Behavioral changes
Besides prednisone mention some other primarily glucocorticoids.
What is the mechanism of action of fludrocortisone?
Strong agonist of mineralocorticoid receptors and moderate activation of glucocorticoid receptors.
What is the clinical application of fludrocortisone?
What are the pharmacokinetics of fludrocortisone?
Long duration of action.
What are the toxicities of fludrocortisone?
1. Salt and fluid retention
2. Congestive heart failure
3. Signs and symptoms of glucocorticoid excess
What is the mechanism of mifepristone?
Pharmacologic antagonist of glucocorticoid and progesterone receptors.
What are the clinical applications of mifepristone?
1. Medical abortion
2. Very rarely Cushing's syndrome
How is mifepristone administered?
What is the toxicity of mifepristone?
1. Vaginal bleeding in females
2. Abdominal pain
3. GI upset
What is the mechanism of action of spironolactone?
1. Pharmacologic antagonist of mineralocorticoid receptor.
2. Weak antagonism of androgen receptors.
What are the clinical applications of spironolactone?
1. Aldosterone am from any cause.
2. Hypokalemia due to other diuretics.
What are the pharmacokinetics of spironolactone?
Slow onset and offset of effect.
What are the toxicities of spironolactone?
2. Gynecomastia (not eplerenone)
3. Additive interaction with other K-retaining drugs
What is the mechanism of action of ketoconazole?
Blocks fungal and mammalian CYP450 enzymes.
What is the clinical application of ketoconazole?
Inhibits mammalian steroid hormone synthesis and fungal ergosterol synthesis.
How is ketoconazole administered?
Oral or topical administration.
What is the toxicity of ketoconazole?
Hepatic dysfunction - many drug-drug CYP450 interactions.
What are the advantages of the synthetic glucocorticoids compared to cortisol?
1. Longer half-life
2. Longer duration of action
3. Reduced salt retaining effect
4. Better penetration of lipid barriers for topical activity