Corticoids and Mineralcorticoids Flashcards
(44 cards)
What are glucocorticoids?
corticosteroids (produced in the adrenal cortex), which are a class of steroid hormones. They (i.e. cortisol) bind to the glucocorticoid receptor that is present in almost every cell.
What is the major endogenous glucocorticoid?
hydrocortisone (aka cortisol)
What type of regulation governs glucocorticoids?
negative feedback
What hormone regulates cortisol?
pituitary hormone ACTH (corticotropin), which regulates synthesis and secretion of cortisol.
Are glucocorticoids and mineralocorticoids similar to androgens (testosterone and estradiol)?
YES
What else does ACTH (corticotropin) do?
also a growth factor for adrenal cortex
What happens with a decrease in ACTH (corticotropin)?
decrease in hydrocortisone (cortisol) and atrophy of adrenal cortex.
- Remember, does potency = efficacy?
NO. This doesn’t necessarily mean it’s better.
How do you increase the potency of a steroid?
add a halogen to it.
** What are the 7 glucocorticoid drugs and their equiv. dose?
- hydrocortisone= nice balance between anti-inflammatory and salt retention (20 mg).
- cortisone= nice balance between anti-inflammatory and salt retention (25 mg).
- prednisone= mostly anti-inflammatory (5 mg).
- methylprednisolone= only anti-inflammatory (4 mg).
- triamcinolone= only anti-inflammatory (4 mg).
- dexamethasone= only anti-inflammatory (0.75 mg).
- betamethasone= only anti-inflammatory (0.6 mg).
* So a very small dose of betamethasone is equivalent to a much larger does of cortisone).
** What are the metabolic effects of glucocorticoids?
- INCREASED gluconeogenesis, glycogenolysis, and protein catabolism.
- DECREASED osteoblast formation and activity, calcium absorption from GI tract, secretion of TSH, and protein synthesis.
** What are the anti-inflammatory effects of glucocorticoids?
- DECREASED production of cytokines, interleukins, prostaglandins, proliferation of lymphocytes and macrophages, and migration of lymphocytes and macrophages.
How much glucocorticoid is required for therapeutic purposes?
large (pharmacologic) doses, not physiologic amounts.
*** What are the therapeutic uses of glucocorticoids?
- replacement in adrenal hypofunction
- anti-inflammatory effect
- immunosuppressive effect
- adjunct to myeloproliferative disease and other malignancies.
- endocrine disorders: primary (at the site) and secondary (pituitary) adrenocortical insufficiency, and congenital adrenal hyperplasia.
- rheumatic disorder: RA, bursitis, gouty arthrits
- dermatological: severe psoriasis and severe seborrheic dermatitis.
- allergic states: severe bronchial asthma, contact dermatitis, and drug hypersensitivity.
- palliation of neoplasms: leukemias and lymphomas (adult).
- GI: ulcerative collitis
What are the musculoskeletal ADRs of glucocorticoids?
- muscle weakness
- loss of muscle mass
- tendon rupture
- steroid myopathy
- osteoporosis
- bone fracture
- vertebral compression fractures
- aseptic necrosis (femoral and humoral heads)
- decreased metabolic effects: decreased osteoblast formation and activity, and decreased Ca++ absorption form GI (even with high vit. D).
- hypocalcemia followed by increased PTH, causing further bone degeneration.
What are the fluid/electrolyte ADRs of glucocorticoids?
- Na+ retention, fluid retention, hypertension, and thus CHF in susceptible pts.
- K+ loss and thus HYPOKALEMIC ALKALOSIS.
What are the GI ADRs of glucocorticoids?
- peptic ulcer with perforation
- perforation of small and large bowel (esp in pts with inflammatory disease).
What are the dermatologic ADRs of glucocorticoids?
- thin fragile skin
- impaired wound healing
- erythema
What are the psychological ADRs of glucocorticoids?
- acute= euphoria
- chronic= insomnia, depression, psychosis
What are the immunological ADRs of glucocorticoids?
- signs of infection may be masked
- immunosuppression with large doses (Chx pox and measles can be fatal in children).
What are the endocrine ADRs of glucocorticoids?
- suppression of growth in children
- menstrual irregularities and anovulation in women.
- decreased testosterone in men.
- Cushingoid state= hypercortisolemia, moon face, buffalo hump.
- hypothalamic suppression, and thus pituitary adrenal axis suppression (most common side effect of chronic glucocorticoid use).
What are the ophthalmic ADRs of glucocorticoids?
cataracts or increased intraocular pressure
What are some drug interactions with glucocorticoids?
- enzyme inducers= phenytoin, phenobarbital, rifampin
* Thus you may need an increased dose if on any of these.
What is a glucocorticoid antagonist?
- mifepristone= synthetic compound used to reverse Cushing’s syndrome
- Mitotane= synthetic adrenal cytotoxic agent that directly suppresses adrenal cortex. Used to treat inoperable adrenal cortical carcinoma.
