[03.02] Glucocorticoids, Mineralocorticoids, and Antagonists V2.pdf

Agonists

What type of agents stimulate receptors?

Antagonists

What type of agents block the action of receptors?

Intermediary metabolism, catabolism, immune response, inflammation

What are the four important effects of glucocorticoids?

Cortisone

What is an example of a glucocorticoid?

5-6 am

At what time does ACTH peak, leading to high cortisone levels?

High

Are cortisone levels generally high or low in the morning?

Low

Are cortisone levels generally high or low in the late afternoon to night?

Aldosterone

What is the specific mineralocorticoid regulated by the Renin Angiotensin Aldosterone System (RAAS)?

Regulating sodium and potassium reabsorption in the collecting tubules of the kidney

What is the primary function of mineralocorticoids?

Aldosterone

What is the product of the mineralocorticoid pathway in adrenocortical hormone biosynthesis?

Cortisol

What is the product of the glucocorticoid pathway in adrenocortical hormone biosynthesis?

Dehydroepiandrosterone (DHEA)

What is the product of the androgen and estrogen pathway in adrenocortical hormone biosynthesis?

Blocked at that point

What happens to hormone production when a particular enzyme in the steroidogenesis pathway is deficient?

21β-Hydroxylase (P450c21)

Deficiency of which enzyme will reduce the conversion of progesterone into 11-Deoxycorticosterone?

Salt wasting because of the lack of aldosterone

What is the result of 21β-Hydroxylase (P450c21) deficiency?

11β-Hydroxylase (P450c11)

Deficiency of which enzyme will reduce the conversion of 11-Deoxycorticosterone into corticosterone?

Salt wasting because of the lack of aldosterone

What is the consequence of 11β-Hydroxylase (P450c11) deficiency?

17α-Hydroxylase (P450c17)

Deficiency of which enzyme will reduce the conversion of pregnenolone into 17-Hydroxy-pregnenolone?

Decreased DHEA production (does not lead to salt-wasting symptoms)

What is the impact of 17α-Hydroxylase (P450c17) deficiency?

Hydrocortisone (Cortisol)

What is the standard corticosteroid to which all other glucocorticoids are compared for potency?

Betamethasone

Which long-acting glucocorticoid has the most anti-inflammatory effect, 25-40 times as much as Hydrocortisone?

Fludrocortisone

Which mineralocorticoid has the highest salt-retaining property?

Short to medium-acting, intermediate-acting, long-acting

What are the three categories of glucocorticoid preparations based on duration of activity?

Hydrocortisone (Cortisol)

Which short to medium-acting glucocorticoid has anti-inflammatory, topical, and salt-retaining potencies all rated as 1?

Cortisone

Which short to medium-acting glucocorticoid has zero topical potency but a salt-retaining property of 0.8?

Prednisone

Which short to medium-acting glucocorticoid has an anti-inflammatory potency of 4 and zero topical potency?

Methylprednisolone

Which short to medium-acting glucocorticoid has an anti-inflammatory potency of 5 and a topical potency of 5?

Meprednisone

Which short to medium-acting glucocorticoid has zero salt-retaining property?

Triamcinolone

Which intermediate-acting glucocorticoid has an anti-inflammatory potency of 5 and zero salt-retaining property?

Fluroprednisolone

Which intermediate-acting glucocorticoid has an anti-inflammatory potency of 15 and a topical potency of 7?

Dexamethasone

Which long-acting glucocorticoid has an anti-inflammatory potency of 30 and zero salt-retaining property?

Fludrocortisone

Which mineralocorticoid has an anti-inflammatory potency of 10 and a salt-retaining property of 250?

Angioneurotic edema, asthma, bee stings, contact dermatitis, drug reactions, allergic rhinitis, serum sickness, urticaria

What are some allergic reactions for which glucocorticoids are therapeutically indicated?

Lupus erythematosus, rheumatoid arthritis

What are two examples of collagen-vascular disorders treated with glucocorticoids?

Acute uveitis, allergic conjunctivitis, optic neuritis

What are some eye diseases for which glucocorticoids are indicated?

Inflammatory bowel disease

What gastrointestinal disease is an indication for glucocorticoid use?

Leukemia, lymphoma, autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura

What are some hematologic disorders treated with glucocorticoids?

Acute respiratory distress syndrome

What systemic inflammatory condition is an indication for glucocorticoid use, where sustained therapy can decrease mortality?

Sepsis

What infection is mentioned as an indication for glucocorticoid use?

Arthritis, bursitis, tenosynovitis

What inflammatory conditions of bones and joints are treated with glucocorticoids?

Dexamethasone

Which glucocorticoid is used in large doses to reduce emetic effects of chemotherapy and general anesthesia?

Cerebral edema (following brain surgery), multiple sclerosis

What are some neurologic disorders for which glucocorticoids are indicated?

Prevention and treatment of rejection (immunosuppression)

What is a key therapeutic indication for glucocorticoids in organ transplants?

Bronchial asthma, prenatal prevention of infant respiratory distress syndrome, sarcoidosis

What are some pulmonary diseases treated with glucocorticoids?

Nephrotic syndrome

What renal disorder is an indication for glucocorticoid use?

Atopic dermatitis, psoriasis, pemphigus, seborrheic dermatitis

What are some skin diseases for which glucocorticoids are indicated?

Malignant exophthalmos, subacute thyroiditis

What are some thyroid diseases treated with glucocorticoids?

Hypercalcemia, mountain sickness

What are two miscellaneous conditions for which glucocorticoids are used?

Hydrocortisone (Cortisol)

Which specific glucocorticoid is classified as short-acting, low-potency?

Desonide

What is an example of a low-potency similar drug to Hydrocortisone?

Fluticasone, Mometasone

What are examples of medium-potency similar drugs to Hydrocortisone?

Desoximetasone, Clobetasol

What are examples of high-potency similar drugs to Hydrocortisone?

Ointment for babies, insect bites, contact dermatitis, diaper rashes

For what conditions are medium-potency hydrocortisone-like drugs used topically?

Skin allergies

For what condition are high-potency hydrocortisone-like drugs used?

Activates glucocorticoid receptors, leading to altered gene transcription

What is the primary mechanism of action of Hydrocortisone?

Cholesterol/steroidal hormones

Glucocorticoids and mineralocorticoids are considered what type of hormones?

Suppressed inflammation and allergic reactions

What is the general outcome of hydrocortisone's action on gene transcription?

Replaces cortisol when deficient, such as in acute adrenal insufficiency

What is a crucial clinical use of Hydrocortisone related to hormone replacement?

Acute adrenal insufficiency, insect bites, contact dermatitis, status asthmaticus, thyroid storm

What are the clinical uses for Hydrocortisone?

Very tight airway during attacks

What characterizes a patient in status asthmaticus?

None common when used topically or at physiologic replacement doses

What are the common toxicities of Hydrocortisone when used appropriately?

More than 2 weeks

After what duration of use might glucocorticoids require tapering?

Prednisolone, Methylprednisolone, Dexamethasone, Betamethasone, Triamcinolone

What are some similar drugs to Prednisone?

Methylprednisolone

Which prednisone-like drug is used for Leptospirosis with pulmonary hemorrhage?

Glucocorticoid

What is the drug class of Prednisone?

Suppresses inflammation and immune response

What is the mechanism of action of Prednisone?

Wide variety of inflammatory, allergic, autoimmune, and neoplastic diseases; prevention of transplant rejection; asthma

What are the clinical uses of Prednisone?

Hematologic cancer

What type of cancer is specifically mentioned as responding well to steroids?

Adrenal suppression

What major toxicity of Prednisone can lead to an adrenal crisis?

Exogenous intake of steroids

What causes adrenal suppression?

Gout patients who overuse prednisone

Among which patient population is adrenal suppression due to prednisone common?

Weakness, hypotension, hyponatremia, hypokalemia, hypoglycemia, salt wasting, and sugar wasting

What are the manifestations of adrenal crisis?

Growth inhibition, muscle wasting, osteoporosis, salt retention, glucose intolerance, behavioral changes (steroid-induced psychosis)

What are other toxicities of Prednisone?

Disorientation and inability to recognize surroundings or companions

How might steroid-induced psychosis manifest?

IV form only

What is a characteristic of some similar drugs to Prednisone regarding their administration?

More potent

Why is Prednisone often used for more severe conditions?

Dexamethasone and Betamethasone

Which two high-potency glucocorticoids hasten fetal lung maturation?

34 weeks AOG

At what gestational age is fetal lung maturation usually completed?

Within 48 hours of an anticipated preterm birth (before 34 weeks' gestation)

When are Dexamethasone and Betamethasone administered to promote fetal lung maturation?

Local application, alternate-day therapy, or dose tapering

What three strategies can minimize glucocorticoid toxicities?

"Stress doses"

What is given to patients on long-term glucocorticoid therapy during serious illness or before major surgery?

Incremental IV doses to suppress inflammation and prevent adrenal crisis

What is the purpose of "stress doses"?

Slow dose-tapering

What process is crucial for patients withdrawing from long-term glucocorticoid therapy?

To allow recovery of normal adrenal function

What is the purpose of slow dose-tapering after long-term steroid use?

Adrenal insufficiency

What can occur if exogenous steroid medication is abruptly stopped after long-term use?

More than two weeks

How long does exposure to exogenous steroids typically need to be for adrenals to become unaccustomed to producing their own cortisol?

Fludrocortisone

What is the primary pharmaceutical preparation for mineralocorticoids?

Deoxycorticosterone

What is a similar drug to Fludrocortisone?

Mineralocorticoid

What is the drug class of Fludrocortisone?

Strong agonist of mineralocorticoid (aldosterone) receptors and moderate activation of glucocorticoid receptors

What is the mechanism of action of Fludrocortisone?

Increases Na+ reabsorption and H+ excretion

What specific physiological actions does Fludrocortisone perform?

Chronic adrenal insufficiency (Addison’s disease), congenital adrenal hyperplasia, adrenal replacement therapy post-adrenalectomy

What are the clinical uses for Fludrocortisone?

Addison's disease

What is another name for chronic adrenal insufficiency?

Salt and fluid retention (leading to hypertension and congestive heart failure), hypokalemia

What are the primary toxicities of Fludrocortisone?

Muscle wasting, osteoporosis, glucose intolerance, behavioral changes

What other toxicities of Fludrocortisone are attributed to its glucocorticoid effect?

Loop and thiazide diuretics

Which diuretics should be used with caution with Fludrocortisone due to the risk of additive hypokalemia?

Cushing’s Syndrome

What syndrome is caused by any condition that produces elevated glucocorticoid levels?

The different toxicities of your glucocorticoids

What does Cushing's Syndrome demonstrate about glucocorticoids?

Iatrogenic Cushing’s syndrome due to exogenous steroid intake

What is the most common cause of Cushing’s Syndrome?

Cortisol-secreting adrenal adenoma

What causes Adrenal Cushing’s syndrome?