ADRs of Glucocorticoids - Metabolic (5) - Catabolic (2) - Anti-inflammatory (4) - CNS (5) - Dermatologic (5) - GI (3) - Renal (3) - Other (3)

- Metabolic: increase activities for gluconeogenesis, increaed serum glucose, lipolysis, and insulin , muscle catabolism increases AA availability, - Catabolic: decreased muscle mass and weakness, osteoporosis - Anti-inflammatory: decreases prostaglandins, inhibits leukocytes and tissue macrophages, causes vasoconstriction - CNS: can decrease seizure threshold, NO increase in intracranial pressure, anxiety, insomnia, steroid psychosis - Derm: SQ fat redistribution (moon face), skin thinning, acne, impaired wound healing, fungal infections - GI: increased acid and pepsin, increased fat absorption, decreased calcium absorption (through vit. D) - Renal: decreased GFR, excess water retention, adrenal suppression (when used more than 2-3 days) - Other: suppresion of ACTH, TSH, and FSH, increased platelets and RBCs, surfactant production in unborn babies

Steroids Flashcards by Katie Kirtley

MOA of Glucocorticoids

3 things

Effects mediated by glucocorticoid recepters
Hormone enters cell and binds receptor -> transported to nucleus -> affects RNA transcription and protein synthesis
Feedback suppression for ACTH

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ADME of Glucocorticoids

A/D: 75% bound to corticosteroid-binding protein (CBG), 5% bound to albumin, 20% free
M: half-life 60-90 minutes

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Dosage of Glucocorticoids

4 things

Regimen based on seriousness of disease, amount required for desired effect, duration of therapy
Lowest possible dose
Do NOT stop abruptly
Alternate day dosing: increase in efficacy and decrease in ADRs (useful when large doses are required for prolonged periods)

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ADRs of Glucocorticoids

Metabolic (5)
Catabolic (2)
Anti-inflammatory (4)
CNS (5)
Dermatologic (5)
GI (3)
Renal (3)
Other (3)

Metabolic: increase activities for gluconeogenesis, increaed serum glucose, lipolysis, and insulin*, muscle catabolism increases AA availability,
Catabolic: decreased muscle mass and weakness, osteoporosis
Anti-inflammatory: decreases prostaglandins, inhibits leukocytes and tissue macrophages, causes vasoconstriction
CNS: can decrease seizure threshold, NO increase in intracranial pressure, anxiety, insomnia, steroid psychosis
Derm: SQ fat redistribution (moon face), skin thinning, acne, impaired wound healing, fungal infections
GI: increased acid and pepsin, increased fat absorption, decreased calcium absorption (through vit. D)
Renal: decreased GFR, excess water retention, adrenal suppression (when used more than 2-3 days)
Other: suppresion of ACTH, TSH, and FSH, increased platelets and RBCs, surfactant production in unborn babies

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Endogenous Glucocorticoids

Cortisol (made from cholesterol and released under influence of ACTH)

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Short/Medium acting glucocorticoids (3)

Hydrocortisone
Prednisone
Prednisolone (methylprednisolone)

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Intermediate/Long acting glucocorticoids (3)

Triamcinolone
Betamethasone
Dexamethasone

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Intra-articular injections (glucocorticoids)

5 things

Treat joint disease (esp. RA)
Fast impact on pain and stiffness
Painful, may cause flushing, deterioration, HTN
Do NOT repeat more than every 3 months (leads to necrosis)
Drugs used: betamethasone, dexamethasone, methylprednisolone, triamcinolone

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Epidural injections (glucocorticoids)
3 things

Treat leg or back pain
Not first line treatment
Drugs used: hydrocortisone, methylprednisolone, triamcinolone)

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Dose packs (glucocorticoids)
2 things

High dose initially, then tapers off

- Drugs used: methylprednisolone, dexamethasone, betamethasone, triamcinolone

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Topical (glucocorticoids)

3 things

Very affective for skin disease
Absorption increased by increased skin temperature and hydration
Ointment better than creams

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Opthalmic (glucocorticoids)

3 things

For eye disease
Systemic absorption is rare
Not for glaucoma or cataracts

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Enemas (glucocorticoids)

2 things

For ulcerative colitis

- Drugs used: hydrocortisone

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Aerosols (glucocorticoids)

2 things

For asthma and allergic rhinitis

- Local effect only, first pass effect decreases systemic absorption

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Stimulation of Lung Maturation in the Fetus

If premature newborn is under 34 weeks, betamethasone can be given to stimulate surfactant production in the lungs.

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Acute Addison’s Disease

3 things

Decreased cortisol levels
Caused by: stress or infection
Treatment: start early, correct fluid and electrolyte abnormalities as well as underlying cause, hydrocortisone

Chronic Addison’s Disease

3 things

Decreased cortisol levels
Hyperpigmentation, weakness, fatigue, weight loss, hypotension, inability to maintain blood glucose
Treatment: Hydrocortisone and add Fludrocortisone

Congenital Adrenal Hyperplasia

4 things

Group of disorders characterized by defects in synthesis of cortisol (deficiency in an enzyme needed to convert cholesterol into cortisone: 21-hydroxylase most common)
May seel virilization, HTN and hypokalemia
In high risk pregnancies, protect infant by giving mother dexamethasone
Infant: when CAH is first seen it may be an acute adrenal crisis and should be treated with IV hydrocortison, mineralocorticoids, and electrolytes

Cushing’s Syndrome

4 things

Increased cortisol levels
Usually due to bilateral adrenal hyperplasia secondarily to pituitary adenoma
Moon face, trunk obesity, muscle wasting, thinning of skin, striae, bruising, poor wound healing, osteoporosis, mental disorders, HTN, diabetes
Treatment: surger (to remove adenoma), radiation, drugs (mitotane, metyrapone, mifepristone)

Aldosteronism

Increased cortisol levels
Excessive production of aldosterone by an adrenal adenoma
HTN, polyuria, polydipsia, weakness, tetany (due to K loss)

Mitotane

2 things

Drug used for Cushing’s syndrome

- Management of adrenocortical carcinoma

Metyrapone

4 things

Drug used for Cushing’s syndrome
Blocks production of cortisol (inhibits 11B-hydroxylase)
ADRs: salt/water retention and hirsutism
Adrenal function tests

Mifepristone

4 things

Drug used for Cushing’s syndrome
Glucocorticoid receptor antagonist
Useful to control hyperglycemia in patients who are not surgical candidates
ADRs: hypokalemia, adrenal insufficiency, endometrial hyperplasia

Nutritional measures to minimize adverse effects of glucocorticoids
6 things

Increase potassium and sodium intake
Watch calories
Increase protein
Increase vitamin D (to decrease bone loss, may add bisphosphonates)
Antacids (3/4 times daily)

Mineralocorticoids (3)

- Aldosterone - Desoxycorticosterone - Fludrocortisone

Aldosterone | 5 things

- Not firmly bound to serum proteins - Increases sodium reabsorption from urine, sweat, salivary glands, and GI - Increases excretion of potassium - Not used clinically due to short DOA - Synthesized in zona glomerulosa and stimulated by ACTH

Desoxycorticosterone | 2 things

- Not used clinically | - Precursor of aldosterone

Fludrocortisone | 2 things

- Oral - Used in Addison's disease, hypopituitarism, orthostatic hypotension, aldosterone inssufficiency, CAH (only when symptomatic)

Testosterone | 4 things

- Schedule II - Controls development and maintenance of male sex organs and secondary male sex characteristics - Produces systemic anabolic effects (increased nitrogen, calcium, sodium, potassium, chloride, phosphate) causing increased water retention and bone growth, vascular and less fatty skin, increased erythropoiesis - Anabolic steroids are chemical derivatives of testosterone

7 uses for anabolic steroids

- Help build tissue and prevent breakdown of tissue in debilitating disease - Androgen replacement therapy: hypogonadal men - Protein anabolic agents: after trauma or surgery - Aplastic anemia, sickle cell, hemolytic anemia - Osteoporosis - Growth stimulators in boys with delayed puperty - Aging-androgen production falls with age

Adverse effects of anabolic steroids - Dermatologic (3) - Men (4) - Women (2) - Children (1) - Cardiovascular (5) - Abuse (5) - Other (6)

- Derm: acne, oily, hirsutism - Men: increased libido, atrophy of testicles, aggressiveness, spermatogenesis failure - Women: masculinization and decreased breast size - Children: arrested bone growth (due to premature fusion of epiphysis) - CV: MI, HTN, CHF, thrombosis, cardiac death - Abusers: paranoid psychosis, mania, eurphoria, depression, withdrawal syndrome - Other: liver cancer, stroke, hot flashes, headache, edema, weight gain

Anabolic Steroids (4)

- Danazol - Methenolone - Nandrolone - Stanozolol

Danazol | 3 things

- Weak androgen - Binds to androgen, progesterone, and glucocorticoid receptors - Used for: endometriosis, fibrocystic disease of the breast, hematologic disorders, suppression of ovarian function

Nandrolone | 1 thing

Most effect with regard to increase in hematocrit and response rates in chronic renal failure (so is testosterone)

Methenolone | 1 thing

Used for: aplastic anemia, breast cancer, osteoporosis

Stanozolol | 1 thing

Used for: prophylaxis and treatment of hereditary angioedema

Synthetic human ACTH

Cosyntropin

Androstenedione

- Precursor to testosterone and estrogen - Does not increase testosterone in young men (increases estrogen and lowers HDL) - Structurally similar to steroids - May increase heart diseases and cancers