Steroids Flashcards

1
Q

MOA of Glucocorticoids

3 things

A
  • 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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2
Q

ADME of Glucocorticoids

A
  • 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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3
Q

Dosage of Glucocorticoids

4 things

A
  • 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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4
Q

ADRs of Glucocorticoids

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

Endogenous Glucocorticoids

A

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

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6
Q

Short/Medium acting glucocorticoids (3)

A
  • Hydrocortisone
  • Prednisone
  • Prednisolone (methylprednisolone)
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7
Q

Intermediate/Long acting glucocorticoids (3)

A
  • Triamcinolone
  • Betamethasone
  • Dexamethasone
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8
Q

Intra-articular injections (glucocorticoids)

5 things

A
  • 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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9
Q
Epidural injections (glucocorticoids)
3 things
A
  • Treat leg or back pain
  • Not first line treatment
  • Drugs used: hydrocortisone, methylprednisolone, triamcinolone)
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10
Q
Dose packs (glucocorticoids)
2 things
A
  • High dose initially, then tapers off

- Drugs used: methylprednisolone, dexamethasone, betamethasone, triamcinolone

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11
Q

Topical (glucocorticoids)

3 things

A
  • Very affective for skin disease
  • Absorption increased by increased skin temperature and hydration
  • Ointment better than creams
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12
Q

Opthalmic (glucocorticoids)

3 things

A
  • For eye disease
  • Systemic absorption is rare
  • Not for glaucoma or cataracts
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13
Q

Enemas (glucocorticoids)

2 things

A
  • For ulcerative colitis

- Drugs used: hydrocortisone

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14
Q

Aerosols (glucocorticoids)

2 things

A
  • For asthma and allergic rhinitis

- Local effect only, first pass effect decreases systemic absorption

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15
Q

Stimulation of Lung Maturation in the Fetus

A

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

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16
Q

Acute Addison’s Disease

3 things

A
  • Decreased cortisol levels
  • Caused by: stress or infection
  • Treatment: start early, correct fluid and electrolyte abnormalities as well as underlying cause, hydrocortisone
17
Q

Chronic Addison’s Disease

3 things

A
  • Decreased cortisol levels
  • Hyperpigmentation, weakness, fatigue, weight loss, hypotension, inability to maintain blood glucose
  • Treatment: Hydrocortisone and add Fludrocortisone
18
Q

Congenital Adrenal Hyperplasia

4 things

A
  • 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
19
Q

Cushing’s Syndrome

4 things

A
  • 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)
20
Q

Aldosteronism

A
  • Increased cortisol levels
  • Excessive production of aldosterone by an adrenal adenoma
  • HTN, polyuria, polydipsia, weakness, tetany (due to K loss)
21
Q

Mitotane

2 things

A
  • Drug used for Cushing’s syndrome

- Management of adrenocortical carcinoma

22
Q

Metyrapone

4 things

A
  • Drug used for Cushing’s syndrome
  • Blocks production of cortisol (inhibits 11B-hydroxylase)
  • ADRs: salt/water retention and hirsutism
  • Adrenal function tests
23
Q

Mifepristone

4 things

A
  • 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
24
Q

Nutritional measures to minimize adverse effects of glucocorticoids
6 things

A
  • Increase potassium and sodium intake
  • Watch calories
  • Increase protein
  • Increase vitamin D (to decrease bone loss, may add bisphosphonates)
  • Antacids (3/4 times daily)
25
Q

Mineralocorticoids (3)

A
  • Aldosterone
  • Desoxycorticosterone
  • Fludrocortisone
26
Q

Aldosterone

5 things

A
  • 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
27
Q

Desoxycorticosterone

2 things

A
  • Not used clinically

- Precursor of aldosterone

28
Q

Fludrocortisone

2 things

A
  • Oral
  • Used in Addison’s disease, hypopituitarism, orthostatic hypotension, aldosterone inssufficiency, CAH (only when symptomatic)
29
Q

Testosterone

4 things

A
  • 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
30
Q

7 uses for anabolic steroids

A
  • 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
31
Q

Adverse effects of anabolic steroids

  • Dermatologic (3)
  • Men (4)
  • Women (2)
  • Children (1)
  • Cardiovascular (5)
  • Abuse (5)
  • Other (6)
A
  • 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
32
Q

Anabolic Steroids (4)

A
  • Danazol
  • Methenolone
  • Nandrolone
  • Stanozolol
33
Q

Danazol

3 things

A
  • Weak androgen
  • Binds to androgen, progesterone, and glucocorticoid receptors
  • Used for: endometriosis, fibrocystic disease of the breast, hematologic disorders, suppression of ovarian function
34
Q

Nandrolone

1 thing

A

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

35
Q

Methenolone

1 thing

A

Used for: aplastic anemia, breast cancer, osteoporosis

36
Q

Stanozolol

1 thing

A

Used for: prophylaxis and treatment of hereditary angioedema

37
Q

Synthetic human ACTH

A

Cosyntropin

38
Q

Androstenedione

A
  • 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