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Additional Pharm Lecture > Corticosteroids > Flashcards

Corticosteroids Flashcards

1
Q

the secretion of adrenocortical steroids is controlled by the

A

pituitary release of corticotropin (ACTH)

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2
Q

in the pituitary, ACTH is synthesized as part of

A

pro-opiomelanocortin (POMC)

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3
Q

ACTH production is stimulated by

A

corticotropin-releasing hormone (CRH), synthesized in the hypothalamus

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4
Q

ACTH’s actions are mediated by

A

the melanocortin receptor 2 found in adrenal cortex

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5
Q

most endogenous cortisol is metabolized in the

A

liver

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6
Q

following metabolic conversion due to cortisol in the liver, steroids are excreted by the

A

kidneys
where 90% excreted in urine and can be measured as 17-OH

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7
Q

more than 90% of cortisol circulates bound to

A

corticosteroid-binding globulin

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8
Q

Molecular MOA of adrenocortical hormones
MOA is mediated by?
ligand-bound receptor complex is transported into nucleus, where it interacts with?
besides GREs, the complex influences function of other transcription factors which regulate?

A
  • glucocorticoid receptors or mineralocorticoid receptors
    side note: two genes for the corticoid receptor
  • glucocorticoid receptor elements in promoters of responsive genes
  • growth factors, cytokines, mediate anti-growth, anti-inflammatory, immunosuppressive
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9
Q

Physiologic effects - intermediate metabolism
glucocorticoids affect

A

carb, protein and fat metabolism
net result of glucocorticoid effects is to maintain an adequate glucose supply to the brain

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10
Q

Water and electrolyte balance
mineralocorticoids promotes the reabsorption of?

A

sodium in renal distal tubules
renal excretion of K+ and H+ is enhanced

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11
Q

Cardiovascular and blood cells
glucocorticoids potentiate vasocontrictor action of?
glucocorticoids casuse vasocontriction by?

A
  • adrenergic stimuli
  • suppressing mast cell degranulation
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12
Q

Cardiovascular and blood cells
glucocorticoids ___ plasma hemoglobin conc (erythrocytes and neutrophils) and ___ the total WBC count

A

increase; elevate

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13
Q

Cardiovascular and blood cells
glucocorticoids ___ the number of circulating eosinophils, basophils, monocytes, and lymphocytes

A

decrease

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14
Q

Immune system
glucocorticoids inhibit?
glucocorticoids suppress the release of?

A
  • prostaglandin and leukotriene production by inhibiting phospholipase A2
  • inflammatory cytokines and chemokines
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15
Q

CNS
corticosteroids ___ the blood brain barrier and can influence mood, sleep patterns

A

can cross

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16
Q

skeletal muscle
large amounts of glucocorticoids simulate

A

proteolysis, pain, and muscle weakness

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17
Q

Stress
glucocorticoid secretion in response to stressful stimuli is protective and

A

cortisol secretion increases with stress

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18
Q

Nonendocrine Use: inflammatory, allergic, and immunological disorders
chronic disease may require the

A

prolonged use of suppressive doses
but be careful bc of side effects

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19
Q

Allergic Disorders
inhaled steroids are first-line therapy for?
anaphylactic rxns, steroids are used as adjuncts
treatment?

A
  • asthma
  • prednisone, methylprednisone, triamcinolone, dexamethasone
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20
Q

Cerebal Edema
glucocorticoids most effective in?
treatment?

A

vasogenic type edema -> brain tumors
treatment may include prednisone

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21
Q

Bacterial meningitis
TNF-alpha and interleukin 1-beta play a role in?
Lipopolysaccharide (LPS) may trigger?
treatment?

A
  • meningeal inflammation
    -cytokine release
  • dexamethasone
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22
Q

Collagen disorders
high doses of glucocorticoids beneficial?
azathioprine or cyclophosphamide may slow progression of renal failure in?
agents of choice for?
treatment?

A
  • acute exacerbations
  • lupus nephritis
  • polymyositis and dermatomyositis
  • prednisone, methylprenisolone, triamcinolone, dexamethasone
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23
Q

Hematological disorders
glucocorticoids treat?
recommend as initial therapy for?
inhibit?
treatment?

A

-autoimmune hemolytic anemia (type II drug allergy)
- idiopathic thrombocytopenic purpura
-phagocytosis, increasing life span of platelet
- prednisone, dexamethasone

24
Q

Hepatic disease
glucocorticoids are initial therapy for?

A
  • subacute hepatic necrosis and autoimmune chronic hepatitis
    azathioprine allows for reduction of glucocorticoid dose
25
Renal disease methylprednisolone treats?
- idiopathic nephrotic syndrome
26
Respiratory disorders glucocorticoids like prednisone are used to treat? treatment for respiratory distress syndrome is neonates?
- pulmonary sarcoidosis - betamethasone or dexamethasone enhances maturation of lungs
27
Gastrointestinal rxns decrease the protection provided by the? gastric ulcers may be formed in patients with? synergism with NSAIDs may lead to increase in?
-gastric mucus barrier - rheumatoid arthritis - GI events may mask symptoms of peptic ulcers so hemorrhage may occur without pain
28
Edema cause fluid retention in patients with
-heart or kidney disease restrict dietary Na
29
Carb and lipid metabolism treatment may result in? can aggravate? serum triglyceride are ___
- hyperglycemia - diabetes - elevated
30
Hypokalemia - admin of high doses may cause hypokalemia and metabolic alkalosis severe hypokalemia may cause?
- asthenia, paralysis or arrhythmias restrict Na and eat more K
31
Osteonecrosis most commonly affects the? osteonecrosis associated with?
- femoral head - prolonged corticosteroid treatment and high doses of glucocorticoids
32
growth suppression long term glucocorticoid therapy
suppresses child growth
33
Myopathy glucocorticoid doses cause? myopathy associated with?
protein catabolism, myopathy and loss of muscle mass - triamcinolone
34
Skin and soft tissues common skin cancers when taking oral glucocorticoids? other adverse effects of the skin?
- non-melanoma skin cancers - acne, alopecia, striae
35
Cushingoid features
truncal obesity, buffalo hump, moon face, weight gain
36
Ocular effects - may elevate intraocular pressure causing? - may enhance development of - dont use in patients with ocular herpes bc of? - prolonged use may lead to?
- open-angle glaucoma - 2nd ocular infections by fungi or viruses - risk of corneal perforation - posterior subcapsular cataracts
37
HPA suppression exogenous admin will result in suppression of?
- HPA axis thru negative feedback doses admin just before or at bedtime are more suppressive than those given earlier in day
38
Pregnancy and lactation large doses used during pregnancy may result in?
- fetal adrenal hypoplasia and increase risk of cleft palate glucocorticoids are classified as FDA pregnancy category C
38
Pregnancy and lactation large doses used during pregnancy may result in?
- fetal adrenal hypoplasia and increase risk of cleft palate glucocorticoids are classified as FDA pregnancy category C
39
Physiologic and pharmacologic effects aldosterone promotes reabsorption of Na from
distal part of distal convoluted tubule, from the cortical collecting renal tubules
40
Drug selection fludrocortisone and what it is used to treat?
potent steroid with both glucocorticoid and mineralcorticoid activity - adrenocortical insufficiency
41
Endocrine Disorders Cushing's Syndrome cortisol excess due to?
- tumor in pituitary gland releasing ACTH - ectopic tumor - benign adrenal adenomas
42
Treatment of excessive cortisol
- metyrapone - ketoconozale (antifungal) - ketoconazole
43
Conn's syndrome (hyperaldosteronism) results from increased? most cases caused by? treatment?
- plasma aldosterone which results in hypokalemia, metabolic alkalosis and hypertension - adrenal adenomas or bilateral zona glomerulosa hyperplasia - surgery, spironolactone
44
Hypoadrenalism results from?
- inadequate secretion of ACTH or CRH - congential defects in steroidogenesis
45
Primary adrenocotical insufficiency or ADDISONS disease
autoimmune disease characterized by antibodies against adrenal antigens
46
Secondary adrenocortical insufficiency
caused by surgical ablation of pituitary, pituitary disease or pituitary suppression after longterm glucocorticoids
47
Diagnosis for Hyposecretion of adrenocortical hormones
synthetic ACTH used to test adrenal function in normal individuals, after single iv injection, there is a peak of plasma cortisol and aldosterone 30-60 min later subnormal response confirms diagnosis of adrenal insufficiency
48
Cosyntropin test no rise in cortisol or 17OHCS result in slow rise in cortisol and 17OHCS result in
- addison's due to adrenal failure - pituitary failure
49
treatment for adrenocortical insufficiency
- hydrocortisone and cortisone for initial treatment - fludrocortisone added when hydrocortisone reduced - prednisone and prednisolone potentially
50
Hydrocortisone (activity, half life, uses)
- potent mineralcorticoid activity - half life 80-118 min - adrenocortical insufficiency, anti-inflammatory, ulcerative colitis
51
Prednisone (activity, half life, uses)
- mineralocorticoid activity - half life 60 min - allergic states, autoimmune disorders, dermatologic conditions, edematous states, endocrine disorders, gastrointestinal diseases, hematologic disorders, multiple sclerosis, neoplastic diseases, ophthalmic diseases, respiratory diseases, rheumatic disorders, TB meningitis
52
Triamcinolone (activity, half life, uses)
- no mineralocorticoid activity - half life greater than 200 min - intralesional, nasal inhalation, ocular inflammatory, bronchial asthma, oral lesions and ulcerative lesions, adrenocortical insufficiency, derm issues, endocrine disorders, gastro issues, hemtolotic, neoplastic, nephrotic, allergic, respiratory, lupus erythematosus
53
Dexamethasone (activity, half life, uses)
- no mineralocorticoid activity - half life greater than 300 min - anti-inflammatory or immunosuppressant, conjuctivitis, ear issues
54
Fludrocortisone acetate (activity, half life, adverse effects, uses)
- mineralocorticoid activity - half life greater than 35 min - cardiovascular, CNS, derm, endocrine, GI, neuromuscular, ocular - treat addisons disease, adrenogential syndrome
55
Spironolactone (activity, activity, pharmacodynamics, half life)
- renal competitive aldosterone antagonist - increasing sodium chloride and water excretion while conserving potassium - mineralocorticoid activity - half life greater than 10 min BLACK BOX WARNING: show tumors in chronic toxicity studies in rats
56
Cosyntropin
- synthetic derivative of ACTH - stimualtes adrenal cortex to secrete glucocorticoids, androgenic substances, and aldosterone - used in diagnostic test to differentiate primary adrenal from secondary adrenocortical insufficiency

Additional Pharm Lecture (2 decks)

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