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Pharmacology Exam #2 > Adrenocorticosteroids and Antagonists -pg6 onwards > Flashcards

Adrenocorticosteroids and Antagonists -pg6 onwards Flashcards

1
Q

What function is impaired in Congenital Adrenal Hyperplasia?

A

mostly caused by lack of P450c21 (21-B hydroxylase) function, resulting in the accumulation of 17-hydroxyprogesterone

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2
Q

Lack of cortisol synthesis in Congenital Adrenal hyperplasia causes what?

A

Lack of cortisol synthesis will cause increased release of ACTH and consequently adrenocorticol hyperplasia and increased production of 17-hydroxy-progesterone (normally involved in cortisol production) which will lead to increased production of androgens.

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3
Q

What will the increased production of androgens cause in Congenital Adrenal hyperplasia?

A

The production of androgens will cause virilization of the fetus (normally fine but in this case an unhealthy biological development of the fetus into a male or female sex. ex: if fetus is genetically female and virilization causes the development of male sex organs, the child will be born with testes or ambiguous sex.)

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4
Q

How do you treat Congenital Adrenal hyperplasia in the mother?

A

Give Dexamethasone to the mother to prevent congenital effects

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5
Q

if defect in 11-B hydroxylase what occurs?

A

accumulation of 11 deoxycorticocosterone- normally degraded to androgen- (has mineralocorticoid activity) will result in hypernatermia, hypertension, hypokalemia and hypogonadism

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6
Q

how do you treat a 11-B hydroxylase defect?

A

Dexamethasone

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7
Q

What are the two forms of Adrenal Corticol HYPOFUNCTION?

A
  1. Congenital Adrenal Hyperplasia
  2. 11-B hydroxylase defect

treat both with Dexamethasone

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8
Q

What are symptoms due to in Cushings Syndrome?

A

due to glucocorticoid Hypersecretion (HTN, DM, poor wound healing, osteoporosis, muscle wasting, fat redistribution and facial puffiness, mental disorders)

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9
Q

How do you treat Cushings Syndrome?

A
  • irradiation or surgical removal of tumor or bilateral adrenolectomy
  • -> after adrenolectomy pt has to be maintained on hydrocortisone and sodium sparing drug (FLUDROCORTISONE)

*any dose adjustment of corticosteroids has to be gradually tapered; abrupt change causes withdrawal.

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10
Q

Lack of cortisol synthesis in Congenital Adrenal hyperplasia causes what?

A

Lack of cortisol synthesis will cause increased release of ACTH and consequently adrenocorticol hyperplasia and increased production of 17-hydroxy-progesterone which will lead to increased production of androgens.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What will the increased production of androgens cause in Congenital Adrenal hyperplasia?

A

The production of androgens will cause virilization of the fetus (normally fine but in this case an unhealthy biological development of the fetus into a male or female sex. ex: if fetus is genetically female and virilization causes the development of male sex organs, the child will be born with testes or ambiguous sex.)

How well did you know this?
1
Not at all
2
3
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5
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12
Q

What is Aldosteronism caused by?

A

Adrenal adenomas producing excessive aldosterone, causing Hypernatremia and hypokalemic alkalosis

-could also be due to deficiency in the biosynthetic pathway; producing excessive deoxycorticosterone, corticosterone or 18-hydroxycorticosterone, which have mineralocorticoid function.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

How do you treat Aldosteronism?

A

Patients are treated with Spirinolactone, an aldosterone receptor antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What would you use to diagnose Adrenal Corticoid dysfunction?

A

Dexamethasone used for diagnosis of Cushings Disease (not syndrome). Suppression of ACTH is caused in bonafide Cushing’s disease as opposed to ectopic tumors secreting cortisol

aka: if giving pt dexamethasone, Cortisol wont decrease if unless patient has cushings DISEASE (tumor on pituitary).

How well did you know this?
1
Not at all
2
3
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5
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15
Q

What is Cushings Syndrome due to?

A

It is the bilateral adrenal Hyperplasia secondary to a pituitary adenoma (Cushings Disease) or nodular carcinoma or the adrenal or ectopic tumor OVERPRODUCTION OF CORTISOL

  • Cushings Disease is a kind of Cushings Syndrome. Other causes of Cushings Syndrome include
    taking drugs that increase ACTH -> too much cortisol
    Tumor of the adrenal gland
    Tumor elsewhere in the body that produces cortisol
    Tumors elsewhere in the body that produce ACTH (such as the pancreas, lung, and thyroid)

treat both with Dexamethasone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What is Corticosteroid treatment used for in mothers?

A

Corticosteroid treatment (Betamethasone, IM) of the mother reduces respiratory distress syndrome in prematurely delivered infants by stimulating pulmonary surfactant secretion in the fetal lung.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

When are Corticosteroids used for Non-adrenal disorders?

A
  1. Supress inflammatory and immune responses and alter leukocyte activity.
  2. treatment of transplant rejection
How well did you know this?
1
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18
Q

Corticosteroids supress inflammatory and immune responses and alter leukocyte activity, so what are they used to treat?

A

hence used for treating inflammatory and hyperimmune disorders including those due to autoimmune processes (such as pemphigus, myasthenia gravis, sarcoidosis etc), type I hypersensitivity (allergic hypersensitivity such as urticaria and bronchospasm) etc.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

How should corticosteroids be used?

A

Corticosteroids relieve symptoms but not the cause. If CHRONIC therapy is warranted, medium to intermediate acting steroids such as prednisone/prednisolone should be used preferably alternate day therapy, as well as ancillary drugs such as METHOTREXATE or AZATHIOPRINE to reduce dosage of corticosteroid.

-taper! to avoid drug withdrawal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Because Corticosteroids cause immunosupression what should be tested in certain patients?

A
  • Chest Xrays to check for dormant MYCOBACTERIUM
  • presence of DM, Peptic Ulcers, Osteoporosis, and psychological disturbance are likely to be worsened by corticosteroid therapy –> assess CV functions
How well did you know this?
1
Not at all
2
3
4
5
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21
Q

Why are corticosteroids used to treat transplant rejections?

A

a) corticosteroids supress antigen expression in transplanted tissue.
b) delay revascularization
c) suppress T cell and B cell fx hence reduce acute and chronic transplant rejection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are Corticosteroid toxicities?

A

short term (less than 2 weeks): no serious AE’s
chronic treatment: leads to iatrogenic (symptoms due to illness) Cushings Syndrome.
-changes in appearance due to fat redistribution (steatosis)
(facial puffiness, trunk obesity, fat in neck, back an supraclavicular fosse)
-Osteoporosis
-DM
-Muscle wasting,
-ti

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is Aldosteronism caused by?

A

Adrenal adenomas producing excessive aldosterone, causing Hypernatremia and hypokalemic alkalosis

-could also be due to deficiency in the biosynthetic pathway; producing excessive deoxycorticosterone, corticosterone or 18-hydroxycorticosterone, which have mineralocorticoid function.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

How do you treat Aldosteronism?

A

Patients are treated with Spirinolactone, an aldosterone receptor antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

What would you use to diagnose Adrenal Corticoid dysfunction?

A

Dexamethasone used for diagnosis of Cushings Disease (not syndrome). Suppression of ACTH is caused in bonafide Cushing’s disease as opposed to ectopic tumors secreting cortisol

aka: if giving pt dexamethasone, Cortisol wont decrease if unless patient has cushings DISEASE (tumor on pituitary).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

What is Cushings Syndrome due to?

A

It is the bilateral adrenal Hyperplasia secondary to a pituitary adenoma (Cushings Disease) or nodular carcinoma or the adrenal or ectopic tumor OVERPRODUCTION OF CORTISOL

  • Cushings Disease is a kind of Cushings Syndrome. Other causes of Cushings Syndrome include
    taking drugs that increase ACTH -> too much cortisol
    Tumor of the adrenal gland
    Tumor elsewhere in the body that produces cortisol
    Tumors elsewhere in the body that produce ACTH (such as the pancreas, lung, and thyroid)

treat both with Dexamethasone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

What is Corticosteroid treatment used for in mothers?

A

Corticosteroid treatment (Betamethasone, IM) of the mother reduces respiratory distress syndrome in prematurely delivered infants by stimulating pulmonary surfactant secretion in the fetal lung.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

When are Corticosteroids used for Non-adrenal disorders?

A
  1. Supress inflammatory and immune responses and alter leukocyte activity.
  2. treatment of transplant rejection
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Corticosteroids supress inflammatory and immune responses and alter leukocyte activity, so what are they used to treat?

A

hence used for treating inflammatory and hyperimmune disorders including those due to autoimmune processes (such as pemphigus, myasthenia gravis, sarcoidosis etc), type I hypersensitivity (allergic hypersensitivity such as urticaria and bronchospasm) etc.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

How should corticosteroids be used?

A

Corticosteroids relieve symptoms but not the cause. If CHRONIC therapy is warranted, medium to intermediate acting steroids such as prednisone/prednisolone should be used preferably alternate day therapy, as well as ancillary drugs such as METHOTREXATE or AZATHIOPRINE to reduce dosage of corticosteroid.

-taper! to avoid drug withdrawal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

Because Corticosteroids cause immunosupression what should be tested in certain patients?

A
  • Chest Xrays to check for dormant MYCOBACTERIUM
  • presence of DM, Peptic Ulcers, Osteoporosis, and psychological disturbance are likely to be worsened by corticosteroid therapy –> assess CV functions
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

Why are corticosteroids used to treat transplant rejections?

A

a) corticosteroids supress antigen expression in transplanted tissue.
b) delay revascularization
c) suppress T cell and B cell fx hence reduce acute and chronic transplant rejection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

What are Corticosteroid toxicities?

A

short term (less than 2 weeks): no serious AE’s
chronic treatment: leads to iatrogenic (symptoms due to illness) Cushings Syndrome.
-changes in appearance due to fat redistribution (steatosis)
(facial puffiness, trunk obesity, fat in neck, back an supraclavicular fosse)
-Osteoporosis
-DM
-Muscle wasting,
-thinning

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

What is Aldosteronism caused by?

A

Adrenal adenomas producing excessive aldosterone, causing Hypernatremia and hypokalemic alkalosis

-could also be due to deficiency in the biosynthetic pathway; producing excessive deoxycorticosterone, corticosterone or 18-hydroxycorticosterone, which have mineralocorticoid function.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

How do you treat Aldosteronism?

A

Patients are treated with Spirinolactone, an aldosterone receptor antagonist

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

What would you use to diagnose Adrenal Corticoid dysfunction?

A

Dexamethasone used for diagnosis of Cushings Disease (not syndrome). Suppression of ACTH is caused in bonafide Cushing’s disease as opposed to ectopic tumors secreting cortisol

aka: if giving pt dexamethasone, Cortisol wont decrease if unless patient has cushings DISEASE (tumor on pituitary).

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

What is Cushings Syndrome due to?

A

It is the bilateral adrenal Hyperplasia secondary to a pituitary adenoma (Cushings Disease) or nodular carcinoma or the adrenal or ectopic tumor OVERPRODUCTION OF CORTISOL

  • Cushings Disease is a kind of Cushings Syndrome. Other causes of Cushings Syndrome include
    taking drugs that increase ACTH -> too much cortisol
    Tumor of the adrenal gland
    Tumor elsewhere in the body that produces cortisol
    Tumors elsewhere in the body that produce ACTH (such as the pancreas, lung, and thyroid)

treat both with Dexamethasone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

What is Corticosteroid treatment used for in mothers?

A

Corticosteroid treatment (Betamethasone, IM) of the mother reduces respiratory distress syndrome in prematurely delivered infants by stimulating pulmonary surfactant secretion in the fetal lung.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

When are Corticosteroids used for Non-adrenal disorders?

A
  1. Supress inflammatory and immune responses and alter leukocyte activity.
  2. treatment of transplant rejection
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

Corticosteroids supress inflammatory and immune responses and alter leukocyte activity, so what are they used to treat?

A

hence used for treating inflammatory and hyperimmune disorders including those due to autoimmune processes (such as pemphigus, myasthenia gravis, sarcoidosis etc), type I hypersensitivity (allergic hypersensitivity such as urticaria and bronchospasm) etc.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

How should corticosteroids be used?

A

Corticosteroids relieve symptoms but not the cause. If CHRONIC therapy is warranted, medium to intermediate acting steroids such as prednisone/prednisolone should be used preferably alternate day therapy, as well as ancillary drugs such as METHOTREXATE or AZATHIOPRINE to reduce dosage of corticosteroid.

-taper! to avoid drug withdrawal

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

Because Corticosteroids cause immunosupression what should be tested in certain patients?

A
  • Chest Xrays to check for dormant MYCOBACTERIUM
  • presence of DM, Peptic Ulcers, Osteoporosis, and psychological disturbance are likely to be worsened by corticosteroid therapy –> assess CV functions
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

Why are corticosteroids used to treat transplant rejections?

A

a) corticosteroids supress antigen expression in transplanted tissue.
b) delay revascularization
c) suppress T cell and B cell fx hence reduce acute and chronic transplant rejection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

What are short term Corticosteroid toxicities?

A

short term (less than 2 weeks): no serious AE’s

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

What can the mineralocorticoid activity of cortisone/hydrocortisone cause?

A

Electrolyte imbalances (Hypernatremia, fluid retention, hypokalemia, hyperchloremic alkalosis) causing HTN

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
46
Q

What do you do if a pt with Hypoproteinemia, liver disease or renal disease is being treated with corticosteroids?

A

EDEMA may occur in these patients, hence they must be placed on high protein and K+ enriched diet.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
47
Q

What toxicities occur in heart patients taking corticosteroids?

A

may cause HF in these patients. Effects can be reduced by switching to non-salt retaining steroids, sodium restriction and potassium supplements.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
48
Q

What toxicites occur in children taking corticosteroids?

A

may stunt growth

How well did you know this?
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49
Q

What else may corticosteroid use cause?

A

PU, Hypomania, acute psychosis, depression, cataracts, glaucoma

50
Q

What are chronic corticosteroid use toxicites?

A

chronic treatment: leads to iatrogenic (symptoms due to illness) Cushings Syndrome.
-changes in appearance due to fat redistribution (steatosis)
(facial puffiness, trunk obesity, fat in neck, back an supraclavicular fosse)
-Osteoporosis
-DM
-Muscle wasting,
-thinning of skin
-increased facial hair growth
-punctate (studded/ tiny holes) acne
-aseptic necrosis of the hip

51
Q

What can the mineralocorticoid activity of cortisone/hydrocortisone cause?

A

Electrolyte imbalances (Hypernatremia, fluid retention, hypokalemia, hyperchloremic alkalosis) causing HTN

52
Q

What do you do if a pt with Hypoproteinemia, liver disease or renal disease is being treated with corticosteroids?

A

EDEMA may occur in these patients, hence they must be placed on high protein and K+ enriched diet.

53
Q

What toxicities occur in heart patients taking corticosteroids?

A

may cause HF in these patients. Effects can be reduced by switching to non-salt retaining steroids, sodium restriction and potassium supplements.

54
Q

What toxicites occur in children taking corticosteroids?

A

may stunt growth

55
Q

What else may corticosteroid use cause?

A

PU, Hypomania, acute psychosis, depression, cataracts, glaucoma

56
Q

What are chronic corticosteroid use toxicites?

A

chronic treatment: leads to iatrogenic (symptoms due to illness) Cushings Syndrome.
-changes in appearance due to fat redistribution (steatosis)
(facial puffiness, trunk obesity, fat in neck, back an supraclavicular fosse)
-Osteoporosis
-DM
-Muscle wasting,
-thinning of skin
-increased facial hair growth
-punctate (studded/ tiny holes) acne
-aseptic necrosis of the hip

57
Q

What can the mineralocorticoid activity of cortisone/hydrocortisone cause?

A

Electrolyte imbalances (Hypernatremia, fluid retention, hypokalemia, hyperchloremic alkalosis) causing HTN

58
Q

What do you do if a pt with Hypoproteinemia, liver disease or renal disease is being treated with corticosteroids?

A

EDEMA may occur in these patients, hence they must be placed on high protein and K+ enriched diet.

59
Q

What toxicities occur in heart patients taking corticosteroids?

A

may cause HF in these patients. Effects can be reduced by switching to non-salt retaining steroids, sodium restriction and potassium supplements.

60
Q

What toxicites occur in children taking corticosteroids?

A

may stunt growth

61
Q

What else may corticosteroid use cause?

A

PU, Hypomania, acute psychosis, depression, cataracts, glaucoma

62
Q

What are chronic corticosteroid use toxicities?

A

chronic treatment: leads to iatrogenic (symptoms due to illness) Cushings Syndrome.
-changes in appearance due to fat redistribution (steatosis)
(facial puffiness, trunk obesity, fat in neck, back an supraclavicular fosse)
-Osteoporosis
-DM
-Muscle wasting,
-thinning of skin
-increased facial hair growth
-punctate (studded/ tiny holes) acne
-aseptic necrosis of the hip

63
Q

What is chronic (>2 wks) corticosteroid administration likely to cause?

A
  • Adrenal Suppression (Glucocorticoid-induced adrenal insufficiency)
  • must gradually taper off
  • if suddenly withdrawn, Glucocorticoid-induced adrenal insufficiency will cause major withdrawal effects
64
Q

How should corticosteroids be administered?

A

After the initial dose required to suppress symptoms, the dose could be reduced to what is sufficient to keep symptoms down. Alternate day drug therapy is judicious.

For large dose therapy, medium/intermediate- acting steroids with no mineralocorticoid activity are preferred

** caution in pts with PU, heart disease, HTN w/ HF, inf with Varicella, TB, DM, Osteoporosis or glaucoma

65
Q

which patients should you be cautious administering corticosteroids to?

A

pts with PU, heart disease, HTN w/ HF, inf with Varicella, TB, DM, Osteoporosis or glaucoma

(because they would excerbate these conditions. most of these are AE’s of corticosteroid use..)

66
Q

What dosage forms are available to minimize corticosteroid toxicity?

A
  1. Topical preparations for skin disease, opthalmic forms for eye disease
  2. Intra-articular injections for joint disease
  3. Inhaled steroids for asthma
  4. Hydrocortisone enemas for Ulcerative Collitis etc are ways of administering the drugs to the affected region minimizing systemic effects.
67
Q

What are the corticosteroids used for Asthma?

A 
Aerosols
1. Beclomethasone (QVAR)
2. Triamcinolone (Azmacort)
3. Budesonide (Pulmicort)
4. Flunisolide (Aerobid)
5. Fluticasone (Flovent)
6. Fluticasone/salmeterol (Advair Diskus)
7. Mometasone furoate (Asmanex, Twisthaler)
Nasal Sprays for allergic rhinitis
1. Mometasone (Nasonex)
2. Fluticasone (Flovent)
68
Q

What are the dermatological corticosteroid preparations?

A

Creams and ointments containing corticosteroids applied directly on affected area.

69
Q

What is Aldosterone?

A

main mineralocorticoid, secreted by zona glomerulosa of adrenal cortex

70
Q

What does Aldosterone do?

A

retains Na+ in the distal part of the distal convuluted tubule and cortical collecting duct

71
Q

What is Fludrocortisone?

A

the main (potent) synthetic steroid with significant mineralocorticoid activity used clinically

given in case of adrenal insufficiency (addison’s disease)
doses not sufficient to cause antiinflamm/ antigrowth effects

72
Q

What can the mineralocorticoid activity of cortisone/hydrocortisone cause?

A

Electrolyte imbalances (Hypernatremia, fluid retention, hypokalemia, hyperchloremic alkalosis) causing HTN

73
Q

What do you do if a pt with Hypoproteinemia, liver disease or renal disease is being treated with corticosteroids?

A

EDEMA may occur in these patients, hence they must be placed on high protein and K+ enriched diet.

74
Q

What toxicities occur in heart patients taking corticosteroids?

A

may cause HF in these patients. Effects can be reduced by switching to non-salt retaining steroids, sodium restriction and potassium supplements.

75
Q

What toxicites occur in children taking corticosteroids?

A

may stunt growth

76
Q

What else may corticosteroid use cause?

A

PU, Hypomania, acute psychosis, depression, cataracts, glaucoma

77
Q

What are chronic corticosteroid use toxicities?

A

chronic treatment: leads to iatrogenic (symptoms due to illness) Cushings Syndrome.
-changes in appearance due to fat redistribution (steatosis)
(facial puffiness, trunk obesity, fat in neck, back an supraclavicular fosse)
-Osteoporosis
-DM
-Muscle wasting,
-thinning of skin
-increased facial hair growth
-punctate (studded/ tiny holes) acne
-aseptic necrosis of the hip

78
Q

What is chronic (>2 wks) corticosteroid administration likely to cause?

A
  • Adrenal Suppression (Glucocorticoid-induced adrenal insufficiency)
  • must gradually taper off
  • if suddenly withdrawn, Glucocorticoid-induced adrenal insufficiency will cause major withdrawal effects
79
Q

How should corticosteroids be administered?

A

After the initial dose required to suppress symptoms, the dose could be reduced to what is sufficient to keep symptoms down. Alternate day drug therapy is judicious.

For large dose therapy, medium/intermediate- acting steroids with no mineralocorticoid activity are preferred

** caution in pts with PU, heart disease, HTN w/ HF, inf with Varicella, TB, DM, Osteoporosis or glaucoma

80
Q

which patients should you be cautious administering corticosteroids to?

A

pts with PU, heart disease, HTN w/ HF, inf with Varicella, TB, DM, Osteoporosis or glaucoma

(because they would excerbate these conditions. most of these are AE’s of corticosteroid use..)

81
Q

What dosage forms are available to minimize corticosteroid toxicity?

A
  1. Topical preparations for skin disease, opthalmic forms for eye disease
  2. Intra-articular injections for joint disease
  3. Inhaled steroids for asthma
  4. Hydrocortisone enemas for Ulcerative Collitis etc are ways of administering the drugs to the affected region minimizing systemic effects.
82
Q

What are the corticosteroids used for Asthma?

A 
Aerosols
1. Beclomethasone (QVAR)
2. Triamcinolone (Azmacort)
3. Budesonide (Pulmicort)
4. Flunisolide (Aerobid)
5. Fluticasone (Flovent)
6. Fluticasone/salmeterol (Advair Diskus)
7. Mometasone furoate (Asmanex, Twisthaler)
Nasal Sprays for allergic rhinitis
1. Mometasone (Nasonex)
2. Fluticasone (Flovent)
83
Q

What are the dermatological corticosteroid preparations?

A

Creams and ointments containing corticosteroids applied directly on affected area.

84
Q

What is Aldosterone?

A

main mineralocorticoid, secreted by zona glomerulosa of adrenal cortex

85
Q

What does Aldosterone do?

A

retains Na+ in the distal part of the distal convuluted tubule and cortical collecting duct

86
Q

What is Fludrocortisone?

A

the main (potent) synthetic steroid with significant mineralocorticoid activity used clinically.

given in case of adrenal insufficiency associated with mineralocorticoid deficiency

doses not sufficient to cause antiinflammatory/antigrowth effects

87
Q

What do adrenal tumors/mineralocorticoid overdoses cause?

A
  • Hypokalemia
  • Hypernatremia (aldosterone (a mineralocorticoid) retains Na+.
  • fluid retention (“)
  • HTN (maybe due to high Na+ and fluid?)
  • metabolic alkalosis (loss of K in blood– keeps acidic. remember when a lot of K leaves cells and enters blood we got acidosis? Also, retention of Na means that K leaves (NA+/K+ ATPase pump) just to tie it all in…)
88
Q

How does Aldosterone affect Na/K

A

aldosterone stimulates gene expression of Na/K ATPase pumps and epithelial Na channels to cause increased Na uptake and concurrent loss of K.

89
Q

What is Deoxycorticocosterone (DOC)

A

Deoxycorticocosterone is the precursor of aldosterone, has mineralocorticoid activity.
Unlike aldosterone, its secretion is mainly controlled by ACTH. Secretion may be increased due to adrenal tumors/congenital adrenal hyperplasia due to biosynthetic enzyme deficiency

90
Q

What is an Adrenal Androgen?

A

Dehydroepiandrosterone (DHEA). large amounts of DHEA and small amounts of androstenodione and testosterone are secreted by the adrenal cortex.

-No clear clinical benefit

91
Q

What are the Antagonists of adrenocortical Agents?

A

Biosynthetic Inhibitors

1.

92
Q

What do adrenal tumors/mineralocorticoid overdoses cause?

A
  • Hypokalemia
  • Hypernatremia (aldosterone (a mineralocorticoid) retains Na+.
  • fluid retention (“)
  • HTN (maybe due to high Na+ and fluid?)
  • metabolic alkalosis (loss of K in blood– keeps acidic. remember when a lot of K leaves cells and enters blood we got acidosis? Also, retention of Na means that K leaves (NA+/K+ ATPase pump) just to tie it all in…)
93
Q

How does Aldosterone affect Na/K

A

aldosterone stimulates gene expression of Na/K ATPase pumps and epithelial Na channels to cause increased Na uptake and concurrent loss of K.

94
Q

What is Deoxycorticocosterone (DOC)

A

Deoxycorticocosterone is the precursor of aldosterone, has mineralocorticoid activity.
Unlike aldosterone, its secretion is mainly controlled by ACTH. Secretion may be increased due to adrenal tumors/congenital adrenal hyperplasia due to biosynthetic enzyme deficiency

95
Q

What is an Adrenal Androgen?

A

Dehydroepiandrosterone (DHEA). large amounts of DHEA and small amounts of androstenodione and testosterone are secreted by the adrenal cortex.

-No clear clinical benefit

96
Q

What are the Antagonists of adrenocortical Agents?

A

Biosynthetic Inhibitors

  1. Metyrapone *
  2. Aminoglutethimide (Cytadren)
  3. Ketoconazole (Nizoral)
  4. Mifepristone (RU486) (Mifeprex)
  5. Mitotane (Lysodren) *
  6. Trilostane

Mineralocorticoid Antogonists

  1. Spironolactone
  2. Eplerenone (Inspra)
  3. Drospirenone

*withdrawn in US

97
Q

What is Metyrapone?

A

A Biosynthetic inh.
specific inh. of 11 hydroxylation and inh. synthesis of cortisol and corticosterone biosynthesis. There is consequent increase in ACTH release (because it seems as though there isn’t enough cortisol) and 11- deoxycortisol secretion.
Useful diagnostic test for assessing capacity of anterior pituitary for releasing ACTH. Drug withdrawn from US market.

98
Q

What is Aminoglutethimide (Cytraden)?

A

A Biosynthetic inh.
blocks conversion of cholesterol –> pregnenolone (cannot make cortisol)
used for treatment of Cushings Syndrome

Also an Aromatase inhibitor. Its use to prevent estrogen production in women with breast cancer has been supplanted by TAMOXIFEN

99
Q

What is Ketoconazole?

A

A Biosynthetic inh.
Antifungal imidazole derivative that also inh. biosynthesis of steroidal hormones. Inh. side chain cleavage of cholesterol (….a bunch of shit idwanna type)

This effect is not seen at low doses req for antifungal activity

Used in pts with Cushings Syndrome
Causes HEPATOTOXICITY

100
Q

What is Mifepristone?

A

A Biosynthetic inh.
Progesterone receptor antagonist, has strong antiprogestin activity.
Also inh. glucocorticoid receptor, acts as a competitive antagonist and blocks receptor activation. highly protein bound
Used to treat Cushings Syndrome in inoperable pts with ECTOPIC TUMORS who have failed other means of treatment

Main use as an ABORTIFACIENT in combination with misoprostol

101
Q

What is Mitotane?

A

A Biosynthetic inh.

Used to treat adrenal tumors. Drug withdrawn from US market due to toxicity.

102
Q

What is Trilostane?

A

A Biosynthetic inh.
3B-17 hydroxy steroid dehydrogenase inh. Hence block adrenal and gonadal hormones like aminoglutethemide.
Used for treatment of Cushings Syndrome, including DOGS

GI AE’s in about 50% of pts.

103
Q

What corticosteroids are used to treat Cushings Syndrome?

A

TRilostane (also in dogs)
Mifepristone (due to ectopic tumors)
Aminoglutethemide
Ketoconazole (~meh)

104
Q

What is Sprinolactone?

A

A Mineralocorticoid antagonist

  • competitive aldosterone receptor antagonist. Used to treat PRIMARY ALDOSTERONISM
  • also used as a K+ sparing diuretic
  • also a competitive antagonist at the androgen receptor, and could be used to treat hirsutism in women.
105
Q

What are the AE’s of spironolactone?

A 
Hyperkalemia
Cardiac Arrhythmia (due to hyperkalemia)
Menstrual abnormalities
gynecomastia
sedation
H/A
GI disturbances
skin rashes
106
Q

What do adrenal tumors/mineralocorticoid overdoses cause?

A
  • Hypokalemia
  • Hypernatremia (aldosterone (a mineralocorticoid) retains Na+.
  • fluid retention (“)
  • HTN (maybe due to high Na+ and fluid?)
  • metabolic alkalosis (loss of K in blood– keeps acidic. remember when a lot of K leaves cells and enters blood we got acidosis? Also, retention of Na means that K leaves (NA+/K+ ATPase pump) just to tie it all in…)
107
Q

How does Aldosterone affect Na/K

A

aldosterone stimulates gene expression of Na/K ATPase pumps and epithelial Na channels to cause increased Na uptake and concurrent loss of K.

108
Q

What is Deoxycorticocosterone (DOC)

A

Deoxycorticocosterone is the precursor of aldosterone, has mineralocorticoid activity.
Unlike aldosterone, its secretion is mainly controlled by ACTH. Secretion may be increased due to adrenal tumors/congenital adrenal hyperplasia due to biosynthetic enzyme deficiency

109
Q

What is an Adrenal Androgen?

A

Dehydroepiandrosterone (DHEA). large amounts of DHEA and small amounts of androstenodione and testosterone are secreted by the adrenal cortex.

-No clear clinical benefit

110
Q

What are the Antagonists of adrenocortical Agents?

A

Biosynthetic Inhibitors

  1. Metyrapone *
  2. Aminoglutethimide (Cytadren)
  3. Ketoconazole (Nizoral)
  4. Mifepristone (RU486) (Mifeprex)
  5. Mitotane (Lysodren) *
  6. Trilostane

Mineralocorticoid Antogonists

  1. Spironolactone
  2. Eplerenone (Inspra)
  3. Drospirenone

*withdrawn in US

111
Q

What is Metyrapone?

A

A Biosynthetic inh.
specific inh. of 11 hydroxylation and inh. synthesis of cortisol and corticosterone biosynthesis. There is consequent increase in ACTH release (because it seems as though there isn’t enough cortisol) and 11- deoxycortisol secretion.
Useful diagnostic test for assessing capacity of anterior pituitary for releasing ACTH. Drug withdrawn from US market.

112
Q

What is Aminoglutethimide (Cytraden)?

A

A Biosynthetic inh.
blocks conversion of cholesterol –> pregnenolone (cannot make cortisol)
used for treatment of Cushings Syndrome

Also an Aromatase inhibitor. Its use to prevent estrogen production in women with breast cancer has been supplanted by TAMOXIFEN

113
Q

What is Ketoconazole?

A

A Biosynthetic inh.
Antifungal imidazole derivative that also inh. biosynthesis of steroidal hormones. Inh. side chain cleavage of cholesterol (….a bunch of shit idwanna type)

This effect is not seen at low doses req for antifungal activity

Used in pts with Cushings Syndrome
Causes HEPATOTOXICITY

114
Q

What is Mifepristone?

A

A Biosynthetic inh.
Progesterone receptor antagonist, has strong antiprogestin activity.
Also inh. glucocorticoid receptor, acts as a competitive antagonist and blocks receptor activation. highly protein bound
Used to treat Cushings Syndrome in inoperable pts with ECTOPIC TUMORS who have failed other means of treatment

Main use as an ABORTIFACIENT in combination with misoprostol

115
Q

What is Mitotane?

A

A Biosynthetic inh.

Used to treat adrenal tumors. Drug withdrawn from US market due to toxicity.

116
Q

What is Trilostane?

A

A Biosynthetic inh.
3B-17 hydroxy steroid dehydrogenase inh. Hence block adrenal and gonadal hormones like aminoglutethemide.
Used for treatment of Cushings Syndrome, including DOGS

GI AE’s in about 50% of pts.

117
Q

What corticosteroids are used to treat Cushings Syndrome?

A

TRilostane (also in dogs)
Mifepristone (due to ectopic tumors)
Aminoglutethemide
Ketoconazole (~meh)

118
Q

What is Sprinolactone?

A

A Mineralocorticoid antagonist

  • competitive aldosterone receptor antagonist. Used to treat PRIMARY ALDOSTERONISM
  • also used as a K+ sparing diuretic
  • also a competitive antagonist at the androgen receptor, and could be used to treat hirsutism in women.
119
Q

What are the AE’s of spironolactone?

A 
Hyperkalemia
Cardiac Arrhythmia (due to hyperkalemia)
Menstrual abnormalities
gynecomastia
sedation
H/A
GI disturbances
skin rashes
120
Q

What is Eplerenone?

A

A Mineralocorticoid antagonist
Aldosterone receptor antagonist used for treatment of HTN
more selective than spironolactone, no effect on androgen receptor
May cause Hyperkalemia

121
Q

What is Drospirenone?

A

A Mineralocorticoid antagonist
Aldoserone receptor antagonist; a progestin used in oral contraceptives in combo with estrogens (Yasmin -drospirenone +ethinyl estradiol) that also antagonizes aldosterone

Pharmacology Exam #2 (4 decks)

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