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E2T1 > Adrenal Corticosteroids Drugs DSA > Flashcards

Adrenal Corticosteroids Drugs DSA Flashcards

(49 cards)

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1
Q

adrenal corticoid drugs

A
  • mineralocorticoids

- glucocorticoids

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2
Q

Mineralocorticoids- drug

A

-Fludrocortisone

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3
Q

Glucocorticoids- short to medium acting (<12 h)

A
  • hydrocortisone
  • cortisone
  • prednisone
  • prednisolone
  • methylprednisolone
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4
Q

Glucocorticoids- intermediate acting (12-36 hrs)

A

-triamcinolone

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5
Q

Glucocorticoids- long acting (>36 hrs)

A
  • betamethasone

- dexamethasone

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6
Q

Inhibitors of adrenal corticosteroid action

A
  • steroid syn inhibitors
  • glucocorticoid antagonists
  • aldosterone antagonists
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7
Q

steroid syn inhibitors- drugs

A

-aminoglutethimide
-ketoconazole
-metyrapone
-mitotane
(AKMM)

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8
Q

glucocorticoid antagonists- drugs

A

-mifepristone

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9
Q

aldosterone antagonists- drugs

A
  • spironolactone

- eplerenone

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10
Q

mineralocorticoids- induced by? regulate?

A
  • Ang II and K

- reg electrolyte, H2O balance and BP

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11
Q

Glucocorticoids- induced by? regulate?

A
  • ACTH

- reg metabolism and immunity

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12
Q

weak androgens- converted into?

A
  • potent androgens in males

- estrogens in females

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13
Q

adrenal corticosteroids- pharmacokinetics- transporters

A
  • hydrophobic- transported by protein carriers
  • transcortin (corticosteroid binding globulin- CBG)- high affinity, low capacity transporter- high during pregnancy and hyperthyroidism; low in liver dz
  • 90% of blood cortisol, 60% of blood aldosterone
  • remainder bound to albumin (low affinity/high capacity)
  • albumin- main carrier for synthetic corticosteroid drugs
  • plasma cortisol > 20-30- transcortin is saturated
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14
Q

adrenal corticosteroids- pharmacokinetics- liver

A
  • liver produces transcortin

- 80% of cortisol is metabolized by liver

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15
Q

adrenal corticosteroids- t1/2 of cortisol

A
  • 60-90 min

- inc in liver dz, hypothyroidism

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16
Q

adrenal corticosteroids- moa

A
  • ligands at nuclear R’s- TF’s (ligand act) that modulate gene expression
  • corticosteroids produce their effects after a lag period
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17
Q

mineralocorticoid effects- target cell types

A

principal cells of CT and CD of kidney and other epit cells involved in electrolyte transport:

  • inc epit Na channel (EnaC)
  • inc Na/K pump
  • retention of water and Na, loss of K
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18
Q

Direct effects of mineralocorticoids on CV system

A

-target non-epit tissues of heart and vasculature
Gene expression effects:
-NADPH reductase- ox stress
-collagen, TGFB- fibrosis, cell senescence
-IL-6, cell adhesion molecules- infl
-PAI-1- inhibition of fibrinolysis, blood clotting
Excess aldosterone causes:
-cardiac fibrosis and hypertrophy
-vascular remodeling and infl

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19
Q

glucocorticoid effects- 2 mechanisms

A
  • transactivation- GR-ligand complex binds to GRE in gene promoters to act gene expression- effects on carb, lipid, protein metabolism
  • transrepression- GR-ligand complex binds to other TF complexes to suppress their act of gene transcription- NF-KB, AP-1 TF’s; anti infl, immunosuppressive, anti-growth effects
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20
Q

glucocorticoid R isoforms

Study These Flashcards
A
  • GRalpha- prototypical isoform

- GRbeta- doesnt bind ligands, inactiv- induced by TNF-alpha

21
Q

role of 11B-hydroxysteroid dehydrogenase (11B-HSD) in adrenal corticosteroid action

Study These Flashcards
A
  • aldosterone and cortisol bind the MR with equal affinity
  • daily prod rates are predominantly corticosteroids
  • 11B-HSD converts cortisol into inactive at MR coritsone- making tissues mineralocorticoid responsive
  • dec 11B-HSD activity- results in excessive act of MR mediated by cortisol!!
22
Q

inhibition of 11B-HSD- causes what?

Study These Flashcards
A
  • inc act of MR by cortisol- causes HTN and edema
  • Glycyrrhizin (in licorice) and carbenoxolone inhibits this enzyme
  • inact mutations- cause AME (mineralocorticoid excess syndrome)- leads to HTN
23
Q

Glucocorticoids- metabolic effects- carbohydrates

Study These Flashcards
A
  • inc gluconeogenesis
  • inc glucose output into circulation (inc G6P)
  • inc glycogen syn (inc glycogen synthase)
  • dec glucose uptake by m and adipose tissues (dec GLUT4)
  • development of hyperglycemia!!
24
Q

Glucocorticoids- metabolic effects- lipids

Study These Flashcards
A
  • inc lipolysis- stim of hormone-sensitive lipase in adipose tissue
  • inc mobilization of free fa and glycerol into the gluconeogenic pathway
  • inc lipogenesis- inc insulin secretion
  • net inc in fat deposition!!!
  • fat accum in upper body!! thinning arms and legs
25
Glucocorticoids- metabolic effects- proteins
- dec aa uptake into cells - dec prot syn - mobilization of aa's into gluconeogenic pathway - skeletal m- suppressed prot syn- myopathy and m wasting
26
Glucocorticoids- effects on intermediary metabolism antagonize actions of insulin
- favor lipid and prot breakdown to supply substrates for gluconeogenesis - interference with insulin R signal transduction
27
Glucocorticoids- effects on immune system and infl
(due to transrepression of NF-kB and AP-1 effects) - dec PLA2 and COX2- dec prod of prostaglandins and leukotrienes - dec prod and inc apoptosis of immune cell types - dec prod of cytokines and their R's - dec expression of cell adhesion molecules - dec transmigration of neutrophils and macrophages from blood into tissues
28
Glucocorticoids- effects on immune system and infl- consequences
- dec infl - immune suppression - dec allergic/hypersensitivity rxns
29
glucocorticoids effects on other systems- CV
- inc prod of Epi and NE - inc R sensitivity to Epi and NE - residual mineralocorticoid activity of glucocorticoids - dec in capillary permeability - inc HR and CO - elevated BP
30
glucocorticoids effects on other systems- GI
- dec prod of gastro-protective prostaglandins - dec immune response against H pylori - inc in gastric acid and pepsin secretion
31
glucocorticoids effects on other systems- CNS
- insomnia - irritability - euphoria, followed by depression - dec sexual libido in males
32
glucocorticoids effects on other systems- bone/growth
- dec activity in osteoblasts - dec intestinal and renal Ca absorption - inc in osteoclast activity - growth retardation in children - osteoporosis, bone fractures
33
glucocorticoids effects on other systems- skin
- dec collagen syn - dec fibroblast prolif - dec wound healing, inc bruising - fragile and skin thin with stretch marks (called striae)
34
common clinical indications of adrenal corticosteroid drugs
- replacement therapy - immunosuppression - infl and allergic conditions
35
common clinical indications of adrenal corticosteroid drugs- replacement therapy
- adrenal insuff (Addison's dz)- glucocorticoid and a mineralocorticoid used! - congenital adrenal hyperplasia
36
common clinical indications of adrenal corticosteroid drugs- immunosupression
- after organ or HSC transplantation - autoimmune dz - hematological cancers
37
common clinical indications of adrenal corticosteroid drugs- infl and allergic conditions
- rheumatoid arthritis - IBD - asthma and COPD - allergic rhinitis - skin dizes- infl dermatoses (psoriasis) - hypersensitivity rxns
38
mineralocorticoids- adverse effects
- retention of Na and H2O- edema - HTN - inc preload and cardiac enlargement- CHF - K loss and alkalosis
39
glucocorticoids- adverse effects
- suppressed ability to fight infections- opportunistic infections! - hyperglycemia - skin- striae, easy bruising - m wasting, steroid myopathy - HTN - steroid-induced glaucoma - cataracts - peptic ulcers - psychiatric disorders- euphoria, mania, anxiety - inc appetite and weight gain - osteoporosis - retarded growth in children
40
adrenal corticosteroid drugs- dosing
- use lowest dose for shortest duration possible!! - reduce distribution of drugs into systemic circulation (use topical, inhalational routes) - give single daily doses in morning - alternate day, short-course, pulse therapy admin - dose tapering
41
pt populations in which systemic glucocorticoids admin is problematic
- immunocompromised pts - diabetics - infections - peptic ulcer - CV conditions- HTN, CHF, angina - psychiatric conditions - osteoporosis - children
42
Aminoglutethimide- moa, indications, SE's
- blocks conversion of chol to pregnenolone - reduces prod of all steroid H's - indications- was used for breast cancer tx, adrenocortical cancer - drowsiness, GI upset
43
inhibitors of adrenal corticoid action- drugs
- aminoglutethimide - ketoconazole - metyrapone - mitotane - mifepristone - spironolactone - eplerenone
44
Ketoconazole- moa, indications, SE's
- P450 inhibition - reduces syn of adrenal and sex H's - antifungal drug, Cushing's syndrome, suppresses androgenic hair loss, prostate cancer - SE's- hepatotoxicity, gynecomastia in males
45
Metyrapone- moa, indications, SE's
- inhibition of steroid 11-hydroxylation - suppresses formation of cortisol and corticosterone - Cushing's syndrome! (can be used in pregnant woman!!) - accum of 11-deoxycortisol- inc aldosterone- Na and H2O retention; inc androgens- hirsutism in women - GI upset - dizziness
46
Mitotane- moa, indications, SE's
- Na ionofore, Ca ionofore - PKC and AC inhibitor - non-selective cytotoxic action of adrenal cortex - used for adrenal carcinoma!! - depression, GI upset, rashes
47
Mifepristone- moa, indications, SE's
- glucocorticoid R antagonists - prevents nuclear translocation of GR - progesterone R antagonist - Hypercortisolism in pts with cushing's syndrome - medical termination of intrauterine pregnancy (anti-progesterone action) - dizziness, GI upset, fatigue
48
Spironolactone- moa, indications, SE's
- aldosterone R antagonist - also antagonist at androgen R's - primary hyperaldosteronism, hirsutism in women, diuretic (tx HF and HTN) - hyperkalemia, gynecomastia and impotence in men, menstrual abnormalities in women
49
Eplerenone- moa, indications, SE's
- antagonist of aldosterone at mineralocorticoid Rs - lower affinity for androgen Rs vs spironolactone - used for HTN, HF (reduces cardiac remodeling) - SEs- hyperkalemia

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