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🄼💊MSY2 Pharm (Endocrine/Repro/Thyroid) > Adrenocorticosteroids and Blockers > Flashcards

Adrenocorticosteroids and Blockers Flashcards

1
Q

Physiological Effects of Glucocorticoids on immune system (5)

A
  1. DEC Leukocyte Mobilization (helps allergies)
  2. DEC Cytokines (helps allergies)
  3. DEC Prostaglandins (as COX2 inhibitor)
  4. INC iKB –> inhibits NFKB(repsonsible for inflammation)
  5. Prevents NFKB from entering nucleus
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2
Q

Physiological Effects of Glucocorticoids on CV system (3)

A
  1. INC Vasoactive factor response (Arterial tone)

when low –> hypOtension

when HIGH –> HTN

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3
Q

Physiological Effects of Glucocorticoids on Musculoskeletal system (3)

A
  • required for Muscle Function but also..
  • DEC Muscle Density
  • DEC Bone Density
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4
Q

Physiological Effects of Glucocorticoids on CNS system (2)

A
  • Emotion Modulator (Mood/Mania/Memory)
  • Wakefulness
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5
Q

Physiological Effects of Glucocorticoids on Liver Detox

A

INC enzyme expression and helps detoxify heavy metals/toxins

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6
Q

Physiological Effects of Glucocorticoids on Metabolism (4)

A
  1. Protein Catabolism–> Muscle Degradation
  2. Fat ReDistribution to Visceral
  3. Hepatic Gluconeogenesis
  4. DEC Peripheral glucose utilization
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7
Q

Physiological Effects of Glucocorticoids on GI Tract (3)

A
  1. INC Gastric Acid
  2. INC Digestive Enzymes
  3. DEC Ca+ uptake
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8
Q

How does ACTH affect Cholesterol?

A

INC Cholesterol uptake via GPCR

ACTH is Trophic Factor

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9
Q

Daily Secretion of Cortisol

A

10-20 mg / day

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10
Q

Daily Secretion of Aldosterone

A

0.125 mg / day

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11
Q

Cortisol Half life

A

60-90 min

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12
Q

Aldosterone Half life

A

15-20 min

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13
Q

List the Peak and Trough for Cortisol production

A

Peak = 8 AM (Circadian released)

Trough = 11 pm

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14
Q

Cortisol MOA

A
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15
Q

Compare how [Glucocorticoid Receptors] vs. [Mineralocorticoid Receptors] are affected by Cortisol?

A

Both with Equal Affinity

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16
Q

What enzyme deactivates Cortisol into Cortisone

A

11B HSD2

“time 2 go back to PCKS, Mr.Cortisol”

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17
Q

List the organs that are Aldosterone sensitive (3)

A

Colon

Kidney

Salivary Gland

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18
Q

Which tissues express [11B HSD1] (3)

A

LAB

Liver

Adipose

Brain

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19
Q

List the [short acting] synthetic corticosteroids (2)

A
  1. Hydrocortisone/cortisol
  2. Cortisone
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20
Q

List the [intermediate acting] synthetic corticosteroids (4)

A
  1. Fludrocortisone (High Mineralocorticoid potency)
  2. PrednisoLone (L for L**ive)
  3. Prednisone (inactive)
  4. Triamcinolone
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21
Q

List the [Long acting] synthetic corticosteroids (2)

A

Long Sex for Betty and Dex

  1. Dexamethasone
  2. Betamethasone
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22
Q

Which Corticosteroid has HIGH mineralocorticoid potency

A

Fludrocortisone-IA

IA= Intermediate Acting

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23
Q

Which Corticosteroid has No mineralocorticoid activity AND is not a [substrate of 11B HSD2]

A

Dexamethasone-LA

LA= Long Acting

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24
Q

Which Corticosteroids has the [HIGHEST Glucocorticoid potency] but [no mineralocorticoid acitivty] (2)

A
  1. Dexamethasone LA
  2. Betamethasone LA
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25
Oral Corticosteroid metabolism
Can be active or inactive since inactive agents are converted --\> active by [Liver 11BHSD1]
26
Topical Corticosteroid metabolism
[11BHSD1] is not in skin or joints so Topical Corticosteroids MUST be active already (i.e. hydrocortisone vs. PrednisoLone)
27
Which corticosteroid is given to mother for an effect on the fetus? Why?
Dexamethasone [11BHSD**2**] in Placenta inactivates any corticosteroids that are substrates. Dexamethasone is NOT a substrate of [11BHSD**2**]
28
Which Corticosteroids are used for HRT (2)
Hydrocortisone Fludrocortisone *physiological doses*
29
Indications for [Corticosteroid HRT] (2)
[Adrenal insufficiency] CAH (Congenital Adrenal Hyperplasia)
30
**NonEndocrine** Corticosteroid indications (5)
**CCAAR** 1. Autoimmune 2. Anti-inflammatory/rejection 3. Respiratory (Asthma vs. ARDS) 4. CA (A.L.L.) 5. Cerebral Edema
31
Corticosteroids used for **NonEndocrine** indications (2)
Prednisone Dexamethasone *HIGHER physiological doses*
32
How much time does it take for adrenal function to recover [post exogenous corticosteroid]
12 mo.
33
Sx of Cortisol insufficiency (5)
1. DEC blood glucose--\>impaired brain/heart/kidney 2. DEC response to vasoactive agents--\> hypOtension 3. DEC muscle function 4. Hypercalcemia 5. Hyperpigmentation from INC ACTH on MSU receptors
34
**Cortisol** insufficiency is from primary or secondary adrenal insufficiency?
Secondary ## Footnote *Aldosterone insufficiency is from primary adrenal insufficiency*
35
Drug used to treat [**nonacute** Adrenal Insufficiency] (3)
Hydrocortisone Dexamethasone Fludrocortisone for Primary Adrenal insufficiency
36
When would you see Acute Adrenal Insufficiency? (3)
1. [Undiagnosed Adrenal Insufficiency] pt after serious illness 2. pt with pre-existing adrenal insufficiency but who does NOT INC glucocorticoid usage during illness 3. Abrupt withdrawal of Chronic Glucocorticoid therapy
37
Sx of [Acute Adrenal Insufficiency] (5)
hypOvolemic shock hypOnatremia Hyperkalemia NV Weakness
38
What's the initial tx for [Acute Adrenal Insufficiency] (2)
[IV electrolytes] + [IV Hydrocortisone vs. Dex]
39
What's the ultimate tx for [Acute Adrenal Insufficiency] once it's stable
[IV Hydrocortisone] tapered over 1-2 days to an [oral hydrocortisone + fludrocortisone]
40
Pts with adrenal insufficiency should avoid what situations --\> INC cortisol? (4)
1. Stress 2. Illness 3. Surgery 4. Pregnancy
41
What affect does [CYP21 mutations] have on sex organ development (Male vs. Female)
Males = normal Females = Hypervirilized + [ambiguous genitalia] from excess Testosterone
42
Newborns with [CYP21 mutations] will suffer from [Acute Adrenal Crisis] within ____ weeks
1-3 Weeks [*Salt Wasters, Wt. Loss, hypOtension, dehydration, vomiting*]
43
Tx of CAH after birth (2)
Hydrocortisone + [Fludrocortisone PRN]
44
Which [amniotic fluid substrate] is used as a prenatal screen for CAH
17-Hydroxypregnenolone (precursor of cortisol)
45
CAH (Congenital Adrenal Hyperplasia) is mostly caused by \_\_\_ mutation
CYP21
46
Tx of [CAH-CYP21 mutation] when discovered in utero (Female vs. Male)
Female baby= Give mother **Dexamethasone** 9th week gestation up until delivery Male baby= tx can be delayed until after birth
47
Which Corticosteroid treats RA
Prednisone
48
How long should Prednisone be used to treat RA
\< 3-4 weeks (used for flare ups only)
49
Rhematoid **joint pain** tx regimen and which drug to use
Administered Directly into joint q3 mo. Because of joint, must use [active: PrednisoLone]
50
Which Corticosteroid is used for Severe allergies
***P** for **P**retty Bad Allergies* IV vs. [short term oral] Prednisone/PrednisoLone
51
Which Corticosteroids are used for mild allergies (4)
**A**llergies **F**ar **T**han **B**ad Inhaled Glucocorticoids 1. **T**riamcinolone 2. **A**cetonide 3. **B**eclumetasone 4. **F**luticasone
52
Describe the Route of Delivery for Inhaled Glucocorticoids
High Drug concentration directly to Lung --\>Avoids Significant 1st pass effect. \<1% of swallowed glucocorticoid is bioavailale. Low risk SE or HPA suppression
53
How are Corticosteroids used to treat [NephrOtic syndrome]
DEC inflammation associated with [Minimal change Dz]
54
How are Corticosteroids used to treat CA
DEC WBC # in the blood for ALL
55
**Which drug** and **How** are Corticosteroids used to treat [NRDS]
**Dexamethasone** promotes Lung maturation when birth is \< 31 week gestation
56
When is it indicated to use Corticosteroids for Cerebral Edema? (4)
**1**st, **H**elp **B**rian's **B**rain...with Steroids! 1. [1° AND metastatic brain tumors] 2. Bacterial meningitis (prevents hearing loss) 3. Brain Radiation exposure 4. High Altitutde Cerebral Edema
57
**Contraindications** for using Corticosteroids for Cerebral Edema (3)
Traumatic Brain injury Stroke Intracerebral Hemorrhage
58
MOA for Corticosteroids in Cerebral Edema (3)
* [INC CSF reabsorption] and [DEC CSF production] * DEC endothelial permeability and stabilizes BBB * DEC inflammation and cytokines
59
Under what circumstances does HPA suppression occur following Corticosteroid tx
Chronic use of Corticosteroid (\>20 mg prednisone for \> 3 weeks)
60
How should you withdrawal Corticosteroids to avoid adrenal crisis
Slow taper (10-20% DEC in dose every 1-2 weeks)
61
Name the situations in which low dose Dex does **not** suppress cortisol levels (3)
[Pituitary Adenoma Cushing Dz] [Pareneoplastic Cushing Syndrome (Ectopic)] [Adrenal Cortisol Tumor]
62
Name the situations in which HIGH dose Dex does **not** suppress cortisol levels (2)
[Pareneoplastic Cushing Syndrome (Ectopic)] [Adrenal Cortisol Tumor]
63
Name the [Adrenocorticoid synthesis] inhibitors (3)
1. Ketoconazole = **MOST EFFECTIVE** 2. Etomidate 3. Metyrapone
64
Ketoconazole MOA (3)
1. Inhibits ACTH secretion 2. **High Doses** inhibits [Human CYP11A1 and B1] 3. inhibits [Fungal CYP450]
65
Etomidate is an ____ that inhibits \_\_\_\_\_
Etomidate is an **[IV Anesthetic/Sedative]** that inhibits [**CYP11A1 and B1**]
66
Etomidate Indication
Pts who are NPO
67
Metyrapone MOA. How is Dehydration SE circumvented?
inhibits [CYP11B1 and B2] --\> inhibits Cortisol and Aldosterone Synthesis. DEC aldosterone levels is compensated by INC in 11-DOC
68
Metyrapone SE
INC Androgen precursors --\> Female Hirsuitism ## Footnote *It Blocks CYP11B1 and B2*
69
Which [Adrenocorticoid synthesis inhibitor] can be used in pregnancy
"*Me* Pregnant" Metyrapone
70
Mitotane Indication
Medical Adrenalectomy when Cushing Dz pts can't tolerate surgery
71
Mitotane MOA
Metabolized by CYP11B1 and A1 --\> active compound that destroys mitochondria --\> [Zona **Fasciculata** & **Reticularis Necrosis**]
72
Mitotane Contraindication
Pregnancy (since it causes permanent fetal adrenal damage)
73
Mitotane SE (4)
**NOT** well tolerated; 80% require dose reducations 2° to [NVD, Anorexia, Rash & Ataxia!]
74
[Mifepristone Indication] **in adrenal glands**
Refractory Cushing's Syndrome
75
Mifepristone MOA (2)
[Progesterone R Blocker] and [Glucocorticoid R blocker at high dose]
76
Mifepristone SE (2)
1. Abortion! (DON'T USE IN PREGNANCY) 2. Adrenal insufficiency
77
Name the situations in which HIGH dose Dex **DOES** suppress cortisol levels and what this means
**[Pituitary Adenoma Cushing Dz]** If after giving [low dose Dexamethasone] Cortisol levels don't drop, but only drops with [HIGH dose Dexamethasone] = Dx is **[Pituitary Adenoma Cushing Dz]**
78
In which organs do you find 11BHSD**2** (4)
*"time **2** _go back_ to **PCKS**, Mr.Cortisol"* **P**lacenta **C**olon **K**idney **S**alivary Glands

🄼💊MSY2 Pharm (Endocrine/Repro/Thyroid) (6 decks)

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