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MDCM626 > Adrenocoricoids > Flashcards

Adrenocoricoids Flashcards

1
Q

Most important propery of glucocorticoids?

A
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2
Q

2 parts of the cortex and their functions

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3
Q

Synthesis of aldosterone, cortisol and 11-Deoxycorticosterone.

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4
Q

4 Important roids and their function 2 mineral 2 gluco

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5
Q

2 mineralcorticoids name them

A

11-deoxycorticosterone, aldosterone

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6
Q

Mineral and Antimineralocorticoids

Endogenous agonists? 2

Synthetic Antagonists?

Flowchart

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7
Q

Mineral and Antimineralocorticoids

Synthetic Antagonists 2 types

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8
Q

Spironolactone

What is it?

What is essential for activity?

An intact what is also important?

What at the 7 position improves antagonist activity and oral bioavailability?

Eplerenone has the same activity but what is it lacking?

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9
Q

All synthetic glucocorticoids are preduced from?

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10
Q

What is the active and inactive form of glucocorticoids?

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11
Q

4 routes of glucocorticoid metabolism

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12
Q

What do glucocorticoid esters do?

All of these are inactive? What do they need?

A

Block glucuronidation at the 21 position and prolong the duration of activity

Need to be activated they are inactive prodrugs

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13
Q

What 3 zones is the adrenal cortex broen up into?

What do each of these secrete or produce?

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14
Q

Biosynthetic pathway of 3 products

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15
Q

Adrenal Cortex Steroids Key Fx

Mineralcorticoids what do they do?

Glucocorticoids Favors? Important in function of? Reduce what response?

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16
Q

Aldosterone

Where is it produced?

What is the active form and what does it look like?

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17
Q

Aldosterone has high ____ activity?

Why are semi-synthetics made?

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18
Q

What is absent in 11-deoxycorticosterone? 2 things

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19
Q

Since 11-deoxy lacks an OH at C11 and an Aldehyde at C18 what changes with its acitivity?

But it still has significant activity?

What activtiy does it lack?

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20
Q

Spironolactone

What type of inhibitor is it? At what receptors?

What is it called and why?

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21
Q

Eplerenone (Inspra)

Similar to Spironolactone

what receptor does it act on?

Initially used to treat what? Then used for?

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22
Q

Glucocorticoids

In the synthetic pathway?

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23
Q

Glucocorticoid flow chart

Chart starts with endogenous agonists

A
24
Q

Hydrocortisone (Cortisol) and Cortisone

Where is it produced?

What about it in tissues?

A
25
Q

Cortisol and Cortisone

What is the active form?

Both of these compounds contain too much of what type of activity?

A
26
Q

Metabolism of Glucocorticoids

Undergo extensive metabolism in four main routes

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27
Q

What are the products of 3-keto-4-ene reduction for Hydrocortisone and Cortisone?

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28
Q

Glucocorticoids

What does 3-keto-4-ene reduction do for activity?

What happens to the product of this metabolism once done? What rxn and what does this mean for PK?

A
29
Q

Glucocorticoids

What activity does the 11b-OH give the molecule?

A
30
Q

Metabolism of Glucocorticoids

11b-hydroxyl

What type of process is it and what enzyme is responsible for it?

What type of metabolite is it?

A
31
Q

Metabolism of Glucocorticoids

21 hydroxyl

This is a common site for what 2 rxns?

A
32
Q

Metabolism of Glucocorticoids

21-hydroxyl

MEtabolism at this point leads to increased?

A
33
Q

Metabolism of Glucocorticoids

6b-hydroxylation

Metabolism via what enzyme?

What happends to activity?

A
34
Q

Synthetic Analogs

5 examples of Esters of GLucs

Where is the modification at for these esters?

A
35
Q

3 specific gluco esters

What route are each of these and their names

What do these esters block?

So then these have a?

What are these types of drugs called?

A
36
Q

Synthetic Analogs

Structurally modified gluc nucleus

7ish examples

A
37
Q

This drug has a modification at the 1 to form a double bond between 1 and 2 in the A ring

A
38
Q

Prednisolone and Prednisone both have a d1 Alkene

What does this do for activity?

____ ____ at the C21 position is easily esterified to form what?

A
39
Q

This compound has a methyl group at the C6 position what is it?

What purpose does this serve?

What does it do for activity?

A
40
Q

As well as a 6a methyl group methylprednisolone also has what? It is similar to prednisolone

What is its anti-inflammatory activity compared to hydrocortisone?

A
41
Q

This drug contains a 6a-Fluoro group

What does it do for activity?

What does it decrease?

A
42
Q

6a-fluroprednisolone

Activity compared to hydrocortisone?

The A ring still has?

A
43
Q

This drug has a 9a-Fluorogroup

This one is lacking what in one of the rings? What does this do for activity?

How is binding improved?

A
44
Q

What does a 9a-Fluoro prevent?

What does this compound lack?

This drug is only useful for the treatment of?

A
45
Q

This drug has a 16a-Hydroxy

What does this do for activity?

This drug also has a combinations of two other structural features what does this mean for activity?

A
46
Q

Triamcinolone Has a modification at the 16 position

how can it be modified further to produce a more lipophilic variant?

Why would this be useful?

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47
Q

Triamcinolone activity compared to hydrocortisone?

A
48
Q

These compounds have a 16a or 16b modification

What is the addition?

What does this prevent and suppress?

What activity is reduced?

A
49
Q

What combination in 16a/b Methylprednisolone give potent anti-inflam activity?

A
50
Q

21-chloro

What does it do?

There is also something on the C17 position that increases potency and gives a more lipophilic compound making it good for?

A
51
Q

Momestasone has a combination of 5 things that give it strong anti-inflammatory action

What is the onset of action compared to Triamcinolone?

A
52
Q

What modifications does beclomethasone have?

What gives it its potent gluco action?

A
53
Q

This one is widely used in inhalers?

A

MDCM626 (26 decks)

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