Endogenous Glucocorticoids and Their Effects Quiz
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Questions and Answers

What is the key property of the acetal group in budesonide that leads to prolonged residence in lung tissue?

  • It increases the hydrophilic nature of the compound
  • It has no effect on the compound's properties
  • It increases the hydrophobic nature of the compound (correct)
  • It decreases the hydrophobic nature of the compound

How does the systemic glucocorticoid activity of budesonide compare to fluticasone propionate?

  • It is 4-7 times higher
  • It is the same
  • It is unknown
  • It is 4-7 times lower (correct)

What is the key mechanism of action for ciclesonide's prolonged duration of action in lung tissue?

  • It is directly activated in the lungs (correct)
  • It is resistant to metabolism in the liver
  • It has a high receptor affinity
  • It is more lipophilic than other steroids

What is the primary disadvantage of lipophilicity for inhaled glucocorticoids?

<p>It facilitates their transport away from lung tissues via mucociliary clearance (C)</p> Signup and view all the answers

How does beclometasone dipropionate represent a breakthrough in asthma treatment?

<p>It is currently used as an inhaler (B)</p> Signup and view all the answers

What is the key advantage of non-halogenated glucocorticoids like budesonide compared to halogenated ones?

<p>They have a lower systemic glucocorticoid activity (D)</p> Signup and view all the answers

Which modification to the steroid structure increased glucocorticoid activity by 10-fold?

<p>Introduction of a 9α-fluoro substituent (D)</p> Signup and view all the answers

What effect did the introduction of a double bond at the Δ1 position have on steroid activity?

<p>Increased glucocorticoid activity fourfold without increasing mineralocorticoid activity (C)</p> Signup and view all the answers

How does the change in geometry of ring A caused by the introduction of the C1==C2 function affect glucocorticoid receptor (GR) affinity and pharmacokinetics?

<p>It increases GR affinity and alters metabolism (D)</p> Signup and view all the answers

What is the bioavailability of prednisone and prednisolone when orally administered?

<p>Greater than 80% (B)</p> Signup and view all the answers

Which enzyme is responsible for the interconversion of prednisone and prednisolone in the liver?

<p>11β-hydroxysteroid dehydrogenase (C)</p> Signup and view all the answers

Why are smaller doses of prednisone or prednisolone required compared to hydrocortisone in the treatment of rheumatoid arthritis?

<p>They have higher glucocorticoid activity (C)</p> Signup and view all the answers

What determines the extent of absorption of topical adrenocorticoids?

<p>The type of cream or ointment, the condition of the skin, and the use of occlusive dressings (D)</p> Signup and view all the answers

What percentage of halobetasol propionate was systemically absorbed after topical application in previous studies?

<p>Approximately 6% (A)</p> Signup and view all the answers

Why does the acetonide group in triamcinolone acetonide contribute to its increased activity compared to triamcinolone?

<p>It reduces the polarity of the molecule, leading to better skin absorption (D)</p> Signup and view all the answers

What is the purpose of esterifying one or more alcohol groups in topical glucocorticoids?

<p>To achieve good skin absorption by increasing the lipophilicity of the molecule (D)</p> Signup and view all the answers

What type of esters were found to be less active as topical anti-inflammatories, according to the text?

<p>Phosphate esters (C)</p> Signup and view all the answers

What is the primary factor that determines the activity of topically applied anti-inflammatory agents, according to the information provided?

<p>The lipophilicity of the molecule (B)</p> Signup and view all the answers

What is the main reason for the negligible activity of a certain substance elsewhere in the body?

<p>Rapid metabolism by cytochrome P450 enzymes (D)</p> Signup and view all the answers

Which group of steroids is primarily used for the treatment of Addison disease?

<p>Mineralocorticoids (A)</p> Signup and view all the answers

What is a characteristic shared by mometasone furoate, fluocinolone acetonide, and flunisolide?

<p>High topical anti-inflammatory activity (D)</p> Signup and view all the answers

Why are semisynthetic analogs used instead of naturally occurring aldosterone in treating Addison disease?

<p>Cost-effectiveness (C)</p> Signup and view all the answers

What modification greatly enhances both salt retention and anti-inflammatory activity of hydrocortisone?

<p>Addition of a 9-fluoro group (C)</p> Signup and view all the answers

Which structural difference distinguishes aldosterone from cortisol?

<p>Absence of a 17a-hydroxyl group (B)</p> Signup and view all the answers

What is the core structure of adrenocorticoids?

<p>Pregnane skeleton (B)</p> Signup and view all the answers

What are the undesired side effects of endogenous glucocorticoids?

<p>Oedema and increased susceptibility to infection (C)</p> Signup and view all the answers

Why are glucocorticoids best used as topical anti-inflammatory agents?

<p>They are more effective when applied directly to the affected area. (D)</p> Signup and view all the answers

What was the significance of the discovery that cortisone could relieve the symptoms of rheumatoid arthritis?

<p>It revealed that the effects of cortisone were actually due to its conversion to cortisol. (B)</p> Signup and view all the answers

What is the importance of the functional groups in the structure of cortisol?

<p>All the functional groups are important, and the removal of any reduces or eliminates activity. (D)</p> Signup and view all the answers

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