Podcast
Questions and Answers
Which class of drugs primarily affects glucose homeostasis and possesses anti-inflammatory activity?
Which class of drugs primarily affects glucose homeostasis and possesses anti-inflammatory activity?
What are the two types of corticosteroids produced in the adrenal cortex?
What are the two types of corticosteroids produced in the adrenal cortex?
What type of ring system is the steroid nucleus?
What type of ring system is the steroid nucleus?
Which group of agents are called pregnanes due to their structure?
Which group of agents are called pregnanes due to their structure?
Signup and view all the answers
In inflammatory diseases, which class of drugs is specifically known for their disease-modifying properties?
In inflammatory diseases, which class of drugs is specifically known for their disease-modifying properties?
Signup and view all the answers
What is the effect of glucocorticoids on phospholipids in the cell membrane?
What is the effect of glucocorticoids on phospholipids in the cell membrane?
Signup and view all the answers
What is the role of lipocortin in the mechanism of action of glucocorticoids?
What is the role of lipocortin in the mechanism of action of glucocorticoids?
Signup and view all the answers
Where do glucocorticoids bind to exert their anti-inflammatory effects?
Where do glucocorticoids bind to exert their anti-inflammatory effects?
Signup and view all the answers
What is the primary effect of glucocorticoids on T- and B-lymphocytes production?
What is the primary effect of glucocorticoids on T- and B-lymphocytes production?
Signup and view all the answers
Which classification of receptors do glucocorticoids bind to for their anti-inflammatory activity?
Which classification of receptors do glucocorticoids bind to for their anti-inflammatory activity?
Signup and view all the answers
What is the primary role of glucocorticoids in the management and treatment of inflammation?
What is the primary role of glucocorticoids in the management and treatment of inflammation?
Signup and view all the answers
Which of the following is a characteristic of inflammation?
Which of the following is a characteristic of inflammation?
Signup and view all the answers
What is a key difference between glucocorticoids and mineralocorticoids?
What is a key difference between glucocorticoids and mineralocorticoids?
Signup and view all the answers
What is an essential consideration when modifying the structure of glucocorticoids for different routes of administration?
What is an essential consideration when modifying the structure of glucocorticoids for different routes of administration?
Signup and view all the answers
How do NSAIDs primarily target inflammation?
How do NSAIDs primarily target inflammation?
Signup and view all the answers
How can glucocorticoids be altered to increase lipophilicity for reducing systemic absorption and side effects?
How can glucocorticoids be altered to increase lipophilicity for reducing systemic absorption and side effects?
Signup and view all the answers
Which modification results in prodrugs that require activation by hydrolysis to free the C-21 hydroxyl for bonding?
Which modification results in prodrugs that require activation by hydrolysis to free the C-21 hydroxyl for bonding?
Signup and view all the answers
To design agents with minimal mineralocorticoid activity and maximal anti-inflammatory activity, what should be done?
To design agents with minimal mineralocorticoid activity and maximal anti-inflammatory activity, what should be done?
Signup and view all the answers
In glucocorticoids, which esterification is hindered by the presence of methyls at C-10 and C-13?
In glucocorticoids, which esterification is hindered by the presence of methyls at C-10 and C-13?
Signup and view all the answers
Which hydroxyl group in steroids is the most easily accessible and easiest to esterify for structural modification?
Which hydroxyl group in steroids is the most easily accessible and easiest to esterify for structural modification?
Signup and view all the answers
What structural modification increases glucocorticoid action and eliminates mineralocorticoid action?
What structural modification increases glucocorticoid action and eliminates mineralocorticoid action?
Signup and view all the answers
Why is prednisone considered a prodrug of prednisolone?
Why is prednisone considered a prodrug of prednisolone?
Signup and view all the answers
Which modification is responsible for improving glucocorticoid action by increasing lipophilicity?
Which modification is responsible for improving glucocorticoid action by increasing lipophilicity?
Signup and view all the answers
Inhaled lipophilic prodrugs are commonly used in which type of therapy?
Inhaled lipophilic prodrugs are commonly used in which type of therapy?
Signup and view all the answers
Which structural feature of Solu-Medrol makes it water-soluble?
Which structural feature of Solu-Medrol makes it water-soluble?
Signup and view all the answers
What structural modification can be made to steroids to prolong their activity by slowing C-17 oxidation?
What structural modification can be made to steroids to prolong their activity by slowing C-17 oxidation?
Signup and view all the answers
Which type of ester is commonly used to increase solubility of steroids, making them water-soluble prodrugs for intramuscular or intravenous administration?
Which type of ester is commonly used to increase solubility of steroids, making them water-soluble prodrugs for intramuscular or intravenous administration?
Signup and view all the answers
In systemic glucocorticoid therapy, which hydroxyl groups play a significant role in drug effectiveness?
In systemic glucocorticoid therapy, which hydroxyl groups play a significant role in drug effectiveness?
Signup and view all the answers
Which structural feature in a derivative of hydrocortisone makes it about 3-4 times more potent in glucocorticoid therapy?
Which structural feature in a derivative of hydrocortisone makes it about 3-4 times more potent in glucocorticoid therapy?
Signup and view all the answers
What modification can be made to steroids to alter their delivery routes, such as topical, IM, or IV administration?
What modification can be made to steroids to alter their delivery routes, such as topical, IM, or IV administration?
Signup and view all the answers
Which type of steroids are generally used topically if treatment is long-term?
Which type of steroids are generally used topically if treatment is long-term?
Signup and view all the answers
What is the ideal quality for glucocorticoids used in intranasal/inhalation delivery regarding systemic absorption?
What is the ideal quality for glucocorticoids used in intranasal/inhalation delivery regarding systemic absorption?
Signup and view all the answers
Which organ primarily metabolizes glucocorticoids used for systemic delivery?
Which organ primarily metabolizes glucocorticoids used for systemic delivery?
Signup and view all the answers
What can high logP values indicate for highly potent steroids?
What can high logP values indicate for highly potent steroids?
Signup and view all the answers
Which type of steroids are safely used for short-term treatment?
Which type of steroids are safely used for short-term treatment?
Signup and view all the answers
What is the common route of elimination for glucocorticoids used systemically?
What is the common route of elimination for glucocorticoids used systemically?
Signup and view all the answers
How does high logP benefit intranasal/inhalation delivery of glucocorticoids?
How does high logP benefit intranasal/inhalation delivery of glucocorticoids?
Signup and view all the answers
Which characteristic makes glucocorticoids advantageous in limiting oral absorption during intranasal/inhalation delivery?
Which characteristic makes glucocorticoids advantageous in limiting oral absorption during intranasal/inhalation delivery?
Signup and view all the answers
What are the common side effects associated with long-term therapy of systemic glucocorticoids?
What are the common side effects associated with long-term therapy of systemic glucocorticoids?
Signup and view all the answers
What should be avoided when using highly potent steroids with high logP values?
What should be avoided when using highly potent steroids with high logP values?
Signup and view all the answers
Which factor heavily influences the clinical effectiveness of adrenocorticoids?
Which factor heavily influences the clinical effectiveness of adrenocorticoids?
Signup and view all the answers
What type of enzymatic reactions are involved in the biotransformation of synthetic adrenocorticoids?
What type of enzymatic reactions are involved in the biotransformation of synthetic adrenocorticoids?
Signup and view all the answers
Which of the following is NOT a key aspect discussed in adrenocorticoid medicinal chemistry?
Which of the following is NOT a key aspect discussed in adrenocorticoid medicinal chemistry?
Signup and view all the answers
What influences the varying potencies, selectivities, and pharmacodynamics properties of synthetic adrenocorticoids?
What influences the varying potencies, selectivities, and pharmacodynamics properties of synthetic adrenocorticoids?
Signup and view all the answers
Which process results in the formation of both active and inactive metabolic products of synthetic adrenocorticoids?
Which process results in the formation of both active and inactive metabolic products of synthetic adrenocorticoids?
Signup and view all the answers
What impacts the tissue distribution of synthetic adrenocorticoids?
What impacts the tissue distribution of synthetic adrenocorticoids?
Signup and view all the answers
What plays a crucial role in making some analogs of adrenocorticoids more desirable clinically?
What plays a crucial role in making some analogs of adrenocorticoids more desirable clinically?
Signup and view all the answers
Where do synthetic adrenocorticoids primarily undergo biotransformation?
Where do synthetic adrenocorticoids primarily undergo biotransformation?
Signup and view all the answers
Which factor primarily determines how much of a drug reaches systemic circulation following administration?
Which factor primarily determines how much of a drug reaches systemic circulation following administration?
Signup and view all the answers
What is a common consequence of overstimulation of non-target tissues by adrenocorticoids?
What is a common consequence of overstimulation of non-target tissues by adrenocorticoids?
Signup and view all the answers
How do chemical modifications impact the pharmacokinetics of synthetic adrenocorticoids?
How do chemical modifications impact the pharmacokinetics of synthetic adrenocorticoids?
Signup and view all the answers
What is the primary reason for designing formulations to enhance solubility, permeability, and lipophilicity in adrenocorticoids?
What is the primary reason for designing formulations to enhance solubility, permeability, and lipophilicity in adrenocorticoids?
Signup and view all the answers
Which of the following is NOT a side effect commonly associated with adrenocorticoids?
Which of the following is NOT a side effect commonly associated with adrenocorticoids?
Signup and view all the answers
Why is it important to be aware of potential side effects when using adrenocorticoids in treatment?
Why is it important to be aware of potential side effects when using adrenocorticoids in treatment?
Signup and view all the answers
What role does understanding structure-activity relationships play in designing adrenocorticoid derivatives?
What role does understanding structure-activity relationships play in designing adrenocorticoid derivatives?
Signup and view all the answers
Which structural component of adrenocorticoids is most responsible for their biological activity?
Which structural component of adrenocorticoids is most responsible for their biological activity?
Signup and view all the answers
Which type of receptors do glucocorticoids primarily exert anti-inflammatory effects on?
Which type of receptors do glucocorticoids primarily exert anti-inflammatory effects on?
Signup and view all the answers
Replacing one methyl group in cortisol leads to the formation of which compound known for its strong mineralocorticoid receptor affinity?
Replacing one methyl group in cortisol leads to the formation of which compound known for its strong mineralocorticoid receptor affinity?
Signup and view all the answers
Which modification can result in drugs possessing unique pharmacologic profiles in adrenocorticoids?
Which modification can result in drugs possessing unique pharmacologic profiles in adrenocorticoids?
Signup and view all the answers
Which receptor type is targeted by mineralocorticoids like fludrocortisone?
Which receptor type is targeted by mineralocorticoids like fludrocortisone?
Signup and view all the answers
What is the role of ring A through D in the structure of adrenocorticoids?
What is the role of ring A through D in the structure of adrenocorticoids?
Signup and view all the answers
What role does reduction play in adrenocorticoid metabolism?
What role does reduction play in adrenocorticoid metabolism?
Signup and view all the answers
Which approach involves predicting interactions of novel molecules with target proteins in drug design?
Which approach involves predicting interactions of novel molecules with target proteins in drug design?
Signup and view all the answers
Why is understanding the metabolic profile of adrenocorticoid compounds important?
Why is understanding the metabolic profile of adrenocorticoid compounds important?
Signup and view all the answers
What is the primary focus of fragment-based drug design in adrenocorticoid drug discovery?
What is the primary focus of fragment-based drug design in adrenocorticoid drug discovery?
Signup and view all the answers
What role do oxidation reactions play in adrenocorticoid metabolism?
What role do oxidation reactions play in adrenocorticoid metabolism?
Signup and view all the answers
Which approach utilizes machine learning algorithms to screen small molecule libraries for potential drug candidates?
Which approach utilizes machine learning algorithms to screen small molecule libraries for potential drug candidates?
Signup and view all the answers