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Medicinal Chemistry of Adrenocorticoids: HPA-axis Targeting Steroid Drugs Quiz
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Medicinal Chemistry of Adrenocorticoids: HPA-axis Targeting Steroid Drugs Quiz

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Questions and Answers

What is the main function of hydrocortisone in the body?

  • Immunosuppression (correct)
  • Muscle growth
  • Skin regeneration
  • Bone development
  • Which protein helps the glucocorticoid receptor bind to DNA?

  • CBG
  • Hsp90 (correct)
  • TCR
  • GRE
  • What is the primary mechanism by which glucocorticoids exert their anti-inflammatory effects?

  • Inhibition of cyclooxygenase
  • Inhibition of phospholipase A2 (correct)
  • Inhibition of lipocortin
  • Inhibition of arachidonic acid
  • Which of the following is NOT a common therapeutic indication for glucocorticoids?

    <p>Muscle growth</p> Signup and view all the answers

    Which of the following is a goal of medicinal chemistry in optimizing the properties of glucocorticoids?

    <p>Improving oral bioavailability</p> Signup and view all the answers

    What is the purpose of dissociated ligands in the context of glucocorticoid-GCR interaction?

    <p>Decreasing mineralocorticoid activity</p> Signup and view all the answers

    Which of the following statements is true about cortisol activity?

    <p>Cortisol has a 1x glucocorticoid activity and 1x mineralocorticoid activity.</p> Signup and view all the answers

    Which of the following statements is true about prednisone?

    <p>Prednisone can be used in patients with hepatic insufficiency.</p> Signup and view all the answers

    Which corticosteroid-type ligand has the highest glucocorticoid potency?

    <p>Triamcinolone</p> Signup and view all the answers

    Which of the following statements is true about triamcinolone?

    <p>Triamcinolone does not have enhanced hydrogen bonding.</p> Signup and view all the answers

    Which of the following statements is true about adrenocorticoid interconversion and deactivation?

    <p>Only a few adrenocorticoids are active and interconvertible.</p> Signup and view all the answers

    Which of the following statements is true about 1-Dehydroderivatives?

    <p>1-Dehydroderivatives do not have bioreductive activation.</p> Signup and view all the answers

    Study Notes

    Steroid Drugs Targeting the HPA-axis

    • The Hypothalamic-Pituitary-Adrenal (HPA) axis regulates the body's response to stress, involving the hypothalamus, pituitary gland, and adrenal cortex.
    • The HPA axis produces hormones such as corticotropin-releasing factor (CRF), adrenocorticotropic hormone (ACTH), and hydrocortisone (cortisol).

    Glucocorticoid Neuroendocrinology

    • Glucocorticoids have pleiotropic effects, including anti-inflammatory, immunosuppressive, gluconeogenic, lipolytic, and catabolic actions.
    • Glucocorticoids can also cause hypertension and euphoria.

    Adrenocorticoid Signaling

    • The glucocorticoid receptor (GR) has a DNA-binding domain with zinc fingers, and is bound to heat shock protein 90 (Hsp90).
    • Corticosteroid-binding globulin (CBG) binds to glucocorticoids in the bloodstream.

    Targeting Inflammatory Mediators

    • Glucocorticoids inhibit the action of phospholipase A2, reducing the production of pro-inflammatory eicosanoids.
    • Lipocortin, a glucocorticoid-induced protein, inhibits phospholipase A2.

    Glucocorticoids as Immunosuppressive Drugs

    • Glucocorticoids suppress the immune system by inhibiting T-cell activation and proliferation.
    • Glucocorticoids are often used in combination with other immunosuppressive drugs, such as cyclosporine, azathioprine, and mycophenolate.

    Therapeutic Indications for Glucocorticoids

    • Glucocorticoids are used to treat inflammatory and immune-related disorders, such as asthma, rheumatoid arthritis, and lupus.

    Optimization of Steroid Drugs

    • Medicinal chemistry can optimize the potency, specificity, and bioavailability of steroid drugs, such as hydrocortisone (cortisol).
    • Substituents involved in cortisol activity can be modified to improve its effects.

    Natural and Synthetic Corticosteroids

    • Natural corticosteroids, such as cortisol, can be modified to create synthetic corticosteroids with improved potency and specificity.
    • Examples of synthetic corticosteroids include prednisone and triamcinolone.

    Adrenocorticoid Interconversion and Deactivation

    • Corticosteroids can be interconverted between active and inactive forms, affecting their potency and duration of action.

    Adrenocorticoid SAR

    • The structure-activity relationship (SAR) of adrenocorticoids can be modified to improve their potency, specificity, and metabolic stability.

    1-Dehydroderivatives

    • 1-Dehydroderivatives of corticosteroids, such as prednisone, can exhibit increased anti-inflammatory activity and improved metabolic stability.

    Triamcinolone

    • Triamcinolone is an intermediate-acting glucocorticoid with a fluoro substituent, which increases its potency and duration of action.
    • D-ring substituents in triamcinolone can prolong its duration of action.

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    Description

    Test your knowledge on the medicinal chemistry and pharmacology of adrenocorticoids, focusing on steroid drugs that target the HPA-axis (Hypothalamic-pituitary-adrenal regulation). Explore topics such as cortisol, glucocorticoid effects, and neuroendocrinology. This quiz covers key concepts in adrenocorticoid pharmacology.

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