Steroid Lecture 3: Medicinal Chemistry of Estrogens and Progestins for Hormonal Contraception Quiz
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Questions and Answers

What are the components of representative oral contraceptives as mentioned in the text?

  • Progestin and Testosterone
  • Estrogen and Progestin (correct)
  • Estrogen and Testosterone
  • Estrogen and Fibrinogen

    • Which of the following is considered a mild adverse effect of oral contraceptives according to the text?

  • Weight Loss
  • Increased Blood Coagulability (correct)
  • Reduced Amenorrhea
  • Decreased Skin Pigmentation

    • What is a severe adverse effect of oral contraceptives mentioned in the text?

  • Increased Skin Pigmentation
  • Venous Thromboembolism (VTE) (correct)
  • Prolonged Amenorrhea
  • Edema

    • Which type of contraceptives contain estrogen and progestin together?

    <p>Combination oral contraceptives</p> Signup and view all the answers

    What are some common mild adverse effects associated with oral contraceptives?

    <p>Nausea and Headache</p> Signup and view all the answers

    Which adverse effect can be caused by androgenic progestins in oral contraceptives?

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

    Which compound reduction can occur due to estrogen-induced effects from oral contraceptives?

    <p>Antithrombin III</p> Signup and view all the answers

    Which risk factor is NOT associated with higher risk of myocardial infarction in women?

    <p>High HDL levels</p> Signup and view all the answers

    What effect do high estrogen doses and nonandrogenic progestins have on acne?

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

    Which phase of the menstrual cycle primarily produces progesterone?

    <p>Luteal phase</p> Signup and view all the answers

    What is the main reason for the rapid metabolic deactivation of progesterone?

    <p>Hepatic metabolism</p> Signup and view all the answers

    Which modification enhances progestin potency?

    <p>Removal of C19 angular methyl group</p> Signup and view all the answers

    Which of the following is NOT a beneficial effect associated with progesterone and progestin drugs?

    <p>Increased blood coagulability</p> Signup and view all the answers

    How do progesterone and progestins act as steroid hormone ligands?

    <p>They target a multitude of nuclear steroid receptors</p> Signup and view all the answers

    What is the main reason for the improved oral bioavailability of medroxyprogesterone acetate?

    <p>Rapid deacetylation by first-pass metabolism</p> Signup and view all the answers

    Which compound is known for its enhanced potency and metabolic stability?

    <p>17a-hydroxyprogesterone derivatives</p> Signup and view all the answers

    What is the significance of the introduction of D6,7 in megestrol acetate?

    <p>Enhances progestin activity</p> Signup and view all the answers

    Which compound was synthesized as an orally available androgen but turned out to be a potent progestin instead?

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

    What is the main reason for the surprising activity of 17a-Ethinyltestosterone as an oral progestin?

    <p>Introduction of D6,7</p> Signup and view all the answers

    Which compound rapidly deacetylates by first-pass metabolism after oral administration?

    <p>'Medroxy' progesterone</p> Signup and view all the answers

    What effect does the suppression of metabolic hydroxylation/inactivation at C6 have on medroxyprogesterone acetate?

    <p>Increased potency</p> Signup and view all the answers

    What is the primary use of drospirenone?

    <p>Birth control and postmenopausal hormone replacement therapy</p> Signup and view all the answers

    What is the dosage of drospirenone in combined oral contraceptives?

    <p>3 mg/ 30 µg</p> Signup and view all the answers

    Which of the following is a characteristic of drospirenone?

    <p>Anti-mineralocorticoid effect</p> Signup and view all the answers

    Which of the following is a property of drospirenone?

    <p>Anti-androgenic effect</p> Signup and view all the answers

    Which of the following molecules displays a spiro-cyclic structure?

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

    Which of the following is a common use of drospirenone?

    <p>Birth control and postmenopausal hormone replacement therapy</p> Signup and view all the answers

    What is the mechanism of action of drospirenone in the kidney?

    <p>It inhibits aldosterone binding</p> Signup and view all the answers

    What is the role of heat shock protein 70 (HSP70) in androgen activation?

    <p>It helps to fold the androgen receptor correctly.</p> Signup and view all the answers

    What is the biological precursor of dihydrotestosterone?

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

    Which enzyme is responsible for converting testosterone into dihydrotestosterone?

    <p>5α-Reductase</p> Signup and view all the answers

    What is the primary drug target in benign prostatic hyperplasia?

    <p>5α-Reductase</p> Signup and view all the answers

    Which mechanism-based inhibitor of 5α-reductase is specific for type II enzymes?

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

    What is the difference in specificity between finasteride and dutasteride?

    <p>Finasteride is type II specific while dutasteride is non-selective.</p> Signup and view all the answers

    Which drug has a longer elimination half-life, finasteride or dutasteride?

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

    Which condition can be treated with 5α-reductase inhibitors like finasteride and dutasteride?

    <p>Benign prostatic hyperplasia</p> Signup and view all the answers

    Which component of the androgen receptor complex helps to recruit general transcription factors (GTFs) to the androgen-response element?

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

    What is the primary location where dihydrotestosterone exerts its physiological effects?

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

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