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

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

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

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

<p>Acne (D)</p> Signup and view all the answers

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

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

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

<p>Improvement (D)</p> Signup and view all the answers

Which phase of the menstrual cycle primarily produces progesterone?

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

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

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

Which modification enhances progestin potency?

<p>Removal of C19 angular methyl group (A)</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 (D)</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 (C)</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 (B)</p> Signup and view all the answers

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

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

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

<p>Enhances progestin activity (C)</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 (D)</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 (A)</p> Signup and view all the answers

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

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

What is the primary use of drospirenone?

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

What is the dosage of drospirenone in combined oral contraceptives?

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

Which of the following is a characteristic of drospirenone?

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

Which of the following is a property of drospirenone?

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

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

<p>Drospirenone (D)</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 (C)</p> Signup and view all the answers

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

<p>It inhibits aldosterone binding (A)</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. (B)</p> Signup and view all the answers

What is the biological precursor of dihydrotestosterone?

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

Which enzyme is responsible for converting testosterone into dihydrotestosterone?

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

What is the primary drug target in benign prostatic hyperplasia?

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

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

<p>Finasteride (A)</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. (D)</p> Signup and view all the answers

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

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

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

<p>Benign prostatic hyperplasia (C)</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 (B)</p> Signup and view all the answers

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

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

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