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

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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?

Combination oral contraceptives Signup and view all the answers

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

Nausea and Headache Signup and view all the answers

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

Acne Signup and view all the answers

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

Antithrombin III Signup and view all the answers

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

High HDL levels Signup and view all the answers

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

Improvement Signup and view all the answers

Which phase of the menstrual cycle primarily produces progesterone?

Luteal phase Signup and view all the answers

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

Hepatic metabolism Signup and view all the answers

Which modification enhances progestin potency?

Removal of C19 angular methyl group Signup and view all the answers

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

Increased blood coagulability Signup and view all the answers

How do progesterone and progestins act as steroid hormone ligands?

They target a multitude of nuclear steroid receptors Signup and view all the answers

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

Rapid deacetylation by first-pass metabolism Signup and view all the answers

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

17a-hydroxyprogesterone derivatives Signup and view all the answers

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

Enhances progestin activity Signup and view all the answers

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

Ethisterone Signup and view all the answers

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

Introduction of D6,7 Signup and view all the answers

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

'Medroxy' progesterone Signup and view all the answers

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

Increased potency Signup and view all the answers

What is the primary use of drospirenone?

Birth control and postmenopausal hormone replacement therapy Signup and view all the answers

What is the dosage of drospirenone in combined oral contraceptives?

3 mg/ 30 µg Signup and view all the answers

Which of the following is a characteristic of drospirenone?

Anti-mineralocorticoid effect Signup and view all the answers

Which of the following is a property of drospirenone?

Anti-androgenic effect Signup and view all the answers

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

Drospirenone Signup and view all the answers

Which of the following is a common use of drospirenone?

Birth control and postmenopausal hormone replacement therapy Signup and view all the answers

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

It inhibits aldosterone binding Signup and view all the answers

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

It helps to fold the androgen receptor correctly. Signup and view all the answers

What is the biological precursor of dihydrotestosterone?

Testosterone Signup and view all the answers

Which enzyme is responsible for converting testosterone into dihydrotestosterone?

5α-Reductase Signup and view all the answers

What is the primary drug target in benign prostatic hyperplasia?

5α-Reductase Signup and view all the answers

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

Finasteride Signup and view all the answers

What is the difference in specificity between finasteride and dutasteride?

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

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

Dutasteride Signup and view all the answers

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

Benign prostatic hyperplasia 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?

Coactivator Signup and view all the answers

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

Prostate Signup and view all the answers