Endocrine Pharmacology: Female Hormones
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Questions and Answers

When is a progestin added to hormone replacement therapy?

  • To increase ovulation in women experiencing infertility.
  • To prevent polycystic ovary syndrome in women of reproductive age.
  • To prevent endometrial cancer in postmenopausal women with an intact uterus. (correct)
  • To treat breast cancer in women with a history of the disease.

    • What is the primary reason for limiting the duration of tamoxifen treatment to 5 years?

  • To minimize the risk of blood clots and stroke. (correct)
  • To reduce the chances of developing uterine fibroids.
  • To prevent the development of endometrial cancer.
  • To avoid long-term side effects such as hot flashes and mood swings.

    • Which of the following statements accurately describes clomiphene?

  • A selective estrogen receptor modulator (SERM) used to treat breast cancer.
  • An anti-progestin used for medical abortion.
  • An estrogen antagonist used to treat infertility. (correct)
  • A pure estrogen antagonist used to treat infertility.

    • Which of the following drugs is used for emergency contraception within 120 hours of unprotected intercourse?

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

    What is the mechanism of action of mifepristone in medical abortion?

    <p>It acts as an anti-progestin. (A)</p> Signup and view all the answers

    Which of the following is NOT a risk of hormone replacement therapy that should be discussed with the patient?

    <p>Increased risk of infertility. (C)</p> Signup and view all the answers

    What is the most common reason for adding progesterone to estrogen in hormone replacement therapy?

    <p>To prevent endometrial cancer. (A)</p> Signup and view all the answers

    Which of the following is a possible side effect of tamoxifen?

    <p>Increased risk of uterine fibroids. (B)</p> Signup and view all the answers

    What is the primary role of the hypothalamus in the HPG axis?

    <p>Produces hormones that regulate the pituitary gland's hormone production. (B)</p> Signup and view all the answers

    Which of the following drugs is a selective estrogen receptor (ER) agonist?

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

    Which of the following is NOT an inhibitor of estrogen synthesis?

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

    Which drug is a partial agonist of the progesterone receptor (PR)?

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

    What is the main function of the pituitary gland in the HPG axis?

    <p>To produce and release luteinizing hormone (LH) and follicle-stimulating hormone (FSH) in response to hypothalamic signals. (A)</p> Signup and view all the answers

    Which of the following is an example of an estrogen analog?

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

    What is the mechanism of action of fulvestrant?

    <p>It is a pure estrogen receptor antagonist. (A)</p> Signup and view all the answers

    Which of the following drugs is used as a contraceptive and can also be used in hormone replacement therapy (HRT)?

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

    Which of the following statements accurately describes the action of clomiphene?

    <p>It primarily acts as an estrogen receptor antagonist in the pituitary gland. (B)</p> Signup and view all the answers

    What is the primary difference in the mechanism of action between tamoxifen and fulvestrant?

    <p>Tamoxifen targets only the AF2 domain of the estrogen receptor, while fulvestrant inhibits both AF1 and AF2 domains. (A)</p> Signup and view all the answers

    Which of the following statements about the pharmacokinetics of clomiphene is TRUE?

    <p>The half-life of clomiphene is approximately 5 days. (B)</p> Signup and view all the answers

    Why do selective estrogen receptor modulators (SERMs) exhibit different effects in different tissues?

    <p>The binding of SERMs to ER isoforms triggers the recruitment of distinct co-activators or co-repressors in different tissues, leading to tissue-specific responses. (D)</p> Signup and view all the answers

    Which of the following is NOT a characteristic of fulvestrant?

    <p>It primarily targets the AF1 domain of the estrogen receptor. (D)</p> Signup and view all the answers

    What is the primary reason for using the minimum dose and duration in hormone replacement therapy?

    <p>To avoid adverse effects (A)</p> Signup and view all the answers

    Which delivery system is specifically designed to prevent hepatic catabolism of testosterone?

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

    Flutamide is primarily used in the treatment of which condition?

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

    What is the action of finasteride in the treatment of benign prostatic hypertrophy?

    <p>It inhibits 5α-reductase (B)</p> Signup and view all the answers

    Which of the following drugs is associated with hepatotoxicity among androgens?

    <p>17α-alkylated androgens (D)</p> Signup and view all the answers

    In postmenopausal women, what is hormone replacement therapy most commonly used for?

    <p>Treating vasomotor disturbances (A)</p> Signup and view all the answers

    What potential side effect should be discussed with patients starting testosterone therapy?

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

    Which drug class does anastrozole belong to, and what is its primary use?

    <p>Aromatase inhibitor; breast cancer treatment (A)</p> Signup and view all the answers

    What is the mechanism of action of spironolactone?

    <p>Steroidal competitive antagonist at AR and MR (A)</p> Signup and view all the answers

    Which of the following is an active metabolite of spironolactone?

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

    What class of drugs does dutasteride belong to?

    <p>5a-reductase inhibitors (C)</p> Signup and view all the answers

    What is the primary clinical use of finasteride?

    <p>Management of BPH and male pattern baldness (B)</p> Signup and view all the answers

    What is the half-life of spironolactone?

    <p>1-3 hours for the parent compound (C)</p> Signup and view all the answers

    Which of the following hormones is primarily reduced by the action of 5a-reductase inhibitors?

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

    Which of the following describes the additional action of spironolactone apart from its antagonistic effects?

    <p>Inhibiting 17a-hydroxylase activity (C)</p> Signup and view all the answers

    Finasteride specifically inhibits which type of 5a-reductase?

    <p>Type 2 (D)</p> Signup and view all the answers

    Which of the following differentiates dutasteride from finasteride?

    <p>Dutasteride inhibits both Type 1 and Type 2 5a-reductase. (B)</p> Signup and view all the answers

    What role does NADP play in the function of 5a-reductase?

    <p>It acts as a substrate for the reduction process. (D)</p> Signup and view all the answers

    What is a known side effect associated with spironolactone?

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

    Which of the following statements about the pharmacokinetics of spironolactone is accurate?

    <p>It undergoes extensive hepatic metabolism. (B)</p> Signup and view all the answers

    What is a common clinical indication for using abiraterone?

    <p>Prostate cancer treatment (A)</p> Signup and view all the answers

    What role does the enzyme aromatase play in estrogens synthesis?

    <p>Converts androgens to estrogens (B)</p> Signup and view all the answers

    Which hormone is primarily responsible for stimulating the growth of the female reproductive tract?

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

    What is the primary mechanism of action for hormonal contraceptives?

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

    Which of the following compounds acts as an estradiol receptor antagonist?

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

    Which receptor is involved in the cellular response to progesterone?

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

    What is a potential adverse effect of high estrogen levels in hormonal treatment?

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

    Which of the following is a known selective estrogen receptor modulator (SERM)?

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

    What is a key structural requirement for the activity of estrogen receptor agonists?

    <p>Aromatic A ring and C3-OH (C)</p> Signup and view all the answers

    What condition can be treated with estrogen receptor antagonists?

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

    Which of the following hormones is produced predominantly by the ovaries?

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

    What is the role of co-activators in estrogen receptor-mediated transcription?

    <p>Activate transcription of target genes (B)</p> Signup and view all the answers

    What is a common structural characteristic of progesterone receptor agonists?

    <p>Require a 3-ketone (B)</p> Signup and view all the answers

    How do antagonists of estrogen receptors affect receptor activity?

    <p>Induce a conformational change that prevents activation (A)</p> Signup and view all the answers

    Which condition is treated with aromatase inhibitors?

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

    Study Notes

    Endocrine Pharmacology: Female Gonadal Hormone Analogs, Antagonists & Inhibitors

    • Key drugs are categorized as estrogen analogs (agonists), estrogen synthesis inhibitors, estrogen partial agonists, estrogen antagonists (partial agonists/antagonists), progestin agonists, and progestin antagonists.
    • Estrogen analogs (agonists) include estradiol, ethinyl estradiol, conjugated estrogens, and esterified estrogens. Selective estrogen receptor agonists/antagonists include tamoxifen and toremifene, and bazedoxifene. Partial agonists include clomiphene. Antagonists include fulvestrant.
    • Estrogen synthesis inhibitors include exemestane, anastrozole, and letrozole.
    • Progestin analogs (agonists) include progesterone, medroxyprogesterone, levonorgestrel, megestrol, norethindrone, and drospirenone. Progestin partial agonists include danazol. Antagonists include mifepristone.
    • Lecture objectives include explaining female gonadal hormone function in relation to hormone stimulation, biosynthesis, conditions with altered hormone levels, and biological targets for drug therapy. Also cover significant aspects of estrogen/progesterone drugs and anti-estrogen/progesterone drugs, including structure, mechanism of action, pharmacokinetics, indications, contraindications, and adverse effects.
    • Various pharmacological agents are covered. Estrogen analogs include estradiol, ethinyl estradiol, conjugated estrogens, esterified estrogens, taomcifen, toremifene, bazedoxifene, and clomiphene. Estrogen synthesis inhibitors are exemestane, anastrozole, and letrozole. Progestin analogs include progesterone, medroxyprogesterone, levonorgestrel, megestrol, norethindrone, and drospirenone.
    • Conditions benefited from hormone therapy include hormonal deficiency, primary hypogonadism, post-menopause, excessive ovarian androgen secretion, hirsutism, amenorrhea, hormonal contraceptives, infertility & ovulation, pregnancy termination, and precocious puberty.
    • Conditions benefited from antagonists and inhibitors of estrogen/progesterone receptors include breast cancer, hormonal contraception, infertility, and ovulation, pregnancy termination, and precocious puberty.
    • Natural estrogens include estradiol (17β-estradiol; E2), estrone (E1), and estriol (E3), where estradiol is the major secretory estrogen of the ovary, while estrone and estriol are produced in the liver from estradiol or androstenedione.
    • Production of estrogens occurs in mature premenopausal women (ovaries), postmenopausal women and men (adipose tissue), and during pregnancy (placenta).
    • Progestins are produced by ovaries, testes, and adrenal glands.
    • Targets and pharmacological agents include aromatase (enzyme that converts androgens to estrogens, inhibitor anastrozole), estrogen receptors (endogenous agonist estradiol, estrone, estriol), and progesterone receptor(endogenous agonist progesterone).
    • Cellular response targets include genomic effects, non-genomic effects (granulosa cell Ca2+ uptake), estrogen receptors (ER-α and β), and progesterone receptors.
    • Cellular response activation is described by ligand binding, receptor conformation change, co-repressor release, receptor dimerization, DNA binding to PRE, histone acetylation, transcription, and co-activator binding. Cellular response antagonism includes similar binding and dimerization, preventing co-activator binding, and potentially blocking receptor translocation or productive DNA interactions.
    • Estrogenic compounds include steroidal natural (estradiol, estrone, estriol), steroidal synthetic (ethinyl estradiol, mestranol, quinestrol), and nonsteroidal synthetic (diethylstilbestrol, chlorotrianisene, methallenestril).
    • Progestins include Levonorgestrel (Norplant), Medroxyprogesterone acetate (Provera), Megestrol acetate (Megace), Norethindrone acetate (Aygestin), and Progesterone (general).
    • Hormone analogs (including aromatase inhibitors and 5α-reductase inhibitors) are used for various conditions and have specific mechanisms of action (e.g., preventing oxidation to estrone, interfering with estrogen receptor activity).
    • Common side effects and drug-drug interactions (DDIs) are listed for each class of agent. These often involve risks for various cancers, bleeding, and hormonal imbalances.

    Endocrine Pharmacology: Male Gonadal Hormone Analogs, Antagonists & Inhibitors

    • Relevant chapters include Basic & Clinical Pharmacology (Katzung), Principles of Medicinal Chemistry (Foye), and Goodman & Gilman's The Pharmacological Basis of Therapeutics.
    • Lecture objectives cover male gonadal hormone function, including stimulation by hormones, testosterone biosynthesis, effects of altered hormone levels, and biological targets for drug therapy for androgenic and anti-androgenic drugs.
    • Significant aspects of androgenic drugs and anti-androgenic drugs include structure-activity relationships (SARs), mechanisms of action, pharmacokinetics, and related side effects.
    • Includes a summary of key highlights for the section regarding androgen SAR, testosterone analogs, androgen synthesis inhibitors, androgen receptor, 5α-reductase, and other antagonists.
    • Pharmacological agents covered include analogs of testosterone, AR agonists, AR antagonists, androgen synthesis inhibitors, and related drugs.
    • Important molecules include testosterone (19 carbons), pulsatile production peaking at 8 AM, and dihydrotestosterone (DHT).
    • Representative drugs include GnRH receptor antagonists and agonists, androgen receptor agonists and antagonists, 5 alpha reductase, 17 alpha hydroxylase, C17/20 lyase, reversible/irreversible inhibitors, and others.
    • Conditions requiring therapy include male hormone deficiency or Low-T (low endogenous testosterone levels) and benign prostatic hypertrophy (BPH).
    • Androgenic and anabolic activities are discussed, differentiating effects on male sex characteristics, spermatogenesis, and effects like increased growth, protein breakdown, electrolyte, and water retention.
    • SAR relationships are given differentiating androgenic and anabolic required components of steroid structure.
    • Numerous testosterone esters and analogs are listed.
    • Synthetic anabolic agents are discussed including their modifications to steroid core structure, which changes the balance between androgenic and anabolic activities. Examples include nandrolone and oxandrolone.
    • Non-steroidal androgen receptor antagonists/antagonists (like Apalutamide, Bicalutamide, Flutamide, and Nilutamide) and steroidal antagonists/antagonists (like Spironolactone) are covered.
    • Detailed mechanisms of action and pharmacokinetics of selected major drugs are listed, including side effects. Important specific examples are included such as finasteride and dutasteride (5a-reductase inhibitors).

    Other Important Topics

    • Aromatase inhibitors (like exemestane, anastrozole, letrozole) and their mechanisms of action, side effects, and clinical use are detailed, along with their relationship to androgen structures.
    • Classifications of various drugs and their corresponding therapeutic applications are described.
    • Several "pearls" or key takeaways regarding hormone replacement therapy are provided, outlining important considerations. Information on case studies involving hormone imbalances, hormone replacement, and prostate cancer treatment is given.
    • Specific examples are provided in the estrogen and androgen sections.

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    Female Gonadal Hormone Analogs, Antagonists & Inhibitors PDF

    Description

    This quiz covers the categorization and functions of key female gonadal hormone analogs, antagonists, and inhibitors. You'll explore estrogen and progestin types, their functions, and the important drugs used in hormonal therapies. Test your knowledge of these critical components of endocrine pharmacology.

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