Aromatase and Estrogen Functions Quiz
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Questions and Answers

What is the primary function of aromatase?

  • To convert androgens into estrogens. (correct)
  • To increase progesterone levels.
  • To block estrogen receptors.
  • To inhibit the production of androgens.

    • Which of the following is an example of an aromatase inhibitor?

  • Danazol
  • Clomiphene
  • Ketoconazole
  • Anastrozole (correct)

    • Which estrogen is considered a potent endogenous agonist?

  • Estriol
  • Estradiol (correct)
  • Anastrozole
  • Estrone

    • What is the impact that Estrogen has on bone density?

    <p>Increases bone density. (C)</p> Signup and view all the answers

    What is the effect of Clomiphene?

    <p>GnRH agonist. (A)</p> Signup and view all the answers

    Tamoxifen is described by which of the following?

    <p>Selective Estrogen Antagonist (D)</p> Signup and view all the answers

    What is the endogenous agonist of Progesterone Receptors?

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

    Where are Type I Estrogen receptors predominantly found?

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

    Which is the major secretory estrogen of the ovary?

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

    What can ER-a (Estrogen receptor) be found?

    <p>Female reproductive tract and mammary glands (C)</p> Signup and view all the answers

    Which of these is NOT a target of pharmacological/biological agents?

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

    Aromatization of a steroid ring, is a function of:

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

    What does Aromatase do?

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

    The genomic effects of estradiol will:

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

    What is ethinyl estradiol metabolized into?

    <p>An active metabolite via N-dealkylation (A)</p> Signup and view all the answers

    A 17α-alkyl group is added to some hormones to do what?

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

    What does 'EXTENDS duration of action' refer to?

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

    What can proliferation of endometrial tissue lead to?

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

    Which enzyme is responsible for the N-dealkylation of ethinyl estradiol?

    <p>CYP3A4 (A)</p> Signup and view all the answers

    Which modification results in extended activity?

    <p>Long Fatty chain at C9 (B)</p> Signup and view all the answers

    What is a key characteristic of toremifene (Foreston)?

    <p>It is related to estrogen (A)</p> Signup and view all the answers

    What is broken down by hydrolysis?

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

    What is the typical dosage for a substance?

    <p>5-10mg (C)</p> Signup and view all the answers

    What is a common effect of estrogen on the endometrium?

    <p>Promotion of tissue proliferation (A)</p> Signup and view all the answers

    Which of the following is an indication of EE/drospirenone?

    <p>Premenstrual dysphoric disorder (B)</p> Signup and view all the answers

    Which of the following is a characteristic of ADS?

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

    What does ADS release?

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

    What modification prevents oxidation to estrone?

    <p>Using a ketone (D)</p> Signup and view all the answers

    Which of the following is not given?

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

    What route of metabolism is associated to Ethinyl estradiol?

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

    Which of the following is a brand name associated with EE (ethinyl estradiol) and noretindrone?

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

    What does 'PO QP' refer to?

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

    Which of the following is a brand name associated with EE (ethinyl estradiol) and norgestimate?

    <p>Ortho Tri-Cyclen (D)</p> Signup and view all the answers

    How is testosterone enanthate typically administered?

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

    What is the function of CIT-OA?

    <p>Important for ER activity (C)</p> Signup and view all the answers

    What is the half life ($t_{\frac{1}{2}}$) of 17\alpha-alkyl groups?

    <p>12-14 days (A)</p> Signup and view all the answers

    What is the primary effect of an increase in anabolic activity?

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

    What does the symbol '&' mean?

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

    What ratio is mentioned in relation to testosterone enanthate?

    <p>Estrogenic to Insulin-like Growth Factor 1 (IGF-1) (C)</p> Signup and view all the answers

    What is the anabolic strength mentioned in relation to 19-nor?

    <p>4x stronger anabolic (B)</p> Signup and view all the answers

    What effect does testosterone enanthate have on anabolic activity?

    <p>Increases anabolic activity (D)</p> Signup and view all the answers

    What type of tissue is affected in benign prostatic hyperplasia?

    <p>Inner prostate tissue (A)</p> Signup and view all the answers

    What is the primary goal of treating benign prostatic hyperplasia?

    <p>Reduce tissue growth to restore urinary function (C)</p> Signup and view all the answers

    What enzyme converts testosterone to dihydrotestosterone?

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

    Which class of drugs is used, along with 5α-reductase inhibitors, to treat benign prostatic hyperplasia?

    <p>Androgen receptor antagonists (A)</p> Signup and view all the answers

    What type of tissue growth is associated with advanced prostate carcinoma?

    <p>Growth of superficial prostate tissue (A)</p> Signup and view all the answers

    What is the primary goal in treating advanced prostate carcinoma?

    <p>Reduce androgen biosynthesis and/or effects (B)</p> Signup and view all the answers

    Which of the following is a non-steroidal antiandrogen?

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

    What is the function of finasteride?

    <p>5-alpha reductase inhibitor (A)</p> Signup and view all the answers

    Which of the following decreases SGBG synthesis?

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

    What is the role of SGBG?

    <p>Binds to testosterone and albumin (D)</p> Signup and view all the answers

    Which of the following agents is an AR antagonist?

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

    What modification is present on the testosterone molecule at the 17 position?

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

    What structural feature is absent in the steroidal antiandrogen?

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

    Which of the following is an indication for Yaz and Yasmin?

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

    Conjugated estrogens are prodrugs that require what process?

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

    What can result from too low estrogen levels?

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

    What is a common side effect of high estrogen levels?

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

    Too low levels of progestin can lead to what?

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

    What side effect is associated with high progestin levels?

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

    What is a common androgenic effect?

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

    Which of the following describes Raloxifene (Evista)?

    <p>Selective estrogen receptor modulator (C)</p> Signup and view all the answers

    What is the mechanism of action of Clomiphene?

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

    In post-menopausal women, increased dose of estrogen increases the risk for:

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

    What is a potential effect of estrogen on clotting factors?

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

    The chloro-ethyl substituent replaces ethyl in which medication?

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

    What is a primary effect of Bazedoxifene (Duaree)?

    <p>Reduces proliferation of endometrial tissue (B)</p> Signup and view all the answers

    What type of bleeding is associated with Progestin levels being too low?

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

    Which of the following is a hormonal contraceptive?

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

    Flashcards

    GnRH Hormones

    Gonadotropin-Releasing Hormones that stimulate the release of FSH and LH.

    FSH

    Follicle-Stimulating Hormone, involved in the growth of ovarian follicles.

    LH

    Luteinizing Hormone, triggers ovulation and development of the corpus luteum.

    Estrogens

    A group of hormones responsible for the development of female secondary sexual characteristics.

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    Aromatization

    Process by which androgens are converted to estrogens.

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    Anastrozole

    Aromatase inhibitor that reduces estrogen production.

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    Estrogen Receptors

    Proteins that mediate the effects of estrogens in tissues.

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    Tamoxifen

    A selective estrogen receptor modulator (SERM) used to treat breast cancer.

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    Progesterone

    Hormone that prepares the endometrium for potential implantation of an embryo.

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    Mifepristone

    A medication that blocks progesterone, used for medical abortion.

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    Clomiphene

    A medication that stimulates ovulation by blocking estrogen receptors.

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    Ketoconazole

    An antifungal that also inhibits steroidogenesis and reduces androgen levels.

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    Estradiol

    The most potent form of estrogen, crucial for reproductive functions.

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    Estrone

    A weak form of estrogen, converted from androgens, present in post-menopausal women.

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    Inhibitors

    Agents that decrease or suppress hormonal actions or enzyme functions.

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    Testosterone Enanthate

    A synthetic form of testosterone used for hormonal therapy.

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    Anabolic Activity

    The process of building up organs and tissues, particularly muscle mass.

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    Administration Route

    The method by which a medication is delivered; in this case, intramuscular (IM).

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    19-nor

    A chemical structure related to certain anabolic steroids that is a derivative of testosterone.

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    Strength Ratio

    The comparative strength of certain anabolic steroids, indicating potency.

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    17d-metinyl

    A synthetic anabolic steroid that mimics testosterone.

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    Metabolism

    The chemical processes that occur within a living organism to maintain life.

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    Hydrolysis

    A chemical process that splits molecules by adding water.

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    Nanavolone

    An anabolic steroid related to testosterone with alterations for improved effects.

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    Oxymetholone

    An anabolic steroid known for its muscle-building properties.

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    Oxandrolone

    A synthetic anabolic steroid used for weight gain and muscle wasting treatments.

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    Duration of action

    The length of time a drug remains effective in the body.

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    B-fluto group

    A chemical modification in anabolic steroids that alters lipophilicity and effects.

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    Ketone

    A class of compounds that contains a carbonyl group.

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    CYP3A4

    An enzyme that metabolizes many drugs in the liver.

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    Ethinyl estradiol

    A synthetic form of estrogen used in contraceptives.

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    N-dealkylation

    The removal of an alkyl group from a nitrogen atom.

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    Premenstrual Dysphoric Disorder

    A severe form of premenstrual syndrome (PMS).

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    Endometriosis

    A condition where tissue similar to the lining inside the uterus grows outside.

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    Drospirenone

    A synthetic progestin used in hormonal contraceptives.

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    Norethindrone

    A synthetic progestin used in birth control pills.

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    Norgestimate

    A progestin used in hormonal contraceptives.

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    Toremifene

    A medication used in the treatment of breast cancer.

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    Modulator

    A substance that helps to regulate the activity of another substance.

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    Ortho-Cyclen

    A combination birth control pill containing estrogen and progestin.

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    Estrostep

    A birth control pill that contains estrogen and a progestin.

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    Active Metabolite

    A metabolite that is pharmacologically active in the body.

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    SGBG

    Sex hormone-binding globulin, a protein that binds sex hormones.

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    Testosterone Analogs

    Synthetic compounds mimicking testosterone effects.

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    Prostate Hypertrophy

    Enlargement of the prostate gland, often benign.

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    Dihydrotestosterone

    An active metabolite of testosterone linked to prostate growth.

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    5α-Reductase

    Enzyme that converts testosterone to dihydrotestosterone.

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    Finasteride

    A 5α-reductase inhibitor used for treating prostate issues.

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    Anabolic Agents

    Substances that promote muscle growth and recovery.

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    Flutamide

    An androgen receptor antagonist used in prostate cancer treatment.

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    Bicalutamide

    Another androgen receptor antagonist used for advanced prostate cancer.

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    Spironolactone

    A potassium-sparing diuretic with androgen-blocking effects.

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    Androgen Agonists

    Drugs that mimic the effects of androgens like testosterone.

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    Methyltestosterone

    An oral anabolic steroid derived from testosterone.

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    Advanced Prostate Carcinoma

    Advanced stage of prostate cancer that can spread.

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    Yaz + Yasmin

    Hormonal contraceptives used to treat acne, containing drospirenone.

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    Estrogen Prodrugs

    Estrogens that require hydrolysis to become active, increasing their solubility.

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    Raloxifene

    A Selective Estrogen Receptor Modulator (SERM) used for osteoporosis treatment.

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    Progestin

    Synthetic hormones that mimic progesterone, used in contraceptives.

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    Fluvestrant

    An ER antagonist effective for tamoxifen-resistant breast cancer treatments.

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    Aromatase Inhibitors

    Medications that prevent the conversion of androgens to estrogens.

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    Bazedoxifene

    A SERM used to treat osteoporosis, often combined with estrogen.

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    Hirsutism

    Excessive hair growth often associated with higher androgen levels.

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    Breakthrough Bleeding

    Unexpected bleeding that can occur with hormonal contraceptive use.

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    Progestin Receptor Antagonist

    Drugs that block the action of progestins at their receptors.

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    Study Notes

    Female Hormone Regulation

    • Gonadal hormones regulate the female reproductive system
    • Hypothalamus releases GnRH, stimulating the anterior pituitary to release FSH and LH.
    • Ovaries produce estrogen and progesterone, crucial for maturation, bone density, and pregnancy.
    • Aromatase converts androgens to estrogens.
    • Estrogen receptors (ERα and ERβ) are crucial for various metabolic effects.
    • Progesterone receptors regulate various functions during pregnancy.
    • Natural estrogens include estradiol, estrone, and estriol, with estradiol being the major secretory estrogen of the ovary.
    • Estrogen analogs/contraceptives are used to prevent pregnancy and manage certain medical conditions.
    • Estrogen receptor modulators (SERMs), such as tamoxifen and raloxifene, affect estrogen action in different tissues.

    Progesterone Regulation

    • Progesterone analogs are used to maintain or regulate uterine lining.
    • Progesterone is crucial for maintaining the uterine lining during pregnancy.
    • Progesterone plays a role in various physiological responses, including insulin and ventilation.
    • Progesterone analogs and antagonists have various uses.
    • Progesterone agonists are similar to endogenous hormones.
    • Progesterone antagonists have a different action.
    • Steroid core structure, ring modifications, and ketone position strongly influence the activity and properties of various progesterone analogs and agonists.

    Aromatase Inhibitors

    • Aromatase inhibitors prevent the conversion of androgens to estrogens.
    • Exemestane and Anastrozole are irreversible aromatase inhibitors, while Letrozole is a reversible inhibitor, all used in treating various conditions.
    • Aromatase inhibitors are commonly used in cancer treatment to lower estrogen levels.

    Male Hormone Regulation

    • Androgens are crucial for male development and characteristics.
    • Testosterone is the primary androgen.
    • Dihydrotestosterone (DHT) is a metabolite of testosterone.
    • Androgen receptor agonists and antagonists have different uses in treating male-related conditions like prostate cancer and benign prostatic hyperplasia.
    • 5α-reductase inhibitors block testosterone conversion to DHT, used for specific male conditions.
    • Androgen suppression is a therapy that lower levels of androgens.

    Androgen Receptor Antagonists

    • Non-steroidal androgen receptor antagonists include apalutamide, bicalutamide, nilutamide, and flutamide.
    • Steroidal androgen antagonist include spironolactone.
    • Androgen synthesis inhibitors reduce androgen levels.
    • Abiraterone is an androgen synthesis inhibitor.

    Sedatives and Hypnotics

    • Barbiturates (like phenobarbital and secobarbital) and benzodiazepines (like diazepam and lorazepam) are central nervous system (CNS) depressants used for anxiety and sleep disturbance.
    • Barbiturates enhance GABA receptor activity to prolong chloride channel opening.
    • Benzodiazepines enhance GABA action at specific sites for their therapeutic effects.
    • Non-benzodiazepines are used for sleep and reduce anxiety in certain instances.
    • Buspirone and Diphenhydramine are non-benzodiazepine anxiolytics or sleep drugs.

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    Exam #3 PDF

    Description

    Test your knowledge on aromatase, estrogen functions, and their roles in the body. This quiz covers key concepts like the effects of estrogen on bone density, common inhibitors, and pharmacological agents impacting estrogen receptors. Perfect for students studying endocrinology or related fields.

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