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Questions and Answers
What is the primary purpose of using lutropin α in women with anovulation?
What is the primary purpose of using lutropin α in women with anovulation?
Which of the following statements about the administration of hCG is correct?
Which of the following statements about the administration of hCG is correct?
What are the typical signs of hypogonadism in males that may be treated with exogenous androgen?
What are the typical signs of hypogonadism in males that may be treated with exogenous androgen?
What serious complication of treatment is most commonly associated with ovarian stimulation in women?
What serious complication of treatment is most commonly associated with ovarian stimulation in women?
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Which of the following conditions is NOT typically treated with ovulation induction agents like lutropin α?
Which of the following conditions is NOT typically treated with ovulation induction agents like lutropin α?
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What enzyme is responsible for cleaving the long side chain of cholesterol to form pregnenolone?
What enzyme is responsible for cleaving the long side chain of cholesterol to form pregnenolone?
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Which reaction is NOT catalyzed by CYP17A1?
Which reaction is NOT catalyzed by CYP17A1?
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What is the product formed from the metabolism of pregnenolone by CYP17A1?
What is the product formed from the metabolism of pregnenolone by CYP17A1?
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Which enzyme converts testosterone into dihydrotestosterone?
Which enzyme converts testosterone into dihydrotestosterone?
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Where are androgens primarily converted to estrogens?
Where are androgens primarily converted to estrogens?
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Which statement about pregnenolone is correct?
Which statement about pregnenolone is correct?
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What major steroid does progesterone convert into after further metabolism?
What major steroid does progesterone convert into after further metabolism?
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Which estrogen is considered the most potent naturally occurring estrogen?
Which estrogen is considered the most potent naturally occurring estrogen?
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Which enzyme is primarily responsible for the aromatization of precursor androgens to estrogens?
Which enzyme is primarily responsible for the aromatization of precursor androgens to estrogens?
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Which tissues exhibit high expression of CYP19 for estrogen production?
Which tissues exhibit high expression of CYP19 for estrogen production?
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After menopause, where does the majority of circulating estrogen in women originate from?
After menopause, where does the majority of circulating estrogen in women originate from?
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What are the two subtypes of nuclear estrogen receptors?
What are the two subtypes of nuclear estrogen receptors?
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Which of the following tissues is NOT capable of aromatizing androgens to estrogens?
Which of the following tissues is NOT capable of aromatizing androgens to estrogens?
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What mechanism do nuclear estrogen receptors operate through?
What mechanism do nuclear estrogen receptors operate through?
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Which term best describes the common activity shared by all estrogens?
Which term best describes the common activity shared by all estrogens?
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In men, which tissue serves as the main source of circulating estrogens?
In men, which tissue serves as the main source of circulating estrogens?
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What is a significant factor in the growth of breast cancers?
What is a significant factor in the growth of breast cancers?
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Which condition is characterized by the growth of endometrial tissue outside the uterus?
Which condition is characterized by the growth of endometrial tissue outside the uterus?
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How does continuous administration of GnRH influence pituitary function?
How does continuous administration of GnRH influence pituitary function?
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What is required for the conversion of testosterone to DHT in prostate tissue?
What is required for the conversion of testosterone to DHT in prostate tissue?
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What initiates the release of gonadotropins from the pituitary gland?
What initiates the release of gonadotropins from the pituitary gland?
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What is the role of GnRH in the reproductive hormone regulation?
What is the role of GnRH in the reproductive hormone regulation?
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What type of growth is associated with benign prostatic hyperplasia (BPH)?
What type of growth is associated with benign prostatic hyperplasia (BPH)?
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What effect does the administration of anti-estrogens have on breast cancer cells expressing ER?
What effect does the administration of anti-estrogens have on breast cancer cells expressing ER?
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Which hormone does GnRH primarily stimulate the secretion of from the pituitary?
Which hormone does GnRH primarily stimulate the secretion of from the pituitary?
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Which of the following conditions is a contraindication for estrogen use?
Which of the following conditions is a contraindication for estrogen use?
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What is a common adverse effect associated with progestin-only contraceptive drugs?
What is a common adverse effect associated with progestin-only contraceptive drugs?
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What is the primary mechanism by which combination estrogen-progestin contraceptives inhibit ovulation?
What is the primary mechanism by which combination estrogen-progestin contraceptives inhibit ovulation?
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Which of the following hormones is primarily used in combination contraceptives?
Which of the following hormones is primarily used in combination contraceptives?
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Which of the following is a potential outcome of unopposed estrogen use in women with a uterus?
Which of the following is a potential outcome of unopposed estrogen use in women with a uterus?
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Which progestin-related adverse effect is associated with androgen-like progestins?
Which progestin-related adverse effect is associated with androgen-like progestins?
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Which type of oral contraceptive is characterized by a constant dose of estrogen and progestin throughout the cycle?
Which type of oral contraceptive is characterized by a constant dose of estrogen and progestin throughout the cycle?
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What effect does combination contraceptives have on cervical mucus?
What effect does combination contraceptives have on cervical mucus?
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What is the primary purpose of administering progestin alongside estrogen in contraceptive therapies?
What is the primary purpose of administering progestin alongside estrogen in contraceptive therapies?
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Which of the following describes the incidence of venous thromboembolic disease in users of combination oral contraceptives?
Which of the following describes the incidence of venous thromboembolic disease in users of combination oral contraceptives?
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Study Notes
Reproductive Pharmacology Lecture Notes
- This lecture covers pharmacological agents used in reproductive pharmacology, including endogenous molecules (e.g., steroid hormones, peptide hormones) and synthetic drugs.
Session Learning Objectives
- Identify classes of gonadal steroids and describe their effects and mechanisms.
- Detail clinical uses of gonadal steroids, considering administration routes, combinations, adverse effects, and contraindications.
- Describe classes of drugs used to modify gonadal steroid actions.
- Explain the clinical use of oxytocin.
Session Outline
I. Overview of Pharmacological Classes
- The lecture covers classes of pharmacological agents for reproductive processes.
- Includes endogenous and synthetic molecules.
II. Gonadal Steroids
- Brief review and introduction to compounds.
- Estrogens
- Progestins
- Androgens
- Steroid hormone biosynthesis begins with cholesterol.
- CYP11A1 (aka P450scc) cleaves the long side chain of cholesterol to form pregnenolone.
- Pregnenolone can be converted directly to progesterone (major progestin).
- Pregnenolone is metabolized by CYP17A1 to produce DHEA and androstenedione (adrenal androgens).
- Androgens are converted to testosterone.
- Testosterone can be converted into dihydrotestosterone (DHT).
- Androgens are converted to estrogens by aromatization (CYP19).
III. Clinical Uses of Gonadal Steroids
- Female hormone replacement therapy
- Primary hypogonadism
- Postmenopausal hormonal therapy
- Contraception
- Combination estrogen-progestin contraceptives
- Progestin-only contraception
- Emergency contraception
- Use of androgens and anabolic steroids
- Replacement therapy in hypogonadism
- Other reported uses
- Adverse effects and contraindications
IV. Modulators of Gonadal Steroid Action
- Gonadotropin releasing hormone (GnRH) agonists
- GnRH receptor antagonists
- Gonadotropins
- Aromatase inhibitors
- Selective estrogen receptor modulators (SERMs)
- 5α-reductase inhibitors
- Androgen receptor antagonists
- Progesterone receptor antagonists
V. Oxytocin
- Uses
- Adverse effects and contraindications
I. Overview of Pharmacological Classes
- Covers pharmacological agents used in reproductive processes, including endogenous molecules (like steroid hormones) and synthetic drugs.
A. Estrogens
- 17β-estradiol (E2) is the most potent naturally occurring estrogen.
- Estrone (E1) and estriol (E3) are less potent.
- All estrogens are derived from aromatization of androgens.
- Ovaries and placenta have high CYP19 (aromatase) expression.
- Certain non-reproductive tissues can aromatize androgens.
- After menopause, adipose tissue is a major source of estrogen.
B. Progestins
- Natural progestin is progesterone.
- Required for pregnancy maintenance.
- Synthetic derivatives have varying effects (estrogenic, anti-estrogenic, etc.).
- Many have other hormonal effects (e.g., estrogenic, anti-estrogenic, androgenic, etc.).
- Some are chemically and pharmacologically similar to progesterone (e.g., hydroxyprogesterone, medroxyprogesterone, etc.).
- Some are 17-ethinyl testosterone derivatives (e.g., dimethisterone) or 19-nortestosterone derivatives (e.g., norethindrone).
- Some third-generation compounds (e.g., desogestrel) have lower androgenic activity.
C. Androgens
- Essential for male sexual development and maturation, and sex characteristics.
- DHEA and androstenedione are adrenal androgens.
- Testosterone is the main circulating androgen.
- DHT is the most potent intracellular androgen.
- Testosterone is a prohormone.
- 5α-reductase converts testosterone into DHT.
III. Clinical Uses of Gonadal Steroids
- Female Hormone Replacement Therapy: Primary hypogonadism, Postmenopausal hormonal therapy
- Contraception: Combination estrogen-progestin, Progestin-only, Emergency
- Androgens and Anabolic Steroids: Replacement therapy, other uses, adverse effects, contraindications.
IV. Modulators of Gonadal Steroid Action
- Drugs that modify the action of gonadal steroids
- Includes agonists, antagonists and other related agents.
V. Oxytocin
- A 9 amino acid peptide hormone.
- Secreted by the posterior pituitary.
- Stimulates uterine contractions (labor).
- Involved in milk ejection.
- Clinical uses include inducing labor, etc.
- Short half-life.
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Description
Explore the pharmacological agents involved in reproductive health, focusing on both endogenous molecules and synthetic drugs. Learn about gonadal steroids, their clinical uses, and the mechanisms underlying their actions, including the role of oxytocin. This lecture provides a comprehensive review for understanding reproductive pharmacology.
