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Questions and Answers
Which of the following is the most potent estrogen produced by the ovary?
Which of the following is the most potent estrogen produced by the ovary?
Estrone has approximately two-thirds the estrogenic potency of estradiol.
Estrone has approximately two-thirds the estrogenic potency of estradiol.
False
What is the principal estrogen produced by the placenta during pregnancy?
What is the principal estrogen produced by the placenta during pregnancy?
Estriol
Synthetic estrogens like ________ undergo less first-pass metabolism than naturally occurring steroids.
Synthetic estrogens like ________ undergo less first-pass metabolism than naturally occurring steroids.
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Match the following hormones or compounds with their descriptions:
Match the following hormones or compounds with their descriptions:
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What is a therapeutic use of gonadal hormones?
What is a therapeutic use of gonadal hormones?
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Selective estrogen-receptor modulators (SERMs) include compounds like raloxifene and ethinyl estradiol.
Selective estrogen-receptor modulators (SERMs) include compounds like raloxifene and ethinyl estradiol.
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What are the primary hormones produced from cholesterol by the gonads?
What are the primary hormones produced from cholesterol by the gonads?
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Which condition is a contraindication for the use of oral contraceptives?
Which condition is a contraindication for the use of oral contraceptives?
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Androgens have no effects on sperm production.
Androgens have no effects on sperm production.
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What hormone is primarily responsible for stimulating steroidogenesis in Leydig cells?
What hormone is primarily responsible for stimulating steroidogenesis in Leydig cells?
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Testosterone undergoes rapid hepatic catabolism when replaced __________.
Testosterone undergoes rapid hepatic catabolism when replaced __________.
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Match the following types of androgens with their characteristics:
Match the following types of androgens with their characteristics:
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What is a primary effect of clomiphene (Clomid)?
What is a primary effect of clomiphene (Clomid)?
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Raloxifene significantly reduces the risk of coronary events.
Raloxifene significantly reduces the risk of coronary events.
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What adverse effects can clomiphene (Clomid) cause?
What adverse effects can clomiphene (Clomid) cause?
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Progesterone is produced in response to _____ hormone.
Progesterone is produced in response to _____ hormone.
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Match the following progestins with their brand names:
Match the following progestins with their brand names:
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Which of the following is a therapeutic use of progestins?
Which of the following is a therapeutic use of progestins?
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Progestins increase sodium reabsorption in the kidney.
Progestins increase sodium reabsorption in the kidney.
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Name one risk associated with taking raloxifene.
Name one risk associated with taking raloxifene.
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Progestins cause an increase in _____ body temperature.
Progestins cause an increase in _____ body temperature.
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Which of the following does progesterone help develop?
Which of the following does progesterone help develop?
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How long are active pills taken before switching to placebo?
How long are active pills taken before switching to placebo?
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Progestin-only pills are more effective than combined oral contraceptives (COCs).
Progestin-only pills are more effective than combined oral contraceptives (COCs).
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What is the primary use of the transdermal patch?
What is the primary use of the transdermal patch?
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Postcoital contraception reduces the probability of pregnancy to between _____ and 3 percent.
Postcoital contraception reduces the probability of pregnancy to between _____ and 3 percent.
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Match the following contraceptive methods with their duration of effectiveness:
Match the following contraceptive methods with their duration of effectiveness:
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What is a common adverse effect of oral contraceptives?
What is a common adverse effect of oral contraceptives?
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Emergency contraception can only be effective if taken within 48 hours of unprotected intercourse.
Emergency contraception can only be effective if taken within 48 hours of unprotected intercourse.
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What hormone is primarily used in emergency contraceptive pills?
What hormone is primarily used in emergency contraceptive pills?
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The mechanism of action of contraceptives includes inhibiting _____ and thickening the cervical mucus.
The mechanism of action of contraceptives includes inhibiting _____ and thickening the cervical mucus.
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Which of the following statements is true regarding the effects of oral contraceptives?
Which of the following statements is true regarding the effects of oral contraceptives?
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Which of the following progestins is used as an injectable contraceptive?
Which of the following progestins is used as an injectable contraceptive?
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Synthetic progestins generally have a low level of androgenic activity.
Synthetic progestins generally have a low level of androgenic activity.
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Name one adverse effect associated with the use of progestins.
Name one adverse effect associated with the use of progestins.
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Mifepristone is considered a progesterone __________.
Mifepristone is considered a progesterone __________.
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Match the following contraceptive methods with their main mechanisms:
Match the following contraceptive methods with their main mechanisms:
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What is the most common pharmacologic intervention for preventing pregnancy?
What is the most common pharmacologic intervention for preventing pregnancy?
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Drospirenone is a highly androgenic progestin.
Drospirenone is a highly androgenic progestin.
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What is a common clinical use of progestins besides contraception?
What is a common clinical use of progestins besides contraception?
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The primary purpose of COCs is to decrease __________.
The primary purpose of COCs is to decrease __________.
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Which progestin derivative has been associated with an increased risk of osteoporosis?
Which progestin derivative has been associated with an increased risk of osteoporosis?
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Study Notes
Gonadal Hormones
- Gonadal hormones are produced by the gonads - ovaries and testes.
- They are essential for sexual development, reproduction, and maintaining secondary sex characteristics.
- They are used therapeutically in various ways:
- Hormone replacement therapy (HRT): For individuals experiencing hormonal imbalances due to conditions such as menopause or hypogonadism.
- Contraception: Inhibiting ovulation, impairing gametogenesis, and interfering with gestation.
- Cancer management: In some cases, they can be used in chemotherapy for hormone-sensitive cancers.
Estrogens
- Estradiol: Most potent estrogen, produced by the ovaries, dominant in premenopausal women.
- Estrone: Metabolite of estradiol, approximately one-third the potency of estradiol, primary estrogen after menopause.
- Estriol: Another estradiol metabolite, less potent, present in significant amounts during pregnancy due to placental production.
- Conjugated estrogens: Derived from pregnant mares' urine, used in HRT (Premarin).
- Plant-derived conjugated estrogens: Also available.
- Selective Estrogen Receptor Modulators (SERMs): Bind to estrogen receptors, exert either estrogenic or antiestrogenic effects on target tissues, examples include tamoxifen and raloxifene.
Estrogen Mechanism of Action
- Estrogen diffuses across cell membranes and binds to specific nuclear receptor proteins.
- These receptors regulate gene expression, leading to effects on target tissues like the uterus, breasts, and bone.
Clomiphene (Clomid)
- Partial estrogen agonist, interferes with negative feedback of estrogens on the hypothalamus.
- Increases the secretion of gonadotropin-releasing hormone (GnRH) and gonadotropins (FSH), stimulating ovulation.
- Used to treat infertility associated with anovulatory cycles.
- Adverse effects are dose-related, including headache, nausea, hot flashes, visual disturbances, and ovarian enlargement.
Progestins
- Progesterone: Natural progestin, produced in response to LH, plays a crucial role in preparing the uterus for implantation.
- Synthetic progestins: Often used in oral contraceptives (OCs), derived from 19-nortestosterone, some have androgenic activity due to structural similarity with testosterone.
Progestin Mechanism of Action
- After diffusing across cell membranes, progestins bind to their nuclear receptors.
- This leads to changes in gene expression, affecting various tissues and functions like the uterus, breasts, and metabolism.
Therapeutic Uses of Progestins
- Hormone replacement therapy (HRT): For women undergoing menopause or experiencing hormonal imbalances.
- Contraception: Combined with estrogens in OCs or used sequentially.
- Dysfunctional uterine bleeding: Helps regulate menstrual cycles.
- Dysmenorrhea: Reduces menstrual cramps.
- Endometriosis: Managing pain and symptoms.
Progestins - Adverse Effects
- Headache, depression, weight gain, changes in libido.
- Androgenic progestins can lead to increased LDL/HDL cholesterol ratio, acne, and hirsutism.
- Medroxyprogesterone acetate (Depo-Provera) can increase the risk of osteoporosis.
Mifepristone (RU 486)
- Progesterone antagonist, also has antiglucocorticoid activity.
- Causes abortion by interfering with progesterone, leading to a decline in hCG.
- Major adverse effects include uterine bleeding and incomplete abortions.
- Used for emergency contraception and potentially as an oral contraceptive.
Contraceptives
-
Mechanisms of action:
- Preventing ovulation: Most common pharmacologic intervention.
- Impairing gametogenesis or gamete maturation: Direct impact on egg and sperm development.
- Interfering with gestation: Preventing successful implantation or supporting a pregnancy.
Types of Contraceptives
-
Combined Oral Contraceptives (COCs): Most common, contain estrogen and progestin, taken daily for 21 days followed by 7 days of placebo.
- Monophasic: Constant dose of estrogen and progestin.
- Triphasic: Constant dose of estrogen but increasing doses of progestin over a 3-week period.
- Transdermal Patch: Ethinyl estradiol and norelgestromin, applied weekly.
- Progestin-Only Pills (mini-pill): Less effective than COCs.
- Injectable Progestin: Depo-Provera, administered every 3 months.
- Progestin Implants: Subdermal implant containing etonogestrel, effective for 3 years, reversible by surgical removal.
- Progestin Intrauterine Devices (IUDs): Levonorgestrel-releasing IUD, highly effective, long-term contraception (5 years).
Postcoital Contraception
- Emergency contraception (morning-after pill).
- Reduces pregnancy probability to between 0.2 and 3 percent.
- High doses of progestin (levonorgestrel) or estrogen plus progestin administered within 72 hours of unprotected intercourse.
- Mifepristone can also be used for emergency contraception.
Contraceptives - Adverse Effects
- Most due to estrogen component, but cardiovascular effects are influenced by both estrogen and progestin.
- Breast fullness, depression, fluid retention, headache, nausea, vomiting.
- Benefits include decreased risk of endometrial and ovarian cancers.
- Contraindications: Cerebrovascular and thromboembolic disease, estrogen-dependent neoplasms, liver disease, pregnancy, heavy smokers over 35.
Androgens
- Group of steroids with anabolic and/or masculinizing effects.
- Testosterone: Most important androgen, produced by Leydig cells in the testes.
- Other androgens: DHT, androstenedione, DHEA.
Androgens: Therapeutic Uses
- Hormone replacement therapy (HRT): For men with hypogonadism.
- Hypogonadism: Conditions leading to low testosterone levels.
- Male infertility: Stimulating sperm production.
Androgens: Mechanism of Action
- Testosterone diffuses across cell membranes and binds to androgen receptors.
- This activation of androgen receptors regulates gene expression, leading to male sexual development, muscle growth, and other androgen-dependent functions.
Androgens: Adverse Effects
- Liver problems: Hepatotoxicity, especially with oral administration of alkylated androgens.
- Prostate enlargement: Can exacerbate existing conditions.
- Cardiovascular risks: Increased risk of heart attacks and strokes.
- Other adverse effects: Acne, hair loss, mood changes, aggression.
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Description
Explore the crucial roles of gonadal hormones, including estrogens, in sexual development, reproduction, and hormone therapy. Understand the applications of these hormones in treatments for menopause, contraception, and cancer. Test your knowledge on the different forms of estrogen and their functions.
