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Questions and Answers
What condition is raloxifene primarily used to treat?
What condition is raloxifene primarily used to treat?
Which statement accurately reflects a side effect of raloxifene?
Which statement accurately reflects a side effect of raloxifene?
What is the initial dosing recommendation for treatment starting on the third or fifth day of the menstrual cycle?
What is the initial dosing recommendation for treatment starting on the third or fifth day of the menstrual cycle?
What is the primary mechanism of action for gonadotropin therapy?
What is the primary mechanism of action for gonadotropin therapy?
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What is a characteristic feature of selective estrogen receptor modulators (SERMs) like raloxifene?
What is a characteristic feature of selective estrogen receptor modulators (SERMs) like raloxifene?
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Which of the following is a consideration for patients using raloxifene?
Which of the following is a consideration for patients using raloxifene?
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Which of the following is listed as an adverse effect of clomiphene therapy?
Which of the following is listed as an adverse effect of clomiphene therapy?
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What is defined as obesity in terms of body mass index (BMI)?
What is defined as obesity in terms of body mass index (BMI)?
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What is a key reason for adding progestogen to estrogen therapy in women with an intact uterus?
What is a key reason for adding progestogen to estrogen therapy in women with an intact uterus?
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Which treatment is the first-line therapy for menstrual abnormalities according to the Endocrine Society?
Which treatment is the first-line therapy for menstrual abnormalities according to the Endocrine Society?
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How long must progestogen be taken to effectively prevent endometrial hyperplasia?
How long must progestogen be taken to effectively prevent endometrial hyperplasia?
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What is metformin's role in the treatment of irregular menses?
What is metformin's role in the treatment of irregular menses?
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In which scenario may pharmacological treatment for obesity be considered?
In which scenario may pharmacological treatment for obesity be considered?
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What is the recommended duration for the use of diethylpropion, phentermine, and phendimetrazine?
What is the recommended duration for the use of diethylpropion, phentermine, and phendimetrazine?
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Which of the following is a common synthetic progestogen used in HRT preparations?
Which of the following is a common synthetic progestogen used in HRT preparations?
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What are the older medications approved for short-term treatment of obesity?
What are the older medications approved for short-term treatment of obesity?
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What potential cardiovascular risk is associated with the use of certain obesity medications?
What potential cardiovascular risk is associated with the use of certain obesity medications?
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Which of the following factors does NOT play a role in obesity?
Which of the following factors does NOT play a role in obesity?
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What is the typical plasma ratio of estradiol to estrone?
What is the typical plasma ratio of estradiol to estrone?
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What underlying condition is primarily associated with the development of polycystic ovary syndrome (PCOS)?
What underlying condition is primarily associated with the development of polycystic ovary syndrome (PCOS)?
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Which route of administration for estrogens in HRT allows for sustained release?
Which route of administration for estrogens in HRT allows for sustained release?
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Which hormone is typically found at normal or low concentrations in individuals with PCOS?
Which hormone is typically found at normal or low concentrations in individuals with PCOS?
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What characteristic is true about progesterone compared to synthetic progestogens?
What characteristic is true about progesterone compared to synthetic progestogens?
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Which of the following is NOT one of the criteria for PCOS according to the 2003 Rotterdam criteria?
Which of the following is NOT one of the criteria for PCOS according to the 2003 Rotterdam criteria?
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What percentage of women is thought to be affected by polycystic ovary syndrome?
What percentage of women is thought to be affected by polycystic ovary syndrome?
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Which of the following is NOT a potential comorbidity associated with PCOS?
Which of the following is NOT a potential comorbidity associated with PCOS?
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According to the 1990 NIH criteria, which condition must be excluded when diagnosing PCOS?
According to the 1990 NIH criteria, which condition must be excluded when diagnosing PCOS?
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Which of the following regarding the duration of action of estrogens is accurate?
Which of the following regarding the duration of action of estrogens is accurate?
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What is a common outcome for weight loss medication once treatment is stopped?
What is a common outcome for weight loss medication once treatment is stopped?
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Which statement about progestogens in HRT is correct?
Which statement about progestogens in HRT is correct?
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What is one of the clinical signs of hyperandrogenism in patients with PCOS?
What is one of the clinical signs of hyperandrogenism in patients with PCOS?
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Which therapy goal aims to reduce the progression to Type 2 Diabetes in patients with PCOS?
Which therapy goal aims to reduce the progression to Type 2 Diabetes in patients with PCOS?
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What limitation is noted regarding the study of concurrent use of obesity medications?
What limitation is noted regarding the study of concurrent use of obesity medications?
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Which nonpharmacologic therapy is considered crucial for overweight or obese patients with PCOS?
Which nonpharmacologic therapy is considered crucial for overweight or obese patients with PCOS?
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What is the mechanism of action of Clomiphene citrate in fertility improvement?
What is the mechanism of action of Clomiphene citrate in fertility improvement?
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What is the LH/FSH ratio indicative of in a patient suspected of having PCOS?
What is the LH/FSH ratio indicative of in a patient suspected of having PCOS?
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Which of the following is a biochemical sign of hyperandrogenism that should not be the sole criterion for diagnosing PCOS?
Which of the following is a biochemical sign of hyperandrogenism that should not be the sole criterion for diagnosing PCOS?
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Study Notes
Estrogens in Hormone Replacement Therapy (HRT)
- Plasma half-lives of natural estrogens are comparable to ovarian-secreted estrogens.
- Synthetic estrogens, like ethinylestradiol, have a longer duration of action than natural estrogens.
- Normal plasma ratio of estradiol to estrone is approximately 1:1 to 2:1.
- Main routes of estrogen administration in HRT are oral, transdermal (patch/gels/cream), subcutaneous (implants), and vaginal (creams/medicated rings).
Progestogen Therapy
- Progestogen is added to estrogen therapy to protect the endometrium from hyperplasia and neoplasia in women with intact uteri.
- Effective endometrial protection requires progestogen use for a minimum of 12 days.
- Required progestogen dose for hyperplasia prevention varies depending on the compound's potency.
- Common progestogens include medroxyprogesterone, dydrogesterone, norethisterone, and levonorgestrel; they are active after oral administration.
- Synthetic progestogens may activate receptors beyond the progesterone receptor, with unpredictable long-term effects.
- Micronised progesterone has better oral bioavailability compared to standard preparations.
Raloxifene
- Raloxifene is a SERM that selectively binds to estrogen receptors and is used to increase bone mineral density.
- It counteracts estrogen effects on breast and endometrial tissues in post-menopausal women.
- Increased risk of thromboembolism is noted, particularly within the first four months of use.
- Not effective for treating vasomotor symptoms in peri-menopausal women and may induce hot flushes.
- Raloxifene neither stimulates the uterine endometrium nor causes uterine bleeding.
Obesity
- Defined as having a BMI of 30 kg/m² or greater, partially stemming from calorie consumption exceeding expenditure.
- Genetics, metabolism, behavior, environment, and socioeconomic factors contribute to obesity.
- Individuals with BMI >30 or >27 with two comorbidities may qualify for pharmacological obesity treatment.
- Obesity drugs are primarily approved for short-term use; some newer options are for long-term management.
- Anorexiants like phentermine and diethylpropion are used short-term (up to 3 months), with caution against abuse potential.
- Common adverse effects of short-term obesity medications include increased blood pressure, heart rate, and risk of dysrhythmias.
Polycystic Ovary Syndrome (PCOS)
- PCOS can cause infertility in up to 20% of infertile couples and is linked to androgen excess or hyperandrogenism.
- Insulin resistance is central to PCOS, leading to ovulatory dysfunction due to increased LH and decreased FSH.
- Affects 6%-10% of women, making it a prevalent endocrine disorder with various potential comorbidities such as T2D and obesity.
Diagnosis
- PCOS diagnosis criteria remain debated; NIH (1990) and Rotterdam (2003) criteria outline hyperandrogenism, irregular ovulation, and exclusion of secondary causes.
- Clinical signs of hyperandrogenism include hirsutism, acne, and pattern alopecia.
- Biochemical indicators include elevated testosterone levels and an LH/FSH ratio exceeding 2.
- Women with obesity may present with prediabetes or T2D.
Therapy Goals
- Aim to normalize ovulatory cycles and menstrual regularity.
- Enhance fertility and manage clinical manifestations of hyperandrogenism.
- Reduce risks of progression to T2D and associated cardiovascular diseases.
Nonpharmacologic Therapy
- Weight loss of 5%-10% is emphasized for overweight or obese PCOS patients.
- Mechanical hair removal is recommended for hirsutism.
Pharmacotherapy
- Clomiphene citrate is first-line for fertility; it induces ovulation by modulating estrogen receptors and is dosed at 50 mg for 5 days.
- Gonadotropins can normalize LH/FSH levels to stimulate ovulation; adverse effects include multiple pregnancies and ovarian hypertrophy.
- Hormonal contraceptives are recommended for menstrual irregularities and hirsutism.
- Metformin may improve metabolic abnormalities, though its role in fertility remains ambiguous.
- Spironolactone can aid in managing hirsutism when combined with hormonal contraceptives.
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Description
This quiz covers key concepts of estrogen administration in hormone replacement therapy (HRT). It discusses the characteristics of naturally occurring estrogens, their plasma half-life, and compares them with synthetic estrogens like ethinylestradiol. Test your knowledge on the various routes of estrogen administration.
