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What is the mechanism of action (MOA) of Leuprolide, and what physiological effects does it have at the start of treatment?
What is the mechanism of action (MOA) of Leuprolide, and what physiological effects does it have at the start of treatment?
Leuprolide works as a GnRH analog, leading to an initial surge in gonadotropins, termed the 'start-up flare'. This can have physiological effects such as increased testosterone levels initially, before suppression occurs.
Identify two toxicities associated with Leuprolide.
Identify two toxicities associated with Leuprolide.
Two toxicities associated with Leuprolide are anti-androgenic effects and nausea.
How does blocking phosphodiesterase type 5 (PDE5) affect erectile dysfunction treatment?
How does blocking phosphodiesterase type 5 (PDE5) affect erectile dysfunction treatment?
Blocking PDE5 retains cGMP levels, leading to increased blood flow and smooth muscle relaxation, which helps in achieving an erection.
Mention one contraindication for the use of PDE5 inhibitors.
Mention one contraindication for the use of PDE5 inhibitors.
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What are the potential side effects of hormone replacement therapy (HRT)?
What are the potential side effects of hormone replacement therapy (HRT)?
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How does HRT affect osteoclast activity?
How does HRT affect osteoclast activity?
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What role does the aromatase enzyme play in hormone regulation?
What role does the aromatase enzyme play in hormone regulation?
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What are some vasomotor symptoms associated with HRT?
What are some vasomotor symptoms associated with HRT?
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Study Notes
Pharmacology of the Reproductive System
- Reproductive hormones are controlled by a complex interplay between the hypothalamus, anterior pituitary, and gonads (ovaries and testes).
- The hypothalamus releases GnRH, which stimulates the anterior pituitary to release FSH and LH.
- FSH and LH stimulate the gonads to produce sex hormones (estrogen and testosterone).
- Leuprolide is a GnRH agonist.
- Pulsatile GnRH release is physiologic, continuous release leads to infertility.
- Leuprolide's mechanism of action involves initially stimulating then suppressing GnRH release, causing a temporary increase in hormone levels (a "flare-up").
- Leuprolide is used to treat conditions like prostate cancer, uterine fibroids, and endometriosis.
- Toxicities of Leuprolide include anti-androgenic effects, nausea, and vomiting.
- Flutamide and Bicalutamide and Nilutamide & Spironolactone are competitive receptor antagonists.
- Finasteride inhibits 5α-reductase, preventing the conversion of testosterone to dihydrotestosterone (DHT).
- Androgens, such as testosterone, have anabolic effects (increased lean body mass) and metabolic effects (increased clotting factors, decreased HDL).
- Androgens also play a crucial role in development (male reproductive tract, male sex organs, long bone growth), and maintaining secondary sex characteristics in adulthood.
- Testosterone effects differ in males and females.
- Females should not use testosterone products.
- Tamsulosin is an alpha-antagonist used for benign prostatic hyperplasia (BPH).
- Sildenafil (Viagra), vardenafil, and tadalafil are phosphodiesterase 5 (PDE5) inhibitors that treat erectile dysfunction by increasing blood flow to the penis.
- Side effects of PDE5 inhibitors include headache, hypotension, flushing, and dyspepsia.
- Contraindications for PDE5 inhibitors include nitrate use, which can lead to life-threatening hypotension.
- Minoxidil is a K channel opener used for male-pattern androgenic alopecia.
- Combined oral contraceptives (COCs) use estrogen and progestin to prevent ovulation.
- Progestins have a range of effects, including differentiation of uterine endometrium, suppression of myometrial contractions, maintenance of pregnancy, and prevention of endometrial hyperplasia.
- Mifepristone is a progesterone receptor antagonist used for 1st trimester abortion.
Questions related to hypogonadism and treatment
- A 14-year-old boy's delayed puberty is linked to hypogonadism due to a hypothalamic-pituitary-gonadal axis failure.
- Anemia isn't a typical adverse effect.
- Decreased libido or increased calcium deposition at epiphyseal plates are not typical adverse effects.
- Increased serum HDL cholesterol levels or leukocytosis are not typical adverse effects.
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Description
This quiz covers the pharmacological aspects of reproductive hormones, focusing on the roles of GnRH, FSH, and LH in hormone production within the gonads. It also discusses the mechanisms and clinical applications of GnRH agonists like Leuprolide, along with their toxicities and the effects of related androgen receptor antagonists. Test your understanding of these crucial concepts in reproductive pharmacology.
