week 8- male and female repro

Question 1

What is the MOA of Leuprolide

Answer 1

GnRH analog that acts as an agonist when used in a pulsatile fashion and an antagonist when used in a continuous fashion due to receptor downregulation​.

Question 2

adverse effects of Leuprolide

Answer 2

Hypogonadism, decreased libido, erectile dysfunction, nausea, vomiting​.

11. Crumbling column: 12. Flopped over column: 13. Sweaty dancers: 14. Cracked disco ball: Side effects of GnRH analogs include structural changes (osteoporosis, decreased muscle, increased fat, gynecomastia), sexual changes (loss of libido, erectile dysfunction), hot flashes, fatigue, N/V/D; rarely can cause pituitary apoplexy

Question 3

What are the clinical uses of Leuprolide in its pulsatile vs. continuous administration?

Answer 3

Pulsatile: Used for infertility (stimulates FSH & LH secretion).
Continuous: Used for prostate cancer, uterine fibroids, endometriosis, and precocious puberty​.

4. Rotten apple core: GnRH analogs are used to treat advanced prostate CA and breast CA 5. Crab bra: GnRH analogs are used to treat advanced prostate CA and breast CA 6. Blue & pink shorts: GnRH analogs are used to lower endogenous sex hormone levels in gender transition 7. Boulders: GnRH analogs can decrease size of fibroids (leiomyoma) and decrease the number of endometriosis lesions 8. Splattered paint: GnRH analogs can decrease size of fibroids (leiomyoma) and decrease the number of endometriosis lesions 9. Precocious dancer + Tall platform boots: GnRH analogs can treat precocious puberty; slows the appearance of secondary sex characteristics and allows normal skeletal growth 10. Test-tube glow sticks: GnRH analogs are used in IVF to suppress spontaneous ovulation

Question 4

What is the MOA of Anastrozole

Answer 4

Inhibits the enzyme aromatase, which converts androgens (such as androstenedione and testosterone) into estrogens (estrone and estradiol).
Leads to decreased estrogen levels

12. Anastasia flower: anastrozole1. ♂ trowel + aromatic flower + Estrogrow: estrogens are synthesized from precursor androgens by the aromatase enzyme (CYP19A1); present in fat, liver, muscle and breast tissue of postmenopausal women

Question 5

What is the clinical use of Anastrozole

Answer 5

ER-positive breast cancer in postmenopausal women.
Can be used off-label for conditions requiring estrogen suppression, such as gynecomastia prevention in men undergoing prostate cancer therapy or ENDOMETRIOSIS.

Question 6

What are the adverse effects of Anastrozole

Answer 6

Hot flashes
Osteoporosis (due to reduced estrogen)
Arthralgia (joint pain)
Increased risk of cardiovascular events in some patients.

16. HOT temperature: SERMs and aromatase inhibitors can cause hot flashes; presents as a sudden feeling of warmth over the face, neck, and chest, and profuse sweating 17. Dry cactus flower: SERMs and aromatase inhibitors are associated with vaginal dryness; more common with aromatase inhibitors 18. Sore back: common side effect of aromatase inhibitors are joint, muscle and back soreness 19. Decaying table legs: aromatase inhibitors can ↓ BMD; monitor BMD, supplement vitamin D and calcium

Question 7

What is the mechanism of action of Raloxifene?

Answer 7

Selective Estrogen Receptor Modulator (SERM); acts as an estrogen antagonist in breast and uterus but as an agonist in bone, reducing bone resorption.

5. Silkworms: selective-estrogen receptor modulators (SERMs) compete with estrogen for receptor binding; inhibit tumor growth 6. Uterus terrarium + bone & heart-shaped silk: SERMs have partial agonist activity on bone and lipids → reduces postmenopausal bone loss; produces favorable cholesterol, lipid, and lipoprotein profiles; tamoxifen is also a partial agonist on endometrium

Question 8

What are the clinical uses of Raloxifene?

Answer 8

• Osteoporosis prevention and treatment (reduces vertebral fractures).
• Reduces risk of ER-positive breast cancer (especially in postmenopausal women).

7. Time to Relax: tamoxifen is used for the treatment (and prevention in high-risk people) of estrogen-receptor breast cancer; raloxifene is used for the prevention of invasive breast cancer in high-risk people (and treatment of postmenopausal osteoporosis)

Question 9

What are the major adverse effects of Raloxifene?

Answer 9

• Increased risk of DVT/PE (due to pro-thrombotic effects).
  Hot flashes.
• No increased risk of endometrial cancer (unlike tamoxifen).

10. Muddy, clogged nest: SERMs ↑ risk of thromboembolic events; consider risks and benefits in patients with a Hx of thromboembolic events 20. Nauseated gardener: common side effect of SERMs is nausea

Question 10

What is the primary mechanism of action of Clomiphene?

Answer 10

Clomiphene is a selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in the hypothalamus.
Clomiphene blocks estrogen receptors in the hypothalamus, leading to increased GnRH release, which in turn increases FSH and LH to stimulate ovulation.

Question 11

What are the clinical uses of Clomiphene?

Answer 11

First-line treatment for infertility in PCOS
Ovulation induction in anovulatory women
Off-label use in male infertility (increases FSH & LH)

Question 12

What are the major side effects of Clomiphene?

Answer 12

Multiple pregnancies (twins/triplets)
Ovarian enlargement (risk of ovarian hyperstimulation syndrome)
Hot flashes
Visual disturbances (scintillating scotomas, blurred vision)
Mood swings

Question 13

What is the mechanism of action of Finasteride?

Answer 13

Finasteride is a 5α-reductase inhibitor that prevents the conversion of testosterone to dihydrotestosterone (DHT).

Question 14

What are the clinical uses of Finasteride?

Answer 14

Benign prostatic hyperplasia (BPH) – reduces prostate size
Male pattern baldness (androgenetic alopecia) – promotes hair regrowth

Question 15

What are the major side effects of Finasteride?

Answer 15

Sexual dysfunction (↓ libido, erectile dysfunction, ↓ ejaculate volume)
Gynecomastia (due to increased estrogen/testosterone ratio)
Teratogenicity (contraindicated in pregnancy)

Question 16

What is the mechanism for:
Prazosin, Doxazosin, Terazosin:
and
Tamsulosin*

Answer 16

Prazosin, Doxazosin, Terazosin, Tamsulosin: α1-selective antagonists that inhibit α1-adrenergic receptors, leading to smooth muscle relaxation in the vasculature and urinary tract.
**Tamsulosin: **Selective for α1A/D receptors in the prostate (vs. α1B receptors in blood vessels), reducing smooth muscle tone and improving urine flow​.

28. Opera singer: "-osin" suffix of alpha-1 selective antagonists (e.g. prazosin, terazosin, doxazosin, tamsulosin) 29. Extinguished single alpha candle: alpha-1 receptor antagonist

Question 17

What are the side effects of Prazosin, Doxazosin, Terazosin:
and
Tamsulosin*

Answer 17

First-dose orthostatic hypotension (most prominent in nonselective α1-blockers).
Dizziness, headache.
Reflex tachycardia (due to vasodilation).
Xerostomia (dry mouth)​

26. Tiltable: alpha receptor antagonists can cause orthostatic hypotension (alpha-1 antagonist effect) 27. Heart shaped reflex hammer: alpha blocker induced hypotension causes reflex tachycardia

Question 18

What are the clinical uses for: Prazosin, Doxazosin, Terazosin:
and
Tamsulosin*

Answer 18

Prazosin, Doxazosin, Terazosin:

Benign Prostatic Hyperplasia (BPH) – Relaxes smooth muscle in the bladder neck and prostate.
**Hypertension **(except Tamsulosin) – Causes vasodilation.
Post-Traumatic Stress Disorder (PTSD) (Prazosin) – Reduces nightmares​.
Tamsulosin:

BPH – Selectively relaxes prostatic smooth muscle, improving urine flow without significantly affecting blood pressure​.

30. Banister compressing prostate: alpha-1 antagonists (e.g. terazosin) treat symptoms of BPH (relax smooth muscle in the urethra and prostate) 31. Dilated sleeves: alpha-1 antagonists "-osins" cause vasodilation 32. Praying opera singer: prazosin (alpha-1 antagonist) 33. PTSD dog tags: prazosin can be used to treat PTSD

Question 19

What is the mechanism of action of Oxybutynin, Tolterodine, and Trospium?

Answer 19

muscarinic antagonists that inhibit M3 receptors, leading to relaxation of detrusor smooth muscle and reduced bladder contractions.

21. Ox butler: oxybutynin (M3 muscarinic antagonist) Turtle butler: tolterodine (M3 muscarinic antagonist)

Question 20

What are the clinical uses of Oxybutynin, Tolterodine, and Trospium?

Answer 20

These medications are used to treat overactive bladder (urge urinary incontinence) by reducing bladder spasms and improving urinary control.

22. Turning off bladder: oxybutynin and tolterodine treat incontinence (antagonize M3 receptors → relax smooth muscle in ureters and bladder wall)

Question 21

What are the adverse effects of Oxybutynin, Tolterodine, and Trospium?

Answer 21

Common side effects include anticholinergic effects, such as dry mouth (xerostomia), constipation, blurred vision, drowsiness, tachycardia, and urinary retention.

31. Hot as a hare: antimuscarinics inhibit M3 receptors on sweat glands → decreased sweating → hyperthermia 32. Dry as a cracker: antimuscarinics decrease salivation and lacrimation → dry mouth and eyes 33. Blind as a bat: antimuscarinics cause mydriasis and cycloplegia → blurred vision 34. High-pressure as a kettle: antimuscarinics cause mydriasis → decreased outflow of aqueous humor → acute angle closure glaucoma 35. Mad as a hatter: antimuscarinics cross the BBB and antagonize central M1 receptors → sedation, agitation, hallucination, coma (especially in elderly patients)

Question 22

What is the mechanism of action of Sildenafil, Tadalafil, and Vardenafil?

Answer 22

PDE-5 inhibitors. They inhibit phosphodiesterase-5 (PDE-5), preventing the breakdown of cGMP. This leads to increased cGMP levels, which enhances nitric oxide (NO) activity, causing smooth muscle relaxation, vasodilation, and increased blood flow​.

28. FILL: -fill suffix of phosphodiesterase isoform 5 (PDE-5) inhibitors (e.g. sildenafil, tadalafil) 29. Don't phoster disinterest: phosphodiesterase isoform 5 (PDE-5) inhibitors (e.g. sildenafil tadalafil 30. Grump: PDE-5 inhibitors increase cGMP

Question 23

What are the clinical uses of Sildenafil, Tadalafil, and Vardenafil?

Answer 23

Erectile dysfunction – Enhances blood flow to the corpus cavernosum.
Pulmonary hypertension – Causes pulmonary vasodilation.
Benign prostatic hyperplasia (BPH) – Tadalafil only​.

31. Erect bat: PDE-5 inhibitors (e.g. sildenafil, tadalafil) treat pulmonary hypertension and erectile dysfunction

Question 24

What are the adverse effects of Sildenafil, Tadalafil, and Vardenafil?

Answer 24

Facial flushing
Headache
Dyspepsia (indigestion)
Hypotension (especially with nitrates, which is contraindicated)
“Hot and sweaty” sensation followed by headache and heartburn
**Sildenafil only: **Cyanopia (blue-tinted vision) due to PDE-6 inhibition in the retina​.