repro Flashcards
Leuprolide
- MOA
- Use
- Toxicity
MOA: GnRH analog - pulsatile = agonist - continuous = antagonist -- downregulate GnRH receptor in pituitary --> continuous: initial increase in T + DHT + estrogen followed by decrease, "start up flare" Use: - infertility (pulsatile) - Endometriosis - prostate cancer w/ flutamide (continuous) - uterine fibroids (continuous) - precocious puberty (continuous) Toxicity - antiandrogen - nausea - vomiting
Testosterone
- MOA
- Use
- Toxicity
MOA: agonist at androgen receptors
Use:
- hypogonadism
- promote secondary sex characteristic development
- stimulate anabolism for recovery in burn or injury
Toxicity:
- masculinization in females
- reduces intratesticular testosterone in males causing gonad atrophy (inhibits release of LH via negative feedback)
- Premature closure of epiphyseal plates
- increase LDH, decrease HDL
Methyltestosterone
- MOA
- Use
- Toxicity
MOA: agonist at androgen receptors
Use:
- hypogonadism
- promote secondary sex characteristic development
- stimulate anabolism for recovery in burn or injury
Toxicity:
- masculinization in females
- reduces intratesticular testosterone in males causing gonad atrophy (inhibits release of LH via negative feedback)
- Premature closure of epiphyseal plates
- increase LDH, decrease HDL
Finesteride
- MOA
- Use
- Toxicity
Antiandrogen MOA: - 5-alpha reductase inhibitor - no conversion of T --> DHT Use: - BPH (takes months for gland to decrease in size and symptoms to improve) - male pattern baldness Toxicity - gynecomastia
Flutamide
- MOA
- Use
Antiandrogen MOA: - nonsteroidal competitive inhibitor of androgens at the testosterone receptor Use: - prostate cancer
Ketaconazole
- MOA
- Use
- Toxicity
Antiandrogen MOA: - inhibits steroid synthesis (inhibits 17,20 desmolase) Use: - PCOS - prevent hirsutism Toxicity - gynecomastia - amenorrhea
Spironolactone
- MOA
- Use
- Toxicity
Antiandrogen / K+ sparing diuretic MOA: - inhibits steroid binding to androgen receptor Use: - PCOS - prevent hirsutism Toxicity - gynecomastia - amenorrhea
Ethinyl estradiol
- MOA
- Use
- Toxicity
Estrogen MOA: bind estrogen receptor Use: - hypogonadism - ovarian failure - menstrual abnormalities - HRT postmenopause - PCOS - decrease LH levels - Men = androgen dependent prostate cancer Toxicity: - risk of endometrial cancer - bleeding in postmenopausal women - thrombi Contraindications - estrogen positive breast cancer - DVT history
Magnesium Sulfate
- MOA
- Use
- Toxicity
MOA: block membrane + intracellular calcium channel
Use:
- preeclampsia
- decreases risk of cerebral palsy in infant
DES
- MOA
- Use
- Toxicity
Estrogen MOA: bind estrogen receptor Use: - hypogonadism - ovarian failure - menstrual abnormalities - HRT postmenopause - PCOS - decrease LH levels - Men = androgen dependent prostate cancer Toxicity: - risk of endometrial cancer - bleeding in postmenopausal women - Exposed in utero: clear cell adenocarcinoma of the vagina - thrombi Contraindications - estrogen positive breast cancer - DVT history
Mestranol
- MOA
- Use
- Toxicity
Estrogen MOA: bind estrogen receptor Use: - hypogonadism - ovarian failure - menstrual abnormalities - HRT postmenopause - PCOS - decrease LH level - Men = androgen dependent prostate cancer Toxicity: - risk of endometrial cancer - bleeding in postmenopausal women - thrombi Contraindications - estrogen positive breast cancer - DVT history
Clomiphene
- MOA
- Use
- Toxicity
SERM MOA: partial agonist at estrogen receptors in hypothalamus* - prevents normal feedback inhibition - increases release of LH + FSH - stimulates ovulation Use: - infertility - PCOS - lets you get pregnant Toxicity: - hot flashes - ovarian enlargement - multiple simultaneous pregnancies - visual problems
Tamoxifen
- MOA
- Use
- Toxicity
SERM MOA: - antagonist on breast tissue - agonist in bone - agonist in endometrium Use: - treat + prevent recurrence of ER(+) breast cancer Toxicity - endometrial cancer risk - hot flashes
Raloxifene
- MOA
- Use
- Toxicity
SERM MOA: - agonist on bone - endometrial + breast antagonist Use - osteoporosis
Hormone replacement therapy
Use
- menopausal symptoms (hot flashes, vag atrophy)
- osteoporosis (increased estrogen, decreased osteoclast activity)
Toxicity
- unopposed = increased risk of endometrial cancer
—-> add progesterone
- CV risk
Anastrozole
- MOA
- Use
- Toxicity
MOA: aromatase inhibitors
- no estrogen synthesis from androgenic substrate
Use:
- postmenopausal women with breast cancer
Exemestane
- MOA
- Use
- Toxicity
MOA: aromatase inhibitors
- no estrogen synthesis from androgenic substrate
Use:
- postmenopausal women with breast cancer
Progestins
- MOA
- Use
MOA: bind progesterone receptors - reduce growth of endometrium - increase vascularization of endometrium Use: - oral contraceptives - treat endometrial cancer - abnormal uterine bleeding
Mifepristone (RU-486)
- MOA
- Use
- Toxicity
MOA: competitive inhibitor of progestins at progesterone receptor Use: - terminate pregnancy - give with misoprostol* (PGE1) Toxicity - heavy bleed - GI (n,v,anorexia) - abdominal pain
Oral Contraceptives
- componentes
- MOA
- Contraindications
- Synthetic progestins + estrogen
MOA: - both: inhibit LH/ FSH –> no estrogen surge –> no LH surge (low gonadotropins) –> no ovulation
- Progestin: thickening of cervical mucus (limiting access of sperm to uterus), inhibit endometrial proliferation (less suitable for implantation)
- may prevent ovarian and endometrial cancer
Contraindications - smokers > 35 yoa
- hx of thromoembolism and stroke
- hx of estrogen dependent tumors
Terbutaline
- MOA
- Use
MOA: B2 agonist that relaxes uterus
Use:
- reduce premature uterine contractions
Tamsulosin
- MOA
- Use
- Toxicity
MOA: a1 antagonist
Use:
- BPH symptom relief
– relax smooth muscle in bladder neck, prostate capsule, prostate urethra
– selective for alpha1A,D receptor on prostate
Toxicity
- Orthostatic hypotension
Sildenafil
- MOA
- Use
- Toxicity
MOA: inhibit phosphodiesterase 5 - increase cGMP (inhibit phosphodiesterase- no cGMP breakdown) = decrease intracellular Ca+ = myosin dephosphorylation - smooth muscle relaxation in corpus cavernosum* - increase blood flow - erection Use: erectile dysfunction Toxicity - headache - flushing - dyspepsia - impaired blue green color vision - life threatening hypotension if taking nitrates
Vardenafil
- MOA
- Use
- Toxicity
MOA: inhibit phosphodiesterase 5 - increase cGMP (inhibit phosphodiesterase- no cGMP breakdown) = decrease intracellular Ca+ = myosin dephosphorylation - smooth muscle relaxation in corpus cavernosum - increase blood flow - erection Use: erectile dysfunction Toxicity - headache - flushing - dyspepsia - impaired blue green color vision - life threatening hypotension if taking nitrates
