Pharmacology-Reproductive Flashcards
Leuprolide: mechanism and action when pulsatile
GnRH analog, agonist when pulsatile
Leuprolide: mechanism and action when continuous
GnRH analog, antagonist when continuous (downregulates GnRH receptor in pituitary leading to decreased FSH and LH)
Leuprolide: use (pulsatile)
infirtility
Leuprolide: use (continuous)
uterine fibroids, precocious puberty, prostate cancer
what must be given with Leuprolide for the treatment of prostate cancer?
flutamide
Leuprolide: toxicity
Antiandrogen, nausea, vomiting
Testosterone, methyltestosterone: mechanism
agonist at androgen receptors
Testosterone, methyltestosterone: use
- treat hypogonadism and promotes secondary sex characteristics
- (+) anabolism to promote recovery after burn or injury!
Testosterone, methyltestosterone: toxicity
- masculinization in females
- reduces intratesticular testosterone in males by (-) Lh release
- gonadal atrophy
- premature closure of epiphyseal plates
Testosterone, methyltestosterone: effect on LDL, HDL
- increased LDL and decreased HDL
Antiandrogens: names
finasteride, flutamide, ketoconazol, spironolactone
What enzyme converts testosterone to DHT
5alpha-reductase
Finasteride: mechanism
5alpha reductase inhibitor
Finasteride: use
- BPH
- promotes hair growth (male pattern baldness)
- (can encourage female breast growth)
Flutamide: mechanism
non-steroidal competitive inhibitor of androgens at Test. receptor
Flutamide: use
prostate carcinoma
Ketoconazole: mechanism
inhibit steroid synthesis
Ketoconazol: what specific enzyme does it inhibit
17-20 desmolase
Spironolactone: mechanism
inhibits steroid binding
Ketoconazol and Spironolactone: use
treatment of polycystic ovarian syndrome to prevent hirsutism
Ketoconazol and spironolactone: side effects
gynecomastia, amenorrhea
Estrogens: names
ethinyl estradoil, DES, mestranol
Estrogens: mechanism
bind to estrogen receptors
Estrogens: use
hypogonadism or ovarian failure
menstrual abnormalities
HRT in postmenopausal women
Estrogen use in men with what?
androgen-dependent prostate cancer
Estrogen: toxicity
- bleeding in post-menopausal women
- increased risk of thrombi
Estrogen: increased risk of what cancers
- endometrial cancer
- clear cell adenoma of vagina in females exposed to DES in utero
Estrogen: contraindications
- ER(+) breast cancer
- history of deep vein thrombosis
Selective estrogen receptor modulators (SERMS) names:
Clomiphene, Tamoxifen, Raloxifen
Clomiphene: mechanism + use
- partial agonist at estrogen receptors in hypothal
- prevents normal feedback inhibition, increases release of LH and FSH (+) ovulation
Clomiphene: uses
infertility and polycystic ovarian syndrome
Clomiphene: side effects
hot flashes, ovarian enlargement, multiple pregnancies, visual disturbances
Tamoxifen: mechanism
estrogen receptor antagonist on breast tissue
Tamoxifen: use
treat and prevent recurrence of ER(+)breast cancer
Raloxifene: mechanism
esterogen receptor agonist on bone
Raloxifene: use
reduce resorption of bone so treat osteoporosis
HRT: use
- relief or prevention of menopausal symptoms + osteoporosis
Why must add progesterone to HRT?
unopposed ERT increases risk of endometrial cancer, so use progesterone too but will increase risk of CV accident
Anastrozole/exemestane: mechanism
aromatase inhibitor
Anastrozole/exemestane: use
postmenopausal women with breast cancer
Progestins: mechanism
bind progesterone receptors, reduce growth and increase vascularization of endometrium
Progestins: use
- oral contraceptives
- endometrial cancer
- abnormal uterine bleeding
Mifepristone: what is code?
RU-486
Mifepristone: mechanism
competitive inhibitor of progestins @ progesterone receptors
Mifepristone: use
- termination of pregnancy
What do you admin w/ Mifepristone?
Misoprostol (PGE1)
Mifepristone: toxicity
Heavy bleeding, GI effects (nausea, vomiting, anorexia), abdominal pain
Oral Contraception (synth progestins + estrogens): mechanism
- (-) LH/FSH surge -> (-) estrogen surge -> no LH surge -> no ovulation
Action of Progestins:
thicken cervical mucus, inhibit endometrial prolif
Oral Contraception: contraindications:
Smokers over 35 (increased risk of cardiovasc events)
Patients w/ history of thrombi, stroke, or estrogen-dependent tumor
Terbutaline: mechanism
B2 agonist that relaxes uterus
Terbutaline: use
reduces premature uterine contractions
Tamsulosin: mechanism
a1 antagonist (a1A,D selective), inhibiting smooth muscle contraction
Tamsulosin: use
treat BPH
Sildenafil, vardenafil: mechanism/use
(-) phosphodiesterase 5, causing increased in cGMP, smooth muscle relaxation in corpus cavernosum, increasing blood flow, leading to penile erection
Sildenafil, vardenafil: toxicity
headache, flushing, dyspepsia, impaired blue-green coloured vision
Sildenafil, vardenafil: what occurs in patients on nitrates?
life-threatening hypotension
Danazol: mechanism
synthetic androgens, act as partial agonist at androgen receptors
Danazol: use
endometriosis
hereditary angioedema
Danazol: toxicity
weight gain, edema, acne, hirsutism, masculinization, hepatotoxicity
Danazol: what effects on HDL?
decrease