Repro_Pharm Flashcards
Leuprolide- MOA?
GnRH analog w/ agonist properties when used in pulsatile fashion
- antagonist properties when used in continuous fashion (downregulates GnRH receptor in pituitary –> dec’d FSH/LH)
“LEUprolide can be used in LIEU of GnRH”
Leuprolide- Clinical uses?
- Infertility (pulsatile)
- Prostate cancer (continuous w/ Flutamide)
- Uterine fibroids (continuous)
- Precocious puberty (continuous)
Leuprolide- Toxicity?
- Anti-androgen
- Nausea
- Vomiting
Testosterone- MOA?
Agonist @ androgen receptors
Testosterone- Clinical uses?
- Treats hypogonadism & promotes development of secondary sex characteristics
- Stimulation of anabolism to promote recovery after burn or injury
Testosterone- Toxicity?
- Causes masculinization in females
- Reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy
- Premature closure of epiphyseal plates
- Inc’d LDL, dec’d HDL
Methyltestosterone- MOA?
Agonist @ androgen receptors
Methyltestosterone- Clinical uses?
- Treats hypogonadism & promotes development of secondary sex characteristics
- Stimulation of anabolism to promote recovery after burn or injury
Methyltestosterone- Toxicity?
- Causes masculinization in females
- Reduces intratesticular testosterone in males by inhibiting release of LH (via negative feedback), leading to gonadal atrophy
- Premature closure of epiphyseal plates
- Inc’d LDL, dec’d HDL
5-alpha-reductase: function?
Converts Testosterone –> DHT (more potent)
Finasteride- MOA?
5-alpha-reductase inhibitor (dec’d conversion of Testosterone to DHT)
Finasteride- Clinical uses?
- BPH
- Promotes hair growth – used to treat male-pattern baldness
(to prevent male-pattern baldness, give a drug that will encourage female breast growth)
Flutamide- MOA?
A non-steroidal competitive inhibitor of androgens @ the Testosterone receptor
Flutamide- Clinical uses?
Prostate Carcinoma
Ketoconazole- MOA?
Inhibits steroid synthesis (inhibitrs 17,20-desmolase)
Ketoconazole- Clinical uses?
Polycystic Ovarian Syndrome (to prevent hirsutism)
Ketoconazole- Side effects?
Gynecomastia & amenorrhea
Spironolactone- MOA?
Inhibits steroid binding
Spironolactone- Clinical uses?
Polycystic Ovarian Syndrome (to prevent hirsutism)
Spironolactone- Side effects?
Gynecomastia & amenorrhea
Ethinyl Estradiol- MOA?
(Estrogen)
Binds estrogen receptors
Ethinyl Estradiol- Clinical uses?
Women:
- Hypogonadism or ovarian failure
- Menstrual abnormalities
- HRT in postmenopausal women
Men:
- Androgen-dependent prostate cancer
Ethinyl Estradiol- Toxicity?
- Inc’d risk of endometrial cancer
- Bleeding in postmenopausal women
- Inc’d risk of thrombi
Ethinyl Estradiol- Contraindications?
- ER-positive breast cancer
- History of DVTs
DES- MOA?
(Estrogen)
Binds estrogen receptors
DES- Clinical uses?
Women:
- Hypogonadism or ovarian failure
- Menstrual abnormalities
- HRT in postmenopausal women
Men:
- Androgen-dependent prostate cancer
DES- Toxicity?
- Inc’d risk of endometrial cancer
- Bleeding in postmenopausal women
- Clear cell adenocarcinoma of vagina if exposed in-utero
- Inc’d risk of thrombi
DES- Contraindications?
- ER-positive breast cancer
- History of DVTs
Mestranol- MOA?
(Estrogen)
Binds estrogen receptors
Mestranol- Clinical uses?
Women:
- Hypogonadism or ovarian failure
- Menstrual abnormalities
- HRT in postmenopausal women
Men:
- Androgen-dependent prostate cancer
Mestranol- Toxicity?
- Inc’d risk of endometrial cancer
- Bleeding in postmenopausal women
- Inc’d risk of thrombi
Mestranol- Contraindications?
- ER-positive breast cancer
- History of DVTs
Clomiphene- MOA?
Selective Estrogen Receptor Modulator (SERM)
- Partial agonist @ estrogen receptors in hypothalamus
- Prevents normal feedback inhibition & increases release of LH & FSH from pituitary, which stimulates ovulation
Clomiphene- Clinical uses?
- Infertility
- Polycystic Ovarian Syndrome
Clomiphene- Adverse effects?
- Hot flashes
- Ovarian enlargement
- Multiple, simultaneous pregnancies
- Visual disturbances
Tamoxifen- MOA?
Selective Estrogen Receptor Modulator (SERM)
- Antagonist on breast tissue
Tamoxifen- Clinical uses?
Used to treat & prevent recurrence of ER-positive breast cancer
Raloxifene- MOA?
Selective Estrogen Receptor Modulator (SERM)
- Agonist on bone, CV system, & blood lipoproteins (reduces resorption of bone)
- Antagonist in breast & uterus
Raloxifene- Clinical uses?
Used to treat Osteoporosis
also decreases risk of both breast & uterine cancer
Hormone Replacement Therapy –
a) What is it used for?
b) What are its components?
c) Potential AEs?
a) Used for relief or prevention of menopausal symptoms (e.g. hot flashes, vaginal atrophy) & osteoporosis ( ↑estrogen, ↓osteoclast activity)
b) Unopposed estrogen replacement therapy (ERT) ↑the risk of endometrial cancer, so progesterone is added
c) Possible ↑CV risk
Anastrozole - MOA?
Aromatase inhibitor
Anastrozole - Clinical uses?
Used in postmenopausal women w/ breast cancer
Exemestane - MOA?
Aromatase inhibitor
Exemestane - Clinical uses?
Used in postmenopausal women w/ breast cancer
Progestins - MOA?
Bind progesterone receptors, reduce growth & ↑ vascularization of endometrium
Progestins - Clinical uses?
- Oral contraceptives
- Tx of endometrial cancer & abnormal uterine bleeding
Mifepristone (RU-486) - MOA?
Competitive inhibitor of progestins @ progesterone receptor
Mifepristone - Clinical uses?
Termination of pregnancy
– Administered w/ Misoprostol (PGE1)
Mifepristone - Toxicity?
- Heavy bleeding
- GI effects (nausea, vomiting, anorexia)
- Abdominal pain
Terbutaline - MOA?
B2-agonist that relaxes the uterus
Terbutaline - Clinical uses?
Reduces premature uterine contractions
Tamsulosin - MOA?
α-1 antagonist
- selective for α-1A,D receptors (found on prostate) & vascular α-1B receptors
Tamsulosin- Clinical uses?
Used to treat BPH by inhibiting smooth muscle contraction
Sildenafil - MOA?
Inhibits phosphodiesterase 5, causing ↑cGMP, smooth muscle relaxation in the corpus cavernous, ↑blood flow, & penile erection
Sildenafil - Clinical uses?
Treatment of erectile dysfunction
Vardenafil - MOA?
Inhibits phosphodiesterase 5, causing ↑cGMP, smooth muscle relaxation in the corpus cavernous, ↑blood flow, & penile erection
Vardenafil - Clinical uses?
Treatment of erectile dysfunction
Sildenafil - Toxicity?
- Headache
- Flushing
- Dyspepsia
- Impaired blue-green color vision
- Risk of life-threatening hypotension in patients taking nitrates
” Hot & Sweaty,” but then Headache, Heartburn, & Hypotension
Vardenafil - Toxicity?
- Headache
- Flushing
- Dyspepsia
- Impaired blue-green color vision
- Risk of life-threatening hypotension in patients taking nitrates
” Hot & Sweaty,” but then Headache, Heartburn, & Hypotension
Danazol - MOA?
Synthetic androgen that acts as a partial agonist @ androgen receptors
Danazol - Clinical uses?
Endometriosis & hereditary angioedema
Danazol - Toxicity?
- Weight gain
- Edema
- Acne
- Hirsutism
- Masculinization
- ↓HDL levels
- Hepatotoxicity
Medroxyprogesterone - Clinical uses?
- Reduces the incidence of endometrial hyperplasia & the risk of endometrial carcinoma in postmenopausal women on estrogen replacement therapy
- Also used parentally as long-acting contraceptive
Medroxyprogesterone - AEs of prolonged use?
Decreased bone mineral density in women of all ages
