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53 Cards in this Set
- Front
- Back
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What drug is a GnRH analog? Mechanism? |
Leuprolide
- When used in pulsatile fashion → agonist - When used in continuous fashion → antagonist (downregulates GnRH receptor in pituitary → ↓ FSH/LH) |
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What is the mechanism of Leuprolide?
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GnRH analog:
- When used in pulsatile fashion → agonist - When used in continuous fashion → antagonist (downregulates GnRH receptor in pituitary → ↓ FSH/LH) |
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What are the clinical uses of Leuprolide? What mechanism of administration should be used for each use?
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- Infertility (pulsatile = agonist)
- Prostate cancer (continuous = antagonist - use with flutamide) - Uterine fibroids (continuous = antagonist) - Precocious puberty (continuous = antagonist) |
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What are the possible side effects of Leuprolide (GnRH analog)?
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- Anti-androgen
- Nausea - Vomiting |
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What are the types of estrogens used in medications? Mechanism?
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- Ethinyl estradiol
- DES - Mestranol *Bind to estrogen receptors |
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What What are the clinical uses of estrogens (ethinyl estradiol, DES, Mestranol)?
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- Hypogonadism or ovarian failure
- Menstrual abnormalities - Hormone Replacement Therapy (HRT) in post-menopausal women - In men with androgen-dependent prostate cancer |
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What are the possible side effects of taking estrogens?
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- ↑ Risk of endometrial cancer, bleeding gin post-menopausal women, clear cell adenocarcinoma of vagina in females exposed to DES in utero
- ↑ Risk of thrombi - Contraindications: ER(+) breast cancer, history of DVTs |
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What drugs are selective estrogen receptor modulators (SERMs)?
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- Clomiphene
- Tamoxifen - Raloxifene |
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What is the mechanism of Clomiphene?
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Selective Estrogen Receptor Modulator (SERM):
- Antagonist at estrogen receptor in hypothalamus - Prevents normal feedback inhibition and ↑ release of LH and FSH from pituitary, which stimulats ovulation |
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What are the uses of Clomiphene?
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Selective Estrogen Receptor Modulator (SERM):
- Used to treat infertility due to anovulation (eg, polycystic ovarian syndrome, PCOS) |
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What are the side effects of Clomiphene?
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Selective Estrogen Receptor Modulator (SERM):
- Hot flashes - Ovarian enlargement - Multiple simultaneous pregnancies - Visual disturbances |
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What is the mechanism of Tamoxifen?
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Selective Estrogen Receptor Modulator (SERM):
- Antagonist on breast tissue - Agonist in uterus and bone |
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What are the uses of Tamoxifen?
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Selective Estrogen Receptor Modulator (SERM):
- Used to treat and prevent recurrence of ER(+) breast cancer because it is an ER antagonist in breast tissue |
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What are the side effects of Tamoxifen?
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Selective Estrogen Receptor Modulator (SERM):
- Endometrial cancer (ER agonist in uterus) - Thromboembolic events |
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What is the mechanism of Raloxifene?
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Selective Estrogen Receptor Modulator (SERM):
- Agonist on bone - Antagonist on uterus |
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What are the uses of Raloxifene?
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Selective Estrogen Receptor Modulator (SERM):
- Used to treat osteoporosis (ER agonist in bone) by ↓ resorption of bone |
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What are the side effects of Raloxifene?
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Selective Estrogen Receptor Modulator (SERM):
- ↑ Risk of thromboembolic events |
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What is Hormone Replacement Therapy (HRT) used for?
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Relief or prevention of menopausal symptoms (eg, hot flashes, vaginal atrophy) and osteoporosis (↑ estrogen, ↓ osteoclast activity)
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What are the possible consequences of Hormone Replacement Therapy (HRT)?
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- Unopposed estrogen replacement therapy ↑ risk of endometrial cancer, so progesterone is added
- Possible increased cardiovascular risk |
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What drugs are aromatase inhibitors used in post-menopausal women with breast cancer?
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- Anastrozole
- Exemestane |
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What is the mechanism and use of Anastrozole and Exemestane?
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- Aromatase inhibitors
- Used in post-menopausal women with breast cancer |
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What is the mechanism and effect of Progestins used in medications?
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- Binds progesterone receptors
- ↓ Growth and ↑ vascularization of endometrium |
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What are the uses of Progestins?
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- Used in oral contraceptives
- Treatment of endometrial cancer - Treatment of abnormal uterine bleeding |
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What drug is used for the termination of pregnancy?
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Mifepristone (RU-486); administered with misoprostol (PGE1)
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What is the mechanism of Mifepristone? Use?
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- Competitive inhibitor of progestins at progesterone receptors
- Used for termination of pregnancy with Misoprostol |
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What is the mechanism of Misoprostol? Use?
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- PGE1 analog
- Used for termination of pregnancy with Mifepristone |
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What is the mechanism of oral contraception (synthetic progestins and estrogen)?
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- Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge
- If no estrogen surge → no LH surge → no ovulation |
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Besides repressing ovulation, how else does progestin in oral contraceptives help to prevent pregnancy?
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- Thickening of cervical mucus, which limits access of sperm to uterus
- Also inhibits endometrial proliferation, thus making endometrium less suitable for the implantation of an embryo |
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What are the contraindications for oral contraceptives?
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- Smokers >35 years old (↑ risk of CV events)
- Patients with history of thromboembolism and stroke - Patients with history of estrogen-dependent tumor |
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What drug decreases contraction frequency in women during labor? Mechanism?
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Terbutaline - β2 agonist
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What is the mechanism and use of Terbutaline?
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- β2 agonist
- Relaxes uterus - Used to ↓ frequency of contractions in women during labor |
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What drug is used for endometriosis and hereditary angioedema? Mechanism?
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Danazol
- Synthetic androgen that acts as a partial agonist at androgen receptors |
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What is the mechanism and use of Danazol?
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- Synthetic androgen that acts as a partial agonist at androgen receptors
- Used for Endometriosis and Hereditary Angioedema |
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What are the side effects of Danazol?
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- Weight gain
- Edema - Acne - Hirsutism - Masculinization - ↓ HDL levels - Hepatotoxicity |
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What drug treats hypogonadism? Mechanism?
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Testosterone, Methyltestosterone
- Agonist at androgen receptors |
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What drug promotes development of 2° sex characteristics? Mechanism?
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Testosterone, Methyltestosterone
- Agonist at androgen receptors |
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What drug stimulates anabolism to promote recovery after burn or injury? Mechanism?
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Testosterone, Methyltestosterone
- Agonist at androgen receptors |
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What are the uses of Testosterone and Methyltestosterone?
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- Hypogonadism
- Promotes development of 2° sex characteristics - Stimulation of anabolism to promote recovery after burn or injury |
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What are the side effects of Testosterone and Methyltestosterone?
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- Causes masculinization in females
- ↓ Intratesticular testosterone in males by inhibiting release of LH (via negative feedback) → gonadal atrophy - Premature closure of epiphyseal plates - ↑ LDL and ↓ HDL |
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What is the effect of 5α-Reductase? What drugs inhibit this enzyme?
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- Inhibits conversion of T → DHT
- Finasteride: 5α-reductase inhibitor |
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What is Finasteride used for?
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- BPH
- Hair growth (male pattern baldness) |
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What are the side effects of Finasteride?
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Gynecomastia
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What drug is used for prostate carcinoma? Mechanism?
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Flutamide
- Non-steroidal competitive inhibitor of androgens at the testosterone receptor |
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What drugs are used to treat polycystic ovarian syndrome to prevent hirsutism?
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- Ketoconazole
- Spironolactone |
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What drug inhibits steroid synthesis? Mechanism? Use?
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Ketoconazole
- Inhibits 17,20-desmolase - Used for polycystic ovarian syndrome to prevent hirsutism |
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What drug inhibits steroid binding and steroid synthesis? Mechanism? Use?
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Spironolactone
- Inhibits steroid binding - Inhibits 17α-hydroxylase - Inhibits 17,20-desmolase - Used for polycystic ovarian syndrome to prevent hirsutism |
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What are the side effects of Ketoconazole and Spironolactone?
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- Gynecomastia
- Amenorrhea |
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What drugs treat BPH? Mechanism?
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- Finasteride: 5α-reductase inhibitor
- Tamsulosin: α1-antagonist |
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What is the mechanism of Tamsulosin? Use?
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- α1-antagonist specific for α1A,D receptors which are found on prostate
- Inhibits smooth muscle relaxation - Used to treat BPH |
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What drugs treat erectile dysfunction?
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- Sildenafil
- Vardenafil |
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What is the mechanism of Sildenafil and Vardenafil?
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- Inhibits phosphodiesterase 5 → ↑ cGMP
- Leads to smooth muscle relaxation in the corpus cavernosum - ↑ Blood flow and penile erection |
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What are the potential side effects of Sildenafil and Vardenafil?
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- Headache
- Flushing - Dyspepsia - Impaired blue-green color vision - Risk of life-threatening hypotension in patients taking nitrates "Hot and sweaty" but then Headache, Heartburn, and Hypotension |
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When is use of Sildenafil and Vardenafil contraindicated? Why?
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In patients who need to take nitrates for angina because this combination can cause life-threatening hypotension
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