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23 Cards in this Set
- Front
- Back
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What is the mechanism of Leuprolide?
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GnRH analog (LEUprolide can be given in LIEU of GnRH)
1. Pulsatile= agonistic 2. Continuous= antagonist |
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What can Leurprolide be used for?
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Infertility if pulsatile,
Prostate cancer if continuous (and w/flutamide). Uterine fibroids |
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Other than nausea and vomiting, what must you watch out for with leuprolide?
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It can have antiandrogenic effects
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Giving exogenous testosterone (methyltestosterone) can cause what s/e?
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1. Masculinized females
2. Inhibits LH--> gonadal atrophy 3. Premature closure of the epiphyseal growth plate in bones. 4. Negative lipid profile: incr LDL, decr HDL |
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What is the MoA of Finasteride?
What can it be used for? |
Also known as Propecia, it is a 5alpha-reductase inhibitor (decreasing concentration of DHT). Used in BPH and also promotes hair growth.
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What is the MoA of Flutamide, and what is it used for?
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Nonsteroidal competitive inhibitor of androgens at the testosterone-R.
Tx: Prostate Cancer |
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What is the difference in the MoA between ketoconazole and spironolactone? What do they treat?
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Ketoconazole inhibits steroid synthesis (via inhibiting desmolase).
Spironolactone inhibits steroid binding. Both tx PCOS and hirsutism, but can result in gynecomastia and amenorrhea. |
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Estrogens (ethinyl estradiol, DES, mestranol) bind to estrogen-R. What can they be used for?
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1. Hypogonadism, or ovarian failure
2. Menstrual abnormalities 3. HRT in postmenopausal women 4. Androgen-dependent prostate cancer |
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What toxicities for estrogens carry?
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1. Risk of endometrial cancer
2. Bleeding in post-menopausal women 3. Clear cell adenocarcinoma of the vagina in women exposed to DES in utero 4. Risk of thrombi |
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Who shouldn't receive estrogen replacement?
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ER-positive Breast Cancer patients, and women with a history of DVT.
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What are the three Slective Estrogen Receptor Modulators (SERMs)?
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Clomiphene, Tamoxifen, and Raloxifene
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How does Clomiphene work?
What does it treat (2)? |
Partial agonist at estrogen-Rs in Hypothalamus, preventing feedback inhibition--> increased relased of LH and FSH from pituitary--> stimulates ovulation.
Tx: infertility and PCOS |
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What s/e are associated with Clomiphene?
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Hot flashes, ovarian enlargement, multiple simultaneous pregancies, visual disturbances.
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How does Tamoxifen work? What do we use it to treat (1)?
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Estrogen-R Antagonist on breast tissue.
Treat and prevent recurrence of ER-positive Breast cancer. "Tam-y's Boobs" |
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How does Raloxifene work? What do we use it to treat (1)?
hint: Ral-B-oxifene |
Estrogen-R Agonist on Bone, reducing resorption of bone.
Tx: osteoporosis |
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What risk is increased with unopposed estrogen therapy (hormone replacement therapy, or HRT)? What do we add to the therapy?
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Increased risk of endometrial cancer.
Progesterone is added. |
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Anastrazole and exemestane inhibit aromatase. Which patients are these drugs used in?
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Postmenopausal women with breast cancer.
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How do progestins work? What are they used for (3)?
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Bind Progesterone-Rs , reduce growth, and increase vascularization of the endometrium.
1. Used in Oral contraceptives 2. Tx of endometrial cancer 3. Abnormal uterine bleeding |
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How does Mifepristone (RU-486) work?
What do we use it for? What s/e are associated? |
Competitive inhibitor of progestins at progesterone-Rs.
Termination of pregnancy, administered with misoprostol (PGE1) S/E: Heavy bleeding, GI effects (n&v, anorexia), abdominal pain |
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How does Dinoprostone induce labor?
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It is a PGE2 analog that causes cervical dilation and uterine contractions, resulting in labor.
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How does Ritodrine/terbutaline work and what is it used for?
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Beta2-agonists that relax the uterus; reduce premature uterine contractions. This prevents an early delivery.
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How does Tamsulosin work and what is it used for?
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alpha1-antagonist used to tx BPH by inhibiting smooth muscle contraction
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How does Sildenafil and Vardenafil work?
What do they tx? Toxicity? |
MoA: inhibit cGMP phosphodiesterase--> increase cGMP--> smooth muscle relaxation in corpus cavernosum, increasing blood flow--> erection. (tx ED)
Toxicity: Dyspepsia, impaired blue-green color vision, life-threatening hypotension in patients taking nitrates. Headaches, flushing |
