Gonadal Hormones Flashcards
Ethinyl estradiol + L-Norgestrel is an example of what?
Prototype contraceptive.
Norethindrone is an example of what?
Prototype contraceptive.
Etonogestrel is an example of what?
Prototype contraceptive.
What are the therapeutic uses of estrogen and progestin preparations?
Replacement therapy, contraception, ovarian suppression, dysmenorrhea, endometriosis, hirsutism, bleeding disorders.
What are the adverse rxns of estrogen/progestin preparations?
Nausea, breast tenderness, hyper pigmentation, increase inf blood glucose, venous thromboembolic disorders, gallbladder disease, edema, headaches, hypertension. Increase in endometrial, ovarian, breast, and uterine cancers. Increase in heart disease, heart attacks, MI, strokes. Abnormal uterine bleeding, hypertension, weight gain, acne, hirsutism.
If they are used as oral contraceptives, what are the adverse effects?
No increase in MI/ stroke. Increase in venous thromboembolism, cervical cancer. Very small increase in breast cancer. Decrease in endometrial/ovarian cancer.
When used as HRT, what are the adverse effects?
Increase CV events, breast cancer, stroke, pulmonary emboli, and venous thromboembolism.
What are the 3 selective estrogen receptor modulators (SERMs)?
Tamoxifen, Clomiphene, Raloxifene,
What is the mechanism of action of Tamoxifen?
It is a competitive estrogen antagonist.
What is the mechanism of action of Clomiphene?
It is a SERM. Induces ovulation.
What is the mechanism of action Raloxifene?
It is a SERM. Mimics estrogen action in bone. Anti-estrogen action in uterus and breast.
What are the two estrogenic inhibitors?
Fluvestrant and Exemestane.
What is the mechanism of action of Fluvestrant?
It is a selective estrogen receptor down regulator (SERD). Accelerates the proteasomal degradation of the estrogen receptor.
What is Fluvestrant used to treat?
Metastatic breast cancer.
What is the mechanism of action of Exemestane?
It is an aromatase inhibitor.
What is Exemestane used to treat?
Post-menopausal women.
What is Mifepristone?
It is a progesterone receptor antagonist.
What is Mifepristone used for?
It is an abortifacient in the first months of pregnancy. Also used as an emergency contraceptive.
What are the biological effects of testosterone/
Growth/development; Muscular and skeletal development; Linear bone growth; Increase in RBC production.
What is testosterone usually converted to?
5-alpha-DHT.
What are the therapeutic uses of andogrens?
Hypogonadism, anabolic effects, refractory anemia, endometriosis.
What are the preparations of androgen?
Testosterone, Methytestosterone, Fluoxymesterone, Nandrolone, Oxandrolone.
What are the adverse reactions of androgens?
Masculinization, prostatic hypertrophy, edema, hypertension, CV disease, cholestatic jaundice, premature epiphyseal closure, liver dysfunction, CNS excitation.
What are the 3 anti androgens?
Leuprolide, Flutamide, and Finasteride.