Term
| Give me a brief summary of the menstrual cycle in 20 words or less. |
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Definition
| Follicle in ovary matures and secretes increasing amount of estrogen --> releases ovum --> follicle transforms into corpus luteum --> secretes progesterone |
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Term
| What are the plasma proteins that bind to Estrogen and Progesterone? |
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Definition
Estrogen - SHBG (Sex Hormine Binding Globuliln) and Albumin
Progesterone - Transcortin |
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Term
| What causes the side effects of steroid hormones when used in large amounts? |
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Definition
Crossreactivity with receptors for other hormones
Ex - Progesterone may have weak androgenic and glucocorticoid effects |
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Term
| What are the effects of Estrogens on Cholesterol? |
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Definition
Increase HDL
Lower LDL
(this is why less CHD in pre-menopausal women) |
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Term
| What are the effects of Estrogens on bone? |
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Definition
Closes epiphyseal plates
Antagonizes bone resorption (decreases osteoclast activity)
Shapes pelvis |
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Term
| What are the effects of Estrogens on tumors? |
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Definition
Stimulates progression of endometrial and breast tumors
Useful in treating prostate tumors |
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Term
| Progesterone is a precursor for what? |
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Definition
Estrogens
Androgens
Adrenocortical Steroids |
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Term
| What are the actions of Progesterones during pregnancy? |
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Definition
Inhibits uterine contraction
Maintains pregnancy |
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Term
| What are the actions of Progesterones in carbohydrate metabolism? |
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Definition
Increases insulin levels
Promotes glycogen storage |
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Term
| What are the effects of Progesterones on cholesterol? |
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Definition
Decreases HDL
Increases LDL |
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Term
| What synthetic estrogen is used for oral contraception? |
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Definition
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Term
| What are the SERMS (Selective Estrogen Receptor Modulators)? |
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Definition
Tamoxifen, Raloxifene
Tissue selective
Treatment of Breast Cancer
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Term
Should Estrogens, Progestins, or both be used in the following treatments?
Menopause
Osteoporisis
Ovarian Failure
Irregular menstrual cycle
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Definition
Menopause - estrogen
Osteoporisis - estrogen
Ovarian Failure - both
Irregular menstrual cycle - progestin |
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Term
| What two drugs are used to induce Ovulation (infertility treatment)? |
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Definition
Clominphene and Fulvestrant
(estrogen antagonists) |
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Term
| What are the 2 Estrogen antagonists and what is their mechanism? |
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Definition
Clomiphene and Fulvestrant
Antagonists in all tissues (ERα and ERβ)
Block feedback inhibition of estrogen in the hypothalamus --> stimulates GnRH release --> stimulates LH and FSH release --> increased Estrogen and Progesterone secretion
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Term
| What is the Aromatase Inhibitors and what is its mechanism? |
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Definition
Anastrozole
Aromatase - CYTP450 enzyme for conversion of androgen to estrogen
Breast cancer treatment if Tamoxifen fails
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Term
| What drugs should be used to treat Breast Cancer if Tamoxifen fails? |
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Definition
Aromatase Inhibitors
(Anastrozole)
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Term
| What classes of drugs should be used to treat Breast Cancer? Endometrial Cancer? Prostate cancer? |
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Definition
Breast Cancer
SERMs - Tamoxifen, Raloxifene
Aromatase Inhibitors - Anastrozole
(if Tamoxifen fails)
Endometrial Cancer
Progestins - Norethindrone
Anti-Estrogens - Clominphene, Fulvestrant
Prostate Cancer
Androgen Antagonists - Flutamide
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Term
| What are some side effects of Estrogen Therapy? |
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Definition
Stroke (Increased clotting factors)
Menstrual disorders
Breast pain
Hypertension
Endometrial cancer
Decreased lactation |
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Term
| What are the relationships between Estrogens and Progestins and CHD? |
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Definition
Estrogens - decrease risk
Progestins - increase risk |
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Term
| What is the Progestin (estrogen precursors)? |
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Definition
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Term
| What is the "morning after" contraceptive? |
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Definition
| Mifepristone (anti-progestin) |
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Term
| What is the two Anti-Progestin? |
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Definition
Mifepristone
Used as contragestation drugs
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Term
| What are the three mechanism of Testosterone action? |
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Definition
1) Binds Androgen Receptor - causes DNA response element to cause tissue dependent transcription activation or repression
2) Converted to 5α-Dihydrotestosterone (DHT) - more potent than testosterone and binds androgen receptors 10x tighter
3) Converted to Estradiol - binds estrogen receptor |
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Term
| What 3 organs produce Testosterone? |
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Definition
Testis
Ovaries
Adrenal Glands |
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Term
| What is the short acting Testosterone deriviative? |
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Definition
Methyltestosterone (oral)
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Term
| What is the long acting Testosterone deriviatives? |
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Definition
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Term
| What is the oral testosterone derivatives? |
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Definition
Methyltestosterone
(short acting)
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Term
| What Synthetic Testosterone is used to treat Endometriosis? |
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Definition
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Term
| What are side effects of Androgen Supplementation? |
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Definition
Females - Virilizing : facial hair, voice changes
Males - Feminizing - due to testosterone conversion to estradiol
LH and FSH suppresion - small testis, decreased spermatogenesis, decreased testosterone synthesis
CHD - increased LDL and decreased HDL |
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Term
| What are the 2 Androgen Receptor Antagonists? Mechanism? |
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Definition
Cyproterone Acetate
Flutamide
Competes with DHT at androgen receptor, preventing translocation into the nucleus
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Term
| What is Cyproterone Acetate used to treat? |
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Definition
(Androgen Receptor Antagonist - prevents testosterone and DHT binding --> decreased LH release --> decreased testosterone)
Acne
Baldness
Hirsutism
Virilizing Syndrome
Increased libido in sex deviant males |
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Term
| What drug can be used to treat Prostate Cancer? |
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Definition
Androgen Antagonists
Flutamide
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Term
| What drug blocks DHT production? Mechanism? |
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Definition
Finasteride
Antagonizes 5α-Reductase - no conversion of testosterone to DHT
Treat BPH and male pattern baldness
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Term
| What drug can be used to treat Benign Prostatic Hyperplasia and Male Pattern Baldness? |
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Definition
Finasteride
(5A-Reductase Inhibitor)
Teratogenic - shouldn't even be touched if pregnant, can be absorbed by skin
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Term
| What drug can be used to treat Benign Prostatic Hypertrophy? |
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Definition
Finasteride
(5α-Reductase Inhibitor)
Also used to treat male-pattern baldness
Teratogen |
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Term
| What drug is used to decrease libido in sex deviant males? |
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Definition
Cyproterone Acetate
(Androgen Antagonist)
Also used to treat: acne, baldness, and hirsutism
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Term
| What class of drugs thicken the cervical mucus and decrease oviduct motility? |
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Definition
Progestins
(Norethindrone)
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Term
| What drugs act in the hypothalamus to increase LH and FSH? |
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Definition
Estrogen-Antagonists
(Clomiphene and Fulvestrant)
Increase GnRH secretion by blocking feedback inhibition --> induces ovulation (infertility treatment)
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Term
| What does 5α-reductase do? |
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Definition
Conversion of testosterone to DHT
(blocked by Finasteride) |
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Term
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Definition
CYTP450 enzyme that catalyzes estrogen synthesis
(inhibited by Anastrozole) |
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Term
| What is the best form of birth control (other than not doing the deed)? |
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Definition
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