Pharm: L20: Contraceptives and Sex Hormones Flashcards
(17 cards)
Estrogens
- ESTRADIOL
- Ethinyl Estradiol
- Conjugated Estrogens
- See below on infow
Antiestrogens
- TAMOXIFEN
a. Antagonist
b. Agonist - RALOXIFENE
- CLOMIPHENE
- Selective ESTROGEN receptor Modulartor (SERM)
a. Breast: Used as Prophylactic Tx in BREAST CANCER; Reduces Risk
b. BONE (limit Bone loss); UTERUS (may Increase risk of Uterine Cancer) - Like TAMOXIFEN but an ANTAGONIST in UTERUS: for OSTEOPOROSIS
- SERM; Antagonizes Neg Feedback of ESTROGEN in HYPOTHALAMUS
a. STIMULATES LH & FSH, Inducing Ovulation (Multiple Pregnancies)
Aromatase Inhibitors (estrogen)
- ANASTROZOLE
a. What does it do?
b. Use?
c. Adverse Effects?
- a. Inhibits AROMATASE
b. Advanced Breast Cancer AFTER TAMOXIFEN FAILURE; Breast Cancer in POSTMENOPAUSAL WOMEN
c. MENOPAUSAL SYMPTOMS
Progestins
- PROGESTERONE
a. Regulated by what?
b. Produced by what 2 things?
c. MECHANISM?
d. Biological Functions?
- a. LH
b. CORPUS LUTEUM and Fetal/Placental Unit in Pregnant Women
c. NUCLEAR RECEPTOR, mRNA Synthesis
d. UTERUS: Converts Endometrium to SECRETORY STATE (MAINTAINS PREGNANCY)
ENDOCERVICAL GLANDS: Regulates Cervical Mucus
BREASTS: Development during Pregnancy and Puberty
THERMOGENIC ACTION: Increases Body TEMPERATURE
Progestins: Progesterone Derivatives
- MEDROXYPROGESTERONE
a. What is it?
Varying Levels of ANDROGEN ACTIVITY
Progestins: 19-Nortestosterone Derivatives
- LEVONORGESTREL
* Progestins in General - Uses
- Side Effects
- Both PROGESTIN and ANDROGENIC ACTIVITY
- CONTRACEPTIVES; Prevent ENDOMETRIAL HYPERPLASIA in HRT
- Maybe Increased BP; High Doses can Reduce PLASMA HDL Levels: (19-Nortestosterones); Depression and Drowsiness
Progestins: Anti-Progestins
- MIFEPRISTONE
a. Use
b. Side Effects - DANAZOL
a. Treat what?
b. Side Effects?
- PROGESTERONE/GLUCOCORTICOID RECEPTOR ANTAGONIST
a. TERMINATE PREGNANCY and Prevent Implantation
b. Vomit, Diarrhea, Vaginal Bleeding - Weak Progestin and Androgen
a. ENDOMETRIOSIS
b. Weight Gain, Edema, Acne and Oily Skin, Libido changes
Combo Oral Contraceptives
- DROSPIRENONE/ETHINYL ESTRADIOL
a. Purpose
b. Side Effects?
c. Benefits?
d. Absolute CI
e. Relative CI
- a. Prevent Ovulation; LOW DOSES generally.
* Usually Estrogen/Progestin pills
b. WEIGHT GAIN, Nausea, Edema, Cardiovascular, Migraine, Depression
c. VERY EFFECTIVE BIRTH CONTROL; Decrease OVARIAN and UTERINE CANCERS RISK
d. Thromboembolitits, Thrombophlebitis, Cerebrovascular Disorders
e. LIVER DISEASE
Androgens:
- TESTOSTERONE: What is it?
a. Men
b. Women
- Androgen Receptor Antagonist
a. Testicular Deficiency
b. Female HYPOPITUITARISM (estrogens and Androgens)
Androgens: Anti-Androgens
- FLUTAMIDE
a. Used in what? - SPRIONOLACTONE
a. What is it?
- PROSTATE CANCER w/LONG-ACTING GnRH AGONIST
- HIRSUTISM and PMS in women
a. Mineralocorticoid Antagonist
Androgen: 5a-Reductase Inhibitor
- FINASTERIDE
a. What does it do?
b. Uses
c. What does it do?
- a. Inhibits 5a-RDUCTASE (No DHT)
b. BENIGN PROSTATIC HYPERPLASIA and MALE PATTERN BALNESS
c. TERATOGENIC
Estrogen: Use?
- Synthetic
- Conjugated
- Estradiol
- Oral Contraceptives
- HRT
- Creams/Patchesd
Estrogen Side Effects
Endometrial HYPERPLASIA
Nausea and Breast Tenderness
MIGRAINES!!
THROMBOEMBOLISM; Accelerated BLOOD CLOTTING
Estrogens: CIs
- What are they?
ESTROGEN-DEPENDENT NEOPLASMS; THROMBOEMBOLIC DISORDERS; Smoking; Preggers
Drug Interaction
- What can reduce effectiveness.
- Oral Contraceptives reduce Effectiveness of what 4 things?
- P450 Induces, ANTIBIOTICS
2. Anticoagulants, Anticonvulsants, TCAs, Oral Hypoglycemics
Anabolic Effects of ANDROGENS
Increase Bone Density; AA incorporation into muscle and RBC Mass
Androgens Side Effects
- Men
- Women
- BOTH
- Decreased Spermatogenesis
- Masculinization; Pseudohermaphroditisn of FETUS in Pregnant Women
- OILY SKIN, ACNE; Decreased HDL; Psychological Changes.
