B14-4 Androgens, Estrogens, Progestins Flashcards
What is estrogen used for? Side effects? Contraindications?
- postmenopausal symptoms, contraception
- Nausea, breast tenderness, migraines, fluid retention
- HTN, thromboembolism, breast and/or endometrial cancer (give w/ progestogen)
Name the 3 SERM’s, what they’re typically used for, and unique side effects for each one
- Tamoxifen: used for Breast cancer, can cause Endometrial Hyperplasia and thromboembolism
- Raloxifine: used for Osteoporosis, can cause thromboembolism
- Clomiphene: used for infertility, induces ovulation, can cause ovarian cysts/enlargement/multiple gestation
Name a full estrogen receptor antagonist. What is it used for? Side effects?
- Fulvestrant
- Hormone responsive (HR) breast cancer
- Nausea & liver toxicity
Name the two nonsteroidal Aromatase Inhibitors
Anastrozole & Letrozole
Name the steroidal Aromatase Inhibitor
Exemestane
What are Aromatase Inhibitors used for? Side effects?
- Breast cancer (tamoxifen resistant) & Infertility (2nd line Tx after clomiphene)
- nausea and hot flashes
Name the 1st line of Tx for infertility. What kind of drug? Side effects?
- Clomiphene
- SERM
- nausea, hot flashes & ovarian cysts
1st line of Tx for breast cancer? What kind of drug? Side effects?
- Tamoxifen
- SERM
- thromboembolism & endometrial hyperplasia
This SERM is a good alternative, or 2nd line, Tx for Osteoporosis behind Alendronate. What are its side effects?
- Raloxifene
- Hot flashes & thromboembolism
What kind of drug is Danazol? What is it used for? Side effects?
- estrogen synthesis inhibitor
- Tx for Endometriosis
- hepatotoxicity, thromboembolism, intracranial HTN
What kind of drug is Ketoconazole? How does it work? What is it used for? Side effects?
- Gonadal & adrenal hormone synthesis blocker
- Cushings, prostate cancer, antifungal
- Hepatotoxicity, QT prolongation, diabetes insipidus
What are progestogens used for?
- contraceptives, either alone or in combination w/ estrogen
- Hormone Replacement Therapy (HRT) in combination w/ estrogen to prevent estrogen-induced endometrial cancer
Which progestogens are more likely to cause androgenic effects like acne & hirsutism?
1st Gen: Norethindrone
2nd Gen: Levonorgestrel
Which progestogen is K+ sparring? Which gen is this drug?
- Drospirenone
- 4th gen
What kind of drug is Mifepristone? What is it used for? Side effects?
- Antagonist of progesterone & glucocorticoid receptors
- Used for Abortion in early pregnancy (up to 49 days after the last menstraul period)
- can cause refractory Cushing’s syndrome due to the antagonistic affect on glucocorticoid receptors
- can cause uterine bleeding & bacterial infections
What kind of drug is Ulipristal? What is it used for?
- Partial Progesterone agonist and weak glucocorticoid antagonist
- emergency contraceptive for up to 5 days
What are androgens used for? Side effects?
- hypogonadism, chronic wasting associated with HIV & cancer, or to increase body mass/strength/endurance in athletes
- Can cause virilization (hirsutism, alopecia, deep voice, acne) in women and feminization (at high doses) in men
- Can cause liver failure, elevated LDL and decreased HDL, HTN
Name the two 5a-reductase inhibitors. What kind of drugs are these? What are they used for? Side effects?
- Finasteride and Dutasteride
- Antiandrogens
- “Finna end this BPH, Du end this BPH, so my ascanride”
- Alopecia & decreased libido/ejaculation
Name two androgen receptor blockers. What are they used for? Side effects?
- “men that play the flut have no androgens and are bi-, so they probably have prostate cancer and liver toxicity but no libido”
- Flutamide and Bicalutamide
- Prostate cancer
- decreased libido and Hepatotoxicity
Name the first line ED medication, what kind of drug it is, and any potential side effects
- Sildenafil: PGE5i analog, can cause low BP (so do NOT take with nitroglycerine or other vasodilators), blurred vision (and/or blue tinted vision- Cyanopsia)
Name the 2nd line medication for ED, what kind of drug it is, and any potential side effects
- Alprostadil: PGE1 analog, Priapism (long-lasting erections), localized pain and/or burning
What class of drugs is the 1st line treatment for BPH? Name the two drugs
- “sil-y tam-y is l-osin those alphas”
- Alpha-1 Blockers
- Silodosin and Tamsulosin
