Fitzy Specifics Flashcards
Goserelin and Leuprolide MOA and use?
GnRH agonist for lowering T and Estrogen
Major SE of GnRH agonists?
Flare
- Bone Pain
- Prostatic Hypertrophy – Urethral obstruction
- FATAL spinal cord compressiomn
Delayed SE of GnRH agonists?
Low T/E
Impotence
Osteoporosis
Hot Flashes (E)
Degralix MOA and use?
GnRH antagonist for Prostate Cancer
Problem with Degralix duration?
Short duration with cost and compliance issues
Degralix SE?
HISTAMINE (Rash, anaphylaxis, hypotnesion)
Dutasteride and Finasteride MOA?
5-a-reductase inhibitors
Major Toxicity of 5-a-reductase inhibitors?
TERATOGENIC even if wife handles the pill
Abraterone Acetate MOA and use?
CYP17 inhibitor for Castration-resistant prostate cancer
Aminoglutethimide MOA?
NON-STEROIDAL
Inhibits Aromatase
Inhibits conversion of cholesterol –> Pregnenolone
Aminoglutethimide SE?
Acute = Nausea, fever, fatigue Chronic = Adrenal insufficiency, Myelosuppresion
3rd gen aromatase inhibitors?
Exematide (Steroidal)
Anastrozole (Non-steroidal)
Letrozole
1st line TX for ER+ breast cancer?
Aromatase inhibitors
SE of aromatase inhibitors?
Good effect?
Acute = headache, nausea
Polyarthralgia, osteoporosis
Lowers LDL and raises HDL
Aromatase main effect in Pre-menopausal women?
T –> Estradiol in OVARIES
Aromatase main effect in Post=menopausal women?
Androstene –> Estrone in ADIPOSE
Bicalutamide and Flutamide MOA?
Inhibit Androgen receptor translocation to cell surface
Use of biclutamide/flutamide?
Prevent flare during GnRH analog administration
Delayed tox of biclutamide/flutamide?
LIVER TOX
gynecomastia
Decreased T
Hydroxyprogesterone
Medroxyprogesterone
Megestrol
MOA?
Progesterone R antagonists
Uses of Progesterone R antagonists?
2nd line for ER+ breast cancer
Endometrial cancer
SERMs (3)?
Tamoxifen
Toremifine
Raloxifene
SERD?
Fulvistrant
SERM agonist in bone and uterus?
Tamoxifen
SERM agonist in uterus, no bone effect?
Toremifene
SERM agonist in bone, antagonist in uterus?
Raloxifene
SERD antagonist in uterus and bone?
Raloxifene
Which SERM increases risk of endometrial cancer?
Tamoxifen
Which SERM is used as a 2nd line ER+ breast cancer tx?
Tamoxifen
Which SERM is used for prevention if DCIS?
Tamoxifen
Which estrogen modulators are administered orall?
Tamoxifen
Toremifene
Raloxifene
Which estrogen modulator is administered IM injection?
Fulvestrant
SE of all estrogen modulators?
Hot flashes nausea vomiting dysmennorhea Vaginal Bleed Dermatitis
Specific fulvestrant SE?
GI symptoms
Headache
Back Pain
Pharyngitis
Peak conc of SERMs?
4-7 hrs (Faster)
PEak conc of SERD?
7 days (Slower)