Antineoplastics Flashcards Preview

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Flashcards in Antineoplastics Deck (8)
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1
Q

Goserelin, Leuprolide

A

GnRH analogs –> initially stimulate FSH and LH –> transient rise in steroid synthesis (FLARE)
- long-term continuous administration –> GnRH receptors decrease and desensitized –> decreased FSH and LH secretion
Uses - prostate cancer, premenopausal ER+ breast cancer
Tox - flare, pain, urethral obstruction, spinal cord compression
delayed - decreased testosterone

2
Q

Degarelix

A

GnRH antagonist –> competitive GnRH antagonist –> prevents LH secretion with no initial flare (much faster reduction in testosterone)
Tox - decreased testosterone, promote histamine release

3
Q

Dutasteride, Finasteride

A

5-alpha reductase inhibitors –> competitive inhibitors of 5-alpha reductase (test—->DHT)
Uses - BPH, baldness
Tox - decreased testosterone, and teratogenic

4
Q

Abiraterone Acetate

A

17alpha-hydroxylase inhibitors –> prodrug converted to competitive inhibitor of 17alpha-hydroxylase (pregnenolone –> progesterone) –> blocks ALL androgens
Uses - w/ prednisone –> metastatic castration
Tox - decreased testosterone

5
Q
Irreversible = exemestane
Reversible = aminoglutethimide, anastrozole, letrozole
A

Aromatase inhibitors –> target conversion of testosterone and androstenedione to estradiol
Uses - first line for hormone receptor
- 2nd-line tx when tamoxifen has failed
Tox - Amino = N/V, fever, adrenal insufficiency, myelosuppresion
Ana, letro, exem = nausea, headache, fatigue, polyarthralgia, decreased bone density

6
Q

Bicalutamide, Flutamide, Nilutamide

A

Anti-androgens -> inhibit ligand binding and translocation of androgen receptor to nucleus –> increased release of FSH and LH –> increased testosterone synthesis but blockade of effects
Tox - FLutamide = diarrhea, N/V, decreased testosterone, gynecomastia

7
Q

Raloxifene, Tamoxifen, Toremifene

A

compete with estrogen for binding to estrogen receptor
- antagonist in breast
- absorbed orally, peaks in 4-7 hrs, excreted in stool, no additional benefit after 5 years
Tox - increased risk of endometrial cancer, increased risk of stroke

8
Q

Fulvestrant

A

compete with estrogen for binding to estrogen receptor
- antagonist in breast
- administered intramuscularly in 1 month intervals, peaks at 7 days
Tox - GI, headache, back pain, pharyngitis