Prostate Drugs Flashcards
Alfuzosin MOA
Short-acting selective Alpha-1 Blocker
Alfuozosin Tox
GI-xerostomia, nausea; CNS- dizziness, somnolence, asthenia, h/a, insomnia
Alfuozosin M&E
CYP3A4; fecal/renal elim
Does alfuozosin need does titration?
No
Tadalafil MOA
PDE-5 Inhibitor: decreases breakdown of cGMP; Relief of BPH occurs via smooth muscle relaxation
Tadalafil Tox
Uncommon; h/a, nausea, indigestion, nasopharyngitis, URTI; more rare-NAION, retinal artery occlusion, hearing loss
Tadalafil M&E
CYP3A4; fecal elim
Tadalafil DDI
Nitrates-profound hypotension exacerbated by alcohol
Saw Palmetto?
useless shit drug
Androgen Receptor Blockers (3)
Bicalutamide, flutamide, nilutamide
Bicalutamide MOA
Androgen Receptor Blocker; Prostate > Central; Antagonist + some agonist activity
Bicalutamide Tox
GI tox, hot flashes, aches/pains
Flutamide MOA
Androgen Receptor Blocker; Prostate; Antagonist
Flutamide Tox
GI tox, hot flashes, aches/pains
AND
Blood Dyscrasia
Flutamide BBW
Hepatotoxicity/Failure
Nilutamide MOA
Androgen Receptor Blocker; prostate & central
Nilutamide Tox
GI tox, hot flashes, aches/pains
AND
HF/ HTN, Blood Dyscrasia; Increased time to accommodate transition from light to dark
Nilutamide BBW
Respiratory insufficiency
Estramustine MOA
Targeted Alkylator; Estradiol w/ Alkylating Moiety which is a MT inhibitor: promotes dis-assembly and G2/M arrest and produces DNA strand breakage
Estramustine Tox
Common: GI upset, gynecomastia, mastalgia, and impotence;
Testosterone levels decreased via negative feedback on HPA;
Due to Estradiol: edema, thromboembolism, MI, PE, stroke;
Elevated hepatic enzymes, hyperbilirubinemia
Estramustine Administration
Oral
GnRH agonists
Goserelin, Histrelin, Leuprolide, Triptorelin
Histrelin Tox
Unique=Seizures & Suicidal Ideation;
Edema, HTN, h/a, fatigue, depression, dec bone mineral density, spinal compression, elevated TG, weight gain, DM, reduced libido, sexual dysfxn, gynecomastia, rarely hepatotox, aches/pains
Goserelin Tox
Edema, HTN, h/a, fatigue, depression, dec bone mineral density, spinal compression, elevated TG, weight gain, DM, reduced libido, sexual dysfxn, gynecomastia, rarely hepatotox, aches/pains
Leuprolide Tox
Unique=MI/HF
Edema, HTN, h/a, fatigue, depression, dec bone mineral density, spinal compression, elevated TG, weight gain, DM, reduced libido, sexual dysfxn, gynecomastia, rarely hepatotox, aches/pains
Triptorelin Tox
Edema, HTN, h/a, fatigue, depression, dec bone mineral density, spinal compression, elevated TG, weight gain, DM, reduced libido, sexual dysfxn, gynecomastia, rarely hepatotox, aches/pains
Pregnancy Categories of GnRH agonists
Cat X
Goserelin Admin
SC; Initial transient dz flare avoided by 2-4 wks of AR blockers
Histrelin Admin
SC; Initial transient dz flare avoided by 2-4 wks of AR blockers
Leuprolide Admin
IM/SC; Initial transient dz flare avoided by 2-4 wks of AR blockers
Triptorelin Admin
IM; Initial transient dz flare avoided by 2-4 wks of AR blockers
Degarelix MOA
GnRH Antagonist; Reduced LH & FSH secretion; castrate testosterone levels w/in 3 days (quicker than GnRH Agonists)
Degarelix Tox
Hot sweats, injxn site rxns, weight gain, HTN, arthralgia, chills, fatigue, impotence, elevated hepatic enzyme levels (reversible), QT prolongation
Degarelix Admin
SC; Avoids initial dz flare
Abiraterone MOA
17-Alpha-Reductase Inhibitor
Abiraterone Tox
Produce hypermineralocorticoid state: HTN, hypokalemia, and fluid retention, caution w/ pre-existing CV issues; elevated hepatic enzymes; routine LFT’s required
Abiraterone Pregnancy Cat
Cat X: women cannot handle drug, condom should be used if partner is pregnant
Adjuvant tx with abiraterone
Tx in combo w/ corticosteroid to avoid hypermineralocorticoid state
Sipuleucel-T MOA
Individualized immunotherapy to stimulate T cell immunity against Prostatic Acid Phosphatase (PAP)
Sipuleucel-T Tox
Mild infusion rxns; fever/chills/dyspnea; N/V; paresthesias, citrate tox, fatigue
