Drugs for BPH Flashcards
What receptor dominates in the lower bladder, prostate, and penile urethra?
Alpha-1-a
What receptor dominates in the upper bladder?
Alpha-1-d
What are beta-sitosterols and Saw palmetto?
They are natural supplements often taken to treat BPH. There is no proof that they actually work.
What are the potential complications of untreated BPH?
Urinary retention
Bladder, urinary tract, and kidney issues
What drugs for BPH belong to Alpha -1 blocker group?
Prazosin Alfuzosin Terazosin Doxazosin Tamulosin Silodosin
What is the MOA of the Alpha-1 blockers?
They block alpha 1 stimulation and relax the smooth muscle of the urethra and prostate.
What are some common adverse effects of alpha 1 blockers?
GI (xerostomia, nausea)
CNS (HA, somnolence, insomnia, dizziness)
What are the disadvantages of alpha-1-a blockage?
Abnormal ejaculation
Blocks dopa
What are the advantages of alpha-1-a blockage?
decreased CV effects
Which Alpha 1 blocker is the best?
Alfuzosin is the best b/c it has the most clinical effect with the least adverse effects.
Your patient who is taking an alpha-1 blocker needs surgery for their cataracts. What complication should you be concerned about?
Floppy iris syndrome. Surgery can continue if surgical technique is changed.
Which of the alpha-1 blockers are short acting?
Prazosin
Alfuzosin
Which of the alpha 1 blockers are Long acting?
Terazosin
Doxazosin
Which alpha 1 blockers are alpha 1a selective?
Tamulosin
silodosin
Which alpha 1 blockers are metabolized by CYPs?
Alfuzosin
Doxazosin
Tamulosin
Silodosin
Everything except Prazosin, and Terazosin (which is not mentioned)
Which alpha 1 blocker undergoes non-CYP metabolism?
Prazosin
Which alpha 1 blockers undergo fecal elimination?
Prazosin
Doxazosin
Which Alpha 1 blockers undergo mixed elimination?
Alfuzosin (3:1 fecal:renal)
Terazosin (3:2 hepatic:renal)
Tamulosin (3:2 Renal:fecal)
Silodosin (2:1 fecal:renal)
What is the MOA of Tadalafil?
Tadalafil is a PDE-5 inhibitor. It prevents the breakdown of cGMP in smooth muscle, which leads to a decrease of intracellular Ca and smooth muscle relaxation. This is used to treat BPH
What is the metabolism and elimination of Tadalafil?
CYP3A4
Fecal elimination
What adverse effects are associated with Tadalafil?
All are uncommon:
No-arteritic optic neuropathy
Retincal artery occlusion
Hearing loss
What are the contraindications for Tadalafil?
Organic Nitrates (hypotension, worse with EtOH)
What is the MOA of Finasteride?
Specific type 2, 5-alpha-reductase inhibitor. Prevents the conversion of Testosterone to DHT. (competitive inhibition)
What is the MOA of Dutasteride?
Type 1 and Type 2 5-alpha-reductase inhibitor. (competitive inhibition)
What is the difference between type 1 and Type 2 5-alpha-reductase inhibitors?
Type 2 is found in the prostate.
How are the 5-alpha-reductase inhibitors metabolized?
CYP3A4
What adverse effects are associated with the 5-alpha-reductase inhibitors?
Pregnancy Cat X Erectile dysfunction, Decreased libido, gynecomastia Increased prostate Cancer Decreased PSA levels
