Lecture 2: Male GU Pharm Flashcards
Which α receptor is on the detrusor m. and when stimulated by NE can lead to detrusor instability?
α1D
Which α receptor subtype is found on prostate smooth muscle and is resposnsible for contraction when stimulated by NE?
α1A
Which two α1 receptor antagonists used in BPH are selective for the α1 >>>> α2 receptor?
- Terazosin
- Doxazosin
What are the AE’s associated w/ terazosin and doxazosin used to treat BPH?
Postural hypotension, dizziness, fatigue –> α1 receptor antagonists
Which two α1 receptor antagonists used for BPH are uroselective and bind α1A = α1D?
1) Tamsulosin
2) Silodosin
What are the AE’s associated with tamsulosin and silodosin used for BPH?
- Reduced ejaculation
- IFIS = intraoperative floppy iris syndrome
Which α1 receptor antagonist has functional uroselectivity and is used to treat BPH?
Alfuzosin
What is a serious AE associated with Alfuzosin used in treatment of BPH?
QT prolongation
Which three α1 receptor antagonists used in BPH increase the concentration of CYP3A4 substrates?
- Tamsulosin
- Silodosin
- Alfuzosin
What is the best monotherapy for prompt relief of BPH symptoms (days)?
α1 receptor antagonists
Alfuzosin should not be given to tx BPH in patients with what impairment?
Hepatic impairment
What are the two steroid 5α-reductase inhibitors used for BPH?
How quickly do they work?
- Finasteride and Dutasteride
- Delayed action –> shrinkage and sx relief in 3-6 months
What are the direct effects (MOA) of steroid 5α reductase inhibitors?
- Directly inhibit production of DHT in prostate epithelial cells
- Cause TestosteroneaccumulationandDHT depletion
Which steroid 5α reductase inhibitor is specific for SAR-2?
Finasteride = SpeciFIc inhibitor of SAR-2
Which steroid 5α-reductase inhibitor is a dual inhibitor of both SAR-1 and 2?
Dunasteride = DUal inhibitor