BPH/ED Pharm Flashcards
What are the five alpha 1 adrenergic receptor antagonists? their effect?
a. terazosin, doxazosin, tamsulosin, silodosin, alfuzosin
b. relax muscle tone, rapid relief of symptoms (days);
they compete with NE to reduce spasm, promote muscle relaxation, improve urine flow
What is the receptors for each of the following?
a. Prostate
b. Detrustor
c. SC
d. BVs
a. alpha 1 A (smooth m contraction)
b. alpha 1 D > alpha 1 A (instability)
c. alpha 1 D (control of urinary function)
d. alpha 1 B > alpha 1 A (vascular resistance)
Terazosin
a. specificity
b. uroselective
c. adverse effects
d. drug interactions
a. alpha 1»_space;»» alpha 2
b. no
c. postural hypotension, dizziness, fatigue
d. PDE-5 (sildenafil, vardenafil)
Tamsulosin
a. specificity
b. uroselective
c. adverse effects
d. drug interactions
a. alpha 1 A = alpha 1 D > alpha 1 B
b. yes, alpha 1 A = alpha 2 D
c. reduced ejaculaiton, IFIS
d. PDE-5 (sildenafil, vardenafil); increased concentration of CYP 34A substrates
Doxazosin
a. specificity
b. uroselective
c. adverse effects
d. drug interactions
a. alpha 1»_space;»» alpha 2
b. no
c. postural hypotension, dizziness, fatigue
d. PDE-5 (sildenafil, vardenafil)
Silodosin
a. specificity
b. uroselective
c. adverse effects
d. drug interactions
a. alpha 1 A = alpha 1 D > alpha 1 B
b. yes, alpha 1 A = alpha 2 D
c. reduced ejaculaiton, IFIS
d. PDE-5 (sildenafil, vardenafil); increased concentration of CYP 34A substrates
Alfuzosin
a. specificity
b. uroselective
c. adverse effects
d. drug interactions
a. non specific alpha 1 selective
b. yes (functional –> distributes prostate>serum)
c. QT prolongation
d. PDE-5 (sildenafil, vardenafil); increased concentration of CYP 34A substrates
What is the function and timelines of finasteride and dutasteride?
- prevent enlargement and encourage shrinkage of prostate
- 3 to 6 months
- Steroid 5 alpha reductase (SAR) inhibitors
*adverse effects: ED, gynecomastia, depressed libido, ejaculation disturbances
Prostates that have undergone hyperplasia have excess SAR 1 or 2?
2 (found only in prostate)
*SAR converts T to DHT
What is the serum DHT increased more with the use of dutasteride?
- Finasteride –> speciFIc inhibitor SAR 2
- Dutasteride –> Dual inhibitor SAR 1 and 2
Why should you be careful to prescribe finasteride or dutasteride to a patient with liver disease?
these drugs are metabolize by CYP3A
Sildenafil (viagra)
a. onset (min)
b. duration of action (hr)
c. stomach contents
d. t1.2 (hr)
e. clearance
a. 60
b. 4
c. empty
d. 4
ehepatic CYP 3A4
Vardenafil
a. onset (min)
b. duration of action (hr)
c. stomach contents
d. t1.2 (hr)
e. clearance
a. 60
b. 4-5
c. empty
d. 4
e. hepatic CYP3A4
Tadalafil
a. onset (min)
b. duration of action (hr)
c. stomach contents
d. t1.2 (hr)
e. clearance
a. 60
b. 36
c. doesn’t matter
d. 18
e. hepatic CYP3A4
*adverse effects: back pain, myalgia, limb pain
Avanafil
a. onset (min)
b. duration of action (hr)
c. stomach contents
d. t1.2 (hr)
e. clearance
a. 15 (high dose), 30 (low dose)
b. 4
c. doesn’t matter
d. 4
e. hepatic CYP3A4
