Drugs used in BPH Flashcards Preview

Renal Week 3 > Drugs used in BPH > Flashcards

Flashcards in Drugs used in BPH Deck (22):
1

What short acting selective alpha-1 blockers are used to treat BPH?

• Prazosin
• Alfuzosin

2

What Long acting Selective alpha-1 blockers are used in BPH?

• Terazosin
• Doxazosin

3

What alpha-1 partially selective blockers are used in BPH?

• Tamsulosin
• Silodosin

4

What PDE-5 inhbititors are used to treat BPH?

• Tadalafil

5

What 5-alpha Reductase inhibitors are used to Treat BPH?

• Finasteride
• Dutasteride

6

Differentiate the locations of the alpha-1a and alpha-1d receptors?

• Alpha-1a - Predominates in lower GU tract (trigone through prostate and into urethra)

• Alpha-1d - predominates in the Detrussor muscle of the urinary bladder

7

What can be said about the following for the alpha-1 blockers?
• Metabolism
• Duration of Action

Metabolism:
• extensive CYP metabolism

Duration of Action:
• LONG duration of action EXCEPT for prazosin

**Long Duration of action means compliance on these drugs is better**

8

What makes the use of prazosin difficult?

• You need to Titrate the dose because the drug shows great variability from patient to patient

9

What are common side effects of all of the alpha-1 blockers?

• Orthostatic Hypotension, Syncope

• Xerostomia, Nausea, Dizziness, Somnolence, Asthenia, Headache, Insomnia

10

Tamsulosin and Sildosin
• MOA?
• Specific Side effects?

MOA:
• partially selective alpha-1a antagonists

Side effects that differ from other alpha-antagonists:
• Diminished CV function
• Increased Sexual (ejaculation) dysfunction

11

What is the best alpha blocker currently used to treat BPH?
• why?

• Alfuzosin - has no significant effects on dizziness, asthenia, and ejaculatory dysfunction

12

How do PDE-5 inhibitors work to increase urine flow?

• PDE5 breaks down cGMP made by Guanylyl Cylcase in response to NO stimulation

• Blocking PDE5 allows form more cGMP to activate PKG which phosphorylates Ca2+ channels allowing for Ca2+ efflux and smooth muscle relaxation

13

Tadalafil
• aka?
• use?
• Side Effects?
• Contraindications for use?

aka Cialis - PDE5 inhibitor
• relieves BPH

Side Effects = rare:
• Nasopharyngitis, URTIs
• Vision and hearing loss

Contraindications:
• DO NOT USE WITH ORGANIC NITRATES
• Profound Hypotension
• Exacerbated by alcohol consumption

14

What does 5-alpha-reductase do?
• what are the two different subtypes?
• where are they found?

• Catalyzes the conversion of Testosterone to dihydrotesterone.

2 subtypes:
• Type I: non-genital skin (liver, bone)
• Type II: Urogenital Tissue in men, and genital skin in men and women

15

What is special about dihydrotesterone?

• Binds with higher affinity than testosterone

• Activates gene expression more efficiently than testosterone

16

How do 5-alpha-reductase inhibitors work to reduce the effects of BPH?

• Reduce Dihydrotestosterone driven proliferation of the prostate

17

What 2 drugs act on 5-alpha-reductase?
• how do they differ?

• Finasteride - inhibits type 2
• Dutasteride - inhibits type 1 and 2 enzyme

***besides receptor specificity differences, they are the same in all other ways***

18

Finasteride and Dutasteride
• Administration
• Metabolism
• Pregnancy safety?

Administration:
• Oral

Metabolism:
• Heavy CYP3A4 metabolism

Pregnancy Category X (not carried in semen)

19

5-alpha reductase inhibitors.
• Name them.
• Side effects.

Finasteride (type 2) and Dutasteride (type 1 and 2)

Side Effects:
• Ejaculation Dysfunction, decreased libido, Gynecomastia (man boobs)

• Decreased PSA levels

20

What is the issue of giving finasteride or dutasteride to someone with prostate cancer?

• These drugs may decrease PSA levels

**They also may increase the cancer of getting prostate cancer

21

What is the use of Beta-Stiosterols for BPH?

*Reduce SYMPTOMS of BPH but do NOT decrease prostate size significantly

22

What is Saw Palmetto's use in BPH?

*Unlike Beta-Stiosterols, there is not significant change in side effects with using Saw Palmetto