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Flashcards in Urology Pharmacology Deck (55)
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1

Drugs used to treat BPH?
4

1. Alpha-1 blockers

2. 5 alpha-reductase inhibitors

3. Combo
Dutasteride-Tamulosin (Jalyn)

4. Tadalafil (Cialis)

2

What are the alpha one blockers?
5


What is the Combo 5-alpha reductase inhibitor-alpha-1 blocker?

1. Terazosin (Hytrin)
2. Doxazosin (Cardura)
3. Alfuzosin (Uroxatrol)
4. Tamsulosin (Flomax)
5. Silodosin (Rapaflo)


Dutasteride-Tamulosin (Jalyn)

3

Alpha-1 Blockers
1. More effective than 5-alpha-reductase inhibitors for what?

2. MOA?

3. Alpha-1 receptors are located where?

All drugs in this class have similar efficacy

1. short and long term symptom management

2. relax smooth muscle in the bladder neck and the prostatic capsule and prostatic urethra

3. in the base of the bladder and in the prostate

4

Alpha-1 Blockers Efficacy
1. Symptom scores decreased by _____%?

2. Urine flow rates increased by _____%?

3. Which are more effective than the 5-alpha-reductase inhibitor Finasteride (Proscar)? 2

4. Efficacy of Tamsulosin (Flomax) and Finasteride (Proscar) compare how?

1. 30-40

2. 16-25

3. Doxazosin (Cardura) and Terazosin (Hytrin)

4. were equal

5

Alpha-1 Blockers
SE
1. Most common? 2
2. Generally start dosing how?

1. Most common are
-dizziness and
-orthostatic hypotension


2/ Generally start at a small dose at bedtime and titrate up slowly over several weeks

6

1. Which alpha-1 blockers cause more BP lowering than others? 2

2. When can it cause severe hypotension?

1.
-Terazosin (Hytrin) and
-Doxazosin (Cardura) (cause more BP lowering than the others)

Tamsulosin (Flomax), Alfuzosin (Uroxatrol) and Silodosin (Rapaflo) have less BP effects


2. Can cause severe hypotension if used with phosphodiesterase-5 inhibitors

7

Other SE of alpha-1 blockers?
3

1. Asthenia (muscle weakness)
2. Nasal congestion
3. Problems with ejaculation


Found primarily with Tamsulosin (Flomax)
Can decrease volume of ejaculate by 90%
35% of patients may have no ejaculate
Up to 28% have retrograde ejaculation on Silodosin (Rapaflo)

8

5 alpha-reductase inhibitors
What are the meds? 2

1. Finasteride (Proscar)
2. Dutasteride (Avodart)

9

5 alpha-reductase inhibitors
Only agents that provide long term what? 2

1. decrease in prostate size and
2. decreased need for prostatic surgery

10

MOA of 5-ARI’s
1. Competitive inhibitor of both what? 2

2. MOA?

3. Serum dihydrotestosterone decreases by ___%?
-Primary androgen in what?

4. Serum testosterone increases by ____%
-Decreases _______ size

1.
-tissue and
-hepatic 5-alpha reductase

2. inhibition of the conversion of testosterone to dihydrotestosterone and markedly suppresses serum dihydrotestosterone levels

3. 70
- prostate and hair follicles

4. 10
-prostatic

11

MOA of 5-ARI’s
1. May be how long to notice a reduction in symptoms?

2. Increase in maximum what?

3. Reduction in what by about 18%?

4. Decreased need for ______?

5. Decreased development of what?

6. The larger the what the more effective the medication?

7. Which one is usually more potent?

1. up to a year

2. urinary flow rate

3. mean prostatic volume

4. surgery

5. acute urinary retention

6. prostate volume

7. Dutasteride (Avodart) may be more potent than Finasteride (Proscar)

12

MOA of 5-ARI’s
1. Major side effects? 2

2. Timeline?

3. _________ serum PSA by 50%

4. Use a factor of __ when interpreting PSA results in the first 24 months of therapy
Use a factor of __ after 24 months

5. Decreased development of prostate cancer but concern for possible increased incidence of what?

1.
-Decreased libido
-Ejaculatory or erectile problems

2. May only have these effects for the first year of therapy

3. Decreases

4. 2, 2.5

5. high grade lesions

13

Cialis for BPH
1. MOA?
2. What can you not use with it?
3. Dosing?
4. Takes how long to note symptom improvement for BPH?

1. Cialis blocks PDE5 in the prostate and bladder

2. Do not use with
-nitrates or
-alpha-1 blockers

3. 5mg daily dose

4. Takes 2-4 weeks to note symptom improvement when used for BPH

14

Erectile Dysfunction
Which drug classes for use? 2

1. Prostaglandin injectable
2. Phosphodiasterase inhibitors

15

Erectile Dysfunction
Which drugs are in the following categories:
1. Prostaglandin injectable? 1
2. Phosphodiasterase inhibitors? 4

1. Prostaglandin injectable
-Alprostadil

2. Phosphodiasterase inhibitors
-Tadalafil (Cialis)
-Vardenafil (Levitra)
-Sildenafil (Viagra)
-Avanafil (Stendra)

16

Alprostadil (Caverject, Muse)
1. Drug category?
2. Forms? 2
3. MOA?
4. Onset?
5. Duration of action?

1. Drug category: Prostaglandin, Vasodilator

2. Forms:
- Intracavernosal injections,
-urethral pellets

3. MOA
Causes vasodilation by means of direct effect on vascular and smooth muscle; relaxes trabecular smooth muscle by dilation of cavernosal arteries when injected along the penile shaft, allowing blood flow to and entrapment in the lacunar spaces of the penis (ie, corporeal veno-occlusive mechanism)

Onset and duration of action
4. Onset 5-20 minutes
5. Duration less than 1 hour

17

Alprostadil (Caverject, Muse)
1. Contraindications? 3

2. SE? 3

1. Contraindications
-Conditions that predispose the patient to priapism
-Anatomic or fibrotic conditions of the penis
-For the pellets (Muse) – urethral stricture, perineal pain

2. Side effects
-Syncope
-Priapism
-May cause BP lowering

18

Phosphodiasterase inhibitors MOA
1. The physiologic mechanism of erection of the penis involves release of what into where?

2. NO then activates the enzyme _____________, which results in increased levels of cyclic guanosine monophosphate (cGMP),

3. producing smooth muscle relaxation and inflow of blood to the what?

4. Enhances the effect of NO by inhibiting what, which is responsible for degradation of cGMP in the corpus cavernosum?

5. Do not directly cause what?

1. nitric oxide (NO) in the corpus cavernosum during sexual stimulation

2. guanylate cyclase

3. corpus cavernosum

4. phosphodiesterase type 5 (PDE-5)

5. penile erections

19

Phosphodiasterase inhibitors Contraindications
2

1. Men taking nitrates
2. Caution with alpha-1 blockers due to risk for severe hypotension

20

Phosphodiasterase inhibitors
Adverse reactions
6

1. Severe hypotension (with nitrates or alpha-1 blockers)

2. Common: flushing, headaches, dyspepsia

3. Visual effects: transient blue vision with sildenafil (Viagra), may increase risk for nonarteritic ischemic optic neuropathy

4. Hearing loss

5. Priapism

6. Drug interactions: CYP3A4 inhibitors may increase the serum concentration of the PDE-5

21

Administration of Phosphodiasterase inhibitors
1. In general take _____ prior to intercourse?

2. Which drugs have a quicker onset of action (30 min)? 2

3. What will delay the onset of action in Sildenafil (Viagra) and Vardenafil (Levitra)?

4. ______ dose Tadalafil (Cialis) is available

5. Duration of action ____ hours on average except for Tadalafil (Cialis) up to___ hours

1. 60 min

2. Vardenafil (Levitra) and Avanafil (Stendra)

3. Food and alcohol

4. Daily

5. 8-12, 36

22

Hold nitrates for 1.___ hours after use of a PDE-5 or for 2.___ hours if used taldafil (Cialis)

1. 24

2. 48

23

Testosterone replacement
Treats what?

To treat low testosterone levels in primary or secondary hypogonadism

24

1. Whats primary hypogonadism?

2. Secondary? 2

1. Primary – Testes fail to produce testosterone

2. Secondary – Pituitary or hypothalamus malfunction

25

Testosterone replacement
MOA?

1. Direct action by binding to the androgen receptor

2. Act in tissues that express the enzyme 5-alpha reductase
-Converts to dihydrotestosterone
-Binds more readily to the androgen receptor than testosterone

3. Can act as an estrogen after converting to estradiol via an aromatase and bind to the estrogen receptor

26

Testosterone replacement
Principles of therapy
1. Only use in men that are what?
2. Symptoms that are treated? 7

3. Goal of therapy?

4. Do not use it to treat impaired what?
-why?

1. Only for use in men who are hypogonadal

2.
-Decreased libido;
-decreased AM erections;
-loss of body hair;
-low bone density;
-gynecomastia;
-small testes;
-decreased muscle mass

3. Goal of therapy is to return testosterone levels back to the normal range

4. Do not use it to treat impaired spermatogenesis
-Testosterone therapy suppresses pituitary gonadotropin secretion and leads to more impairment of spermatogenesis

27

Testosterone replacement: Prior to starting therapy? 3

1. Screen for prostate cancer in men over 50 or in men over age 40 if any risk factors

2. Screen for erythrocytosis

3. If sleep apnea is present, make sure it is being treated

28

Side effects of testosterone?
10

1. Polycythemia
2. Worsening of BPH symptoms
3. Acne
4. Increase in PSA
5. Oral and prolonged IM doses associated with a multitude of liver issues (jaundice, hepatitis, elevated LFTs)
6. Increased risk of prostate cancer
7. Decreased spermatogenesis
8. Fluid retention
9. Worsening of sleep apnea
10. Possible increased risk of cardiovascular events

29

Contraindications
Testosterone replacement?
7

1. Known prostate cancer
2. Known breast cancer
3. Severe lower urinary tract symptoms
4. HCT > 50%
5. Untreated severe sleep apnea
6. PSA > 4.0 mcg/L
7. PSA > 3.0 mcg/L with any prostate CA risk factors

30

Tesosterone replacement: On the FDA watch list?
Why?

The FDA is investigating the risk of stroke, heart attack, and death in men taking FDA-approved testosterone products. The FDA is evaluating information from 2 separate studies that suggest an increased risk of cardiovascular events among groups of men prescribed testosterone therapy, although the agency has not concluded that these products increase the risk of stroke, heart attack, or death.