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Flashcards in Renal/Uro pharm Deck (40)
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31

Comparison of 5-alpha reductase inhibitors vs alpha-1 blockers

5-AR inhibitors:
- Symptom improvement from ~6 months
- increased flow from 1 month
- Effects on symptoms and flow demonstrated to 10 yr
- Reduce prostate volume
- Reduce the risk of AUR (acute urinary retention)
- Reduce the risk of surgery
- Decrease PSA (< 1 month

Alpha-1 blockers;
- increased flow from < 1 month
- Effect on symptoms and flow > 12 months not well established
- Do not reduce prostate volume
- Do not prevent AUR and surgery (Delay??)

32

Treatment of Erectile Dysfunction

Phosphodiesterase-5 inhibitors:
- Prevent break down of cGMP

Lifestyle modifications:
- Smoking cessation
- Limit/avoid EtOH
- Diet
- Exercise

Medication-induced
- Anti-HTN
- SSRIs
- Hormonal agents
- H2-receptor antagonists

33

Oral PDE5 inhibitors

Sildenafil
Tadalafil
Vardenafil

AEs:
1. Contraindicated with nitrates
- Can potentiate vasodilation and hypotension associated with NO
- Several early deaths in elderly men with concomittant heart disease on nitrates
2. Caution in vascular disease, coronary disease, vascular risk factors (cardiac eval)
3. Any recent MI, arrhytmias, obstructive hypertrophic cardiomyopathy

34

Second-line therapy for ED

1. MUSE: Medicated uretheral suppository for erection
- Administers local alprostadil (PGE-1) to enhance erection
- Useful in non-responsive patients or patients on nitrates
** PGE-1= stimulates adenylyl cyclase--> increased cGMP

2. Intracavernosal injection (PDE-inhibitors: alprostadil, papaverine)
- More reliable, instant predictable erection
- Fewer AEs, contraindications
* Phentolamine= alpha-blocker

35

Muscarinic receptors in bladder

Normal contraction mediated by activation of muscarinic receptors in detrusor muscles (Ach binding):
- M3 receptor= primary mediator of bladder contraction
- M2= more prevalent

36

Fesoterodine
Derofenisine
Tolteradine
Solifenacin

MOA:
1. Antimuscarinic action
- Inhibits binding of acetylcholine to cholinergic receptor and suppresses bladder contractions
2. Antispasmodic
- Allows detrusor smooth-muscle relaxation to control overactive bladder and urge urinary incontinence

Effects on Urinary Bladder= Motor and sensory
- Increase bladder capacity
- Reduce urinary frequency
- Diminsh urinary incontinence episodes resulting from involuntary bladder contractions

AEs:
- Dry mouth
- Headache
- Constipation
- Diarrhea
- Pain
- Dyspepsia

37

Oxybutynin

Tertiary amine, antimuscarinic agent
HIgher rates of AEs than tropsium

38

Tropsium

Quarternary amine
Less likely to cross BBB- better for use in older patients with concern of interfering with cognitive function

39

Mirabegron

Beta-3 adrenergic agonist
- Relaxes bladder detrusor muscle

40

Testosterone replacement

ROA:
Oral androgens not used in US
- Difficulty with achieving consistent levels
- Hepatotoxicity
Injectable agents
Transdermal/topical agents
Buccal preparations
Long acting implants

Used to treat symptoms of hypogonadism:
- ED, low libido, depression, fatigue, anemia

Diagnosis both clinical and serological
- Should have endocrine eval before T replacement
** Need to be careful in prostate cancer