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Toronto Notes 2019 Common Medications Urology U45 Table 28. Prostatic Carcinoma Medications (N>0, M>0)
Drug
leuprolide, goserelin
“androgen deprivation therapy”
*cyproterone acetate
flutamide, bicalutamide abiraterone
enzalutamide
*Very rarely used
Class
GnRH agonist
Steroidal antiandrogen
Non-steroidal antiandrogen
Non-steroidal antiandrogen
Non-steroidal antiandrogen
Mechanism
Initially stimulates LH, increasing testosterone and causing “flare” (initially increases bone pain)
Later causes low testosterone
Competes with DHT for intracellular receptors: 1. Prevent flare produced by GnRH agonist
2. Use for complete androgen blockade
3. May preserve potency
As above
Irreversible CYP17 inhibition, blocking synthesis of androgens in tumour, testis, and adrenal glands
Androgen receptor signaling inhibitor (full antagonist)
Adverse Effects
Hot flashes Headache Decreased libido
Hepatotoxic: AST/ALT monitoring
Adrenal insufficiency (concurrent treatment with steroids often required) Hypertriglyceridemia Peripheral edema
Peripheral edema Fatigue and weakness Hot flashes
Adverse Effects
Dry mouth Blurred vision Constipation Supraventricular tachycardia
As above
Blood pressure should be monitored
As above
Weight gain Orthostatic hypotension Prolonged PR interval
Urinary retention, UTI
Table 29. Continence Agents and Overactive Bladder Medications
Drug
oxybutynin
oxybutynin, tolterodine, trospium, solifenacin, darifenacin, fesoterodine
mirabegron
imipramine
Botulinum toxin A bladder injections
Class
Antispasmotic
Anticholinergic
β3 agonist Tricyclic
antidepressant
Neurotoxin
Mechanism
Inhibits action of ACh on smooth muscle
Decreases frequency of uninhibited detrusor contraction Diminishes initial urge to void
Muscarinic receptor antagonist Selective for bladder
Increases bladder volume Decreases detrusor pressure
Beta sympathetic receptor blocker in the bladder; relaxes bladder during storage phase
Sympathomimetic effects: urinary sphincter contraction Anticholinergic effects: detrusor relaxation
Prevents the release of neurotransmitters
Indication
Overactive bladder Urge incontinence + urgency + frequency
Overactive bladder Urge incontinence + urgency + frequency
Overactive bladder Urge incontinence + urgency + frequency
Stress and urge incontinence
Refractory OAB incontinence both neurogenic and non- neurogenic
Note: All anti-cholinergics are equally effective and long-acting formulations are better tolerated. Newer muscarinic M3 receptor specific agents (solifenacin, darifena- cin) are equally efficacious as older drugs, however, RCTs based on head-to-head comparison to long acting formulations are lacking.