Genitourinary Module Flashcards
Name the main antimuscarinics used to treat urinary incontinence
Oxybutynin, propantheline, darifenacin, solifenacin, tolterodine
What is the MOA of urinary antimuscarinics?
Non-selective muscarinic receptor antagonists
Reduce bladder muscle contractility and increase bladder capacity
What is the indication/s for urinary antimuscarinics?
Urinary urge incontinence
Name some ADRs for urinary antimuscarinics
Drowsiness & seizures (H1 block)
hallucinations and agitation (wrong dosage)
Blurry vision, dry mouth, constipation (M-receptor block)
Palpitation and cardiac arrhythmias
Which urinary antimuscarinics are more selective? (Uroselectivity)
Darifenacin, solifenacin, tolterodine
Which antimuscarinics has the highest incidence of dry mouth?
Oxybutynin
Which urinary antimuscarinics will increase QT interval and constipation?
Solifenacin
True or False
Oxybutynin has an increased likelihood of CNS effects?
TRUE
What are the four concepts of uroselectivity?
Receptor-selective, tissue selective, clinically uroselective, functionally selective
Explain the following type of uroselectivity:
Receptor-selectivity
Difference in potency for one receptor compared to another
(E.g. selectivity for alpha 1A subtype that regulate smooth muscle contraction compared to vascular smooth muscle contraction alpha 1B)
Explain the following type of uroselectivity:
Tissue selective
Primarily distributed in the target tissues of the urinary tracts versus other tissues and organs
Explain the following type of uroselectivity:
Clinically uroselective
The drug is able to produce the desired pharmacological effect with few side effects
(E.g. improves urinary flow rate and BPH symptoms with few ADR such as dizzy, orthostatic hypotension)
Explain the following type of uroselectivity:
Functional selectivity
The drug is able to act on the physical function of the organ, changing its function from normal
(E.g. preferentially dec urethral pressure versus arterial BP)
Name the urinary selective alpha blockers
Alfuzosin, prazosin, silodosin, tamsulosin, terazosin
What is the MOA of urinary alpha-1 selective blockers?
Blocks alpha 1 receptor > decreasing circulating Ca2+ > relax smooth muscle (SM) in bladder neck and prostate > dec resistance to urine outflow
E.g. MOA of alpha-agonist = Noreadrenaline
Binding noreadrenaline to alpha1 receptor > mobilization of intracellular Ca2+ stores > smooth muscle contraction (SM)
Which alpha 1 blockers show equal selectivity to all receptor subtypes?
Terazosin, doxazosin, alfuzosin
Makes them non-selective =)
Which urinary alpha 1 blockers show receptor selectivity?
Tamsulosin (Alpha1a = alpha1 d > Alpha1 B)
Silodosin (Alpha1a > alpha1 d > Alpha1 B)
What is the indication for genitourinary selective alpha-1 blockers?
Symptomatic relief of benign prostatic hyperplasia (BPH)
Name some ADRs of Prazosin
(just know some/be able to explain some)
Depression, nervousness
Headache, drowsiness = blood vessel changes due to alpha1-Ab inhibition
Palpitations, tachycardia = physiological reflex reaction to alpha 1Ab block
Orthostatic hypotension = alpha 1Ab block > decrease PVR > decrease BP
Priapism, impotence, gynaecomastia
Nasal congestion, nosebleeds = alpha1 antagonism > vasodilation
Name some Tamsulosin ADRs
Constipation, Diarrhoea
Blurry vision, floppy iris syndrome
Postural hypotension
Priapism, abnormal ejaculation (retrograde ejaculation)
What is the MOA of 5-alpha-reducatse inhibitors
block 5-alpha reductase > prevent conversion of testosterone to dihydrotestosterone (DHT, stimulate prostatic growth) > reduce prostate size and improve urinary output
Name the two relevant 5-alpha-reducatse inhibitors
Dutasteride, finasteride
What are the indications for genitourinary 5-alpha-reducatse inhibitors (Dutasteride, finasteride)
Benign prostatic hyperplasia (BPH)
Male pattern baldness
Name some notable side effects for genitourinary 5-alpha-reducatse inhibitors
Impotence, ejaculation disorders, decreased libido
breast tenderness/enlargement = less testosterone