Male Disorders Pharm-Fitzpatrick Flashcards
Finasteride and dutasteride are these types of drugs
Steroid 5alpha reductase inhibitors
Sildenafil, vardenafil, and tadalafil are these types of drugs
PDE5 inhibitors for ED
List a1 antagonists for symptomatic relief of lower urinary tract syndromes
Terazosin Doxazosin Tamsulosin Silodosin Alfuzosin
Drug class to relax muscle tone
DYNAMIC REMEDY
Rapid relief of symptoms - days
List the dominant alpha1 receptor subtype for the following:
Prostate: __
Detrusor: __
Spinal cord: __
Blood vessels: __
Prostate=alpha1A
Detrusor=alpha1D > alpha1A
SC=alpha1D
Blood vessels=alpha1B > or equal to alpha1A
Alpha1 antagonists compete with ___. This mechanism reduces spasm, promotes muscle relaxation and improves urine flow
NE
List alpha1 antagonists that are non-specific for a1 subtypes`
Terazosin
Doxazosin
Alfuzosin
List the a1 antagonists that are subtype specific and which subtypes are dominant
Tamsulosin
Silodosin
a1A=a1D > a1B
These a1 antagonists have no uroselectivity, adverse effects include postural hypotension and need to titrate the 1st doe, and fatigue. Drug interactions with PDE-5 inhibitors
Terazosin and doxazosin
This uroselective a1 antagonist has adverse effects such as QT prolongation and interacts with CYP450
Alfuzosin
These uroselective a1 antagonists target a1A and a1D equally, adverse effects such as reduced ejaculation, intraoperative floppy iris syndrome, and has interactions with CYP450
Tamsulosin and silodosin
These 5a reductase inhibitors slow BPH progression
Finasteride and dutasteride
Drug class that prevents enlargementand shrinks prostate
Structural remedy
Delayed action –> shrinkage and symptom relief ~ 3-6 months
Finasteride and dutasteride slow BPH progression by inhibiting what enzyme?
SAR II
What are direct effects of SAR II inhibition for tx of BPH?
- T accumulation
- DHT depletion
What are indirect effects of SAR II inhibition for tx of BPH?
AR receptor less occupied –> no gene transcription
This steroid 5a reductase inhibitor is a specific inhibitor of SAR II:
Finasteride
This steroid 5a reductase inhibitor has dual inhibitor function on SAR I and SAR II
Dutasteride
What are some adverse events associated with 5a reductase inhibitors for tx of BPH?
ED
Gynecomastia
Depressed libido
Ejaculation disturbances
This PDE-5 inhibitor is now approved by the FDA for use in BPH
Tadalafil
Describe the pathway from GTP to smooth muscle relaxation and ultimately a boner:
GTP –> NO (from NANC neurons) interacts with guanylate cyclase –> cGMP –> smooth muscle relaxation –> boner
Sildenfail, vardenafil, and tadalafil inhibit this enzyme that converts cGMP –> GMP
PDE-5
This PDE-5 inhibitor has a span of efficacy of about 36 hrs and a half life of 18 hrs
Tadalafil
PDE-5 inhibitors are cleared by this hepatic enzyme
CYP3A4
In addition to PDE-5, sildenafil and vardenafil act on this PDE receptor subtype
PDE-6 on the retina –> adverse effect of blue vision disturbance
What are some side effects of Tadalafil
Back pain
Myalgia
Limb pain
NSAIDS okay
Can be used for BPH
What are contraindications with PDE-5 inhibitor usage?
Organic nitrates –> may induce extreme hypotension
When you use Vardenafil and an a1 receptor antagonist, what should you consider?
Pt should be hemodynamically stable prior to initiating therapy. INITIATE vardenafil AT THE LOWEST RECOMMENDED DOSE
When tadalafil is used for tx of BPH, concurrent ___ are not recommended.
Alpha1 blockers
Alpha blockers should be initated at the lowest recommended dose in pts currently taking __
Sildenafil
This injectable drug stimulates PDE-1 for ED
Caverject
Papaverine and phentolamine
Doxazosin, terazosin, alfuzosin, tamsulosin, and silodosin are these types of drugs:
Alpha1 adrenergic antagonists
