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BPH - Coggle Diagram
BPH
Alpha Blockers
ADR: dizziness, malaise, fatigue, headache
DDI: alpha agonist, beta agonist, 3A4 inducers, 3A4 inhibitors
use with caution with PDE5 inhibitors
PK: 3A4
Special Populations
use with caution in hepatic impairment
Beers Criteria - risk of orthostatic hypotension
Cmax and AUC increased 27% and 34%
ER matrix is excreted in stool - use with caution in patients with stricture/narrowing of GI tract
Regimen: IR - 1 mg PO once daily, may titrate (double) the dose at 1-2 week intervals up to 8 mg once daily if tolerable. ER - 4 mg once daily, may titrate every 3-4 weeks up to 8 mg once daily
restart at starting dose if discontinued for several days
convert to ER form IR: stop final evening dose of IR before morning dose of ER
prazosin BID or TID dosing
Patient Education
MOA: competitive inhibitor of postsynaptic alpha-1 receptors in prostate stromal and bladder neck tissues which reduces sympathetic tone-induced urethral stricture
relax prostate smooth muscle
3rd gen are uroselective
Monitoring: BP routinely and for at least 6 hours after initial dose and with each dose increase, signs of hypotension
Contraindications: hypersensitivity to doxazosin or other quinazolines
Warnings: allergic reactions, CNS depression, floppy iris syndrome, decrease in WBC, orthostatic hypotension, priapism
use with caution in HF, angina, recent MI (within last 6 months)
rule out prostate cancer before initiation
Allergies: sulfa allergy - avoid tamsulosin
5 Alpha Reductase Inhibitors
Contraindications
hypersensitivity, pregnancy, women of childbearing potential
Monitoring: serial PSA - establish new PSA baseline 6+ months after initiation and monitor periodically, objective and subjective signs of relief of BPH (improve urine flow, reduction in urgency, relief of urinary difficulty)
Warnings
monitor patients with severely diminished urinary flow, increased risk of prostate cancer
Patient Education
rise slowly after sitting or laying down to avoid dizziness and passing out
ADR: sexual dysfunction (dose and time related)
DDI
none known
PK: DHT levels return to normal within 14 days of discontinuation, prostate volume returns to baseline within 3 months of discontinuation
M: 3A4 substrate with 2 active metabolites
E: longer half life in patients older than 70
Special Populations
mean AUC increases 15% in geriatric patients
use with caution in hepatic impairment due to extensive liver metabolism
pregnant women and women of childbearing potential should not touch or handle crushed or broken tablets
Regimen: 5 mg PO once daily as single agent or in combination with alpha-1 antagonist x6-12 months
reserve for patients with significantly enlarged prostates, patients intolerant of alpha-1 antagonists, or hematuria
if non-severe, can use for longer duration
MOA: competitive inhibitor of type II 5-alpha reductase which inhibits the conversion of testosterone to DHT to decrease serum DHT levels
reduces size of prostate
PDE-5 Inhibitors
MOA: PDE-5 mediated reduction in smooth muscle and endothelial cell proliferation, decreased nerve activity, increased smooth muscle relaxation and tissue perfusion of the prostate and bladder
relax prostate smooth muscle
Regimen: 5 mg PO once daily (treat with tadalafil and finasteride up to 26 weeks for BPH)
renal dose adjustment once CrCl <50, do not use if CrCl <30
use with caution in hepatic impairment
PK: 3A4 substrate
ADR: flushing, headache, nausea, myalgia, limb pain, respiratory tract infection, nasopharyngitis
Warnings: anginal chest pain after administration, color discrimination, hearing loss, hypotension, priapism, vision loss
Contraindications: do not use with nitrates due to risk of severe hypotension (wait 48 hours after PDE-5 inhibitor before taking nitrate for chest pain)
Monitoring: BP, efficacy and safety, urine flow, PSA
Special Populations: not recommended for patients with hypotension (<90/50), uncontrolled HTN (>170/100), HF, arrhythmias, stroke, MI, angina
use with caution in patients with bleeding disorders and PUD due to effect on platelets
geriatric (>65) have 25% higher exposure than younger patients (<50)
DDI: nitrates, alpha 1 blockers, 3A4 inducers and inhibitors
Patient Education: do not split tablets
Non-Pharmacologic
low fat diet
regular exercise
no smoking
avoid excess caffeine
void before bed and long car rides
Goals
control symptoms
prevent progression and reduce risk of complications
delay need for surgery
Goal Monitoring
patient report of symptoms
prostate size
PSA
Urinary Muscarinics/Anticholinergics
Non-selective
oxybutynin
Dosing
(overactive bladder) 5-10 mg Qday (extended release); 5 mg 2-3x/day (immediate release); adjust dose as needed in increments of 5mg q1-2 weeks
Special Populations
No renal/hepatic dose adjustments; increase cautiously in geriatrics (Beer's Criteria); B pregnancy risk factor
Side Effects
Anticholinergic effects (CNS, drowsiness, dizziness, blurred vision, tachycardia, etc.); constipation, nausea, xerostomia
Monitoring Parameters
incontinence episodes, postvoid residual, anticholinergic reactions
MOA
direct antispasmodic effect on smooth muscle , also inhibits the action of acetylcholine on smooth muscle to increase bladder capacity, decrease uninhibited contractions, and delays desire to void decreasing urgency and frequency
PK/PD
rapid and well absorbed; highly protein bound; hepatic metabolism via CYP3A4; high first-pass metabolism; excreted in urine
tolterodine
Dosing
(overactive bladder) 2mg BID (immediate release); 4mg Qday (extended release)
Special Populations
1mg BID in CrCl 10-30 mL/min/significantly reduced hepatic function (immediate release); 2mg Qday in CrCl 10-30 mL/Child-Pugh class A/B (extended release); not recommended in CrCl <10 mL/min/Class C hepatic dysfunction
Side Effects
xerostomia, headache
Warnings/Precautions
Angioedema, CNS effects, QT prolongation
Dose adjustment recommended in patients taking CYP3A4 inhibitors
PK/PD
highly protein bound, rapid absorption with immediate release; bioavailability increased 53% with food; excreted mostly in urine
MOA
competitive antagonist of muscarinic receptors increasing residual urine volume and decreasing detrusor muscle pressure
Monitoring Parameters
anticholinergic effects (dry mouth, constipation, dizziness); renal function (BUN, creatinine); hepatic function; postvoid residual volume (baseline)
M3 Selective
solifenacin
MOA
: inhibits muscarinic receptors resulting in decreased urinary bladder contraction, increased residual urine volume, and decreased detrusor muscle pressure
Dosing
: Initial: 5 mg PO once daily; if tolerated, may increase to 10 mg PO once daily
PK/PD
: ~ 90% oral bioavailability, no effect from food, ~ 98% protein binding
Extensive hepatic metabolism via CYP3A4
69% renal excretion, with <15% unchanged; 23% fecal excretion
AEs
: constipation, dry mouth, bowel/colon obstruction, prolonged QT interval, anaphylaxis, confusion, HA, somnolence (pediatric, 1.1%), angioedema, hallucinations
Warnings/Precautions
: Beers criteria = avoid use in elderly with delirium as it may induce or worsen; not recommended in those at risk of QT prolongation; decreased GI motility
Special pops
: do not exceed 5 mg/day in CrCl <30 mL/min or moderate hepatic impairment (Child-Pugh B); not recommended in severe hepatic impairments (C-P C); do not exceed 5 mg/ day with concomitant use of strong CPY3A4 inhibitors
Monitoring
: Overactive bladder: improvement in sx; anticholinergic CNS effects: HA, hallucinations, somnolence)
B3 Agonists
Myrbetriq (Mirabegron)
Dosing
(overactive bladder) 25 mg Qday (see efficacy within 8 weeks) may increase to 50 mg Qday based on patient efficacy and tolerability
Special Populations
Renal dose adjustment w/ CrCl <30 mL/min; Hepatic dose adjustment when Child-Pugh class B (25mg max), not recommended in class C;
Side Effects
Hypertension
Warnings/Precautions
Angioedema, blood pressure effects (monitor BP periodically during therapy)
Monitoring
BP at baseline and periodically during therapy; S/S of urinary retention
MOA
Activates B3AR in bladder resulting in relaxation of the detrusor smooth muscle during the urine strorage phase, increasing the bladder capacity
PK/PD
onset of action within 8 weeks; steady state within 7 days; metabolized through multiple pathways; excreted in urine/feces; bioavailability is dose dependent and higher in females vs males;