UROLOGY PHARM Flashcards
ALPHA-1 BLOCKER DRUGS
Tamsulosin (Flomax) Terazosin (Hytrin) Doxazosin (Cardura) Alfuzosin (Uroxatrol) Silodosin (Rapaflo)
Combo 5-alpha reductase inhibitor-alpha-1 blocker
Dutasteride-Tamsulosin (Jalyn)
more effective than 5-alpha reductase inhibitors for short & long term symptom management
alpha-1 blockers
MOA OF ALPHA-1 BLOCKERS
relaxes smooth muscle in bladder neck, prostatic capsule, and prostatic urethra
where are alpha-1 receptors located
in the base of the bladder and in the prostate
which 2 alpha-1 blockers were more effective than finasteride (proscar)
doxazosin
terazosin
which alpha-1 blocker has equal efficacy with finasteride
Tamsulosin (Flomax)
MOST COMMON SE OF ALPHA-1 BLOCKERS
DIZZINESS
ORTHOSTATIC HYPOTENSION
which alpha-1 blockers cause more BP lowering effects than others
Doxazosin (Cardura) & Terazosin (Hytrin)
which alpha-1 blockers have less BP effects
Tamsulosin (Flomax)
Silodosin (Rapaflo)
Alfuzosin (Uroxatrol)
TSA! = less BP effects
how to start patients on alpha-1 blockers
generally start a small dose at bedtime and titrate up slowly over several weeks
⦁ ***Alpha-1 blockers = can cause severe hypotension if used with
PDE-5 inhibitors
***Alpha-1 blockers = can cause severe __________ if used with PDE-5 inhibitors
hypotension
SE OF ALPHA-1 BLOCKERS
- dizziness & hypotension….also
⦁ Asthenia (muscle weakness)
⦁ nasal congestion
⦁ problems with ejaculation
which alpha-1 blocker has the most problems with ejaculation
Tamsulosin (Flomax)
alpha-1 blockers problems with ejaculation
- can decrease volume of ejaculate by 90%
- 35% of patients may have no ejaculate
- up to 28% have retrograde ejaculation in Silodosin (Rapaflo)
which alpha-1 blocker causes retrograde ejaculation
Silodosin (rapaflo)
5-alpha reductase inhibitor drugs (5-ARI)
Finasteride (Proscar)
Dutasteride (Avodart)
he only agents that provide LONG TERM DECREASE IN PROSTATE SIZE and decreased need for prostatic surgery
5- ARIs
5-ARI MOA
- competitive inhibitor of both tissue & hepatic 5-alpha reductase
- 5- alpha reductase converts testosterone to dihydrotestosterone
- by inhibiting 5-alpha-reductase = blocks conversion of testosterone to dihydrotestosterone = suppresses serum dihydrotestosterone levels
⦁ serum dihydrotestosterone decreases by 70%
⦁ serum testosterone increases by 10% - This decreases prostate size
EFFICACY OF 5-ARIs
- may take up to a year to notice reduction in symptoms
⦁ reduction in obstructive symptoms = 23%
⦁ reduction in non-obstructive symptoms = 18% - increase in maximum urinary flow rate
- reduction in mean prostatic volume by about 18%
- decreased need for surgery
- decreased development of acute urinary retention
- the larger the prostate volume, the more effective the medication
- Dutasteride (Avodart) may be more potent than Finasteride (Proscar)
the larger the prostate volume, the more _____________________ (5-ARI)
effective the medication is
which 5-ARI is more potent than the other
- Dutasteride (Avodart) may be more potent than Finasteride (Proscar)
MAJOR SE OF 5-ARIs
⦁ decreased libido
⦁ ejaculatory or erectile problems (ED)
- may only have these SE for the first year of therapy
⦁ decreases serum PSA by 50%
- in the first 24 months of therapy = multiply PSA by 2 when interpreting results - after 24 months of therapy = multiply PSA by 2.5 when interpreting results
what classes/meds are used for treatment of BPH
⦁ Alpha-1 blockers
⦁ 5 alpha-reductase inhibitors
⦁ Combo = Dutasteride-Tamsulosin (Jalyn)
⦁ Tadalafil (Cialis) = 5PDE-inhibitor
PDE5-INHIBITORS SHOULD NOT BE USED WITH
nitrates
alpha-1 blockers
- can cause severe hypotension
MOA of Cialis (PDE5-inhbiitor) for BPH
Cialis blocks PDE5 in the prostate in bladder
- the mechanism of how cialis reduces BPH symptoms is not completely understood
takes ____________ to note symptom improvement with Cialis when used for BPH
2-4 weeks
PDE-5 INHIBITORS (phosphodiesterase inhibitors)
Tadalafil (Cialis)
Vardenafil (Levitra)
Sildenafil (Viagra)
Avanafil (Stendra)
prostaglandin injectable
Alprostadil (Caverject), Muse (pellets) = vasodilator
drug classes/meds used for ED
PDE-5 inhbiitors & prostaglandin injectables (alprostadil)
MOA OF ALPROSTADIL (prostaglandin injectable)
- causes vasodilation by directly acting on vascular & smooth muscle. Relaxes trabecular smooth muscle by dilation of cavernosal arteries when injected along the penile shaft –> allows blood flow to the penis and entrapment of blood flow through veno-occlusive mechanism
onset/duration of action of alprostadil
- Onset = 5-20 minutes
- Duration = < 1 hour
CONTRAINDICATIONS TO PROSTAGLANDIN INJECTABLES (alprostadil)
⦁ conditions that predispose the patient to priapism (painful erection > 4 hrs)
⦁ anatomic or fibrotic conditions of the penis
⦁ For the pellets (Muse) = urethral stricture or perineal pain