Flashcards in Renal 2 Pharmacology Deck (56)
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1
Male Disorder A1 adrenergic antagonist drugs
Doxazosin
Terazosin
Alfuzosin-BPH only
Tamsulosin-BPH only
Silodosin-BPH only
2
Male Disorder 5a-reductase inhibitor drugs
Finasteride
Dutasteride
3
Erectile Dysfunction Drugs
-phosphodiesterase-5 (PDE5) inhibitors
Sildenafil
Vardenafil
Tadalafil
-can also tx ysubg PGE1
4
Benign Prostatic Hyperlasia (BPH)--what is it? Treatment?
-enlargement obstructs bladder outlet
-Tx using alpha 1 adrenergic antogonists, steroid 5alpha reductase inhibitors, PDE5 inhibitor
5
Lower Urinary Tract Symptoms (LUTS)
-interrupted stream
-hesitation
-frequency
-dribbling
-fullness
-urgency
-weak stream
6
Drugs for symptomatic relief of LUTS
-antagonists of a1 receptors
-Terazosin, Doxasozin, Tamsulosin, Silodosin, Alfuzosin
-Drug class to relax muscle tone
-dynamic remedy
-rapid relief of symptoms ~days
7
a1 adrenoreceptors in blood vessels
a1B more than a1A
8
A1 receptors in prostate
-smooth muscle contraction
-a1A
9
a1 receptors in detrusor
instability
a1D>a1A
10
A1 receptors in spinal cord
-control of urinary function
-a1D
11
Stimulation of genitourinary a1-receptors
mediate bladder outlet obstruction
12
Detrusor instability caused by =
a1D receptors + NE
13
Muscle contraction caused by=
a1A receptors + NE
14
a1 antagonists
-compete with NE
-this mechanism reduces spasm, promotes muscle relaxation and improves urine flow
15
Non-specific a1 antagonists
-Terazosin
-Doxazosin
-Alfuzosin
16
a1 antagonists specific for a1A and/= A1D
-Tamsulosin
-Silodosin
17
Terazosin and Doxazosin
-no uroselectivity
-adverse effects: postural hypotension, titrate 1st dose; fatigue
-Drug interaction with PDE-5 inhibitors
18
Alfuzosin
-uroselective (functional) (doesn't discriminate between subtypes but tends to accumulate in prostate!)
-a1 antagonist
-adverse effects: QT prolongation
-drug interaction with CYP450
-take immediately after meal every day
19
Tamsulosin and Silodosin
-uroselective for a1A and a1D (a1 antagonist)
-adverse effects: reduced ejaculation; intraoperative floppy iris syndrome (IFIS)
-drug interaction with CYP450
20
Avoid alfuzosin in
hepatic impairment
21
Steroid 5a reductase inhibitors (SARI, 5ARI)
-Finasteride
-Dutasteride
-drug class that prevents enlargement and shrinks prostate
-structural remedy (slow BPH progression)
-delayed action-->shrinkage and symptoms relief ~3-6 months
22
Why is the prostate enlarging?
-aging puls dihydrotestosterone
23
Enable prostate epithelium survival and growth
-androgenic steroids, testosterone and dihydrotestosterone (DHT)
-DUT potency ~10x >testosterone
-T converted to DHT via SAR (steroid alpha reductase) types I and II
-hypertrophic prostate has ecess SARII
24
Steroid 5a-reductase (SAR) types I and II convert
serum testosterone to DHT in cells
25
Hypertrophic prostate has excess
SAR-II
26
DHT 'starvation' may cause
epithelial atrophy, shrinkage, gradual relief of LUTS
27
DHT starvation can be caused by
inhibiting SAR II
28
Direct Effects of SAR II Inhibition (Finasteride or Dutasteride)
-testosterone accumulation
-DHT depletion
29
Indirect Effects of SAR II Inhibition
-AR receptor less occupied
-no gene transcription
30
