Renal 2 Pharmacology Flashcards Preview

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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

Finasteride Selectivity

-specific inhibitor of SAR II