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pharmacology 2 > prostate disease and erectile dysfunction > Flashcards

prostate disease and erectile dysfunction Flashcards

(49 cards)

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1
Q

the prostate

A

fibromuscular and glandular organ

tubuloalveolar glands arranged in lobules surrounded by stroke

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2
Q

3 regions of the prostate

A

TZ - surrounds the urethra, forms benign prostatic hyperplasia and 20% of prostate cancers
PZ - most of the prostate tissue - 70% of cancers
central zone

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3
Q

androgen receptor

A

expresses in both stromal and epithelial cells

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4
Q

development of prostate is driven by

A

5a-dihydrotestosterone

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5
Q

DHT

A

dihydrotestosterone
metabolite of testosterone, converted in the prostate by 5a-reductase type 2
more potent than testosterone due to higher affinity for the androgen receptor

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6
Q

5a-reductase

A

2 types

type 2 used in the prostate

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7
Q

benign prostatic hyperplasia

A

nodular overgrowth of both epithelial and fibromuscular components of the periurethral and transition zone of the prostate
androgen dependant and does not predispose to prostate cancer

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8
Q

symptoms of benign prostatic hyperplasia

A

obstructive - decreased force of urinary stream, hesitancy initiating voiding
irritative symptoms - dysuria. frequency, urgency, nocturia

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9
Q

dynamic obstruction

A

prostate, prostate capsule and bladder neck have rash a1-adrengeric sympathetic innervation
tension of smooth muscle mediated by these receptors contributes to both obstructive and irritative symptoms

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10
Q

a1- adrenageric blockers

A

receive rritative and obstructive symptoms

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11
Q

5a-reductase inhibitor

A

finasteride

dutasteride

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12
Q

drugs used to treat BPH

A

alpha adrenergic blockers

5a-reductase inhibitors - finasteride and dutasteride

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13
Q

selective a1-adrenergic blockers

A

prazosin - oldest, short half life, more side effects
terazosn - longer half life
alfuzosin
tamsulosin - selective a1(A)-antagonist, selectivity for the bladder, less postural hypotension

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14
Q

tamsulosin

A
  • selective a1(A)-antagonist, selectivity for the bladder, less postural hypotension
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15
Q

terazosin

A

anger half life than prazosin

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16
Q

a1-adrengergic blockers in BPH side effects

A

usually mild
fall in blood pressure due to vasodilatation
postural hypotension - dizziness, syncope
tiredness
headache
ejaculatory dysfunction (tamsulosin)

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17
Q

5a-reductase nhibtors most effective in men wth

A 
men with larger prostate 
reduce prostate volume 
reduce rate of disease progression  
improve symptoms and urine flow 
decrease incidence of acute urinary retention and requirement for prostate surgery
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18
Q

dutasteride

A

type 1 and type 2
5a-reductase inhibitor
more effective when combined wth alpha blocker (eg. tamsulosin)
prostate volume reduces after 1 month

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19
Q

sexual adverse effects of 5a-reductase inhibits

A

erectile dysfunction
ejaculatory disorders
reduced libido
gynaecomastia

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20
Q

sexual dysfunction with 5a-reductase inhibitors is more common when

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A

used in combination with tamsulosin
when used as a mono therapy most side effects resolve spontaneously with ongoing therapy by 2 years but she effects more likely to be ongoing when used in combination with tamsulosin

21
Q

finasteride

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A

type 2 5a-reductase inhibitor

similar side effect profile as dutasteride

22
Q

androgens and prostate cancer

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A

growth and development of normal prostate and prostate cancer is androgen dependant
anti-androgen therapy induces apoptosis and reduced cell proliferation

23
Q

androgen indépendant growth

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A

inevitable n advanced prostate cancer disease
tumour recurrence and progression
called castrate resistant prostate cancer

24
Q

androgen receptor antagonists

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A

hormonal therapy used for prostate cancer

flutamide, bicalutamide, nilutamide

25
inhibitors of androgen production
hormonal therapy in prostate cancer | GnRH analogues
26
total androgen blockade
combination of GnRH agonist with androgen receptor antagonist provide maximal blockade of androgen receptor activation
27
flutamide
androgen receptor blocker binds competitively with androgen receptor anti androgen side effects - gynaecomastia, hot flashes, libido reduction, reduction in muscle mass and crease in bodily fat
28
enzalutamide
androgen receptor inhibitor binds to receptor with greater affinity than bicalitamide reduces efficiency of androgen receptor nuclear translocation used in more advanced disease - even in castrate resistant prostate cancer
29
cyproterone acetate
a derivative of progesterone competes with DHT for androgen receptor (partial agonist) supplies hypothalamic GnRH secretion may be used in combination with GnRH agonists ant androgen side effects
30
GnRH agonists
endogenous GnRH secretion from hypothalamus is pulsatile continuous GnRH agonist inhibits pituitary LH and FSH secretion, thereby decreasing testosterone may cause an initial flare of disease due to a transient rise in testosterone levels
31
GnRH administered by
subcutaneous injection or IM depot
32
abiraterone acetate
inhibits cytochrome P450 (CYP)17A1 which its an essential enzyme in the biosynthesis of testosterone inhibits androgen production in the testis and adrenal used to treat metastatic castration resistant prostate cancer hypertension and hypokalaemia, abnormal LFTs
33
prostate cancer therapies for skeletal metastasis
zoledronic acid - an intravenous biphopshate denosumab - a monoclonal antibody directed against RANK ligand both are osteoporosis therapies wth reduce skeletal related events hypocalcaemia, osteonecrosis of the jaw
34
erectile dysfunction
inability to develop and maintain an erecton in absence of ejaculatory disorder
35
erectile dysfunction is a risk marker for
future cardiovascular events
36
sexual arousal is activated in
higher cortical centres
37
phosphodiesterase inhibitors
drug therapy for erectile dysfunction sildenafil, vardenafil, tadalafil increased cGMP in response to ntrol oxide release resulting in increased smooth muscle relaxation and vascular engorgement only acts in the presence of sexual stimulation
38
phosphodiesterase 5
breaks down cGMP, the second messenger of NO
39
side effects of PDE 5 inhibitors
headache facial flushing nasal congestion dyspepsia side effects usually mild and transient may increase res of nonarteritic anterior ischaemia optic neuropathy
40
phosphodiesterase subtype selectivity
PDE-6 - in the retina, sildenafil causes blue vision | PDE-11 - skeletal muscle, tadalafil causes muscle and back pain
41
sildenfail
plasma concentration maximal at 30-120 minutes terminal half life 4 hours taken 1 hour prior to sexual activity ingestion after or with a meal slows one of action
42
tadalafil
longer duration of action can be taken as daly medication at a reduced dose food does not interfere with absorption
43
PDE-5 inhibitor contraindications
``` men taking nitrate drugs for heart disease - risk of severe hypotension caution in men with severe CVD severe postural hypotension severe aortic stenosis retinitis pigmentosa ``` introduce with caution in men using alpha blockers
44
efficacy of PDE-5 inhibitors
does not restore erection quality to full normal extent | diabetics and post radial prostatectomy tend to have lower response rates
45
intracavernosal alprostadil
``` 70-80% efficacy use limited by adverse side effects penile pain penile fibrotic changes priaprism - if erection lats longer than 60 minutes ```
46
priapism
if erection last longer than 60 minutes | psuedaephidrine can be given
47
transurethral alprostadil
administered as an intraurethral suppository with the aid of an applicator less effective than intracavernosal injections systemic absorption can result in hypotension side effects - penile pain, bleeding, dizziness, female partner may report vaginal burning or itching
48
testosterone replacement
only works when the individual is androgen deficient
49
non-pharmacological interventions
vacuum devices | penile prostheses

pharmacology 2 (19 decks)

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