ED and BPH drugs - Androgen deficiency Flashcards

1
Q

What are drugs used to treat ED

A

Oral active phosphodiesterase type 5 inhibitors
* viagra (sildenafil)
* tadalafil (cialis)
* vardenafil (levitra)

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2
Q

What are drugs used to treat BPH

A

Alpha-1 blockers
* selective and non-selective

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3
Q

what are the non-selective alpha1 blockers

A
  • doxazosin
  • prazosin
  • terazosin
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4
Q

what are the selective alpha-1 blockers

A
  • alfuzosin
  • tamsulosin
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5
Q

what is the MOA of PDE-5 inhibitors

A

inhibits phosphodiesterase type 5, enhancing effects of nitric oxide-activated in crease in cGMP.
cGMP promotes smooth-muscle relaxation resulting in increase blood flow to the penis

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6
Q

What is the PK of PDE5i

A

varenafil and sildenafil - 30-60 minutes works for 4-5 hours
tadalafil - lasts much longer - up to 36 hours

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7
Q

what are contraindications of PDE5i

A

nitrates - combo can result in severe hypotension

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8
Q

what are AE of PDE5i

A

Hypotension, Hot (flushing), Headache, Heartburn
“blue vision” - sildenafil
priapism (rare)

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9
Q

what medications are used to treat BPH

A

alpha-1 adrenergic antagonists
5 alpha-reductase inhibitors
anticholinergic agents
PDE5-i

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10
Q

what are the alpha-1 adrenergic antagonists

A

first line therapy for BPH
doxazosin, terazosin, alfuzosin, tamsulosin

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11
Q

what are the 5-alpha-reductase inhibitors

A

finasteride, dutasteride

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12
Q

what are the anticholinergic agents used for BPH

A

tolterodine, oxybutynin, darifenacin

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13
Q

what is the MOA of alpha-1 adrenergic antagonists

A

blocks alpha-1 adrenergic receptors in the periphery which result in smooth muscle relaxation
decreases tone in smooth muscle of bladder neck and prostate and improves urine flow

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14
Q

what medications have more effect on alpha1a receptor subtype that is found on smooth muscle of prostate and have less effect on blood pressure

A

Tamsulosin and alfuzosin

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15
Q

what are the AE of alpha-1 adrenergic antagonists

A

orthostatic hypotension
interaction with PDE5-i (exacerbate hypotension)
ejaculatory dysfunction
reflex tachy, HA, dizziness, vertigo, nausea, nassal congestion/rhinitis
intraoperative floppy iris syndrome during cataract surgery (tamsulosin)

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16
Q

what is the MOA of 5-ARI meds

A

inhibits type 2 5-alpha-reductase - interfering with the conversion of testosterone to 5-alpha-dihydrotestosterone (DHT). DHT stimulates prostate growth

17
Q

what stimulates prostate growth

A

DHT

18
Q

what are the uses of 5-ARI meds

A

reduce:
prostate size
PSA
longer-term risk of acute urinary retention

19
Q

what are the AE of 5-ARI

A

erectile dysfunction
decreased libido
abnormal ejaculation

20
Q

what is the most important androgen in humans

A

testosterone

21
Q

what are the physiologic effects of testosterone

A

changes in skin (pubic, axillary, beard)
larynx
skeletal growth and increase in lean body mass
male development and masculinization of females
anabolic effect on muscles and bone mass
erythrocyte production

22
Q

what drugs are used to treat androgen deficiency

A
  • methyltestosterone
  • fluoxymesterone
  • testosterone
23
Q

what are the indications for androgen treatment

A

primary/secondary hypogonadism
delayed puberty
menopausal symptoms
occasionally used for metastatic breast cancer (ER + inoperable tumors)

24
Q

What are the contraindications of Methyltestosterone/fluoxymesterone

A

prostate cancer
women who are or may become pregnant
caution if cardiovascular risk

25
Q

what are the AE of methyltestosterone/fluoxymesterone

A

males: priapism, impotence, gynecomastia, BPH
females: masculinization, acne, facial hair
may increase risk of stroke/MI

26
Q

what are the synthetic androgens

(anabolic androgenic steroids)

A

Stanozolol
oxandrolone
nandrolone
(and many more)

27
Q

what are the indications of anabolic steroids

A

AIDS wasting
low testosterone state
transgender

28
Q

what are the AE of anabolic steroids

A

increase BP, low HDL leading to increased risk of MI/CVA
masculinization in women
testicular atrophy, impotence, infertility in men
premature closure of growth plates
mood swings, psychosis, aggressive behavior
acne
possible increase risk for injury due to weakend CT