ED and BPH drugs - Androgen deficiency Flashcards
What are drugs used to treat ED
Oral active phosphodiesterase type 5 inhibitors
* viagra (sildenafil)
* tadalafil (cialis)
* vardenafil (levitra)
What are drugs used to treat BPH
Alpha-1 blockers
* selective and non-selective
what are the non-selective alpha1 blockers
- doxazosin
- prazosin
- terazosin
what are the selective alpha-1 blockers
- alfuzosin
- tamsulosin
what is the MOA of PDE-5 inhibitors
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
What is the PK of PDE5i
varenafil and sildenafil - 30-60 minutes works for 4-5 hours
tadalafil - lasts much longer - up to 36 hours
what are contraindications of PDE5i
nitrates - combo can result in severe hypotension
what are AE of PDE5i
Hypotension, Hot (flushing), Headache, Heartburn
“blue vision” - sildenafil
priapism (rare)
what medications are used to treat BPH
alpha-1 adrenergic antagonists
5 alpha-reductase inhibitors
anticholinergic agents
PDE5-i
what are the alpha-1 adrenergic antagonists
first line therapy for BPH
doxazosin, terazosin, alfuzosin, tamsulosin
what are the 5-alpha-reductase inhibitors
finasteride, dutasteride
what are the anticholinergic agents used for BPH
tolterodine, oxybutynin, darifenacin
what is the MOA of alpha-1 adrenergic antagonists
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
what medications have more effect on alpha1a receptor subtype that is found on smooth muscle of prostate and have less effect on blood pressure
Tamsulosin and alfuzosin
what are the AE of alpha-1 adrenergic antagonists
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)
what is the MOA of 5-ARI meds
inhibits type 2 5-alpha-reductase - interfering with the conversion of testosterone to 5-alpha-dihydrotestosterone (DHT). DHT stimulates prostate growth
what stimulates prostate growth
DHT
what are the uses of 5-ARI meds
reduce:
prostate size
PSA
longer-term risk of acute urinary retention
what are the AE of 5-ARI
erectile dysfunction
decreased libido
abnormal ejaculation
what is the most important androgen in humans
testosterone
what are the physiologic effects of testosterone
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
what drugs are used to treat androgen deficiency
- methyltestosterone
- fluoxymesterone
- testosterone
what are the indications for androgen treatment
primary/secondary hypogonadism
delayed puberty
menopausal symptoms
occasionally used for metastatic breast cancer (ER + inoperable tumors)
What are the contraindications of Methyltestosterone/fluoxymesterone
prostate cancer
women who are or may become pregnant
caution if cardiovascular risk
what are the AE of methyltestosterone/fluoxymesterone
males: priapism, impotence, gynecomastia, BPH
females: masculinization, acne, facial hair
may increase risk of stroke/MI
what are the synthetic androgens
(anabolic androgenic steroids)
Stanozolol
oxandrolone
nandrolone
(and many more)
what are the indications of anabolic steroids
AIDS wasting
low testosterone state
transgender
what are the AE of anabolic steroids
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
