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29 Cards in this Set

  • Front
  • Back
what does detumescence mean?
is being flaccid; the oppiste is tumescence: state of being swollen or engorged
what tissues of the penis are involved in erection?
corpora cavernosa
what are the types of erectile dysfunction?
psychogenic, organic, or mixed
explain the main mechanism of an erection.
vasodilation occurs and blood flows into the cavernosal arteries in the corpora cavernosa, blood fills both columns of erectile tissue; this swelling causes the veins to be compressed and blood is not allowed out of the penis
explain the molecular mechanism of an erection.
nitric oxide activates guanylate cyclase; guanylate cyclase is needed to convert GTP to cGMP; cGMP causes smooth muscle relaxation and thus tumescence (aka erection)
what causes detumescence?
PDE5 (phosphodiesterases) degrade cGMP; thus treatments for erectile dysfunction (ie. maintainence of an erection) include inhibiting PDE5
what neurotransmitters are involved in penile smooth muscle relaxation?
ACh, NO, Vasoactive Intestinal polypeptide (VIP), prostaglandin E1, calcitonin gene-related peptide
what neurotransmitters are invovled in penile smooth muscle contraction?
NorE, Endothelin 1, neuropeptide Y, and ATP
list the potential risk factors for ED?
Diabetes, Smoking, aging, hypertension, hyperlipidemia, vascular disease, depression, and variety of drugs
clonidine, methyldopa, hydrochlorothiazide, beta andrenocetpor antagonist are what type of drugs and can cause what?
antihypertensives; ED
MAOI, TCAs, phenothiazines, and benzodiazepines are what can of drugs and can cause what?
psychotropics; ED
sedatives, narcotics, ethanol, and anxiolytics are what type of drugs and can cause what?
CNS depressants; ED
These are other miscellaneous treatments that may cause ER.
atropinics, estrogens, cimetidine, anticancer drugs
in the past this injectable was used and worked by directly relaxing the cavernosal smooth muscles due to the action of intracellular Ca levels.
papaverine (direct intracavernosal injection)
this injectable is an irreversible alpha receptor antagonist (this it keeps it from constricting)
why are the injectables less commonly used today?
high incidence of penile fibrosis and penile fibrotic nodules
what injectable is used more commonly today?
PGE1 (alprostadil); have to give it locally b/c it gets broken down too fast orally and is poorly absorbed
what are PGE1's main MOA?
calcium mobilization and prejunctional action affecting neurotransmitter release
besides the injectable, how else is alprostadil used?
intra-urethral delivery...whew.(high incidence of burning and itching)
what oral drugs utilize the PDEV inhibitor method and work by increasing the amount of cGMP?
sildenafil (Viagra); vardenafil (Levitra); and tadalafil (Cialis) - "-fil the penis"
Name the time to peak, half-life, and whether there are food interactions to sildenafil?
peak=60min; T1/2=3-4hrs; interaction with food= yes
Name the time to peak, half-life, and whether there are food interactions to vardenafil?
peak=50min; T1/2=4-5hrs; interaction with food= yes
Name the time to peak, half-life, and whether there are food interactions to tadalafil?
peak=120min; T1/2=18hrs; interaction with food=no
by what enzyme are the PDE5 drugs metabolized?
P450 3A4
name some inhibitors of CYP3A4?***(bolded)
cimetidine, ketoconazole, erythromycin (thus, these will decrease the clearance and keep the drug in the system longer)
name the side-effects of PDE5.
headache, flushing, dyspepsia, nasal congestion, priaprism (with sildenafil may get blue/green hue since it inihibts PDE6 too which is round in the retina) TADALAFIL*** does not disrupt PDE-6
what is absoultely contra-indicated when taking a PDE5 inhibitor and why***?
any drug containing nitrates; nitroglycerin, isosorbide methylnitrate;amyl nitrate (used illicity) should never be combined either; May cause life-threatening HYPOTENSION
name a possible drug interaction with PDE5 inhibitors?
anything that lowers BP, especially alpha adrenergic antagonists (used with BPH) exception: tamsulosin (Flomax) may be used safely with tadalafil***
what sublingual dopamine agonist is being used in europe to treat ED.
apomorphine - a CNS drug