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33 Cards in this Set

  • Front
  • Back
Probability of having some form of ED for men aged __ yrs. or older is about 55%.
Probability of having some form of ED for men aged 40 yrs. or older is about 55%.
ED is Usually defined as______,_____, or _____
psychogenic, organic or mixed
Erection involves _____________ of cavernosal smooth muscle whereas detumescence involves ________
relaxation

contraction
Transmitter of the NANC system
NO
GTP is converted to cGMP by what?
activated guanylyl cyclase

(activeated by NO)
cGMP causes erection. cGMP is converted to GMP by what?
PDE 5
What inhibits PDE 5 to allow for more cGMP to stick around?
sildenafil
Neurotransmitters/neuromodulators involved in penile smooth muscle relaxation:
Acetylcholine
Nitric Oxide
Vasoactive intestinal polypeptide
Prostaglandin E1
Calcitonin gene-related peptide
Neurotransmitters/neuromodulators involved in penile smooth muscle contraction:
Norepinephrine
Endothelin-1
Neuropeptide Y
ATP
What is better for the high risk (cardio, endo) pt?

a) sildenafil
b) sildenafil apomorphine
sildenafil apomorphine
Potential risk factors for ED
Aging
Smoking
Hypertension
Hyperlipidemia
Diabetes mellitus
Vascular disease
Depression
Variety of drugs
Antihypertensives that can cause erectile dysfunction
Clonidine, methyldopa, hydrochlorothiazide, beta adrenoceptor antagonists
Psychotropics that can cause erectile dysfunction
Monoamine oxidase inhibitors, tricyclic antidepressants, phenothiazines, benzodiazepines
CNS depressants that can cause erectile dysfunction
Sedatives, narcotics, ethanol, anxiolytics
Miscellaneous Drugs that cause erectile dysfunction
Atropinics, estrogens, cimetidine, anticancer drugs
Traditionally (direct intracavernosal injection)
P_________: Direct relaxation of cavernosal smooth muscle due to action on intracellular calcium levels. May also be a contribution from inhibition of PDE.
Ph________________: irreversible alpha receptor antagonist.
Traditionally (direct intracavernosal injection)

Papaverine: Direct relaxation of cavernosal smooth muscle due to action on intracellular calcium levels. May also be a contribution from inhibition of PDE.
Phenoxybenzamine: irreversible alpha receptor antagonist.
Papaverine and Phenoxybenzamine

Their monotherapy largely discontinued - high incidence of penile _________ & penile f_______ nodules
Papaverine and Phenoxybenzamine

Their monotherapy largely discontinued - high incidence of penile fibrosis & penile fibrotic nodules
direct intracavernosal injection

In several countries a Trimix strategy widely used (mixture of ph________, p___________ & ____). Pharmacologic synergy = lower dose results in reduction in incidence of penile fibrosis.
The use of _____ as monotherapy exceeds the use of all other injectables.
direct intracavernosal injection

In several countries a Trimix strategy widely used (mixture of phentolamine, papaverine & PGE1). Pharmacologic synergy = lower dose results in reduction in incidence of penile fibrosis.
The use of PGE1 as monotherapy exceeds the use of all other injectables.
PGE1 (__________)
PGE1 (alprostadil)
PGE1: Prime action is on _________ mobilization, but there may also be a prejunctional action affecting neurotransmitter release.
PGE1: Prime action is on calcium mobilization, but there may also be a prejunctional action affecting neurotransmitter release.
Attempt to reduce the pain at injection site –____________ delivery system developed for alprostadil. (decreased responder rate & magnitude of response, high incidence of urethral burning & itching)
Attempt to reduce the pain at injection site –intra-urethral delivery system developed for alprostadil. (decreased responder rate & magnitude of response, high incidence of urethral burning & itching)
Sildenafil only works under conditions of______________
sexual stimulation.
Pharmacokinetics (Time to peak conc):

Sidenafil (VIAGRA)

Vardenafil (LEVITRA)

Tadalafil (CIALIS)
Sidenafil (VIAGRA) 60 min

Vardenafil (LEVITRA) 50 min

Tadalafil (CIALIS) 120 min
Pharmacokinetics (Half-life)

Sildenafil

Vardenafil

Tadalafil
Sildenafil 3-4 hours

Vardenafil 4-5 hours

Tadalafil 18 hours
Pharmacokinetics (Food interaction)
Sildenafil

Vardenafil

Tadalafil
Pharmacokinetics (Food interaction)
Sildenafil YES

Vardenafil YES

Tadalafil NO
All 3 PDE-5 inhibitors are metabolized by the cytochrome ________ enzyme.
P450 3A4
Inhibitors of CYP3A4, such as __________, __________, _____________ will decrease the clearance of these drugs.
cimetidine, ketoconazole and erythromycin
PDE-5 Inhibitors adverse effects
Headache
Flushing
Dyspepsia
Nasal congestion
Disturbances in color vision (loss of blue/green discrimination) reported with sildenafil, probably because of inhibition of PDE-6 (a PDE found in the retina that is impt in color vision). Tadalafil does not appear to disrupt PDE-6.
Concurrent _______ ________ are ABSOLUTELY contraindicated due to the ability of the PDE inhibitors to potentiate the activity of NO
Concurrent organic nitrates are ABSOLUTELY contraindicated due to the ability of the PDE inhibitors to potentiate the activity of NO
PDE5 inhibitors will augment the response to drugs that activate NO synthesis; these are primarily ____________, isosorbide methylnitrate or other nitrate-based medications.This drug interaction can result in life-threatening hypotension due to profound NO mediated vasodilation.
PDE5 inhibitors will augment the response to drugs that activate NO synthesis; these are primarily nitroglycerin, isosorbide methylnitrate or other nitrate-based medications.This drug interaction can result in life-threatening hypotension due to profound NO mediated vasodilation.
______ nitrate, which is sometimes used illicitly, should NEVER be combined with PDE5 inhibitors.
Amyl nitrate, which is sometimes used illicitly, should NEVER be combined with PDE5 inhibitors.
Concurrent treatment with _____ adrenergic antagonists (used to alleviate symptoms associated with benign prostatic hyperplasia) is contraindicated (due to potential hypotension with combination therapy). EXCEPTION: __________ may be used safely with ________.
Concurrent treatment with alpha adrenergic antagonists (used to alleviate symptoms associated with benign prostatic hyperplasia) is contraindicated (due to potential hypotension with combination therapy). EXCEPTION: Tamsulosin may be used safely with tadalafil.
A novel sublingual formulation of the dopamine agonist, ____________, has been developed specifically for treatment of patients with ED. (Nausea is said to subside with continued use.)
A novel sublingual formulation of the dopamine agonist, apomorphine, has been developed specifically for treatment of patients with ED. (Nausea is said to subside with continued use.)