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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%.
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Probability of having some form of ED for men aged 40 yrs. or older is about 55%.
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ED is Usually defined as______,_____, or _____
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psychogenic, organic or mixed
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Erection involves _____________ of cavernosal smooth muscle whereas detumescence involves ________
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relaxation
contraction |
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Transmitter of the NANC system
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NO
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GTP is converted to cGMP by what?
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activated guanylyl cyclase
(activeated by NO) |
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cGMP causes erection. cGMP is converted to GMP by what?
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PDE 5
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What inhibits PDE 5 to allow for more cGMP to stick around?
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sildenafil
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Neurotransmitters/neuromodulators involved in penile smooth muscle relaxation:
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Acetylcholine
Nitric Oxide Vasoactive intestinal polypeptide Prostaglandin E1 Calcitonin gene-related peptide |
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Neurotransmitters/neuromodulators involved in penile smooth muscle contraction:
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Norepinephrine
Endothelin-1 Neuropeptide Y ATP |
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What is better for the high risk (cardio, endo) pt?
a) sildenafil b) sildenafil apomorphine |
sildenafil apomorphine
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Potential risk factors for ED
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Aging
Smoking Hypertension Hyperlipidemia Diabetes mellitus Vascular disease Depression Variety of drugs |
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Antihypertensives that can cause erectile dysfunction
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Clonidine, methyldopa, hydrochlorothiazide, beta adrenoceptor antagonists
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Psychotropics that can cause erectile dysfunction
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Monoamine oxidase inhibitors, tricyclic antidepressants, phenothiazines, benzodiazepines
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CNS depressants that can cause erectile dysfunction
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Sedatives, narcotics, ethanol, anxiolytics
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Miscellaneous Drugs that cause erectile dysfunction
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Atropinics, estrogens, cimetidine, anticancer drugs
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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. |
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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 |
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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. |
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PGE1 (__________)
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PGE1 (alprostadil)
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PGE1: Prime action is on _________ mobilization, but there may also be a prejunctional action affecting neurotransmitter release.
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PGE1: Prime action is on calcium mobilization, but there may also be a prejunctional action affecting neurotransmitter release.
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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)
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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)
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Sildenafil only works under conditions of______________
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sexual stimulation.
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Pharmacokinetics(Time to peak conc):
Sidenafil (VIAGRA) Vardenafil (LEVITRA) Tadalafil (CIALIS) |
Sidenafil (VIAGRA) 60 min
Vardenafil (LEVITRA) 50 min Tadalafil (CIALIS) 120 min |
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Pharmacokinetics(Half-life)
Sildenafil Vardenafil Tadalafil |
Sildenafil 3-4 hours
Vardenafil 4-5 hours Tadalafil 18 hours |
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Pharmacokinetics(Food interaction)
Sildenafil Vardenafil Tadalafil |
Pharmacokinetics(Food interaction)
Sildenafil YES Vardenafil YES Tadalafil NO |
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All 3 PDE-5 inhibitors are metabolized by the cytochrome ________ enzyme.
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P450 3A4
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Inhibitors of CYP3A4, such as __________, __________, _____________ will decrease the clearance of these drugs.
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cimetidine, ketoconazole and erythromycin
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PDE-5 Inhibitors adverse effects
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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. |
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Concurrent _______ ________ are ABSOLUTELY contraindicated due to the ability of the PDE inhibitors to potentiate the activity of NO
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Concurrent organic nitrates are ABSOLUTELY contraindicated due to the ability of the PDE inhibitors to potentiate the activity of NO
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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.
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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.
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______ nitrate, which is sometimes used illicitly, should NEVER be combined with PDE5 inhibitors.
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Amyl nitrate, which is sometimes used illicitly, should NEVER be combined with PDE5 inhibitors.
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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 ________.
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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.
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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.)
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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.)
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