Mens Health pt.1 Flashcards
Erectile dysfunction facts ?
Rapidly growing interest in class of drugs
Men living longer and gender gap narrowing
56% men reported some degree of ED -
ED rises sharply with age
What NT is key in cascade of erections?
nitric oxide
you need nitric oxide sysnthesis and parasympathetic innervation to get an erection ( smooth muscle relaxation to allow blood flow into the cavernousum)
there is no relationship between ED and?
testosterone
Six causes of ED?
Vasculogenic (Leriche) - most common and this is the one we treat
Psychogenic - mental, guilty
Hormonal
Drugs
Other (mechanical, surgery, combination)
What is the most common cause of ED?
Vasculogenic most common
ED risk factors and non-pharmacological causes?
alcohol
tobacco
hypercholesterolemia
Phosphodiesterase type 5 (PDE5) Inhibitors examples?
Sildenafil (Viagra)
Tadalafil (Cialis)
Verdenafil (Levitra)
** these rely SMOOTH muscle and allow blood to flow into the v=cavernousum ( they were originally used for HTN)**
Oral phosphodiesterase type 5 (PDE5) inhibitors discovery ?
Discovered while searching for a new antihypertensive agent
Phosphodiesterase type 5 (PDE5) MOA?
Main catalyst responsible for conversion of cGMP (cyclic guanosine monophosphate) to GMP
cGMP - relaxes smooth muscle , these meds increase cGMP
End result of Phosphodiesterase type 5 (PDE5) MOA?
End result is relaxing smooth muscle of the penile arteries and corpus cavernosum resulting in an erection
No drug effect without some type of sexual stimulation ( for it to work)
PDE5s there is no effect w/o?
some type of sexual stimulation
PDE5s require?
Requires intact parasympathetic nervous system and adequate release of nitric oxide
All three PDE5s are all absorbed ______?
orally
___________ inhibited in presence of food
sildenafil (Viagra)
sildenafil Viagra and vardenafil (Levitra) onset action ________ and duration_____.
30-120 min
4 hours
tadalafil (Cialis) onset _____ and duration effect _____
16 min
36 hours
**cialis is the weekended lol but viagra is only 4 hours **
Phosphodiesterase type 5 (PDE5) is metabolized by the ?
liver CYP 450
Phosphodiesterase type 5 (PDE5) Inhibitors : sildenafil and vardenafil ?
4 to 5 hours
Phosphodiesterase type 5 (PDE5) Inhibitors : tadalafil ?
17.5 hours
Tadalafil (Cialis) dosing?
5 mg
PDE5s has generally fewer side effects such as?
Priapism
(painful erection lasting longer than 6 hours), prolonged erection lasting greater
**typically well tolerated medications **
Caution with PDE5s when used with ?
nitrates
** ( if they on these meds then do not give then Nitro cause it can plummet the BP )**
Nitrates lead to ___________ that progresses to cardiac arrest?
hypotension
Nitrates facts?
Antihypertensive
Drop in BP
Additive effect with other drugs
Cause orthostatic hypotension when used with alpha blockers and more so when most blood is going to the penis and not the head)
Tx for ED: injectable prostaglandins?
Alprostadil (Caverject)
_______ ______ are injected directly into the side of the penis and produces an erection
injectable prostaglandins
injectable prostaglandins dilates the ________ of the penis and allows blood to flow to engorge the penis
arteries
How long does it take to get a erection after a injectable prostaglandins? How long does it last?
5 to 15 minutes
The erection will last 30 minutes to an hour or up to orgasm.
If using injectable prostaglandins then a patient must?
A patient must learn to perform a penile self-injection each time he wishes to engage in sexual activity.
Pharmacokinetics of Injectable Prostaglandins?
Rapid absorbed within 10 min
Effects last 1 hour
75% metabolized one-pass lungs
Half-life 5 to 10 minutes
Injectable Prostaglandins adverse reactions?
Localized pain
Priapism
Contraindicated in Peyronie’s disease and penile implants
First dose under direct supervision for duration less than 1 hour
27 to 30 gauge needle proximal dorsal 1/3
BPH facts?
Affects 50% men over 60 and 90% men over 70 years old
Compression urethra caused by prostate enlargement and they get urinary retention and dribbling and hesitancy , decreased caliber, nocrutia,
Drugs Used in the Treatment of Benign Prostatic Hypertrophy?
Alpha blockers
5-Alpha reductase inhibitors
**alpha receptors that are expressed at the base of the bladder and the prostate **
Alpha blockers MOA?
Relax smooth muscle in the prostate gland -
it does not shrink the
prostate
Decrease obstruction of urine flow
Alpha blockers are effective within _ month?
1
Effect ceases when the medication is stopped
Alpha blockers examples?
Terazosin (Hytrin)
Doxazosin (Cardura)
Tamsulosin (Flomax)
Alfuzosin (Uroxatrol)
Prazosin (Minipress)
Alpha blockers have ____________ effects
Anti-hypertensive effects
When prescribing A-blocers, look at other medications that may interact with __?
BP
Alpha-1 meds side effect ?
orthostatic hypotension
What alpha blockers are more selective at prostate and bladder and Less side effects of hypotension?
Newer meds:
tamsulosin (Flomax)
and
alfuzosin (Uroxatrol)
Alpha blocker are well absorbed _____?
orally
Alpha blockers are metabolized by the ?
liver
** ( careful with other drugs that are metabolized with the liver and clotting agents like anticoags, and careful in people with liver disease)**
Alpha blockers side effects?
Hypotension (first dose in clinic or bedtime with discussion about activity)
Headache
Dizziness
Muscle pain
Watch with occasional use of
PDE5 Inhibitors
5-Alpha reductase inhibitors MOA?
Inhibit the conversion of testosterone to dihydrotestosterone, suppressing prostate growth (decrease in prostate volume 30%)
shrink it
5-Alpha reductase inhibitors is effective within?
2 to 6 months
Usually the response is sustained after therapy
5-Alpha reductase inhibitors
examples?
finasteride (Proscar) - most common
dutasteride (Avodart)
5-Alpha reductase inhibitors
are well absorbed ______?
orally
5-Alpha reductase inhibitors
is metabolized by the ?
liver to active metabolites
Drugs Used in the Treatment of Benign Prostatic Hypertrophy Conscientious considerations?
Must consider latest guidelines and literature
Must pay attention to other medications patient is on
May require up to 6months of therapy to show effect. not over night change
Drugs Used in the Treatment of Benign Prostatic Hypertrophy: Family patient education
?
Discuss all medications, OTC, supplement for possible interactions
saw palmetto, ginseng
Drugs Used in the Treatment of Benign Prostatic Hypertrophy FDA cat? and why?
FDA Category X
cause
producing genitalia abnormalities in male offspring
You cannot donate blood if you are on what agents or for 6 months after?
alpha blockers
5 -alpha reductase inhibitors
Drugs Used in the Treatment of Benign Prostatic Hypertrophy considerations if pregnant?
should not be handled by pregnant women - inhibit development of male genitalia in fetus)
Tx of BPH: how long until you see results?
3–6 months
BPH meds are not a ___ , they are only for ?
cure
only for sxs. relief
_________ used in male pattern baldness sold as “Propecia”, its only for androgenic male pattern baldness. this will actually grow hair back
Finesteride
Testosterone Deficiency facts?
Normal decline in older men
Will not enhance vitality (sample begs to differ) and sexual activity ( yes to this)
That’s not what they say on TV?
Hypogonadism term interchanged
Normal aging
Klinefelters syndrome (androgen deficit)
Forms that testosterone is available in?
Oral
Injectables - highest
bioavailability
SL
IM
Transdermal
Usually injectable
There are black market issues with ?
testosterone - steroids
“Low T” clinics - low testosterone clinics
Drugs Used to Treat Testosterone Deficiency clinical uses?
Androgen replacement therapy in the treatment of delayed male puberty
Male hypogonadism -
genetic abnormality
Replacement therapy in cases of deficiency of endogenous hormone
Exogenous testosterone absorption is completely via?
IM administration
99% of exogenous testosterone is bound to ?
hormone globulin
Exogenous testosterone
is metabolized by?
First pass metabolism in liver to active metabolite
Exogenous testosterone
excretion?
Excreted 90% in urine (screening PED’s)
Exogenous testosterone
adverse effects?
CV: HTN
DERM: acne, alopecia
ENDO: breast tenderness, gynecomastia
HEME: leukopenia, suppression of clotting
NEURO: aggression
GI: N/V
GU: impotence, atrophy
MS: weakness
**adverse effects come from overdosing usually **
Exogenous testosterone considerations?
All forms require careful monitoring for side effects
If no visible response in 3–4 months change therapy
If oral form do LFT every 3–6 months
If on testosterone therapy then monitor ?
Lipids
PSA
hematocrit
DRE
and if oral then monitor LFT every 3-6 mo
Testosterone deficiency meds: patient teaching?
Inform patient his age and physical condition may limit results for testosterone
Inform women of child-bearing age not to handle dosage forms
Inform patient must not use if have BPH and abnormal lipid profile - cause it will cause side effects
Inform of need to screen for prostate and breast cancers
Propecia effectiveness?
Less effective when hair loss is temporal or frontal - more effects if it is male pattern baldness pattern
Propecia: New hair is lost after _______ if treatment is discontinued
4–6 months
Propecia: Results are not seen until after ________ of use
2–6 months
Propecia: Can not donate blood until after ______ past last use due to teratogenicity issue
6 months
Propecia causes birth defects in?
women
Testosterone deficit meds are not approved for use in what population?
Pediatric
Testosterone deficit meds are contraindicated in?
women
Testosterone deficit meds: geriatric special population consideration?
Discuss precautionary labeling associated with PDE5 use.
Need dosage adjustment in elderly using BPH drugs
Terazosin (Hytrin) is a ?
reversible selective alpha blocker
Doxazosin (Cardura) has a longer ___ than the others?
HL
Tamsulosin (Flomax) has?
lesser effect on BP than the others.
Will not lower BP.
used a lot with kidney stones
Alfuzosin (Uroxatrol) can cause?
increase QT prolongation
