What is vardenafil, and how does it work (mechanism of action)?
Vardenafil is an oral drug that is used to
treat
impotence, the inability to attain or maintain a penile erection. It has a
mechanism of action that is similar to sildenafil (Viagra), and tadalafil (Cialis).
Penile erection is caused by the engorgement of the penis with blood. This
engorgement occurs when the blood vessels delivering blood to the penis increase
in size and increase the delivery of blood to the penis. At the same time, the
blood vessels carrying blood away from the penis decrease in size and decrease
the removal of blood from the penis. Sexual stimulation that leads to the
engorgement and erection causes the production and release of nitric oxide in
the penis. Nitric oxide then activates the enzyme, guanylate cyclase to produce
cyclic guanosine monophosphate (cGMP). The cGMP is primarily responsible for
increasing and decreasing the size of the blood vessels carrying blood to and
from the penis, respectively. Vardenafil prevents an enzyme called
phosphodiesterase-5 (PDE-5) from destroying cGMP so that cGMP persists longer.
The longer cGMP persists, the more prolonged the engorgement of the penis.
Vardenafil was approved by the FDA in August 2003.
What brand names are available for vardenafil?
Levitra, Staxyn ODT
Is vardenafil available as a generic drug?
No
Do I need a prescription for vardenafil?
Yes
What are the side effects of vardenafil?
The most common side effects of vardenafil are facial
flushing (reddening), headaches, stomach upset, diarrhea, flu like symptoms, and
nausea. Vardenafil also may cause chest pain, low blood pressure, blurred vision
and changes in color vision, abnormal ejaculation and priapism (painful erection
lasting more than 6 hours). Patients should seek immediate medical help if they
experience an erection lasting more than 4 hours. Rare cases of sudden loss of
hearing have been reported with phosphodiesterase inhibitors such as vardenafil,
sometimes associated with ringing in the ears and dizziness. If changes in
hearing occur, patients should discontinue their vardenafil and seek immediate
medical attention.
What is the dosage for vardenafil?
For most individuals, the recommended dose of vardenafil
regular tablets is 10 mg per day taken 60 minutes before intercourse. If there
is no response or side effects, the dose may be increased to 20 mg or, if there
are side effects, it may be reduced to 5 mg.
Individuals 65 years of age or
older should begin therapy with 5 mg.
Individuals who are taking medications
that increase the blood levels of vardenafil should start treatment with 2.5 to
5 mg of vardenafil. (See drug interactions.)
Orally disintegrating tablets (ODT)
are not interchangeable with regular vardenafil tablets because they are better
absorbed and produce higher blood levels than regular tablets. The recommended
dosing when using ODT is one tablet 60 minutes before intercourse. Only one
tablet should be used per day. It should be placed on the tongue until it
disintegrates and should not be swallowed with water.
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Which drugs or supplements interact with vardenafil?
The breakdown and elimination of vardenafil from
the body is inhibited by erythromycin, clarithromycin (Biaxin), ketoconazole (Nizoral),
itraconazole (Sporanox), indinavir (Crixivan), ritonavir (Norvir), atazanavir (Reyataz),
grapefruit juice. Therefore, these drugs increase the concentration of
vardenafil in the blood and should not be combined with vardenafil. Vardenafil
reduces the concentration of ritonavir and indinavir and may reduce the effect
these drugs. Vardenafil increases heart rate and also exaggerates blood pressure
lowering effects of nitrates (for example, nitroglycerine). In patients with
chest pain (angina), particularly those who take nitrates,, vardenafil can cause
chest pain by increasing heart rate and lowering blood pressure. Therefore,
patients with angina should not use vardenafil. Vardenafil also exaggerates the
blood pressure lowering effects of alpha-blocking drugs, for example, terazosin
(Hytrin), and should not be used by individuals who also use alpha-blockers.
Vardenafil also adds to the blood pressure reducing effect of other medications.
QUESTION
Erectile dysfunction (ED) is…
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Is vardenafil safe to take if I’m pregnant or breastfeeding?
Vardenafil is not approved for use in women.
Vardenafil has not been evaluated in women who are
breastfeeding.
What else should I know about vardenafil?
What preparations of vardenafil are available?
Tablets: 2.5, 5, 10 and 20 mg. Tablet (orally
disintegrating): 10 mg.
How should I keep vardenafil stored?
Vardenafil should be stored at room temperature between 15-30
C (59-86 F).