Examples
| Generic Name | Brand Name |
|---|
| levodopa/carbidopa | Sinemet, Sinemet CR [controlled-release] |
| levodopa/carbidopa/entacapone | Stalevo |
How It Works
Levodopa is a medicine that the brain
converts to
dopamine.
Carbidopa is a medicine (called
a decarboxylase inhibitor) that, when taken with levodopa, helps prevent the
levodopa from converting to dopamine outside the brain. The combination of
carbidopa and levodopa has several benefits:
- It allows more levodopa to get to the brain and
thus increases the supply of dopamine in the brain.
- It decreases
side effects caused by increased dopamine levels outside the brain by reducing
the supply of “free” dopamine outside the brain. (Increased dopamine levels
outside the brain can result in side effects such as nausea, vomiting, and low
blood pressure.)
- It enhances the effect of levodopa, so that less
levodopa is needed to control symptoms.
Why It Is Used
Levodopa is a medicine used to
control symptoms of
Parkinson's disease and may be used at all stages of
the disease. Although in the past levodopa was often the first drug used to
treat people who were newly diagnosed with Parkinson's disease, more experts
are recommending that initial treatment begin with a dopamine agonist. Levodopa
can then be added when the dopamine agonist no longer controls symptoms
adequately. Treatment with levodopa (or any medicine) should be started only
when symptoms start to significantly affect a person's work or daily
activities.1
Close monitoring is required
for people with certain medical conditions who are taking levodopa. These
medical conditions include:
- Heart and blood vessel
disease.
- Hormone problems.
- Mental
illness.
- Kidney or liver disease.
- Glaucoma.
- Open sores in the stomach lining
(stomach ulcer).
- Skin cancer (melanoma) or undiagnosed skin
sores.
Levodopa/carbidopa may interfere with certain medicines
that are used to treat depression.
How Well It Works
Levodopa is the most effective
medicine for relieving symptoms of Parkinson's disease. It helps reduce tremor,
stiffness, and slowness and helps improve muscle control, balance, and walking.
It does not affect
freezing, dementia, or problems with involuntary
(autonomic) functions, such as constipation, urinary problems, impotence, or
pain.2
Levodopa does not slow the disease
process, but it improves muscle movement and delays severe disability. The use
of levodopa allows people with Parkinson's disease to remain independent and
able to function for longer periods of time. However, the majority of people
taking levodopa develop complications caused by long-term levodopa therapy
within 5 to 10 years. Movement problems (motor fluctuations)
are the most common and troublesome complication.2
Side Effects
Levodopa can cause many side effects,
including:
- Sudden, jerky, uncontrollable movements
(dyskinesias).
- Loss of appetite.
- Nausea and vomiting
with or without stomach pain. Levodopa can be taken after meals at first to
reduce nausea, but as your body adjusts to the medicine and nausea stops, it is
most effective when it is taken 30 minutes before meals or 2 hours after meals
(on an empty stomach).
- Drooling and difficulty
swallowing.
- Increased hand tremor.
- Headache, dizziness,
or fainting.
- Numbness or weakness.
- Grinding of
teeth.
- Confusion, hallucinations (seeing or hearing things that
aren't really there),
delusions, and nightmares. These are more common in
older adults.
- Insomnia, agitation, anxiety, malaise, fatigue, and
euphoria.
- Decreased blood pressure when rising from a seated
position (orthostatic hypotension).
See Drug Reference for a full list of side effects. (Drug
Reference is not available in all systems.)
What To Think About
The question of whether it is
better to use
levodopa or a dopamine agonist as the first treatment
in Parkinson's disease will be different for each person. Levodopa controls
symptoms better than dopamine agonists in most people. And levodopa has fewer
side effects than dopamine agonists. But concern about
levodopa-related motor fluctuations is leading some
experts to recommend initial treatment with dopamine agonists, especially in
people who are younger than 60. As the disease progresses, your doctor may also
prescribe levodopa along with a dopamine agonist. It is important to work with
your doctor to find the medicines that work the best for you.
As
motor fluctuations become more severe, it may be necessary to add another type
of medicine to the person's levodopa treatment. Options include:
- A dopamine agonist (such as bromocriptine, pramipexole, or
ropinirole), which may be used in combination with levodopa to reduce the
amount of levodopa needed and reduce side effects and motor
fluctuations.
- A catechol O-methyltransferase (COMT) inhibitor (such
as entacapone), which may be used if adding a dopamine agonist to levodopa
treatment does not control symptoms and reduce motor fluctuations. Sometimes a
COMT inhibitor may be used from the outset of treatment with levodopa, rather
than waiting until motor fluctuations develop.
- Stalevo, a new
medicine that combines entacapone, levodopa, and carbidopa. This may be more
convenient for some people because they would need to take only one pill
instead of two.
- A monoamine oxidase (MAO) inhibitor (such as
rasagiline or selegiline), that prolongs the effects of dopamine in the brain
by preventing its breakdown. Selegiline may be prescribed in some cases, but it
is not commonly used.
Treating Parkinson's disease with a combination of the
medicines listed above, rather than just increasing the levodopa dose, may
produce a more consistent, longer-lasting effect on symptoms and may result in
fewer motor fluctuations. A neurologist who is experienced in treating
Parkinson's disease is usually best qualified to make these medicine
adjustments.
Using carbidopa with
levodopa reduces side effects such as nausea, decreased appetite, and decreased
blood pressure. The controlled-release form of levodopa (Sinemet CR) also may
cause less nausea. Different people will respond to levodopa/carbidopa for
different lengths of time. However, some people begin to develop side effects
that limit the medicine's effectiveness. The effect of levodopa depends in part
on how much food is in the stomach and the amount of time between taking the
medicine and eating a meal.
Tremor may be less responsive to
levodopa, but it often improves to some degree.
Because of
occasional serious side effects, people taking levodopa/carbidopa should have
regular medical evaluations of their liver, blood, kidneys, and heart. Abruptly
stopping levodopa can cause serious problems and should be avoided.
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