Dopamine agonists
How they work
Dopamine agonists are a class of drug that mimic the effects of
the brain chemical dopamine. These agonists stimulate nerve cells
and produce similar effects to the natural dopamine found in our
brains.
Examples
Commonly prescribed dopamine agonists are:
- pramipexole dihydrochloride (Mirapexin®)
- ropinirole hydrochloride (Requip®)
- pergolide mesilate (Celance®)
- bromocriptine mesylate (Parlodel®)
- cabergoline (Cabaser®, Dostinex®)
- rotigotine (Neupro®)
- apomorphine hydrochloride (APO-go®)
Why they are used
Dopamine agonists may be used alone or in combination with
levodopa to relieve the motor symptoms of Parkinson's.
People who are newly diagnosed with Parkinson's may be
prescribed a dopamine agonist alone. This occurs frequently when
the person is younger than 60 years of age.
Agonists can also be given in combination with levodopa therapy.
This often occurs in people with more advanced Parkinson's, whose
response to levodopa begins to fluctuate, and whose motor symptoms
are not well-controlled.
Taking levodopa for a long time often leads to motor
complications that are difficult to manage. Therefore, by
commencing treatment with a dopamine agonist instead of levodopa,
the onset of levodopa-related motor problems can be postponed.
How they are taken
A variety of dopamine agonists are currently available. These
differ in what form they are delivered, how long their effects
last, and potential side effects.
Most agonists are taken by mouth as tablets or capsules for up
to several times a day. There is also a patch for rotigotine that
is applied once daily onto the skin. Apomorphine is available as a
single injection or as a continuous infusion under the skin.
Advantages
The effects of dopamine agonists tend to last longer than
levodopa. People on agonists are less prone to side effects such as
dyskinesias (uncontrolled movements) and 'on/off' fluctuations.
Agonists are delivered in a range of different forms including:
tablets/capsules; skin patch; injection and continuous supply under
the skin.
Disadvantages
When agonists are used alone, they can be less effective than
levodopa at controlling the motor symptoms of Parkinson's.
Dopamine agonists need to be carefully introduced to minimise
their side effects. Agonists are therefore started at a low dose
and increased gradually until the best benefits are achieved.
Side effects
Common side effects of dopamine agonists include:
- nausea and vomiting
- drowsiness and sudden 'attacks' of sleepiness
- dizziness or fainting due to low blood pressure
- hallucinations and confusion
- existing dyskinesias may become more troublesome
Compulsive behaviour
There is growing evidence that suggests a link between certain
dopamine agonists and compulsive behaviour.
Compulsive behaviour is when a person is unable to resist an
impulse or temptation such as gambling, shopping, eating and sex.
This behaviour performed repetitively, excessively or obsessively
may cause harm to the individual or others.
Studies have shown that compulsive behaviour is an uncommon side
effect. It is currently estimated that up to 14% of people with
Parkinson's taking dopamine agonists experience some form of
compulsive behaviour to varying degrees.
There is also the possibility that some people may become
addicted to their dopamine agonists. These people take increasing
doses despite experiencing side effects.
Read more on compulsive behaviour
Heart valve and lung problems
Recent studies have shown that people taking pergolide
(Celance®) or cabergoline (Cabaser®, Dostinex®) have a higher risk
of heart valve and lung problems than people taking other dopamine
agonists.
Both pergolide and cabergoline are part of a sub-class of drugs
called ergolines. These drugs cause a condition called fibrosis in
various organs of the body. Fibrosis is the hardening of tissues
that can make the organs not work properly.
In 2007, the US Food and Drug Administration (FDA) announced
that manufacturers of pergolide would voluntarily withdraw these
drugs from the market due to concerns over its effect on heart
valves. Pergolide is still available in the UK, however, the use of
the drug is restricted and people are carefully monitored for
adverse side effects.
Apomorphine
Apomorphine is a dopamine agonist that is administered by
(subcutaneous) injection under the skin. When sudden fluctuations
in symptoms occur, in spite of all efforts to adjust medication,
injections of apomorphine may be used - almost like a 'rescue
remedy' - between doses of a person's usual tablets.
Many people self-inject intermittently with a syringe or a
ready-loaded disposable APO-go pen. In some cases, a more
continuous supply of apomorphine is required which is administered
via a pump. This portable, battery-driven syringe pump works by the
insertion of a needle under the skin. It can be injected into the
outside thigh, or into the stomach (below the navel).
Advantages
It acts very quickly and reliably so that people who need to be
active at specific times can continue with their normal
activities.
It can bring great relief to people who are experiencing extreme
variations in mobility and prolonged 'off' periods.
Disadvantages
Apomorphine can only help those people with Parkinson's who show
a response to Sinemet® or Madopar®. It can cause nausea and
therefore another drug called domperidone (Motilium®), which acts
specifically against nausea and sickness, has to be taken in
addition, at least while apomorphine is being introduced.
More information can be found on our Apomorphine information
sheet, available to download from our Publications section
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