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EPDA - European Parkinsons Disease Association EPDA - European Parkinsons Disease Association EPDA - European Parkinsons Disease Association EPDA - European Parkinsons Disease Association EPDA - European Parkinsons Disease Association EPDA - European Parkinsons Disease Association EPDA - European Parkinsons Disease Association
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Types of medication available

There are several types of medication used to treat Parkinson’s. What is available to you will depend on the country in which you live.

Most medications have two names. One is a generic name that always uses a small letter and describes the active ingredient in the medication, for example co-careldopa. This is likely to be the universal name of the drug internationally. The other is a brand or trade name by which it is marketed, and there are variations from country-to-country. Brand or trade names always uses a capital letter, for example Sinemet®. The EPDA website has a comprehensive section on the medication currently available to treat Parkinson’s in Europe. See www.epda.eu.com/medinfo

Medications come in various forms: capsules, tablets, patches and some are available in liquid form or dispersible powders for those who have difficulty swallowing. There are also occasions when it is necessary to administer medication by injection or via a small pump. For example, apomorphine is given by injection under the skin or through a small pump which provides a continuous infusion, and Duodopa® is given through a small pump directly into the small intestine.


The medications commonly used to treat Parkinson’s

FAQ
What is the most frequently used drug treatment for Parkinson’s?

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Parkinson's medication at a glance

Generic name Brand name ®

Levodopa
Oral
  • Co-careldopa
  • Co-beneldopa

Infusion

  • Co-careldopa

Dopamine agonists
Oral
  • Bromocriptine
  • Cabergoline
  • Lisuride
  • Pergolide
  • Pramipexole
  • Ropinirole

Transdermal

  • Rotigotine

Subcutaneous

  • Apomorphine
Generic name Brand name ®

COMT inhibitors

  
  • Entacapone
  • Tolcapone
  • Co-careldopa / entacapone combination

 MAO-B inhibitors

  
  • Selegiline
  • Rasagiline

Anticholinergics

  
  • Benztropine
  • Orphenadrine
  • Procyclidine
  • Trihexyphenidyl (formerly benzhexol)

 Amantadine

  
  • Amantadine

Levodopa

Dopamine is unable to cross the blood-brain barrier and a dopamine replacement treatment, known as levodopa, is administered which then converts to active dopamine in the brain. This reverses many of the disabling motor symptoms of Parkinson’s.

Levodopa preparations invariably contain a decarboxylase inhibitors (DCI), for example co-careldopa (Sinemet®) and co-beneldopa (Madopar®). DCIs prevent levodopa breakdown outside the brain, making each dose more effective so that much lower amounts of levodopa can be given, avoiding many side effects1 .  For more than 80% of people first treated with this combination, an excellent or good response can be expected.

Side effects may include nausea and vomiting, lowering of blood pressure on standing, psychological symptoms and drowsiness. It may be necessary to gradually increase the dosage over time to avoid or reduce these adverse effects.

In the early years of levodopa treatment, control of symptoms is usually good. Over time, however, wearing off effects and fluctuations in symptom control become evident and are associated with the development of dyskinesia (involuntary movements). These were thought to begin typically between three to five years after treatment begins. But recent research has revealed that it can happen earlier – with one out of three patients experiencing wearing off within one to two years of taking levodopa2. This is believed to be the result of long term levodopa treatment combined with continued neurodegeneration. At this stage, it will often be necessary to make adjustments to minimise the wearing off effects. For example, the use of longer-acting formulations (Sinemet®CR, Madopar®SR) or water-soluble preparations (e.g. Madopar®dispersible) may be required, or changes made to the frequency and dosages of standard drugs.

It is thought that as many as 50% of people experience levodopa-related motor problems after five years of sustained therapy. This may relate to levodopa’s short half-life and erratic absorption from the bowel, which leads to blood level fluctuations. These result in discontinuous and pulsatile stimulation of dopamine receptor and influence brain cell functioning, believed to play a part in long term levodopa motor complications.1 The use of long acting levodopa formulations, subcutaneous infusion and continuous transdermal dopamine agonist therapy, all lead to more sustained dopaminergic stimulation of the dopamine receptors.3

Duodopa®

Duodopa®, an intestinal gel containing levodopa and a decarboxylase inhibitor, may also be prescribed. This is administered directly into the small intestine from an external enteral tube. It is currently used in some centres to treat severe cases of Parkinson’s that are dopamine responsive, but inadequately controlled by other preparations. Clinical experience in Sweden, the Netherlands and the UK is encouraging and suggests that Duodopa allows more sustained levels of dopamine to reach the appropriate nerve cells.3


For further information on levodopa see  www.epda.eu.com/medinfo/levodopa

Dopamine agonists

Dopamine agonists imitate or mimic levodopa’s action by directly stimulating the brain’s dopamine receptors. Although not quite as effective as levodopa, they can provide good symptom control and may delay the onset of motor complications associated with long term levodopa use. The most common dopamine agonists prescribed are:

  • apomorphine - given by subcutaneous injection and begins to work very quickly, in ten minutes or so. But whereas the effects of levodopa are felt between two to four hours, apomorphine wears off after about ninety minutes.
    Isolated, single doses may be used to treat the wearing off effects of levodopa, or sudden ‘off’ periods, and other people may require daily injections4
  • rotigotine (Neupro®) – a soluble dopamine agonist that can penetrate the skin and provide sustained dopamine levels over 24 hours when administered as a patch.  Used both in early and late stages of Parkinson’s to smooth out motor fluctuations associated with taking levodopa. It is a user-friendly and convenient ‘once daily’ therapy
  • ergot-derived formulations (bromocriptine, lisuride, pergolide and cabergoline) - older dopamine agonist drugs that have an ergot derived structure. Ergot is a fungus that the first dopamine agonist medications were derived from. Pulmonary, retroperitoneal fibrosis and fibrosis of heart valves are very rare complications of the use of these drugs. In the UK, people with Parkinson’s are no longer prescribed them and they have been withdrawn from most people previously taking them
  • non-ergot preparations (apomorphine, pramipexole and ropinirole) - newer, non-ergot drugs. Clinical trials have demonstrated their ability to delay motor complications when used in the early stages of Parkinson’s. Side effects tend to be higher than levodopa and include more peripheral limb swelling and psychological symptoms.
In general, people who are under 70 and otherwise healthy may initially be treated with a dopamine agonist. However, most will be receiving or eventually need levodopa.1


For further information on dopamine agonists see  http://www.epda.eu.com/medinfo/dopamineAgonists

FAQ
I have been told that I may need to use a syringe driver for my apomorphine injections. What is a syringe driver?

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FAQ
My consultant wants me to take apomorphine, but I am worried that it may be addictive. What should I do?

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Important!

Drowsiness and/or sudden sleep episodes are potential adverse effects of all dopaminergic medications, particularly when doses are being increased or changed.

Catechol-O-Methyl Transferase (COMT) inhibitors

COMT inhibitors prolong the effects of levodopa doses by preventing the breakdown of the drug in the brain. The preparations available, entacapone (Comtess®, Comtan®) and tolcapone (Tasmar®), can decrease the length of ‘off’ times and may allow levodopa doses to be reduced.

Stalevo®, a tablet containing levodopa, carbidopa and entacapone is prescribed for people experiencing ‘end of dose’ motor fluctuations using standard levodopa/carbidopa combinations.


For further information on COMT inhibitors  see www.epda.eu.com/medinfo/COMTInhibitors

Monoamine-oxidase B (MAO-B) inhibitors

MAO-B inhibitors slow the breakdown of dopamine in the brain to produce more sustained effects. Selegiline (Elderpryl®and Zelapar®) and rasagiline (Azilect®) are the medications available and they are recommended for people who experience ‘end of dose’ deterioration when taking levodopa/carbidopa combinations. Rasagiline may also be used on its own in early Parkinson’s.

It has been suggested that MAO-B inhibitors may offer potential neuroprotection to brain cells but this is unproven. 


For further information on MAO-B inhibitors see www.epda.eu.com/medinfo/MAO-Binhibitors

Anticholinergic drugs

Anticholinergic drugs are older drugs that reduce the effects of acetylcholine, a neurotransmitter in relative excess in the brains of people with Parkinson’s due to dopamine depletion. They reduce tremor and rigidity, can have positive effects on drooling, but have little effect on bradykinesia (slowed ability to start and continue movements). Side effects, such as memory impairment and other neuropsychiatric complications limit their use, particularly in the elderly.


For further information on anticholinergics  see www.epda.eu.com/medinfo/anticholinergics

Amantadine

Amantadine is an old drug with weak dopamine agonist effects. It improves mild slowness, tremor and stiffness, and recent research suggests it is effective in treating dyskinesias that result from taking levodopa. It may, however, cause side effects such as hallucinations, insomnia, ankle swelling and skin mottling.


For further information on amantadine  see www.epda.eu.com/medinfo/amantadine

Did you know?

The biggest challenge to medieval medicine came in the form of the Bubonic Plague, a form of highly contagious and fatal pneumonia. In 1347, there was an outbreak in Constantinople (modern day Istanbul) and traders carried the disease throughout Europe. During the middle ages, the only treatments were superstitious remedies, prayer, herbal medicines and recipes for clearing the air of miasma or poison.

 

References


  1. Jankovic JJ. Therapeutic strategies in Parkinson’s disease. In: Jankovic JJ and Tolosa E (Eds). Parkinson’s disease and movement disorders. Philadelphia: Lippincott Williams and Williams, 2002: 116-51.
  2. Parkinson Study Group. Pramipexole vs levodopa as initial treatment for Parkinson’s disease. JAMA 2000; 284: 1931-1938; Parkinson Study Group.  Entacapone improves motor fluctuations.
  3. Wolters E. Deep brain stimulation and continuous dopaminergic stimulation in advanced Parkinson’s disease. Parkinsonism Related Disord 2007; 13(Suppl): S18-23.

  4. Colzi A, Turner K and Lees A. Continuous subcutaneous waking day apomorphine in the long term treatment of levodopa induced interdose dyskinesias in Parkinson’s disease. J Neurol Neurosurg Psychiatry 1998; 64(5): 573-76.

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