Rasagiline: A Treatment for Parkinson’s

November 7, 2019
Rasagiline is one of the most commonly prescribed treatments for Parkinson's disease. In this article, we're going to tell you more about its effects, pharmacokinetics, and contraindications.

Parkinson’s disease is one of the most common neurodegenerative diseases. Rasagiline, also known under the brand name Azilect, is a highly effective pharmaceutical treatment for this condition. It’s similar to selegiline, and has been proven to improve a patient’s motor function within one day after starting treatment.

According to its data sheet, this medication is good for treating Parkinson’s disease either on its own or in conjunction with other medications such as levodopa. It’s generally most effective on its own during the early stages of the disease. Once the disease has become more advanced, it’s better to combine it with other medications.

The first thing patients will notice is an improvement in motor function. With time, it can also help with the stiffness, bradykinesia, and shaking. Many studies have shown that rasagiline is an effective treatment for Parkinson’s. 

Like we mentioned above, this treatment is most commonly sold under the brand name Azilect. It’s an oral medication that comes in 1-milligram doses once per day, whether they’re also using levodopa or not. There’s no need to adjust the doses, and patients can take it with or without food. They can also use it with other Parkinson’s treatments.

A pill bottle lying on its side.

The mechanism of action of rasagiline

Rasagiline is an irreversible inhibitor of monoamine oxidase-B (MAO-B). What that oxidase enzyme does is catalyze the oxidation of monoamines and the degradation of neurotransmitters such as dopamineThis means rasagiline slows down dopamine metabolism, making it last longer in your synapses, increasing its concentration, and improving motor function.

It also has very powerful neuroprotective properties. Oddly enough, those properties don’t come from its primary mechanism of action. It actually seems to come from a metabolite called aminoindane. This amino acid also happens to have positive effects in terms of Parkinson’s treatment, acting on some of the intracellular signaling pathways related to apoptosis.

Although it’s chemically similar to selegiline, the difference is that it doesn’t metabolize amphetamine derivatives. This means that it has a lower risk of causing negative, heart-related side effects. Some studies have even shown that it’s more powerful. The problem is that it’s almost always more expensive than other drugs.

Side effects

Rasagiline tends to have a good tolerance profile as well. Its side effects aren’t too serious or very intense. According to studies, there are low rates of people who quit the drug due to negative side effects. Those side effects also have a lot to do with how a person takes it. The most common in cases of monotherapy (only using rasagiline) are:

A woman with a headache putting her hands on her temples.

When combined with levodopa (combination therapy), the most frequent negative reactions are:

  • Dyskinesia or abnormal, involuntary movements.
  • Orthostatic hypotension.
  • Weight loss.
  • Decreased appetite.
  • Gastrointestinal issues such as abdominal pain, constipation, nausea, or vomiting. 

One thing you shouldn’t combine with rasagiline are anti-depressants. This combination can have some extremely serious consequences, especially with drugs such as fluoxetine and fluvoxamine. Here are some other types of medications you should never combine rasagiline with:

  • Any other MAO inhibitors, including natural products such as St. John’s wort.
  • SSRIs or selective serotonin reuptake inhibitors.
  • SNRis or serotonin-norepinephrine reuptake inhibitors. 
  • Tricyclic antidepressants.
  • Tetracyclic antidepressants.

You should also avoid taking it alongside any decongestants or cough medications such as dextromethorphan. That means you also need to avoid any anti-mucus build-up treatments because they tend to contain those substances. 

You also have to be careful with patients who have liver issues or liver failure. The liver, in particular, is an organ to pay attention to during rasagiline treatment because the liver absorbs and metabolizes it extremely quickly through cytochrome P450.

As with any medication, rasagiline has its pros and its cons. But overall, it’s a highly effective treatment without overly serious side effects. The main con nowadays seems to be its high cost.

  • Agencia Europea del Medicamento (2019). Ficha técnica. Rasagilina. [Online] Disponible en: https://www.ema.europa.eu/en/documents/product-information/rasagiline-mylan-epar-product-information_es.pdf
  • Gipuzkoa, P. (2008). Rasagilina en la enfermedad de Parkinson. Neurología23(4), 238-245.
  • Pagonabarraga, J., & Kulisevsky, J. (2010). Rasagilina: eficacia y protección en la enfermedad de Parkinson. Rev Neurol51, 535-41.