When Is The Drug Rasagiline Used?

Rasagiline is a medicine that is used to treat Parkinson’s disease. It can be given as supportive therapy with levodopa or as a treatment on its own. Discover more about this drug and its contraindications today. 

The drug  rasagiline is used to treat Parkinson’s disease. It can be given as supportive therapy in combination with levodopa. The latter is a precursor to dopamine, which is often used as first-line therapy. However, rasagiline can also be prescribed as the treatment on its own.

Parkinson’s disease is a disease of the nervous system  in which the death of certain nerve cells leads to a deficiency in the neurotransmitter dopamine. As a result, movement disorders arise, among other things. Find out today how the drug rasagiline can help in this case.

Mechanism of action of rasagiline

This medicine belongs to a group of selective irreversible monoamine oxidase inhibitors (MAOIs). By inhibiting MAO-B, this drug protects against the extraneuronal breakdown of dopamine  and consequently increases the concentration of this messenger substance in the brain.

That is why rasagiline was used in combination with levodopa from the start. Today this combination is used in patients who suffer from motor fluctuations at the end of the dose.

Dosage and administration of rasagiline

This medicine is given orally at a dose of 1 mg every 24 hours. As mentioned earlier, rasagiline can be used in combination with levodopa or on its own. Patients can take the drug with or without food. No change in dose is necessary in the elderly either.

The drug is not recommended in children as there are no data on its safety and effectiveness in children and adolescents. 

Rasagiline: contraindications

Treatment with rasagiline is not recommended in the following cases:

• In case of hypersensitivity to this drug or an adjuvant of the drug.
• If the patient is already being treated with another MAOI. Some of these drugs or natural remedies do not require a prescription,  such as St. John’s wort. It must be at least two weeks after you stop taking these medicines before rasagiline is administered or any other MAOI or petidine is used.
• In patients with moderate or severe hepatic insufficiency. In addition, special care should be taken at the beginning of treatment with this medicinal product if there is mild hepatic insufficiency. If the liver failure worsens, treatment must be discontinued. 

Interactions with other drugs and other consequences

As mentioned earlier, treatment with rasagiline in combination with other MAOIs or with antidepressants is contraindicated. Some examples:

• Natural antidepressants like St. John’s wort
• Serotonin Reuptake Inhibitors (SRI)
• Serotonin norepinephrine reuptake inhibitors (SSNRIs)
• Tricyclic and tetracyclic antidepressants

In addition, the combination with sympathomimetics, which are used, for example, in drugs that are used for inhalation in asthma, is not recommended. Drugs for colds that contain ephedrine or pseudoephedrine should also not be combined with rasagiline. 

Contraindications are also present with the simultaneous administration of rasagiline and dextromethorphan.

The enzyme cytochrome P450 (CYP450) is involved in the metabolism of most drugs. In vitro metabolic studies indicate that the isoenzyme of cytochrome P450 1A2 / CYP1A2) is the most important enzyme in the metabolism of rasagiline.

Co-administration of this drug with ciprofloxacin (CYP1A1 inhibitor) can alter the blood concentrations of rasagiline and should therefore be used with caution.

There is also a risk  that the blood level of rasagiline may decrease in smokers due to the induction of the metabolic enzyme CYP1A2.

Administration during pregnancy?

There are currently no clinical data on the possible effects of rasagiline use during pregnancy. Studies in animal models  indicate that there are no direct or indirect effects that could be harmful during pregnancy or affect fetal development, parturition or postpartum development. 

However, precautions must be  extreme when prescribing rasagiline to a pregnant woman. This medicine could affect breast-feeding because experimental data show that the medicine can inhibit the secretion of prolactin.

However, it is not known whether this active ingredient passes into breast milk. Therefore, great caution should be exercised with pregnant and breastfeeding women.