Rasagiline: Under What Conditions Is It Prescribed?
Rasagiline is prescribed for the treatment of Parkinson’s disease (PD). It can be used in adjunctive therapy with levodopa – a dopamine precursor that began as the treatment of choice for Parkinson’s disease – or as monotherapy without levodopa.
Parkinson’s disease is a type of movement disorder that occurs when neurons do not make enough of a very important brain chemical known as dopamine. Here’s how rasagiline helps.
Mechanism of action of rasagiline
This drug is a selective MAO-B inhibitor. The inhibition of MAO-B protects dopamine from extraneuronal degradation, increasing its concentration in the brain. For this reason, it was initially used as a complement to levodopa and, today, it is used in combination in patients with motor fluctuations at the end of the dose.
Dosage and method of administration
The form of administration is orally, at a dose of 1 mg every 24 hours, alone or in combination with levodopa. It can be taken with or without food. In elderly patients, no dosage modification is necessary.
In the pediatric population, rasagiline is not recommended due to lack of safety and efficacy data in children and adolescents.
When is rasagiline contraindicated?
Rasagiline treatment is contraindicated in the following cases:
- When there is hypersensitivity to the active principle or to any of the excipients.
- When there is already treatment with a monoamine oxidase (MAO) inhibitor. This includes medicines and natural products not subject to medical prescription, such as St. John’s Wort. At least 14 days must elapse between stopping rasagiline and starting treatment with MAO inhibitors or pethidine.
- In patients with moderate and severe hepatic impairment. In addition, special caution should be exercised when initiating treatment with rasagiline in patients with mild hepatic impairment. If mild to moderate liver failure progresses, treatment interruption will be necessary.
Interaction with other medicinal products and other forms of interaction
As we have already mentioned, the administration of rasagiline with other MAO inhibitors or antidepressants is contraindicated:
- Natural antidepressants like St. John’s Wort.
- SSRI – selective serotonin reuptake inhibitors.
- SNRI – norepinephrine and serotonin reuptake inhibitors.
- Tricyclic and tetracyclic antidepressants
It is also not recommended in concomitant administration with sympathomimetic drugs, such as those found in nasal and oral decongestants, or in anticatarrhal drugs that contain ephedrine or pseudoephedrine.
Concomitant administration of rasagiline and dextromethorphan is contraindicated .
The enzyme cytochrome P450 (CYP450) is involved in the metabolism of most drugs. In vitro metabolism studies indicated that the cytochrome P450 1A2 (CYP1A2) isoenzyme is the main enzyme responsible for the metabolism of rasagiline.
Co-administration of rasagiline and ciprofloxacin, an inhibitor of CYP1A2, can alter plasma concentrations of rasagiline and should therefore be administered with caution.
Furthermore, there is a risk that the plasma levels of rasagiline in smoking patients may be decreased, due to the induction of the metabolizing enzyme CYP1A2.
What adverse reactions can it produce?
In the following list we detail the most frequent adverse reactions:
- Flu or infections caused by the influenza virus
- Skin carcinoma
- Leukopenia
- Allergy, rhinitis or conjunctivitis
- Decreased appetite
- Depression, hallucinations
- Headache
- Vertigo
- Angina pectoris
- Dermatitis
- Flatulence
- Urination urgency
- Fever or malaise
- Musculoskeletal pain, neck pain, and arthritis
Is it indicated during pregnancy?
Currently, there are no clinical data on exposure to rasagiline during pregnancy. Studies in animal models do not indicate direct or indirect harmful effects on pregnancy, embryo-fetal development, parturition or postnatal development.
However, extreme caution should be exercised when prescribing rasagiline to pregnant women. Rasagiline may interfere with lactation, since according to experimental data, rasagiline inhibits prolactin secretion.
However, it is unknown whether rasagiline is excreted in human milk. Therefore, precautions should be increased when administered in lactating women.
