Rasagiline: What is it? Drug Studies, Side Effects, Precautions and Interactions

It is a propangilamina no amphetamine, which in doses of up to 1 mg once a day, is a selective and irreversible inhibitor of monoamine oxidase B (MAO-B).

The results of preclinical studies in vitro and in vivo have shown that rasagiline increases the release of dopamine in the striatum.

Rasagiline is associated with better results in patients with early and advanced Parkinson’s disease , however, there are some indications that the drug may have effects of disease modification.

It reduces the time of “inactivity” in patients with moderate to advanced disease with motor fluctuations.

It can also help reduce the amount of “off” time (slow periods of movement or stiffness). It is believed that Parkinson’s disease is caused by very little dopamine in the brain.

Drug studies

Large randomized and clinical studies have shown that rasagiline is effective as monotherapy in patients with early Parkinson’s disease and that the early onset of rasagiline is associated with better long-term outcomes compared to delayed therapy.

As an adjunct to levodopa, rasagiline reduces downtime in patients experiencing motor fluctuations (for example, attrition).

In a clinical trial, patients initiated with rasagiline monotherapy at the onset of Parkinson’s disease had a lower functional decline than patients whose treatment was delayed for 6 months.

Using a delayed onset design, the study indicated that rasagiline may also have neuroprotective properties in addition to its symptomatic effects.

In this study, patients treated with 1 mg of rasagiline per day for 12 months showed a lower functional decrease than subjects whose treatment with rasagiline was delayed for 6 months.

This suggests that early initiation with rasagiline (even before the onset of functional deterioration) is associated with better long-term outcomes.

For the management of patients with motor fluctuations, the efficacy of rasagiline seems similar to that of entacapone.

Therefore, when an adjunct agent is required to control motor fluctuations, rasagiline is considered a first-line agent. Rasagiline has an absolute bioavailability of 36% and its main metabolite is 1-R-aminoindan, which lacks effects similar to amphetamines.

Consequently, clinical studies demonstrated good tolerability of rasagiline treatment and found no difference in the frequency of cardiovascular and psychiatric adverse events between patients treated with rasagiline and those treated with placebo.

In general, the data associated with rasagiline to reduce the “disconnect” time are of high quality.

In addition to the demonstrated efficacy in reducing downtime in patients experiencing motor fluctuations while receiving levodopa, rasagiline has shown good tolerability in patients receiving other complementary therapies, a common scenario in the real-world management of Parkinson’s disease. .

Conventional use to reduce “off” time is supported by less robust data quality. However, the selegiline tablet that disintegrates orally appears to offer a similar benefit by reducing rasagiline downtime, although no direct comparative data are available.

Side effects of rasagiline

To reduce the risk of dizziness and lightheadedness, get up slowly after being in a sitting or lying position, especially when you start taking rasagiline for the first time.

Very rarely a very serious reaction to high blood pressure can occur if you consume a large amount of tyramine while taking rasagiline and for 2 weeks after you stop it.

The serotonin syndrome is a life-threatening reaction due to serotonergic overstimulation that occurs, among other characteristics, with changes in mental state, myoclonus and autonomic instability.

Because monoaminooxidases catalyze the oxidation of serotonin, concern has been expressed about the risk of serotonin syndrome in patients taking rasagiline along with other serotonergic agents, and the prospect of the rasagiline list lists antidepressants in this context.

No cases of serotonin syndrome have been reported in rasagiline trials.

Precautions

Before using this medication, tell your doctor or pharmacist your medical history, especially heart disease (such as coronary artery disease, heart attack , chest pain, heart failure ), stroke, high blood pressure , severe / frequent headaches , liver disease.

Also mental / mood disorders (such as schizophrenia, bipolar disorder, depression ), diabetes, overactive thyroid , certain type of adrenal gland tumor ( pheochromocytoma) and sleep disorders.

Interactions of rasagiline with other medications

Interactions with other medications can change how your medications work or increase the risk of serious side effects. Rasagiline should not be used with any of these medications.

Some products that may interact with this medication include diet pills / appetite suppressants (such as diethylpropion), medications for attention deficit disorder (such as atomoxetine, methylphenidate), apraclonidine, bupropion, buspirone, carbamazepine , cyclobenzaprine , deutetrabenazine.

Also, dextromethorphan, methyldopa, certain supplements (such as tryptophan, tyramine), tetrabenazine, certain “triptans” used to treat migraine headaches (such as rizatriptan, sumatriptan, zolmitriptan), valbenazine.

Tell your doctor if you have taken fluoxetine within 5 weeks before starting rasagiline. Ask your doctor how long to wait between starting or stopping any of these medications and starting with rasagiline.

Before using rasagiline, report the use of medications that can increase the risk of extremely high blood pressure (hypertensive crisis) when combined with rasagiline, including herbal products (such as ephedra).

Also allergies and cough and cold products (including dextromethorphan , decongestants such as phenylephrine / pseudoephedrine) and stimulants (such as amphetamines, ephedrine, epinephrine , phenylalanine).

In conclusion, rasagiline can be a relatively ideal drug once a day for the treatment of Parkinson’s disease, both in the early stages as well as in monotherapy and in advanced stages in combination with levodopa. Its effectiveness is equal to that of entacapone.

Rasagiline significantly reduces periods of inactivity in patients with motor fluctuations and improves daily without problem dyskinesias. The drug is well tolerated and does not show adverse events, even after long-term treatment. Rasagiline has the potential to demonstrate clinical neuroprotection.