Rasagiline Mesylate and Food

Rasagiline may be taken with or without food. There is no need to avoid most foods and beverages during treatment with rasagiline, as long as you are not receiving more than 1 mg per day of the medication. However, certain foods such as some of the aged cheeses (for example, Boursault, Liederkrantz, Mycella, and Stilton) may contain very high amounts of tyramine and should generally be avoided if possible. Consumption of very high levels of tyramine (greater than 150 mg) while on rasagiline treatment may lead to dangerous increases in your blood pressure, a condition known as hypertensive crisis. Talk to your doctor or pharmacist if you are uncertain about what foods, if any, to avoid. You should seek immediate medical attention if you experience sudden and severe headache, blurred vision, confusion, seizures, chest pain, nausea or vomiting, sudden numbness or weakness (especially on one side of the body), speech difficulties, fever, sweating, lightheadedness, and/or fainting during treatment with rasagiline, as these may be signs and symptoms of a hypertensive crisis. It is important to tell your doctor about all other medications you use, including vitamins and herbs, since some medications may increase the blood levels of rasagiline and possibly lead to interactions with tyramine-rich foods. Do not stop using any medications without first talking to your doctor.

GENERALLY AVOID: Foods that contain large amounts of tyramine may precipitate a hypertensive crisis in patients treated with monoamine oxidase (MAO) inhibitors. The mechanism involves inhibition of MAO-A, the enzyme responsible for metabolizing exogenous amines such as tyramine in the gut and preventing them from being absorbed intact. Once absorbed, tyramine is metabolized to octopamine, a substance that is believed to displace norepinephrine from storage granules. Although rasagiline is a selective inhibitor of MAO-B at the recommended dosages of 0.5 or 1 mg/day, selectivity is not absolute and may diminish with increasing dosage. There were no cases of hypertensive crisis in the clinical development program associated with rasagiline treatment at 1 mg/day, in which most patients did not follow dietary tyramine restriction. However, rare cases of hypertensive crisis have been reported during the postmarketing period in patients who ingested unknown amounts of tyramine-rich foods while taking recommended dosages of rasagiline or selegiline, another MAO-B inhibitor.

Rasagiline peak plasma concentration (Cmax) and systemic exposure (AUC ) are decreased by approximately 60% and 20%, respectively, during coadministration with a high-fat meal. The time to peak concentration (Tmax) is not affected by food.

MANAGEMENT: Dietary restriction is not ordinarily required during rasagiline treatment with respect to most foods and beverages that may contain tyramine such as air-dried and fermented meats or fish, aged cheeses, most soybean products, yeast extracts, red wine, beer, and sauerkraut. However, certain foods like some of the aged cheeses (e.g., Boursault, Liederkrantz, Mycella, Stilton) may contain very high amounts of tyramine and could potentially cause a hypertensive reaction in patients taking rasagiline even at recommended dosages due to increased sensitivity to tyramine. Patients should be advised to avoid ingesting very high levels of tyramine (e.g., greater than 150 mg), and to promptly seek medical attention if they experience potential signs and symptoms of a hypertensive crisis such as severe headache, visual disturbances, confusion, stupor or coma, seizures, chest pain, unexplained nausea or vomiting, and stroke-like symptoms. Rasagiline should not be used at dosages exceeding 1 mg/day (0.5 mg/day for patients with mild hepatic impairment or concomitant use of ciprofloxacin or other CYP450 1A2 inhibitors), as it can increase the risk of hypertensive crisis and other adverse reactions associated with nonselective inhibition of MAO. Rasagiline can be administered with or without food.