Azilect (rasagiline) and Alcohol / Food Interactions

There are 2 alcohol/food/lifestyle interactions with Azilect (rasagiline) which include:

ADJUST DOSE: Coadministration with inhibitors of CYP450 1A2 may increase the plasma concentrations of rasagiline, which is primarily metabolized by the isoenzyme. In 12 healthy volunteers, administration of rasagiline (2 mg/day) with the potent CYP450 1A2 inhibitor ciprofloxacin (500 mg twice a day) resulted in an 83% increase in rasagiline systemic exposure (AUC), with no change in elimination half-life. Because the MAO-B selectivity of rasagiline may diminish with increasing dosage above the recommended range of 0.5 to 1 mg/day, there may be an increased risk of hypertensive crisis and other adverse reactions associated with nonselective inhibition of MAO if the maximum dosage is used in the presence of ciprofloxacin. The interaction has not been studied with other CYP450 1A2 inhibitors.

MANAGEMENT: Rasagiline should be prescribed at a maximum dosage of 0.5 mg/day during coadministration with potent CYP450 1A2 inhibitors such as ciprofloxacin. In patients receiving other, less potent CYP450 1A2 inhibitors, it may be appropriate to initiate therapy at 0.5 mg/day, then increase gradually as needed and as tolerated. Patients should be advised 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.

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.

You should also know about...

Azilect (rasagiline) drug Interactions

There are 688 drug interactions with Azilect (rasagiline)

See also...

• Azilect (rasagiline) Side Effects
• Azilect (rasagiline) Consumer Information

• Drug Interactions Checker

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