Lurasidone Hydrochloride and alcohol

Avoid consuming grapefruit or grapefruit juice during treatment with lurasidone, as it may increase blood levels of the medication. This can increase the risk of side effects such as Parkinson-like symptoms, abnormal muscle movements, seizures, high blood sugar, diabetes, high cholesterol, weight gain, sex hormone irregularities, and heat-related disorders such as heat intolerance or heat stroke. In addition, you may be more likely to experience side effects associated with low blood pressure such as dizziness, lightheadedness, headache, flushing, fainting, and heart palpitations. You should also avoid the use of alcohol while being treated with lurasidone. Alcohol can increase the nervous system and blood-pressure lowering effects of lurasidone. You may experience increased drowsiness, dizziness, difficulty concentrating, and impairment in thinking and judgment. Talk to your doctor or pharmacist if you have any questions or concerns. Lurasidone should be taken with food consisting of at least 350 calories. Avoid driving or operating hazardous machinery until you know how the medication affects you, and use caution when getting up from a sitting or lying position.

GENERALLY AVOID: Grapefruit juice may significantly increase the plasma concentrations of lurasidone. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. The interaction has been studied with diltiazem, a moderate CYP450 3A4 inhibitor. In a pharmacokinetic study, administration of a single 20 mg dose of lurasidone with diltiazem (extended release formulation 240 mg/day for 5 days) resulted in a 2.1-fold increase in lurasidone peak plasma concentration (Cmax) and a 2.2-fold increase in systemic exposure (AUC) compared to administration alone. In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.

GENERALLY AVOID: Alcohol may potentiate some of the central nervous system and hypotensive effects of lurasidone. Use in combination may result in increased sedation, dizziness, hypotension, and impairment of judgment, thinking, and psychomotor skills.

ADJUST DOSING INTERVAL: Food increases the oral bioavailability of lurasidone. According to the product labeling, lurasidone mean Cmax and AUC were increased approximately 3-fold and 2-fold, respectively, when administered with food relative to under fasting conditions. Lurasidone AUC was not affected by meal size (in the range of 350 to 1000 calories) or fat content. In clinical studies, lurasidone was administered with food.

MANAGEMENT: Patients treated with lurasidone should avoid consumption of grapefruit and grapefruit juice as well as alcohol. Lurasidone should be taken with food (at least 350 calories).