TACROLIMUS (Generic for PROGRAF)

Tacrolimus 0.1%, Topical ointment

Grapefruit juice

· Severity: Severe

· Notes for Consumers: Avoid grapefruit juice while taking Tacrolimus. Grapefruit and Grapefruit juice increase Tacrolimus blood levels significantly leading to side effects like stomach pain, confusion, trouble passing urine or change in the amount of urine, dizziness, headache, mood changes, nausea, vomiting, tremor, yellowing o eyes or skin, or feeling unusually weak or tired. An interaction with topical Tacrolimus is unlikely.

· Notes for Professionals: Grapefruit and grapefruit juice consumption by patients receiving tacrolimus should be avoided; concurrent use may increase tacrolimus serum concentrations and increase the risk of toxicity. Tacrolimus is a sensitive CYP3A4 substrate with a narrow therapeutic index; grapefruit juice is a strong CYP3A4 inhibitor.

Tacrolimus 0.1%, Topical ointment

Food

· Severity: Severe

· Notes for Consumers: Tacrolimus may be taken with or without food, but it is critical that you always take tacrolimus consistently with or without food to maintain consistent blood levels of this drug. Avoid grapefruit juice while taking Tacrolimus. Grapefruit and Grapefruit juice increase Tacrolimus blood levels significantly leading to side effects like abdominal pain, confusion, decreased urination, dizziness, headache, mood changes, nausea-vomiting, tremor, yellowing of skin or eyes, weakness, or other problems. An interaction with topical Tacrolimus is unlikely.

· Notes for Professionals: The extent of absorption of tacrolimus when given orally with high-fat food is reduced as compared with administration in the fasted state. The systemic exposure (mean AUC) of tacrolimus was decreased by 37% when given with a high-fat meal. The systemic exposure was reduced to a similar extent when tacrolimus was given immediately after or 1.5 hours after meal ingestion as compared with the fasted state. While patients may take tacrolimus with food, it is critical that they always take tacrolimus consistently with or without food to ensure consistent whole blood concentrations.

Tacrolimus 0.1%, Topical ointment

Alcohol

· Severity: Major

· Notes for Consumers: Do not drink alcoholic beverages while taking Tacrolimus extended-release capsules (Astagraf XL). Alcohol may increase blood levels of Astagraf XL and increase the risk of serious side effects. In roughly 3 to 7 out of every 100 persons using topical tacrolimus (Protopic), drinking alcohol may cause the skin or face to become flushed or red and feel hot. Let your prescriber know if you notice such reactions, particularly if they are bothersome. In some cases, your prescriber can recommend a treatment that might lessen the reaction when you drink alcohol socially. If the reaction is particularly uncomfortable, it may be best to limit your alcohol intake.

· Notes for Professionals: Alcoholic beverages should not be consumed while taking the extended-release tacrolimus capsules (Astagraf XL). Concomitant alcohol use may increase the rate of release of tacrolimus and/or adversely alter the pharmacokinetic properties and effectiveness and safety. A flushing syndrome (alcohol intolerance) has been reported in patients treated with topical tacrolimus or pimecrolimus upon ingestion of ethanol. The flushing occurred in the face or at the sites of medication application, usually within 5-15 minutes of ethanol ingestion, and lasted for an average duration of 1 hour. Patients describe redness and warm sensations, which sometimes result in discomfort. The reaction does not appear to occur in all patients; roughly 3-7% report a notable effect. The possible mechanism of the effect is the inhibition of acetaldehyde dehydrogenase, leading to increased acetaldehyde dehydrogenase concentrations in the skin. Aspirin appears useful in attenuation of the reaction in those patients for whom the reaction is bothersome.

<b>DISCLAIMER:</b><em> This drug information content is provided for informational purposes only and is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Patients should always consult their physician with any questions regarding a medical condition and to obtain medical advice and treatment. Drug information is sourced from GSDD (Gold Standard Drug Database ) provided by Elsevier.</em>