ENVARSUS XR

Tacrolimus 1mg, Oral tablet, extended release

Alcohol

· Severity: Major

· Notes for Consumers: Do not drink alcohol while taking this medication. Drinking alcohol may alter the effects of your medication. Serious side effects may occur. Contact your care team if you experience new or worsening side effects.

· Notes for Professionals: Alcohol-containing 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 upon ingestion of alcohol. The flushing occurred in the face or at the sites of medication application, usually within 5 to 15 minutes of alcohol 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% to 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.

Tacrolimus 1mg, Oral tablet, extended release

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 1mg, Oral tablet, extended release

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.

<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>