Compounded Tacrolimus

Tacrolimus is a prescription medicine in a class called calcineurin inhibitors. When it is applied to one area of the body, it calms the immune activity in that area. Its main appeal is that it is steroid-sparing: unlike topical corticosteroids, tacrolimus does not thin the skin, so it can be used on delicate places like the face, eyelids, skin folds, and the ear canal, and over longer stretches of time.

Commercially, tacrolimus is sold as a topical ointment (0.03% and 0.1%) for atopic dermatitis, and as capsules, granules, and an injection for preventing organ transplant rejection. Bayview compounds tacrolimus in the forms that no manufacturer makes — otic (ear) solutions, rectal enemas, anhydrous gels, creams, foams, and shampoos — to your prescriber's order.

Compounded preparations are not FDA-approved. A valid prescription is required, and Bayview Pharmacy does not provide consultations or determine whether a medication is appropriate for you.

How does it work?

Inflammation in conditions like eczema is driven largely by immune cells called T cells. To switch on, a T cell needs an internal signal relayed by an enzyme called calcineurin. Tacrolimus blocks calcineurin, so the T cell never gets the message, and the chemical signals that cause redness, swelling, and itch are turned down.

Because it is applied where the problem is, tacrolimus acts mostly at that spot. Very little is normally absorbed into the bloodstream through skin — though absorption goes up when skin is broken or inflamed, and it is more of a consideration for the rectal route (more on that below). Unlike a corticosteroid, tacrolimus does not cause skin thinning, stretch marks, or the visible small blood vessels that can follow long steroid use, which is why prescribers reach for it on the face, eyelids, skin folds, and ear canal.

What is it used for?

The only FDA-approved topical use is moderate to severe atopic dermatitis (eczema), as a second-line therapy for short-term and non-continuous treatment in people who did not respond well to other topical prescription treatments or for whom those are not advisable. Everything else on this page is off-label, and the quality of the supporting evidence varies a lot by route. We think you should know which is which.

• Ear (otic solution) — chronic otitis externa and eczema of the ear canal. The ear canal is thin-skinned and easily damaged by repeated steroid drops, so a steroid-sparing option is attractive. The evidence here is limited to small studies and case series, not large randomized trials. There is no FDA-approved otic tacrolimus.
• Rectal enema — ulcerative proctitis and distal ulcerative colitis that has not responded to standard treatment. This route has the most supportive off-label evidence of the group, but it is still small. A double-blind placebo-controlled trial of rectal tacrolimus in resistant ulcerative proctitis reported clinical response in 73% of patients versus 10% on placebo, and was stopped early after only 20 patients because the benefit appeared so clear — which is encouraging, but 20 patients is a small trial. A retrospective series of 23 patients found about half achieved remission (Cohen & Weisshof, Gastroenterology & Hepatology, 2020). A 2024 review concluded the data “are supportive of the use of topical tacrolimus in selected patients” while pointing out that most reports were retrospective, open-label, short, and small (Khayatan, Lemberg & Day, J Clin Med, 2024).
• Oral lichen planus. A gel or rinse applied to sore mouth lesions. Supported by open-label trials and comparative studies rather than large definitive ones.
• Vitiligo, especially on the face and neck, where topical tacrolimus is a common steroid-sparing choice. Response is slow, partial, and not guaranteed.
• Scalp inflammation and alopecia areata (shampoo and foam). This is the weakest evidence of the group — largely case reports and small series. Combination foams such as minoxidil with tacrolimus and clobetasol are prescriber-designed formulas, not studied products. If your prescriber orders one, ask what result they are hoping for and by when.

How do the strengths and forms compare?

Tacrolimus is compounded in several strengths, bases, and combinations depending on where it needs to go. The table below is for education only; your prescriber selects the form and strength.

Preparations are described for education only and are not a statement that any form or strength is better for a particular person. Your prescriber selects the preparation, strength, and schedule.

How is it used?

Use tacrolimus exactly as your prescriber directs, and only on the area they specify. Wash your hands before and after, unless your hands are the area being treated.

• Skin (gel, cream, ointment). Apply a thin layer to the affected area, usually twice a day. Do not cover the area with bandages or occlusive wraps unless your prescriber tells you to — covering increases absorption.
• Ear drops. Warm the bottle briefly in your hand, lie with the affected ear up, place the number of drops ordered, and stay in that position for a few minutes. Do not touch the dropper to your ear.
• Rectal enema. Usually given at bedtime so it stays in place overnight. Empty your bowel first if you can, lie on your left side, insert gently, and then try to retain it. Your prescriber will tell you how long a course to use.
• Shampoo or foam. Apply to the scalp as directed, leave in contact for the time your prescriber specifies, then rinse if instructed.

Tacrolimus works gradually. Most people are told to use it for a defined stretch and then stop or step down, rather than continuously — the approved label specifically directs avoiding continuous long-term use. Do not extend a course, increase the amount, or use it on new areas without asking your prescriber. A Bayview pharmacist is available if you have questions about your prescription.

Side effects & safety

Burning and stinging where you apply it is very common early on — and it usually fades. On the approved ointment label, skin burning or stinging was reported by roughly half of patients (46–58%) and itching by about 41–46%. The AAD notes this “tends to disappear as the skin heals.” It is typically worst in the first days of treatment and on the rawest skin. Knowing to expect it is the main reason people stick with the medicine long enough for it to work.

• Alcohol flushing. Some people get facial flushing, warmth, or redness after drinking alcohol while using topical tacrolimus.
• Sun sensitivity. Treated skin can be more sensitive to sunlight.
• Skin infections. Because tacrolimus damps down local immunity, cold sores, shingles, warts, and other skin infections can occur or spread more easily. Tell your prescriber about any new blisters, sores, or spreading rash.
• Ear route: stinging or itching in the canal.
• Rectal route: local irritation, urgency, or cramping. Tacrolimus given rectally can be absorbed into the bloodstream. Levels are usually low or undetectable, but they are not always — one series reported a mean serum level of about 5.5 ng/mL and one patient with a reversible rise in creatinine along with tremor, headache, and fatigue. Reviews recommend checking blood tacrolimus levels regardless of the route used. Your prescriber may order blood tests; please do them.
• Boxed warning: as described above, rare cases of skin cancer and lymphoma have been reported in people using topical calcineurin inhibitors. A causal relationship has not been established.

Who should not use it?

Do not use tacrolimus if you have had a hypersensitivity reaction to tacrolimus or to any ingredient in your preparation. The approved ointment is not for children younger than 2 years, and only the 0.03% strength is approved for ages 2 through 15.

Talk with your prescriber before using it if you have a weakened immune system, an active skin infection at the treatment site, a skin condition such as Netherton syndrome or widespread erythroderma where absorption may be much higher, a history of skin cancer or lymphoma, or kidney or liver problems. Tacrolimus should not be applied to skin that is actively infected or to a suspected malignant lesion.

Tell your prescriber and pharmacist about your full health history, allergies, and every medicine and supplement you take — including any oral tacrolimus or other immune-suppressing medicine — and whether you are pregnant, planning to become pregnant, or breastfeeding. A valid prescription is required, and your prescriber determines whether tacrolimus is appropriate for you.

How should it be stored?

Store your preparation exactly as directed on your label. Most tacrolimus creams, gels, ointments, foams, and shampoos are kept at room temperature, around 68–77°F (20–25°C), away from heat and light. Compounded otic solutions and rectal enemas are frequently refrigerated — follow your label. Do not freeze.

Keep everything in the container it came in, tightly closed and out of the reach of children, and do not share it with anyone. Do not use it past the beyond-use date on the label, and dispose of unused medication as your pharmacist directs or through a drug take-back program rather than flushing it.

Why is this compounded?

Tacrolimus is only manufactured as a topical ointment, oral capsules and granules, and an injection. There is no commercial ear drop, no rectal enema, no gel, no foam, and no shampoo — so when a prescriber wants tacrolimus to reach the ear canal, the rectum, or the scalp, a compounding pharmacy has to make it. The same is true of combination formulas such as tacrolimus with ketotifen, or with minoxidil and clobetasol.

As a 503A compounding pharmacy, Bayview Pharmacy prepares each order in small batches using quality ingredients. Compounded preparations are not FDA-approved, they are not reviewed by the FDA for safety or effectiveness, and a valid prescription is required. Because most of these routes rest on limited evidence, we think it is worth asking your prescriber what result they expect and how they will decide whether it is working.