Dermus

Indications

Capsules and other forms taken by mouth (and injection in hospital):

• to prevent the body from rejecting a transplanted kidney, liver or heart;
• to treat rejection that is not controlled by other medicines.

Ointment (0.03% and 0.1%):

• moderate to severe atopic eczema (atopic dermatitis) when standard treatments such as steroid creams have not worked or are not suitable;
• to help prevent flare-ups in people whose eczema comes back often.

How It Works

Tacrolimus is an immunosuppressant of the calcineurin inhibitor type. It calms the activity of certain white blood cells (T cells) that drive rejection and skin inflammation. Taken by mouth it works throughout the body; as an ointment it acts mainly in the skin.

Dosage and Administration

By mouth: only as prescribed by the transplant specialist. The dose is based on body weight and then adjusted using regular blood level tests. Take it at the same times each day, usually on an empty stomach (1 hour before or 2 to 3 hours after food). Do not switch between brands or between quick and slow-release forms unless the specialist arranges it. The injection is given by a doctor or nurse in hospital.

Ointment: apply a thin layer to the affected skin twice a day until the eczema clears, then as advised (for example once a day, or twice a week to prevent flares). The 0.03% strength is for adults and children from 2 years; the 0.1% strength is for adults and young people from 16 years. Wash hands after use unless treating the hands.

Interactions

Many medicines change Tacrolimus levels. Levels can rise with Ketoconazole, Fluconazole, Itraconazole, Clarithromycin, Erythromycin, Diltiazem and grapefruit juice, and fall with Rifampicin, Carbamazepine, Phenytoin and St John's wort. Ciclosporin should not be used at the same time. Potassium-sparing diuretics (such as Spironolactone) and potassium supplements can raise potassium too much, and pain medicines like Ibuprofen can add to kidney strain. Avoid live vaccines. Tell your doctor about all medicines, vitamins and herbal products you take.

Contraindications

• Allergy to Tacrolimus or to macrolide antibiotics
• Ointment: children under 2 years, and skin that is infected

Side Effects

By mouth, common: shaking (tremor), headache, high blood pressure, raised blood sugar or diabetes, kidney problems, high potassium or low magnesium, diarrhoea, nausea, trouble sleeping and more infections.

Ointment, common: burning, warmth, stinging or itching where it is applied, usually settling within a few days; facial flushing after drinking alcohol; skin infections such as cold sores.

Long-term immune suppression slightly raises the risk of skin cancer and lymphoma.

Get medical help at once for fever, chills or other signs of infection; a seizure, confusion or vision changes; passing much less urine; chest pain or an irregular heartbeat; or signs of transplant rejection that your team has told you about.

Pregnancy and Lactation

Transplant patients who are pregnant or planning pregnancy must not stop Tacrolimus on their own; the specialist will decide and monitor closely. Tacrolimus passes into breast milk, so discuss breastfeeding with the specialist. The ointment should be avoided in pregnancy unless the doctor advises it, and must not be applied to the breasts when breastfeeding.

Precautions and Warnings

• Regular blood tests (Tacrolimus level, kidney function, sugar, potassium) and blood pressure checks are needed with treatment by mouth.
• Protect your skin from the sun and avoid sunbeds.
• Avoid live vaccines and close contact with people who have infections.
• Tremor or blurred vision can affect driving.

Overdose

Taking too much by mouth can cause tremor, headache, nausea, kidney problems and raised blood levels. Contact the transplant team or go to hospital straight away. Swallowing ointment is unlikely to be serious, but get medical advice.

Therapeutic Class

Immunosuppressant (calcineurin inhibitor).

Storage

Store below 25°C in a dry place, away from light and out of the reach of children. Keep capsules in their original pack until use.