tacrolimus monohydrate at a glance
Medicine class
Calcineurin inhibitor and immunosuppressant.
Main roles
Transplant rejection prevention or treatment; topical treatment of selected moderate-to-severe atopic dermatitis.
Brand consistency
Oral products must be prescribed and dispensed by brand; switching requires specialist supervision and blood-level monitoring.
Food and grapefruit
Oral formulations are generally taken on an empty stomach as directed; grapefruit and grapefruit juice should be avoided.
What is tacrolimus monohydrate used for?
Licensed uses represented by the selected UK products include:
Preventing rejection after kidney, liver or heart transplantation; the organs and age groups covered differ between oral products.
Treating transplant rejection that has not responded adequately to other immunosuppressants.
Treating moderate-to-severe atopic dermatitis with 0.03% ointment in adults, adolescents and children aged 2 years or older when conventional treatment has been inadequate or unsuitable.
Maintenance treatment of suitable atopic dermatitis patients with frequent flares after an initial response to tacrolimus ointment.
How does tacrolimus monohydrate work?
Tacrolimus binds to FKBP12 inside cells and inhibits calcineurin. This reduces T-cell activation and inflammatory cytokine production, helping prevent graft rejection systemically and reducing local skin inflammation when applied as an ointment.
tacrolimus monohydrate preparations and strengths
Ointment
Route: Cutaneous
Strengths: 0.03%, 0.1%
Capsule
Route: Oral
Strengths: 0.5 mg, 0.75 mg, 1 mg, 2 mg, 3 mg, 5 mg
How to take tacrolimus monohydrate
Follow the instructions for the exact named product; oral formulations have different release characteristics and are not interchangeable. Take oral tacrolimus consistently in relation to food, usually on an empty stomach, and avoid grapefruit. Swallow capsules or prolonged-release tablets whole. Prepare Modigraf suspension only with suitable non-PVC equipment and use it immediately. Apply ointment as a thin layer to instructed skin areas, avoiding eyes, mucous membranes and occlusive dressings; wash hands afterwards unless they are being treated.
Check the brand and formulation whenever a new supply is received.
Do not change, crush, open or substitute a formulation unless its specific instructions permit this and the specialist team agrees.
Minimise sunlight and ultraviolet exposure on ointment-treated skin and use suitable protection.
tacrolimus monohydrate side effects
Common or expected effects
- Oral treatment: tremor, headache, sleep disturbance, nausea, diarrhoea, high blood pressure, raised blood glucose or potassium, infection and impaired kidney function.
- Ointment: burning, itching, warmth, redness or irritation at the application site; these effects often lessen after treatment begins.
- Ointment may also be associated with folliculitis, acne, cold sores or other local skin infections, and facial flushing or irritation after alcohol.
Get urgent medical advice
- Serious infection or unusual fever.
- Kidney injury, important electrolyte disturbance or severe neurological effects.
- Severe allergic or blistering skin reactions.
- Thrombotic microangiopathy, which may present with unusual bruising, profound fatigue, fever, neurological symptoms or kidney impairment.
- Eczema herpeticum or other rapidly spreading, painful or blistering infection on ointment-treated skin.
tacrolimus monohydrate in pregnancy
Tacrolimus may be used during pregnancy when a specialist considers it necessary; transplant treatment should not be stopped without advice. Systemic tacrolimus crosses the placenta, so maternal treatment and the newborn may require specialist monitoring. Tacrolimus ointment should be used only when clearly necessary.
tacrolimus monohydrate while breastfeeding
The selected UK product information advises against breastfeeding during systemic tacrolimus treatment because tacrolimus enters breast milk. It also advises against breastfeeding during treatment with Protopic ointment despite low systemic absorption. Discuss feeding options with the transplant, dermatology or maternity team.
tacrolimus monohydrate interactions
Tacrolimus has clinically important interactions, especially with oral treatment. New prescriptions, over-the-counter products and herbal remedies should be checked with the specialist team or pharmacist.
Grapefruit or grapefruit juice
May raise tacrolimus exposure and increase toxicity risk; avoid.
Strong CYP3A4 inhibitors, including clarithromycin, azole antifungals, ritonavir and cobicistat
Can rapidly increase tacrolimus concentrations, requiring specialist review and close monitoring.
Strong CYP3A4 inducers, including rifampicin, carbamazepine and phenytoin
Can lower tacrolimus concentrations and increase rejection risk.
Common questions about tacrolimus monohydrate
Answers are fully visible for fast scanning and source review.
Why must oral tacrolimus be prescribed by brand name?
Different products can produce clinically important differences in exposure. Unsupervised switching has been associated with toxicity and transplant rejection.
Can tacrolimus capsules and prolonged-release tablets be swapped?
Not without transplant-specialist supervision. A change requires therapeutic drug monitoring because the formulations release and deliver tacrolimus differently.
Why are tacrolimus blood tests needed?
Tacrolimus has a narrow therapeutic range: low exposure may permit rejection, while excessive exposure increases toxicity, including kidney and neurological harm.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.