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Last Updated on March 16, 2024

Tacrolimus is a medicine used to treat a number of skin conditions, including eczema and psoriasis. It works by suppressing the immune system, which can reduce inflammation and itching. Although tacrolimus is a prescription drug, there has been some interest in making it available over the counter in the UK. However, at the moment tacrolimus is only available on prescription from a healthcare professional.

Tacrolimus 0.5, 1 and 5 mg is offered by most online pharmacies. First read recommendations on purchasing drugs online in the event you prefer to buy Prograf online.

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There are several reasons why tacrolimus is not available over the counter in the UK. First and foremost, it is a powerful drug that should only be used under the guidance of a healthcare professional. Tacrolimus can also have serious side effects, including an increased risk of skin cancer. It is therefore important that patients receive appropriate medical supervision and monitoring when using this medication.

Although tacrolimus is not currently available over the counter in the UK, patients who require this medication can obtain it with a prescription from their healthcare provider. In some cases, patients may be able to obtain tacrolimus from online pharmacies or other sources, but it is important to exercise caution and ensure that any medication obtained in this way is safe and appropriate for use. Patients should always consult their healthcare provider before taking any medication.

What is tacrolimus?

Tacrolimus is a natural substance of the macrolid lactone type that was discovered in soil bacteria. It suppresses the immune system and is therefore an immunosuppressant. It is used to prevent organ transplant rejection and in autoimmune diseases such as eczema. Read all about the immunosuppressant tacrolimus: how it works, how it is used and side effects.

How does tacrolimus work?

The function of the immune system in the human body is mainly mediated by the white blood cells circulating in the blood. A subset of these leukocytes are called T cells or T lymphocytes. After being formed in the bone marrow, they travel through the bloodstream to the thymus (a gland behind the breastbone), where they take action. They learn to distinguish between endogenous and exogenous structures. These exogenous structures can be, for example, body cells that have been infected with viruses and have foreign proteins on their surface. However, human organs from other people (organ transplants) can be recognised as foreign by immune cells.

Since the body classifies anything foreign as potentially harmful, the T-cells are used to trigger a defence response by recognising these foreign structures. Once activated – i.e. recognised as foreign – they produce various chemical messengers called cytokines, such as interleukins (IL), interferons (IF) and tumour necrosis factor (TNF). This mechanism triggers the immune system’s defence response, for example against the transplanted organ.

Tacrolimus immunosuppressant prevents the release of cytokines in T cells – immune system activation does not occur.

Pharmacokinetics and metabolism of tacrolimus

After taking tacrolimus as a tablet, capsule or suspension, the medicine is absorbed into the blood via the gastrointestinal tract. Peak blood levels are reached after one to three hours. About a quarter of the total dose taken reaches the systemic circulation. The drug is partially broken down in the intestinal wall and, after absorption into the blood, is further broken down in the liver. The half-life of tacrolimus – the time it takes for half of the absorbed dose to be excreted – varies between 11 and 15 hours. Excretion is mainly via the bile in the faeces.

When is tacrolimus used?

Tacrolimus is indicated for the prevention and treatment of graft rejection following liver, kidney or heart transplantation.

Tacrolimus ointment is used as a maintenance therapy or for the treatment of flares in patients with moderate to severe atopic dermatitis.

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The use of tacrolimus is generally medium to long term. In the topical treatment of atopic eczema, the duration of treatment depends on the course of the disease.

How tacrolimus is taken?

Tacrolimus is usually administered under a doctor’s supervision at the start of treatment. The doctor monitors the individual Tacrolimus absorbed into the body and measures the blood levels of the immunosuppressant over several days. This allows the Tacrolimus dosage to be calculated on a daily basis. If the doctor has prescribed a non-delayed (i.e. non-sustained) dosage form, Tacrolimus should be taken in the morning and evening. If a sustained-release formulation has been prescribed, the active ingredient must be taken in the morning. Tacrolimus should be taken one hour before or two to three hours after a meal with a glass of water. Taking food at the same time inhibits the absorption of Tacrolimus into the blood.

Tacrolimus ointment should be applied twice a day at the start of treatment. After a significant improvement of the symptoms, the daily application can be reduced.

What are the side effects of tacrolimus?

Side effects occur mainly when taking tablets, capsules or suspensions; treatment with Tacrolimus ointment usually causes only local irritation.

During treatment with tacrolimus, more than ten per cent of patients experience side effects such as high blood sugar, high levels of potassium in the blood, diabetes, insomnia, tremor and impaired kidney function.

Side effects of tacrolimus are also common: Anemia, low electrolyte levels in the blood, decreased appetite, high blood lipids, confusion, anxiety, nightmares, depression or other mental disorders, convulsions, paraesthesia, nerve pain, blurred vision, tinnitus, palpitations, bleeding, difficulty breathing, cough, sore throat, gastrointestinal tract inflammation, indigestion, liver inflammation, liver function test abnormalities, sweating, itching, rash, muscle and joint pain.

What should I watch for while taking tacrolimus?

Because the level of tacrolimus in the blood is crucial to the effectiveness of the immunosuppressant, the preparation must not be changed during treatment. It must always be obtained from the same company. Special care must be taken to ensure that there is no unintentional switch from immediate release to retarded forms or vice versa. If such a change is intended, it should only be made under medical supervision with strict monitoring of the tacrolimus blood levels.

Tacrolimus is metabolised in the liver by the enzyme cytochrome P450-3A4. This enzyme metabolises many other drugs. Concomitant use may therefore lead to changes in blood levels: Some drugs can speed up the breakdown of tacrolimus, while others can slow it down, which can have a significant effect on its effectiveness. The list of these drugs is extensive, so it is important to check with your doctor or pharmacist on an individual basis. These include antibiotics, medicines for fungal infections, medicines for HIV infection and herbal medicines such as St. John’s wort.

Tacrolimus should not be used during pregnancy or while breast-feeding because of the lack of data and the risk of harm to the baby from the immunosuppressant.

Tacrolimus is approved for use in children, but at a reduced dose. The same applies to patients with liver impairment. Elderly patients do not usually need to have their dose adjusted.

How to get tacrolimus?

At the start of treatment, the drug is administered directly in hospital. For further treatment or to treat atopic eczema with tacrolimus ointment, the drug can be obtained from a pharmacy with a prescription.

How long has tacrolimus been on the market?

Tacrolimus was discovered in 1987 in the soil bacterium Streptomyces tsukubaensis. It was the second highly effective immunosuppressant after rapamycin (also known as sirolimus), which was discovered in 1975. The drug was first approved in the US in 1994 for the treatment of liver transplant patients and later for other recipients of donor organs. The drug was first approved in Germany in 1998, and there are now numerous generics of tacrolimus on the German market.

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