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The active ingredient Tacrolimus is a natural substance from the so-called Makrolidlacton type and was discovered in soil bacteria. It suppresses the immune system, so it is an immunosuppressant. It is used to prevent rejection reactions after organ transplantation and in autoimmune diseases such as eczema. Here you can read everything to know about immunosuppressant Tacrolimus: mode of action, application forms and side effects
How Tacrolimus acts
The function of the immune system in the human body mainly mediated by the white blood cells circulating in the blood. A subset of these leukocytes are known as T-cells or T-lymphocytes. These migrate after their formation in the bone marrow via the bloodstream to the thymus (gland behind the breastbone) to intervene there. This “learn” them to distinguish endogenous from exogenous structures. These exogenous structures can for example be body cells that are infected with viruses and thereby contribute foreign proteins on their surface. But human organs derived from other people (organ transplants), may be recognized as foreign by immune cells.
Since the body everything foreign is classified as potentially harmful, the T cells are used to start a defensive reaction by detection of these strange structures. They produce after activation – ie the recognition of foreign structures – different chemical messengers, called cytokines, such as interleukins (IL), interferons (IF) and the tumor necrosis factor (TNF). This mechanism will start the defense reaction of the immune system, for example, the transplanted organ.
Tacrolimus immunosuppressant prevented as the release of cytokines in T cells – immune system activation does not occur
Up, degradation and excretion of Tacrolimus
After taking Tacrolimus as a tablet, capsule or suspension drinking the drug via the gastrointestinal tract is absorbed into the blood. After one to three hours, set the highest blood levels. Of the total ingested dose about a quarter reaches the systemic circulation. The drug is already broken down in the gut wall partially, after the absorption into the blood it is further degraded in the liver. The so-called half-life – the time after which half of the recorded amount of drug is excreted – varies with Tacrolimus between eleven and 15 hours. Excretion is mainly via the bile in the feces.
When will Tacrolimus used?
The active ingredient Tacrolimus is indicated for the prevention and treatment of rejection reactions after a liver, kidney or heart transplant.
As Tacrolimus ointment, the active ingredient for maintenance therapy or for the treatment of a flare, in patients with atopic eczema (atopic dermatitis) is used in moderate and severe cases.
The use of Tacrolimus is generally medium to long term lifetime. In the topical treatment of atopic eczema, the treatment time depends on the course of the disease.
How Tacrolimus is applied
The active ingredient Tacrolimus is administered at the beginning of the internal use usually under medical supervision. Here, the doctor checks the individual Tacrolimus absorbed into the body and measures the blood levels of the immunosuppressant over several days. This allows the position to be taken Tacrolimus dosage calculated daily. The doctor prescribed a non-delayed dosage form (ie without sustained release), Tacrolimus should be taken morning and evening. When prescribing a retarded dosage form, the active ingredient needs to be taken in the morning. Sober carried Taking Tacrolimus has one hour before or two to three hours after a meal with a glass of water. Concomitant food intake inhibits Tacrolimus absorption into the blood.
The use of Tacrolimus ointment is to take place at the beginning of treatment twice daily. After significant improvement in symptoms the application at a time can be reduced every day.
What are the side effects of Tacrolimus?
Side effects occur particularly when taking a tablet, capsule or suspension drinking; treatment with Tacrolimus ointment leads in most cases at most to local irritation.
During therapy with Tacrolimus show up at more than ten percent of patients adverse drug reactions such as high blood sugar, high levels of potassium in the blood, diabetes, insomnia, tremor, and impaired renal function.
Often occur also Tacrolimus side effects: 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 , blood clotting disorders with clot formation, dyspnea, cough, sore throat, inflammation of the gastrointestinal tract, indigestion, inflammation of the liver, liver function test abnormalities, sweating, itching, rash, and muscle and joint pain.
What should be considered when taking Tacrolimus?
Because of the Tacrolimus levels is crucial for the effectiveness of the immunosuppressant in the blood, the preparation must not be changed during treatment. There must always be obtained from the same company. Particular care must be taken that no unintended change of immediate release to delayed-release (“retard”) forms or vice versa happens. Should such a change be intentional, this may only be performed under medical supervision to rigorous inspections of Tacrolimus blood levels.
Tacrolimus is metabolized in the liver by the cytochrome P450-3A4 enzyme. This metabolizes many other active substances. In the simultaneous intake can therefore lead to changes in blood levels: Some drugs may accelerate the decomposition of Tacrolimus, other delay it, which can have a major impact on its effectiveness. The list of these medicines is extensive, which is why the income on an individual basis with the doctor or pharmacist should be ascertained. For example, this includes antibiotics, anti fungal infections, drugs against HIV infections and herbal remedies such as St. John’s wort.
The intake of Tacrolimus during pregnancy and lactation should be avoided, because the data are not sufficient on the one hand and on the other hand have been shown the child endangering effect by taking the immunosuppressant.
Tacrolimus is approved for use in children, but in reduced dosage. The same applies to patients with hepatic impairment. In elderly patients, usually no dose adjustment is required.
How to obtain drugs with Tacrolimus
At the start of treatment the drug is administered directly stationary. For further processing or for the treatment of atopic eczema with Tacrolimus ointment, the drug can be purchased with a prescription at the pharmacy.
Since when Tacrolimus is known?
The active ingredient Tacrolimus was discovered in 1987 in the soil bacterium Streptomyces tsukubaensis. It was the second highly effective immunosuppressant after previously discovered (also known as sirolimus) rapamycin in 1975. For the first time the drug was approved in the US in 1994 for the treatment of liver transplant patients, and later also for other recipients of donor organs. In Germany, the agent was first approved 1998th There are now numerous generics with the active ingredient Tacrolimus on the German market.