Immulimus 0.03% Medisun treats the moderate or severe allergic eczema (10g)

ATC code: d11ah01

tacrolimus is a macrolid (macrolactam) extracted from streptomyces tsukubaensis, has a strong immunosuppressive effect like cyclosporin in terms of pharmacological but not related to structure; The drug also has antibacterial activity but very limited. The exact mechanism of immunosuppressive effects of Tacrolimus is not well known.

tacrolimus has the effect of inhibiting T cells T-lymphocytes through inhibiting Interleukin-2 production. Tacrolimus inhibits 100 times stronger than cyclosporin and the same dose. It has shown that Tacrolimus inhibits the activation of T lymphocytes by connecting an intracellular protein, FKBP-12. Tacrolimus-FKBP-12 complex, calcium ion, calcium and calcineurin are created and inhibited the phosphatase activity of calcineurin and therefore has the ability to prevent phosphorylation reduction and transfusion of T-cells of T cells (NF-AT) activated, an ingredient of cellular cells through the generation of lymphocytes. Interleukin-2, gamma interferon). Tacrolimus also inhibits the transcription of genes with il-3, IL-4, IL-5, GM-CSF and TNF-A, all of these genes involved in the active process at the initial stage of T. In addition, people have proven that Tacrolimus has the ability to inhibit the release of intermediate substances that have been formed from the skin of the skin, alkalis and alkalis. high for IgE on langerhans cells. While Tacrolimus is not toxic to the gene and does not interact directly with DNA, the drug can cause damage to local immune monitoring. Tacrolimus is used to prevent the discharge of transplantation in kidney transplantation, heart, liver other genes of the same species. Need to use in combination with corticosteroids.

tacrolimus is also used to treat Crohn disease with holes and allergic eczema.

Pharmacokinetics

absorption

Plasma concentrations ranging from not detected to less than 20 nanogam/ml (in adults, most of less than 5 nanogam/ml). But in young children applying 0.1% ointment only once to treat chronic eczema, high serum concentration (24 nanogam/ml). Birth of less than 0.5%.

Metabolism

Tacrolimus metabolizes very strongly in the liver and gastrointestinal tract through the enzyme system of oxidase, first of all the Cytochrom P450 system (CYP3A4) forms 8 metabolites (the main metabolitus is 31-Demethyl tacrolimus, which is similar to Tacrolimus in vitro).

Elimination

less than 1% of the dose is excreted intact through the urine. The emissions are mainly into the bile in the form of hydroxylation. Half life eliminated from 21 to 61 hours on healthy volunteers.

Be cautious when used

Patients with eczema organs are often susceptible to skin infections. If there is a clinical skin infection, the risk and benefits of the use of Tacrolimus ointment should be considered.

Although the causal relationship has not been established, some rare cases may experience malignant diseases including malignant diseases of the skin and lymphas that have been reported in patients using Tacrolimus ointment. During the use of Tacrolimus ointment, skin exposure should be limited to natural light or artificial light.

Do not use Tacrolimus ointment for damaged skin because it is likely to increase the absorption of tacrolimus into the system. For example: Netherton syndrome, fish scales, body redness or skin graft waste (Graft Versus Host). Do not apply in the mouth. There have been reports on increased blood concentration after taking Tacrolimus ointment for the above cases.

If there is no sign, the symptoms of the eczema are not improved, so the treatment regimens should be considered. The safety and effectiveness of Tacrolimus ointment is used on the spot in children under 2 years old.

Avoid the Tacrolimus ointment in contact with the eyes and mucosa. If the drug sticks to the eyes and the mucosa, it is necessary to clean and wash with water. Do not give Tacrolimus to treat skin diseases.

The effect of drugs on driving and operating machinery

does not affect the ability to drive and operate machinery.

Using drugs for women during pregnancy and lactation

Using drugs in pregnant women: tacrolimus can go into the placenta and reach the concentration of the placenta 4 times higher than the plasma concentration. There have been reports on high blood potassium and kidney failure in newborns. Need to consider when using the drug.

Using drugs in breastfeeding women: tacrolimus can go to breast milk. Contraindications for breastfeeding when using tacrolimus.

Interactive drug

Medications that affect the liver's urine enzymes

Because Tacrolimus is mainly transformed with Cytochrom P450's isenzyme, Cytochrom P450, Tacrolimus should simultaneously use the above -mentioned drugs that require monitoring of Tacrolimus concentration in the whole blood to adjust the dose of Tacrolimus to match. The following drugs have been reported can increase or decrease the concentration of Tacrolimus in the blood:

Medications can increase the concentration of Tacrolimus in the blood

aluminum hydroxyd-magnesi hydroxyd; Bromocriptin; Chloramphenicol; cimetidin; Cisaprid; Clarithromycin; Lotrimazol; Itraconazole; ketoconazole; Lanzoprazol; methylprednisolon; metoclopramid; nefazodon; nicardipin; nifedipin; Omeprazol; Troleandomycin; Verapamil; Voriconazole; HIV protease enzyme inhibitors.

Drugs can reduce the concentration of Tacrolimus in the blood

carbamazepin; Caspofungin; phenobarbital; phenytoin; Rifabutin; Rifampin; Sirolimus; The female tree (John's: Hypericum Perforatum).

Need to use tacrolimus cautiously on people who use Retrovirus anti -Retrovirus drugs that can be metabolized by CYP3A enzymes (e.g. nelfinavir, ritonavir).

Modified drugs by the liver's urine enzymes: simultaneous use of tacrolimus with phenytoin may increase the level of phenytoin in plasma. Immunological inhibitors: Very cautious when using combined immunosuppressive therapy. The recommendation must not be combined to use Tacrolimus and Sirolimus.

Poison with kidneys (such as aminoglycoside antibiotics, amphotericin b, cisplatin, ganciclovir, cyclosporin): Due to the ability of the force to weaken the kidney function, need to be cautious when coordinated.

Potassium diuretics. Can increase the potassium serious, so it is necessary to avoid coordination.

Vaccines: It should be noted for the ability of the body's immune system to use Tacrolimus to decrease in response to vaccines. It is recommended to avoid vaccinations such as measles vaccines, mumps, rubella, polio vaccines, BCG, yellow fever, tytrophy ty21A.

ibuprofen when combined with Tacrolimus has caused kidney failure in 2 liver transplants.

Metronidazole can increase 2 times the blood concentration of cyclosporin and tacrolimus, so it increases blood creatinine levels in both cases.