Immulimus 0.1% Medisun skin cream for allergic eczema (10g)

ATC: 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 the immunosuppressive effect of Tacrolimus is not well known.

tacrolimus has the effect of inhibiting T cells T, through inhibition of Interleukin-2.

tacrolimus inhibits 100 times stronger than cyclosporin.

proved that Tacrolimus inhibits the activity of T lymphocytes by cohesion to an intracellular protein, FKBP-12.

Tacrolimus complex-FKBP-12, Calci, Calmodulin and Calcineurin are formed and inhibited the phosphatase activity of calcineurin and therefore has the ability to prevent phosphorylation and transfer of cellular factors of T (NF-AT) cells (NF-AT) activated, a component of the Human Code through the process of cell cells through the overcoming of the code to formulate the code to form the code of transcription Lymphokin (eg interleukin-2, gama interferon).

Tacrolimus also inhibits the process of sessions where the genes have the symbols IL-3, IL-4, IL-5, GM-CSF and TNF-A, all of these genes are involved in the activity process at the initial stage of T cells.

In addition, it has been proven that Tacrolimus has the ability to inhibit the release of intermediate substances that have been formed from skin protection, alkaline leukocytes and reducing the expression of highly affinity letters to IGE in Langerhans cells.

Although 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 a transplant organization 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.

Dynamic pharmacokinetics

absorption

A plasma plasma concentration from non -detection levels 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 is below 0.5%.

transformation

Tacrolimus metabolizes very strongly in the liver and gastrointestinal tract through the oxidase enzyme system, first of all the Cytochrom P-450 system (CYP3A4) forms 8 main metabolic metabolites of 31-Demethyl tacrolimus, which is similar to Tacrolimus In Vitro).

Elimination

less than 1% of the dose is excreted intact through the urine.

The main excretion line is in the form of bile in the form of hydroxylation.

Half life eliminates 21 - 61 hours on healthy volunteers.

Be cautious when taking medication

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 lympha 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 disease (Graft Versus Host).

Not applied in the oral area.

There has been a report on the increase in the concentration of the sample after taking TNCrolimus ointment for the above cases.

If there is no sign, the symptoms of the eczema are not improved, should consider continuing treatment regimens.

Not yet established the safety and effectiveness of the Tacrolimus ointment 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 ability to drive and operate machinery

People who often drive or operate machinery should use Immulimus 0.1%?

does not affect the ability to drive and operate machinery.

Women during pregnancy and lactation

Women during pregnancy should use Immulimus 0.1%?

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 babies. Need to consider when using the drug.

Should women breastfeeding should take Immulimus 0.1%?

tacrolimus can go to breast milk. Contraindications for medication during breastfeeding.

Drug interaction

drug interactions may affect the activity of the drug or cause side effects. Should notify the doctor or pharmacist a list of drugs and functional foods you are using. Do not use or increase or decrease the dose of the drug without the guidance of a doctor.

Medications that affect the liver's urine enzymes:

Because Tacrolimus is mainly metabolized by ISOENZYM CYP3A4 of Cytochrom P450, simultaneous use of Talolinus with the above drugs requires monitoring of the concentration of Tacrolimus in the whole blood to adjust the dose of Tacrolirius to suit.

The following drugs have been reported can increase or decrease the concentration of tarolirius in the blood:

Medications can increase the concentration of tarolirius in the blood:

aluminum hydroxyd-filanesi hydroxyd; Bottle Criptin; Chloramphenicol; cimetidin; Cisaprid; Clarithromycin; Lotrimazol; Itraconazole; ketoconazole; Lanzaprazol; methylprednisolon; metoclopramid; nefazodon; nicardipin; nifedipin; Omeprazol; Troleandomycin; Verapamil; varicellazol; HIV protease enzyme inhibitors.

Medications can reduce the level of tarolirius in the blood:

carbamazepin; Caspofungin; phenobarbital; phenytoin; Rifabutin; Rifumpin; Sirolimus; The female tree.

Need to use tacrolimus carefully on people who use Retrovirus anti -Retrovirus drugs that can be metabolized by CYP3A enzymes (for example: Selfinavir, Ritonavir).

Modified drugs by liver enzymes and urine: simultaneous use of tacrolimus with phenytoin may increase the level of phenytoin in plasma.

Immunological inhibitors: Very cautious when using combined immunosuppressive therapy.

It is not recommended to use Tacrolimas and Sirolimus.

Poison with body (such as aminoglycosid antibiotics, artphone tricin b, cisplastin, gaciclovir, cyclosporin): due to the ability to put the force of kidney function, need to be cautious when coordinated.

Potassium diuretics: can increase severe blood potassium, so it is necessary to avoid coordination.

Vaccines: Need to pay attention to the body's immune system capabilities using Tacrolimus use in response to vaccine. It is recommended to avoid vaccinating live vaccines such as measles vaccines, mumps, rubella, polio vaccines, BCG, typhoid gold sauce 21A.

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

Metronidazole can increase by 2 times the blood concentration of cyclosporin and tacrolirus, which should increase blood creatinine levels in both cases.