Sellsept

Cellsept is the drug that is the main one after organ transplantation.

Indications of the sellsepta

You can use the drug in combination with hormonal drugs (corticosteroids) and immunosuppressants (cyclosporine) for adults and children from the age of twelve. Indications are prevention and therapeutic treatment of rejection of organs such as the heart, kidney and liver, as well as increasing the chances of survival of patients.

Release form

The medication is available in the form of tablets or capsules with engraving. Ten pieces in a blister. The package can be from five to ten plates.

Pharmacodynamics

To prevent and treat the rejection of transplanted organs, medication is used in conjunction with cyclosporine, hormones and antitumocyte globulin.

This helps to reduce the ineffectiveness of treatment in the first six months after transplantation, and in a daily dose of two grams reduces the number of dead grafts and the death rate of patients for the year after transplantation, while at a daily dose of three grams - on the contrary, increases the number of patients earlier than the term dropped out of the study.

With respect to Azathioprine, with the reception of Cellsepta much less mortality, rejection and subsequent transplantations. This provides a similar survival in patients with a primary kidney transplant.

In pre-clinical studies, carcinogenic actions, fertility declines in rats, with double the recommended doses, were not found. MMF can cause instability in chromosomes, only in a dose that has a cytotoxic effect.

In animal tests, it is indicated that if the transplant almost increases the dose of 0.5 and the heart is 0.3 times, the first generation (without the toxic effect on the mother) causes various developmental defects.

At the results of toxicology studies, it is noted that the organs of the hematopoietic and lymphatic system are mostly affected.

Non-clinical toxicity data correspond to undesirable reactions to the medication.

Pharmacokinetics

After ingestion of the medication, immediate adsorption and metabolism occur, forming a metabolite of IFC. Bioavailability, when taken by ingestion compared with the intravenous injection of Cellsept, is approximately 94%, but the concentration with this method of reception is not detected.

The concentration indices (by forty percent) and AUC (by thirty percent) are six months after the operation higher than in the period up to forty days after it.

Consumption of food does not affect the adsorption of IFC, but its concentration is reduced by forty percent.

Six to twelve hours after the use of the drug, a second increase in the concentration of Cellsept occurs. This indicates the onset of his hepatic-intestinal decay. If at the same time to appoint Kolestyramin, AUC decrease by forty percent. This means the cessation of the hepatic intestinal cycle. Research data show that IFC binds to the plasma protein.

In the process of hepatic intestinal decay, the drug metabolizes under the influence of glucuronyltransferase with the formation of phenolic glucuronide.

The excretion occurs mainly by the kidneys (about 93%), of which 87% - in the form of IFNC, and 0.99% - IFC. The remaining 6% are excreted with feces. A large concentration of IFPC can not be much isolated by hemodialysis, but usually this procedure does not remove IFC and IFPC. Bile acid secreters abort the liver-intestinal decay.

As the studies show, two 500 mg tablets are equivalent to four 250 mg capsules.

The filtration rate in the glomerulus of the kidneys is 30 to 75% higher in patients with severe chronic renal failure than in healthy individuals. There are no data on the frequent use of Cellsept in this category of patients.

In people with cirrhosis of the alcoholic character, the pharmacokinetics are not changed. This allows us to state that pathological processes in the liver parenchyma will not be a contraindication for the use of Selsset.

Dosing and administration

Therapeutic doses for use Selsepta:

A warning:

• kidney transplantation

The daily dose should not be more than 3 grams. Nevertheless, more effective, as studies show, will be taking two grams.

• heart, liver transplant

The daily dose is no more than 3 g.

Therapy of the kidney transplant department

You need to take three grams a day. The initial dose should be taken as soon as possible after the transplant.

People with a chronic form of kidney failure. Do not use a dose of more than two grams a day.

People over 65 years. Those who suffered a kidney transplant should not take more than two grams.

Children from the age of twelve:

• prevention of rejection of the transplanted kidney. With a surface volume of up to one and a half meters - a dose of 750 mg 2 times a day, more than a meter and a half - two grams.
• rejection therapy of the transplanted kidney. Information, as well as a heart or liver transplant, is not available for possible use.

[1]

Use of the sellsepta during pregnancy

Cellsept significantly increases the likelihood of intrauterine malformations of the fetus (for example, abnormal development of organs and systems). Therefore, the patient who plans pregnancy should be warned about such possible consequences of taking the medication.

Treatment with medication should not be started until there is an exact negative result of pregnancy. Before starting therapy and six weeks after it, the patient should use two types of contraception during intimate relationships or abstain from them for the duration of treatment, even if she has been diagnosed with infertility.

Therapy by Sellsept during gestation can be carried out only if the positive effect for the mother will exceed the harm for the child.

It is also necessary to make a choice between breastfeeding and therapy with Sellsept, since there is no information about the isolation of the drug with milk. But, it should be borne in mind that, during studies in rats, they had MMP in their milk.

Contraindications

The drug should not be used in the period of exacerbation of pathologies of the gastrointestinal tract and any personal sensitivity to its components.

Side effects of the sellsepta

Because of the presence of the main pathological process and the sharing of Cellsept with other medicines, all the undesirable effects of the treatment.

Most often, patients can be found: diarrhea, lowering of white blood cell count, blood infection and vomiting.

Lymphoma was recorded in one percent of patients who underwent transplantation of organs that had taken Cellsepts together with other immunosuppressants and who had been under medical supervision for at least one year. Skin carcinoma (except for melanoma) - was found in 1.6 - 4.2% of cases, other types - up to two percent. Observations of patients for another two years did not make significant changes in the data on malignant tumors that occurred after the organ transplantation.

With an increase in the degree of immunosuppression, the risk of developing infections that occur in people with greatly weakened immunity proportionately increases. Most often in this case there were: candidiasis of the skin and mucous membranes, as well as herpes.

In childhood, in patients who take Sellsept, adverse reactions in the form of diarrhea and anemia are recorded more often than in adults (especially up to six years), but the type and frequency of all adverse effects are similar to adults.

In old age, the risk of various undesirable reactions of the organism to the use of Cellsept is somewhat higher than in patients of a young age. Therefore, this category of patients should be prescribed dose is weaker (two grams per day).

Of the unregistered side effects, the most common are:

1. Colitis
2. Inflammation of the pancreas
3. Meningitis
4. Multifocal-type leukoencephalopathy
5. Anomalies of fetal development

Overdose

Information on the drug overdose is not documented. But the one obtained during the research makes it possible to talk about the possible occurrence of immunosuppression.

If a patient develops agranulocytosis, the dose should be immediately lowered or Sellsept's treatment stopped. For elimination, you can also use Kolestyramin, and the procedure for hemodialysis will be practically ineffective.

Interactions with other drugs

1. Acyclovir. With renal failure, joint administration of drugs will lead to an increase in their concentration in the serum.
2. Ganciclovir. Does not affect the pharmacokinetics. But at their one-time use, it is necessary scrupulous supervision over a condition of the patient by medical personnel.
3. Antacids, which include magnesium and aluminum. Reduce the period of sucking Cellsept.
4. Kolestyramin. Reduces the AUC to forty percent if you take one and a half grams of Sellsept after taking four grams three times a day, lasting four days Kolestyramin.
5. Cyclosporine. Selsept does not affect Cyclosporine. But with a joint admission, the effect of IFC is reduced to 50%.
6. Oral contraceptives. Do not exert influence Selsept. While passing the therapy with medication, other methods of contraception need to be additionally applied.
7.  Norfloxacin, Metronidazole. One antibacterial drug does not alter the bioavailability of the drug. But a single dose of Cellsept together with Norfloxacin and Metronidazole significantly reduces the AUC (by thirty percent).
8. Rifampicin. With a simultaneous use of drugs, and a one-stage transplantation of the lungs and kidneys, you need a dose change under the supervision of medical personnel.
9. Augmentin, Ciprofloxacin. With the combined use of Cellsept and antibacterial therapy with these drugs, the minimum concentration is reduced by 54%. Further, if the patient continues therapy, this action decreases, and after the end of the antibiotic intake disappears.
10. Tacrolimus. Has no effect, only in patients with stable transplanted liver AUC grows by twenty percent in Tacrolimus.
11. Calcium channel blockers. There is an increase in the density of MHCI.
12. Vaccines are alive. Can not be shared with Selsept.

[2]

Storage conditions

The drug belongs to the category of potent drugs. Keep in a dark place that is inaccessible to children. Observing the temperature regime is not more than 30 ° С.

Special instructions

Reviews

The drug has proven itself on the best side, is widely distributed in various clinics of transplantology. Assign it to prevent acute organ rejection. Thanks to Sellsept significantly improved survival of patients after transplantation .

Shelf life

3 years.