The transplant rejection reaction is the body's immune response to transplantation of foreign tissues or organ. There are several types of rejection: fulminant (a minute after connecting tissues or organs to the systemic circulation), acute (0-3 weeks after surgery) and chronic (a few months later).
To reduce the risk of such reactions, specialists use various immunosuppressants that act in a depressing manner on the human immune system. Some of them can be prescribed throughout the patient's life.
Mycophenolic acid (ATX code: L04AA06) is one of the most commonly used selective immunosuppressants. About what properties the specified substance possesses, and how it should be used correctly, is described below.
Trade name, form, packaging, description and composition
What form of release does mycophenolic acid have? The trade name of the drug with such an active substance is Mayfortic. It goes on sale in the form of light green and round tablets (coated with an enteric coating) with beveled edges and the inscription “C” on one side. You can buy such a tool in two different dosages: 180 and 360 mg. The latter is made in the form of oval and grayish-pink tablets, on one side of which the inscription "ST" is printed.
In addition to the active component (acidum mycophenolicum), the mentioned medicine also contains auxiliary substances. These include: anhydrous lactose, crospovidone, corn starch, povidone K30, magnesium stearate and colloidal silicon dioxide.
As for the enteric coating, it consists of: hypromellose phthalate, titanium dioxide, yellow / red iron oxide and indigo carmine.
Drug action
What is the Mayfortik drug and how does its active component (mycophenolic acid) work? Instructions for use report that it is an immunosuppressive medicine. Its main component is able to inhibit the synthesis of guanosine nucleotides. This is due to the selective suppression of the main enzyme for the synthesis of purines inosine monophosphate dehydrogenase (inosine monophosphate dehydrogenase). Through this mechanism, the proliferation of B- and T-lymphocytes is suppressed (to a greater extent than other blood cells, since the proliferation of lymphocytes depends primarily on de novo synthesis).
The principle of action of mycophenolic acid complements the work of calcineurin inhibitors, which disrupt the production of cytokines and act on T-lymphocytes during the resting period of the cell cycle.
Pharmacokinetics of the drug
What pharmacokinetic properties are inherent in mycophenolic acid? After oral administration, this substance is intensively absorbed into the systemic circulation. Due to enteric coating, the highest concentration of MPA in the blood is reached after 1.5-2 hours. In the course of the research, it was proved that the special composition of the film coating of the Mayfortik tablets prevents the release of the active ingredient in an acidic environment.
In people with a kidney transplant (stably functioning) who are already receiving basic immunosuppressive treatment with cyclosporine in the form of a microemulsion, the degree of absorption of mycophenolic acid from the digestive tract is 93%, and the bioavailability is 72%.
When taking a dose of 180-2160 mg of the drug, the pharmacokinetics of its main substance is linear and dose-dependent. Eating does not affect the effect of the drug, but its maximum concentration decreases by about 33%.
Mycophenolic acid binds to blood proteins by 97%. A decrease in the number of binding sites with plasma proteins (for example, with liver failure, hypoalbuminemia, uremia, etc.) can increase the concentration of free MPA in the blood.
Mycophenolic acid is metabolized by glucuronyl transferase. In this case, the main pharmacologically inactive metabolite is formed - phenol glucuronide.
The half-life of the substance in question is about 12 hours. Mostly, the drug is excreted together with urine and in very small quantities - unchanged.
Indications for taking the drug
In what cases can mycophenolic acid be prescribed to the patient? An indication for taking the Mayfortik drug is acute transplant rejection in people with kidney transplants (allogeneic) who receive basic immunosuppressive treatment with glucocorticosteroids and cyclosporin in the form of a microemulsion. The drug is used as a prophylactic.
Drug prescribing
In what cases should patients not take mycophenolic acid? The instruction indicates that the main contraindication to the use of "Mayfortika" is the high sensitivity of the patient to the main and auxiliary substances of the tablets. In addition, with extreme caution, this medicine is prescribed for people with congenital lack of hypoxanthine-guanine phosphoribosyltransferase (including Kelly-Sigmiller and Lesch-Nyhen syndromes), as well as digestive diseases, especially during exacerbations.
The drug "Mayfortik" (mycophenolic acid): instructions for use
Reception of the funds in question must be carried out under the strict supervision of specialists. The tablets are taken orally. They are swallowed in their entirety, without breaking or chewing. "Mayfortik" is acceptable to take on an empty stomach, and with food.
When does the treatment with the mentioned drug begin? Mycophenolic acid is prescribed to patients in the first two days after transplantation. In this case, a single dosage is 720 mg, which is taken twice a day (that is, the daily dose is 1440 mg).
Correct the indicated dosage regimen in the elderly is not required.
Special monitoring is required for patients who have severe renal impairment.
In people with severe liver diseases that are associated with damage to the parenchyma, dosage adjustment "Mayfortika" is not required.
Persons with a delayed restoration of the kidney transplant do not need to change the dose of the drug.
Side effects
Mycophenolic acid, the dosage of which was indicated above, causes such undesirable effects:
- Malignant neoplasms (increased risk of lymphomas and other neoplasms, including skin).
- Infectious diseases (or opportunistic infections). People who took the drug as part of combination immunosuppressive therapy for one year had CMV infection, candidiasis, and herpes simplex.
- Viral, fungal and bacterial infections, including wound infections, respiratory tract infections (upper sections), osteomyelitis, sepsis.
- Anemia, lymphopenia, thrombocytopenia, lymphocele, lymphadenopathy, neutropenia, leukopenia.
- Insomnia, headache, delusional perception, sleep disturbance, tremor.
- Cough, stridor.
- Diarrhea, bloating, dry mouth, abdominal pain, anorexia, constipation, GERD, dyspepsia, loose stools, flatulence, vomiting, gastritis, nausea, peptic ulcer, abdominal wall tension, discoloration of the tongue, esophagitis, pancreatitis, subileus, belching , peritonitis, halitosis, intestinal obstruction, ulceration of the lips, bleeding in the digestive tract, gingival hyperplasia, etc.
- Fatigue, thirst, pyrexia, weakness, flu-like illness, leg swelling.
- Hyperlipidemia, hypercholesterolemia, diabetes mellitus, hypophosphatemia.
- Bruises, alopecia.
- Pulmonary edema, tachycardia, ventricular extrasystoles.
- Conjunctivitis and blurred vision.
- Arthritis, muscle cramps, back pain.
- Malignant and benign tumors (e.g., skin papilloma, Kaposi’s sarcoma, basal cell carcinoma, squamous cell carcinoma, lymphoproliferative disorders).
- Increased blood creatinine, urethral stricture, hematuria, impotence, renal tubule necrosis.
It's important to know!
Mayfortic treats a patient only with highly qualified transplant specialists.
People who receive immunosuppressive therapy have an increased risk of developing malignant neoplasms, including skin. Therefore, during the treatment period, it is necessary to protect the body with clothing and use special sunscreens.
Patients receiving therapy with Mayfortic tablets should immediately inform the doctor of all unexpected hematomas, cases of infection, bleeding, and any manifestations of depressed bone marrow function.
Drug overdose
Cases of overdose when taking Mayfortik tablets have not been observed to date. However, this fact does not mean that a violation of the dosing regimen of the drug is permissible. Moreover, mycophenolic acid has a high degree of binding to plasma proteins (about 97%), that is, with an overdose of a drug, hemodialysis will be ineffective.
Special information
Excessive immunosuppression increases the risk of developing infections, including fatal infections.
In people who receive Mayfortic, it is necessary to regularly determine the number of white blood cells in the blood. With neutropenia, the drug should be discontinued.
The drug in question was used in combination with substances such as basiliximab, antithymocyte globulin, glucocorticoids and cyclosporin. The safety and effectiveness of Mayfortic with other immunosuppressive drugs have not been studied.
The effect of taking pills on a person’s ability to drive vehicles and work with complex mechanisms has not been established. At the same time, the pharmacodynamic features of “Mayfortika”, its principle of operation and registered side effects indicate a low probability of any effect. However, doctors should warn patients of possible negative effects after taking the medicine and caution when working that requires an increased concentration of attention.
Pediatric use
The safety and efficacy of mycophenolic acid in children has not been studied. Specialists have only limited data on the pharmacokinetic properties of this substance in babies who have undergone kidney transplantation. To date, specific recommendations for dosing medicines in children have not been developed.
Lactation and the period of pregnancy
The use of “Mayfortika” during gestation is possible only according to indications when the benefit for the expectant mother exceeds the probable risk to the child.
When using the drug during pregnancy, there is a high risk of developing congenital pathologies (including abnormalities of the inner ear, craniofacial region and extremities, as well as heart defects and congenital diaphragmatic hernias).
To date, it is not known whether mycophenolic acid is excreted in human milk. In order to avoid the development of adverse events in the newborn under the influence of the drug, it is necessary to stop taking "Mayfortika" or breastfeeding.
Similar tools
What can replace mycophenolic acid? There are few analogues of this tool. Usually it is replaced with Mycophenolic Acid - TL (Russian-made) or Felomic, (manufacturer: Nanofarma Development LLC, Russia). Both products have the same active ingredient as Mayfortik.
Terms and conditions of storage, formula
The structural formula of mycophenolic acid is presented in the photo below.
The drug in question belongs to list B. It must be kept in a place inaccessible to children, at a temperature of up to 30 degrees, only in the original packaging.
The medicine should be protected from exposure to steam and moisture. Shelf life is 2.5 years. The medication should not be used after the specified period.