Tacrolimus (FK506, Advagraf, Prograf, Protopic, Tacrosel)
Tacrolimus is the international name of a medicinal drug from the group of immunosuppressants (cytostatics), which is used for the prevention and treatment of liver, kidney and heart transplant rejection reactions, as well as for immunosuppressive therapy resistant to standard regimens.
Trade names: advagraf, prograf, tacrosel, protopik, FK506. You can get a detailed description of the drug here.
Tacrolimus is a potent drug, so it is used with extreme caution under the control of the patient's health condition. Special attention is paid to the selection of the dosage regimen of the drug, taking into account the individual biological characteristics of each patient – the condition of the liver and kidneys, endocrine system, body weight, age, diet, etc.
The choice of the optimal dose is complicated by the fact that a positive therapeutic effect occurs when the drug concentration in the blood is 5-20 ng/ml. That is, the range is very narrow. Period of maximum concentration - 1-3 hours after administration, period of equilibrium concentration of the drug, after regular administration - 3 days.
If the amount of tacrolimus is insufficient, the desired result from the treatment does not occur, and if its level in the blood is higher than the therapeutic norm, the likelihood of severe side effects of the drug increases. According to the official medicines register of the Russian Federation, blood samples should be obtained 12 hours after the last dose of Tacrolimus for drug monitoring when taking Tacrolimus orally.
The most successful treatment is observed at concentrations of less than 20 ng/ml during this period. However, there are other monitoring protocols based on concentration studies Tacrolimus after 2 or 4 hours.
Tacrolimus itself has the following side effects:
- Very often 1/10
- Often 1/100
- Not often 1/1000
- Rarely 1/10000
Cardiovascular system:
- Increased BP
- Decreased BP, tachycardia, arrhythmias, conduction disturbances, thromboembolism, ischemia, angina, vascular disease
- ECG changes, heart attack, heart failure, shock, myocardial hypertrophy, cardiac arrest
Digestive system
- Diarrhea, nausea, vomiting
- Increased activity of liver enzymes, abdominal pain, constipation, weight changes, appetite disturbances, inflammation of the GI tract, jaundice, biliary tract and gallbladder dysfunction
- Ascites, intestinal obstruction, hepatotoxicity, pancreatitis
- Liver failure
Hematopoiesis
- Anemia, leukopenia, thrombocytopenia, hemorrhagia, leukocytosis, blood clotting disorders
- Suppression of hematopoietic function, pancytopenia, microangiopathy
Renal system
- Renal dysfunction, creatinine increase
- Renal tissue damage, renal failure
- Proteinuria
Musculoskeletal system
- Convulsions
- Myasthenia gravis, arthritis
Nervous system and senses
- Tremor, headache, insomnia
- Dysesthesia, parasthesia, visual and hearing impairment, confusion, depression, dizziness, agitation, neuropathy, ataxia, psychosis, hallucinations, encephalopathy
- Increased intracranial pressure, amnesia, cataracts, speech impairment, paralysis, coma, deafness
- Blindness
Respiratory system
- Dyspnea, pleural effusion
- Pulmonary atelectasis, bronchospasm
Skin
- Itching, alopecia, rash, sweating, acne
- Hirsutism
- Lyell syndrome
- Stevens-Johnson syndrome
Metabolic disorders
- Hyperglycemia, hyperkalemia
- Hypomagnesemia, hyperlipidemia, hypophosphatemia, hypokalemia, hyperurecemia, hypokalcemia, hyponatremia, hypovolemia, acidosis, dehydration
- Hypoproteinuria, hyperphosphatemia, increased amylase, hypoglycemia
There is a risk of malignant and benign neoplasms associated with Epstein-Barr virus, lymphoproliferative diseases and melanoma. The course of viral, bacterial, fungal and protozoal infectious diseases worsens.
To avoid or reduce the risk of side effects from taking tacrolimus, it is necessary to strictly monitor its concentration in the blood to be able to reasonably adjust the dose of the medicines. For this purpose, test is used in medical practice: drug monitoring of tacrolimus levels in the blood.