Basiliximab
When ATH:
L04AC02
Characteristic.
Chimeric mousy / human monoclonal antibody (IgG1k), obtained by recombinant DNA technology.
Soluble in water. The molecular weight of about 144 kDa.
Pharmacological action.
Immunosuppressive.
Application.
Prevention of acute graft rejection (as part of combination immunosuppressive therapy with cyclosporine and corticosteroids) in patients with kidney transplant.
Contraindications.
Hypersensitivity.
Pregnancy and breast-feeding.
There was no maternal toxicity, эmbriotoksichnosti, teratogenicity in monkeys Cynomolgus the introduction of them basiliximab. Immunotoxicological studies have not been conducted in the offspring.
Considering, basiliximab that is an immunoglobulin G (IgG1k), and IgG molecules pass through the placental barrier, and the fact, that IL-2 receptor may play an important role in the development of the immune system, use during pregnancy is possible, if the effect of therapy outweighs the potential risk to the fetus. There are no adequate and well-controlled studies in pregnant women have not held.
Women of childbearing age should use effective contraception before treatment, as well as for 4 Months after its completion.
Category actions result in FDA - B. (The study of reproduction in animals revealed no risk of adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not done.)
Nursing women should decide the issue of termination of breastfeeding (unknown, Do penetrates basiliximab in breast milk. Many drugs, incl. human antibodies, excreted in the breast milk of women. There is a potential risk of adverse effects).
Side effects.
According to data from four randomized, double-blind, placebo-controlled clinical trials, side effects were observed in 96% patients (in Group, treated drug, and the group, placebo). The most frequently observed adverse effects on the gastrointestinal tract (69%, in the placebo group - 67%).
From the digestive tract: ≥10% – constipation, abdominal pain, nausea, vomiting, dyspepsia, diarrhea; 3-10% - esophagitis, flatulence, gastroenteritis, gastrointestinal bleeding, giperplaziya right, ground, ulcerative stomatitis.
From the nervous system and sensory organs: ≥10% – tremor, headache, insomnia; 3-10% — asthenia, malaise, dizziness, neuropathy, gipesteziya, paraesthesia, ažitaciâ, alarm, depression, Cataract, conjunctivitis, blurred vision.
Cardio-vascular system and blood (hematopoiesis, hemostasis: ≥10% — hypertension, anemia; 3–10% – worsening hypertension, gipotenziya, angina, heart failure, chest pain, arrhythmia, Atrial fibrillation, tachycardia, disease, hematoma, gemorragija, purpura, thrombocytopenia, thrombosis, polycythemia, leukopenia.
From the respiratory system: ≥10% - shortness of breath, upper respiratory tract infection; 3–10% — bronchitis, bronchospasm, cough, pharyngitis, pneumonia, lung diseases, pulmonary edema, rhinitis, sinusitis.
On the part of the musculoskeletal system: 3–10% – back pain, myalgia, arthralgia, arthropathy, fractures, convulsions.
With the genitourinary system: ≥10% - urinary tract infections; 3–10% – swelling of the genitals, impotence, albuminuria, bladder diseases, dizurija, frequent urination, hematuria, increase in non-protein nitrogen, oligurija, impairment of renal function, renal tubular necrosis, ureteropathy, urinary retention.
For the skin: ≥10% – acne, Surgical wound complications; 3–10% — herpes simplex, herpes zoster, hypertryhoz, skin diseases, skin ulceration.
Allergic reactions: 3-10% - fast, rash, swelling of the face, generalized edema.
Other: ≥10% – pain syndrome, peripheral edema, fever, viral infection, hyperkalemia / hypokalemia, hypercholesterolemia, gipofosfatemiя, hyperuricemia; 3–10% - accidental injury, infection, moniliaz, swelling of the legs, chills, sepsis, Acidosis, degidratatsiya, hypercalcemia / hypocalcemia, hyperlipidemia, hypertriglyceridemia, gipoglikemiâ, gipomagniemiya, hypoproteinemia, weight gain, cyst.
Malignancy. In controlled clinical trials in renal transplantation significant increase in the number of malignant lymphoproliferative disease in patients on a background of basiliximab was not observed (Frequency was <1%). However, we can not exclude an increased risk of malignant diseases in the application of immunosuppressive therapy.
Infection. The total number of cytomegalovirus infections was similar in patients on background basiliximab (17%) placebo (15%), receiving double or triple immunosuppressive therapy. However, in patients with triple-immunosuppressive therapy frequency of severe CMV infection was higher (11%), than placebo (5%).
Post-marketing studies. Pronounced acute hypersensitivity reactions, including anaphylaxis, characterized by hypotension, taxikardiej, Heart Failure, shortness of breath, wheezing, bronchospasm, pulmonary edema, respiratory failure, krapivnicej, rash, itching and / or sneezing, as well as the cytokine release syndrome, It has been reported with use of basiliximab.
Cooperation.
In clinical studies with a joint appointment with other immunosuppressants (incl. azathioprine, corticosteroids, cyclosporine, mycophenolic mofetil) interactions between registered.
Dosing and Administration.
B / bolus or infusion (the drug is pre-diluted in 5 ml water for injection, then bring the volume to 50 ml 0,9% solution of sodium chloride or 5% glucose solution) for 20-30 min, adults and children weighing more than 40 kg - in dose 20 mg for 2 h before transplantation and after 4 day after surgery (in the case of rejection of the transplanted organ is not administered a second dose). For children weighing less than 40 kg total dose is 20 mg (2 administration of the 10 mg).
Precautions.
Basiliximab may only use doctors, experienced in immunosuppressive therapy following organ transplantation. Patients should be warned of the possible risk, associated with immunosuppressive therapy.
During and for a short time after infusion basiliximab requires monitoring of cardiac function and lung (to prevent possible anaphylactoid reaction).
Cases of developing hypersensitivity reactions, including anaphylaxis, both the first, and the second administration basiliximab. In case of hypersensitivity reactions further application basiliximab contraindicated.
When using basiliximab are at increased risk of wound infection. It should be taken into account, that patients, receiving immunosuppressants, increased risk of systemic infections, and lymphoproliferative malignancies.
Be wary appoint patients with infectious diseases (may increase), malignant tumors , incl. history (immunosuppression increases the likelihood of tumor diseases). Dental procedures should be completed before the start of therapy, carry them with caution during treatment (possible increase in the incidence of microbial infections, slowing the healing process).
