Chimeric murine / human monoclonal antibody produced by recombinant DNA technology that acts as an immunosuppressant by specifically binding to the alpha chain of the receptor for interleukin 2 (also known as the CD25 antigen). It is a glycoprotein obtained by culturing a murine myeloma cell line, genetically modified to express plasmids that contain the human genes of the heavy and light constant chains as well as the genes of the heavy and light variable chains that encode the RFT5 antibody that acts as selective ligand to the receptor for IL-2.
International non-proprietary name
Basiliximab.
Composition
Each bulb contains 20 mg of basiliximab.
Pharmacokinetics
- Adults: Pharmacokinetic studies have been performed after single and repeated doses in kidney transplant patients. Cumulative doses ranged from 15 to 150 mg. Peak basiliximab concentrations after a 20 mg intravenous infusion over 30 min were 7.1 ± 5.1 mg / mL. At steady state, the volume of distribution is 8.6 ± 4.1 L, although the distribution among the different body compartments is not exactly known. The elimination half-life is 7.2 ± 3.2 days. No significant differences have been observed between genders, ages (between 20 and 69 years) or races.
- The pharmacokinetics have been evaluated in children (2 to 11 years) and adolescents (12-15 years) with kidney transplantation . In children, both volume of distribution and clearance are reduced by 50%, compared to adults. Pharmacokinetic parameters are not clinically significantly affected by age, body weight, or body surface area in this pediatric population. In adolescents, the disposition of basiliximab is similar to that of adults.
- When basiliximab serum levels are greater than or equal to 0.2 µg / mL, complete and constant binding of the product to IL-2 receptors is obtained. When concentrations fall below this threshold, the number of T cells expressing free receptors increases, returning to normal values within 1-2 weeks. The relationship between basiliximab serum concentrations and receptor saturation is identical in adults and children. In vitro studies have shown that basiliximab binds only to lymphocytes.
- With the recommended treatment regimen, the mean duration of IL-2 receptor saturation by basiliximab is 36 ± 14 days. However, the duration of blockade of these receptors is not known to be clinically significant. Its administration does not produce changes in the number of circulating lymphocytes or in their phenotypes.
Indications
Prophylaxis of organ rejection in kidney transplant patients (in combination with cyclosporine and corticosteroids).
Contraindications
Known hypersensitivity to basiliximab or to any of the excipients of the product. Lactation.
Precautions
- Immunoglobulins are known to cross the placental barrier. Contraception should be used before drug administration , during therapy, and 4 months after.
- LM: contraindicated during treatment and for a period of 4 months after the last dose, breastfeeding or the drug should be discontinued.
- Basiliximab can cause serious hypersensitivity reactions, even after the first exposure. In the event that a patient who has experienced a hypersensitivity reaction has to be re-exposed, extreme caution will be exercised. The potential risks that such reexposure may cause on immunosuppression are unknown.
Adverse reactions
Hypersensitivity
Serious reactions including anaphylaxis have been observed, both acute (onset in the first 24 h) after the first exposure to basiliximab and on re-exposure, after several months. These reactions include hypotension , tachycardia , heart failure, dyspnea , bronchospasm, pulmonary edema , respiratory failure, rash, itching, and sneezing . Immunogenicity: specific antibodies to other medications.
Other reactions
Constipation , nausea , diarrhea , abdominal pain , vomiting , dyspepsia , moniliasis , hyperkalemia, hypokalemia , hyperglycemia, hyperuricemia, hypophosphataemia , hypocalcemia , weight gain, hypercholesterolemia, acidosis; headaches, tremor, dizziness, insomnia, dysuria, increased urea nitrogen, urinary tract infections, pain, peripheral edema, fever , viral infections, leg edema , asthenia , high blood pressure , dyspnea, upper respiratory tract infections, cough , rhinitis , pharyngitis , surgical wound complications, acne , anemia .
Interactions
- No studies have been performed to determine possible interactions with other drugs.
- In clinical studies, basiliximab has been administered with azathioprine, cyclosporine, corticosteroids, mycophenolate mofetil, and muromonab, with no increase in adverse reactions.
Posology
Adults
2 doses of 20 mg each. The first should be administered within 2 hours prior to transplantation, and the second should be administered 4 days after the operation. This last dose should be avoided due to serious complications such as severe hypersensitivity or loss of the transplant.
Kids
For children and adolescents 2 to 15 years of age, the recommended doses are 12 mg / m2 each, with a maximum of 20 mg / dose. As in the case of adults, the first dose should be administered within 2 hours prior to transplantation and the second within 4 days, unless serious complications occur.
Treatment of acute overdose and serious adverse effects
Anaphylaxis reactions must be anticipated and the necessary elements available for their treatment. General measures.
Basic information to the patient
Nothing to point out.
Distribution level
Exclusive use of hospitals
Regulation to prescription
Only for Transplant Program.
VEN classification
Special medicine
Producer laboratory
International
ATC code
L04AC02
Defined daily dose
0.004 g