STUDY ON ACUTE TOXICITY AND ANTIDOTE ACTIVITY OF LYOPHOBIC DRUG “CALCIUM FOLINATE”
Abstract
To combat the toxic effects of methotrexate on bone marrow cells and GI (gastrointestinal tract) tract causing a disorder of nucleic acid synthesis and the growth of proliferating tissues, a lyophobic drug “Calcium folinate” was used as an antidote for the development of Necrotizing ulcerative stomatitis, enteropathy, and etcetera. It is intended for oral and parenteral administration with the bioavailability approximately 97% for a 25 mg dose, 75% for a 50 mg dose, and 37% for a 100 mg dose. In combination with fluorouracil, it can be used in the palliative treatment on patients with colorectal cancer as well. Calcium folinate solution is intended for intravenous (i / v) administration with the maximum rate of 160 mg/min and intramuscular (i/m), while intrathecal (endolumbar) administration of the solution is strictly prohibited. In form of infusion solutions diluted with 0.9% sodium chloride solution or 5% glucose solution, calcium folinate is used for the treatment of megaloblastic anemia and the therapy and prevention of folate deficiency in cases when oral administration of folic acid is impossible or for some reason ineffective, for example, in patients with parenteral nutrition or severe malabsorption syndrome. The study of acute toxicity was carried out according to conventional methods on 72 white mice (both sexes) within 14 days. As a result, it was found that under the drug administration, there is a significant decrease in death compared with the control 6.00 to 1.83 (0.43÷3.23). The study of the antidote activity of the drug showed that the drug has a reliable antidote effect.
Keywords:
Calcium folinate, Methotrexatum, acute toxicity, antidote activity, JV «Jurabek Laboratories».Full Text:
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