Chemical Properties
Butafosfan is a white crystalline powder, very easily is dissolved in water. soluble in organic solvents such as ethanol, which should be purged with an inert gas. The solubility of butafosfan in ethanol is approximately 1 mg/ml. It has the effect that improves energy metabolism and strengthen immunologic function.
Uses
Butafosfan is an organic phosphorus supplement that is given, most commonly with cyanocobalamin, to cattle, swine, horses, and poultry for the prevention or treatment of deficiencies. When given with cyanocobalamin, butafosfan alters lipid metabolism, serving to decrease the prevalence of subclinical ketosis.
benefits
Butafosfan works by increasing the body's ability to metabolise glucose and other nutrients, as well as supporting the production of adenosine triphosphate, which is the main source of cellular energy. Cyanocobalamin, a form of vitamin B12, is essential for normal nerve function and red blood cell formation.
Mechanism of action
Butafosfan works by improving the body’s ability to metabolize glucose and other nutrients, as well as by supporting the production of ATP, which is the primary source of energy for cells. The association of Butafosfan and cyanocobalamin could favors the phosphorylation of molecules that intermediate metabolic pathways, such as a gluconeogenesis, glycolysis, and the Krebs cycle, improving the synthesis of the co-nutrients (ATP and ADP mainly) and consequently increasing blood glucose. However, it is still unclear if these results refer mainly to one of the nutrients, Butafosfan or cyanocobalamin[1].
Side effects
Common side effects may include indigestion, such as vomiting or diarrhoea, and local irritation at the injection site. In rare cases, more serious side effects, such as allergic reactions or neurological damage, may occur.
Metabolism
In vitro metabolism studies in rat liver microsomes and hepatocytes revealed no metabolites of butafosfan using liquid chromatography-mass spectrometry (LC-MS) for the analysis. The intravenous administration of butafosfan to cattle at a dose level of 5.6 mg/kg bw as a singledose resulted in a pharmacokinetic profile in serum corresponding to a three-compartment model.Three half-lives were calculated to 1.7 minutes,13.2 minutes and 1.38 hours; the latter describingthe terminal elimination process. Urine is the major route of excretion of butafosfan and a meanof 74% and 0.2% of parent compound was recovered in urine and faeces respectively, within thefirst 12 hours. This study was not radiolabelled, but was conducted in accordance with GLPstandards and the analyses were performed with liquid chromatography-tandem massspectrometry (LC-MS/MS).
Toxicity evaluation
The acute toxicity of butafosfan is very low. The oral LD50 in mice was approximately 16 000 mg/kg bw. After parenteral administrations, the following LD50 values were obtained in mice: approximately 21 000 mg/kg bw (subcutaneously), approximately 10 000 mg/kg bw (intravenously) and greater than 2500 mg/kg bw (intraperitoneally). Mice dosed orally or subcutaneously died within 3 and 2 days, respectively, while survivors had recovered by that time. The LD50 value in chicken (intramuscularly) was 9974 mg/kg bw. Observed toxic signs were excitation, cyanosis, sternal recumbency and diarrhoea.
References
[1] Weiller M, et al. Butaphosphan Effects on Glucose Metabolism Involve Insulin Signaling and Depends on Nutritional Plan. Nutrients, 2020; 12: 1856.