Metabolite analysis of the urine, bile and feces was conducted by TLC, HPLC, mass spectrometry and NMR spectroscopy. Unaltered test article was the major labeled compound in all excreta. Major metabolic reactions included cyclization, hydrolysis and hydroxylation, yielding 7 major metabolites (M1, M2, M5, M6, M9, M10 and M19). M19, M10 and M9 were also identified in excreta from goats and hens, and in corn silage.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
毒性数据
大鼠LC50 >2,930毫克/立方米
LC50 (rat) >2,930 mg/m3
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
/SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/
/SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
解毒与急救
/SRP:/ 高级治疗：对于无意识、严重肺水肿或严重呼吸困难的病人，考虑进行口咽或鼻咽气管插管以控制气道。使用气囊面罩装置的正压通气技术可能有益。考虑使用药物治疗肺水肿……。对于严重的支气管痉挛，考虑给予β激动剂，如沙丁胺醇……。监测心率和必要时治疗心律失常……。开始静脉输注D5W /SRP: "保持开放"，最小流量/。如果出现低血容量的迹象，使用0.9%的生理盐水（NS）或乳酸林格氏液。对于伴有低血容量迹象的低血压，谨慎给予液体。注意液体过载的迹象……。使用地西泮或劳拉西泮治疗癫痫……。使用丙美卡因氢氯化物协助眼部冲洗……。 /Poisons A and B/
/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
非人类毒性摘录
实验室动物：兔子的急性暴露/初级眼刺激；轻度到中度刺激（7天内解决）。
/LABORATORY ANIMALS: Acute Exposure/ Primary Eye Irritation in Rabbits; mild to moderate irritation (resolved within 7 days).
Following oral administration /in rats/, Diflufenzopyr was partially absorbed and rapidly eliminated; 20-40% of the dose was eliminated in urine and 49-79% in feces. By contrast, intravenously dosed rats excreted 61-89% of the dose in urine. Elimination /half-time/ in urine and feces was 6 hr.
A metabolism study of diflufenzopyr was conducted in laying hens and lactating goats. The data showed diflufenzopyr was rapidly eliminated from the animals. With a feeding level of 10 ppm in the diet, residue levels in edible tissues, milk, and eggs were less than 0.12 ppm. ...
Wistar rats were administered (14)C-labeled Diflufenzopyr (SAN 835 H phenyl-labeled: radiochemical purity > 98%; pyridinyllabeled: radiochemical purity > 98%; unlabeled test article purity = 99.4%) according to each of four protocols: 1) a single i.v. dose at 1 mg/kg, 2) a single oral dose at 10 mg/kg, 3) a single oral dose at 1000 mg/kg, 4) fourteen daily oral doses of unlabeled test article at10 mg/kg followed by a single oral dose of labeled compound at 10 mg/kg. For protocols 1, 2 and 3, five males and five females were monitored according to each of 3 schedules: a) until sacrifice at 72 hrs post-dosing, b) until sacrifice at 24 hrs post-dosing, c) bile-duct cannulated animals followed until sacrifice at 48 hrs post-dosing. For the repeated dosing protocol, five males and five females were sacrificed at 24 hrs and 72 hrs after dosing with the labeled test article. Intravenous administration led to rapid elimination in the urine of between approximately 58 and 68% of both labeled forms by 7 hrs, and between 70 and 90% by 72 hrs. Of the approximate 7-20% excreted in the feces, almost all was a result of bilary excretion. Oral dosing at both 10 and 1000 mg/kg resulted in elimination of both labels mainly through the feces (approximately 55-80% by 72 hrs). Excretion in the urine accounted for approximately 20-39%, with approximately 3-10% excreted in the bile. Tissue retention at 72 hrs was low after either intravenous or oral dosing, being 0.37% or less for the phenyl-labeled compound (highest in blood) and 0.04% or less for the pyridinyl compound (highest in kidney and liver). The percent absorption for both labeled compounds, calculated by dividing the amount of labeled compound excreted in the urine after oral dosing by the amount excreted in the urine after i.v. dosing, was between 30 and 50%, with no difference between the 10 and 1000 mg/kg dose levels. ... There were no significant differences in test article absorption, elimination, tissue distribution or metabolism by males versus females. Likewise, high and low dose levels gave similar results, suggesting no saturation for absorption or elimination. There was less tissue retention of the pyridinyl-labeled compound and greater retention of the phenyl-labeled compound in the blood. Lastly, single versus multiple dosing showed that the test article did not bioaccumulate or induce metabolizing enzymes.
