地胺磷 | 950-10-7

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磷酸及其衍生物
• 中文名称: 地胺磷
• 中文别名: 地安磷[含量＞5]；地安磷；二噻磷；二噻磷乳剂
• 英文名称: N-diethoxyphosphoryl-4-methyl-1,3-dithiolan-2-imine
• 英文别名: Mephosfolan
• CAS: 950-10-7
• 化学式: C₈H₁₆NO₃PS₂
• 分子量: 269.3
• InChiKey: LTQSAUHRSCMPLD-UHFFFAOYSA-N

物化性质

• 稳定性/保质期：
  明火可燃，受热时会释放出有毒的氧化磷、氧化硫和氧化氮气体。

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  98.5
• 氢给体数：
  0
• 氢受体数：
  6

ADMET

代谢

在甲基上发生氧化，形成一级醇，同时还在植物中形成硫氰酸根离子。

Undergoes oxidation at the methyl group to form primary alcohol in addition to the formation of the thiocyanate ion in plants.

来源:Hazardous Substances Data Bank (HSDB)

代谢

在大鼠尿液中，服用赛特罗兰（cytrolane）后，薄层色谱（TLC）和质谱（MS）表明甲基部分被攻击以产生羧酸离子。P-N键的水解随后是环开和释放出硫氰酸盐。后者是主要的组织代谢物。

In the urine of rats dosed with cytrolane, TLC and MS indicated that the methyl moiety was attacked to produce carboxylic ions. Hydrolysis of the P-N bond was followed by ring opening and release of thiocyanate. The latter was the main tissue metabolite.

来源:Hazardous Substances Data Bank (HSDB)

代谢

(14)C Cytoleine ..., 在亚氨基碳上进行标记，被应用于棉植物的叶片上。42天后，大约60%的标记以不变的Cytoleine形式被回收。一个次要代谢物...和一个主要代谢物...被分离为葡萄糖苷。在用beta-葡萄糖苷酶水解葡萄糖苷部分后，确定了苷元的身份。另一个次要代谢物被鉴定为硫氰酸盐。其他观察到的代谢物未被鉴定。羟基甲基及其葡萄糖苷在其他棉花研究中也有观察到。

(14)C Cytrolane ..., labeled at the imino carbon, was applied to leaves of cotton plants. After 42 days, about 60% of the label was recovered as unchanged cytrolane. A minor metabolite ... and a major metabolite ... were isolated as glucosides. Identification of the aglycones was made after hydrolysis of the glucosidic moiety with beta-glucosidase. Another minor metabolite was identified as thiocyanate. Other observed metabolites were not identified. The hydroxymethyl and its glucoside were also observed in other studies with cotton.

来源:Hazardous Substances Data Bank (HSDB)

代谢

当使用(14)C标记的赛特隆烷施用于水稻时，大约91%的残留物是未改变的物质。其余的放射性由大约17种代谢物组成。认为不可提取的放射性以(14)C标记的纤维素、木质素和淀粉的形式存在。养在稻田里的鱼将赛特隆烷代谢成硫氰酸盐和许多其他代谢物。

When (14)C labeled cytrolane was applied to rice, about 91% of the residue was unchanged material. The remainder of the radioactivity was composed of about 17 metabolites. Unextractable radioactivity was believed to be in the form of (14)C-labeled cellulose, lignin and starch. Fish kept in the rice paddy metabolized cytrolane to thiocyanate and many other metabolites.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 副作用

其他毒物 - 有机磷

Other Poison - Organophosphate

来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases

毒理性

• 解毒与急救

1. 确保气道通畅，如有必要，通过抽吸分泌物来清理。如果呼吸抑制，通过机械辅助肺通气给予氧气。在给予阿托品之前尽可能提高组织氧合，以最小化心室颤动的风险。在严重中毒的情况下，可能需要机械辅助肺通气数天。2. 通过静脉注射硫酸阿托品，如果静脉注射不可能，则通过肌肉注射。在中度到重度中毒的情况下：成人剂量和12岁以上的儿童：每15分钟重复给予0.4-2.0毫克，直到阿托品化。用0.02-0.05毫克/千克体重的重复剂量维持阿托品化。/有机磷农药/

1. INSURE THAT A CLEAR AIRWAY EXISTS BY ASPIRATION OF SECRETIONS IF NECESSARY. ADMIN OXYGEN BY MECHANICALLY ASSISTED PULMONARY VENTILATION IF RESPIRATION IS DEPRESSED. IMPROVE TISSUE OXYGENATION AS MUCH AS POSSIBLE BEFORE ADMIN ATROPINE TO MINIMIZE RISK OF VENTRICULAR FIBRILLATION. IN SEVERE POISONINGS, IT MAY BE NECESSARY TO SUPPORT PULMONARY VENTILATION MECHANICALLY FOR SEVERAL DAYS. 2. ADMIN ATROPINE SULFATE IV, OR IM IF IV INJECTION IS NOT POSSIBLE. ... IN MODERATELY SEVERE POISONING: ADULT DOSAGE AND CHILDREN OVER 12 YR: 0.4-2.0 MG REPEATED EVERY 15 MIN UNTIL ATROPINIZATION IS ACHIEVED. MAINTAIN ATROPINIZATION WITH REPEATED DOSAGE OF 0.02-0.05 MG/KG BODY WEIGHT. /ORGANOPHOSPHATE PESTICIDES/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

2. 严重中毒的人可能对阿托品表现出显著的耐受性；可能需要两倍或更多倍于上述建议的剂量。可以根据需要增加阿托品的剂量并缩短给药间隔以控制症状。当阿托品需求量很大时，可能需要持续静脉输注阿托品。逆转毒蕈碱样症状和体征，而不是任意剂量限制，是期望的终点。应尽可能使用不含防腐剂的阿托品产品。注意：未中毒或仅轻微有机磷中毒的人可能会因大剂量阿托品出现阿托品中毒的迹象。发热、肌肉颤动和谵妄是阿托品中毒的主要迹象。如果患者在完全阿托品化时出现这些症状，应暂时停止阿托品给药，同时重新评估中毒的严重程度。/有机磷杀虫剂/

2. SEVERELY POISONED INDIVIDUALS MAY EXHIBIT REMARKABLE TOLERANCE TO ATROPINE; TWO OR MORE TIMES THE DOSAGES SUGGESTED ABOVE MAY BE NEEDED. THE DOSE OF ATROPINE MAY BE INCREASED AND THE DOSING INTERVAL DECREASED AS NEEDED TO CONTROL SYMPTOMS. CONTINUOUS INTRAVENOUS INFUSION OF ATROPINE MAY BE NECESSARY WHEN ATROPINE REQUIREMENTS ARE MASSIVE. REVERSAL OF MUSCARINIC SYMPTOMS AND SIGNS, NOT AN ARBITRARY DOSE LIMIT, IS THE DESIRED END-POINT. PRESERVATIVE-FREE ATROPINE PRODUCTS SHOULD BE USED WHENEVER POSSIBLE. NOTE: PERSONS NOT POISONED OR ONLY SLIGHTLY POISONED BY ORGANOPHOSPHATES MAY DEVELOP SIGNS OF ATROPINE TOXICITY FROM SUCH LARGE DOSES. FEVER, MUSCLE FIBRILLATIONS, AND DELIRIUM ARE THE MAIN SIGNS OF ATROPINE TOXICITY. IF THESE APPEAR WHILE THE PATIENT IS FULLY ATROPINIZED, ATROPINE ADMINISTRATION SHOULD BE DISCONTINUED, AT LEAST TEMPORARILY, WHILE THE SEVERITY OF POISONING IS REEVALUATED. /ORGANOPHOSPHATE PESTICIDES/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

3. 在给予解磷定之前，抽取（肝素化）血液样本进行胆碱酯酶分析，因为解磷定往往会逆转胆碱酯酶的抑制。4. 在严重中毒的情况下给予解磷定（普罗帕明，2-PAM）……在这种情况下，呼吸抑制、肌肉无力和抽搐都非常严重。……成人剂量（以及12岁以上的儿童）：静脉注射1.0-2.0克，每分钟不超过0.2克。儿童剂量（12岁以下）：静脉注射20-50毫克/千克（根据严重程度），每分钟注射的总量不超过一半。剂量……如果需要，可以在1-2小时后重复，然后每隔10-12小时重复一次。在非常严重的中毒情况下，剂量……可以加倍。/有机磷农药/

3. DRAW BLOOD SAMPLE (HEPARINIZED) FOR CHOLINESTERASE ANALYSIS BEFORE ADMINISTRATION OF PRALIDOXIME, WHICH TENDS TO REVERSE THE CHOLINESTERASE DEPRESSION. 4. ADMIN PRALIDOXIME (PROTOPAM, 2-PAM) IN CASES OF SEVERE POISONING ... IN WHICH RESP DEPRESSION, MUSCLE WEAKNESS & TWITCHINGS ARE SEVERE. ... ADULT DOSAGE AND CHILDREN OVER 12): GIVE 1.0-2.0 G IV @ NO MORE THAN 0.2 G/MIN. CHILD'S DOSE (UNDER 12 YR): GIVE 20-50 MG/KG (DEPENDING ON SEVERITY) IV, INJECTING NO MORE THAN HALF TOTAL DOSE/MIN. DOSAGE ... MAY BE REPEATED IN 1-2 HR THEN @ 10-12 HR INTERVAL IF NEEDED. IN VERY SEVERE POISONINGS, DOSAGE ... MAY BE DOUBLED. /ORGANOPHOSPHATE PESTICIDES/

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 解毒与急救

4. 准备好机械辅助呼吸，如果呼吸抑制...下降...。5. 对于因皮肤、衣物、头发和/或眼睛接触有机磷污染而中毒的患者，必须在进行复苏和解毒措施的同时进行去污处理，以保护生命。... 6. 如果...摄入的量足以引起中毒，必须清空胃和肠道。A. 通过插管、抽吸和灌洗清空胃，使用等渗盐水中的活性炭悬浮液。必须采取严格措施保护呼吸道免受反流的物质吸入。如果受害者昏迷或意识模糊，在进行胃插管之前插入带套囊的气管内插管。在胃插管和灌洗过程中，保持受害者头部低于胃部水平...。保持受害者头部向左转。/有机磷杀虫剂/

4. BE PREPD TO ASSIST PULMONARY VENTILATION MECHANICALLY IF RESP ... DEPRESSED ... . 5. IN PATIENTS WHO HAVE BEEN POISONED BY ORGANOPHOSPHATE CONTAMINATION OF SKIN, CLOTHING, HAIR, AND/OR EYES, DECONTAMINATION MUST PROCEED CONCURRENTLY WITH WHATEVER RESUSCITATIVE AND ANTIDOTAL MEASURES ARE NECESSARY TO PRESERVE LIFE. ... 6. IF ... INGESTED IN QUANTITY PROBABLY SUFFICIENT TO CAUSE POISONING, THE STOMACH AND INTESTINE MUST BE EMPTIED. A. EMPTY THE STOMACH BY INTUBATION, ASPIRATION, AND LAVAGE, USING SLURRY OF ACTIVATED CHARCOAL IN ISOTONIC SALINE. RIGOROUS PRECAUTIONS MUST BE TAKEN TO PROTECT THE AIRWAY FROM ASPIRATION OF REGURGITATED. IF VICTIM IS UNCONSCIOUS OR OBTUNDED, INSERT A CUFFED ENDOTRACHEAL TUBE PRIOR TO GASTRIC INTUBATION. KEEP VICTIM'S HEAD BELOW LEVEL OF STOMACH DURING GASTRIC INTUBATION AND LAVAGE ... . KEEP VICTIM'S HEAD TURNED TO THE LEFT. /ORGANOPHOSPHATE PESTICIDES/

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

被根和叶吸收。

Absorbed by the roots and leaves.

来源:Hazardous Substances Data Bank (HSDB)