Methoxyflurane
(Synonyms: 甲氧氟烷) 目录号 : GC38814
Methoxyflurane 是一种卤化的挥发性麻醉剂，在亚麻醉剂量下具有有效的镇痛作用。Methoxyflurane 在小型实验动物中广泛用作麻醉剂，已有数十年历史。Methoxyflurane 具有肾毒性的风险。
Cas No.:76-38-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Methoxyflurane is a halogenated volatile anaesthetic agent with potent analgesic effects at sub-anaesthetic doses. Methoxyflurane widely used as an open-circuit anaesthetic in small laboratory animals for several decades. Methoxyflurane has the risk of nephrotoxicity[1][2].
Methoxyflurane is delivered via a hand-held inhaler[3].
The developmental toxicity of trace, subanesthetic, and anesthetic exposure to Methoxyflurane is examined in Swiss/ICR mice. No adverse effects on reproduction or fetal development were demonstrated following exposure to trace (2 ppm) and subanesthetic (60 ppm) concentrations of Methoxyflurane for 4 hours daily on days 6 through 15 of pregnancy. Exposure to an anesthetic concentration (2000 ppm; 0.2%) for the same period resulted in decreased fetal weight, decreased ossification, and delayed renal maturation. Additionally, the incidence of minor skeletal anomalies was increased. It is concluded that gestational exposure of mice to trace of subanesthetic concentrations of Methoxyflurane does not result in reproductive loss or morphologic abnormalities in their offspring[4].
[1]. Occupational exposure to methoxyflurane administered for procedural sedation: an observational study of 40 exposures. Br J Anaesth. 2018 Jun;120(6):1435-1437. [2]. Porter KM, et al. The role of inhaled methoxyflurane in acute pain management. Open Access Emerg Med. 2018 Oct 18;10:149-164. [3]. Methoxyflurane nephrotoxicity. JAMA. 1971 Aug 16;217(7):958-9. [4]. Wharton RS, et al., Developmental toxicity of methoxyflurane in mice. Anesth Analg. 1980 Jun;59(6):421-5.
| Cas No. | 76-38-0 | SDF | |
| 别名 | 甲氧氟烷 | ||
| Canonical SMILES | COC(F)(F)C(Cl)Cl | ||
| 分子式 | C3H4Cl2F2O | 分子量 | 164.97 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.0617 mL | 30.3085 mL | 60.6171 mL |
| 5 mM | 1.2123 mL | 6.0617 mL | 12.1234 mL |
| 10 mM | 0.6062 mL | 3.0309 mL | 6.0617 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
The Reincarnation of Methoxyflurane
J Anesth Hist 2020 Jun;6(2):79-83.PMID:32593381DOI:10.1016/j.janh.2019.07.001.
Methoxyflurane was an inhaled agent commonly used for general anesthesia in the 1960s, but its clinical role gradually decreased in the 1970s because of reports of dose-dependent nephrotoxicity. In 1999 its manufacturer, Abbott Laboratories, discontinued distribution of Methoxyflurane in the United States and Canada. Outside of North America, however, Methoxyflurane has been reborn as an inhaled analgesic used for pain relief in the prehospital setting and for minor surgical procedures. First used in Australia and New Zealand, and subsequently in over thirty-seven other countries, low concentrations of Methoxyflurane are administered with a hand-held inhaler which provides conscious sedation, so that patients can self-assess their level of pain and control the amount of inhaled agent. The Penthrox inhaler, originally developed in Australia after several other hand-held vaporizers were tried, is currently being used worldwide as a portable and disposable self-administered agent delivery system. Methoxyflurane-induced nephrotoxicity continues to be a major concern, but with cautious administration of recommended doses Methoxyflurane has been established as a remarkably safe analgesic agent with minimal side effects for patients in need of rapid and potent pain relief.
Methoxyflurane nephropathy
Environ Health Perspect 1976 Jun;15:111-9.PMID:1001288DOI:10.1289/ehp.7615111.
Investigations of methoxyflurane-induced nephrotoxicity in man have been extensively aided by the use of an animal model. To be of value the animal model must share similar metabolic pathways with man and have the same clinical manifestations of the diseases process. The Fischer 344 rat appears to meet these criteria. The predominant factors in the production of Methoxyflurane nephrotoxicity appear to be high Methoxyflurane dosage and serum inorganic fluoride concentration. It is likely that secondary factors include: (1) a high rate of Methoxyflurane metabolism and sepsitivity of the kidney to inorganic fluoride toxicity: (2) concurrent treatment with other nephrotoxic drugs; (3) preexisting renal disease; (4) surgery of the urogenital tract, aorta, or renal vasculative; (5) repeat administration of Methoxyflurane due to accumulation of inorganic fluoride and, perhaps, Methoxyflurane induction of its own metabolism: and (6) concurrent treatment with enzyme-inducing drugs such as phenobarbital.
Methoxyflurane: a review with emphasis on its role in dental practice
Aust Dent J 2016 Jun;61(2):157-62.PMID:26101794DOI:10.1111/adj.12346.
Methoxyflurane was developed as an anaesthetic agent and introduced into clinical practice in 1960. It soon became evident that it possessed analgesic properties that other drugs did not. Due to toxicity concerns, it lost favour in general anaesthesia and had been largely abandoned by the late 1970s. The manufacturer withdrew it in 1999, and the Food and Drug Administration in the United States did not renew its licence in 2005. It has also been withdrawn by the European Union. However, it continues to be used in Australasia, primarily as an inhaled self-administered analgesic by emergency services immediately following trauma. It has become attractive for use in dental practice, likely due to its effectiveness as an analgesic and its additional sedative qualities. Its acceptance is controversial as its use in dentistry is largely elective. Despite its good safety record in analgesic doses, adverse reactions have been recorded. Practitioners should be well aware of risks associated with its use before considering administration, and carefully assess whether or not there are equally good alternative options that do not the carry the same risks. Methoxyflurane is reviewed below with an emphasis on its use in dental practice.
Analgesic use of inhaled Methoxyflurane: Evaluation of its potential nephrotoxicity
Hum Exp Toxicol 2016 Jan;35(1):91-100.PMID:25926525DOI:10.1177/0960327115578743.
Methoxyflurane is a volatile, halogenated analgesic, self-administered in a controlled low dose from the Penthrox(®) inhaler for short-term pain relief. It was formerly used in significantly higher doses to produce anaesthesia, when it caused a specific type of dose-related renal tubular damage. The pathogenesis of the renal damage and clinical use of Methoxyflurane are discussed here with evidence that a low but effective analgesic dose is not associated with the risk of renal adverse effects. The maximum dose employed to produce analgesia is limited to Methoxyflurane 6 mL/day and 15 mL/week, producing a minimum alveolar concentration (MAC) of 0.59 MAC-hours. Renal damage is due to the metabolism of Methoxyflurane and release of fluoride ions. Exposure of humans to Methoxyflurane ≤2.0 MAC-hours, resulting in serum fluoride ≤40 µmol/L, has not been associated with renal tubular toxicity. The safety margin of analgesic use of Methoxyflurane in the Penthrox ((®)) inhaler is at least 2.7- to 8-fold, based on Methoxyflurane MAC-hours or serum fluoride level, with clinical experience suggesting it is higher. It is concluded from clinical experience in emergency medicine, surgical procedures and various experimental and laboratory investigations that the analgesic use of Methoxyflurane in subanaesthetic doses in the Penthrox inhaler does not carry a risk of nephrotoxicity.
Precautions when using Methoxyflurane
Vet Clin North Am Small Anim Pract 1992 Mar;22(2):318-20.PMID:1585563DOI:10.1016/s0195-5616(92)50621-0.
Methoxyflurane has a high blood/gas partition coefficient and a low vapor pressure. Mask inductions may be excessively slow, necessitating early high vaporizer control knob settings or additional injectable induction agent. Recoveries may be very prolonged. Methoxyflurane is extensively metabolized, and this may be associated with hepatotoxicity and nephrotoxicity.