盐酸利多卡因 | 6108-05-0

• 物质功能分类: 原料药 - 麻醉剂 - 局部麻醉剂
• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 盐酸利多卡因
• 中文别名: 一水N-二乙基氨基乙酰基-2,6-二甲基苯胺盐酸盐；N-二乙基氨基乙酰基-2,6-二甲基苯胺盐酸盐一水合物；一水盐酸利多卡因；利多卡因HCL；盐酸利多卡因一水合物；N-二乙基氨基乙酰基-2,6-二甲基苯胺盐酸盐
• 英文名称: 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide
• 英文别名: lidocaine hydrochloride monohydrate；2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide;hydrate;hydrochloride
• CAS: 6108-05-0
• 化学式: C₁₄H₂₂N₂O*ClH*H₂O
• 分子量: 288.818
• InChiKey: YECIFGHRMFEPJK-UHFFFAOYSA-N

物化性质

• 熔点：
  75-79℃
• 溶解度：
  可溶于水中
• LogP：
  2.359 (est)

计算性质

• 辛醇/水分配系数(LogP)：
  -2.65
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  34.5
• 氢给体数：
  3
• 氢受体数：
  3

安全信息

• TSCA：
  Yes
• 危险等级：
  6.1
• 危险品标志：
  Xn
• 安全说明：
  S36
• 危险类别码：
  R22
• WGK Germany：
  3
• 海关编码：
  2924299090
• 危险品运输编号：
  UN 2811 6
• 储存条件：
  室温且干燥环境中保存。

SDS

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Section 1. Chemical Product and Company Identification
Lidocaine Hydrochloride monohydrate
Common Name/
Trade Name
Lidocaine Hydrochloride monohydrate

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Section 4. First Aid Measures
Eye Contact Check for and remove any contact lenses. In case of contact, immediately flush eyes with plenty of water for
at least 15 minutes. Cold water may be used. Get medical attention if irritation occurs.
Skin Contact Wash with soap and water. Cover the irritated skin with an emollient. Get medical attention if irritation
develops. Cold water may be used.
Serious Skin Contact Not available.
Inhalation If inhaled, remove to fresh air. If not breathing, give artificial respiration. If breathing is difficult, give oxygen.
Get medical attention.
Serious Inhalation Not available.
Ingestion Do NOT induce vomiting unless directed to do so by medical personnel. Never give anything by mouth to an
unconscious person. If large quantities of this material are swallowed, call a physician immediately. Loosen
tight clothing such as a collar, tie, belt or waistband.
Serious Ingestion Not available.

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Section 5. Fire and Explosion Data
Flammability of the Product May be combustible at high temperature.
Auto-Ignition Temperature Not available.
Flash Points Not available.
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...), halogenated compounds.
Fire Hazards in Presence of Slightly flammable to flammable in presence of heat.
Various Substances
Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available.
of Various Substances Risks of explosion of the product in presence of static discharge: Not available.
Fire Fighting Media SMALL FIRE: Use DRY chemical powder.
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
Special Remarks on As with most organic solids, fire is possible at elevated temperatures
Fire Hazards
Special Remarks on Explosion Fine dust dispersed in air in sufficient concentrations, and in the presence of an ignition source is a potential
Hazards dust explosion hazard.

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Section 6. Accidental Release Measures
Small Spill Use appropriate tools to put the spilled solid in a convenient waste disposal container. Finish cleaning by
spreading water on the contaminated surface and dispose of according to local and regional authority
requirements.
Large Spill Use a shovel to put the material into a convenient waste disposal container. Finish cleaning by spreading
water on the contaminated surface and allow to evacuate through the sanitary system.

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Section 7. Handling and Storage
Keep away from heat. Keep away from sources of ignition. Ground all equipment containing material. Do not
Precautions
ingest. Do not breathe dust. Wear suitable protective clothing. If ingested, seek medical advice immediately
and show the container or the label. Keep away from incompatibles such as oxidizing agents.
Storage Keep container tightly closed. Keep container in a cool, well-ventilated area.
Lidocaine Hydrochloride monohydrate

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Section 8. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below
recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep
exposure to airborne contaminants below the exposure limit.
Personal Protection Safety glasses. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent.
Gloves.
Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be
a Large Spill used to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a
specialist BEFORE handling this product.
Exposure Limits Not available.

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Section 9. Physical and Chemical Properties
Physical state and appearance Solid. (crystalline powder.) Odor Odorless.
Taste Not available.
Molecular Weight 288.81 g/mole
Color White.
pH (1% soln/water) Not available.
Not available.
Boiling Point
Melting Point 74°C (165.2°F)
Critical Temperature Not available.
Specific Gravity Not available.
Vapor Pressure Not applicable.
Vapor Density Not available.
Volatility Not available.
Not available.
Odor Threshold
Water/Oil Dist. Coeff. Not available.
Ionicity (in Water) Not available.
Dispersion Properties See solubility in water.
Solubility Easily soluble in cold water.
Insoluble in diethyl ether.
Soluble in benzene, ethanol, chloroform

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Section 10. Stability and Reactivity Data
The product is stable.
Stability
Instability Temperature Not available.
Excess heat, incompatible materials
Conditions of Instability
Incompatibility with various Reactive with oxidizing agents.
substances
Corrosivity Non-corrosive in presence of glass.
Special Remarks on Not available.
Reactivity
Special Remarks on Not available.
Corrosivity
Polymerization Will not occur.
Lidocaine Hydrochloride monohydrate

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Section 11. Toxicological Information
Routes of Entry Absorbed through skin. Inhalation. Ingestion.
Toxicity to Animals Acute oral toxicity (LD50): 292 mg/kg [Mouse].
Chronic Effects on Humans Causes damage to the following organs: the nervous system.
May cause damage to the following organs: cardiovascular system, central nervous system (CNS).
Other Toxic Effects on Hazardous in case of ingestion.
Humans Slightly hazardous in case of skin contact (irritant), of inhalation.
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on
May cause adverse reproductive effects and birth defects (teratogenic) based on animal test data
Chronic Effects on Humans
Special Remarks on other Aute Potential Health Effects:
Toxic Effects on Humans Skin: May cause skin irritation and numbness (anesthetic effect). When applied to the skin, it produces an
anesthetic effect by blocking the signals at the nerve endings of the skin. when compounded with an ointment
and applied topically, It may be absorbed by the skin cause systemic effects similar to that of ingestion.
Eyes: May cause eye irritation and numbness.
Inhalation: Dust may cause respiratory tract irritation and numbness.
Ingestion: Harmful of swallowed. May cause abdominal discomfort, nausea, vomiting. May affect
behavior/central nervous system (convulsions/seizures, drowsiness, lightheadedness, dizziness, confusion,
disorientation, muscle twitching or trembling, somnolence, unusual excitement, unusual tiredness or
weakness, nervousness, restlessness), cardiovascular system (hypotension, change in heart rate with
possibe cardiac arrest). May also cause shortness of breath or trouble breathing, ringing or buzzing in the
ears, feeling hot, cold or numb, increased sweating, blurred or double vision.
Chronic Potential Health Effects:
Skin: May cause allergic skin reaction with rash, hives, swelling, or abnormal sensation at the site of
application.
Ingestion/Inhalation: It is rare, but it may cause allergic reaction with cough, difficulty swallowing or tongue
swelling, dizziness or fainting, hives or swelling of the eyelids, face or lips; itching or skin rash, stuffy nose,
chest tightness, shortness of breath, trouble breathing or wheezing.
Medical Conditions Aggravated by Exposure: Hypersensitivity to material; respiratory depression; existing
cardiac conditions; broken or inflammed skin, burns, or open wounds at the place of application. More can be
absorbed into the body quickly, which increases the chance of side effects; Liver disease (severe). The risk
of side effects may be increased because of the slower removal of lidocaine from the body.

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Section 12. Ecological Information
Ecotoxicity Not available.
BOD5 and COD Not available.
Possibly hazardous short term degradation products are not likely. However, long term degradation products
Products of Biodegradation
may arise.
Toxicity of the Products The products of degradation are more toxic.
of Biodegradation
Not available.
Special Remarks on the
Products of Biodegradation

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Section 13. Disposal Considerations
Waste must be disposed of in accordance with federal, state and local environmental
Waste Disposal
control regulations.
Lidocaine Hydrochloride monohydrate

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Section 14. Transport Information
DOT Classification Not a DOT controlled material (United States).
Not applicable.
Identification
Not applicable.
Special Provisions for
Transport
DOT (Pictograms)

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Section 15. Other Regulatory Information and Pictograms
No products were found. It is not listed on the TSCA inventory because it is a hydrate.
Federal and State
Regulations
California prop. 65: This product contains the following ingredients for which the State of California has
California
found to cause cancer which would require a warning under the statute: No products were found.
Proposition 65
Warnings
California prop. 65: This product contains the following ingredients for which the State of California has
found to cause birth defects which would require a warning under the statute: No products were found.
Other Regulations OSHA: Hazardous by definition of Hazard Communication Standard (29 CFR 1910.1200).
EINECS: This product is not on the European Inventory of Existing Commercial Chemical Substances.
Canada: Not listed on Canadian Domestic Substance List (DSL) or Canadian Non- Domestic Substance List
(NDSL).
China: Not listed on National Inventory.
Japan: Not listed on National Inventory (ENCS).
Korea: Not listed on National Inventory (KECI).
Philippines: Not listed on National Inventory (PICCS).
Australia: Not listed on AICS.
WHMIS (Canada) Not available under WHMIS (Canada).
Other Classifications
DSCL (EEC) R22- Harmful if swallowed. S36- Wear suitable protective clothing.
S46- If swallowed, seek medical advice
immediately and show this container or label.
Health Hazard
HMIS (U.S.A.) 2 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
2 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
Lidocaine Hydrochloride monohydrate
ADR (Europe)
(Pictograms)
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent.

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SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

理化性质

盐酸利多卡因是白色结晶，无臭味微苦而麻。它极易溶于水、乙醇和有机溶剂，但不溶于乙醚。其水溶液在酸碱条件下不会分解，并且经过反复高压灭菌后也很少变质。

作用与用途

盐酸利多卡因具有强穿透力、高弥散性以及快速起效的特点。它的麻醉效能是普鲁卡因的两倍，但毒性只有后者的一半。注射5分钟后即可产生麻醉效果，并且可持续1～1.5小时（比普鲁卡因长出约50%）。该药物可抑制中枢神经系统并缩短心室不应期，适用于控制室性心动过速、治疗室性早搏和室性心动过速及心室颤动等心律失常症状。对心脏疾病或强心苷引起的心律失常有效，但对室上性心动过速效果不佳。

适应证

盐酸利多卡因是一种中效酰胺类局麻药，主要用于局部麻醉和抗心律失常治疗：

• 浸润麻醉、硬膜外麻醉、表面麻醉（包括胸腔镜检查或腹腔手术时的黏膜麻醉）及神经传导阻滞。
• 治疗急性心肌梗死后的室性早搏和室性心动过速，以及洋地黄中毒、心脏外科手术、心导管引起的室性心律失常。对于室上性心律失常通常无效。

用法与用量

不同部位使用盐酸利多卡因的浓度有所不同：

• 表面麻醉：2%～5%
• 浸润麻醉：0.25%～0.5%
• 神经传导阻滞和硬膜外麻醉：2%，每个注射点，马、牛8～12毫升；羊3～4毫升
• 皮下注射：2%，极量，猪、羊80毫升；马、牛400毫升；犬25毫升；猫8.5毫升

治疗心律失常时，静脉注射的剂量为每公斤体重犬初剂量2～4毫克，随后以每分钟25～75微克的速度滴注。猫的初始剂量为250～500微克，接着以每分钟20微克的速度持续输注。

不良反应

盐酸利多卡因常见的不良反应发生率约为6.3%，大多数与用药量有关。常见症状包括嗜睡、头晕、眩晕、恶心、呕吐、倦怠、欣快感、精神错乱、肌肉抽搐、惊厥、视力模糊和意识不清等。大剂量使用时，可能会导致严重窦性心动过缓、心脏停搏及房室传导阻滞，并使心肌收缩力减弱，血压下降。高血药浓度还会引起心房传导阻滞、QRS波增宽和其他心律失常。

注意事项

• 对其他局麻药过敏者可能对盐酸利多卡因也过敏。
• 下列情况下应慎用：妊娠期、新生儿（尤其是早产儿）、肝血流量减少、肝肾功能不全、充血性心力衰竭、严重心肌损伤、低血容量和休克患者。
• 超量使用可能导致惊厥或心脏骤停；老年人需要根据需求和耐受程度调整剂量，70岁以上者剂量应减半。麻醉时要避免误入血管并防止局麻药中毒。
• 治疗心律失常时应注意监测血压及心电图，并准备好抢救设备；P-R间期延长或QRS波增宽、出现其他心律失常或原有症状加重需立即停药。

用途

盐酸利多卡因作为酰胺类局麻药，通过血液吸收后或静脉给药，对中枢神经系统有明显的兴奋和抑制双重作用。低血药浓度时表现为镇痛和嗜睡、提高痛阈；剂量加大则效果增强，亚中毒血药浓度下具有抗惊厥作用。

反应信息

• 作为反应物：
  描述：

  盐酸利多卡因 以 1,2-二氯乙烷 为溶剂， 生成 利多卡因
  参考文献：
  名称：

  DERMAL FILLER COMPOSITIONS

  摘要：

  本发明提供了一种高度注射性、持久的基于透明质酸的水凝胶填充剂组合物，其中在存在碳二亚胺偶联剂的情况下，采用二胺或多胺交联剂制成。

  公开号：

  US20160113855A1
• 作为产物：
  描述：

  2-(二乙基氨基)乙酰胺 、 2-氯-1,3-二甲苯 在 potassium carbonate 、 盐酸 、 水 作用下， 以 N,N-二甲基甲酰胺 、 乙酸乙酯 、 丙酮 为溶剂， 反应 2.0h， 以92.1%的产率得到盐酸利多卡因
  参考文献：
  名称：

  一种1¹/₅水盐酸利多卡因化合物

  摘要：

  本发明公开了一种1 1 / 5 水盐酸利多卡因化合物及制法，该化合物用粉末X射线衍射测定法测定，以2θ±0.2°衍射角表示在6.7°，13.5°，16.6°，20.2°，27.1°，34.0°处显示出特征衍射峰。本发明制备的1 1 / 5 水盐酸利多卡因化合物具有热稳定性好、纯度高、吸湿性弱的优点，而且工艺简单，收率高，重复性强，适合于工业化生产。

  公开号：

  CN110590590A

文献信息

• [EN] CROSS-LINKED PYRROLOBENZODIAZEPINE DIMER (PBD) DERIVATIVE AND ITS CONJUGATES<br/>[FR] DÉRIVÉ DE DIMÈRE DE PYRROLOBENZODIAZÉPINE RÉTICULÉ (PBD) ET SES CONJUGUÉS
  申请人：HANGZHOU DAC BIOTECH CO LTD

  公开号：WO2020006722A1

  公开（公告）日：2020-01-09

  A novel cross-linked cytotoxic agents, pyrrolobenzo-diazepine dimer (PBD) derivatives, and their conjugates to a cell-binding molecule, a method for preparation of the conjugates and the therapeutic use of the conjugates.

  一种新型的交联细胞毒剂，吡咯苯并二氮杂环二聚体（PBD）衍生物，以及它们与细胞结合分子的结合物，一种制备这些结合物的方法以及这些结合物的治疗用途。
• ANTI-TUMOR EFFECT POTENTIATOR
  申请人：Fukuoka Masayoshi

  公开号：US20120225838A1

  公开（公告）日：2012-09-06

  There is provided an agent for potentiating the effects of an anti-tumor agent. An anti-tumor effect potentiator containing, as an active ingredient, a uracil compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents a C 1-5 alkylene group and one of methylene groups constituting the alkylene group is optionally substituted with an oxygen atom; R 1 represents a hydrogen atom or a C 1-6 alkyl group; R 2 represents a hydrogen atom or a halogen atom; and R 3 represents a C 1-6 alkyl group, a C 2-6 alkenyl group, a C 3-6 cycloalkyl group, a (C 3-6 cycloalkyl) C 1-6 alkyl group, a halogeno-C 1-6 alkyl group or a saturated heterocyclic group.

  提供了一种用于增强抗肿瘤药物效果的药剂。 一种抗肿瘤效应增强剂，其包含以下式(I)所代表的尿嘧啶化合物或其药用可接受的盐作为活性成分： 其中X代表一个C1-5烷基基团，构成该烷基基团的亚甲基基团之一可以选择性地被氧原子取代； R1代表氢原子或一个C1-6烷基基团；R2代表氢原子或卤原子；R3代表一个C1-6烷基基团，一个C2-6烯基基团，一个C3-6环烷基基团，一个(C3-6环烷基)C1-6烷基基团，一个卤代C1-6烷基基团或一个饱和杂环基团。
• 2-OXO-2- (2-PHENYL-5,6,7,8-TETRAHYDRO-INDOLIZIN-3-YL) -ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ANTIFUNGAL AGENTS
  申请人：Payne Lloyd James

  公开号：US20110009390A1

  公开（公告）日：2011-01-13

  The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.

  该发明提供了式(I)的化合物，以及其在药学和农业上可接受的盐：其中：R1、R2、R3、R4、R5、R6、R7、R8、A1、L1和n如本文所定义。这些化合物及其药学上可接受的盐在制造用于预防或治疗真菌病的药物方面是有用的。式(I)的化合物及其在农业上可接受的盐也可用作农业杀菌剂。
• Pyridopyrimidinones derivatives as telomerase inhibitors
  申请人：Pharmacia Italia S.p.A.

  公开号：US20040009993A1

  公开（公告）日：2004-01-15

  The invention provides novel pyrido[2,3-d]pyrimidin-7(8H)-ones derivatives active as telomerase inhibitors, the use of the derivatives as therapeutic agents, such as antitumoral agents, processes for preparation of the derivatives, and to pharmaceutical compositions comprising the derivatives.

  这项发明提供了作为端粒酶抑制剂活性的新型吡啶并[2,3-d]嘧啶-7(8H)-酮衍生物，以及这些衍生物作为治疗剂（如抗肿瘤剂）的用途，制备这些衍生物的方法，以及包含这些衍生物的药物组合物。
• [EN] TUNICAMYCIN ANALOGUES<br/>[FR] ANALOGUES DE TUNICIAMYCINE
  申请人：UNIV OXFORD INNOVATION LTD

  公开号：WO2018224822A1

  公开（公告）日：2018-12-13

  The invention relates to tunicamycin analogues which are compounds according to Formula (I), or pharmaceutically acceptable salts thereof, (I) Wherein [Base] and R1 to R9 are as defined herein. The tunicamycin analogues are useful in the prevention or treatment of bacterial infection, in particular of tuberculosis.

  该发明涉及类似于噻唑霉素的化合物，其为符合以下式（I）的化合物或其药学上可接受的盐，（I）其中[Base]和R1至R9如本文所定义。这些噻唑霉素类似物在预防或治疗细菌感染方面具有用处，特别是结核病。