顺苯磺酸阿曲库铵安全数据表
SAFETY DATA SHEET
SECTION 1: Identification of the substance/mixture and of the company/undertaking
1.1. Product identifier
NIMBEX
Trade name or designation
of the mixture
-
Registration number
Synonyms NIMBEX FORTE * NIMBEX INJECTION 2 MG/ML * NIMBEX INJECTION 5 MG/ML * NIMBEX
INJECTION 10 MG/ML * NIMBIUM INJECTION * CIS-ATRACURIUM BESYLATE, FORMULATED
PRODUCT
Issue date28-November-2013
Version number09
Revision date28-November-2013
Supersedes date07-June-2013
1.2. Relevant identified uses of the substance or mixture and uses advised against
Identified uses Medicinal Product
This safety data sheet is written to provide health, safety and environmental information for people
handling this formulated product in the workplace. It is not intended to provide information relevant
to medicinal use of the product. In this instance patients should consult prescribing
information/package insert/product label or consult their pharmacist or physician. For health and
safety information for individual ingredients used during manufacturing, refer to the appropriate
safety data sheet for each ingredient.
Uses advised against No other uses are advised.
1.3. Details of the supplier of the safety data sheet
GlaxoSmithKline UK
980 Great West Road
Brentford, Middlesex TW8 9GS UK
UK General Information (normal business hours): +44-20-8047-5000
Email Address: msds@https://www.wendangku.net/doc/ee10015376.html,
Website: https://www.wendangku.net/doc/ee10015376.html,
1.4. Emergency telephone
number
TRANSPORT EMERGENCIES::
UK In-country toll call: +(44)-870-8200418
International toll call: +1 703 527 3887
available 24 hrs/7 days; multi-language response
SECTION 2: Hazards identification
2.1. Classification of the substance or mixture
The mixture has been assessed and/or tested for its physical, health and environmental hazards and the following classification applies.
Classification according to Directive 67/548/EEC or 1999/45/EC as amended
Exempt from requirements - product regulated as a medicinal product, cosmetic product or medical device.
Classification according to Regulation (EC) No 1272/2008 as amended
Exempt from requirements - product regulated as a medicinal product, cosmetic product or medical device.
2.2. Label elements
Label according to Regulation (EC) No. 1272/2008 as amended
Exempt from requirements - product regulated as a medicinal product, cosmetic product or medical device.
Supplemental label information Not applicable.
2.3. Other hazards Caution - Pharmaceutical agent.
SECTION 3: Composition/information on ingredients
3.2. Mixtures
Notes
INDEX No.
REACH Registration No.
CAS-No. / EC No.%Chemical name
General information
Classification:
DSD:Xn;R22, R52Acute Tox. 4;H302
CLP:
-
-96946-42-8
-
CIS-ATRACURIUM BESYLATE
0.2< 1.05
90 - 100CLP: Regulation No. 1272/2008.DSD: Directive 67/548/EEC.M: M-factor
vPvB: very persistent and very bioaccumulative substance.PBT: persistent, bioaccumulative and toxic substance.
#: This substance has been assigned Community workplace exposure limit(s).Other components below reportable levels Composition comments
The full text for all R- and H-phrases is displayed in section 16.
SECTION 4: First aid measures
General information
Pre-placement and periodic health surveillance is not usually indicated. The final determination of the need for health surveillance should be determined by local risk assessment. Ensure that medical personnel are aware of the material(s) involved, and take precautions to protect
themselves. In the case of accident or if you feel unwell, seek medical advice immediately (show the label where possible).
4.1. Description of first aid measures
Inhalation Call a physician if symptoms develop or persist.
Skin contact Wash off with soap and water. Get medical attention if irritation develops and persists.Eye contact Rinse thoroughly with plenty of water for at least 15 minutes and consult a physician.
Ingestion
IF SWALLOWED: Call a POISON CENTRE or doctor/physician if you feel unwell. Do not induce vomiting without medical advice. Rinse mouth.
4.2. Most important symptoms and effects, both acute and delayed
Direct contact with eyes may cause temporary irritation. The following adverse effects have been noted with therapeutic use of this material: symptoms of hypersensitivity (such as skin rash, hives,itching, and difficulty breathing); changes in heart rate or pulse; changes in blood pressure.4.3. Indication of any
immediate medical attention and special treatment needed
No specific antidotes are recommended. Provide general supportive measures and treat
symptomatically. In case of shortness of breath, give oxygen. Keep victim warm. Keep victim under observation. Symptoms may be delayed.
SECTION 5: Firefighting measures
General fire hazards This product is non-flammable.
5.1. Extinguishing media
Suitable extinguishing media
Water fog. Foam. Dry chemical powder. Carbon dioxide (CO2).Unsuitable extinguishing media
None known.
5.2. Special hazards arising from the substance or mixture During fire, gases hazardous to health may be formed.
5.3. Advice for firefighters
Special protective
equipment for firefighters
Self-contained breathing apparatus and full protective clothing must be worn in case of fire.Special fire fighting procedures
Move containers from fire area if you can do so without risk.
SECTION 6: Accidental release measures
6.1. Personal precautions, protective equipment and emergency procedures
For non-emergency personnel
Keep unnecessary personnel away. Keep people away from and upwind of spill/leak. Wear
appropriate personal protective equipment. Ensure adequate ventilation. Local authorities should be advised if significant spillages cannot be contained. For personal protection, see section 8.
For emergency responders Keep unnecessary personnel away. Use personal protection recommended in Section 8 of the MSDS.
6.2. Environmental precautions
Prevent further leakage or spillage if safe to do so. Avoid discharge into drains, water courses or onto the ground.
6.3. Methods and material for containment and cleaning up Large Spills: Stop the flow of material, if this is without risk. Dike the spilled material, where this is possible. Cover with plastic sheet to prevent spreading. Absorb in vermiculite, dry sand or earth and place into containers. Prevent product from entering drains. Following product recovery, flush area with water.
Small Spills: Wipe up with absorbent material (e.g. cloth, fleece). Clean surface thoroughly to remove residual contamination.
Never return spills in original containers for re-use.
6.4. Reference to other
sections
For personal protection, see section 8. For waste disposal, see section 13. SECTION 7: Handling and storage
7.1. Precautions for safe handling Provide adequate ventilation. Wear appropriate personal protective equipment. Observe good industrial hygiene practices. Avoid release to the environment. Do not empty into drains.
7.2. Conditions for safe storage, including any incompatibilities Store in original tightly closed container. Store in a cool, dry place out of direct sunlight. Store away from incompatible materials (see Section 10 of the MSDS).
7.3. Specific end use(s)Medicinal Product
SECTION 8: Exposure controls/personal protection
8.1. Control parameters
Occupational exposure limits
GSK
Value Components Type
15 MIN STEL100 mcg/m3
CIS-ATRACU R IUM
BESYLATE (CAS
96946-42-8)
OHC2 Biological limit values No biological exposure limits noted for the ingredient(s). Recommended monitoring
procedures
Follow standard monitoring procedures.
Derived No Effect Level (DNEL)Not available.
Predicted no effect
concentrations (PNECs)
Not available.
8.2. Exposure controls
Appropriate engineering controls An Exposure Control Approach (ECA) is established for operations involving this material based upon the OEL/Occupational Hazard Category and the outcome of a site- or operation-specific risk assessment. Good general ventilation (typically 10 air changes per hour) should be used. Ventilation rates should be matched to conditions. If applicable, use process enclosures, local exhaust ventilation, or other engineering controls to maintain airborne levels below recommended exposure limits. If exposure limits have not been established, maintain airborne levels to an acceptable level.
Individual protection measures, such as personal protective equipment
General information Follow all local regulations if personal protective equipment (PPE) is used in the workplace.
Personal protection equipment should be chosen according to the CEN standards and in
discussion with the supplier of the personal protective equipment.
Eye/face protection Not normally needed. If contact is likely, safety glasses with side shields are recommended. (eg.
EN 166)
Skin protection
- Hand protection The choice of an appropriate glove does not only depend on its material but also on other quality
features and is different from one producer to the other. Glove selection must take into account
any solvents and other hazards present. With respect to the above precautions select suitable
chemical resistant protective gloves (EN 374) with a protective index 6 (>480min permeation time).
- Other Not normally needed.
Respiratory protection No personal respiratory protective equipment normally required. Where breathable aerosols/dust
are formed, use suitable combination filter for gases/vapours of organic, inorganic, acid inorganic,
alkaline compounds and toxic particles (eg. EN 14387).
Thermal hazards Wear appropriate thermal protective clothing, when necessary.
Hygiene measures An occupational/industrial hygiene monitoring method has been developed for this material. For
advice on suitable monitoring methods, seek guidance from a qualified environment, health and
safety professional. Always observe good personal hygiene measures, such as washing after
handling the material and before eating, drinking, and/or smoking. Routinely wash work clothing
and protective equipment to remove contaminants.
Environmental exposure controls
Hazard guidance and
Not available.
control recommendations
SECTION 9: Physical and chemical properties
9.1. Information on basic physical and chemical properties
Appearance
Physical state Liquid.
Form Liquid.
Colour Not available.
Odour Not available.
Odour threshold Not available.
pH 3.3 - 3.8
Melting point/freezing point Not available.
Not available.
Initial boiling point and boiling
range
Flash point Not available.
Evaporation rate Not available.
Flammability (solid, gas)Not available.
Upper/lower flammability or explosive limits
Not available.
Flammability limit - lower
(%)
Not available.
Flammability limit - upper
(%)
Vapour pressure Not available.
Vapour density Not available.
Relative density Not available.
Solubility(ies)Not available.
Not available.
Partition coefficient
(n-octanol/water)
Auto-ignition temperature Not available.
Decomposition temperature Not available.
Viscosity Not available.
Explosive properties Not available.
Oxidizing properties Not available.
9.2. Other information No relevant additional information available.
SECTION 10: Stability and reactivity
10.1. Reactivity The product is stable and non-reactive under normal conditions of use, storage and transport.
10.2. Chemical stability Material is stable under normal conditions.
10.3. Possibility of hazardous
No dangerous reaction known under conditions of normal use.
reactions
10.4. Conditions to avoid Contact with incompatible materials.
10.5. Incompatible materials Strong oxidising agents.
10.6. Hazardous
Irritating and/or toxic fumes and gases may be emitted upon the products decomposition. decomposition products
SECTION 11: Toxicological information
General information Caution - Pharmaceutical agent.
Information on likely routes of exposure
Ingestion May be harmful if swallowed.
Inhalation Not established.
Skin contact Not established. May be irritating to the skin.
Eye contact Direct contact with eyes may cause temporary irritation.
Symptoms
Direct contact with eyes may cause temporary irritation. The following adverse effects have been noted with therapeutic use of this material: symptoms of hypersensitivity (such as skin rash, hives,itching, and difficulty breathing); changes in heart rate or pulse; changes in blood pressure.
11.1. Information on toxicological effects
Acute toxicity
May be harmful if swallowed.CIS-ATRACURIUM BESYLATE Read across, Data for atracurium besylate Result: Harmful if swallowed
Test results
Components
Species
CIS-ATRACURIUM BESYLATE (CAS 96946-42-8)
NOAEL Rat Other Acute 2 mg/kg, subcutaneous injection
LOEL Rabbit Other Subacute 2.5 mg/kg/day, subcutaneous injection,d6-10 of pregnancy
NOAEL
Dog 2 mg/kg, 3 weeks, subcutaneous injection,twice/week
Monkey
3.75 mg/kg, 3 weeks, subcutaneous injection, twice/week
* Estimates for product may be based on additional component data not shown.Skin corrosion/irritation
Prolonged skin contact may cause temporary irritation.
Corrosivity
CIS-ATRACURIUM BESYLATE
SAR / QSAR, Data for cis-atracurium besylate
Result: Negative; not considered a significant irritant Species: Rabbit
Serious eye damage/eye irritation
Direct contact with eyes may cause temporary irritation.
Eye
CIS-ATRACURIUM BESYLATE
Data from cis-atracurium besylate
Respiratory sensitisation Not established.Skin sensitisation Not established.
Germ cell mutagenicity No data available to indicate product or any components present at greater than 0.1% are mutagenic or genotoxic.
Germ cell mutagenicity
Mutagenicity
CIS-ATRACURIUM BESYLATE
Ames
Result: negative
Chromosomal aberration assay Result: negative
L5178Y mouse lymphoma thymidine kinase locus assay Result: positive
in vivo cytogenetics assay Result: negative Species: Rat
Carcinogenicity Not classifiable as to carcinogenicity to humans.Reproductive toxicity Knowledge about health hazard is incomplete.
Reproductive toxicity
Reproductivity
CIS-ATRACURIUM BESYLATE
5 mg/kg/day Embryofetal Development Result: Maternal toxicity; Foetal NOAEL Species: Rabbit
Specific target organ toxicity -single exposure
Nervous system.Specific target organ toxicity -repeated exposure None known.
Aspiration hazard Due to partial or complete lack of data the classification is not possible.Mixture versus substance information Not available.Other information
Not available.
SECTION 12: Ecological information
12.1. Toxicity
Components Test results
Species
CIS-ATRACURIUM BESYLATE (CAS 96946-42-8)
Aquatic
Acute
IC50 Activated Sludge Respiration
> 4000 mg/l, 3 hours, Nominal, OECD
209
Residential sludge
NOEC320 mg/l
Residential sludge
EC50
Crustacea14 mg/l, 48 hours, Nominal, OECD 202
Water flea (Daphnia magna)
NOEC 5.6 mg/l
Water flea (Daphnia magna)
MIC
Microtox300 mg/l
Azotobacter chroococcum
> 1000 mg/l
Chaetomium globosum
> 1000 mg/l
Pseudomonas fluorescens
MIC
Other> 1000 mg/l
Anabaena flos-aquae
> 1000 mg/l
Aspergillus clavatus
> 1000 mg/l
Bacillus megaterium
* Estimates for product may be based on additional component data not shown.> 1000 mg/l
Penicillium canescens
12.2. Persistence and
degradability
No data is available on the degradability of this product.
Persistence and degradability
Photolysis
Half-life (Photolysis-aqueous)
CIS-ATRACURIUM BESYLATE 2.45 Days Measured, pH 5 Buffer Solution
UV/visible spectrum wavelength
CIS-ATRACURIUM BESYLATE280 nm
Hydrolysis
Half-life (Hydrolysis-acidic)
CIS-ATRACURIUM BESYLATE19 Days Measured
Half-life (Hydrolysis-basic)
CIS-ATRACURIUM BESYLATE< 4 Minutes Measured
Half-life (Hydrolysis-neutral)
CIS-ATRACURIUM BESYLATE 6.4 Hours Measured
Biodegradability
Percent degradation (Aerobic biodegradation-ready)
CIS-ATRACURIUM BESYLATE82.26 %, 28 days Modified Sturm test.
12.3. Bioaccumulative potential No data available.
Partition coefficient
n-octanol/water (log Kow)
CIS-ATRACURIUM BESYLATE-2.3
12.4. Mobility in soil No data available.
12.5. Results of PBT
and vPvB
assessment
Not available.
12.6. Other adverse effects Not available.
SECTION 13: Disposal considerations
13.1. Waste treatment methods
Residual waste Dispose of in accordance with local regulations. Empty containers or liners may retain some
product residues. This material and its container must be disposed of in a safe manner (see:
Disposal instructions).
Contaminated packaging Empty containers should be taken to an approved waste handling site for recycling or disposal.
Since emptied containers may retain product residue, follow label warnings even after container is
emptied.
EU waste code The Waste code should be assigned in discussion between the user, the producer and the waste
disposal company.
Disposal methods/information
Collect and reclaim or dispose in sealed containers at licensed waste disposal site. This material and its container must be disposed of as hazardous waste. Do not allow this material to drain into sewers/water supplies. Do not contaminate ponds, waterways or ditches with chemical or used container. Dispose of contents/container in accordance with local/regional/national/international regulations.
SECTION 14: Transport information
ADR
Not regulated as dangerous goods.
IATA
Not regulated as dangerous goods.
Read safety instructions, SDS and emergency procedures before handling. IMDG
Not regulated as dangerous goods.
MARPOL Annex II applies to liquids used in a ship's operation that pose a threat to the marine environment. These materials may not be transported in bulk. 14.7. Transport in bulk
according to Annex II of
MARPOL73/78 and the IBC Code
SECTION 15: Regulatory information
15.1. Safety, health and environmental regulations/legislation specific for the substance or mixture EU regulations
Regulation (EC) No. 1005/2009 on substances that deplete the ozone layer, Annex I
Not listed.
Regulation (EC) No. 1005/2009 on substances that deplete the ozone layer, Annex II
Not listed.
Regulation (EC) No. 850/2004 On persistent organic pollutants, Annex I as amended
Not listed.
Regulation (EC) No. 689/2008 concerning the export and import of dangerous chemicals, Annex I, part 1 as amended
Not listed.
Regulation (EC) No. 689/2008 concerning the export and import of dangerous chemicals, Annex I, part 2 as amended
Not listed.
Regulation (EC) No. 689/2008 concerning the export and import of dangerous chemicals, Annex I, part 3 as amended
Not listed.
Regulation (EC) No. 689/2008 concerning the export and import of dangerous chemicals, Annex V as amended
Not listed.
Regulation (EC) No. 166/2006 Annex II Pollutant Release and Transfer Registry
Not listed.
Regulation (EC) No. 1907/2006, REACH Article 59(1) Candidate List as currently published by ECHA
Not listed.Authorisations
Regulation (EC) No. 1907/2006, REACH Annex XIV Substances subject to authorization, as amended
Not listed.Restrictions on use
Regulation (EC) No. 1907/2006, REACH Annex XVII Substances subject to restriction on marketing and use as amended
Not listed.
Directive 2004/37/EC: on the protection of workers from the risks related to exposure to carcinogens and mutagens at work
Not listed.
Directive 92/85/EEC: on the safety and health of pregnant workers and workers who have recently given birth or are breastfeeding
Not listed.Other EU regulations
Directive 96/82/EC (Seveso II) on the control of major-accident hazards involving dangerous substances
Not listed.
Directive 98/24/EC on the protection of the health and safety of workers from the risks related to chemical agents at work
Not listed.
Directive 94/33/EC on the protection of young people at work
Not listed.Other regulations The product is classified and labelled in accordance with EC directives or respective national laws.This Safety Data Sheet complies with the requirements of Regulation (EC) No 1907/2006.National regulations
Follow national regulation for work with chemical agents.
15.2. Chemical safety
assessment
No Chemical Safety Assessment has been carried out. SECTION 16: Other information
List of abbreviations Not available.
References GSK Hazard Determination
Information on evaluation method leading to the classification of mixture The classification for health and environmental hazards is derived by a combination of calculation methods and test data, if available.
R22 Harmful if swallowed.
Full text of any statements or
R-phrases and H-statements
under Sections 2 to 15
R52 Harmful to aquatic organisms.
R52/53 Harmful to aquatic organisms, may cause long-term adverse effects in the aquatic
environment.
H302 Harmful if swallowed.
Revision information SECTION 5: Firefighting measures: Unsuitable extinguishing media
Regulatory Information: United States
Training information Follow training instructions when handling this material.
Disclaimer The information and recommendations in this safety data sheet are, to the best of our knowledge,
accurate as of the date of issue. Nothing herein shall be deemed to create any warranty, express
or implied. It is the responsibility of the user to determine the applicability of this information and
the suitability of the material or product for any particular purpose.
顺式阿曲库铵说明书
【药品名称】注射用顺苯磺酸阿曲库铵 【英文名】Cisatracurium Besylate for injection 【汉语拼音】Zhusheyong Shunbenhuangsuan Aquku'an 【主要成分】本品的主要成份为顺苯磺酸阿曲库铵，其化学名为: (1R，1'R，2R，2'R)—2，2'—(3，11—二氧代—4，10—二氧十三烷撑)二(1，2，3，4-四氢—6，7-二甲氧—2—甲基—1—藜芦基异喹啉)二苯磺酸盐 【化学结构式】 【分子式】CHN0S26582182【分子量】1243．49 【性状】本品为类白色至微黄色冻干块状物或粉末。 【药理毒理】药理作用 顺苯磺酸阿曲库铵是一神经肌肉阻滞剂。 顺苯磺酸阿曲库铵是中效的、非去极化的、具异喹啉鎓苄酯结构的骨骼肌松弛剂。 人体临床研究表明，本品与剂量依赖的组胺释放无关，甚至在剂量高达ED的8倍时95亦是如此。顺苯磺酸阿曲库铵在运动终板上与胆碱能受体结合，以拮抗乙酰胆碱的作用，从而产生竞争性的神经肌肉传导阻滞作用。这种作用很容易被抗胆碱酶药物如新斯的明或腾喜龙拮抗。． 当以阿片类药物麻醉时(硫喷妥钠／芬太尼／咪达唑仑)，顺阿曲库铵的ED(刺激尺神95经引起的拇内收肌颤搐反应受到95%抑制所需的药量)大约为／kg体重。 以氟烷麻醉时，儿童顺阿曲库铵的ED为／kg体重。95毒理作用 急性毒性:阿曲库铵的有意义的急性毒性研究无法进行。毒性反应见‘药物过量'章节。 亚急性毒性:狗和猴为期三周的重复给药研究表明没有化合物特异性中毒征象。 致突变性:当顺阿曲库铵浓度达5000μg／板时，体外微生物致突变试验未表明有致突变作用。大鼠的体内细胞遗传试验中，皮下注射剂量为4mg／kg体重时，未观察到明显的染色体异常。当顺阿曲库铵的浓度为40μg／ml或更高时，小鼠的体外淋巴细胞致突变试验表明有致突变性。很少和／或短暂使用药物出现的个别致突变阳性结果，其临床相关性尚有疑问。 致癌性:致癌研究尚未进行。 局部耐受性:对家兔进行的一项动脉内研究结果表明，本品耐受性良好，且未观察到与药物有关的变化。 【药代动力学】顺阿曲库铵主要是通过在生理pH值及体温下发生的Hofmann清除(化学过程)而降解为劳丹素和单季铵盐丙烯酸盐代谢物，后者通过非特异性酶水解而形成单季铵盐乙醇代谢物。顺阿曲库铵的清除具有较强的器官依赖性。肝和肾为代谢物的主要清除途径。这些代谢物不具有神经肌肉传导阻滞作用。 成年患者的药代动力学在剂量范围内(即2-4倍的ED)的研究表明，顺阿曲库铵非房95室药代动力学与剂量无关。 群体药代动力学证实上述现象并将剂量延伸至／kg(ED的8倍)。健康成年手术患者95给予本品的药代动力学参数如下: 参数平均值范围 率清除121-161mL／稳态分布容积kg 22-29min清除半衰期 老年患者的药代动力学 未见老年和青年患者药代动力学具有临床意义的差别。其恢复情况亦无明显变化。 肝肾损害患者的药代动力学．
5种药市场调查情况
5.2.公司目前经营产品的市场规模、市场结构与划分 5.2.3中长链脂肪乳注射液 目前国内仅贝朗医疗（苏州）有限公司1家进口企业。全国共有9家制药厂生产中长链脂肪乳注射液。正在申请中长链脂肪乳注射液6类仿制药生产的企业有：四川科伦药业股份有限公司、黑龙江科伦制药有限公司。市场上主要国产竞争厂家包括：华瑞制药，广州百特侨光，侨光制药是国内最先生产中长链脂肪乳注射液的企业，结束了中/长链脂肪乳注射液完全依赖进口的局面，填补了国内空白。 2006年，全国100家三甲医院的脂肪乳输液销售额合计约达3.4亿元人民币，再加上其它医院的脂肪乳输液，估计全国脂肪乳输液总销售额大约有5亿~6亿元人民币。 由于脂肪乳大输液的单价较贵，平均每瓶脂肪乳大输液零售价在80元人民币左右，约为基础型大输液的几十倍，故而限制了它在普通百姓中的大量应用。随着我国国民收入的逐年增长，今后无论营养性脂肪乳输液或治疗性脂肪乳输液的临床用量将会越来越多。 5.2.4复方氨基酸注射液 国家局已批德国贝朗医疗有限公司进口的复方氨基酸注射液，费森尤斯卡比(奥地利)公司（分包装企业：华瑞制药）进口的两种规格复方氨基酸（15）双肽（2）注射液。 国产复方氨基酸注射液（18AA-Ⅱ）生产企业共7家，复方氨基酸（15）双肽（2）注射液生产企业仅四川科伦1家。 自2008年，广东利泰占据氨基酸输液市场份额第一位，其它主要生产厂家有四川科伦、华瑞制药、辰欣药业、山东齐都药业、北京费森尤斯卡比等，以上这些厂家瓜分了超过50%的氨基酸输液市场份额。 5.2.5罗库溴铵注射液 罗库溴铵近几年也保持了稳定的增长速度，目前市场规模超过1亿。欧加农的产品占据了最大的市场份额，华北制药和仙琚制药瓜分余下市场。2013年罗库溴铵市场份额情况：欧加农67%、华北制药20%、仙琚制药13%。 目前申请罗库溴铵注射液进口注册的企业有：费森尤斯卡比（中国）投资有限公司；申请罗库溴铵注射液6类仿制药生产的企业有：浙江华海药业股份有限公司、清远嘉博制药有限公司、峨眉山通惠制药有限公司、四环药业股份有限公司。未来竞争可能趋于激烈，格局可能类似于目前的维库溴铵。目前华北制药和仙琚制药的罗库溴铵的招标价格约为60 元/支（50mg），原研产品欧加农招标价格略高约为80元/支（5mg），单个患者用药费用约为维库溴铵的2.5倍，较顺阿曲库铵略低。 5.2.6顺苯磺酸阿曲库铵注射液 目前，肌松药物市场规模约10亿元，与手术量增速基本相当。阿曲库铵和顺阿曲库铵合计占据超过50%的市场，恒瑞医药是当仁不让的老大。目前，国内制剂上市有4家，分别是：葛兰素史克、浙江仙琚制药、江苏恒瑞医药和东英（江苏）药业，其中仙琚制药产品几无销售，恒瑞持续占据顺阿曲库铵一半以上市场。2013年顺阿曲库铵市场份额情况：恒瑞医药56%、GSK 10%、东英药业34%。 法默森公司正在申请苯磺顺阿曲库铵注射液进口注册；海南皇隆制药股份有限公司正在申请注射用苯磺顺阿曲库铵6类仿制药生产。
阿曲库铵Atracurium杂质
阿曲库铵Atracurium全套杂质列表信息 序号英文名称中文名称CAS 结构式 1 Cis-Atracurium Besylate 顺阿曲库铵苯磺酸 2 Atracurium Impurity C1 (trans-Monoacrylate) 阿曲库铵杂质C1 （反式单丙烯酸 酯） No. N/A 3 Atracurium Besilate Impurity C2 Iodide 阿曲库铵斯汀碘杂 质C2 碘 No. N/A 4 Atracurium Impurity H (Mixture of cis, trans(H1), cis, cis(H2), tans, trans Isomer) 阿曲库铵杂质H No. N/A 5 Atracurium Impurity I (Mixture of cis, trans(I1), cis, cis(I2), tans, trans Isomer) 阿曲库铵杂质I No. N/A 6 Atracurium Impurity K (Mixture of cis, trans, cis, cis(K1 & K2), tans, trans Isomer) 阿曲库铵杂质K No. N/A 7 Atracurium Impurity C (Mixture of Diastereomers) 阿曲库铵杂质C No. N/A 8 Atracurium Besylate Impurity D Iodide (Mixture of Diastereomers) 阿曲库铵地平碘杂 质D（非对映体混 合物） No. N/A 9 Atracurium Besilate Impurity C1 and C2 Iodide 阿曲库铵斯汀碘杂 质C1和C2 No. N/A 10 Atracurium Iodide (Mixture of Diastereomers) 阿曲库铵碘化物 （非对映体的混合 物） No. N/A
不同剂量顺式阿曲库铵对小儿肌松作用比较
不同剂量顺式阿曲库铵对小儿肌松作用比较 [摘要] 目的：比较不同剂量顺式阿曲库铵在小儿外科手术中的肌松作用，探讨其临床使用中最适剂量。方法：48位患儿随机分为3组，分别应用2倍ED95，3倍ED95和4倍ED95的顺式阿曲库铵进行随机对照研究，观察3组患儿肌松药起效时间、有效作用时间、插管条件、血流动力学等指标。结果：3组间注射顺式阿曲库铵前及注射1～5min 后心率、平均动脉压差异无统计学意义。高剂量组（3倍ED95和4倍ED95）顺式阿曲库铵起效时间、有效作用时间、体内作用时间均短于和久于2倍ED95剂量组，差异有统计学意义。3组间恢复指数差异无统计学意义。高剂量组能获得较好的插管条件，与低剂量组比较差异具有统计学意义。但3倍ED95和4倍ED95剂量组在起效时间、插管条件等方面差异无统计学意义。结论：小儿应用3倍ED95和4倍ED95顺式阿曲库铵有着更快速的神经肌松作用，且持续时间更长、血流动力学更稳定。3倍ED95为最合适的诱导剂量。 [关键词] 顺式阿曲库铵；剂量；神经肌肉阻滞；小儿 中图分类号：R614.2 文献标识码：A 文章编号：2095-5200（2014）03-011-03 [Abstract] Objective：To investigate the most proper dose
of cisatracurium by comparing the neuromuscular blockade of children under cisatracurium anesthesia. Method：The study was designed as a randomized controlled clinical trial including 48 children divided into 3 groups. The onset time，effective duration，intubating condition and hemodynamic change were observed. Result：There is no statistically significant difference between heart rate and mean average blood pressure of children of 3 groups before or 1-5 minutes after the injection of cisatracurium. Higher doses of cisatracurium （3×ED95 and 4×ED95）showed onset time and effective duration were statistically significant lower and longer than lower dose of cisatracurium （2×ED95）respectively. At the same time，higher dose of cisatracurium had a better intubating condition than lower dose of cisatracurium，statistically. But no statistically significant difference was observed on onset time，intubating condition and so on between 3×ED95 and 4×ED95 dose of cisatracurium. Conclusion：The usage of 3×ED95 and 4×ED95 dose of cisatracurium provide a more effective and rapidly neuromuscular blockade in children with longer duration and hemodynamic hemostasis. 3×ED95 dose of cisatracurium is recommended as the initial dose. [Key words] cisatracurium；doses；neuromuscular
不同剂量顺式阿曲库铵在小儿麻醉中的肌松作用
不同剂量顺式阿曲库铵在小儿麻醉中的肌松作用 发表时间：2017-03-13T14:23:15.580Z 来源：《医药前沿》2017年2月第6期作者：阳力李艳华莫永广 [导读] 小儿麻醉中使用0.15mg/kg剂量的顺式阿曲库铵进行麻醉，插管效果较好，安全可靠有效率高。 （桂林市中医医院麻醉科广西桂林 541002） 【摘要】目的：研究分析不同剂量顺式阿曲库铵在小儿麻醉中的肌松作用。方法：回顾性分析我院于2015年3月-2016年3月收治的80例ASA麻醉患儿的病历资料，随机的分为对照组和观察组，对照组中的40例小儿患者采取0.10mg/kg剂量的顺式阿曲库铵进行麻醉，观察组中的40例小儿患者采取0.15mg/kg剂量的顺式阿曲库铵进行麻醉，对比分析两组患者注射前和注射后的血流动力学变化情况。结果：（1）观察组患者插管条件评级过程，其优良率（90%）和对照组（70%）比较，明显较高，P<0.05，有统计学意义。（2）观察组患者麻醉体内作用时间和阻滞维持时间和对照组比较，明显较低，P<0.05，有统计学意义。两组患者肌肉恢复时间和舒张压和心率等进行比较， P>0.05，无显著差异。结论：小儿麻醉中使用0.15mg/kg剂量的顺式阿曲库铵进行麻醉，插管效果较好，安全可靠有效率高，值得临床推广应用。 【关键词】不同剂量；小儿麻醉；顺式阿曲库铵；肌松 【中图分类号】R726.1 【文献标识码】A 【文章编号】2095-1752（2017）06-0213-02 小儿外科手术治疗对小儿麻醉药物有着越来越高的要求，通过减少对小儿身体技能的影响，尽可能的提高小儿治疗的疗效。顺式阿曲库铵这种麻醉药，主要是阿曲库铵的同分异构体，也即是顺式旋光异构体的结构，对少儿心血管系统没有直接的影响，临床中有着最佳的肌松效果，同时也要要求有着合适的剂量[1]。关于如何做好小儿麻醉中顺式阿曲库铵剂量的选择，始终是医学高度重视的一个焦点[2]。我院通过对小儿麻醉患者采取不同剂量的顺式阿曲库铵进行麻醉，有一定的价值发现，现总结报告如下。 1.资料和方法 1.1 一般资料 我院于2015年3月-2016年3月收治的80例ASA麻醉患儿的病历资料，随机的分为对照组和观察组。对照组中的40例麻醉患儿23例男性，17例女性，年龄在2.7岁到7.8岁之间，平均年龄为（4.6±0.3）岁。观察组中的40例麻醉患儿22例男性，18例女性，年龄在2.5岁到7.9岁之间，平均年龄为（4.2±0.5）岁。对比分析两组患者的一般资料，P>0.05，无统计学意义。 1.2 方法 所有患儿手术之前，患者均禁水禁食，同时采取阿托品注射液0.01mg/kg、米达唑仑注射液0.10mg/kg、依托咪酯脂肪注射液 0.15mg/kg和芬太尼注射液0.003mg/kg进行静脉注射，对照组中的40例小儿患者采取0.10mg/kg剂量的顺式阿曲库铵进行麻醉，观察组中的40例小儿患者采取0.15mg/kg剂量的顺式阿曲库铵进行麻醉，对比分析两组患者注射前和注射后的血流动力学变化情况。所有患者均进行气管插管，结合麻醉机进行呼吸的控制和调整，同时设置呼吸参数。对比分析两组患者注射前和注射后的血流动力学变化情况。 1.3 统计学方法 应用统计学软件SPSS 18.0处理数据，用t检验剂量资料，计数资料用χ2检验，P<0.05，有统计学意义。 2.结果 2.1 两组患者的插管条件优良率 观察组患者插管条件评级过程，其优良率（90%）和对照组（70%）比较，明显较高，P<0.05，有统计学意义。见表1。 2.2 两组患者血流动力学变化情况 如表2所示，观察组患者麻醉体内作用时间和阻滞维持时间和对照组比较，明显较低，P<0.05，有统计学意义。两组患者肌肉恢复时间和舒张压和心率等进行比较，P>0.05，无显著差异。 3.讨论 顺式阿曲库胺和阿曲库铵有着类似的代谢途径，顺式阿曲库胺主要是结合Hofmann途径逐渐的降解，产生的代谢产物其神经肌肉没有传导阻滞的作用。阿曲库胺代谢产物主要是DN-甲四氢罂粟碱，伴有高浓度的血中水平，小儿常伴有惊厥表现[3]。小儿麻醉中顺式阿曲库胺的应用，往往减少对患儿心率和血压的影响，肌松效果相对较好。 我院通过对小儿麻醉患者采取0.10mg/k和0.15mg/k剂量的顺式阿曲库铵进行麻醉，研究结果表明，观察组患者插管条件评级过程，其优良率（90%）和对照组（70%）比较，明显较高，P<0.05，有统计学意义。观察组患者麻醉体内作用时间和阻滞维持时间和对照组比较，明显较低，P<0.05，有统计学意义。两组患者肌肉恢复时间和舒张压和心率等进行比较，P>0.05，无显著差异。因此，小儿麻醉中使
艾斯康(含答案版)
艾斯康麻醉考试试题 办事处：姓名：分数： 填空题（共60分，每空1分） 1、艾斯康的通用名为注射用顺苯磺酸阿曲库铵，为苄异喹啉类非去极化肌松药。 2、根据作用机制的不同，肌松药可分为：去极化肌松药和非去极化肌松药 3、顺阿曲库铵作为一种中效的非去极化肌松药，和乙酰胆碱共同竞争乙酰胆碱受体结合，故又称为竞争性肌松药。 4、顺阿曲库铵由于没有组胺释放，血流动力学稳定，因此，适用于心脏病人手术。顺阿曲库铵可安全有效用于体外循环冠脉搭桥手术。 5、除艾斯康外，市场上常用的非去极化肌松药有：阿曲库铵、维库溴铵、罗库溴铵、泮库溴铵、米库氯铵（列举三种即可）。 6、艾斯康的剂型是冻干粉针剂，规格是10mg/瓶。 7、艾斯康的保存很重要，光线和温度会改变艾斯康的活性，可能导致药效的降低 8、根据作用时间的长短，可将肌松药分为：短效、中效、长效肌松药。 9、顺阿曲库铵只在酸性溶液中稳定，所以不能与碱性溶液共用注射器或同时给药(如硫喷妥钠)。 10、顺阿曲库铵无剂量依赖性的组胺释放作用。 11、艾斯康在全麻手术应用的核心获益点有： 1）在达到良好肌松效果的同时无组胺释放； 2）在体内主要经Hofmann降解(78%)，13％以原型从肾脏排泄，8％
靠酯酶水解； 3）对肝肾等脏器功能的依赖性较小，肝肾功能损害患者无需调整剂量； 4）泵注可稳定血药浓度。 12、艾斯康在全麻手术中的用法： 1）全麻诱导期：诱导剂量为4-6倍ED95，一般为2 支艾斯康； 2）全麻维持期：在诱导过后可以通过两种方式给药，持续泵注：1-2μ g/kg/min （泵注速率），根据手术时长，采取不同的配泵方案；单次推 注：手术每30min 静脉推注一次，单次推注剂量为0.05mg/kg 。 13、月潜力量=月全麻量*4支（以2小时手术时间计算） 14、顺式阿曲库铵易被抗胆碱酯酶药所拮抗，如新斯的明、依酚氯铵，可安全应用于临床。 15、与成人相比，小儿应用顺阿曲库铵起效较和肌松恢复都较成人快。 16、采用部分非去极化肌松药时，可通过下列三种方法缩短插管时间： 1）加大肌松药用量； 2）“预注”技术； 3）限时法（提前给药）。 17、气管插管条件不仅与肌松药种类和剂量有关，还与麻醉深度有关。因此，加深麻醉深度以及给予小剂量短效麻醉性镇痛药均能改善插管条件。 18、影响肌松药起效时间的因素主要有： 1）药物剂量； 2）注射速度； 3）和病人的循环功能状况。
注射用顺苯磺酸阿曲库铵说明
核准日期： 2006年11月3日 注射用顺苯磺酸阿曲库铵说明书 请仔细阅读说明书并在医师指导下使用。 【药品名称】 通用名称：注射用顺苯磺酸阿曲库铵 英文名称：Cisatracurium Besilate for Injection 汉语拼音：Zhusheyong Shunbenhuangsuan Aquku’an 【成份】 本品的主要成份为顺苯磺酸阿曲库铵，其化学名称为：(1R，1’R，2R，2’R)-2，2’-(3，11-二氧代–4，10–二氧十三烷亚甲基)二(1，2，3，4-四氢-6，7-二甲氧–2-甲基–1-藜芦基异喹啉)二苯磺酸盐。 其结构式为： 分子式：C65H82N2O18S2 分子量： 其辅料为乳糖和枸橼酸。 【性状】 本品为白色疏松块状物或粉末。白色无定型粉末，有隐湿性，无臭。 【适应症】 本品用于手术和其他操作以及重症监护治疗。作为全麻的辅助用药或在重症监护病房(ICU)起镇静作用，它可以松弛骨骼肌，使气管插管和机械通气易于进行。 【规格】 10mg 【用法用量】 使用前用灭菌注射用水5ml溶解。与其它神经肌肉传导阻滞剂一样，建议在使用本品过程中监测神经肌肉功能以满足个体化剂量的要求。
静脉单次注射给药用法 成人剂量 气管插管：本品用于成人插管的推荐剂量为每公斤体重或遵医嘱。用丙泊酚诱导麻醉后，按此剂量给予本品，120秒后即可达到良好至极佳的插管条件。 高剂量可以缩短对神经肌肉阻滞作用的起效时间。 下表总结了阿片类(硫喷妥钠/芬太尼/咪唑安定)或丙泊酚麻醉的健康成年病人每公斤体重注射～本品后的平均药效学数据。 维持用药：采用维持剂量延长本品神经肌肉的阻滞作用。对以阿片类或丙泊酚麻醉的病人，给予公斤体重的本品可以继续产生大约20分钟临床有效的神经肌肉阻滞作用。 连续使用维持剂量不会导致神经肌肉阻滞作用延长。 自然恢复：神经肌肉阻滞一旦进行自然恢复，其恢复速度与本品给药量无关。当使用阿片类或丙泊酚进行麻醉时，从25％～75％及5%～95%恢复的平均时间分别约为13和30分钟。 拮抗：给予标准剂量抗胆碱药物可以很容易地拮抗本品的神经肌肉阻滞作用。T1平均达10％恢复时给予拮抗剂，从25％到75％恢复及到临床完全恢复(T4/T1≥的平均时间分别约为4分钟和9分钟。 2～12岁的儿童的给药剂量 2～12岁儿童的首剂顺苯磺酸阿曲库铵注射液的推荐给药剂量为公斤体重，并在5～10秒内进行。下表为阿片类麻醉时平均药效学数据。在相同的麻醉背景下，以公斤体重的剂量给药，儿童比成人起效时间快，临床作用时间短且自行恢复快。
最理想的肌肉松弛剂
商品名: 库泰 生产厂家: 江苏东英药业有限公司 包装: 10瓶/盒，30盒/箱 规格: 0.5mg 简介: 独特的作用机制，最理想的肌肉松弛剂，广泛的患者人群 独特的作用机制，最理想的肌肉松弛剂，广泛的患者人群 【商品名】库泰 【规格】5mg 【包装】10瓶/盒，30盒/箱 【有效期】1.5年 【生产厂家】江苏东英药业有限公司 【有效期】一年半 【简要处方说明书】 本品为中等起效、中等作用持续时间的肌肉松弛剂，用于住院和门诊病人全身麻醉的辅助用药，以便气管内插管、提供受伤期间的肌肉松弛或ICU病房中的人工呼吸机通气。 顺苯磺阿曲库铵只允许静脉内注射或滴注使用，使用前用注射用生理盐水将药物溶解。顺苯磺阿曲库铵的剂量必须个体化。临床上利用外周神经刺激的方法可以达到顺苯磺阿曲库铵的最佳应用、减少药物过量或剂量不足的可能性以及帮助评价病人恢复情况。下述剂量可作为给药剂量指导。 静脉推注给药：成人起始剂量：顺苯磺阿曲库铵作为丙泊酚/氧化亚氮/氧诱导插管的一个组分进行气管插管时，0.15mg/kg和0.20mg/kg给药剂量分布可以在2分钟或1.5分钟内获得良好或极好的插管条件。临床作用平均持续时间分布为55分钟和61分钟。 成人维持剂量：长时间手术过程中顺苯磺阿曲库铵维持肌肉松弛的推荐剂量为0.03mg/kg。每一维持剂量可维持20分钟。维持剂量应按照临床需求选择，一般应在起始剂量给药40～50分钟（0.12mg/kg）和50～60分钟（0.20mg/kg）后给药。 对本品过敏病人禁用。 注意事项： （1）本品只可静脉注射，肌肉注射可引起肌肉组织坏死。 （2）因可致肌张力增高，一次剂量不宜太大。 （3）用于危重病人抢救，保持轻度肌松，配合呼吸机治疗，但持续时间不宜超过1周 （4）患神经肌肉疾病、严重电解质紊乱病人慎用。 （5）本品须冷藏，以免发生Hoffman降解。
顺苯磺酸阿曲库铵安全数据表
SAFETY DATA SHEET SECTION 1: Identification of the substance/mixture and of the company/undertaking 1.1. Product identifier NIMBEX Trade name or designation of the mixture - Registration number Synonyms NIMBEX FORTE * NIMBEX INJECTION 2 MG/ML * NIMBEX INJECTION 5 MG/ML * NIMBEX INJECTION 10 MG/ML * NIMBIUM INJECTION * CIS-ATRACURIUM BESYLATE, FORMULATED PRODUCT Issue date28-November-2013 Version number09 Revision date28-November-2013 Supersedes date07-June-2013 1.2. Relevant identified uses of the substance or mixture and uses advised against Identified uses Medicinal Product This safety data sheet is written to provide health, safety and environmental information for people handling this formulated product in the workplace. It is not intended to provide information relevant to medicinal use of the product. In this instance patients should consult prescribing information/package insert/product label or consult their pharmacist or physician. For health and safety information for individual ingredients used during manufacturing, refer to the appropriate safety data sheet for each ingredient. Uses advised against No other uses are advised. 1.3. Details of the supplier of the safety data sheet GlaxoSmithKline UK 980 Great West Road Brentford, Middlesex TW8 9GS UK UK General Information (normal business hours): +44-20-8047-5000 Email Address: msds@https://www.wendangku.net/doc/ee10015376.html, Website: https://www.wendangku.net/doc/ee10015376.html, 1.4. Emergency telephone number TRANSPORT EMERGENCIES:: UK In-country toll call: +(44)-870-8200418 International toll call: +1 703 527 3887 available 24 hrs/7 days; multi-language response SECTION 2: Hazards identification 2.1. Classification of the substance or mixture The mixture has been assessed and/or tested for its physical, health and environmental hazards and the following classification applies. Classification according to Directive 67/548/EEC or 1999/45/EC as amended Exempt from requirements - product regulated as a medicinal product, cosmetic product or medical device. Classification according to Regulation (EC) No 1272/2008 as amended Exempt from requirements - product regulated as a medicinal product, cosmetic product or medical device. 2.2. Label elements Label according to Regulation (EC) No. 1272/2008 as amended Exempt from requirements - product regulated as a medicinal product, cosmetic product or medical device. Supplemental label information Not applicable. 2.3. Other hazards Caution - Pharmaceutical agent. SECTION 3: Composition/information on ingredients 3.2. Mixtures