5-[3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoyloxy]Pentyl 3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoate
Atracurium
CAS: 64228-79-1
Molecular Formula: C53H72N2O12
5-[3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoyloxy]Pentyl 3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoate - Names and Identifiers
| Name | Atracurium |
| Synonyms | Atracurium Cisatracurium ATRACURIUM BESYLATE Atracurium for peak identification CRS 5-[3-[1-[(3,4-DiMethoxyphenyl)Methyl]-6,7-diMethoxy-2-Methyl-3,4-dihydro-1H-isoquinolin-2-yl]propano 2,2'-{pentane-1,5-diylbis[oxy(3-oxopropane-3,1-diyl)]}bis[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolinium] 2,2'-[1,5-pentanediylbis[oxy(3-oxo-3,1-propanediyl)]]bis[1-[(3,4-dimethoxyphenyl)methyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-isoquinolinium 2,2'-[1,5-Pentanediylbis[oxy(3-oxo-3,1-propanediyl)]]bis[1-[(3,4-dimethoxyphenyl)methyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methylisoquinolinium] 2,2'-[Pentane-1,5-diylbis[oxy(3-oxo-3,1-propanediyl)]]bis[1-[(3,4-dimethoxyphenyl)methyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methylisoquinolin-2-ium] (1R,2R,1'R,2'R)-2,2'-{pentane-1,5-diylbis[oxy(3-oxopropane-3,1-diyl)]}bis[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolinium] 2,2'-{pentane-1,5-diylbis[oxy(3-oxopropane-3,1-diyl)]}bis[1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-2-methyl-1,2,3,4-tetrahydroisoquinolinium] bisbenzenesulfonate 5-[3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoyloxy]Pentyl 3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoate 5-[3-[1-[(3,4-Dimethoxyphenyl)methyl]-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-2-yl]propanoyloxy]pentyl 3-[1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-2-yl]propanoate |
| CAS | 64228-79-1 |
| EINECS | 264-743-4 |
| InChI | InChI=1/C53H72N2O12/c1-54(22-18-38-32-48(62-7)50(64-9)34-40(38)42(54)28-36-14-16-44(58-3)46(30-36)60-5)24-20-52(56)66-26-12-11-13-27-67-53(57)21-25-55(2)23-19-39-33-49(63-8)51(65-10)35-41(39)43(55)29-37-15-17-45(59-4)47(31-37)61-6/h14-17,30-35,42-43H,11-13,18-29H2,1-10H3/q+2/t42-,43-,54-,55-/m1/s1 |
5-[3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoyloxy]Pentyl 3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoate - Physico-chemical Properties
| Molecular Formula | C53H72N2O12 |
| Molar Mass | 929.14 |
| Melting Point | 185-194 ºC |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| Storage Condition | -20°C Freezer |
| Physical and Chemical Properties | Melting point 185-194°C |
5-[3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoyloxy]Pentyl 3-[1-[(3,4-Dimethoxyphenyl)Methyl]-6,7-Dimethoxy-2-Methyl-3,4-Dihydro-1H-Isoquinolin-2-Yl]Propanoate - Reference Information
| muscle relaxant | atracurium is a medium-aged non-depolarizing muscle relaxant, and its besylate is commonly used. It is mainly eliminated by non-enzymatic degradation, and can also be hydrolyzed to inactive metabolites by pseudo cholinesterase, and then excreted by kidney and bile. The effect was weaker than that of the Carine, but the effect was fast (1 minute), the duration was short (15 minutes), the repeated administration was not cumulative, the ganglion block was mild, and the heart rate was not affected. Clinical use for a variety of surgery requires muscle relaxation in order to control the breath of intravenous administration, the initial dose of 0.3 to 0.6mg/kg, and then can be intravenous drip per minute 5 to 10g/kg maintenance. |
| trait | its benzenesulfonate is a white to yellow-white powder with slight hygroscopicity. Soluble in water, soluble in ethanol, acetonitrile and dichloromethane. Containing cis-CIS, cis-trans, anti-trans three isomers. |
| pharmacological action | atracurium is a benzisoquinoline compound of the synthetic bis-quaternary ammonium ester type, it is a medium-aging canister, a kind of non-depolarizing muscle relaxant. It acts primarily through competitive binding to cholinergic receptors and can be reversed by anticholinesterase agents such as neostigmine. Rapid onset, muscle relaxant effect is good. Intravenous injection of 0.4~0.5mg/kg, in 1~2 minutes, 3~5 minutes to reach the peak, the effect of maintenance time is 15~30 minutes, repeated administration of no accumulation effect. Non-reactive metabolites can be degraded by Hofmann (I. E., by non-specific esterase degradation and base hydrolysis) at physiological temperatures and pH environments. The plasma protein binding rate is about 80%. Mainly in the form of metabolites excreted in urine and bile, elimination half-life of about 20 minutes. Small amount of penetration through the placenta. skeletal muscle relaxation for various surgical anesthesia, easy to control breathing, especially suitable for tracheal intubation, cesarean section to maintain muscle relaxation, but also sustainable infusion to maintain a long time neuromuscular blockade. It is suitable for patients with liver and kidney dysfunction, jaundice, pheochromocytoma surgery and outpatient surgery. |
| indications | is mainly used for bone relaxants during anesthesia in various surgical operations, which is easy to control breathing, it is especially suitable for the muscle relaxation required for tracheal intubation. Maintenance of muscle relaxation in caesarean section. |
| adverse reactions | high dose can cause blood pressure decrease, heart rate increase or bradycardia. Occasionally, it may cause urticaria and bronchospasm. |
| note | 1. This product allergy and myasthenia gravis patients disabled; Neuromuscular disease, severe electrolyte disorders, severe cardiovascular disease patients and pregnant women with caution. 2. This product can be stored for 24 hours after being diluted with sterilized physiological saline, and it should be used up within 8 hours after being diluted with glucose injection to avoid degradation. 3. Overdose (dose> 0.5mg/kg) can cause excessive histamine release, causing tachycardia. |
| drug interaction | 1. Avoid mixing this product with basic drugs such as thiopental sodium in the same syringe. 2. Enflurane, isoflurane, aminoglycoside and Polypeptide antibiotics can enhance the role of this product. Its muscle relaxant effect can be antagonized by cholinesterase inhibitors such as neostigmine. 3. No combination with succinylcholine. |
| atracurium benzenesulfonate | atracurium benzenesulfonate is a new non-polar muscle relaxant synthesized by chemical synthesis. Its mechanism of action is primarily through competition for cholinergic receptors, blocking acetylcholine transmission. This product can be reversed by neostigmine and other anticholinesterase drugs, and its muscle relaxant effect is 1/5~1/4 of vecuronium bromide. The metabolism of this product does not depend on the role of enzymes, also does not depend on the metabolism and excretion of liver and kidney, but in the plasma natural degradation inactivation. This product intravenous injection of 0.4~0.5mg/kg, in 1~2 minutes markedly, 3~5 minutes muscle relaxant effect reached the peak, the maintenance time of 15~30 minutes, repeated administration of no accumulation, plasma elimination half-life of about 20 minutes, liver and kidney function does not affect its elimination half-life. Enflurane, isoflurane and this product have synergistic effect in muscle relaxation. This product does not affect the heart rate and blood pressure, and mild histamine release. clinically, it is used as a skeletal muscle relaxant in anesthesia for various surgical operations, especially for patients with liver and kidney dysfunction, and also for muscle relaxation during tracheal intubation and maintenance of muscle relaxation during cesarean section. This information was edited by chemical book Xiaonan (2015-09-17). |
| cis-Atracurium | cis-atracurium is one of the 10 isomers of atracurium, accounting for about 15% of the total atracurium mixture. Like the parent, it is a non-depolarizing muscle relaxant. The ED95 of cisatracurium is 0.05 mg/kg, and the muscle relaxation titer is 3~5 times of Atracurium. Its lipid solubility is low, and it is not directly hydrolyzed by plasma nonspecific esterase, and 80% is inactivated by Hofmann degradation. No histamine release effect, low incidence of allergic reactions. Clinical data showed no sign of histamine release in healthy patients undergoing elective surgery by rapid intravenous injection of 8 × ED95 cis-Atracurium. However, the amount of atracurium 2 × ED95 has histamine releasing effect. The effect on cardiovascular function was light. The metabolites are few, and N-methyltetrahydropapaverine, a decomposition product of cis-Atracurium, is about 1/3 to 1/10 of the equivalent dose of atracurium, and long-term application will not cause convulsion due to excessive plasma concentration. Can be used for tracheal intubation and maintenance of muscle relaxation during general anesthesia, especially for patients with liver and renal insufficiency surgery anesthesia. |
Last Update：2024-04-09 19:05:07
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