Pancuronium dibromide   中文名称: 泮库溴铵

在鸡胚胎背根神经节神经元中检查泮库溴铵对跨膜钠电导的影响。当以 50 μM 至 1 mM 的浓度进行外部灌注时，泮库溴铵会快速且可逆地抑制电流。半有效剂量为 170 μM 时，抑制作用具有浓度依赖性，但不依赖于电压。通过与静息和开放状态下的钠通道相互作用，泮库溴铵可以降低钠电流[2]。

在体重 250-300 g 的雄性豚鼠中，静脉注射泮库溴铵 (0.5 mg/kg) 可逆转因迷走神经刺激和注射乙酰胆碱 (ACh) 引起的心动过缓。泮库溴铵 (0.04 mg/kg) 会放大迷走神经诱导的支气管收缩，导致 100% 神经肌肉阻滞[1]。大鼠尾骨和输精管表现出泮库溴铵介导的肾上腺素能神经刺激增强作用[3]。

Absorption, Distribution and Excretion
241 to 280 mL/kg
Plasma cl=1.1–1.9 mL/minute/kg
BOTH LIVER & KIDNEYS ARE INVOLVED IN DEGRADATION & EXCRETION OF ... PANCURONIUM ...
AFTER IV INJECTION, EFFECTS...BECOME MAXIMAL IN LESS THAN 3 MIN IN ADULTS & 90 SEC IN CHILDREN. ... PLASMA HALF-LIFE IS PROBABLY SLIGHTLY LESS THAN 2 HR. PANCURONIUM IS MOSTLY EXCRETED UNCHANGED INTO URINE.
PLACENTAL TRANSFER OF...PANCURONIUM BROMIDE...OCCURS RAPIDLY AFTER ADMIN TO MOTHERS, BUT FETAL:MATERNAL DRUG CONCN RATIO ARE VERY LOW.
PLASMA LEVELS OF PANCURONIUM OBEYED TWO-COMPARTMENT KINETICS IN SEVEN PATIENTS ON IV INJECTION & THE BETA-PHASE HALF-TIME VARIED BETWEEN 90 AND 162 MIN. THE MEAN VOLUME OF THE CENTRAL COMPARTMENT WAS 100 ML/KG, WHILE THE OVERALL DISTRIBUTION VOLUME WAS 261 MG/KG. IN PATIENTS WITH CHRONIC RENAL FAILURE, THE PLASMA CLEARANCE...WAS SIGNIFICANTLY REDUCED, WHILE VOLUMES OF BOTH THE OVERALL & CENTRAL COMPARTMENTS WERE SIGNIFICANTLY INCREASED.
For more Absorption, Distribution and Excretion (Complete) data for PANCURONIUM BROMIDE (6 total), please visit the HSDB record page.

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Metabolism / Metabolites
Hepatic.
IN CATS, 8 HR AFTER IV INJECTION OF PANCURONIUM BROMIDE, UNCHANGED PANCURONIUM BROMIDE IN URINE, BILE, & LIVER ACCOUNTED FOR 58% OF DOSE, 3-HYDROXY-DERIV FOR 14.5%, 17-HYDROXY-DERIV FOR 7% & 3,17-DIHYDROXY-DERIV FOR 4.5%.

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Biological Half-Life
1.5 to 2.7 hours.
PLASMA HALF-LIFE IS PROBABLY SLIGHTLY LESS THAN 2 HR.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
No information is available on the use of pancuronium during breastfeeding. Because it is highly polar and poorly absorbed orally, it is not likely to reach the breastmilk in high concentration or to reach the bloodstream of the infant. When a combination of anesthetic agents is used for a procedure, follow the recommendations for the most problematic medication used during the procedure.
◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

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Protein Binding
77 to 91%

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Interactions
FROM CLINICAL VIEWPOINT, MOST IMPORTANT PHARMACOLOGICAL INTERACTIONS OF THESE DRUGS ARE WITH CERTAIN GENERAL ANESTHETICS, CERTAIN ANTIBIOTICS, AND ANTI-CHOLINESTERASE COMPOUNDS. /NEUROMUSCULAR BLOCKING AGENTS/
...DIETHYL ETHERS, AS WELL AS PRIOR SUCCINYLCHOLINE, INTENSIFY & PROLONG ACTION /OF PANCURONIUM/.
ETHER EXERTS STABILIZING EFFECT ON POSTJUNCTIONAL MEMBRANE & THEREFORE, ACTS SYNERGISTICALLY WITH COMPETITIVE BLOCKING AGENTS. ... HALOTHANE, CYCLOPROPANE, FLUROXENE, METHOXYFLURANE, & ENFLURANE LIKEWISE ACT SYNERGISTICALLY WITH COMPETITIVE BLOCKING AGENTS, BUT TO LESSER EXTENT. /NEUROMUSCULAR COMPETITIVE BLOCKING AGENTS/
AMINOGLYCOSIDE ANTIBIOTICS PRODUCE NEUROMUSCULAR BLOCKADE BY INHIBITING ACETYLCHOLINE RELEASE FROM THE PREGANGLIONIC TERMINAL (THROUGH COMPETITION WITH CA(2+)) AND ... BY STABILIZING THE POSTJUNCTIONAL MEMBRANE. THE BLOCKADE IS ANTAGONIZED BY CALCIUM SALTS, BUT ONLY INCONSISTENTLY BY ANTICHOLINESTERASE AGENTS. THE TETRACYCLINE ANTIBIOTICS ALSO CAN PRODUCE NEUROMUSCULAR BLOCK, POSSIBLY BY CHELATION OF CALCIUM IONS. ADDITIONAL ANTIBIOTICS THAT HAVE NEUROMUSCULAR BLOCKING ACTION ... INCLUDE POLYMYXIN B, COLISTIN, CLINDAMYCIN, & LINCOMYCIN. /NEUROMUSCULAR BLOCKING AGENTS/
For more Interactions (Complete) data for PANCURONIUM BROMIDE (27 total), please visit the HSDB record page.

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Non-Human Toxicity Values
LD50 Rat oral 202 mg/kg
LD50 Rat ip 479 ug/kg
LD50 Rat sc 436 ug/kg
LD50 Rat iv 153 ug/kg
For more Non-Human Toxicity Values (Complete) data for PANCURONIUM BROMIDE (10 total), please visit the HSDB record page.

[1]. Pancuronium and gallamine are antagonists for pre- and post-junctional muscarinic receptors in the guinea-pig lung. Naunyn Schmiedebergs Arch Pharmacol. 1987 Apr;335(4):367-71.

[2]. Extracellular pancuronium affects sodium current in chick embryo sensory neurons. Br J Pharmacol. 1994 Jan;111(1):283-7.

[3]. A comparison of the effects of pancuronium bromide and its monoquaternary analogue, ORG NC 45, on autonomic and somatic neurotransmission in the rat. Br J Pharmacol. 1980;71(1):225-33.

Pancuronium is a steroid ester in which a 5alpha-androstane skeleton is C-3alpha- and C-17beta-disubstituted with acetoxy groups and 2beta- and 16beta-disubstituted with 1-methylpiperidinium-1-yl groups. It is a non-depolarizing curare-mimetic muscle relaxant. It has a role as a muscle relaxant, a cholinergic antagonist and a nicotinic antagonist. It is a steroid ester and an acetate ester.
A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than curare but has less effect on the circulatory system and on histamine release.
Pancuronium is a Nondepolarizing Neuromuscular Blocker. The physiologic effect of pancuronium is by means of Neuromuscular Nondepolarizing Blockade.
Pancuronium is a synthetic, long-acting bis-quaternary steroid and non-depolarizing neuromuscular blocking agent, with muscle relaxant activity. Pancuronium competitively binds to and blocks the nicotinic acetylcholine receptor at the neuromuscular junction, thereby preventing acetylcholine (ACh) binding and resulting in skeletal muscle relaxation and paralysis.
A bis-quaternary steroid that is a competitive nicotinic antagonist. As a neuromuscular blocking agent it is more potent than CURARE but has less effect on the circulatory system and on histamine release.
See also: Pancuronium Bromide (has salt form); Pancuronium bromide monohydrate (is active moiety of).

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Drug Indication
Used as a muscle relaxant during anesthesia and surgical procedures.

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Mechanism of Action
Nondepolarizing neuromuscular blocking agents inhibit neuromuscular transmission by competing with acetylcholine for the cholinergic receptors of the motor end plate, thereby reducing the response of the end plate to acetylcholine. This type of neuromuscular block is usually antagonized by anticholinesterase agents.
LOW CONCN OF PANCURONIUM BROMIDE (5X10-8 G/ML OR LESS), HAD NO PRESYNAPTIC EFFECT ON MURINE PHRENIC NERVE-DIAPHRAGM PREPN. AT HIGH CONCN (5X10-7 G/ML), PANCURONIUM BROMIDE DEPRESSED QUANTAL RELEASE TO 26% OF CONTROL IN CUT-FIBER PREPN & 40% OF CONTROL IN HIGH-MAGNESIUM PREPN. POSTSYNAPTIC EFFECTS REVEALED DEPRESSION TO 16 & 22% OF CONTROL, RESPECTIVELY, AT A CONCN OF 5X10-7 G/ML. PANCURONIUM BROMIDE HAD NO EFFECT ON DIRECTLY ELICITED ACTION POTENTIALS & ELECTRIC MEMBRANE CONSTANTS. THUS, PRESYNAPTIC AS WELL AS POSTSYNAPTIC EFFECTS OF PANCURONIUM BROMIDE IN PARALYTIC DOSES ARE ESSENTIAL IN CONTRIBUTING TO THE TOTAL EFFICACY OF NEUROMUSCULAR DEPRESSION.
THE PHARMACODYNAMICS OF D-TUBOCURARINE (D-TC), PANCURONIUM BROMIDE, METOCURINE, & GALLAMINE WERE STUDIED IN RAT PHRENIC NERVE-HEMIDIAPHRAGM PREPN WITH VASCULAR PERFUSION AT 25, 31, & 37 °C. D-TC, METOCURINE, & GALLAMINE EACH DEMONSTRATED A NEAR 2-FOLD INCREASE IN ED50 AT 25 °C COMPARED WITH 37 °C. NO SUCH RELATIONSHIP WAS APPARENT WITH PANCURONIUM BROMIDE. SLOPES OF THE DOSE-RESPONSE CURVES WERE NOT INFLUENCED BY TEMP; HOWEVER, THE SLOPES FOR METOCURINE & D-TC WERE LOWER THAN THOSE FOR PANCURONIUM BROMIDE & GALLAMINE. THUS, IN THE RAT, PANCURONIUM BROMIDE RETAINS POTENCY AT HYPOTHERMIA, WHEREAS THE OTHER RELAXANTS DECREASE POTENCY. IN ADDITION, METOCURINE & D-TC EXHIBIT LESS STEEP DOSE-RESPONSE CURVES UNDER THESE EXPTL CONDITIONS.

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Therapeutic Uses
Neuromuscular Nondepolarizing Agents; Nicotinic Antagonists
THE MAIN CLINICAL USE OF THE NEUROMUSCULAR BLOCKING AGENTS IS AS AN ADJUVANT IN SURGICAL ANESTHESIA TO OBTAIN RELAXATION OF SKELETAL MUSCLE, PARTICULARLY OF THE ABDOMINAL WALL ... MUSCLE RELAXATION IS ALSO OF VALUE IN VARIOUS ORTHOPEDIC PROCEDURES, SUCH AS THE CORRECTION OF DISLOCATIONS & THE ALIGNMENT OF FRACTURES. /NEUROMUSCULAR BLOCKING AGENTS/
...MAY BE USED MORE SAFELY IN PT WITH CARDIOVASCULAR DISEASE OR BRONCHIAL ASTHMA THAN ANY OTHER NEUROMUSCULAR BLOCKING DRUG. ...IT HAS ACTUALLY BEEN USED IN MGMNT OF STATUS ASTHMATICUS TO RELAX MUSCLES, THEREBY FACILITATING ARTIFICIAL RESPIRATION & DECR OXYGEN DEMAND. ... DURATION OF ACTION OF USUAL DOSE IS GENERALLY 30-60 MIN...
/NEUROMUSCULAR BLOCKING AGENTS/ HAVE BEEN USED TO FACILITATE LARYNGOSCOPY, BRONCHOSCOPY, & ESOPHAGOSCOPY, IN COMBINATION WITH A GENERAL ANESTHETIC AGENT. /NEUROMUSCULAR BLOCKING AGENTS/
For more Therapeutic Uses (Complete) data for PANCURONIUM BROMIDE (9 total), please visit the HSDB record page.

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Drug Warnings
THE NEUROMUSCULAR BLOCKING AGENTS ARE POTENTIALLY HAZARDOUS DRUGS. CONSEQUENTLY, THEY SHOULD BE ADMINISTERED TO PATIENTS ONLY BY ANESTHESIOLOGISTS & OTHER CLINICIANS WHO HAVE HAD EXTENSIVE TRAINING IN THEIR USE & IN A SETTING WHERE FACILITIES FOR RESPIRATORY & CARDIOVASCULAR RESUSCITATION ARE IMMEDIATELY AT HAND. /NEUROMUSCULAR BLOCKING AGENTS/
...IT IS ADVISABLE TO USE DRUG CAUTIOUSLY IN PRESENCE OF RENAL OR LIVER DISEASES.
EFFECT OF SPECIFIC DOSE OF ... PANCURONIUM MAY /POSSIBLY/ BE REDUCED IN PT WITH HIGH PLASMA GLOBULIN LEVELS (EG THOSE WITH LIVER DISEASE).
GREAT CARE SHOULD BE TAKEN WHEN ADMIN MUSCLE RELAXANTS TO DEHYDRATED OR SEVERELY ILL PATIENTS. /NEUROMUSCULAR BLOCKING AGENTS/
For more Drug Warnings (Complete) data for PANCURONIUM BROMIDE (17 total), please visit the HSDB record page.

C35H60N2O4.2BR

732.67

730.292

15500-66-0

16974-53-1 (cation);15500-66-0 (bromide);22189-36-2 (bromide hydrate);

441289

Off-white to pink solid powder

214 - 217ºC

0.036

52.6

0

4

6

41

1000

10

CC(=O)O[C@H]1C[C@@H]2CC[C@@H]3[C@@H]([C@]2(C[C@@H]1[N+]4(CCCCC4)C)C)CC[C@]5([C@H]3C[C@@H]([C@@H]5OC(=O)C)[N+]6(CCCCC6)C)C

NPIJXCQZLFKBMV-YTGGZNJNSA-L

InChI=1S/C35H60N2O4.2BrH/c1-24(38)40-32-21-26-13-14-27-28(35(26,4)23-31(32)37(6)19-11-8-12-20-37)15-16-34(3)29(27)22-30(33(34)41-25(2)39)36(5)17-9-7-10-18-36;;/h26-33H,7-23H2,1-6H3;2*1H/q+2;;/p-2/t26-,27+,28-,29-,30-,31-,32-,33-,34-,35-;;/m0../s1

1,1-((2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-3,17-diacetoxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthrene-2,16-diyl)bis(1-methylpiperidin-1-ium) bromide

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 2.5 mg/mL (3.41 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (3.41 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (3.41 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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配方 4 中的溶解度: 100 mg/mL (136.49 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。