Non-depolarizing neuromuscular blocker; muscle relaxant

Absorption, Distribution and Excretion
Poor gastrointestinal absorption. Studies on the distribution, metabolism, and excretion of rocuronium in cats and dogs indicate that it is primarily excreted via the liver. 0.3 L/kg [3 to <12 months]
0.26 L/kg [1 to <3 years]
0.21 L/kg [3 to <8 years]
0.25 L/kg/hr [Adults (27 to 58 years)]
0.21 L/kg/hr [Elderly (≥65 years)]
0.16 L/kg/hr [Normal kidney and liver function]
0.13 L/kg/hr [Kidney transplant patients]
0.13 L/kg/hr [Patients with liver dysfunction]
0.35 +/- 0.08 L/kg/hr [Pediatric patients aged 3 to <12 months]
0.32 +/- 0.07 L/kg/hr [Pediatric patients aged 1 to 3 years]
0.44 +/- 0.16 L/kg/hr [3 to 8 years] [Pediatric Patient]

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Metabolism/Metabolites
Rocuronium bromide is metabolized to the less active metabolite 17-deacetylated rocuronium bromide, which is primarily excreted via the liver.

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Biological Half-Life
Rapid distribution half-life is 1-2 minutes, and slow distribution half-life is 14-18 minutes. Renal impairment has no net effect on the half-life, but the half-life is almost doubled in patients with impaired liver function.

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Limited information exists regarding the use of rocuronium bromide during lactation, but there is currently no evidence of adverse effects on infants. Due to its short duration of action, high polarity, and poor oral absorption, rocuronium bromide is unlikely to enter breast milk or the infant's bloodstream at high concentrations. When multiple anesthetics are used during surgery, the medication recommendations for the most likely adverse reaction should be followed. Using rocuronium bromide as a component of general anesthesia for cesarean section may delay the onset of lactation. ◉ Effects on Breastfed Infants
Four mothers of breastfeeding infants aged 3 to 5 months underwent general anesthesia with propofol and remifentanil as induction agents and endotracheal intubation with 0.5 mg/kg rocuronium bromide. After induction, propofol was discontinued, and anesthesia was maintained for 57 to 70 minutes using xenon inhalation. Breastfeeding resumed 1.5 to 5 hours post-surgery. No infants experienced significant dizziness or drowsiness. After the mothers were discharged, all infants were in good condition at home without any adverse events.
◉ Effects on Lactation and Breast Milk
A randomized study compared the effects of cesarean section versus vaginal delivery under general anesthesia, spinal anesthesia, or epidural anesthesia on serum prolactin and oxytocin levels and time to lactation initiation. General anesthesia was induced with propofol 2 mg/kg and rocuronium bromide 0.6 mg/kg, followed by sevoflurane and rocuronium bromide 0.15 mg/kg as needed. After delivery, all patients received an intravenous infusion of 30 IU of oxytocin dissolved in 1 L of normal saline, and 0.2 mg of ergonovine if blood pressure was normal. Patients in the general anesthesia group received fentanyl at 1 to 1.5 μg/kg postpartum. Patients in the general anesthesia group (n=21) had higher postoperative prolactin levels and a longer mean time to lactation initiation (25 hours) than other groups (10.8 to 11.8 hours). Postpartum oxytocin levels were higher in the non-pharmacological vaginal delivery group than in the general anesthesia and spinal anesthesia groups.
Protein binding
Approximately 30% is bound to human plasma proteins.

[1]. Konishi J, Suzuki T, Kondo Y, Baba M, Ogawa S. Rocuronium and sugammadex used effectively for electroconvulsive therapy in a patient with Brugada syndrome. J ECT. 2012 Jun;28(2):e21-2.

[2]. Zhang Y, Xiang Y, Liu J. Prevention of pain on injection of rocuronium: a comparison of lidocaine with different doses of parecoxib. J Clin Anesth. 2012 Jul 2.

[3]. Suzuki T, Nameki K, Shimizu H, Shimizu Y, Nakamura R, Ogawa S. Efficacy of rocuronium and sugammadex in a patient with dermatomyositis. Br J Anaesth. 2012 Apr;108(4):703.

[4]. Illodo Miramontes G, Doniz Campos M, Filgueira Garrido P, Vázquez Martínez A. Rocuronium used in rapid sequence intubation and reversal with sugammadex in a patient with myasthenia gravis.Rev Esp Anestesiol Reanim. 2011 Dec;58(10):626-7.

[5]. García Sánchez JI, Martínez Hurtado ED, Tordecilla Echenique YY, Santa-Ursula TJ. Rocuronium used after sugammadex.Rev Esp Anestesiol Reanim. 2011 Dec;58(10):620-1.

Rocuronium bromide is a 5α-androstane compound with 3α-hydroxy, 17β-acetoxy, 2β-morpholino, and 16β-N-allylrocurolino substituents. It is a neuromuscular blocker, muscle relaxant, and drug allergen. It is an androstane compound, a 3α-hydroxy steroid, a quaternary ammonium ion, an acetate, a morpholino compound, and a tertiary amine compound. It is derived from the hydride of 5α-androstane. Rocuronium bromide (rapid-acting rocuronium bromide) is a deacetoxy analog of vecuronium bromide, with a faster onset of action. It is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Rocuronium bromide was marketed in 1994 and has a rapid onset of action and a moderate duration of action. It is commonly marketed under the brand names Zemuron and Esmeron. This drug is associated with a risk of allergic reactions in certain high-risk patients, such as those with asthma. However, other non-depolarizing neuromuscular blocking agents also have similar rates of allergic reactions. [Sugammadextrin sodium], a γ-cyclodextrin derivative, has been introduced as a novel drug to reverse the effects of rocuronium bromide. Rocuronium bromide is a non-depolarizing neuromuscular blocking agent. The physiological effects of rocuronium bromide are achieved through non-depolarizing neuromuscular blockade. It is an androstanol non-depolarizing neuromuscular blocking agent. It has a monoquaternary ammonium structure and is a weaker nicotine receptor antagonist than pancuronium bromide. See also: Rocuronium bromide (active ingredient). Drug Indications For use in inpatients and outpatients as an adjunct to general anesthesia to facilitate rapid sequential and routine endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Mechanism of Action Rocuronium bromide exerts its effect by competing with cholinergic receptors on the motor endplate. This effect can be antagonized by acetylcholinesterase inhibitors, such as neostigmine and ethanocyanine chloride. Rocuronium bromide exerts its effect by competitively binding to nicotinic cholinergic receptors. The binding of vecuronium bromide reduces the chance of acetylcholine binding to nicotinic receptors on the postsynaptic neuromuscular junction membrane. Therefore, depolarization is prevented, calcium ions cannot be released, and muscle contraction cannot occur. There is evidence that non-depolarizing drugs can also affect acetylcholine release. It is hypothesized that non-depolarizing drugs bind to postsynaptic (“cureus”) receptors, thus potentially interfering with the flow of sodium and potassium ions, which are responsible for the depolarization and repolarization of membranes related to muscle contraction.

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Pharmacodynamics
Neuromuscular blocking agents are a class of drugs that primarily induce skeletal muscle relaxation by reducing the response of the neurotransmitter acetylcholine (ACh) at the neuromuscular junction in skeletal muscle.
At this site, acetylcholine (ACh) typically causes electrical depolarization of the postsynaptic membrane of the motor endplate, leading to the conduction of muscle action potentials and ultimately inducing skeletal muscle contraction. Neuromuscular blocking agents are classified as depolarizing and non-depolarizing. Rocuronium bromide is a non-depolarizing neuromuscular blocking agent, with a dose-dependent onset rate ranging from rapid to moderate, and a moderate duration of action. Similar to vecuronium bromide, rocuronium bromide has a longer duration of action in infants than in children. However, unlike vecuronium bromide, rocuronium bromide retains its moderate-acting neuromuscular blocking agent properties in infants.

C32H53N2O4+

529.77422

529.40

C, 72.55; H, 10.08; N, 5.29; O, 12.08

143558-00-3

Rocuronium Bromide;119302-91-9

441290

Typically exists as solid at room temperature

4.304

59

1

5

6

38

898

10

O[C@@H]1[C@@H](N2CCOCC2)C[C@@]3(C)[C@](CC[C@]4([H])[C@]3([H])CC[C@@]5(C)[C@@]4([H])C[C@H]([N+]6(CC=C)CCCC6)[C@@H]5OC(C)=O)([H])C1

YXRDKMPIGHSVRX-OOJCLDBCSA-N

InChI=1S/C32H53N2O4/c1-5-14-34(15-6-7-16-34)28-20-26-24-9-8-23-19-29(36)27(33-12-17-37-18-13-33)21-32(23,4)25(24)10-11-31(26,3)30(28)38-22(2)35/h5,23-30,36H,1,6-21H2,2-4H3/q+1/t23-,24+,25-,26-,27-,28-,29-,30-,31-,32-/m0/s1

[(2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)-3-hydroxy-10,13-dimethyl-2-morpholin-4-yl-16-(1-prop-2-enylpyrrolidin-1-ium-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate

Rocuronium; 143558-00-3; Zemuron; Rocuronium ion; Rocuronium cation; UNII-WRE554RFEZ; WRE554RFEZ; CHEBI:8884;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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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。