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

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

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)