What Is Vecuronium?

Vecuronium bromide, also known as vancoronin bromide, is a white or off-white chemical. Chemical name 1- [3-17-diacetoxy 2- (1-piperidinyl) -5-androstane-16-yl] -1-methylpiperidine, the molecular formula is C ₃₄ H ₅₇ BrN ₂ O _{4 has a} molecular weight of 325.4242. It is odorless, bitter, and hygroscopic. It is very soluble in ethanol, slightly soluble in water, and almost insoluble in ether; it is very soluble in dilute hydrochloric acid. Vecuronium bromide is an anesthetic (skeletal muscle relaxant). It is mainly used in combination with general anesthetics in clinical practice. It can be used for various operations and can also be used for endotracheal intubation during general anesthesia.

Chinese name: Vecuronium bromide
Foreign name: vecuronium bromide

CAS number: 50700-72-6
Molecular formula: C34H57BrN2O4

Vecuronium bromide

Vecuronium Bromide Basic Information

Chinese name: Vecuronium bromide

Chinese alias: bromide vankoronin;

English name: vecuronium bromide

English alias: Vecuronium bromide; Vecuronium Bromide; Vecuronium Bromide Hydrate;

CAS number: 50700-72-6

Molecular formula: C ₃₄ H ₅₇ BrN ₂ O ₄

Chemical structure:

Molecular weight: 637.73100

Exact mass: 636.35000

PSA: 55.84000

LogP: 2.86660 ^[1]

Vecuronium bromide properties

Melting point: 227-229 ° C

Storage conditions: Store in original container in a cool dark place. ^[1]

Vecuronium bromide pharmacological action

It is a monoquaternium steroid, a derivative of pancuronium bromide, a medium-effect non-depolarizing muscle relaxant. Its effect is similar to that of pancuronium bromide and tuberclosporine. Vecuronium can compete with cholinergic receptors and block the effects of acetylcholine, which can be reversed by anticholinergic drugs such as neostigmine. The muscle relaxation effect of vecuronium bromide is 1/3 stronger than that of pancuronium bromide, but the latency period for the muscle relaxation effect is short. The duration of muscle relaxation produced by the same dose in the initial period is shorter than that of pancuronium bromide and the recovery is faster. Intravenous injection of 0.08 to 0.1 mg / kg, markedly effective within 1 minute, peaked in 3 to 5 minutes, and the maintenance time of muscle relaxation is about 1/3 to 1/2 of pancuronium bromide, that is, 15 to 30 minutes, but as the dose increases, The maintenance time is extended. Its muscle relaxation effect is 1.2 to 1.7 times that of pancuronium bromide. When combined with certain inhalation anesthetics such as aflurane and isoflurane, the muscle relaxation effect is enhanced without significant block of ganglion and vagus nerve. It does not interfere with the reuptake of norepinephrine and adrenaline, and has no histamine release effect, so it does not affect heart rate and blood pressure, nor does it affect intracranial pressure. There is no or only slight accumulation ^[2] .

Vecuronium bromide pharmacokinetics

The pharmacokinetics of vecuronium bromide conforms to the two-compartment open model. Plasma absorption half-life is about 4 minutes and elimination phase half-life is about 31 minutes. The average steady-state blood drug concentration was 0.137 g / ml. After intravenous injection, 60% to 90% are combined with plasma proteins. It is mainly metabolized in the liver, and the muscle relaxation effect of metabolites is very weak. 85% of patients with bile and 15% are excreted through the kidney, and patients with chronic renal insufficiency have a 12% decrease in clearance rate. Muscle relaxation is prolonged by 32%. In patients with hepatic impairment, the intensity of the action and the duration of maintenance are increased. Vecuronium is transported through the placenta in a small amount, and the plasma half-life is 31 to 80 min. Does not accumulate in the body ^[2] .

Vecuronium bromide indication

Combined with general anesthesia, it is suitable for various operations and can also be used for endotracheal intubation during general anesthesia ^[2] .

Vecuronium contraindications

Disable pregnant women. Allergic to vecuronium bromide or bromide is contraindicated ^[2] .

Vecuronium bromide considerations

The safety of vecuronium in pregnant women has not been concluded. Because infants are more sensitive to vecuronium bromide, recovery time is 1.5 times that of adults. Not suitable for infants under the full moon. Not recommended for children. When vecuronium is used in patients with cirrhosis, cholestasis or severe renal insufficiency, the duration of muscle relaxation and recovery time are prolonged ^[2] .

Vecuronium bromide adverse reactions

Vecuronium bromide has a minimal cardiovascular effect, with occasional bronchospasm, skin flushing, rash, and allergic reactions. When vecuronium is used in patients with cirrhosis, cholestasis or severe renal dysfunction, the duration of muscle relaxation and recovery time are prolonged. Continuous use of vecuronium bromide up to 130 mg / kg (3 times the 95% blockade) did not find any tachycardia or arterial pressure changes, no accumulation, and no allergies ^[2-3] .

Vecuronium bromide dosage

Intravenous injection or intravenous drip cannot be injected intramuscularly. The dose for adults for tracheal intubation is 0.08 0.1mg / kg; the maintenance dose during surgery is 0.01 0.015mg / kg, (or 0.03 0.05mg / kg for intravenous injection ) Repeat as needed. Combined with anflurane or isoflurane, it can reduce the first two medicinal doses by 20% to 30%. The initial dose for children 1 to 10 years old can be slightly increased, and the interval between repeated administrations can be shortened as appropriate; 10 to 17 years old are treated the same as adults ^[2-3] .

Vecuronium drug interactions

Vecuronium bromide and halothane, diethyl ether, thiopental, methoxyfluflurane, ketamine, fentanyl, diuretics, aminoglycoside antibiotics, peptide antibiotics, thiamine hydrochloride, quinidine, fish essence The combined application of protein and metronidazole enhances the efficacy. Combined with neostigmine, tensiron, pyridospermine, phenytoin sodium, and carbamazepine, the efficacy is reduced ^[2] .

Vecuronium Bromide Expert Reviews

According to domestic reports, 45 children undergoing elective surgery were given intravenous vecuronium bromide at the same time during anesthesia, the first dose was 100 g / kg, and then continuous intravenous injection was 60 g / (kg · h) or 70 g / (kg H). Results The onset time of muscle relaxation was (143.91 ± 29.85) s, and the muscle relaxation effect was good. It can be effectively used for various types of pediatric surgical anesthesia ^[2] .

Introduction to Vecuronium Pharmacopeia

[Identification] (1) Take about 10mg of this product, add 2ml of water to dissolve, add 1ml of 1,2-dichloroethane and 1 drop of methyl orange indicator liquid, shake, separate, acidify the organic layer with sulfuric acid, that is red . (2) Take about 10mg of this product, add 10ml of water to dissolve it, and add silver nitrate test solution dropwise to form a light yellow curd-like precipitate. The precipitate can be slightly soluble in ammonia test solution, but almost insoluble in nitric acid. (3) The infrared light absorption spectrum of this product should be consistent with the reference spectrum ^[4] .

[Check] The clarity and color of the solution: Take 0.1g of this product, add 25ml of water, place in a warm water bath, shake the medicine to dissolve, and let it cool. The solution should be clear and colorless; The second appendix of the Chinese Pharmacopoeia 2000 (A first method) comparison must not be deeper. Relevant substances were taken from this product, and 0.02mol / L hydrochloric acid solution-ethanol (1: 1) was added to make a test solution containing 5.0mg per 1ml and a control solution containing 0.1mg per 1ml. Tested according to high performance liquid chromatography (Chinese Pharmacopoeia 2000, Appendix VD), using octadecylsilane bonded silica as a filler, ammonium chloride methanol solution (take 1.6g of ammonium chloride, dissolved in 8ml concentrated ammonia solution , Add 0.25mol / L perchloric acid solution to dissolve and dilute to 200ml, and then add 800ml of methanol to mix and make)) as mobile phase; detection wavelength is 210nm; the number of theoretical plates should not be lower than the calculated cuscuronium bromide peak In 2000, the resolution of vecuronium bromide and each impurity peak should meet the requirements. Take 20l of the control solution and inject it into the liquid chromatograph, adjust the sensitivity of the instrument so that the peak height of the main component chromatographic peak is about 10% of the full range; then accurately measure 20l of each of the two solutions and inject them into the liquid chromatograph, and record the chromatogram 3 times the peak retention time of the main component. Except for the solvent peak, the area of the impurity peaks and their sum should not be larger than 1/2 and 3/4 of the main peak area of the control solution, respectively. Dichloromethane and pyridine are taken from this product and determined according to the method for determination of residual organic solvents (Chinese Pharmacopoeia 2000 Edition, Appendix P), which should meet the requirements. Loss on drying Take this product and dry it to constant weight at 105 . Lose weight should not exceed 1.0%. (Appendix L of the Second Part of Chinese Pharmacopoeia 2000). Take this product for acidity, add water to make a solution containing about 4 mg of vecuronium bromide per 1 ml, and determine it according to law (Chinese Pharmacopoeia 2000 Edition, Appendix II H), the pH value should be 3.8 ~ 4.2 ^[4] .

[Content determination] Take about 0.25g of this product, accurately weigh, add 15ml of glacial acetic acid and acetic anhydride, add 5ml of mercury acetate test solution and 2 drops of naphthol benzyl alcohol indicator solution, and use perchloric acid titration solution (0.1mol / L) Titrate until the solution is yellow-green, and correct the titration result with a blank test. Each 1ml of perchloric acid titrant (0.1mol / L) is equivalent to 31.89mg of C ₃₄ H ₅₇ BrN ₂ O ₄ ^[4] .

[Category] muscle relaxant.

[Storage] shading, sealed, and stored in a cool place. ^[4] ^[5]