Muscle relaxants | Pancuronium bromide (pancuronium brom ide), the chemical name is dibromide (1, 1 ′-[3 α,17 β-Diacetoxy-5 α-androstane -2 β,16 β-diyl] bis [1-methylpiperidine]), it is a long-acting non-depolarizing muscle relaxant in the synthetic bisquaternary ammonium steroid. It is the earliest muscle relaxant used in the ICU. Its effect is 4-5 times stronger than that of rightline. All M choline receptors in the body have a blocking effect. The effect is similar to that of carrine chloride, but there are no side effects such as ganglion block and blood pressure drop, and it will not cause bronchospasm. It may also excite the heart β receptor or anti-vagal effect to increase the heart rate, increase blood pressure and increase Cardiac output. It is used as an auxiliary medicine for surgical or orthopedic anesthesia to obtain sufficient muscle relaxation. It can also be used for convulsive diseases such as tetanus. |
Synthesis method | Using 5 α-androst-2-ene-17-one as raw material, the target compound Pancuronium bromide was synthesized through a 6-step reaction. Fig. 1 shows the synthesis route of pancuronium bromide |
mechanism of action | after this product binds to N2 choline receptors on skeletal muscle cells, it does not produce depolarization, but competitively blocks the depolarization of the neurotransmitter acetylcholine, thus producing skeletal muscle relaxation effect. Its muscle relaxation efficiency is 3~5 times that of tuguoarine, and the effect is faster. This product cannot be taken orally, only for intravenous injection. 3~4 minutes after intravenous injection, the effect is obvious, and the maintenance time is about 20~30 minutes. About 30% of this product is metabolically inactivated in the liver, and most of it is excreted through the kidneys in its original form. Compared with tubuarine, this product is characterized by a moderate excitatory effect on the cardiovascular system, and no obvious histamine release effect. Continuous use has no accumulation and no adverse effects on the fetus. Neostigmine can resist the muscle relaxation effect of this product. |
adverse reactions | can specifically block the cardiac atrioventricular node M choline receptor, with moderate vagus nerve effect, thus increasing heart rate, blood pressure, and even ventricular arrhythmia in individual patients. |
taboo | hypertension, severe liver and kidney insufficiency and patients with obstructive jaundice should be used with caution. |
precautions | 1. for patients with renal insufficiency and biliary obstruction, the duration is prolonged. 2. It has a moderate inhibitory effect on pseudo-cholinesterase activity, but it is relatively short-lived, and cholinesterase inhibitors have an antagonistic effect on it. 3. Repeated use has a savings effect. (2015-12-2) |
Production method | The following compounds react with isopropenol acetate to carry out enol esterification, and then epoxidize p-chloroperbenzoic acid, hydrolyze potassium hydroxide, and make one of the epoxides ring to form a carbonyl group, then react with piperidine, sodium borohydride is reduced, acetylated, and finally reacted with two molecules of methyl bromide, and quaternized into salt to obtain pancuronium bromide. |
toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |