Antiarrhythmic Effects of Skeletal Muscle Relaxants

Changing trends in the use of anxiolytic agents and recent reassessment of their neuropharmacological activity has prompted this evaluation of the peripheral neuromuscular activity of the benzodiazepine, flurazepam. In previous reports we have documented peripheral neuromuscular activity of chlordiazepoxide and diazepam on the rat phrenic nerve diaphragm preparation. The water soluble benzodiazepine, flurazepam, has been studied on the rat phrenic nerve diaphragm and frog rectus abdominis in vitro. On the former preparation flurazepam enhanced and then blocked the response to indirect electrical stimulation (0.2 Hz) and readily blocked posttetanic potentiation and prevented the preparation from sustaining a tetanic contracture (30 Hz). On the later preparation, flurazepam blocked in a noncompetitive manner the response of the frog muscle to applied cholinergic agonists. Studies on the rat preparation with the neuromuscular blocking drug succinylcholine have shown an unexpected protection against blockade in preparations pretreated with low concentrations of flurazepam. This was not observed when flurazepam was given prior to d-tubocurarinc. The application of adenosine to rat diaphragms during steady-state partial blockade caused by flurazepam or d-tubocurarine showed an inhibiting action of adenosine which was reversed by theophylline. Pretreatment of rat preparations with dipyridamole significantly enhanced the blocking action of standard concentrations of succinylcholine.These results, along with those in the literature, encourage a reassessment of the action of purines and benzodiazepines on skeletal muscle and encourage a consideration of a possible involvement of purinergic neuromodulation of transmission which is unmasked when the safety factor for transmission is altered by muscle relaxants. The possible clinical significance of protection against succinylcholine by benzodiazepines is noted.

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A Review - Carisoprodol as Skeletal Muscle Relaxant

International Journal of Scientific Research in Science and Technology ◽

10.32628/ijsrst20716 ◽

2020 ◽

pp. 40-44

Author(s):

A. A Patil ◽

M. K. Shirsat ◽

V. R. Salunkhe

Keyword(s):

Skeletal Muscle ◽

Allocation Concealment ◽

Muscle Relaxants ◽

Chemical Methods ◽

Physiochemical Properties ◽

Musculoskeletal Conditions ◽

Intention To Treat ◽

Physico Chemical ◽

Derivatives Of ◽

Host Target

In the world of pharmacology, the prescription of a medicine and its dosage play important role. Different physico-chemical methods are in vogue in describing the interactions of the drug molecule with host target among them, the chief being spectroscopic, chromatographic and quantum mechanical techniques. Skeletal muscle relaxants are divided into two categories: antispastic (for conditions such as cerebral palsy and multiple sclerosis) and antispasmodic agents (for musculoskeletal conditions). Antispastic agents (e.g., baclofen [Lioresal], dantrolene [Dantrium]) should not be prescribed for musculoskeletal conditions because there is sparse evidence to support their use. Rather, anantispasmodic agent may be more appropriate Many of the studies evaluating the effectiveness of skeletal muscle relaxants are hampered by poor methodologic design, including incomplete reporting of compliance, improper or no mention of allocation concealment, not utilizing intention-to-treat methods, and inadequate randomization. skeletal muscle relaxants have been evaluated in systematic reviews and meta-analyses.These include Methocarbamol, Meprobamate, Metaxalone, Carisoprodol, Dantrium and Baclofen. Chemically Carisoprodol is N-isopropyl-2-methyl-2-propyl-1,3-propanediol dicarbamate. Methods like nitration, Sulphonation, Methylation, Esterification, Acetylation and Diazotization was used for formation of new derivative which can be detected in UV region. Different reactions of diazotization were used for getting a new and novel derivative of Carisoprodol. Physiochemical properties, TLC, UV, IR and NMR analysis of Carisoprodol and newly obtained derivatives of Carisoprodol was studied and it showed that there was change in color, odour, taste, melting point, solubility pattern of original drug and derivatives.

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