Mechanisms of action of eperisone on isolated dog saphenous arteries and veins.

Inoue, Sumito; Bian, Ka; Okamura, Takeshi; Okunishi, Hideki; Toda, Noboru

doi:10.1254/jjp.50.271

Cited by 12 publications

(10 citation statements)

References 12 publications

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“…They act centrally by relaxing skeletal and vascular smooth muscles to improve circulation and suppress pain reflex 3,4. These drugs are usually prescribed in combination with NSAIDs as painkillers.…”

Section: Discussionmentioning

confidence: 99%

Oral Muscle Relaxant May Induce Immediate Allergic Reactions

et al. 2012

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Eperisone and afloqualone act by relaxing both skeletal and vascular smooth muscles to improve circulation and suppress pain reflex. These drugs are typically prescribed with non-steroidal anti-inflammatory drugs (NSAIDs) as painkillers. However, there have been no reports on serious adverse reactions to oral muscle relaxants; and this is the first report to describe three allergic reactions caused by eperisone and afloqualone. All three patients had histories of allergic reactions after oral intake of multiple painkillers, including oral muscle relaxants and NSAIDs, for chronic muscle pain. An open-label oral challenge test was performed with each drug to confirm which drugs caused the systemic reactions. All patients experienced the same reactions within one hour after oral intake of eperisone or afloqualone. The severity of these reactions ranged from laryngeal edema to hypotension. To confirm that the systemic reaction was caused by eperisone or afloqualone, skin prick testing and intradermal skin tests were performed with eperisone or afloqualone extract in vivo, and basophil activity tests were performed after stimulation with these drugs in vitro. In one patient with laryngeal edema, the intradermal test with afloqualone extract had a positive result, and CD63 expression levels on basophils increased in a dose-dependent manner by stimulation with afloqualone. We report three allergic reactions caused by oral muscle relaxants that might be mediated by non-immunoglobulin E-mediated responses. Since oral muscle relaxants such as eperisone and afloqualone are commonly prescribed for chronic muscle pain and can induce severe allergic reactions, we should prescribe them carefully.

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Section: Discussionmentioning

confidence: 99%

Oral Muscle Relaxant May Induce Immediate Allergic Reactions

et al. 2012

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“…This indicates that eperisone blocks muscarinic receptors at the effector site. This antimuscarinic effect of eperisone has been re cently reported in isolated dog saphenous arteries and veins (14). Some antispasmodics such as trihexyphenidyl and benztropine exert their antispasmodic effect, at least in part, through blockade of muscarinic receptors (15).…”

Section: Discussionmentioning

confidence: 73%

Anti-Nicotinic and Anti-Muscarinic Actions of Eperisone in the Isolated Canine Atrium.

et al. 1991

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ABSTRACT-The effects of eperisone, an antispastic agent, on the chronotropic and inotropic responses to acetylcholine, nicotine or stimulation of intracardiac autonomic nerves were evaluated in isolated, blood-perfused canine atrium. Eperisone (10-300,ug) injected into the sinus node artery of the isolated atrium produced dose-related nega tive chronotropic and inotropic effects, which were not affected by atropine. In the same doses, eperisone inhibited the negative chronotropic and inotropic responses to an injection of acetylcholine and intracardiac parasympathetic stimulation. Eperisone also suppressed the negative followed by positive cardiac responses to nicotine, but did not modify the positive responses to intracardiac sympathetic stimulation or nor epinephrine. The inhibitory effect persisted much longer for the responses to nicotine or parasympathetic stimulation than for those to acetylcholine. These results suggest that eperisone at doses that induce direct cardiac depressant effects exerts its blocking action on nicotinic receptors at parasympathetic ganglia and sympathetic nerve termi nals and on muscarinic receptors at the effector cells in the dog heart.

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“…32 Moreover, treatment with eperisone attenuates the contractions induced by norepinephrine and serotonin in the arteries, as well as the contractions induced by clonidine and phenylephrine in the veins. 32 In healthy volunteers, a single dose of eperisone 300 mg has a sympatho-suppressive action and enhances the blood flow in resting skeletal muscles, with no effect on the sympathetic nerve activity in actively contracting muscles, eg, while standing or hand-gripping. 18 Thus, in patients with LBP, eperisone is also expected to improve the blood flow to muscles and improve the hypoxic condition.…”

Section: Discussionmentioning

confidence: 99%

“…31 With reference to this, preclinical studies have shown that ep- erisone exerts several activities on the saphenous artery and veins, thus regulating the blood flow to skeletal muscles of the lower limbs. 32,33 For example, eperisone relaxes the saphenous arteries and veins previously contracted by norepinephrine, serotonin, acetylcholine, potassium, or barium. 32 Moreover, treatment with eperisone attenuates the contractions induced by norepinephrine and serotonin in the arteries, as well as the contractions induced by clonidine and phenylephrine in the veins.…”

Section: Discussionmentioning

confidence: 99%

“…32,33 For example, eperisone relaxes the saphenous arteries and veins previously contracted by norepinephrine, serotonin, acetylcholine, potassium, or barium. 32 Moreover, treatment with eperisone attenuates the contractions induced by norepinephrine and serotonin in the arteries, as well as the contractions induced by clonidine and phenylephrine in the veins. 32 In healthy volunteers, a single dose of eperisone 300 mg has a sympatho-suppressive action and enhances the blood flow in resting skeletal muscles, with no effect on the sympathetic nerve activity in actively contracting muscles, eg, while standing or hand-gripping.…”

Section: Discussionmentioning

confidence: 99%

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Open experience with a new myorelaxant agent for low back pain

Sartini

Guerra²

2008

Adv Therapy

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Eperisone had an analgesic and muscle relaxant effect in patients with LBP. It should be noted that while it is common practice in rheumatology to combine a pain killer with a muscle relaxant in order to achieve a satisfactory result on both symptoms, the present results with eperisone were achieved with a single drug. With an improved tolerability profile compared with nonsteroidal anti-inflammatory drugs, and a lack of significant adverse effects on the CNS, eperisone hydrochloride represents a valuable alternative to traditional analgesics and muscle relaxants for the treatment of LBP.

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Mechanisms of action of eperisone on isolated dog saphenous arteries and veins.

Cited by 12 publications

References 12 publications

Oral Muscle Relaxant May Induce Immediate Allergic Reactions

Oral Muscle Relaxant May Induce Immediate Allergic Reactions

Anti-Nicotinic and Anti-Muscarinic Actions of Eperisone in the Isolated Canine Atrium.

Open experience with a new myorelaxant agent for low back pain

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