Disease relevance of eperisone

• Muscle cramps in chronic liver diseases and treatment with antispastic agent (eperisone hydrochloride) [1].
• The efficacy and safety of eperisone in patients with cervical spondylosis: results of a randomized, double-blind, placebo-controlled trial [2].

High impact information on eperisone

• This depressant action of eperisone was rapidly reversible but was often accompanied by a reduction of the amplitude of the action potentials [3].
• Eperisone, an antispastic agent, possesses vasodilating actions on the guinea-pig basilar artery [4].
• The first-pass metabolism of eperisone was confirmed in the perfused rat small intestine in situ [5].
• Metabolism of eperisone to an omega-1-hydroxylated metabolite (HMO), the first step of eperisone metabolism, was studied using rat intestinal microsomes in vitro [5].
• METHODS: The systemic availabilities of eperisone were estimated by administering the drug into the duodenum, portal vein, and femoral vein in rats in vivo [5].

Biological context of eperisone

• In vitro, (+)-3-(3-[3H]hydroxyphenyl)-N-(1-propylpiperidine) ((+)-[3H]3-PPP) specific binding, in rat brain membrane, was prevented by eperisone and the IC50 value was 0.43 nM [6].
• These results suggest that eperisone predominantly inhibits synaptic transmission of the MVN ascending neurons [7].
• Transdermal eperisone elicits more potent and longer-lasting muscle relaxation than oral eperisone [8].
• The cross-correlation analysis suggested that the membrane potentials of both tonic and phasic motoneurons are equally lowered by eperisone or that monosynaptic transmission from primary afferents of muscle spindles to motoneurons is inhibited by eperisone [9].
• The safety analysis showed persistent vomiting (n=1), fatigue (n=1), headache and dry mouth (n=2), epigastric pain (n=1) and slight changes in blood pressure under Eperisone which was generally well tolerated by the patients [10].

Anatomical context of eperisone

• Eperisone was biotransformed to HMO by rat intestinal microsomes, and this was inhibited by alpha-naphthoflavone and an anti-rat CYP1A antibody [5].
• CONCLUSIONS: Those data strongly suggest that eperisone may be metabolized to HMO by CYP1A in rat intestinal microsomes during the first-pass through the epithelium of the small intestine [5].
• Effects of eperisone, an antispasmodic in skeletal muscle, were investigated in helical strips of dog saphenous artery and vein [11].
• Effects of eperisone applied by microiontophoresis on neurons in the medial and lateral vestibular nuclei [7].
• In addition, iontophoretically applied eperisone in doses of 50-100 nA inhibited the orthodromic spike elicited by vestibular nerve stimulation in the MVN monosynaptic neurons projecting to the abducens nucleus (ascending neuron), without affecting that in the MVN neurons projecting to the spinal cord (descending neuron) [7].

Associations of eperisone with other chemical compounds

• Long-lasting muscle relaxant activity of eperisone hydrochloride after percutaneous administration in rats [12].
• 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 [13].
• The sympatho-suppressive effect of eperisone may be related to the drug-induced increase of blood low in the resting skeletal muscles; also it may be one more mechanism through which the drug can exert its muscle relaxant action [14].
• The uptake of choline by the isolated bovine brain capillaries was significantly inhibited by eperisone, scopolamine and thiamine in consistent with the in vivo results [15].
• In the sciatic nerve isolated from mice, mexiletine, lidocaine, eperisone, and tolperisone impaired the propagation of low frequency action potentials (evoked at 0.2 Hz) [16].

Gene context of eperisone

• Eperisone is determined using ESI in a single-quadrupole MS [17].

Analytical, diagnostic and therapeutic context of eperisone

• In contrast, intravenous injection of eperisone produced either a rapidly reversible depression of responses to both noxious and innocuous stimuli or had no effect on these responses [3].
• In the intestinal perfusion experiment, the appearance clearance to the portal vein from the intestinal lumen was much lower than the elimination clearance from the intestinal lumen, resulting in high metabolic clearance of eperisone in the small intestine [5].
• Treatment with eperisone (10(-5) M) potentiated the contractile response to electrical stimulation of adrenergic nerves; the potentiating effect was suppressed by yohimbine [11].

References