Conclusion: These results suggest that Guaifenesin possesses muscle relaxant and anticonvulsant properties and may have a potential clinical use in absence seizure. Key Words: Guaifenesin, Anticonvulsant, Pentylenetetrazol Introduction Epilepsy is the most common disabling chronic illness of the central nervous system,1 and affects at least 50 million people Inhibitors,research,lifescience,medical worldwide. Although antiepileptic drugs are the mainstay of epilepsy treatment, less than 70% of those afflicted with epilepsy achieve satisfactory seizure control with the available antiepileptic drugs.2 In addition, many of the current anticonvulsants have various complications
and serious side effects such as hepatotoxicity and agranulocytosis,1,3,4 which necessitates new drugs with more suitable margins of safety and more tolerability. In modern pharmacology, drug development and introduction of new Inhibitors,research,lifescience,medical drugs are mainly based on our understanding
about the pathophysiology of the disease. The exact pathophysiological basis of epilepsy is unknown;5 however, the excitatory glutamatergic system seems to play a key role in generating and spreading epileptic discharge.6 Indeed, recent researches are focused on the development of drugs that counteract the activity of this system. Guaifenesin is an expectorant used widely in cough preprations.7 It is drawn upon as a skeletal muscle relaxant in some animal anaesthetic Inhibitors,research,lifescience,medical Inhibitors,research,lifescience,medical procedures as well.8 Chemically, Guaifenesin is a Propanediol drug. Previous studies have shown the central nervous system effects of Propanediol drugs, mainly Mephenesin, and their relevant
mechanisms. A study performed by Pralong et al.9 reported that Mephenesin might be an antagonist of excitatory amino acids and might have NMDA-blocking activity and proposed that the Inhibitors,research,lifescience,medical NMDA-blocking activity of Mephenesin might be relevant to its muscle-relaxing activity. This notion was subsequently bolstered by some other studies, inhibitor Paclitaxel demonstrating the muscle-relaxing effect of Mephenesin in relation to an excitatory transmitter-blocking activity.10 Interestingly, the chemical structure of Guaifenesin bears close resemblance to Mephenesin and both drugs have profound Carfilzomib muscle-relaxing activity.11 It can, therefore, be suggested that the muscle relaxant activity of Guaifenesin may be in consequence of NMDA-blocking activity.12 It is also noteworthy that Guaifenesin has been utilized successfully in fibromyalgia.13 The notion that increased levels of excitatory amino acids possibly participate in pain processes in fibromyalgia,14 has led to the suggestion that the NMDA and glutamate-blocking activities of Guaifenesin are likely to contribute to its effectiveness in fibromyalgia. Taken together, glutamate and NMDA receptors have important roles in the pathophysiology of epilepsy, and there is evidence suggestive of the NMDA antagonistic activity of Guaifenesin.