DOI: http://dx.doi.org/10.18203/2319-2003.ijbcp20192206

A study to evaluate the skeletal muscle relaxant property of Pregabalin and Gabapentin in albino rats

Sushma V. Naidu, Vibha Rani

Abstract


Background: Skeletal muscle relaxants are the drugs which reduce unwanted spasm without interfering with consciousness and voluntary movements. The centrally acting muscle relaxants like Diazepam, is known to be GABA mimetics and other antiepileptics like Gabapentin and Pregabalin also act through the release of GABA. This study is done to investigate skeletal muscle relaxant property of these drugs in comparison to Diazepam.

Methods: T Models used in the experiment are Grip Strength Test, Rota Rod Method, Beam Walk Test, Photoactometer Test. Animals were divided into 6 groups of 6 rats each: Group 1: Control group treated with normal saline (0.1 ml/10gm), Group 2: Standard-15mg/kg of Diazepam, Group 3:T1-60 mg/kg of Gabapentin, Group 4:T2-10 mg/kg of Pregabalin, Group 5:T3-60 mg/kg of Gabapentin+Diazepam, Group 6:T4- 10 mg/kg of Pregabalin+Diazepam. Mean and standard deviation was calculated for each group. One way ANOVA was used for multiple group comparisons followed by post hoc Tukey’s test for statistical significance between the groups.

Results: Treatment with the above test drugs produced significant muscle relaxation and caused decreased fall off, sliding time, increase climbing time and decreased locomotor activity in all models indicating motor incoordination. The results obtained from both standard and test groups showed a highly significant difference in muscle relaxation when compared with the control group.

Conclusions: The test drugs showed skeletal muscle relaxant property in rats comparable to Diazepam. In view of these results, it can open a new avenue for these drugs to be used as skeletal muscle relaxants after conducting clinical trials.


Keywords


Diazepam, Gabapentin, Pregabalin, Skeletal muscle relaxation

Full Text:

PDF

References


Satoskar RS, Rege NN, Tripathi RK, Bhandarkar SD. Skeletal muscle relaxants, Pharmacology and pharmacotherapeutics. 25th Ed. RELX India Pvt Ltd. Popular Prakashan;2017:317-325.

Veena NS, Sivaji K, Benerji GV, Babu MF, Kumari DR. Skeletal muscle relaxant property of diazepam by using rotarod on albino mice. Indian J Basic Applied Med Res. 2015;4(4):714-21.

George M, Joseph L, Sharma A. Antidepressant and skeletal muscle relaxant effects of the aqueous extract of the Prosopis cineraria. Brazilian J Pharmaceut Sci. 2012 Sep;48(3):577-81.

Seth SD, Seth Vimlesh. Skeletal muscle relaxants, Textbook of pharmacology. 3rd Ed. Delhi, India:Elsevier-New;2009:36-38.

Katzung BG, Trevor AJ. Skeletal muscle relaxants, Basic & Clinical Pharmacology. 13th Ed. New York, NY: McGraw-Hill; 2015:267-283.

Rowbotham M, Harden N, Stacey B, Bernstein P, Magnus-Miller L. Gabapentin for the treatment of postherpetic neuralgia: a randomized controlled trial. JAMA. 1998 Dec 2;280(21):1837-42.

Morello CM, Leckband SG, Stoner CP, Moorhouse DF, Sahagian GA. Randomized double-blind study comparing the efficacy of gabapentin with amitriptyline on diabetic peripheral neuropathy pain. Arch Intern Med. 1999 Sep 13;159(16):1931-7.

Backonja M, Beydoun A, Edwards KR, Schwartz SL, Fonseca V, Hes M, et al. Gabapentin for the symptomatic treatment of painful neuropathy in patients with diabetes mellitus: a randomized controlled trial. JAMA. 1998 Dec 2;280(21):1831-6.

Elinor Ben-Menachem. Pregabalin Pharmacology and Its Relevance to Clinical Practice. Epilepsia 2004;45(6):13-8.

Crofford LJ, Rowbotham MC, Mease PJ, Russell IJ, Dworkin RH, Corbin AE, et al. Pregabalin for the treatment of fibromyalgia syndrome: results of a randomized, double-blind, placebo-controlled trial. Arthritis Rheum. 2005 Apr;52(4):1264-73.

Priebe MM, Sherwood AM, Graves DE, Mueller M, Olson WH. Effectiveness of gabapentin in controlling spasticity: a quantitative study. Spinal Cord. 1997 Mar;35(3):171.

Gruenthal M, Mueller M, Olson WL, Priebe MM, Sherwood AM, Olson WH. Gabapentin for the treatment of spasticity in patients with spinal cord injury. Spinal Cord. 1997;35(10):686-9.

Bradley LJ, Kirker SG. Pregabalin in the treatment of spasticity: a retrospective case series. Disabil Rehabil. 2008;30(16):1230-2.

Mueller ME, Gruenthal M, Olson WL. Gabapentin for relief of upper motor neuron symptoms in multiple sclerosis. Arch Phys Med Rehabil. 1997;78(5):521-4.

Pollmann W, Feneberg W. Current management of pain associated with multiple sclerosis. CNS Drugs. 2008;22(4):291-324.

Greenfield LJ. Molecular Mechanisms of Antiseizure Drug Activity at GABA-A Receptors. Seizure. 2013;22(8):589-600.

Nevins ME, Nash SA, Beardsley PM. Quantitative grip strength assessment as a means of evaluating muscle relaxation in mice. Psychopharmacology (Berl). 1993;110(1-2):92-6.

Hamm RJ, Pike BR, O'Dell DM, Lyeth BG, Jenkins LW. The rota rod test: an evaluation of its effectiveness in assessing motor deficits following traumatic brain injury. J neurotrauma. 1994;11(2):187-96.

Al-Naggar TB, Gomez-Serranillos MP, Carretero ME, Villar AM. Neuropharmacological activity of Nigella sativa L. extracts. J ethnopharmacol. 2003 Sep 1;88(1):63-8.

Luong TN, Carlisle HJ, Southwell A, Patterson PH. Assessment of Motor Balance and Coordination in Mice using the Balance Beam. J Vis Exp. 2011;(49):2376.

Sousa N, Almeida OF, Wotjak CT. A hitchhiker's guide to behavioral analysis in laboratory rodents. Genes Brain Behav. 2006;5 Suppl 2:05-24.

Zhang X, Li H, Hu S, Zhang L, Liu C, Zhu C, et al. Brain edema after intracerebral hemorrhage in rats: the role of inflammation. Neurol India. 2006 Oct 1;54(4):402.

Aryal B, Tae-Hyun K, Yoon-Gyoon K, Hyung-Gun K. A comparative study of the pharmacokinetics of traditional and automated dosing/blood sampling systems using gabapentin. Indian J Pharmacol. 2011 May;43(3):262.

Baillie JK, Power I. The mechanism of action of gabapentin in neuropathic pain. Current opinion in investigational drugs (London, England: 2000). 2006 Jan;7(1):33-39.

Kukkar A, Bali A, Singh N, Jaggi AS. Implications and mechanism of action of gabapentin in neuropathic pain. Arch Pharm Res. 2013 Mar;36(3):237-51.

Ben-Menachem E. Pregabalin pharmacology and its relevance to clinical practice. Epilepsia. 2004;45 Suppl 6:13-8.

Freynhagen R, Strojek K, Griesing T, Whalen E, Balkenohl M. Efficacy of pregabalin in neuropathic pain evaluated in a 12-week, randomised, double-blind, multicentre, placebo-controlled trial of flexible- and fixed-dose regimens. Pain. 2005 Jun;115(3):254-63.