Abstract
Tizanidine is an alpha 2-adrenergic receptor agonist with myospasmolytic action. It is indicated for the treatment of back pain as monotherapy or in combination with nonsteroidal anti-inflammatory drugs (NSAIDs). Published experimental and clinical studies suggest that tizanidine reduces the frequency of NSAID-induced gastrointestinal (GI) adverse effects. In animal experiments tizanidine reduced baseline and induced gastric acid secretion, reversed NSAID-induced changes in gastric mucosal and gastric fluid glycoprotein content, and reduced NSAID-induced gastric ulcers. In clinical studies the frequency of GI adverse events and the frequency of occult blood in stool were generally reduced when tizanidine was combined with an NSAID as compared with NSAID treatment alone. The mechanism of action is probably through reduction of gastric acid secretion and favorable effects on gastric glycoprotein content by means of stimulation of gastric and central alpha 2-adrenergic receptors. Experimental and clinical data supporting a gastroprotective effect of tizanidine are reviewed in this paper, and the possible mechanisms are discussed.
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