Experiments were performed on intact and spinalized rats anesthetized with urethane and alpha-chloralose. In intact rats, administration of tizanidine (0.1 mg/kg, i.v.) decreased the mono- (MSR) and polysynaptic reflex potentials (PSR). Blood pressure was initially elevated and then lowered by tizanidine. Although pretreatments with hexamethonium and phentolamine prevented the tizanidine-induce...

PURPOSE Tizanidine is a clonidine derivative and has the same effects, such as sedation, anxiolysis and analgesic response. We evaluated the effect of tizanidine on infiltration pain during epidural catheterization. METHODS Forty patients scheduled to undergo epidural anesthesia in elective surgery were randomly allocated into two groups. The control group received placebo 60 minutes before a...

The selectivity of tizanidine to the imidazoline-receptor and alpha 2-adrenoceptor recognized by 3H-p-aminoclonidine was examined in rat kidney membranes and was compared with those of other imidazoline compounds. Tizanidine bound to the imidazoline-receptors with approximately 20 times higher affinity than the alpha 2-adrenoceptors. The order of relative selectivity to imidazoline receptor was...

Clinical trials with tizanidine when administered alone have shown that 5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiodiazole (tizanidine) is safe and effective for spasticity control. However, given its mechanism of action and requirement for titration, clinical experience suggests that tizanidine is likely to be used in combination with other antispastic agents with different mechanisms ...

BACKGROUND Amiloride has been reported to produce a wide variety of actions, thereby affecting several ionic channels and a multitude of receptors and enzymes. Intrathecal α2-adrenergic receptor agonists produce pronounced analgesia, and amiloride modulates α2-adrenergic receptor agonist binding and function, acting via the allosteric site on the α2A-adrenergic receptor. OBJECTIVES To investi...

Most drugs that act on the central nervous system (CNS) require dose titration to avoid withdrawal syndrome. Tizanidine withdrawal syndrome is caused by adrenergic discharge due to its α2-agonist mechanism and is characterized by hypertension, reflex tachycardia, hypertonicity, and anxiety. Although tizanidine withdrawal syndrome is mentioned as a potential side effect of cessation, it is not c...

BACKGROUND Although intrathecal clonidine produces pronounced analgesia, antinociceptive doses of intrathecal clonidine produce several side effects, including hypotension, bradycardia, and sedation. Intrathecal tizanidine, another alpha(2)-adrenergic agonist, has provided antinociception without producing pronounced hemodynamic changes in animal studies. However, it has been unclear whether an...

OBJECTIVE To investigate the effects of antispastic drugs baclofen and tizanidine on reflexes and volitional tasks. DESIGN Double-blind, placebo-controlled, crossover, before-after trial, pilot study. SETTING Research laboratory in a rehabilitation hospital. PARTICIPANTS Men with chronic (>6mo) motor incomplete spinal cord injury (N=10) were recruited for the study. INTERVENTIONS Tizani...

Objective: In order to prolong the duration of intrathecal lidocaine, various drugs are used along with it. Due to the promising effects of tizanidine on central nervous system, it can be assumed that tizanidine can have a positive effect on increasing the anesthesia duration too. Thus, we aimed to investigate the effect of oral tizanidine on the duration of lidocaine spinal anesthesia.Me...

Background: A major problem in surgical procedures is postoperative pain. The effectiveness of prescribing preoperative tizanidine in reducing postoperative pain is not clear. The aim of this study was to determine the efficacy of tizanidine as a premedication in reducing pain after septoplasty. Methods: This double blind clinical trial study was performed in 71 patients aged from 18 to 50 yea...