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Morphine-induced antinociception is antagonized by the K(+)-channel blocker glibenclamide (glyburide; Glib), implicating ATP-sensitive (KATP) K+ channels in the analgesic effect of opioids. The present study examined the generality of this conclusion by measuring the effect of Glib on supraspinal (intracerebroventricular; i.c.v.) antinociception produced by representative mu-opioids and the non-opioids pilocarpine and two alpha 2-adrenoceptor agonists (clonidine and tizanidine) using the mouse tail-flick test. Concurrent administration of Glib (40 micrograms, i.c.v.) produced a significant rightward shift of the dose-response curve of morphine, levorphanol, methadone, pilocarpine, clonidine and tizanidine; a modest, but not statistically significant, rightward shift of the dose-response curves of the mu-selective peptides DAMGO ([D-Ala2,N-Me-Phe4,Gly-ol5]-enkephalin) and PL017 ([N-Me-Phe3,D-Pro4]-morphiceptin); and no shift of the dose-response curves of alfentanil, carfentanil, fentanyl, sufentanil, or beta-endorphin. Glib produced a leftward shift of the dose-response curve of etorphine. These data support the involvement of KATP-type K+ channels in mediation of supraspinal antinociception, differentiate Glib-sensitive and Glib-insensitive opioid agonists, and reveal fundamental differences among antinociceptive agents in the extent of demonstrable utilization of this transduction pathway.
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Trial patients were treated with a subcutaneously implanted programmable continuous infusion pump (SynchroMed, Medtronic), filled with baclofen (a muscle relaxant) to treat patients with chronic disabling spasticity who did not respond to a maximum dose of oral baclofen, dantrolene and tizanidine.
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Effects of tizanidine, a centrally acting muscle relaxant, on gastric acid secretion and gastric ulcers were studied in the rat. Tizanidine (5 mg/kg, s.c.) did not influence basal acid secretion, but inhibited the centrally stimulated acid secretion in anesthetized rats. Intraduodenal administration of tizanidine (10 mg/kg) also inhibited the centrally stimulated acid secretion. The compound potentiated bethanechol-induced acid secretion at 10 mg/kg, s.c. Clonidine was found to have similar effects to tizanidine at the lower dose. Both tizanidine and clonidine inhibited basal acid secretion at a relatively low dose in conscious rats. Tizanidine (5 mg/kg, s.c.) did not modify indomethacin- and stress-induced ulcers, but Shay ulcers were slightly inhibited by the drug. Indomethacin ulcers were significantly inhibited by 10 mg/kg, s.c., 10 mg/kg, p.o. or 20 mg/kg, p.o. of tizanidine. Clonidine also was found to be a strong inhibitory agent of indomethacin-, stress- and Shay-ulcers. These results suggest that similar to clonidine, a high dosage of tizanidine influences gastric acid secretion and gastric ulcers, although the activity is lower than that of clonidine.
Centrally acting alpha-2 adrenergic agonists are one of several pharmacologic agents used in the treatment of spasticity related to disorders of the central nervous system. In addition to their effects on spasticity, certain adverse cardiorespiratory effects have been reported. Adults chronically treated with angiotensin converting enzyme inhibitors may have a limited ability to respond to hypotension when the sympathetic response is simultaneously blocked. The authors present a 10-year-old boy chronically treated with lisinopril, an angiotensin converting enzyme inhibitor, to control hypertension who developed hypotension following the addition of tizanidine, an alpha-2 agonist, for the treatment of spasticity. The possible interaction of tizanidine and other antihypertensive agents should be kept in mind when prescribing therapy to treat either hypertension or spasticity in such patients.
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A simple method that can be performed at the bedside using a spring balance was developed in order to quantify spasticity. The effects of tizanidine on spasticity were evaluated in 30 patients with sequelae of cerebrovascular disease using this method. Treatment with tizanidine was effective in 60% of the patients; there were high correlations between spasticity before and after tizanidine administration and the severity of symptoms and also between the degree of improvement in spasticity and in that of the symptoms. Atonic seizures, due to overdose of tizanidine, were observed in only one patient. The simple spasticity quantification method developed was useful for monitoring tizanidine administration in order to prevent drug overdose. The method appears to be very useful for evaluating the degree of spasticity at the bedside and in measuring the effects of antispastic drugs.
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MSS progresses despite treatment with currently available antispastic agents, and it is associated with a high level of disability. Spasticity treatment represents a minor element of the overall cost of managing MSS patients in Spain. The approach to the assessment of spasticity varies between centers.
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This study included 18 subjects (12 men, 6 women; mean [SD] age, 26  years). The mean height and body weight of the subjects were 176 (8) cm and 70.1 (9.6) kg, respectively. The peak exposure, as measured by mean natural logarithm-transformed C(max) values, was significantly lower with the capsule compared with the tablet (2.7 vs 4.0 ng/mL; P < 0.019), and mean TmaX was significantly longer (2.6 vs 1.2 hours; P < 0.001). The 90% CIs for the capsule:tablet treatment ratios were 70.55 to 121.94 for AUC(0-lat) and 70.12 to 118.75 for AUC(0-infinity). The capsule did not achieve the protocol-defined definition of bioequivalence when given after a high-fat meal. All AEs were transient and mild in intensity, with asthenia being the most common event with the capsule and tablet formulations, occurring in 5 (28%) and 8 (44%) subjects, respectively.
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The usual causes of sinusbradycardia like hypothyroidism, hypothermia, intracranial pressure elevation, typhoid fever, sick sinus syndrome, hyperreactive carotid sinus reflex, organic heart disease, electrolyte disorders, and pharmacotherapy with beta-blockers, digitalis, and antiarrhythmics have been excluded in this case. Bradycardia can occur as a side effect of tizanidine. As this substance is metabolized by cytochrome P450 1A2 and rofecoxib inhibits this enzyme, an interaction between these drugs is probable. Liver function disorders and gastrointestinal symptoms, in the present case mainly due to the acute right heart failure, have also been described as side effects under tizanidine, diclofenac as well as rofecoxib. Supposedly, the combination of tizanidine/rofecoxib used to be prescribed frequently for lumbar pain as selective cyclooxygenase-(COX-)2 inhibitors are visibly replacing the nonsteroidal antirheumatics due to their better side effect profile. An augmented risk of cardiovascular events under rofecoxib led to its withdrawal from the market at the end of September 2004.
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Cerebral vasospasm after subarachnoid hemorrhage (SAH) has remained a major cause of morbidity and mortality in patients with SAH. Excitatory neurotransmitters are gathered in the extracellular space during ischemia due to cerebral vasospasm and initiate or stimulate a series of pathophysiological biochemical processes which consequently lead to neuronal death. Tizanidine (Sandoz compound DS 103-282, 5-chloro-4,2 (2-imidazolin-2-yl-amino)-2,1,3-benzothiazol hydrochloride) is a centrally-acting muscle relaxant and a selective alpha 2 adrenoreceptor agonist which shows its effect by stimulating presynaptic alpha 2 adrenoreceptors in central ASPergic and GLUergic system by inhibiting aspartic acid and glutamic acid release. In this study, the effect of Tizanidine on vasospasm was evaluated.
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A double-blind study was carried out in 30 patients suffering from spasticity due to cerebrovascular lesions to compare the long-term efficacy and tolerability of tizanidine hydrochloride with that of baclofen. A 2-week titration phase identified the optimum dose of tizanidine (max. 20 mg/day) or baclofen (max. 50 mg/day) in each patient. Patients were then treated with this dose for a 50-week maintenance phase. Efficacy and tolerability parameters were evaluated first on a monthly and then on a bimonthly basis. Both tizanidine and baclofen caused an improvement in the symptoms associated with spasticity. In end-point analysis, 87% of patients showed an improvement (p less than 0.01) in excessive muscle tone - the major efficacy parameter in this study - in the tizanidine group, while 79% improved (p less than 0.01) in the baclofen group. Side-effects in the tizanidine group were mild and transient and no patients discontinued the study; in the baclofen group, 3 patients discontinued the study due to severe side-effects. However, both drugs were assessed as effective and fairly well tolerated in the long-term. Although there were no statistically significant differences between the two drugs, the global assessment of antispastic efficacy revealed a nearly significant difference (p = 0.057) in favour of tizanidine and the global assessment of tolerability was also in favour of tizanidine.
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Twenty-three placebo-controlled studies (using baclofen, dantrolene, tizanidine, botulinum toxin, vigabatrin, prazepam and threonine) and thirteen comparative studies met the selection criteria. Only thirteen of these studies used the Ashworth scale, of which only three of the six placebo-controlled trials and none of the seven comparative studies showed a statistically significant difference between test drugs. Spasms, other symptoms and overall impressions were only assessed using unvalidated scores and results of functional assessments were inconclusive.
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Microsomal and crude synaptosomal fractions were prepared from the longitudinal muscle of guinea-pig ileum. A specific binding of [3H]yohimbine (10 nM) to alpha 2-adrenoceptor in the crude synaptosomal fraction was inhibited by tizanidine and clonidine. Tizanidine is about one-third as potent as clonidine. A specific binding of [3H]QNB (0.3 nM) to muscarine receptor in the microsomal fraction was inhibited by atropine (10(-8)-10(-7) M) but not by tizanidine (up to 10(-4) M). Tizanidine inhibited spontaneous movements of guinea pig ileum and rat stomach (in situ) and intestinal transit in mice, and induced mydriasis in mice. These effects induced by tizanidine might be due to activation of alpha 2-adrenoceptor but not to atropine like action.
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Direct laryngoscopy and tracheal intubation can result in blood pressure and heart rate increase which in turn may lead to myocardial ischemia, cerebral hemorrhage, and even death in susceptible patients. Tizanidine is α2-receptor agonists that suppresses central sympathetic system.
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The central alpha 2 adrenoceptor agonist tizanidine is a myotonolytic agent used in the treatment of spasticity in patients with cerebral or spinal injury. Wide interpatient variability in the effective plasma concentrations of tizanidine means that the optimal dosage must be titrated over 2 to 4 weeks for each patient (dosages of 2 to 36 mg/day have been used in clinical trials). Maximum effects occur within 2 hours of administration. Antispastic efficacy has been demonstrated for tizanidine in placebo-controlled trials, with reduction in mean muscle tone scores of 21 to 37% versus 4 to 9% for patients receiving placebo. Improvement in muscle tone occurred in 60 to 82% of tizanidine recipients, compared with 60 to 65% of baclofen and 60 to 83% of diazepam recipients. Spasm frequency and clonus are also reduced by tizanidine. The most common adverse effects associated with tizanidine are dry mouth and somnolence/drowsiness. Muscle strength, as assessed by objective means, appears not to be adversely affected by tizanidine and subjective muscle weakness is reported less often by tizanidine recipients than by those receiving baclofen or diazepam. Global tolerability was assessed as good to excellent in 44 to 100% of patients receiving tizanidine, compared with 38 to 90% of baclofen and 20 to 54% of diazepam recipients. In conclusion, tizanidine is an antispastic agent with similar efficacy to that of baclofen and a more favourable tolerability profile. While drowsiness is a frequently reported adverse effect with both agents, subjective muscle weakness appears to be less of a problem with tizanidine than with baclofen. Tizanidine, therefore, appears to be an attractive therapeutic alternative for patients with spasticity associated with cerebral or spinal damage.