Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0026838 (spasticity)
 6,471 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

This report summarizes experience with baclofen (Lioresal) in the management of spasticity and muscle spasms in 113 patients treated for up to six years. Baclofen was found to be of little help in nine patients with spasticity of cerebral origin, but was effective in reducing spasticity of spinal origin in 72 out of 90 patients (80%). It also reduced the number and severity of spasms in 76 out of 87 patients (87%). Side effects necessitating reduction of dosage were experienced by 20% of patients. Baclofen appears to be a safe and effective agent in the management of spasticity, with the advantage that adequate dosage can usually be achieved without sedation. Beneficial effects have persisted throughout the follow-up period.
 ...
PMID:Bacloffen (Lioresal) in the long-term management of spasticity. 82 Sep 53

In 17 in-patients suffering from spasticity due to multiple sclerosis, the effect and tolerability periods were 4 weeks each. As to efficacy, the variables: spasticity, clonus, flexor spasms, gait and bladder function were evaluated clinically. No significant difference was found between the two drugs. As far as side-effects are concerned, sedation was specifically inquired about. Apart from that, spontaneoulsy reported side-effects were recorded. Sedation was more often seen during treatment with diazepam, while the side-effects during baclofen treatment were more varied. The total number and severity of side-effects were equal in the two treatment groups. A preference for one of the two treatment periods was stated by the investigator before the code was broken. A significant difference (p less than 0.001) in favor of Lioresal was found. This is discussed in the light of the fact that no significant difference was found for the individual symptoms or side-effects.
 ...
PMID:A double-blind trial with baclofen (Lioresal) and diazepam in spasticity due to multiple sclerosis. 109 Jan 3

Fourteen patients with spinal cord damage were treated with Ba-34647 (Lioresal, Ciba-Geigy), a new antispasticity drug. The treatment was initiated for excessive skeletal muscle spasticity and voiding difficulty. Seven of the patients had been wearing indwelling catheters and seven were catheter-free. The former were given trials at voiding after removal of catheters; the usual assistive methods common to most bladder training regimens were administered. Despite this, the trials were unsuccessful in reducing residual urine to acceptable levels. With addition of therapeutic doses of the drug without the training regimen, voiding trials were also unsuccessful excepting the response of one patient. The drug plus the training regimen was effective in reducing residual urine to acceptable levels in all patients. On discontinuing or decreasing the dosages of the drug, there was gradual but rapid build-up of residual urine despite the active training regimen. Restoration of effective dosage again led to satisfactory voiding function in all patients. The catheter-free group suffered from frequency, nocturia, and bed-wetting owing to excessive residual urine despite the employment of active training regimens. With addition of optimal dosages of Ba-34647, these problems were markedly reduced. They increased with drug discontinuation or dosage decrease and again improved upon restoration of effective doses. Bladder training, including active assistance to the expulsion of urine, is essential to the evaluation of antispasticity drugs for their effect on voiding.
 ...
PMID:Bladder training: its role in evaluating the effect of an antispasticity drug on voiding in patients with neurogenic bladder. 120 Aug 14

Baclofen (Lioresal, Ciba-Geigy) is an analog of the inhibitory neurotransmitter GABA and is used clinically to control spasticity. Recent studies have demonstrated that this compound produces a marked inhibition of synaptically evoked responses in area CA3 of the hippocampal slice, suggesting that this drug could influence behavior mediated by the limbic system. In the present study, male rats of the Fischer-344 strain were trained on a one-trial passive avoidance task and tested for retention 1 week later. After the training trial, separate groups of rats received either 5 or 10 mg/kg/4 ml IP of baclofen or the distilled H2O vehicle immediately, 10 min, or 60 min after training. One week later, the rats that received baclofen immediately after training reentered the test chamber with a significantly higher frequency than controls, although no differences in vacillatory responses were observed between groups. Similar effects were observed following posttrial administration of chlordiazepoxide. In a separate experiment rats were tested for locomotor activity after receiving the same doses of baclofen. Although baclofen decreased activity during a 30-min period after dosing, rats exposed to baclofen showed no significant change in activity relative to controls 1 week later. These data are consistent with the interpretation that baclofen may interfere with memory consolidation or retention.
 ...
PMID:Baclofen disrupts passive avoidance retention in rats. 281 19

Tizanidine (Sirdalud) was compared to baclofen (Lioresal) in a randomized, double-blind, cross-over trial. Each medication was introduced over a three week titration period and then maintained at the highest tolerated dose for five weeks. The two treatment phases were separated by a one week drug withdrawal and a two week washout period. Sixty-six patients entered the trial and forty-eight completed both treatment phases. At the end of the trial, neurologists and physiotherapists thought that baclofen was superior on the basis of perceived efficacy and tolerance (p less than or equal to 0.05). Although the efficacy of tizanidine or baclofen was judged as good to excellent by 24 and 39% of patients respectively, this difference was not statistically significant. Muscle weakness was the most common adverse effect. This was significantly more troublesome in patients treated with baclofen. Somnolence and xerostomia were more common in patients treated with tizanidine. Both baclofen and tizanidine appear to be useful adjuncts in the treatment of spasticity in patients with multiple sclerosis. Preference of either drug is tempered principally by side-effects.
 ...
PMID:Tizanidine versus baclofen in the treatment of spasticity in patients with multiple sclerosis. 334 56

Baclofendagger (Lioresal), a derivative of gamma-aminobutyric acid, was introduced in 1966 as a possible treatment for spasticity due to corticospinal tract lesions. Preliminary studies suggested that it may be more effective than other spasmolytic agents currently available, and a double-blind controlled trial in a group of 23 patients against placebo has shown it to be significantly more effective.
 ...
PMID:Baclofen in the treatment of spasticity. 493 43

63 patients with multiple sclerosis underwent urodynamic evaluation. Hyperreflexia of the bladder was found in 64% and areflexia in 8%. Hypertrophy or sclerosis of the bladder neck (internal sphincter) was detected in 27% of the patients and a spastic external sphincter (dyssynergia) was encountered in 57%. 16 patients were admitted for surgery: 9 for TUR of the bladder neck, 5 for percutaneous selective sacral nerve block, 2 for ileal diversion, 2 for prolonged bladder distension and 1 for nephrectomy for staghorn calculi of the renal pelvis. Highly effective conservative therapy is available in the form of Lioresal for treatment of the hyperactive detrusor muscle and Dibenzyran - an alpha-adrenergic blocking agent - to relieve bladder neck spasticity.
 ...
PMID:[Urological complications in patients with multiple sclerosis (author's transl)]. 692 26

Baclofen (Lioresal) is a derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). It is used to treat spasticity particularly for the relief of flexor spasms, pain, clonus, and muscular rigidity. There have been many rare neurologic side effects reported with its use. These side effects, in particular, hallucinations and seizures, have been observed predominantly following precipitous withdrawal of the drug. We present a case demonstrating a muscular dyskinetic side effect when baclofen treatment was first initiated. The mechanism by which baclofen affects spasticity and how the resulting side effect of dyskinesia developed in our patient is not known. They are, however, most probably related to dopamine receptor hypersensitivity and the resulting imbalance of the dopaminergic/cholinergic systems. Clinicians should be aware of this additional adverse effect of muscular dyskinesia, with the use of baclofen, and its reversibility when baclofen is discontinued.
 ...
PMID:Baclofen-induced dyskinesia. 832 1

Baclofen (Lioresal) is a drug of choice to treat spasticity and is increasingly being administered intrathecally via an implantable pump in cases refractory to oral therapy. Emergency physicians will likely treat patients with baclofen withdrawal or overdose as this treatment becomes more widespread. The syndrome of baclofen withdrawal presents with altered mental status, fever, tachycardia, hypertension or hypotension, seizures, and rebound spasticity, and may be fatal if not treated appropriately. Baclofen withdrawal may mimic other diseases including sepsis, meningitis, autonomic dysreflexia, malignant hyperthermia, or neuroleptic malignant syndrome. Treatment consists of supportive care, reinstitution of baclofen, benzodiazepines, and diagnosis and eventual repair of intrathecal pump and catheter malfunction.
 ...
PMID:Intrathecal baclofen withdrawal mimicking sepsis. 1274 45

gamma-Aminobutyric acid-B (GABA(B)) receptors are broadly expressed in the nervous system and have been implicated in a wide variety of neurological and psychiatric disorders. To date the only GABA(B) drug on the market is the agonist baclofen (Lioresal((R))) that is used to treat severe spasticity of cerebral and spinal origin. In addition baclofen is effective in animal models for many central and peripheral disorders, but side-effects and the development of tolerance prohibited a more widespread use of this drug in man. Similarly GABA(B) antagonists show great therapeutic promise but their shortcomings, e.g. the lack of brain penetration or some proconvulsive potential, prevented clinical development. The cloning of GABA(B) receptors in 1997 revived interest in these receptors as drug targets. The long-awaited availability of the tools that were necessary to develop more selective and safer drugs stimulated an impressive activity in the field. The demonstration that GABA(B) receptors needed to heteromerize for function provided new insights into the structure of G-protein coupled receptors in general and enabled to identify allosteric GABA(B) drugs. Gene knockout mice revealed neuronal systems that are under tonic GABA(B) control and therefore best suited for therapeutic intervention. Significant advances were made in clarifying the relationship between GABA(B) receptors and the receptors for gamma-hydroxybutyrate (GHB), a drug of abuse. Here we provide and update on the molecular composition, the physiology and the pharmacology of GABA(B) receptors and discuss to what extent our current knowledge influences ongoing and future drug discovery efforts.
 ...
PMID:GABA(B) receptors as potential therapeutic targets. 1287 Oct 35


1 2 Next >>